Full Text Available Objective: The study was conducted to investigate the antibacterial and anthelmintic activities and to determine total phenolic contents of methanolic extract of Piper betel leaves. Materials and Methods: The extract was subjected to assay for antibacterial activity using both gram positive and gram negative bacterial strains through disc diffusion method; anthelmintic activity with the determination of paralysis and death time using earthworm (Pheritima posthuma at five different concentrations and the determination of total phenolic contents using the Folin-ciocalteau method. Results: The extract showed significant (p
M K Prashanth
Full Text Available Summary. Argyreia elliptica extracts were prepared with solvents at different polarity (petroleum ether, chloroform, ethyl acetate and methanol and evaluate their antibacterial, anthelmintic and antioxidant properties first time. An antioxidant activity was analyzed using different in vitro tests namely 2,2-diphenyl-1-picrylhydrazyl (DPPH and superoxide radical scavenging methods. Quantitative determination of phenols was carried out using spectrophotometric methods. In addition, the extracts were screened for their biological activity in absence and in presence of metal salts [Fe(III and Zn(II] ions. Results indicate that, the tested bacterial strains were most sensitive to the chloroform (CE and methanol extract (ME. Ethyl acetate (EA, CE and ME extracts showed potent radical scavenging activity. CE and ME extracts showed the highest total phenolic content and its enhanced anthelmintic and antioxidant activities were found in Fe(III combination. The extracts-Zn(II ion combination showed enhanced antibacterial activity against tested bacterial strains compare to the extracts alone.Industrial relevance. Herbal medicines have gained increasing attention worldwide for the treatment of various diseases because of their effectiveness and small side effects as compared to synthetic drugs. In general, the essential trace elements have been found to possess a very important role in biological system and also therapeutic activity depends on some trace elements. The present research reports the phytochemical screening of Argyrea elliptica leaves extracts. The antibacterial, anthilmentic and in vitro antioxidant activity activity of extracts and its metal salt combination was studied. The results scientifically establish the efficacy of the plant extracts and its metal salt combination as antibacterial, anthilmentic and antioxidant agents.Keywords. Argyreia elliptica; Antioxidant; Antibacterial activity; Total phenolic content.
Dr. D. Gopala Krishna
Full Text Available In the present study, the Petroleum Ether and Alcoholic extract of Morinda citrifolia L. (Noni stem were subjected to preliminary screening for Antimicrobial and Aanthelmintic activity. The alcoholic extract exhibited significant Anti bacterial, Antifungal activity, comparable to the standard drug Tetracycline. The Petroleum Ether and Alcoholic extract were evaluated for Anthelmintic activity on adult Indian Earthworms, ‘Pheretima posithuma’. The Alcoholic extract produced more significant Anthelmintic activity than Petroleum ether extract and the activities are comparable with the reference drug Piperazine citrate
Bulwan, Maria; Wójcik, Kinga; Zapotoczny, Szczepan; Nowakowska, Maria
Ultrathin antifouling and antibacterial protective nanocoatings were prepared from ionic derivatives of chitosan using layer-by-layer deposition methodology. The surfaces of silicon, and glass protected by these nanocoatings were resistant to non-specific adsorption of proteins disregarding their net charges at physiological conditions (positively charged TGF-β1 growth factor and negatively charged bovine serum albumin) as well as human plasma components. The coatings also preserved surfaces from the formation of bacterial (Staphylococcus aureus) biofilm as shown using microscopic studies (SEM, AFM) and the MTT viability test. Moreover, the chitosan-based films adsorbed onto glass surface demonstrated the anticoagulant activity towards the human blood. The antifouling and antibacterial actions of the coatings were correlated with their physicochemical properties. The studied biologically relevant properties were also found to be dependent on the thickness of those nanocoatings. These materials are promising for biomedical applications, e.g., as protective coatings for medical devices, anticoagulant coatings and protective layers in membranes. PMID:21967904
Dr. D. Gopala Krishna; C. H. Kethani Devi
In the present study, the Petroleum Ether and Alcoholic extract of Morinda citrifolia L. (Noni) stem were subjected to preliminary screening for Antimicrobial and Aanthelmintic activity. The alcoholic extract exhibited significant Anti bacterial, Antifungal activity, comparable to the standard drug Tetracycline. The Petroleum Ether and Alcoholic extract were evaluated for Anthelmintic activity on adult Indian Earthworms, ‘Pheretima posithuma’. The Alcoholic extract produced more significant A...
C. Tharachand; C Immanuel Selvaraj; Z. Abraham
This study aimed to evaluate the in vitro anthelmintic activity and antibacterial activity of the extracts from the leaves and fruits of Garcinia indica (Dupetit-Thouars) Choisy and Garcinia cambogia(Gaertn.) Desr. using the Indian earthworm Pheretima posthuma. Two concentrations (25 and 50 mg/mL) of various extracts such as petroleum ether, chloroform, ethyl acetate, methanol and water were tested. Albendazole at the concentrations of 25 and 50 mg/mL was used as the standard reference. Signi...
Rosselli, Sergio; Maggio, Antonella; Bellone, Gabriella; Formisano, Carmen; Basile, Adriana; Cicala, Carla; Alfieri, Alessio; Mascolo, Nicola; Bruno, Maurizio
The phytochemical investigation of the acetone and methanol extracts of the flowers of Magydaris tomentosa (Desf.) DC afforded six known coumarins as well as (+)-meranzin hydrate (7), not previously reported as a natural product. The antibacterial activity of umbelliprenin (1), osthol (2), imperatorin (3), citropten (4) and (+)-meranzin hydrate (7) was tested against Gram-positive and Gram-negative bacteria. All coumarins (1-7) isolated in this study inhibited growth of all bacterial strains tested (MIC between 16 and 256 microg/mL), the most active being imperatorin (3) (MICs between 32 and 128 microg/mL) and citropten (4) (MICs between 16 and 256 microg/mL). The anticoagulant activity of compounds 1-4 and 7 was also evaluated. PMID:17128388
Full Text Available This study aimed to evaluate the in vitro anthelmintic activity and antibacterial activity of the extracts from the leaves and fruits of Garcinia indica (Dupetit-Thouars Choisy and Garcinia cambogia(Gaertn. Desr. using the Indian earthworm Pheretima posthuma. Two concentrations (25 and 50 mg/mL of various extracts such as petroleum ether, chloroform, ethyl acetate, methanol and water were tested. Albendazole at the concentrations of 25 and 50 mg/mL was used as the standard reference. Significant anthelmintic effects of the fruits and leaves of G. cambogia and G. indica (P<0.05 were observed and the results were expressed in terms of paralysis and death time. All the extracts showed the dose dependent paralysis and death of earthworms. Among all the extracts used, methanol extract exhibited the highest activity. G. cambogia leaf extract (50 mg/mL had 30% faster paralysis effect on earthworms than the standard reference. Furthermore, the antimicrobial activity of the methanol extracts of the fruits and leaves showed significant (P<0.05 activity against Gram-positive and Gram-negative bacteria. At a concentration of 500 µg/mL, G. indica fruit extract presented higher zones of inhibition against Pseudomonas aeruginosa and Staphylococcus aureus. Hence, it could be concluded that the leaves and fruits of G. indica and G. cambogia contained active anthelmintic and antibacterial phytochemicals, which could find their applications in pharmaceuticals.
Marine pharmacology in 2003-4: Marine Compounds with Anthelminthic, Antibacterial, Anticoagulant, Antifungal, Anti-inflammatory, Antimalarial, Antiplatelet, Antiprotozoal, Antituberculosis, and Antiviral Activities; affecting the Cardiovascular, Immune and Nervous Systems, and other Miscellaneous Mechanisms of Action
Mayer, Alejandro M. S.; Rodriguez, Abimael D.; Berlinck, Roberto G. S.; Hamann, Mark T.
The current marine pharmacology review that covers the peer-reviewed literature during 2003 and 2004 is a sequel to the authors' 1998-2002 reviews, and highlights the preclinical pharmacology of 166 marine chemicals derived from a diverse group of marine animals, algae, fungi and bacteria. Anthelminthic, antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antiprotozoal, antituberculosis or antiviral activities were reported for 67 marine chemicals. Additionally 45 marine com...
Nielsen, Martin Krarup
that Danish veterinarians are now deeply involved with parasite management in equine establishments. However, little is known about the impact on levels of anthelmintic resistance and the risk of parasitic disease under these circumstances. In addition, the legislation makes huge demands on diagnosis...
Watt, Barbara E; Proudfoot, Alex T; Bradberry, Sally M; Vale, J Allister
Anticoagulant pesticides are used widely in agricultural and urban rodent control. The emergence of warfarin-resistant strains of rats led to the introduction of a new group of anticoagulant rodenticides variously referred to as 'superwarfarins', 'single dose' or 'long-acting'. This group includes the second generation 4-hydroxycoumarins brodifacoum, bromadiolone, difenacoum, flocoumafen and the indanedione derivatives chlorophacinone and diphacinone. Most cases of anticoagulant rodenticide exposure involve young children and, as a consequence, the amounts ingested are almost invariably small. In contrast, intentional ingestion of large quantities of long-acting anticoagulant rodenticides may cause anticoagulation for several weeks or months. Occupational exposure has also been reported. Anticoagulant rodenticides inhibit vitamin K(1)-2,3 epoxide reductase and thus the synthesis of vitamin K and subsequently clotting factors II, VII, IX and X. The greater potency and duration of action of long-acting anticoagulant rodenticides is attributed to their: (i) greater affinity for vitamin K(1)-2,3-epoxide reductase; (ii) ability to disrupt the vitamin K(1)-epoxide cycle at more than one point; (iii) hepatic accumulation; and (iv) unusually long biological half-lives due to high lipid solubility and enterohepatic circulation. Substantial ingestion produces epistaxis, gingival bleeding, widespread bruising, haematomas, haematuria with flank pain, menorrhagia, gastrointestinal bleeding, rectal bleeding and haemorrhage into any internal organ; anaemia may result. Spontaneous haemoperitoneum has been described. Severe blood loss may result in hypovolaemic shock, coma and death. The first clinical signs of bleeding may be delayed and patients may remain anticoagulated for several days (warfarin) or days, weeks or months (long-acting anticoagulants) after ingestion of large amounts. There are now sufficient data in young children exposed to anticoagulant rodenticides to
Simultaneous antibacterial and anticoagulant properties of polypropylene non-woven textiles Elaboration d'un textile polypropylène non-tissé présentant simultanément des propriétés antibactériennes et anticoagulantes
Full Text Available The aim of this work was to prepare a non-woven Polypropylene (PP textile functionalized with bioactive molecules to improve simultaneously its anticoagulation and antibacterial properties. The immobilization of either heparin (anticoagulation agent or gentamicin (aminoglycoside antibiotic was already proven to be effective on non-woven PP textiles. This work details how we managed to immobilize both gentamicin and heparin on the textile . The immobilization times were studied in order to determine the best compromise between cytocompatibility, anticoagulant effect and antimicrobial activity. Cetté étude décrit le procédé de fonctionnalisation d'un textile polypropylène (PP non-tissé afin d'améliorer à la fois ses propriétés antibactériennes et anticoagulantes. Dans des précédents travaux, l'immobilisation soit de l'héparine (agent anticoagulant, soit de la gentamicine (agent antibiotique aminoglycoside a déjà été reportée. Des effets respectivement anticoagulants et antibactériens ont été obtenus. Cette étude décrit la faç on d'immobiliser ces deux principes actifs sur un même textile. L'effet des temps d'imprégnation sur les propriétés antibactériennes et anticoagulantes a été étudié afin d'obtenir le meilleur compromis possible en termes de cytocompatibilité, effet anticoagulant et activité antimicrobienne.
Jacqueline B. Matthews
Full Text Available Anthelmintics have been applied indiscriminately to control horse nematodes for over 40 years. Three broad-spectrum anthelmintic classes are currently registered for nematode control in horses: benzimidazoles (fenbendazole, oxibendazole, tetrahydropyrimidines (pyrantel and macrocyclic lactones (ivermectin, moxidectin. Generally, control strategies have focused on nematode egg suppression regimens that involve the frequent application of anthelmintics to all horses at intervals based on strongyle egg reappearance periods after treatment. The widespread use of such programmes has substantially reduced clinical disease, especially that associated with large strongyle species; however, high treatment frequency has led to considerable selection pressure for anthelmintic resistance, particularly in cyathostomin species. Field studies published over the last decade indicate that benzimidazole resistance is widespread globally in cyathostomins and there are also many reports of resistance to pyrantel in these worms. Cyathostomin resistance to macrocyclic lactone compounds is emerging, principally measured as a reduction in strongyle egg reappearance time observed after treatment. Ivermectin resistance is a further concern in the small intestinal nematode, Parascaris equorum, an important pathogen of foals. These issues indicate that horse nematodes must now be controlled using methods less dependent on anthelmintic use and more reliant on management practices designed to reduce the force of infection in the environment. Such strategies include improved grazing management integrated with targeted anthelmintic administration involving faecal egg count (FEC-directed treatments. The latter require that the supporting diagnostic tests available are robust and practically applicable. Recent research has focused on maximising the value of FEC analysis in horses and on optimizing protocols for anthelmintic efficacy testing. Other studies have sought to develop
Gastrointestinal nematode (GIN) resistance to synthetic anthelmintics in small ruminants has led to the evaluation of feed sources containing naturally occurring bioactive secondary metabolites that lessen parasite activity. Plants rich in condensed tannins (CT) can have beneficial anthelmintic pro...
Full Text Available Leaves, wood, seed, bark and pericarp of the fruit of Pongamia glabra were separately dried, powdered and extracted with methanol in Soxhlet extractor. Anthelmintic activity of these various extracts was evaluatedon Indian adult earthworms, Pherentima posthuma. Results showed that the seed part of P. glabra took less time to cause paralysis and death of the earthworms; therefore, seeds were extracted successively withpetroleum ether, ethyl acetate and methanol in Soxhlet extractor. Again these extracts were screened for anthelmintic activity. Results showed that the ethyl acetate extract of seeds of P. glabra was most potentfollowed by petroleum ether extract. It can be concluded that anthelmintic activity of the seed of P. glabra is due to the active principles present mostly in the ethyl acetate and petroleum ether extracts.
Ferreira, Joana Lima; Wipf, Joyce E
Anticoagulants are beneficial for prevention and treatment of venous thromboembolism and stroke prevention in atrial fibrillation. The development of target-specific oral anticoagulants is changing the landscape of anticoagulation therapy and created growing interest on this subject. Understanding the pharmacology of different anticoagulants is the first step to adequately treat patients with best available therapy while avoiding serious bleeding complications. This article reviews the pharmacology of the main anticoagulant classes (vitamin K antagonists, direct oral anticoagulants, and heparins) and their clinical indications based on evidence-based data currently available in the literature. PMID:27235611
@@ VTE of the main treatment for anticoagulant thera-py, anticoagulant therapy drug of choice for low molecu-lar weight heparin (LMWH) for the overwhelming major-ity of clinicians agree that long-term oral anticoagulant therapy is still Vit. K antagonist (mainly warfarin).
Shalaby, Hatem A
Many parasitic helminthes of veterinary importance have genetic features that favor development of anthelmintic resistance, this becoming a major worldwide constrain in livestock production. The development of anthelmintic resistance poses a large threat to future production and welfare of grazing animals. Development of variable degrees of resistance among different species of gastrointestinal nematodes has been reported for all the major groups of anthelmintic drugs. It has been observed that frequent usage of the same group of anthelmintic; use of anthelmintics in sub-optimal doses, prophylactic mass treatment of domestic animals and frequent and continuous use of a single drug have contributed to the widespread development of anthelmintic resistance in helminthes. The degree and extent of this problem especially with respect to multidrug resistance in nematode populations is likely to increase. Maintaining parasites in refugia and not exposed to anthelmintics, seems to be a key point in controlling and delaying the development of resistance, because the susceptible genes are preserved. Targeted selective treatments attract the interest of scientists towards this direction. Additionally, adoption of strict quarantine measures and a combination drug strategy are two important methods of preventing of anthelmintic resistance. Experience from the development of anthelmintic resistance suggests that modern control schemes should not rely on sole use of anthelmintics, but employ other, more complex and sustainable recipes, including parasite resistant breeds, nutrition, pasture management, nematode-trapping fungi, antiparasitic vaccines and botanical dewormers. Most of them reduce reliance on the use of chemicals and are environmental friendly. Finally, if new anthelmintic products are released, an important question will be raised about how they should be used. It is suggested that slowing the development of resistance to a new class are likely to be gained by
Hatem A Shalaby
Full Text Available Many parasitic helminthes of veterinary importance have genetic features that favor development of anthelmintic resistance, this becoming a major worldwide constrain in livestock production. The development of anthelmintic resistance poses a large threat to future production and welfare of grazing animals. Development of variable degrees of resistance among different species of gastrointestinal nematodes has been reported for all the major groups of anthelmintic drugs. It has been observed that frequent usage of the same group of anthelmintic; use of anthelmintics in sub-optimal doses, prophylactic mass treatment of domestic animals and frequent and continuous use of a single drug have contributed to the widespread development of anthelmintic resistance in helminthes. The degree and extent of this problem especially with respect to multidrug resistance in nematode populations is likely to increase. Maintaining parasites in refugia and not exposed to anthelmintics, seems to be a key point in controlling and delaying the development of resistance, because the susceptible genes are preserved. Targeted selective treatments attract the interest of scientists towards this direction. Additionally, adoption of strict quarantine measures and a combination drug strategy are two important methods of preventing of anthelmintic resistance. Experience from the development of anthelmintic resistance suggests that modern control schemes should not rely on sole use of anthelmintics, but employ other, more complex and sustainable recipes, including parasite resistant breeds, nutrition, pasture management, nematode-trapping fungi, antiparasitic vaccines and botanical dewormers. Most of them reduce reliance on the use of chemicals and are environmental friendly. Finally, if new anthelmintic products are released, an important question will be raised about how they should be used. It is suggested that slowing the development of resistance to a new
Ohyama, Makoto; Okada, Yumiko; Takahashi, Masaaki; Sakanaka, Osamu; Matsumoto, Maki; Atsumi, Kunio
The relationship between cyclooctadepsipeptides and their anthelmintic efficacy was examined by converting the natural products, PF1022A, PF1022E and PF1022H. Some analogues substituted at the para position of the phenyllactate moiety showed higher or equivalent activity against the parasitic nematode, Ascaridia galli in chicken when compared with the parent compounds. It is suggested that lipophilicity and the polar surface area, in addition to structural requirements of the derivatives, influenced the anthelmintic efficacy in vivo. PMID:21737929
H.P. Desai*, M.D. Kapadia and A.R. Kharat
Development of anthelmintic resistance and high cost of conventional anthelmintic drugs lead to the evaluation of medicinal plants which acts as an alternative source of anthelmintics. The present study has been undertaken to perform the evaluation of anthelmintic activity of Plumbago zeylanica belonging to family Plumbaginaceae. In the current study, experiments were conducted to evaluate the possible anthelminitic effects of various extracts of the roots of Plumbago zeylanica. Various conce...
Howie, P W
Thromboembolic disorders are still a serious problem in pregnancy and anticoagulants have an important part to play in both treatment and prevention. Warfarin is the most convenient drug to give but can cause maternal and fetal bleeding problems, especially during late pregnancy and delivery. There are also small risks of embryopathy from warfarin in early pregnancy but these may have been overstated. Heparin, which has to be given parenterally, does not cross the placental barrier but can still cause bleeding problems in pregnancy. Full intravenous heparin is only suitable for short-term use, and subcutaneous heparin has been introduced for long-term therapy. This regimen is a useful advance but long-term use still has problems of bruising and maternal bone demineralization. The standard treatment of acute thromboembolic events in pregnancy is continuous intravenous heparin followed by either subcutaneous heparin or warfarin, the latter being changed at 36 weeks gestation. In the prophylaxis of thromboembolism, the trend is towards a more selective approach, anticoagulants being given during pregnancy to those at highest risk and during labour and the puerperium to all with a previous history of thromboembolism. Anticoagulants during pregnancy are necessary in patients with artificial heart valves and, because subcutaneous heparin is not sufficient, warfarin should be used until 36 weeks followed by continuous intravenous heparin until delivery. No method of anticoagulation during pregnancy is entirely free of risk and all management policies must be based on an estimate of risk-benefit ratio in individual patients. PMID:2426029
Koopmans, SA; VanRij, G
A questionnaire was sent to 240 members of the Netherlands Intraocular implant Club (NIOIC) to register their policy followed in 1993 with regard to anticoagulant therapy (ACT) and the use of aspirin in patients having cataract surgery. Ninety-one (32%) forms were suitable for analysis. Most eye sur
Steinberg, Benjamin A; Piccini, Jonathan P
Atrial fibrillation increases the risk of stroke, which is a leading cause of death and disability worldwide. The use of oral anticoagulation in patients with atrial fibrillation at moderate or high risk of stroke, estimated by established criteria, improves outcomes. However, to ensure that the benefits exceed the risks of bleeding, appropriate patient selection is essential. Vitamin K antagonism has been the mainstay of treatment; however, newer drugs with novel mechanisms are also available. These novel oral anticoagulants (direct thrombin inhibitors and factor Xa inhibitors) obviate many of warfarin's shortcomings, and they have demonstrated safety and efficacy in large randomized trials of patients with non-valvular atrial fibrillation. However, the management of patients taking warfarin or novel agents remains a clinical challenge. There are several important considerations when selecting anticoagulant therapy for patients with atrial fibrillation. This review will discuss the rationale for anticoagulation in patients with atrial fibrillation; risk stratification for treatment; available agents; the appropriate implementation of these agents; and additional, specific clinical considerations for treatment. PMID:24733535
Ahmad, Yousif; YH Lip, Gregory
Patients with atrial fibrillation (AF) are at increased thromboembolic risk, and they suffer more severe strokes with worse outcomes. Most thromboembolic complications of AF are eminently preventable with oral anticoagulation, and the increasing numbers of AF patients mean antithrombotic therapy is the most crucial management aspect of this common arrhythmia. Despite the proven efficacy of warfarin, a string of limitations have meant that it is underused by physicians and patients alike. This...
Steinberg, Benjamin A; Piccini, Jonathan P.
Atrial fibrillation increases the risk of stroke, which is a leading cause of death and disability worldwide. The use of oral anticoagulation in patients with atrial fibrillation at moderate or high risk of stroke, estimated by established criteria, improves outcomes. However, to ensure that the benefits exceed the risks of bleeding, appropriate patient selection is essential. Vitamin K antagonism has been the mainstay of treatment; however, newer drugs with novel mechanisms are also availabl...
Ndhlala, Ashwell R; Ghebrehiwot, Habteab M; Ncube, Bhekumthetho; Aremu, Adeyemi O; Gruz, Jiří; Šubrtová, Michaela; Doležal, Karel; du Plooy, Christian P; Abdelgadir, Hafiz A; Van Staden, Johannes
Achyranthes aspera Linn. (Amaranthaceae) commonly known as Prickly Chaff flower (English) is traditionally used for treating a number of ailments. Different parts of the plant are used in treating wounds and ringworm in East Africa and elsewhere for a number of ailments. In this study, leaf extracts of A. aspera collected from two different geographical locations (Ciaat, Eritrea and Ukulinga, South Africa) were evaluated for antibacterial, antifungal, anthelmintic activities and the plant characterized for functional phenolic acids as well as protein binding capacity. The pathogens used in the tests were, two Gram-negative (Escherichia coli and Klebsiella pneumoniae), two Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus), a filamentus yeast-like fungus (Candida albicans) and a free-living nematode (Caenorhabditis elegans). The water and acetone extracts of the samples collected from Ciaat exhibited good antibacterial, antifungal and anthelmintic activity (MIC plant samples collected at Ciaat expressed significant dominant potency compared to similar extracts from Ukulinga. PMID:26635604
Kaliyamoorthy Kalidasan; Velayudham Ravi; Sunil Kumar Sahu; Murugan Lakshmi Maheshwaran; Kathiresan Kandasamy
Objective:To study the spine structure of stingray Himantura imbricata (H. imbricata) and to evaluate the anticoagulant properties of the spine extract obtained through various solvents extracts followed by antibacterial activity against human pathogens. Methods:Spines of H. imbricata were collected from Nagappattinam coast, Tamil Nadu, India and their spines were observed under the light microscope. The grounded spines were subjected to extraction of metabolites using methanol, ethanol, chloroform and acetone. Antibacterial activity was evaluated by disc diffusion technique against 10 human pathogens. Similarly, anticoagulant activity was also assessed by following United States Pharmacopeia method. Results:Light microscopic observation of spine revealed that the venom apparatus of the stingray H. imbricata consisted of two to three spines, glandular tissue and a sheath. The spine extract showed potent antibacterial activity against all tested pathogen. Maximum activity (14 mm) was found against Staphylococcus aureus. Crude extract showed 91.50 USP units/mg of anticoagulant activity. Conclusions: Microscopic observations gave new insight about the spine structure of the stingray. The spine extracts of H. imbricate showed potent activity against human pathogens revealed by the good zone of inhibition. Chloroform extracts conferred the most prominent antibacterial activity. The anticoagulant activity was also comparable with that of standard heparin.
Full Text Available Objective: To study the spine structure of stingray Himantura imbricata (H. imbricata and to evaluate the anticoagulant properties of the spine extract obtained through various solvents extracts followed by antibacterial activity against human pathogens. Methods: Spines of H. imbricata were collected from Nagappattinam coast, Tamil Nadu, India and their spines were observed under the light microscope. The grounded spines were subjected to extraction of metabolites using methanol, ethanol, chloroform and acetone. Antibacterial activity was evaluated by disc diffusion technique against 10 human pathogens. Similarly, anticoagulant activity was also assessed by following United States Pharmacopeia method. Results: Light microscopic observation of spine revealed that the venom apparatus of the stingray H. imbricata consisted of two to three spines, glandular tissue and a sheath. The spine extract showed potent antibacterial activity against all tested pathogen. Maximum activity (14 mm was found against Staphylococcus aureus. Crude extract showed 91.50 USP units/mg of anticoagulant activity. Conclusions: Microscopic observations gave new insight about the spine structure of the stingray. The spine extracts of H. imbricate showed potent activity against human pathogens revealed by the good zone of inhibition. Chloroform extracts conferred the most prominent antibacterial activity. The anticoagulant activity was also comparable with that of standard heparin.
Full Text Available Medicinal plants are part and parcel of human society to combat diseases, from the dawn of civilization. There exists a plethora of knowledge, information and benefits of herbal drugs in our ancient literature of Ayurvedic (Traditional Indian Medicine, Siddha, Unani and Chinese medicine. According to the World Health Organization, 2003 about 80 % of the population of developing countries being unable to afford pharmaceutical drugs rely on traditional medicines, mainly plant based, to sustain their primary health care needs. Herbal medicines are in great demand in the developed as well as developing countries for primary healthcare because of their wide biological and medicinal activities, higher safety margins and lesser costs. In this review we have enlisted the updated anthelmintic medicinal plants which are used as good alternatives for the traditional allopathic anthelmintic agents.
H.P. Desai*, M.D. Kapadia and A.R. Kharat
Full Text Available Development of anthelmintic resistance and high cost of conventional anthelmintic drugs lead to the evaluation of medicinal plants which acts as an alternative source of anthelmintics. The present study has been undertaken to perform the evaluation of anthelmintic activity of Plumbago zeylanica belonging to family Plumbaginaceae. In the current study, experiments were conducted to evaluate the possible anthelminitic effects of various extracts of the roots of Plumbago zeylanica. Various concentrations (5, 10, 15, 20mg/ml of water and methanol extracts were tested and results were expressed in terms of time for paralysis and time for death of worms. Piperazine citrate was taken as a reference standard drug.The anthelmintic activity was observed by gradually increasing the dose of extract. Methanolic extract of Plumbago zeylenica showed higher activity as compared to water extract.
Jabeen, Nyla; Anwar, Sadaf; Mahmood, Qaisar; Zia, Muhammad Abid; Murtaza, Ghulam
The current study aimed to investigate in vitro anthelmintic efficacy of two medicinally important plants against Haemonchus contortus in small ruminants. Fruit peel of Punica granatum Linn. (vern. Anar), leaves and roots of Berberis lycium Royle (vern. Sumbal) were tested for their anthelmintic efficacy. Methanolic extracts of the test plants from various plant parts were tested for anthelmintic efficacy against the Haemonchus contortous using albendazole as a reference standard. The results revealed that both the plant extracts exhibited potent anthelmintic activity at concentrations higher than 50 mg/mL when tested against their respective standard drug. In case of Berberis lycium Royle when the results were compared, methanolic roots extracts showed more potent activity as compared to leaves extracts at the same concentration. It was observed that the in vitro anthelmintic potential of Punica granatum Linn. fruit peel and Berberis lyceium Royale root can be used to treat helminth infections after in vivo trails. PMID:26665413
Wooten, James M
For years, the pharmaceutical industry has been trying to find a safe and effective drug to replace warfarin. Although warfarin is an effective anticoagulant, its pharmacology, adverse effects, and risk profiles dictate that patients taking this medication must be monitored judiciously. The US Food and Drug Administration has approved two drugs for commercial use, dabigatran and rivaroxaban, that will compete directly with warfarin for use in specific indications. Because of direct marketing to patients, physicians are being asked to comment on these new medications. This brief review illustrates the data available for the two new drugs when compared to warfarin for the specified indications. For some patients, these drugs may be highly beneficial and offer an excellent alternative to warfarin. For others, warfarin may still be the preferred drug. PMID:23211502
Low leukocyte count secondary to leukocyte aggregation caused by an ethylene diamine tetra acetic acid (EDTA) occur in both benign and malignant disorders. We report a 71-year-old male patient who was admitted to the hospital with acute chest infection. Complete blood count (CBC) collected in ETDA tube and analyzed by sysmex instrument (SE/9500) revealed low hemoglobin level of 9.4g/dl, white blood cell (WBC) count of 8.2x109/L. Peripheral blood smear review shows multiple leukocyte aggregation (one clump in each field). When we asked for another blood sample in citrate anticoagulant, the CBC showed WBC count of 11.8x109/L and neutrophils of 6.26x109/L. This is a case of low leukocyte count secondary to leukocyte aggregation induced by EDTA. (author)
Kota Chaitanya Sravanthi
Full Text Available The aim of the present study was to investigate the anthelmintic activity of Hibiscus cannabinus leaf extract using adult earthworm, Pheritima posthuma. The methanolic extract of the crude drug at concentrations of 10mg/ml, 20mg/ml, 30mg/ml, 40mg/ml were tested which involve determination of paralysis time and death time. Albendazole was used as standard and it was found that the concentrated methanolic extract (with no traces of solvent of the Hibiscus cannabinus leaves which is used as food in many parts of the world, showed a better anthelminthic activity in comparison with the standard.
Intestinal parasites such Haemonchus contortus is usually controlled by management improvement and regular administration of anthelmintic. However, there is an indication of H. contortus resistance to several anthelmintic available in the market, which makes medicinal plants as an alternative anthelmintic and mengkudu or noni fruit (Morinda citrifolia) have been reported as an effective anthelmintic. To trace the active compounds responsible for anthelmintic activity against H. contortus, the...
Pal Vishesh Kumar
Full Text Available Ethanol extract from the Acalypha indica leaves of investigated for their anthelmintic activity against Pheretima posthuma. Three concentrations (1%, 2.5% and 5% of extract were studied in activity, which involved the determination of time of paralysis and death of the worm. Both the extracts exhibited significant anthelmintic activity at highest concentration of 100 mg/ml. Piperazine citrate in same concentration as that of extract was included as standard reference and distilled water as control. The anthelmintic activity of ethanol extract of Acalypha indica leaf therefore been demonstrated for the first time.
DeLoughery, Thomas G
DeLoughery, Thomas G. Anticoagulation considerations for travel to high altitude. High Alt Med Biol 16:181-185, 2015.-An increasing percentage of the population are on anticoagulation medicine for clinical reasons ranging from stroke prevention in atrial fibrillation to long term prevention of deep venous thrombosis. In recent years, several new direct oral anticoagulants have entered the market. The key questions that should be kept in mind when approaching a potential traveler on anticoagulation are: 1) why is the patient on anticoagulation? 2) do they need to stay on anticoagulation? 3) what are the choices for their anticoagulation? 4) will there be any drug interactions with medications needed for travel? and 5) how will they monitor their anticoagulation while traveling? Knowing the answers to these questions then can allow for proper counseling and planning for the anticoagulated traveler's trip. PMID:26186419
Full Text Available The aqueous extract of Clerodendron inerme leaves was investigated for anthelmintic activity using earthworms(Pheretima posthuma, tapeworms (Raillietina spiralis and roundworms (Ascaridia galli. Various concentrations (10-50 mg/ml of plant extract were tested in the bioassay. Piperazine citrate (10 mg/ml was used as reference standard drug whereas distilled water as control. Determination of paralysis time and death time of the worms were recorded. Extract exhibited significant anthelmintic activity at the concentration of 30 mg/ml. The result shows that aqueous extract possesses vermicidal activity and found to be effective as an anthelmintic. Therefore, the anthelmintic activity of the aqueous extract of Clerodendron inerme has been reported for the first time.
Adrian J. Wolstenholme
Full Text Available The scientific meeting entitled ‘Anthelmintics: From Discovery to Resistance’ was held in San Francisco in February 2014. The themes of the meeting were drug discovery, modes of action and resistance. Both human and veterinary parasites were covered in the oral and poster presentations. The attendees were from both academic and industrial backgrounds. In the present article we introduce a number of the papers that emerged from the meeting. Several of the papers covered current drug discovery efforts underway worldwide, with some specific examples focusing on ion channels, protein kinases and cysteine proteases. These efforts included the repurposing of known drugs as well as the discovery of novel actives. Two papers described recently-developed whole-organism screening techniques. Finally, we introduce several papers looking at mechanisms and management of drug resistance in human and veterinary parasites.
Cooper, Kevin Mark; Whelan, Michelle; Danaher, Martin; Kennedy, David Glenn
Abstract Anthelmintic drugs are widely used for treatment of parasitic worms in livestock but little is known about the stability of their residues in food under conventional cooking conditions. As part of the European Commission-funded research project ProSafeBeef, cattle were medicated with commercially available anthelmintic preparations, comprising 11 active ingredients (corresponding to 21 marker residues). Incurred meat and liver were cooked by roasting (40 min at 190?C) or...
HAQUE RABIUL; MONDAL SUBHASISH; GHOSH PARAG
The aqueous extract of Cinnamomum camphorLeaves was investigated for anthelmintic activity using earthworms(Pheretima posthuma), tapeworms (Raillietina spiralis) and roundworms (Ascaridia galli). Various concentrations (10-70 mg/ml) of plant extract were tested in the bioassay. Piperazine citrate (10 mg/ml) was used as reference standard drug whereas distilled water as control.Determination of paralysis time and death time of the worms were recorded. Extract exhibited significant anthelmintic...
Pena-Espinoza, Miguel Angel; Williams, Andrew; Thamsborg, Stig Milan; Enemark, Heidi
BACKGROUND: Chicory (Cichorium intybus) has potential as a natural anthelmintic in livestock, however evidence of efficacy against cattle nematodes is lacking. Here, we investigated anthelmintic effects of chicory in stabled calves.METHODS: Jersey male calves (2-4 months) were stratified by live weight and allocated randomly to 2 groups: chicory (CHI, n=9) and control (CON, n=6). CHI and CON calves were fed with forage chicory silage (cv. Spadona) and hay ad libitum, resp., for 8 weeks. After...
1.0 Executive summary 1. Internal parasites are a major source of economic loss in grazing ruminants. To a greater or lesser degree, most farms in the UK rely on anthelmintics for control. In most situations these products continue to be highly effective, but anthelmintic resistance is increasing to the limited range of products available, raising serious concerns over the future of worm control. 2. Internal parasites are also of concern on organic farms, where the prophylactic us...
Reinemeyer Craig R
Full Text Available Abstract Since 2002, macrocyclic lactone resistance has been reported in populations of Parascaris equorum from several countries. It is apparent that macrocyclic lactone resistance developed in response to exclusive and/or excessively frequent use of ivermectin or moxidectin in foals during the first year of life. The development of anthelmintic resistance was virtually inevitable, given certain biological features of Parascaris and unique pharmacologic characteristics of the macrocyclic lactones. Practitioners can utilize the Fecal Egg Count Reduction Test to detect anthelmintic resistance in Parascaris, and the same technique can be applied regularly to confirm the continued efficacy of those drugs currently in use. In the face of macrocyclic lactone resistance, piperazine or anthelmintics of the benzimidazole or pyrimidine classes can be used to control ascarid infections, but Parascaris populations that are concurrently resistant to macrocyclic lactones and pyrimidine drugs have been reported recently from Texas and Kentucky. Compared to traditional practices, future recommendations for ascarid control should feature: 1 use of only those anthelmintics known to be effective against indigenous populations, 2 initiation of anthelmintic treatment no earlier than 60 days of age, and 3 repetition of treatments at the longest intervals which prevent serious environmental contamination with Parascaris eggs. In the interest of decreasing selection pressure for anthelmintic resistance, horse owners and veterinarians must become more tolerant of the passage of modest numbers of ascarid eggs by some foals. Anthelmintic resistance is only one of several potential responses to genetic selection. Although still only theoretical, changes in the immunogenicity of ascarid isolates or reduction of their prepatent or egg reappearance periods could pose far greater challenges to effective control than resistance to a single class of anthelmintics.
Ilie M.S.,; Darabus Gh.,; Oprescu I,; Morariu S.,; Narcisa Mederle,; Alina lie,; Imre K,; Florica Morariu
We have tested the efficacy of some vegetal extracts (Parazitol –Medica Laboratories, a natural product with an anthelmintic effect and a Cucurbita sp. oil extract) compared to the classic anthelmintics (Rombendazol – Romvac and Dehelman – KRKA Slovenia) at domestic poultry, whose parasitical status had been previously established through animal killing and necropsies. Parazitol and the pumpkin oil have had a lower efficacy than the levamisole and albendazole upon the species Ascaridia galli....
Robinson, Jeffrey C; Pugliese, Steven C; Fox, Daniel L; Badesch, David B
Pulmonary arterial hypertension (PAH) is characterized by molecular and pathologic alteration to the pulmonary circulation, resulting in increased pulmonary vascular resistance, right ventricular failure, and eventual death. Pharmacologic treatment of PAH consists of use of a multitude of pulmonary vasodilators, sometimes in combination. PAH has been associated with increased thrombosis and disrupted coagulation and fibrinolysis, making anticoagulation an attractive and frequently employed therapeutic modality. Observational studies have provided some insight into the therapeutic potential of anticoagulation in idiopathic PAH, but there is a distinct lack of well-controlled prospective trials. Due to the conflicting evidence, there is a large amount of heterogeneity in the application of therapeutic anticoagulation in PAH and further well-controlled prospective trials are needed to clarify its role in treating PAH. PMID:27137522
Kaliyamoorthy Kalidasan; Velayudham Ravi; Sunil Kumar Sahu; Murugan Lakshmi Maheshwaran; Kathiresan Kandasamy
Objective: To study the spine structure of stingray Himantura imbricata (H. imbricata) and to evaluate the anticoagulant properties of the spine extract obtained through various solvents extracts followed by antibacterial activity against human pathogens. Methods: Spines of H. imbricata were collected from Nagappattinam coast, Tamil Nadu, India and their spines were observed under the light microscope. The grounded spines were subjected to extraction of metabolites using m...
Kaplan, Ray M; Vidyashankar, Anand N
Over the past 10-15 years, we have witnessed a rapid increase in both the prevalence and magnitude of anthelmintic resistance, and this increase appears to be a worldwide phenomenon. Reports of anthelmintic resistance to multiple drugs in individual parasite species, and in multiple parasite species across virtually all livestock hosts, are increasingly common. In addition, since the introduction of ivermectin in 1981, no novel anthelmintic classes were developed and introduced for use in livestock until recently with the launch of monepantel in New Zealand. Thus, livestock producers are often left with few options for effective treatment against many important parasite species. While new anthelmintic classes with novel mechanisms of action could potentially solve this problem, new drugs are extremely expensive to develop, and can be expected to be more expensive than older drugs. Thus, it seems clear that the "Global Worming" approach that has taken hold over the past 40-50 years must change, and livestock producers must develop a new vision for parasite control and sustainability of production. Furthermore, parasitologists must improve methods for study design and data analysis that are used for diagnosing anthelmintic resistance, especially for the fecal egg count reduction test (FECRT). Currently, standards for diagnosis of anthelmintic resistance using FECRT exist only for sheep. Lack of standards in horses and cattle and arbitrarily defined cutoffs for defining resistance, combined with inadequate analysis of the data, mean that errors in assigning resistance status are common. Similarly, the lack of standards makes it difficult to compare data among different studies. This problem needs to be addressed, because as new drugs are introduced now and in the future, the lack of alternative treatments will make early and accurate diagnosis of anthelmintic resistance increasingly important. PMID:22154968
Full Text Available Intestinal parasites such Haemonchus contortus is usually controlled by management improvement and regular administration of anthelmintic. However, there is an indication of H. contortus resistance to several anthelmintic available in the market, which makes medicinal plants as an alternative anthelmintic and mengkudu or noni fruit (Morinda citrifolia have been reported as an effective anthelmintic. To trace the active compounds responsible for anthelmintic activity against H. contortus, the mengkudu fruit was continuosly extracted into hexane, chloroform, metanol and water, followed by in-vitro study on the anthelmintic activity. The in-vitro anthelmintic activity was base on the ability of the extracts to kill the worm and the ability of the extracts to prevent egg development. The study suggested that chloroform fraction which contains alkaloid and anthraquinon have the highest anthelmintic activity and showed significant different compared to control (P≤ 0.05.
Parks, Anna L; Fang, Margaret C
The number of patients with atrial fibrillation (AF) who are of advanced age or have multiple comorbidities is expected to increase substantially. Older patients with AF generally gain a net benefit from anticoagulation. Guidelines typically recommend anticoagulation. There are multiple challenges in the safe use of anticoagulation in frail patients, including bleeding risk, monitoring and adherence, and polypharmacy. Although there are options for chronic oral anticoagulation, clinicians must understand the unique advantages and disadvantages of these medications when developing a management plan. This article reviews issues surrounding the appropriate use and selection of anticoagulants in complex older patients with AF. PMID:27113150
Jabbar, Abdul; Campbell, Angus JD; Charles, Jennifer A; Gasser, Robin B
Background Parasitic nematodes can cause substantial clinical and subclinical problems in alpacas and anthelmintics are regularly used to control parasitic nematodes in alpacas. Although anthelmintic resistance has been reported in ruminants worldwide, very little is known about anthelmintic resistance in alpacas. The present study was carried out to confirm a suspected case of anthelmintic resistance in Haemonchus contortus in alpacas in Australia. Methods Post mortem examination of an alpac...
... products such as soaps, detergents, health and skincare products and household cleaners. How do antibacterials work? ♦ Antibacterials may be ... contain triclosan or other biocide agents? Antibacterials in household products Are there any risks associated with triclosan-containing ...
Radley, A S; Hall, J; Farrow, M.; Carey, P J
AIMS--To compare the quality of outpatient anticoagulant control before and after the transfer of dosing responsibility to designated trained pharmacists from rotating junior medical staff. METHODS--All International Normalised Ratio (INR) values for an eight month period either side of the staff changeover were assessed for precision of therapeutic control according to described standards. Allowing for patient associated effects, observed and expected frequencies of "successful" control for ...
Chighizola, Cecilia Beatrice; Raschi, Elena; Banzato, Alessandra; Borghi, Maria Orietta; Pengo, Vittorio; Meroni, Pier Luigi
The term "lupus anticoagulant" (LA) refers to a heterogeneous group of immunoglobulins behaving as acquired in vitro inhibitors of coagulation. These antibodies, namely anti-β2GPI and anti-prothrombin antibodies, induce the in vitro elongation of clotting time interfering with phospholipid-dependent coagulation cofactors. Positive LA is associated with thrombosis and pregnancy complications, providing one of the three laboratory criteria for the classification of the anti-phospholipid syndrome. LA is the strongest predictor of clinical events, especially when associated with other anti-phospholipid antibodies. Much more controversial is the risk conveyed by isolated and weak LA. LA detection is technically laborious, envisaging screening, mixing and confirming tests. Hopefully critical issues in LA detection, such as the interference of anticoagulants, will be overcome, in the next future. PMID:26789237
Full Text Available Methanolic extract and its ethyl acetate fraction of Cassia tora L. leaves were evaluated for anthelmintic property using the Indian adult earthworm (Pheretima posthuma as a model. Among the earthworms the ethyl acetate fraction was potent. The results were compared with a standard drug, albendazole. The phytochemical analysis of both extracts showed the presence of phenolics like flavonoids and tannins as well as anthraquinones, which may be the active principle. The present study confirms the ethno-medicinal report of the plant as an anthelmintic drug.
Suman Kundu; Saptarshi Roy; Larisha Mawkhleing Lyndem
Objective: To study the in vitro anthelmintic efficacy of Cassia alata (C. alata), Cassia(C. angustifolia) and Cassia occidentalis (C. occidentalis). angustifolia Methods: Crude ethanol extract from leaves of the three plants were prepared in rotary evaporator and different concentrations (10, 20 and 40 mg/mL) of leaf extracts were used for treatment on different representatives of helminthes (Heterakis gallinarum, Raillietina tetragona and Catatropis sp.) from domestic fowl (Gallus gallus domesticus). Loss of motility and death were monitored frequently.Results: C. alata showed early paralysis in all worms treated followed by C. angustifolia. C. occidentalis in combination with C. alata together caused early paralysis in all treated worms than the combination of C. alata with C. angustfolia. While Heterakis gallinarum in control survived for (81.33±2.07) h, treated worms lost their motility at (5.71±0.10) h, (6.60±0.86) h and (13.95±0.43) h with C. angustifolia, C. alata and C. occidentalis respectively at a concentration of 40 mg/mL which showed better efficacy than albendazole. Catatropis sp. survival period was (26.49±1.38) h in control, but with plant treatment, it lost its motility in just (0.57±0.08) h, (1.00±0.12) h and (1.47±0.40) h at 40 mg/mL concentration of C. alata, C. angustifolia and C. occidentalis respectively.Raillietina tetragona on the other hand became paralysed at (1.68±0.27) h, (2.95±0.29) h and (4.13±0.31) h with above concentrations treated with three plants respectively, however in control it survived up to (81.93±4.71) h.Conclusions:This present study indicated broad spectrum vermifugal activity of all plants tested.
Srinivasa U; Amrutia Jay N; Katharotiya Reena; Moses Semuel Rajan
Petroleum ether, chloroform, methanol and aqueous extracts of leaves of Moringa oleifera were screened for various bioactive constituents like glycosides, carbohydrates, tannins, flavonoids, triterpenoids and alkaloids. The chloroform and methanol extracts were evaluated for anthelmintic activity on adult Indian earthworms Pheritima postuma using Piperazine citrate and Rajah Pravartani Vati (Ayurvedic preparation) as a reference standards. The results obtained indicated that the chloroform ex...
Holm, Signe A.; Sørensen, Camilla; Thamsborg, Stig M.; Enemark, Heidi L.
The prevalence of gastrointestinal parasites in Danish goats and the presence of anthelmintic resistance (AR) in 10 selected herds were investigated during April-September 2012. All Danish herds (n = 137) with 10 or more adult goats were invited to participate, and of these 27 herds met the inclu...
Galvan, Noe; Middleton, John R.; Nagy, Dusty W.; Schultz, Loren G.; Schaeffer, Josh W.
A herd of alpacas was examined because of a history of severe endoparasitism, anemia, hypoproteinemia, and weight loss. Resistance of gastrointestinal nematodes to albendazole, fenbendazole, and doramectin was documented. This report suggests that anthelmintic resistance may be an emerging problem in South American camelids in North America.
Holden-Dye, Lindy; Walker, Robert J
Parasitic nematodes infect many species of animals throughout the phyla, including humans. Moreover, nematodes that parasitise plants are a global problem for agriculture. As such, these nematodes place a major burden on human health, on livestock production, on the welfare of companion animals and on crop production. In the 21st century there are two major challenges posed by the wide-spread prevalence of parasitic nematodes. First, many anthelmintic drugs are losing their effectiveness because nematode strains with resistance are emerging. Second, serious concerns regarding the environmental impact of the nematicides used for crop protection have prompted legislation to remove them from use, leaving agriculture at increased risk from nematode pests. There is clearly a need for a concerted effort to address these challenges. Over the last few decades the free-living nematode Caenorhabditis elegans has provided the opportunity to use molecular genetic techniques for mode of action studies for anthelmintics and nematicides. These approaches continue to be of considerable value. Less fruitful so far, but nonetheless potentially very useful, has been the direct use of C. elegans for anthelmintic and nematicide discovery programmes. Here we provide an introduction to the use of C. elegans as a 'model' parasitic nematode, briefly review the study of nematode control using C. elegans and highlight approaches that have been of particular value with a view to facilitating wider-use of C. elegans as a platform for anthelmintic and nematicide discovery and development. PMID:25517625
Reinemeyer, Craig R
Since 2002, selected populations of Parascaris equorum in several countries have been reported to survive treatment with macrocyclic lactone (M/L) anthelmintics. Clinical treatment failures are characterized by negligible fecal egg count reduction, but M/L resistance has been confirmed in ascarids by controlled efficacy testing. Resistance was selected by current parasite control practices for foals, which often include exclusive and excessively frequent use of M/L dewormers, thereby minimizing refugia within the host and in the environment. Chemical control of M/L-resistant isolates can be accomplished with pyrimidine and/or benzimidazole anthelmintics, but a few M/L-resistant populations have recently exhibited resistance to pyrantel pamoate as well. Some specimens of Oxyuris equi regularly survive treatment with macrocyclic lactones, but it is uncertain whether this constitutes resistance or merely confirms the incomplete oxyuricidal efficacy of virtually all broad spectrum equine anthelmintics. Variations in other biological parameters of Oxyuris and Parascaris, specifically atypical infection of older hosts and shorter prepatent periods, have been reported anecdotally. These changes may represent genetic modifications that have evolved in parallel with resistance as a result of anthelmintic selection pressure. PMID:22078748
Stuchlíková, Lucie; Jirásko, Robert; Skálová, Lenka; Pavlík, František; Szotáková, Barbora; Holčapek, Michal; Vaněk, Tomáš; Podlipná, Radka
Benzimidazoles anthelmintics, which enter into environment primarily through excretion in the feces or urine of treated animals, can affect various organisms and disrupt ecosystem balance. The present study was designed to test the phytotoxicity and biotransformation of the three benzimidazole anthelmintics albendazole (ABZ), fenbendazole (FBZ) and flubendazole (FLU) in the harebell (Campanula rotundifolia). This meadow plant commonly grows in pastures and comes into contact with anthelmintics through the excrements of treated animals. Suspensions of harebell cells in culture medium were used as an in vitro model system. ABZ, FLU and FBZ were not found to be toxic for harebell cells, which were able to metabolize ABZ, FLU and FBZ via the formation of a wide scale of metabolites. Ultrahigh-performance liquid chromatography coupled with high mass accuracy tandem mass spectrometry (UHPLC-MS/MS) led to the identification of 24, 18 and 29 metabolites of ABZ, FLU and FBZ, respectively. Several novel metabolites were identified for the first time. Based on the obtained results, the schemes of the metabolic pathways of these anthelmintics were proposed. Most of these metabolites can be considered deactivation products, but a substantial portion of them may readily be decomposed to biologically active substances which could negatively affect ecosystems. PMID:27208642
Full Text Available The aqueous extract of Cinnamomum camphorLeaves was investigated for anthelmintic activity using earthworms(Pheretima posthuma, tapeworms (Raillietina spiralis and roundworms (Ascaridia galli. Various concentrations (10-70 mg/ml of plant extract were tested in the bioassay. Piperazine citrate (10 mg/ml was used as reference standard drug whereas distilled water as control.Determination of paralysis time and death time of the worms were recorded. Extract exhibited significant anthelmintic activity at the concentration of 50 mg/ml. The result shows that aqueous extract possesses vermicidal activity and found to be effective as an anthelmintic. Therefore, the anthelmintic activity of the aqueous extract of Cinnamomum camphorLeaves has been reported. Introduction Infections with helminth are among the most widespread infections in humans and other domestic animals affecting a large number of world population. The majority of these infections due to worms are generally restricted mainly to the tropical regions and the occurance is accelerated due to unhygienic lifestyle and poverty also resulting in the development of symtomps like anaemia, eosinophilia and pneumonia1. Parasitic diseases cause ruthless morbidity affecting principally in population.
Holm Signe A.
Full Text Available The prevalence of gastrointestinal parasites in Danish goats and the presence of anthelmintic resistance (AR in 10 selected herds were investigated during April–September 2012. All Danish herds (n = 137 with 10 or more adult goats were invited to participate, and of these 27 herds met the inclusion criterion of more than 10 young kids never treated with anthelmintics. Questionnaire data on management were collected, and faecal samples from 252 kids were analysed by the McMaster technique. From all herds with a mean faecal egg count (FEC above 300 eggs per g of faeces, pooled samples were stained with peanut agglutinin (PNA for specific detection of Haemonchus contortus. Strongyle eggs were detected with an individual prevalence of 69%, including Nematodirus battus (3.6% and other Nematodirus species (15.0%. Eimeria spp. were observed in 99.6% of the kids. H. contortus was found in 11 of 12 (92% tested herds. Anthelmintics were used in 89% of the herds with mean treatment frequencies of 0.96 and 0.89 treatments per year for kids and adults, respectively. In 2011, new animals were introduced into 44% of the herds of which 25% practised quarantine anthelmintic treatments. In 10 herds the presence of AR was analysed by egg hatch assay and FEC reduction tests using ivermectin (0.3 mg/kg or fenbendazole (10.0 mg/kg. AR against both fenbendazole and ivermectin was detected in seven herds; AR against fenbendazole in one herd, and AR against ivermectin in another herd. In conclusion, resistance to the most commonly used anthelmintics is widespread in larger goat herds throughout Denmark.
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Graham, S P
The current published literature does not indicate whether the long-term effect of anticoagulant or antiplatelet therapy contributes to mortality reduction in patients with LV dysfunction. Evaluating patients for personal risk for emboli or for ischemic coronary artery events may influence the choice of therapies. As more is learned about the mechanisms of drug effects in different populations, physicians may be better able to direct appropriate therapies. Until that time, one must weigh the risks and benefits of each drug alone and in combination. In NYHA class IV patients, the risk for thrombosis owing to spontaneous clotting increases as does the adverse potential of warfarin and the adverse effects of inhibiting prostaglandin mediated vasodilation by aspirin. In NYHA class I and II patients, the quality of life and convenience of multidrug therapy is weighed against the devastating effect of a major stroke. In less symptomatic patients, the long-term risk for acute coronary events may be higher than previously identified. This would suggest that all patients with depressed LV function should be on some type of antiplatelet or anticoagulant therapy. The current WATCH study will provide much needed information about the outcome differences between these agents. Conclusions based on available data include the following: Heart failure is increasing in incidence and prevalence. Atherosclerotic disease is an important causative factor for the development of heart failure or may be a comorbid condition in these patients. There is a measurable rate of stroke in patients with heart failure, although the cause of death in large studies is more often owing to sudden death or progressive heart failure. Sudden death may be from new ischemic events, asystole, or from ventricular tachyarrhythmias. In patients with heart failure, not all strokes are cardioembolic in origin. The benefits and risks of warfarin may be increased as the EF worsens or heart failure functional class
... even if it is not listed below. Aspirin Acetaminophen (e.g., Tylenol, Excedrin) Ibuprofen (e.g., Motrin, ... skin or eyes (jaundice) Rare side effects: Headache Dizziness Shortness of breath Mouth sores or bleeding gums ...
Gasbarre, Louis C
The first documented case of macrocyclic lactone resistance in gastrointestinal (GI) nematodes of cattle was seen in the US approximately 10 years ago. Since that time the increase incidence of anthelmintic resistance has continued at an alarming rate. Currently parasites of the genera Cooperia and/or Haemonchus resistant to generic or brand-name macrocyclic lactones have be demonstrated in more than half of all operations examined. Both of these parasite genera are capable of causing economic losses by decreasing food intake and subsequently animal productivity. Currently, there are no easy and quick means to detect anthelmintic resistant GI nematodes. Definitive identification requires killing of cattle. The most commonly used field detection method is the fecal egg count reduction test (FECRT). This method can be adapted for use as a screening agent for Veterinarians and producers to identify less than desired clearance of the parasites after anthelmintic treatment. Further studies can then define the reasons for persistence of the egg counts. The appearance of anthelmintic resistance is largely due to the development of very effective nematode control programs that have significantly improved the productivity of the US cattle industry, but at the same time has placed a high level of selective pressure on the parasite genome. The challenges ahead include the development of programs that control the anthelmintic resistant nematodes but at the same time result in more sustainable parasite control. The goal is to maintain high levels of productivity but to exert less selective pressures on the parasites. One of the most effective means to slow the development of drug resistance is through the simultaneous use of multiple classes of anthelmintics, each of which has a different mode of action. Reduction of the selective pressure on the parasites can be attained through a more targeted approach to drug treatments where the producer's needs are met by selective
Maisale A B
Full Text Available Vigna unguiculata Linn belonging to family Fabaceae are used traditionally as appetizer, diuretic, laxative, anthelmintic. Seeds are coarse powdered and exhaustively with hot solvent (Soxhlet extraction by ethanol and maceration with chloroform water I.P. Five concentrations (10-100 mg/ml of ethanolic and aqueous extracts were studied for anthelmentic activity by using Eudrilus euginiae earthworms. Both aqueous and ethanolic extracts showed paralysis and death of worms in concentration (10-100 mg/ml dependent manner. Alcoholic extract of Vigna unguiculata showed significant activity than aqueous extract. Piperazine citrate (10 mg/ml and distilled water were included in the assay as standard drug and control respectively. The result showed seeds of vigna unguiculata possessed potential anthelmintic activity. The seeds extract also showed presence of flavonoids, and glycosides by preliminary phytochemical investigations.
Pena-Espinoza, Miguel Angel; Williams, Andrew; Thamsborg, Stig Milan;
BACKGROUND: Chicory (Cichorium intybus) has potential as a natural anthelmintic in livestock, however evidence of efficacy against cattle nematodes is lacking. Here, we investigated anthelmintic effects of chicory in stabled calves. METHODS: Jersey male calves (2-4 months) were stratified by live...... weight and allocated randomly to 2 groups: chicory (CHI, n=9) and control (CON, n=6). CHI and CON calves were fed with forage chicory silage (cv. Spadona) and hay ad libitum, resp., for 8 weeks. After 2 weeks, calves were infected with 10,000 Ostertagia ostertagi and 65,000 Cooperia oncophora larvae....... Fecal egg counts (FEC) and live weights were assessed weekly. Six weeks after infection, calves were slaughtered for worm recovery. In parallel, total sesquiterpene lactone (SL)-extracts from forage chicory (Spadona and cv. Puna II) were prepared and incubated with first-stage larvae (L1) of O...
Full Text Available We have tested the efficacy of some vegetal extracts (Parazitol –Medica Laboratories, a natural product with an anthelmintic effect and a Cucurbita sp. oil extract compared to the classic anthelmintics (Rombendazol – Romvac and Dehelman – KRKA Slovenia at domestic poultry, whose parasitical status had been previously established through animal killing and necropsies. Parazitol and the pumpkin oil have had a lower efficacy than the levamisole and albendazole upon the species Ascaridia galli. Heterakis gallinarum was not affected by the pumpkin oil. Parazitol have a moderate efficacy (36%, while levamisole and albendazole were very efficient (100%. The treatments with albendazole upon the cestods belonging to the genus Raillietina have had a 100% efficacy. In cestods, Parazitol had a better efficacy (57% than the pumpkin oil (14%.
Krücken, Jürgen; Harder, Achim; Jeschke, Peter; Holden-Dye, Lindy; O'Connor, Vincent; Welz, Claudia; von Samson-Himmelstjerna, Georg
The broad-spectrum anthelmintic cyclooctadepsipeptide PF1022A is a fungal metabolite from Rosellinia sp. PF1022, which is a Mycelia sterilia found on the leaves of Camellia japonica. A broad range of structurally related cyclooctadepsipeptides has been characterized and tested for anthelmintic activities. These metabolites have been used as starting points to generate semisynthetic derivatives with varying nematocidal capacity. Predominant among these compounds is emodepside, which exhibits a broad nematocidal potential against gastrointestinal and extraintestinal parasites. Here we review the chemical biology and mode of action of cyclooctadepsides with particular attention to PF1022A and emodepside. We illustrate how they target nematode neuromuscular function, opening up new avenues for antiparasitic treatments with potential capability for important selective toxicity. PMID:22858281
Nalubamba, King S; Mudenda, Ntombi B
There has been an increase in the number of wild ungulates kept in captivity for ecotourism and conservation in Zambia and these animals are susceptible to a number of diseases including gastrointestinal helminth infections. Surveys to determine anthelmintic efficacy to gastrointestinal nematodes in captive-wildlife are not common and there have been no reports of anthelmintic resistance in captive-wildlife in Zambia. This study was carried out to determine the efficacy of the benzimidazole anthelmintic fenbendazole in captive wild impala (Aepyceros melampus) in Zambia. During the month of April 2011, at the end of the rainy season, the faecal egg count reduction test was performed at a private game facility for assessing anthelmintic efficacy of oral fenbendazole and the anthelmintic treatment showed an efficacy of 90%. Haemonchus spp. and Trichostrongylus spp. were the predominant genera present before treatment, but Haemonchus spp. larvae were the only genus recovered from the faecal cultures after anthelmintic treatment. This represents the first documentation of anthelmintic treatment failure in captive wild-antelopes in Zambia. It also demonstrated the ineffectiveness of the common traditional practice of deworming captive-wild antelopes at the end of the rainy season due to the rapid re-infection of impala that occurs due to high pasture infectivity. Suggestions on changes to current anthelmintic use/practices that will make them more efficacious and reduce the possibility of development of anthelmintic resistance in captive wild game in Zambia are also made. PMID:22115945
Tshikudi, Diane M.; Tripathi, Markandey M.; Hajjarian, Zeinab; Nadkarni, Seemantini K.
Defective blood coagulation resulting from excessive procoagulant activity often leads to thrombotic disorders such as stroke and myocardial infarction. A variety of oral and injectable anticoagulant drugs are prescribed to prevent or treat life-threatening thrombosis. However, due to bleeding complications often associated with anticoagulant treatment, routine monitoring and accurate dosing of anticoagulant therapy is imperative. We have developed Optical thromboelastography (OTEG), a non-contact approach that utilizes a drop of whole blood to measure blood coagulation status in patients. Here, we demonstrate the capability of OTEG for rapidly monitoring anticoagulation in whole blood samples. OTEG monitors coagulation status by assessing changes in blood viscosity from temporal intensity fluctuations of laser speckle patterns during clotting. In OTEG a blood drop is illuminated with coherent light and the blood viscosity is measured from the speckle intensity autocorrelation curve, g2 (t). The metrics, clotting time (R+k), clot progression (angle) and maximum clot stiffness (MA) are then extracted. The aim of the current study was to evaluate the accuracy of OTEG in assessing anticoagulation status of common anticoagulants including heparin, argatroban and rivaroxaban status. A dose-dependent prolongation of R+k was observed in anticoagulated blood, which closely corresponded with standard-reference Thromboelastography (TEG) (r 0.87-0.99, P>0.01 for all cases). OTEG angle was unaltered by anticoagulation whereas TEG angle presented a dose-dependent diminution probably linked to clot rupture. In both OTEG and TEG, MA was unaffected by heparin, argatroban or rivaroxaban. We conclude that OTEG can accurately monitor anticoagulation status following treatment, potentially providing a powerful tool for routine monitoring of patients in the doctor's office or in the home setting.
Godier, A; Martin, A-C; Rosencher, N; Susen, S
Direct oral anticoagulants (DOAC) are recommended for stroke prevention in atrial fibrillation and for the treatment of venous thromboembolism. However, they are associated with hemorrhagic complications. Management of DOAC-induced bleeding remains challenging. Activated or non-activated prothrombin concentrates are proposed, although their efficacy to reverse DOAC is uncertain. Therapeutic options also include antidotes: idarucizumab, antidote for dabigatran, has been approved for use whereas andexanet alpha, antidote for anti-Xa agents, and aripazine, antidote for all DOAC, are under development. Other options include hemodialysis for the treatment of dabigatran-associated bleeding and administration of oral charcoal if recent DOAC ingestion. DOAC plasma concentration measurement is necessary to guide DOAC reversal. We propose an update on DOAC-associated bleeding, integrating the availability of dabigatran antidote and the critical place of DOAC concentration measurements. PMID:27297642
Young, K E; Garza, V; Snowden, K; Dobson, R J; Powell, D; Craig, T M
Diversity of parasite populations was compared between two herds of horses, one a regularly treated herd the other a feral herd which has bad no anthelmintic treatment for at least 25 years. Eggs obtained from fecal samples of both herds were tested for anthelmintic resistance by use of an in-vitro larval hatch/development assay (LDA), DrenchRite. A fecal egg reduction test was also performed with the domesticated herd using fenbendazole, pyrantel pamoate and ivermectin. Cyathostomes were the predominant group of worms present in both herds. Trichostrongylus axei was seen in both herds, but Strongylus equinus, Strongylus vulgaris, Gyalocephalus capitatus, Poteriostomum spp. and Strongyloides westeri were only found in the feral horses. Larvae of Strongylus edentatus were found in a single domesticated horse. Fecal egg reduction tests with the domesticated herd showed a 32% egg count reduction for fenbendazole, a 93% reduction with pyrantel, and a 99% reduction with ivermectin. From the LDA, anthelmintic resistance was evaluated by determining the resistance ratio of the domesticated herd compared with the feral herd. For benzimidazoles in the domesticated herd, 45% of the cyathostome population was 9.4 times more tolerant than the feral herd's parasite population. The parasite population in the domesticated herd was 1.5 times more tolerant to Levamisole, and 1.7 times more tolerant to the benzimidazole/levamisole combination than the parasite population within the feral herd. 9% of the parasite population in the domesticated herd was 90 times more tolerant to avermectins than the feral herd's parasite population, even though a subpopulation of worms in the feral herd were tolerant to low concentrations of avermectins despite never being previously exposed to this class of anthelmintic. PMID:10485366
Holden-Dye, L.; Walker, R
Parasitic nematodes infect many species of animals throughout the phyla, including humans. Moreover, nematodes that parasitise plants are a global problem for agriculture. As such, these nematodes place a major burden on human health, on livestock production, on the welfare of companion animals and on crop production. In the 21st century there are two major challenges posed by the wide-spread prevalence of parasitic nematodes. First, many anthelmintic drugs are losing their effectiveness beca...
Nielsen, Martin K
Given the increasing levels of anthelmintic resistance in equine parasites, parasitologists now recommend traditional treatment approaches to be abandoned and replaced by more sustainable strategies. It is of crucial importance to facilitate veterinary involvement to ensure that treatment decisions are based on parasitic knowledge. Despite recommendations given for the past two decades, strategies based on the selective therapy principle have not yet been implemented on a larger scale in equi...
Kerboeuf, Dominique; Guégnard, Fabrice
P glycoproteins (Pgp), members of the ABC transporter superfamily, play a major role in chemoresistance. In nematodes, Pgp are responsible for resistance to anthelmintics, suggesting that they are Pgp substrates, as they are in mammalian cells. However, their binding to nematode Pgp and the functional consequences of this interaction have not been investigated. Our study showed that levamisole and most of the macrocyclic lactones (MLs) are Pgp substrates in nematodes. Ivermectin, although a v...
Mondal Subhasish; Ghosh Parag; Das Debasish; Haque Rabiul
The aqueous extract of Clerodendron inerme leaves was investigated for anthelmintic activity using earthworms(Pheretima posthuma), tapeworms (Raillietina spiralis) and roundworms (Ascaridia galli). Various concentrations (10-50 mg/ml) of plant extract were tested in the bioassay. Piperazine citrate (10 mg/ml) was used as reference standard drug whereas distilled water as control. Determination of paralysis time and death time of the worms were recorded. Extract exhibited significant anthelmin...
Full Text Available Petroleum ether, chloroform, methanol and aqueous extracts of leaves of Moringa oleifera were screened for various bioactive constituents like glycosides, carbohydrates, tannins, flavonoids, triterpenoids and alkaloids. The chloroform and methanol extracts were evaluated for anthelmintic activity on adult Indian earthworms Pheritima postuma using Piperazine citrate and Rajah Pravartani Vati (Ayurvedic preparation as a reference standards. The results obtained indicated that the chloroform extract was more potent compared to other extracts.
Wang, G-X; Han, J; Zhao, L-W; Jiang, D-X; Liu, Y-T; Liu, X-L
The present study was undertaken to investigate the anthelmintic activity of crude extracts and pure compounds from the rhizomes of Paris polyphylla. The methanol extract showed a promising anthelmintic activity against Dactylogyrus intermedius (EC(50) value=18.06 mg l(-¹). Based on these finding, the methanol extract was fractionated on silica gel column chromatography in a bioassay-guided fractionation affording two known steroidal saponins showing potent activity, dioscin and polyphyllin D. Both dioscin and polyphyllin D exhibited significant activity against D. intermedius with EC(50) values of 0.44 and 0.70 mg l(-¹), respectively, which were more effective than the positive control, mebendazole (EC(50) value=1.25 mg l(-¹)). The acute toxicities (LC(50)) of dioscin and polyphyllin D for goldfish were 1.37 and 1.08 mg l(-¹), respectively. These results indicated that P. polyphylla extract and the isolated compounds are potential natural agents for the control of Dactylogyrus infestation. This is the first report on in vivo anthelmintic investigation for P. polyphylla. PMID:20576414
Full Text Available A multiresidue method (LC-MS/MS for determination of wide range of anthelmintics was developed. The method covered benzimidazoles: albendazole (and metabolites, cambendazole, fenbendazol (and metabolites, flubendazole (and metabolites, mebendazole (and metabolites, oxibendazole, thiabendazole (and metabolites, triclabendazole (and metabolites; macrocyclic lactones: abamectin, doramectin, emamectin, eprinomectin, ivermectin, moxidectin; salicylanilides: closantel, ioxynil, nitroxynil, oxyclosamide, niclosamide, rafoxanid and others: clorsulon, derquantel, imidocarb, monepantel (and metabolites, morantel, praziquantel, and pyrantel. The method was used to examine the potential presence of anthelmintics in goat and sheep milk and dairy products from the Polish market. A total of 120 samples of milk, yoghurt, cottage cheese, cream cheese, and curd were analysed. None of the samples were found positive above CCα (1-10 μg/kg except for one cottage cheese in which traces of albendazole sulfone were detected (5.2 ug/kg and confirmed. The results of the study showed negligible anthelmintic residues in the goat and sheep milk and dairy products and confirm their good quality.
Vigano D'Angelo, S; Comp, P C; Esmon, C T; D'Angelo, A.
Protein C is a natural vitamin K-dependent plasma anticoagulant, deficiencies of which have been found in patients with recurrent thrombosis and warfarin-induced skin necrosis. To appreciate more fully the role of protein C in disease states and during oral anticoagulation, a new functional assay for protein C involving adsorption of plasma protein C on a Ca+2-dependent monoclonal antibody, elution, quantitative activation, and assessment of plasma anticoagulant activity, has been developed. ...
E.A. Akl; S. Gunukula; M. Barba; V.E.D. Yosuico; F.F. van Doormaal; S. Kuipers; S. Middeldorp; H.O. Dickinson; A. Bryant; H. Schuenemann
Background Anticoagulation may improve survival in patients with cancer through an antitumor effect in addition to the perceived antithrombotic effect. Objectives To evaluate the efficacy and safety of parenteral anticoagulants in patients with cancer with no therapeutic or prophylactic indication f
DU Xin; MA Chang-sheng; LIU Xiao-hui; DONG Jian-zeng; WANG Jun-nan; CHENG Xiao-jing
@@ Nonvalvular atrial fibrillation (NVAF) is the most common sustained cardiac arrhythmia in clinical practice, which if untreated results in a doubling of cardiovascular morbidity and mortality. AF is an independent predictor of stroke, with an annual risk 5 to 6 times higher than patients in sinus rhythm.1 During recent years, several randomised clinical trials conducted by investigators around the world involving 13 843 participants with NVAF have demonstrated convincingly the value of warfarin therapies for stroke prevention in high risk patients.2-8 However, the dose response of warfarin is complex and its activity is easily altered by concurrent medications, food interactions, alcohol and illnesses. Adherence to medical advice and routine monitoring of the international normalized ratio (INR) is important, because low anticoagulant intensity predisposes the patients to thromboembolic complications and high intensity to haemorrhage. Studies suggested that anticoagulant clinics could improve the quality of anticoagulation control,9 and anticoagulant clinics are common in western countries. However, in China, most AF patients taking warfarin usually attend the outpatient clinic of cardiology, while the quality of anticoagulation control is never investigated. We therefore assessed anticoagulation control in the outpatient clinic of cardiology, and the quality of anticoagulation control since the establishment of anticoagulant clinics.
Full Text Available To know the anthelmintic activity of leaves of Lawsonia inermis, we used maceration method of extraction using solvents like ethanol and methanol. Each extract was tested for anthelminthic activity by following standard method .The ethanolic and methanolic extract displayed anthelmintic activity in dose dependant manner. We found that the ethanolic as well as methanolic extracts were more potent than the positive control as far as their anthelmintic activity was concerned. To correlate phytochemical screening with anthelmintic activity, phytochemical evaluation of the extract was also performed. From our result it may be mentioned that the ethanolic extract was potent as anthelmintic agent due to the presence of glycosides, terpenoids and flavonoids. On the other hand, the methanolic extract was effective probably due to the involvement of alkaloids, glycosides, terpenoids and flavonoids.
Full Text Available Staphylococcus aureus is a Gram-positive bacterium that has become the leading cause of hospital acquired infections in the US. Repurposing Food and Drug Administration (FDA approved drugs for antimicrobial therapy involves lower risks and costs compared to de novo development of novel antimicrobial agents. In this study, we examined the antimicrobial properties of two commercially available anthelmintic drugs. The FDA approved drug niclosamide and the veterinary drug oxyclozanide displayed strong in vivo and in vitro activity against methicillin resistant S. aureus (minimum inhibitory concentration (MIC: 0.125 and 0.5 μg/ml respectively; minimum effective concentration: ≤ 0.78 μg/ml for both drugs. The two drugs were also effective against another Gram-positive bacteria Enterococcus faecium (MIC 0.25 and 2 μg/ml respectively, but not against the Gram-negative species Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and Enterobacter aerogenes. The in vitro antimicrobial activity of niclosamide and oxyclozanide were determined against methicillin, vancomycin, linezolid or daptomycin resistant S. aureus clinical isolates, with MICs at 0.0625-0.5 and 0.125-2 μg/ml for niclosamide and oxyclozanide respectively. A time-kill study demonstrated that niclosamide is bacteriostatic, whereas oxyclozanide is bactericidal. Interestingly, oxyclozanide permeabilized the bacterial membrane but neither of the anthelmintic drugs exhibited demonstrable toxicity to sheep erythrocytes. Oxyclozanide was non-toxic to HepG2 human liver carcinoma cells within the range of its in vitro MICs but niclosamide displayed toxicity even at low concentrations. These data show that the salicylanilide anthelmintic drugs niclosamide and oxyclozanide are suitable candidates for mechanism of action studies and further clinical evaluation for treatment of staphylococcal infections.
Williams, Andrew; Pena-Espinoza, Miguel Angel; Boas, Ulrik;
Chicory is a perennial crop that has been investigated as a forage source for outdoor-reared ruminants and pigs, and has been reported to have anthelmintic properties. Here, we investigated in vitro anthelmintic effects of forage chicory-extracts against the highly prevalent swine parasites Ascaris...... suum and Oesophagostomum dentatum. Methanol extracts were prepared and purified from two different cultivars of chicory (Spadona and Puna II). Marked differences were observed between the anthelmintic activity of extracts from the two cultivars. Spadona extracts had potent activity against A. suum...... anthelmintic activity of forage chicory towards swine nematodes. Our results indicate a significant anthelmintic effect, which may possibly be related to SL composition....
Meegaard, Peter Martin; Holck, Line H V; Pottegård, Anton;
Excessive anticoagulation with vitamin K antagonists is a serious condition with a substantial risk of an adverse outcome. We thus found it of interest to review a large case series to characterize the underlying causes of excessive anticoagulation....
Yates, Scott W
No agents are approved to reverse the effects of newer anticoagulants used to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. This review focuses on ways to monitor, interrupt, and reverse such anticoagulation.
The prevalence of medical conditions representing a risk for thromboembolic complications and requiring antithrombotic therapy increases gradually with age. Two cases of fatal noncritical organ bleeding complication that occurred during the conversion period from initial fondaparinux to vitamin K antagonist are presented. An 81-year-old obese female patient (body mass index 43 kg/m(2)) with previous postoperative thrombosis underwent uneventful total knee replacement under spinal anesthesia. She presented with popliteal hematoma during conversion to oral anticoagulant. A 92-year-old female patient (body mass index 33 kg/m(2)) with left lower limb thrombosis was referred to our orthopedics department from her senior citizens' home for right lower limb hematoma and ischemia that occurred during conversion to oral anticoagulant. Thromboembolic and bleeding events in the elderly are real public health problems. Specific guidelines dedicated to this particular population are needed, which will improve the management of anticoagulation and decrease risk of complications. PMID:26547115
Pook, J F; Power, M L; Sangster, N C; Hodgson, J L; Hodgson, D R
Resistance, especially to the anthelmintic benzimidazoles (BZ), has been reported in horse cyathostomes world-wide. Diagnosis of resistance has traditionally been made by faecal egg count reduction (FECR) trials, however, this technique has limitations. Some of the shortcomings may be resolved by refining the test or by using an in vitro test. FECR tests and the larval development assay (LDA) were performed on adult horses held on 15 different horse properties across a wide geographical area of NSW, Australia. FECR were measured before and 10-14 after days treatment with oxibendazole (OBZ), morantel (MOR) or ivermectin (IVM) at recommended dose rates. Eight properties were rejected following low pre-treatment egg counts, leaving seven in the study. On these, the majority of larvae recovered from faecal cultures were cyathostomes. Using a definition of resistance as a FECR of horse egg counts pre- and post-treatment was developed and results from the same properties compared with the results of the LDA. For example, for the BZ, correlation coefficients of values of lethal concentration to kill 50% of population (LC50) on LDA and FECR percentages were -0.536 before and -0.704 after OBZ treatment. We conclude that the LDA has the potential to be a single visit test for detection of anthelmintic resistance in horse cyathostomes but requires further investigation and standardisation. PMID:12079739
Nutescu, Edith A.; Burnett, Allison; Fanikos, John; Spinler, Sarah; Wittkowsky, Ann
Anticoagulant drugs are the foundation of therapy for patients with VTE. While effective therapeutic agents, anticoagulants can also result in hemorrhage and other side effects. Thus, anticoagulant therapy selection should be guided by the risks, benefits and pharmacologic characteristics of each agent for each patient. Safe use of anticoagulants requires not only an in-depth knowledge of their pharmacologic properties but also a comprehensive approach to patient management and education. Thi...
An adult, intact female Australian shepherd presented for frank vaginal bleeding of unknown duration. The only coagulation profile abnormality upon presentation was mild prolongation of the partial thromboplastin time (PTT). The uterus was removed at surgery and contained a large amount of coagulated blood. Clotting profiles were markedly abnormal48 hours postoperatively. Serum analysis was positive for brodifacoum, an anticoagulant rodenticide. Preoperative coagulation was most likely normalized by vitamin K-1 therapy administered prior to presentation. The only manifestation of anticoagulant rodenticide was hematometra. Rodenticide intoxication should be considered in the differential diagnosis list of hematometra or metrorrhagia
Samuel P. Hammar
Full Text Available We describe a 64-year-old man with extensive diffuse acute lung hemorrhage, presumably as a result of anticoagulation therapy. We evaluated reports in the literature concerning acute exacerbation (acute lung injury of unknown cause in UIP and other forms of fibrotic interstitial pneumonias. We also evaluated autopsy tissue in this case in order to determine the cause of death in this 64-year-old man, who was initially thought to have an asbestos-related disease. Based on the autopsy findings, this man died as a result of anticoagulation therapy; specifically, the use of Xarelto® (rivaroxaban.
Samamaa, M-M; Conard, J; Flaujac, C; Combe, S; Horellou, M-H
Amongst numerous promising anticoagulant molecules, rivaroxaban (Xarelto(®)), dabigatran (Pradaxa(®)) and apixaban (Eliquis(®)) have been registered outside the USA in the prevention of thromboembolic events in patients undergoing total hip or knee prosthetic replacement. Rivaroxaban however has been granted authorisation by the FDA for the thromboprophylaxis after surgery for total hip or knee surgery. Dabigatran has been granted authorisation by the FDA in non-valvular atrial fibrillation (RE-LY trial) while rivaroxaban is expecting approval in this same indication (ROCKET trial). Phase III results in the treatment and in the secondary prevention of established venous thrombosis and pulmonary embolism are encouraging. These small molecules are obtained by chemical synthesis, their molecular weight is lower than 500 daltons. Many coagulation tests may be affected by these molecules. Those modifications should be known in order to avoid misinterpretation of the tests but could also be used to measure plasma concentrations of these products. The choice of a non specific global and readily available test has been documented (Quick time for rivaroxaban and aPTT for dabigatran). Anti-Xa (for rivaroxaban) and anti-IIa (for dabigatran) activities should however be preferred, expressed in ng/ml with calibrated plasmas (containing predetermined concentration of the tested drug). The half-life is around 8 to 12 hours, with a peak activity 2 to 4 hours after ingestion. Dabigatran is mainly eliminated via the kidney, hence requiring dose-adjustment in case of moderate renal insufficiency, and contra-indicated in case of severe renal insufficiency. Rivaroxaban being excreted via kidney and liver, some precautions should apply in case of liver insufficiency. No data are available in pregnancy or pediatrics, clinical trials are ongoing. There are few interactions with concomitant drugs, which should not be ignored. The short half-life of these new agents compensates for the
Das, S S; Dey, Monalisha; Ghosh, A K
The aim of the present study was to evaluate the anthelmintic activity of ethanolic and aqueous extract of leaves and bark of Tamarindus indica Linn using Pheretima posthuma and Tubifex tubifex as test worms. The time of paralysis and time of death were studied and the activity was compared with piperazine citrate as reference standard. The alcohol and aqueous extract of bark of Tamarindus indica exhibited significant anthelmintic activity as evidenced by decreased paralyzing time and death time. The results thus support the use of Tamarindus indica as an anthelmintic agent. PMID:22131633
S S Das
Full Text Available The aim of the present study was to evaluate the anthelmintic activity of ethanolic and aqueous extract of leaves and bark of Tamarindus indica Linn using Pheretima posthuma and Tubifex tubifex as test worms. The time of paralysis and time of death were studied and the activity was compared with piperazine citrate as reference standard. The alcohol and aqueous extract of bark of Tamarindus indica exhibited significant anthelmintic activity as evidenced by decreased paralyzing time and death time. The results thus support the use of Tamarindus indica as an anthelmintic agent.
Nutescu, Edith A; Burnett, Allison; Fanikos, John; Spinler, Sarah; Wittkowsky, Ann
Anticoagulant drugs are the foundation of therapy for patients with VTE. While effective therapeutic agents, anticoagulants can also result in hemorrhage and other side effects. Thus, anticoagulant therapy selection should be guided by the risks, benefits and pharmacologic characteristics of each agent for each patient. Safe use of anticoagulants requires not only an in-depth knowledge of their pharmacologic properties but also a comprehensive approach to patient management and education. This paper will summarize the key pharmacologic properties of the anticoagulant agents used in the treatment of patients with VTE. PMID:26780737
Nielsen, Martin Krarup; Betancourt, Alejandra; Lyons, Eugene T.;
Cyathostomins can cause a severe inﬂammation of equine large intestine characterized by substantial ventral edema and pronounced protein loss. Anthelmintic treatment of horses can result in a localized inﬂammatory response in the colonic mucosa of clinically normal horses. The aim of this study was...... to evaluate the systemic inﬂammatory response of ponies naturally infected with cyathostomins to single dose representatives of three anthelmintic drug classes, namely, oxibendazole, pyrantel pamoate, and moxidectin. Thirty ponies aged between 1 and 18 years of age were allocated to one of three...... anthelmintic treatments groups. Anthelmintic efﬁcacy was evaluated using the fecal egg count reduction test performed weekly between 2 and 8 weeks post-treatment. Inﬂammatory responses were evaluated on days 0, 1, 3, 5, and 14 after treatment using hematology, measurement of the acute phase inﬂammatory markers...
Liu, Guang-Lu; Hao, Bing; Liu, Shao-Peng; Wang, Gao-Xue
In an attempt to develop novel anthelmintic agents, our previously isolated osthol was used as lead structures for further optimization. In our research, a series of coumarin analogs, prepared from 7-hydroxy coumarin or 7-hydroxy-4-methyl coumarin, have been evaluated for their anthelmintic activities. In all of the compounds, 6 and 7 were first synthesized, and their structures were identified based on NMR and MS values. Among the candidates, 8-allyl-7-allyloxycoumarin showed better anthelmintic activity than other compounds against Dactylogyrus infestation with EC(50) value of 1.81 mg/L. The quantitative structure-activity relationship (QSAR) of 16 osthol analogs with anthelmintic activity expressed as pEC(50) and toxicity to goldfish expressed pLC(50), such results can offer useful theoretical references for future experimental works. PMID:22749191
Full Text Available The present work was conducted to investigate the preliminary phytochemical studies and anthelmintic activities on the bark of Acacia suma (Roxb. Family- Fabaceae against adult Indian earthworms, Pheretima posthuma. Various concentrations (5-25 mg/ml of each extract along with the reference samples (Piperazine citrate, Albendazole were subjected for anthelmintic activity study. The qualitative test revealed that the petroleum ether extracts contained only terpenoids but chloroform and hydroalcoholic (Methanol 70% v/v extracts exhibited the presence of carbohydrates, alkaloids, glycosides, flavonoids, tannins and saponins but amino acids and steroids were absent. All the extracts showed anthelmintic activity when compared with petroleum ether and chloroform extracts. The anthelmintic activity of hydroalcoholic extract was comparable with reference drugs.
Heckendorn, F.; Werne, S.; V. Maurer; Perler, E.; Amsler, Z.; Probst, J.; Zaugg, C.; Krenmeyr, I
Gastrointestinal nematodes (GIN) are one of the most important problems affecting health and therefore performance and welfare in small ruminant husbandry. The control of these parasites in the past strongly relied on the repeated use of anthelmintic drugs. This has led to nematode populations which are resistant to most of the currently available anthelmintics. Furthermore customer’s demands for organic and residue free animal products are increasing. The aforementioned problems have given a...
Werne, S.; V. Maurer; Perler, E.; Amsler, Z.; Probst, J.; Zaugg, C.; Krenmayr, I.; Schwery, M.; Volken, H.; Heckendorn, F.
Gastrointestinal nematodes (GIN) are one of the most important problems affecting health and therefore performance and welfare in small ruminant husbandry. The control of these parasites in the past strongly relied on the repeated use of anthelmintic drugs. This has led to nematode populations which are resistant to most of the currently available anthelmintics. Furthermore customer’s demands for organic and residue free animal products are increasing. The aforementioned problems have given a...
Ali, Niaz; Aleem, Umer; Ali Shah, Syed Wadood; Shah, Ismail; Junaid, Muhammad; Ahmed, Ghayour; Ali, Waqar; Ghias, Mehreen
Background Rubus fruticosus is used in tribal medicine as anthelmintic and an antispasmodic. In the current work, we investigated the anthelmintic and antispasmodic activities of crude methanol extract of fruits of R. fruticosus on scientific grounds. Acute toxicity and brine shrimp cytotoxicity activity of the extract were also performed. Methods Acute toxicity study of crude methanol extract of R. fruticosus was performed on mice. In vitro Brine shrimp cytotoxicity assay was performed on sh...
Das, S S; Monalisha Dey; Ghosh, A. K.
The aim of the present study was to evaluate the anthelmintic activity of ethanolic and aqueous extract of leaves and bark of Tamarindus indica Linn using Pheretima posthuma and Tubifex tubifex as test worms. The time of paralysis and time of death were studied and the activity was compared with piperazine citrate as reference standard. The alcohol and aqueous extract of bark of Tamarindus indica exhibited significant anthelmintic activity as evidenced by decreased paralyzing time and death t...
M L Vijaya Kumar; Thippeswamy, B.; I L Kuppust; Naveenkumar, K. J.; C K Shivakumar
Objective: To assess the anthelmintic acivity of Bacillus cereus and Bacillus pumilus metabolites. Materials and Methods: The successive solvent extractions with petroleum ether, ethyl acetate and methanol. The solvent extracts were tested for anthelmintic activity against Pheretima posthuma at 20 mg/ml concentration. The time of paralysis and time of death of the worms was determined for all the extracts. Albendazole was taken as a standard reference and sterile water as a control. Results: ...
Chintoan-Uta, C.; Morgan, E R; Skuce, P. J.; Coles, G.C.
Gastrointestinal (GI) nematodes are among the most important causes of production loss in farmed ruminants, and anthelmintic resistance is emerging globally. We hypothesized that wild deer could potentially act as reservoirs of anthelmintic-resistant GI nematodes between livestock farms. Adult abomasal nematodes and faecal samples were collected from fallow (n = 24), red (n = 14) and roe deer (n = 10) from venison farms and areas of extensive or intensive livestock farming. Principal componen...
Abdelqader, Anas; Qarallah, Bassam; Al-Ramamneh, Diya; Daş, Gürbüz
The use of phytogenic bioactive compounds to control poultry helminthes is increasing in different production systems. In vitro and in vivo anthelmintic activity of citrus peels against Ascaridia galli was investigated. Ethanolic extracts of three citrus peels species were suspended in 0.5% dimethyl sulfoxide (DMSO) to form an experimental composition (EC). EC was mainly composed of Limonene (96%), followed by β-Pinene (1.5%), α-Pinene (0.5%), and Sabinene (0.3%). For in vitro investigation, adult A. galli worms (n=225) were collected from naturally infected chickens and distributed to 3 equal groups. Groups 1, 2, and 3 were exposed to Fenbendazole (0.5mg/ml), EC (50mg/ml), and 0.5% DMSO, respectively. For in vivo investigation, 200 Lohmann Selected Leghorns chicks were infected at 1-day old with 250 embryonated A. galli eggs. At 6 weeks of age, 150 A. galli infected birds were randomly allocated into 5 equal groups. Groups 1, 2, and 3 were treated with 300, 600, and 1200 mg EC kg(-1) body weight, respectively. Group 4 was treated with Fenbendazole (50 mg kg(-1)). Group 5 was left as control. Birds were euthanized 2-weeks post-treatment, and all worms were collected from their intestines. EC possessed significant (P0.05) difference was quantified between number of motile worms exposed either to EC or Fenbendazole 7h post-exposure. A significant (Pgalli burden (Efficacy=97%) followed by 1200 mg EC kg(-1) (68%), 600 mg EC kg(-1) (66%), and 300 mg EC kg(-1) (5%). It is concluded that citrus peels extracts have potential anthelmintic properties against A. galli. PMID:22463876
Torbert, B J; Klei, T R; Lichtenfels, J R; Chapman, M R
Ponies reared with minimal or no exposure to anthelmintics were surveyed for intestinal helminths in order to estimate prevalence and intensity of parasite populations unaltered by frequent exposure to anthelmintics. Thirty-seven mixed breed ponies of varying ages were examined. Thirty-four species of nematodes and 2 species of cestodes were found. Twenty-four of the nematode species (including 1 new species) were in the subfamily Cyathostominae (small strongyles). Eighty-seven percent of the total burden of adult small strongyles in the large intestine was composed of 10 species. By comparing the results of the present survey with those of recent surveys of horses from herds which had been subjected to treatments with anthelmintics, the effect of prolonged usage of anthelmintic treatment on the prevalence of individual species possibly can be estimated. The general ranking of the 10 most common cyathostome species was similar to those described in recent surveys of horses, suggesting that anthelmintic pressure does not affect the prevalence of most cyathostome species. The lack of anthelmintic treatment appeared not to affect prevalence rates for Anoplocephala perfoliata and Anoplocephala magna when compared to other studies. Conversely, prevalence rates for Strongylus spp., Triodontophorus spp., Craterostomum acuticaudatum, Oxyuris equi, and Parascaris equorum were higher than those reported for these species in recent studies of horses. PMID:3819969
Fernanda Ramos; Luiza Pires Portella; Fernando de Souza Rodrigues; Caroline Zamperete Reginato; Luciana Pötter; Alfredo Skrebsky Cezar; Luís Antônio Sangioni; Fernanda Silveira Flores Vogel
Gastrointestinal nematodes resistant to anthelmintics have been reported in several regions of Brazil, and they may be associated with economic losses for the cattle industry. This study aimed to evaluate the resistance status of gastrointestinal nematodes from naturally infected beef cattle to several commercially available anthelmintics, as well as to test the efficacy of combinations of anthelmintics against multi-resistant gastrointestinal nematodes. Ten farms located in Rio Grande do Sul...
Boyko N. N.
Full Text Available The possibility to use vector algebra theory for quantitative description of antibacterial medications and comparison of their properties has been shown. Mathematic formulas for description of medications’ antibacterial action basing on data of simple to use well method have been presented. This method allows evaluation of medications’ antibacterial activity and opportunity to choose the most active ones, as well as compare them with each other. It is noted that medications of natural origin are inferior to those of synthetic origin as for their antibacterial activity, and new galenic medications possess the most antimicrobial properties. The prospects of this method for pharmacoeconomic analysis of medications conducted in order to chose optimal cost/quality ratio has been demonstrated.
Jensen, A S; Idorn, L; Nørager, B;
Adults with congenital heart disease are a growing population. One of the major challenges in the care of these patients is to prevent thromboembolic episodes. Despite relative young age and no typical cardiovascular risk factors, this cohort has a high prevalence of thrombotic events. It is....... Furthermore, there is a lack of scientific evidence regarding how to prevent thromboembolic events with anticoagulation in adults with congenital heart disease. The aim of this paper is to review the current literature pertaining to anticoagulation in adults with congenital heart disease and hence enable...... difficult to use treatment algorithms from the general adult population with acquired heart disease in this heterogeneous population due to special conditions such as myocardial scarring after previous surgery, atypical atrial flutter, prothrombotic conditions and the presence of interatrial shunts...
Court, E L
The pathogenesis of the lupus anticoagulant (LA) has been the focus of much research over the past decade, and a plethora of laboratory tests have been developed to detect it. This essay reviews the nature of LA and its pathogenesis, and a number of approaches employed in its diagnosis. These range from well established tests such as the kaolin clotting time (KCT), activated partial thromboplastin time (APTT) and tissue thromboplastin inhibition test (TTI), to the 'newer' tests such as the dilute Russell's viper venom time (DRVVT) and more recent snake venom tests such as the textarin/ecarin ratio and Taipan snake venom time (TSVT). The criteria for diagnosis are discussed, including pre-analytical variables such as sample preparation, and the effects of therapeutic anticoagulants used to treat thrombotic manifestations of the syndrome or an underlying disease process. PMID:9624740
Moreno Villar, A; Nacle López, I; Barbero Hernández, M J; Lizan Tudela, L
In an attempt to minimize the economic impact due to the incorporation of innovative drugs, health authorities have promoted and supported the evaluation and market positioning of drugs, as equivalent therapeutic alternatives. This issue has recently gained importance, possibly due to the current economic crisis. The equivalent therapeutic alternatives are justified by the need to compete on price, and by the authorities recommendation to establish therapeutic equivalence, price and financing of medicinal products at the same time. The establishment of the new oral anticoagulants and the equivalent therapeutic alternatives is a problematic issue if it is based on the absence of direct comparisons between different drugs and the questionable methodology used in the current indirect comparisons. Currently, it is difficult to determine when a new oral anticoagulant is more recommendable than others, but efforts are being made in order to propose alternatives for the decision based on patient characteristics. PMID:26146035
Full Text Available Fucan is a term used to denote a family of sulfated L-fucose-rich polysaccharides which are present in the extracellular matrix of brown seaweed and in the egg jelly coat of sea urchins. Plant fucans have several biological activities, including anticoagulant and antithrombotic, related to the structural and chemical composition of polysaccharides. We have extracted sulfated polysaccharides from the brown seaweed Dictyota menstrualis by proteolytic digestion, followed by separation into 5 fractions by sequential acetone precipitation. Gel electrophoresis using 0.05 M 1,3-diaminopropane-acetate buffer, pH 9.0, stained with 0.1% toluidine blue, showed the presence of sulfated polysaccharides in all fractions. The chemical analyses demonstrated that all fractions are composed mainly of fucose, xylose, galactose, uronic acid, and sulfate. The anticoagulant activity of these heterofucans was determined by activated partial thromboplastin time (APTT using citrate normal human plasma. Only the fucans F1.0v and F1.5v showed anticoagulant activity. To prolong the coagulation time to double the baseline value in the APTT, the required concentration of fucan F1.0v (20 µg/ml was only 4.88-fold higher than that of the low molecular weight heparin Clexane® (4.1 µg/ml, whereas 80 µg/ml fucan 1.5 was needed to obtain the same effect. For both fucans this effect was abolished by desulfation. These polymers are composed of fucose, xylose, uronic acid, galactose, and sulfate at molar ratios of 1.0:0.8:0.7:0.8:0.4 and 1.0:0.3:0.4:1.5:1.3, respectively. This is the fist report indicating the presence of a heterofucan with higher anticoagulant activity from brown seaweed.
Kaczorowska, Beata; Pawełczyk, Małgorzata; Przybyła, Monika
Brain stroke is a grave society problem. About 20% ischemic strokes are cardiac related problems. Atrial fibrillation (AF) is the most common cause of ischemic strokes. Decision to deploy anticoagulant treatment with AF patient depends on bleeding and thrombo-embolic risk which summerise scale CHA2DS2VASc and HAS-BLED. Past recent years in AF treatment anticoagulants from the group of vitamin K antagonist were used. At present in brain stroke prevention and systemic emboilment, new oral anticoagulants (NOA) which weren't worst than vitamin K antagonists, and they are recomendet in most cases of AF unrelated with heart valve defets. Useing NOA causes lower risk of bleeding, including intracranial heamorrhage. It is believed that this is related to the selective inhibition of specific coagulation factors, and respect other hemostatic mechanisms. Results from clinical studies NOA are encouraging, but still lacks clear answers regarding, among other things: long-term safety of treatment and economically viable in everyday clinical practice. In addition, to date there is no specific antidote for this group of drugs. PMID:27234866
Munson, C F; Reid, A J
Novel oral anticoagulants (NOACs) have emerged as a good alternative to warfarin in the prevention of stroke for patients with atrial fibrillation. NOAC use is increasing rapidly; therefore, greater understanding of their use in the perioperative period is important for optimal care. Studies and reviews that reported on the use of NOACs were identified, with particular focus on the perioperative period. PubMed was searched for relevant articles published between January 2000 and August 2015. The inevitable rise in the use of NOACs such as rivaroxaban (Xarelto™), apixaban (Eliquis™), edoxaban (Lixiana™) and dabigatran (Pradaxa™) may present a simplified approach to perioperative anticoagulant management due to fewer drug interactions, rapidity of onset of action and relatively short half-lives. Coagulation status, however, cannot reliably be monitored and no antidotes are currently available. When planning for discontinuation of NOACs, special consideration of renal function is required. Advice regarding the management of bleeding complications is provided for consideration in emergency surgery. In extreme circumstances, haemodialysis may be considered for bleeding with the use of dabigatran. NOACs will increasingly affect operative planning in plastic surgery. In order to reduce the incidence of complications associated with anticoagulation, the management of NOACs in the perioperative period requires knowledge of the time of last dose, renal function and the bleeding risk of the planned procedure. Consideration of these factors will allow appropriate interpretation of the current guidelines. PMID:27013144
Olesen, Jonas Bjerring; Sørensen, Rikke; Hansen, Morten Lock;
AIMS: Non-vitamin K antagonist oral anticoagulation (NOAC) agents have been approved for stroke prophylaxis in atrial fibrillation (AF). We investigated 'real-world' information on how these drugs are being adopted. METHODS AND RESULTS: Using Danish nationwide administrative registers, we...... the drug came on market. By October, 2013, 40% were being started on warfarin and dabigatran, respectively, and another 20% were started on either rivaroxaban or apixaban. Rivaroxaban and apixaban users generally had a higher predicted risk of stroke and bleeding compared with warfarin and dabigatran users....... Older age, female gender, and prior stroke were some of the factors associated with NOAC use vs. warfarin, whereas chronic kidney disease, myocardial infarction, and heart failure showed the opposite association. CONCLUSION: Among oral anticoagulation-naïve AF patients initiated on oral anticoagulation...
Bouwmeester, Carla; Chim, Christine
Pharmacists are at the forefront when caring for patients requiring anticoagulation resulting from chronic conditions, complex medications therapy, or at risk for drug interactions. As a consequence, there is a greater need for pharmacist-managed anticoagulation clinics in the community setting. This article will review special considerations for oral anticoagulant therapy in the elderly, collaborative therapy management, establishment of policies and procedures, documentation of patient visits, patient counseling, and barriers to successful anticoagulation management. It will also discuss evidence-based guidelines for the use of oral anticoagulants and compare the agents currently approved by the Food and Drug Administration. Finally, barriers to anticoagulation management will be examined, including issues with adherence and communication with patients and health care providers. PMID:23649677
Harper, Paul; Harper, Joe; Hill, Claire
Objective To evaluate the effectiveness of a computerised self-adjusting anticoagulant algorithm to predict appropriate warfarin dosing and to assess its use in clinical practice. Design A 3-year audit of anticoagulant control in patients managed by doctors and pharmacists using computer decision support and an evaluation of the impact of dose adjustments made by the users. Participants 3660 patients on oral anticoagulants; one-third of patients managed by doctors and two-thirds by pharmacists. Setting Anticoagulant supervision in primary care and pharmacies at 60 sites in New Zealand. Main outcome measures The time in the therapeutic range (TTR), the outcome of adherence to the computer dosing algorithm, the percentage of time the clinicians over-ride the algorithm and the impact of their intervention on anticoagulant control. Results A TTR of 72.9% was achieved for all patients. The TTR was significantly better in patients managed by pharmacists than doctors (75.1% versus 67.4%, ppharmacists. Conclusions The clinicians predominantly change the dose when the INR is below the therapeutic range. The changes are not necessary to correct for inaccuracies in the algorithm. The most likely explanation is the clinician's belief that their own dose adjustment would achieve better control; however, in practice, their changes tend to underdose patients. The doctors achieved poorer control than the pharmacists; this is in part due to the action of the doctors over-riding the algorithm. Our results imply that clinicians could achieve better anticoagulant control if they more closely followed the computer algorithm. PMID:25183709
Full Text Available Abstract Background Verbascum thapsus is used in tribal medicine as an antispasmodic, anti-tubercular agent and wormicide. In this study, we investigated the antispasmodic and anthelmintic activities of crude aqueous methanolic extract of the plant. Methods V. thapsus extracts were tested against roundworms (Ascaridia galli and tapeworms (Raillietina spiralis. Each species of worm was placed into a negative control group, an albendazole treatment group, or a V. thapsus treatment group, and the time taken for paralysis and death was determined. In addition, relaxation activity tests were performed on sections of rabbit's jejunum. Plant extracts were tested on KCl-induced contractions and the relaxation activities were quantified against atropine. V. thapsus calcium chloride curves were constructed to investigate the mode of action of the plant extracts. Results We detected flavonoids, saponins, tannins, terpenoids, glycosides, carbohydrates, proteins, fats and fixed oils in V. thapsus. For both species of worm, paralysis occurred fastest at the highest concentration of extract. The relative index values for paralysis in A. galli were 4.58, 3.41 and 2.08, at concentrations of 10, 20 and 40 mg/ml of plant extract, respectively. The relative index for death in A. galli suggested that V. thapsus extract is wormicidal at high concentration. Similarly, the relative indexes for paralysis and death in R. spiralis suggested that the extract is a more potent wormicidal agent than albendazole. The mean EC50 relaxation activity values for spontaneous and KCl induced contractions were 7.5 ± 1.4 mg/ml (6.57-8.01, n = 6 and 7.9 ± 0.41 mg/ml (7.44-8.46, n = 6, respectively. The relaxation activity of the extract was 11.42 ± 2, 17.0 ± 3, 28.5 ± 4, and 128.0 ± 7% of the maximum observed for atropine at corresponding concentrations. The calcium chloride curves showed that V. thapsus extracts (3 mg/ml, had a mean EC50 (log molar [calcium] value of -1.9 ± 0
Full Text Available Helia Robert-Ebadi, Grégoire Le Gal, Marc RighiniDivision of Angiology and Hemostasis (HRE, MR, Department of Internal Medicine, Geneva University Hospital and Faculty of Medicine, Geneva, Switzerland, and Department of Internal Medicine and Chest Diseases, EA 3878 (GETBO, Brest University Hospital, Brest, France (GLGAbstract: Elderly people represent a patient population at high thromboembolic risk, but also at high hemorrhagic risk. There is a general tendency among physicians to underuse anticoagulants in the elderly, probably both because of underestimation of thromboembolic risk and overestimation of bleeding risk. The main indications for anticoagulation are venous thromboembolism (VTE prophylaxis in medical and surgical settings, VTE treatment, atrial fibrillation (AF and valvular heart disease. Available anticoagulants for VTE prophylaxis and initial treatment of VTE are low molecular weight heparins (LMWH, unfractionated heparin (UFH or synthetic anti-factor Xa pentasaccharide fondaparinux. For long-term anticoagulation vitamin K antagonists (VKA are the first choice and only available oral anticoagulants nowadays. Assessing the benefit-risk ratio of anticoagulation is one of the most challenging issues in the individual elderly patient, patients at highest hemorrhagic risk often being those who would have the greatest benefit from anticoagulants. Some specific considerations are of utmost importance when using anticoagulants in the elderly to maximize safety of these treatments, including decreased renal function, co-morbidities and risk of falls, altered pharmacodynamics of anticoagulants especially VKAs, association with antiplatelet agents, patient education. Newer anticoagulants that are currently under study could simplify the management and increase the safety of anticoagulation in the future.Keywords: anticoagulation, elderly patients, venous thromboembolism, hemorrhagic risk, atrial fibrillation, thrombin inhibitors, factor Xa
Cecilia Becattini, Alessandra Lignani, Giancarlo AgnelliInternal and Cardiovascular Medicine and Stroke Unit, University of Perugia, ItalyAbstract: Anticoagulant drugs have an essential role in the prevention and treatment of thromboembolic diseases. Currently available anticoagulants substantially reduce the incidence of thromboembolic events in a number of clinical conditions. However, these agents have limitations that strengthen the case for the development of new anticoagulants. An ideal...
Robinson, Austin A.; Ikuta, Kevin; Soverow, Jonathan
Few prospective studies support the use of anticoagulation during the acute phase of ischemic stroke, though observational data suggest a role in certain populations. Depending on the mechanism of stroke, systemic anticoagulation may prevent recurrent cerebral infarction, but concomitantly carries a risk of hemorrhagic transformation. In this article, we describe a case where anticoagulation shows promise for ischemic stroke and review the evidence that has discredited its use in some circums...
Hookworms of the genus Ancylostoma secrete an anticoagulant that both inhibits the clotting of human plasma and promotes fibrin clot dissolution. This anticoagulant activity is attributable to a 36,000 dalton proteolytic enzyme. The protease can degrade fibrinogen into five smaller polypeptides that intrinsically have anticoagulating properties, covert plasminogen to a mini-plasminogen-like molecule, and hydrolyze a synthetic peptide substrate with specificity for elastolytic enzymes. It is h...
Rybak, Iwona; Ehle, Michael; Buckley, Leo; Fanikos, John
Dabigatran, rivaroxaban, and apixaban are novel oral anticoagulants that offer major advantages over existing agents. The onset of the anticoagulant effect of these agents is rapid. Each agent has a predictable anticoagulant response that eliminates the need for monitoring. Clinical trials have been completed with all three agents in the prevention and treatment of the three leading causes of cardiovascular death: myocardial infarction, stroke, and venous thromboembolism (VTE). Novel agents h...
Witt, Daniel M
The Clinical Pharmacy Anticoagulation Service (CPAS) at Kaiser Permanente Colorado grew from a single pharmacist assisting a single physician to a comprehensive service staffed by over 20 employees. CPAS provides care for over 7200 patients with each CPAS pharmacist managing all aspects of anticoagulation therapy for 150 to 500 patients. Unique aspects of CPAS include its centralized organization structure, the use of telepharmacy, collaboration drug therapy management agreement with referring physicians and a robust research agenda. Results of various CPAS research projects have been published in the peer-reviewed medical literature. PMID:18804262
Park, Joon-Sung; Kim, Gheun-Ho; Kang, Chong Myung; Lee, Chang Hwa
Background/Aims Short hemofilter survival and anticoagulation-related life-threatening complications are major problems in systemic anticoagulation with heparin (SAH) for continuous renal replacement therapy (CRRT). The present study examined if regional anticoagulation with citrate (RAC) using commercially available solutions can overcome the associated problems of SAH to produce economical benefits. Methods Forty-six patients were assigned to receive SAH or RAC. We assessed the coagulation ...
Full Text Available The development of anthelmintic resistance and the high cost of conventional anthelmintic drugs led to the evaluation of medicinal plants as an alternative source of anthelmintics. In the current study, in-vitro experiments were conducted to determine the possible anthelmintic effects of crude aqueous and hydroalcoholic extracts of the leaves of Chenopodium ambrosioides, Lawsonia inermis and seeds of Jatropha curcas, on eggs and adult Haemonchus contortus. Both extracts of C. ambrosioides and J. curcas inhibited the hatching of eggs at a concentration less than or equal to 2mg/ml, while the effect of L. inermis was not dose-dependent and did not inhibit the hatching of eggs of H. contortus, significantly, at all tested concentrations. Based on their ED 50 , the two most potent extracts using egg hatch assay were the hydroalcoholic extract of C. ambrosioides (0.09mg/ml and the aqueous extract of J. curcas (0.1mg/ml in a decreasing order of potency. With regard to the effect of extracts on the survival of adult parasites, extracts from C. ambrosioides have shown a moderate effect, while J. curcas and L. inermis have shown no statistically significant effect on the survival of adult parasites at the concentrations tested, and the few mortality cases recorded were not dose-dependent ( P < 0.05. The overall findings of the present study have shown that C. ambrosioides and J. curcas contain possible anthelmintic compounds and further evaluation of these plants should be carried out.
Benz, G W; Ernst, J V
Anthelmintic activities of albendazole were evaluated in a controlled experiment. Forty calves experimentally infected with gastrointestinal nematodes were allotted to 4 groups. Calves in group 1 were used as nonmedicated controls; calves in groups 2, 3, and 4 were given (by oral route) a suspension containing albendazole at dose concentrations of 2.5, 5.0, and 7.5 mg/kg of body weight on the 35th day after administration of infective nematode larvae. In groups 2, 3, and 4 calves, average overall reductions (based on geometric means) were 77.1, 93.6, and 98.1%, respectively. These reductions were highly significant (P less than 0.01) in calves given doses of 5.0 and 7.5 mg/kg, and were significant (P less than 0.05) in calves given the 2.5-mg/kg dose. Ostertagia ostertagi, Trichostrongylus axei, Cooperia onchophora, Cooperia punctata, and Oesophagostomum radiatum removals at the 5.0- and 7.5-mg/kg dose levels were all highly significant (P less than 0.01); whereas, removals of Haemonchus contortus were not significant, even at the 7.5-mg/kg dose level. PMID:921039
Bhabani Shankar Nayak
Full Text Available Background: The plant Gmelina arborea has been traditionally used in India for several medicinal purposes like anthelmintic, diuretic, antibacterial, antioxidant and antidiabetic. Aim: The present study is an attempt to explore the antibacterial, antioxidant and antidiabetic activities of different extracts of fruits of plant G. arborea using ethanol, ethyl acetate, n-butanol and petroleum ether as solvents. Materials and Methods: A single dose (1000 =g/ml of extract was evaluated for their antibacterial activities on human pathogens like Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. In-vitro antioxidant activity of G. arborea fruits was determined by 1, 1-diphenyl-2-picrylhydrazil (DPPH free radical scavenging and reducing power assay. Ascorbic acid was used as standard and positive control for both the analyses. The antidiabetic activity of above extracts was evaluated in alloxan induced diabetic model of Wistar rats. Statistical Analysis: All data are verified for statistically significant by using one way ANOVA at 1% level of significance (P < 0.01. Results: Only ethanol extract showed significant antibacterial activity against all pathogens and the activities were compared with the standard drug, streptomycin. The n-butanol extract did not show antibacterial activity against any pathogens, whereas ethyl acetate and petroleum ether extracts showed inhibitory action against P. aeruginosa. The extracts showed significant antioxidant activities in a dose dependent manner. The ethanol extract showed good antioxidant activity when compared to the other three extracts. All the extracts were able to reduce sugar level in blood. Ethanol extract was found to have good antidiabetic activity in comparison to other extracts. Conclusion: It can be concluded that the extracts of G. arborea possess antibacterial, antioxidant and antidiabetic activities.
蒋晨阳; 赵莉莉; 王建安; 单江; MOHAMMODBalgaith
Objective: To investigate if intra-aortic balloon pump(IABP) is contraindicated without anticoag-ulation therapy. Methods: Some 153 IABP patients in the King Abdulaziz Cardiac Center(KSA) were random-ly assigned into two groups. Anticoagulation group( Group A) consisted of 71 patients who were given heparin intravenously with target aPTT 50 - 70 seconds. Non-anticoagulation group( Group B) consisted of 82 patients without intravenous heparin during balloon pumping. Hematological parameters including platelet count, D-dimer, Plasminogen activator inhibitor-1 (PAI-1) and fibrinogen degradation products(FDP) were checked respectively at the point of baseline, 24 hours, 48 hours and 24 hours post IABP counterpulsation. Clot deposits on balloon surface, vascular complications from IABP including bleeding and limb ischemia were recorded.Results: Platelet count and PAI-1 level decreased at 24 hours and 48 hours in both groups ( P 0.05) . Three patients in Group A and 2 patients in Group B developed minor limb ischemia( P > 0.05). No major limb ischemia in either group. Two patients in Group A suffered major bleeding and required blood transfusion or surgical intervention, whereas no patient had major bleeding in Group B. Eight patients had minor bleeding in Group A, but only 2 patients in Group B ( P <0.05). No clot deposit developed on IABP surface in either group. Conclusion: IABP is safe without routine anticoagulation therapy. Selecting appropriate artery approach and early detection intervention are key methods for preventing complications.
JIANG Chen-yang(蒋晨阳); ZHAO Li-li(赵莉莉); WANG Jian-an(王建安); SAN Jiang(单江); MOHAMMOD Balgaith
Objective: To investigate if intra-aortic balloon pump(IABP) is contraindicated without anticoagulation therapy. Methods: Some 153 IABP patients in the King Abdulaziz Cardiac Center(KSA) were randomly assigned into two groups. Anticoagulation group(Group A) consisted of 71 patients who were given heparin intravenously with target aPTT 50-70 seconds. Non-anticoagulation group(Group B) consisted of 82 patients without intravenous heparin during balloon pumping. Hematological parameters including platelet count, D-dimer, Plasminogen activator inhibitor-1(PAI-1) and fibrinogen degradation products(FDP) were checked respectively at the point of baseline, 24 hours, 48 hours and 24 hours post IABP counterpulsation. Clot deposits on balloon surface, vascular complications from IABP including bleeding and limb ischemia were recorded. Results: Platelet count and PAI-1 level decreased at 24 hours and 48 hours in both groups (P0.05). Three patients in Group A and 2 patients in Group B developed minor limb ischemia(P>0.05). No major limb ischemia in either group. Two patients in Group A suffered major bleeding and required blood transfusion or surgical intervention, whereas no patient had major bleeding in Group B. Eight patients had minor bleeding in Group A, but only 2 patients in Group B(P<0.05). No clot deposit developed on IABP surface in either group. Conclusion: IABP is safe without routine anticoagulation therapy. Selecting appropriate artery approach and early detection intervention are key methods for preventing complications.
Full Text Available Anticoagulation Clinics (ACs are services specialized in management of patients on anticoagulant treatment. At present, ACs manage patients chiefly on antivitamin K antagonists (AVKs, but patient population has already changed in the last few years, because of an increase of treatments with other anticoagulant drugs, which require different management systems. The strong increase in the number of patients at AC, mainly on long-term treatment, has determined the development of web management, through telemedicine systems, improving the quality of life and maintaining the same clinical quality levels. New oral anticoagulants (NOAs have shown to be as effective as AVK antagonists in stroke prevention in atrial fibrillation and for treatment of venous thromboembolism in addition to VTE prophylaxis in orthopaedic surgery, when administered at a fixed dose, but patient adherence and compliance are crucial for good quality treatment. At present, lacking data from the real world, an oversimplification of treatment with NOAs could cause unjustified risks for patients and also a possible future underuse of good drugs. For these reasons the vigilance must be high and ACs can have a crucial role in defining which is the best management for NOA patients and how to do it, as it happened for AVKs.
Markussen, Mette D.; Heiberg, Ann-Charlotte; Nielsen, Robert;
Norway rats, Rattus norvegicus, Denmark, anticoagulant rodenticide resistance, vitamin K requirement......Norway rats, Rattus norvegicus, Denmark, anticoagulant rodenticide resistance, vitamin K requirement...
Salvador, Juan Pablo; Marco, María Pilar
[EN] The present invention relates to the design of haptens that are structurally related to coumarin oral anticoagulant compounds (COAC), to be used for the production of specific antibodies against said type of substances and the subsequent use thereof for the development of diagnosis tools for use in laboratories or in point-of-care (PoC) devices. In particular, the produced antibodies have been used to develop a diagnosis tool that enables the plasma levels of COAC to be quantified in pat...
Drozd, N N; Tolstenkov, A S; Makarov, V A; Miphtakhova, N T; Voyushina, T L; Sergeev, M E
Original synthetic peptide derivatives exhibit anticoagulant activity in vitro and in vivo. They delayed fibrin clot formation from human blood plasma in tests for the intrinsic coagulation pathway (activated partial thromboplastin time) and final stage of plasma coagulation (thrombin time) and inhibited amidolytic activity of thrombin. We determined the minimum effective dose of the most active compound providing a 2-fold lengthening of blood clotting time (activated partial thromboplastin time test and thrombin time test), which persisted for 2-3 h. PMID:19024001
Borst, G H A; Counotte, G H M
Second-generation anticoagulant rodenticides can give rise to unexpected casualties in nontarget species in zoos. The first two offspring of a pair of turkey vultures (Cathartes aura) died of brodifacoum toxicosis. The adult birds fed rodenticide-killed mice to their offspring. There are previous case reports of small carnivorous birds (Dacelo novae-guinae and Tockus deckeni) killed eating poisoned (difenacoum and brodifacoum) mice. Even a granivorous species (Rollulus roulroul) died, probably by contamination of its food by cockroaches that transported the rodenticide. PMID:12216801
Mansur, F; Luoga, W; Buttle, D J; Duce, I R; Lowe, A; Behnke, J M
Little is known about the efficacy of cysteine proteinases (CP) as anthelmintics for cestode infections in vivo. Hymenolepis microstoma is a natural parasite of house mice, and provides a convenient model system for the assessment of novel drugs for anthelmintic activity against cestodes. The experiments described in this paper indicate that treatment of H. microstoma infections in mice with the supernatant of papaya latex (PLS), containing active cysteine proteinases, is only minimally efficacious. The statistically significant effects seen on worm burden and biomass showed little evidence of dose dependency, were temporary and the role of cysteine proteinases as the active principles in PLS was not confirmed by specific inhibition with E-64. Worm fecundity was not affected by treatment at the doses used. We conclude also that this in vivo host-parasite system is not sensitive enough to be used reliably for the detection of cestocidal activity of compounds being screened as potential, novel anthelmintics. PMID:25226116
Andrew R Williams
Full Text Available Ascaris suum is one of the most prevalent nematode parasites in pigs and causes significant economic losses, and also serves as a good model for A. lumbricoides, the large roundworm of humans that is ubiquitous in developing countries and causes malnutrition, stunted growth and compromises immunity to other pathogens. New treatment options for Ascaris infections are urgently needed, to reduce reliance on the limited number of synthetic anthelmintic drugs. In areas where Ascaris infections are common, ethno-pharmacological practices such as treatment with natural plant extracts are still widely employed. However, scientific validation of these practices and identification of the active compounds are lacking, although observed effects are often ascribed to plant secondary metabolites such as tannins. Here, we extracted, purified and characterised a wide range of condensed tannins from diverse plant sources and investigated anthelmintic effects against A. suum in vitro. We show that condensed tannins can have potent, direct anthelmintic effects against A. suum, as evidenced by reduced migratory ability of newly hatched third-stage larvae and reduced motility and survival of fourth-stage larvae recovered from pigs. Transmission electron microscopy showed that CT caused significant damage to the cuticle and digestive tissues of the larvae. Furthermore, we provide evidence that the strength of the anthelmintic effect is related to the polymer size of the tannin molecule. Moreover, the identity of the monomeric structural units of tannin polymers may also have an influence as gallocatechin and epigallocatechin monomers exerted significant anthelmintic activity whereas catechin and epicatechin monomers did not. Therefore, our results clearly document direct anthelmintic effects of condensed tannins against Ascaris and encourage further in vivo investigation to determine optimal strategies for the use of these plant compounds for the prevention and
Full Text Available Cecilia Becattini, Alessandra Lignani, Giancarlo AgnelliInternal and Cardiovascular Medicine and Stroke Unit, University of Perugia, ItalyAbstract: Anticoagulant drugs have an essential role in the prevention and treatment of thromboembolic diseases. Currently available anticoagulants substantially reduce the incidence of thromboembolic events in a number of clinical conditions. However, these agents have limitations that strengthen the case for the development of new anticoagulants. An ideal anticoagulant should be at least as effective as those currently in use, as well as safe, simple to use, and widely applicable. The majority of new anticoagulants currently under investigation are small molecules with a selective and direct anti-Xa or antithrombin action, allowing oral administration in fixed doses. These new agents are in different phases of clinical development. The anti-Xa agent rivaroxaban and the antithrombin agent dabigatran are already available for the prophylaxis of venous thromboembolism in some countries. Apixaban is in an advanced phase of clinical development and several anti-Xa agents are currently approaching phase III clinical trials. Promising results in terms of efficacy and safety profiles have been obtained with these agents in different clinical conditions. Differences in pharmacokinetics and pharmacodynamics could offer the potential for individualized anticoagulant therapies in the near future.Keywords: anticoagulant therapy, antithrombotic therapy, anticoagulants, direct thrombin inhibitors, factor Xa inhibitors
Atrial fibrillation (AF) increases the risk of stroke.New anticoagulation agents have recently provided alternative and promising approaches.This paper reviews the current state of anticoagulation therapy in AF patients,focusing on various clinical scenarios and on comparisons,where possible,between western and eastern populations.
Rasmussen, Rune Skovgaard; Corell, Pernille; Madsen, Poul;
UNLABELLED: BACKGROUND: Computer-assistance and self-monitoring lower the cost and may improve the quality of anticoagulation therapy. The main purpose of this clinical investigation was to use computer-assisted oral anticoagulant therapy to improve the time to reach and the time spent within the...
Jeremiah D Farelli
Full Text Available Parasitic nematodes are responsible for devastating illnesses that plague many of the world's poorest populations indigenous to the tropical areas of developing nations. Among these diseases is lymphatic filariasis, a major cause of permanent and long-term disability. Proteins essential to nematodes that do not have mammalian counterparts represent targets for therapeutic inhibitor discovery. One promising target is trehalose-6-phosphate phosphatase (T6PP from Brugia malayi. In the model nematode Caenorhabditis elegans, T6PP is essential for survival due to the toxic effect(s of the accumulation of trehalose 6-phosphate. T6PP has also been shown to be essential in Mycobacterium tuberculosis. We determined the X-ray crystal structure of T6PP from B. malayi. The protein structure revealed a stabilizing N-terminal MIT-like domain and a catalytic C-terminal C2B-type HAD phosphatase fold. Structure-guided mutagenesis, combined with kinetic analyses using a designed competitive inhibitor, trehalose 6-sulfate, identified five residues important for binding and catalysis. This structure-function analysis along with computational mapping provided the basis for the proposed model of the T6PP-trehalose 6-phosphate complex. The model indicates a substrate-binding mode wherein shape complementarity and van der Waals interactions drive recognition. The mode of binding is in sharp contrast to the homolog sucrose-6-phosphate phosphatase where extensive hydrogen-bond interactions are made to the substrate. Together these results suggest that high-affinity inhibitors will be bi-dentate, taking advantage of substrate-like binding to the phosphoryl-binding pocket while simultaneously utilizing non-native binding to the trehalose pocket. The conservation of the key residues that enforce the shape of the substrate pocket in T6PP enzymes suggest that development of broad-range anthelmintic and antibacterial therapeutics employing this platform may be possible.
García-Rodriguez, J J; Torrado, J; Bolás, F
The bioavailability and anthelmintic activity of albendazole-cyclodextrin complexes (ABZ-CDC) compared to albendazole suspensions in carboxymethylcellulose (ABZ-CMC) was assessed in a mouse model for Trichinella infections. Swiss CD-1 mice experimentally infected with T. spiralis were treated with both formulations against enteral (adult worms) and parenteral (migrating and encysted larvae). Oral bioavailability was assessed in age matched mice treated with 50 mg/kg of both formulations. The anthelmintic effects and plasma concentration of the active metabolite albendazole-sulphoxide (ABZSO) enantiomer (-) were significantly increased following administration of ABZ-CDC in relation to ABZ-CMC. PMID:11484352
Full Text Available The bioavailability and anthelmintic activity of albendazole-cyclodextrin complexes (ABZ-CDC compared to albendazole suspensions in carboxymethylcellulose (ABZ-CMC was assessed in a mouse model for Trichinella infections. Swiss CD-1 mice experimentally infected with T. spiralis were treated with both formulations against enteral (adult worms and parenteral (migrating and encysted larvae. Oral bioavailability was assessed in age matched mice treated with 50 mg/kg of both formulations. The anthelmintic effects and plasma concentration of the active metabolite albendazole-sulphoxide (ABZSO enantiomer (– were significantly increased following administration of ABZ-CDC in relation to ABZ-CMC.
Full Text Available Different extracts of Lagenaria siceraria were taken for anthelmintic activity against Indian earthworm Pheritima posthuma. Two concentrations (50 and 100 mg/ml of various extracts were tested and results were expressed in terms of time for paralysis and time for death of worms. Albendazole (20 mg/ml was used as reference standard and carboxy methyl cellulose (0.5% as a control group. Dose dependent activity was observed in the plant extracts but methanolic extract exhibited more activity as compared to others. The anthelmintic activity of Lagenaria sicerarialeaves extract has therefore been demonstrated for the first time.
McMahon, Sean R; Brummel-Ziedins, Kathleen; Schneider, David J
Despite advances in interventional and pharmacologic therapy, survivors of myocardial infarction remain at an increased risk of subsequent cardiovascular events. Initial pharmacological management includes both platelet inhibition and parenteral anticoagulation, whereas long-term pharmacological therapy relies on antiplatelet therapy for prevention of thrombotic complications. Biomarkers showing ongoing thrombin generation after acute coronary syndromes suggest that anticoagulants may provide additional benefit in reducing cardiovascular events. We review the pharmacokinetics of novel anticoagulants, clinical trial results, the role of monitoring, and future directions for the use of novel oral anticoagulants in the treatment of coronary artery disease. Clinical trials have shown that long-term use of oral anticoagulants decreases the risk of cardiovascular events, but they do so at a cost of an increased risk of bleeding. Future studies will need to identify optimal treatment combinations for selected patients and conditions that address both the appropriate combination of therapy and the appropriate dosage of each agent when used in combination. PMID:27228186
Weinstock, Matthew J; Uhlmann, Erik J; Zwicker, Jeffrey I
Both venous thromboembolism and intracranial metastases are common complications in the setting of primary brain tumors and metastatic malignancies. Anticoagulation is indicated in the presence of cancer-associated thrombosis in order to limit the risk of pulmonary embolism; however, there is reluctance to initiate anticoagulation in the setting of intracranial metastatic disease due to potential for intracranial hemorrhage. Recent evidence suggests that therapeutic anticoagulation can be safely administered in the setting of metastatic brain tumors. This review examines the current understanding of the pathophysiology of intracranial hemorrhage in malignancy, describes the incidence of intracranial hemorrhage in the setting of brain tumors with therapeutic anticoagulation, and outlines management strategies relevant to the treatment of intracranial hemorrhage in the setting of anticoagulation. PMID:27067980
Caio Julio Cesar dos Santos Fernandes
Full Text Available Worldwide, venous thromboembolism (VTE is among the leading causes of death from cardiovascular disease, surpassed only by acute myocardial infarction and stroke. The spectrum of VTE presentations ranges, by degree of severity, from deep vein thrombosis to acute pulmonary thromboembolism. Treatment is based on full anticoagulation of the patients. For many decades, it has been known that anticoagulation directly affects the mortality associated with VTE. Until the beginning of this century, anticoagulant therapy was based on the use of unfractionated or low-molecular-weight heparin and vitamin K antagonists, warfarin in particular. Over the past decades, new classes of anticoagulants have been developed, such as factor Xa inhibitors and direct thrombin inhibitors, which significantly changed the therapeutic arsenal against VTE, due to their efficacy and safety when compared with the conventional treatment. The focus of this review was on evaluating the role of these new anticoagulants in this clinical context.
Anticoagulant therapy is the cornerstone of treatment of venous thromboembolism (VTE). The treatment needs rapid initial anticoagulaton to minimize the risk of thrombus extension and fata pulmonary embolism, followed by an extended anticoagulation, aimed at preventing recurrent VTE. Till very recently, immediate anticoagulation can only be achieved with parenteral agents, such as heparin, low-molecular-weight heparin, or fondaparinux. Extended treatment usually involves the administration of vitamin K antagonists, such as warfarin. Emerging direct oral anticoagulants have the potential to streamline VTE treatment. These agents include oral anticoagulants that target thrombin or factor Xa. This article reviews the characteristics of these agents, describes the results of clinical trials in venous thromboembolic disease and outlines their strengths and weakness. PMID:24167902
Full Text Available Traditional anticoagulants, such as low molecular weight heparin, unfractionated heparin, fondaparinux and vitamin K antagonists, have been the mainstay of treatment of venous thromboembolism (VTE in the clinical hospital setting and after discharge. These anticoagulants are effective, but are associated with some limitations that may lead to their underuse in many settings. Based on the results of large, randomized clinical trials, new oral anticoagulants have been validated for the treatment of acute deep vein thrombosis and pulmonary embolism, and for the prevention of recurrent VTE. These drugs represent a landmark shift in anticoagulation care and may overcome some of the limitations of traditional agents, with the potential of improving adherence to anticoagulation therapy.
De Lange, J J; Van Kleef, J W; Van Everdingen, J J E
In a patient with a coagulation disorder, the administration of a local anaesthetic by means of a needle or via the insertion of a catheter into the epidural space or spinal cavity may lead to bleeding and haematoma formation, with a danger of pressure on the spinal cord or nerve roots. Employing the method of the Dutch Institute for Healthcare (CBO) for the development of practice guidelines, a working group of anaesthesiologists, a haematologist and a hospital chemist have drawn up recommendations for neuraxis blockade in combination with anticoagulant therapy. In patients with a clinically acquired tendency toward increased bleeding, the management is highly dependent on the cause of the bleeding tendency. If the patient uses acetylsalicylic acid or clopidogrel, the medication must be withdrawn at least 10 days before neuraxis blockade is started. Therapy with glycoprotein-IIb/IIIa-receptor antagonists is an absolute contra-indication for neuraxis blockade. In patients who are using coumarin derivatives, neuraxis blockade results in an increased risk of a neuraxial haematoma. The coumarin derivative should then be withdrawn and replaced by a different form of anticoagulation. The use of low-molecular-weight heparin at the usual prophylactic dosage is not a contra-indication for neuraxis blockade and the risk of a neuraxial haematoma following neuraxis blockade is also not increased significantly by the subcutaneous administration of unfractionated heparin. PMID:15366721
Ciurus, Tomasz; Sobczak, Sebastian; Cichocka-Radwan, Anna
Oral direct inhibitors of thrombin and activated factor Xa are approved as new anticoagulant drugs. In contrast to vitamin K antagonists (VKA) and heparins, the new agents have single targets in the coagulation cascade and more predictable pharmacokinetics, but they lack validated and available antidotes. Unlike VKA, they do not require routine monitoring of coagulation. However, the measurement of their pharmacologic effects might be of value in selected patients. They interfere with the routine coagulation tests, which should be interpreted with caution. Specific tests exist and can be used in case of emergencies. Adequate supportive care and temporary removal of all antithrombotic agents constitute the basis for management of serious bleeding complications. The administration of coagulation factors, such as fresh frozen plasma, prothrombin complex concentrates or recombinant activated FVII, can benefit in life-threatening bleeding or emergency surgery. Specific antidotes for non-vitamin K oral anticoagulants are in clinical development. This review aims at answering in a brief and simplified manner some clinical questions. PMID:26336492
Full Text Available Plants are rich source of antibacterial agents because they produce wide array of bioactive molecules, most of which probably evolved as chemical defense against predation or infection. A major part of the total population in developing countries still uses traditional folk medicine obtained from plant resources With an estimation of WHO that as many as 80% of world population living in rural areas rely on herbal traditional medicines as their primary health care, the study on properties and uses of medicinal plants are getting growing interests. In recent years this interest to evaluate plants possessing antibacterial activity for various diseases is growing. Different solvent extracts (aqueous, alcohol and ethanol of leaves, flower and seed of various plants selected based on an ethnobotanical survey from India were subjected to in vitro antibacterial activity assay against Gram-positive and Gram-negative bacteria employing different diffusion method. Based on local use of common diseases and Ethnobotanical knowledge, an attempt has been made to assess the antibacterial properties of selected medicinal plants viz. Argemone mexicana (Shialkanta, Aster lanceolatus (White panicle, Capparis thonningii and Capparis tomentosa (Woolly caper bush, Cardiospermum halicacabum (Balloonvine, Cassia alata (Herpetic alata, Centaurea sclerolepis, Cinnamomum zeylanicum (Cinnamon, Curcuma longa (Turmeric, Cymbopogon nervatus, Ficus religiosa (Peepal, Indigofera aspalathoides (Ajara, Marrubium vulgare (Horehound, Medicago Spp.(Medick, Burclover, Morus alba (Mulberry, Ocimum sanctum (Tulsi, Origanum marjorana (Marjoram, Oxalis corniculata (Amli, Piper nigrum (Kala mirch, Plectranthus amboinicus (Indian borage, Patharchur, Plumeria acutifolia (Kachuchi, Salvadora persica (Piludi, Salvia repens and Syzygium aromaticum (Clove for potential antibacterial activity against some important bacterial strains, namely Bacillus subtilis, Bacillus cereus, Staphylococcus
Martha L. González-Bárcenas
Full Text Available The development of novel antithrombotic therapy in the past few years and its prescription in patients with cardiovascular and circulatory disease has widened the spectrum of drugs that need to be considered when performing an endoscopic procedure. The balance between the thrombotic risk patients carry due to their medical history and the bleeding risk involved in endoscopic procedures should be thoroughly analyzed by Gastroenterologists. New oral anticoagulants (NOACs impose an additional task. These agents, that specifically target factor IIa or Xa, do not dispose of an anticoagulation monitoring method nor have an antidote to revert their effect, just as with antiplatelet agents. Understanding the fundamental aspects of these drugs provides the necessary knowledge to determine the ideal period the antithrombotic therapy should be interrupted in order to perform the endoscopic procedure, offering maximum safety for patients and optimal results.
Smyser, Timothy J; Johnson, Shylo R; Stallard, Melissa D; McGrew, Ashley K; Page, L Kristen; Crider, Nikki; Ballweber, Lora R; Swihart, Robert K; VerCauteren, Kurt C
Baylisascaris procyonis is a common gastrointestinal parasite of raccoons (Procyon lotor) and is a zoonotic helminth with the potential to cause severe or fatal infection. Raccoons thrive in human-dominated landscapes, and the fecal-oral transmission pathway and lack of effective treatment make B. procyonis a serious threat to public health. The distribution of medicinal baits has emerged as a socially acceptable and cost-effective method for managing disease in free-ranging wildlife. We assessed the suitability of a mass-producible anthelmintic bait for B. procyonis mitigation by evaluating the willingness of free-ranging raccoons to consume anthelmintic baits and determining whether bait consumption successfully cleared B. procyonis infections from raccoons. Anthelmintic baits were modified from standard fishmeal polymer baits, the food attractant commonly used in oral rabies vaccine baits, with the introduction of 220 mg of pyrantel pamoate into the fishmeal mixture. We captured 16 naturally infected raccoons, presented one anthelmintic bait, and monitored B. procyonis infection over 90 d by screening feces for eggs. Treatment cleared B. procyonis infections for nine of 12 raccoons that consumed >10 g of the 15 g bait. We used remote cameras to monitor in situ patterns of bait consumption for anthelmintic baits relative to standard baits. Both anthelmintic and standard baits were rapidly consumed, with no differences in the rate of consumption between bait types. However, after bait contact, raccoons demonstrated a greater willingness to consume standard baits while ignoring anthelmintic baits more frequently (P = 0.06). Initial trials of anthelmintic baits show promise, although refinement in both dose and palatability is needed. At mass production scales, the addition of pyrantel pamoate to fishmeal polymer baits would be inexpensive, potentially making anthelmintic baits a viable management option when coupled with an oral rabies vaccine or used independently
Lassen, B; Peltola, S-M
There is evidence of resistance in horses to anthelmintic treatment using ivermectin and pyrantel. However, little information is available about the parasites, treatment practices or anthelmintic resistance in the horse population in Estonia. In the present study, we examined 41 trotting and riding horses aged < 3 years from four stables in Estonia. Faecal samples were collected, and horses were selected for treatment if the nematode egg count per gram faeces exceeded 200. Horses (n= 32) that shed strongyle-type eggs were treated with pyrantel, whereas Parascaris equorum-positive animals received ivermectin. Up to 78% of horses required anthelmintic treatment and the efficiency of the anthelmintics was evaluated using a faecal egg count reduction test. Resistance of P. equorum was observed in 50% of horses treated with ivermectin and of strongyles in 27% of horses treated with pyrantel. Ivermectin treatment resulted in a mean reduction of 100% for strongyle eggs and an 89% reduction in P. equorum, and pyrantel-treated horses exhibited an 88% reduction in strongyle eggs. These results are considered to be the first indication of resistance to pyrantel, but further studies of ivermectin resistance are required. According to questionnaires completed by the owners of horses, resistance might be explained by a lack of evidence-based strategies, a strong preference for using ivermectin and possibly a subjective evaluation of the body weight of horses. PMID:25007041
For the first time, 39 of the major anthelmintics can be detected in one rapid and sensitive LC-MS/MS method, including the flukicides, which have been generally overlooked in surveillance programs. Utilizing the QuEChERS approach, residues were extracted from liver and milk using acetonitrile, sod...
... the pinworm. (c) A commentary on the life cycle of the pinworm. (d) A commentary on the ways in which... approved by the Office of Management and Budget under control number 0910-0232) ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Package inserts for anthelmintic drug...
Full Text Available The crude extract of Carica papaya (papaya seeds (CP and Cucurbita maxima (Pumpkin seeds (CM were assayed against adult earthworms (Pheretima posthuma for the evaluation of anthelmintic activity. Various concentrations of both extracts were tested and results were expressed in terms of time for paralysis (P and time for death (D of worms. Albendazole was used as a reference standard. The result showed that in both of the extracts (i.e. CP and CM dose of 60 mg / ml possesses more wormicidal activity. The time of paralysis was 1.88 ± 0.52 minute and 1.93 ± 0.57 minute whereas the time of death was 3.45 ± 0.17 minute and 4.90 ± 0.18 minute in the case of Carica papaya and Cucurbita maxima respectively. In conclusion, the use of seeds of Carica papaya (CP and Cucurbita maxima (CM for anthelmintic activity have been confirmed and further studies are suggested to isolate the active principles responsible for the activity. Both the extracts showed significant anthelmintic activity, but the comparative study showed that out of these two, Carica papaya proves to be a better anthelmintic remedy.
The anthelmintic activity of chicory (Cichorium intybus L.) herbage has been attributed to sesquiterpene lactones (SLs). Chicory leaves contain lactucin (LAC), 8-deoxylactucin (DOL), and lactucopicrin (LPIC), but the amounts of these three SLs vary among cultivars. The objective of this study was...
Brito, Danilo R Barros; Fernandes, Rozeverter Moreno; Fernandes, Maria Zenaide de Lima C M; Ferreira, Marcos Daniel de S; Rolim, Fernanda R L; da Silva Filho, Manoel L
The anthelmintic activity of aqueous and ethanolic extracts of Morinda citrifolia fruit (noni) was evaluated in chicken naturally infected by Ascaridia galli. The anthelmintic activity in vitro was determined in adult parasites. The aqueous and ethanolic extracts were used in the following concentrations: 1.69; 3.37; 6.74; 13.48 e 26.96 mg.mL(-1) and 4.17; 8.34; 16.68; 33.36 and 66.72 mg.mL(-1), respectively. The anthelmintic activity in vivo was determined by the administration of 10 mL.kg(-1) of the aqueous (50.1 mg.mL(-1)) and ethanolic (24.6 mg.mL(-1)) extracts during three consecutive days. Later the chickens were euthanized and necropsy was performed in order to count the remaining helminths. The data were analyzed by the Student-Newman-Keuls test. In the concentrations of 13.48 and 26.96 mg.mL(-1), the aqueous extract demonstrated mortality of 46.67 and 50%, respectively, there was a significative difference from the negative control (P 0.05). It follows that the anthelmintic activity of noni fruit test showed satisfactory results in vitro, there is a need for studies in higher concentrations in the in vivo test. PMID:20040206
Praziquantel is an anthelmintic that can be applied to the water to kill tapeworm and trematode parasites in fish. Effective praziquantel treatment rates have been determined but there is little information on the toxicity of this chemical to fish hosts of the parasites. Acute praziquantel toxicit...
S. H. Patil
Full Text Available The present study was designed to evaluate the anthelmintic potential of leaves & shoots extract of Uncaria gambier Roxb. The alcoholic extract of Uncaria gambier Roxb. & its ethyl acetate fraction at different concentrations (25, 50, 75, 100 mg/ml were tested on Indian adult earthworms (Pheretima posthuma by in vitro standard procedure. Time of paralysis and time of death of the worms were considered as the parameters to assess the anthelmintic action. Albendazole and 2% w/v gum acacia in distilled water were used as standard and control respectively. The ethyl acetate fraction of alcoholic extract exhibited potent anthelmintic activity compared to alcoholic extract as evidenced by significant decrease in time of paralysis & death. The observed activity could be due to the presence to phenolic compounds, particularly flavonoids in the test extract. These in vitro studies indicated that the Uncaria gambier Roxb. is a significant source of natural anthelmintic, which might be helpful in preventing the progress of various parasitic disorders.
M Sreejith; N Kannappan; A Santhiagu; Ajith P Mathew
Objective: The present study was carried out to investigate the phytochemical constituents, in vitro antioxidant potential and anthelmintic activities of Flacourtia sepiaria Roxb leaves. Methods: The dried powdered leaves of Flacourtia sepiaria were extracted using petroleum ether, chloroform, ethyl acetate and methanol by a soxhlet extractor and preliminary phytochemical screening was performed using standard protocols. All the extract was evaluated for their potential antioxidant activities using test such as DPPH, superoxide anion radical, hydroxyl radical, nitric oxide radical scavenging abilities, ferrous chelating ability and total phenolic and flavanoid content. Anthelmintic activity of extract was screened in adult Indian earthworm model. Results: Preliminary screening revealed the presence of bioactive compounds especially phenolics, tannins and terpenoids in all extracts. The phenolic and flavanoid content was highest in methanolic extract and lowest in petroleum ether extract. The paralytic (9.46±0.212) and death time (31.43±0.148) of methanolic extract was found to be significant (P Conclusions:The results of the present study indicate that the leaf extracts of Flacourtia sepiaria exhibited strong antioxidant activity and possess significant anthelmintic activity and thus it is a good source of antioxidant and anthelmintic constituents.
Krimpen, van M.M.; Binnendijk, G.P.; Borgsteede, F.H.M.; Gaasenbeek, C.P.H.
Two experiments were performed to determine the anthelmintic effect of some phytogenic feed additives on a mild infection of Ascaris suum in growing and finishing pigs. Usually, an infection of A. suum is controlled by using conventional synthetic drugs. Organic farmers, however, prefer a non-pharma
Full Text Available New oral anticoagulants are an effective and safe alternative to vitamin K antagonists in many fields of clinical practice. The use of the direct inhibitors of activated Factor II (dabigatran and activated Factor X (apixaban and rivaroxaban, both in patients with non-valvular atrial fibrillation (NVAF and those with acute venous thromboembolism (VTE, is of great interest for internal medicine physicians. This paper aims to give practical guidance on management (starting therapy, follow up and bleeding complications of patients treated with dabigatran, rivaroxaban or apixaban for NVAF or acute VTE providing practical tables concerning the phases of therapy, management of complications, drug interaction and dose adjustment if renal impairment occurs.
This review attempts to answer the common questions faced by a clinician regarding thromboembolism and thromboprophylaxis in patients following Fontan surgery. The review is in an easy to understand question and answer format and discusses the currently available literature on the subject in an attempt to arrive at practical clinically relevant solutions. Patients who have undergone the Fontan operation are at a high risk for thromboembolism. Based on available evidence, there is a strong rationale for thromboprophylaxis. However, it is not clear as to which agent should be administered to prevent thromboembolic events. While the available evidence suggests that antiplatelet agents alone may be as good as oral anticoagulants, there is a need for a large multicenter randomized control trial comparing these two common strategies to deliver a clear verdict. PMID:27625521
Full Text Available Bacterial infectious diseases, sharing clinical characteristics such as chronic inflammation and tissue damage, pose a major threat to human health. The steady increase of multidrug-resistant bacteria infections adds up to the current problems modern healthcare is facing. The treatment of bacterial infections with multi-resistant germs is very difficult, as the development of new antimicrobial drugs is hardly catching up with the development of antibiotic resistant pathogens. These and other considerations have generated an increased interest in the development of viable alternatives to antibiotics. A promising strategy is the use of nanomaterials with antibacterial character and of nanostructures displaying anti-adhesive activity against biofilms. Glycan-modified nanodiamonds (NDs revealed themselves to be of great promise as useful nanostructures for combating microbial infections. This review summarizes the current efforts in the synthesis of glycan-modified ND particles and evaluation of their antibacterial and anti-biofilm activities.
Szunerits, Sabine; Barras, Alexandre; Boukherroub, Rabah
Bacterial infectious diseases, sharing clinical characteristics such as chronic inflammation and tissue damage, pose a major threat to human health. The steady increase of multidrug-resistant bacteria infections adds up to the current problems modern healthcare is facing. The treatment of bacterial infections with multi-resistant germs is very difficult, as the development of new antimicrobial drugs is hardly catching up with the development of antibiotic resistant pathogens. These and other considerations have generated an increased interest in the development of viable alternatives to antibiotics. A promising strategy is the use of nanomaterials with antibacterial character and of nanostructures displaying anti-adhesive activity against biofilms. Glycan-modified nanodiamonds (NDs) revealed themselves to be of great promise as useful nanostructures for combating microbial infections. This review summarizes the current efforts in the synthesis of glycan-modified ND particles and evaluation of their antibacterial and anti-biofilm activities. PMID:27077871
Avci, Fikri Y; Karst, Nathalie A; Linhardt, Robert J
Heparin and low molecular weight heparins are major clinical anticoagulants and the drugs of choice for the treatment of deep venous thrombosis. The discovery of an antithrombin binding domain in heparin focused interest on understanding the mechanism of heparin's antithrombotic/ anticoagulant activity. Various heparin-mimetic oligosaccharides have been prepared in an effort to replace polydisperse heparin and low molecular weight heparins with a structurally-defined anticoagulant. The goal of attaining a heparin-mimetic with no unwanted side-effects has also provided motivation for these efforts. This article reviews structure-activity relationship (SAR) of structurally-defined heparin-mimetic oligosaccharides. PMID:14529394
Eduardo B. Saad
Full Text Available Atrial fibrillation is associated with thromboembolic events that may cause important impairment on quality of life. Pulmonary vein isolation is the treatment of choice in cases that are refractory to medical therapy. Once sheaths and catheters are manipulated inside the left atrium, anticoagulation with heparin must be used during the procedure to protect patients from thromboembolic phenomena. Different strategies of anticoagulation are used at different centers. This review summarizes the pathophysiology of thrombus formation in the left atrium, defines which patients are under high risk and describes the main strategies used for anticoagulation.
Lewis, S M; Kroner, B A
The literature describing pharmacy involvement with anticoagulation services primarily does not include information about patients' perceptions of this involvement. A 22-question survey was developed and administered to 296 patients enrolled in the anticoagulation clinic at the VA Pittsburgh Health Care System. Excluded patients had fewer than four clinic visits or were followed outside of the anticoagulation clinic. The study period was nine weeks and any missed patients were telephoned. The median response to each question was determined. Similar questions were analyzed for acquiescent trends. Results indicate that, overall, patients are comfortable with pharmacists providing warfarin monitoring and dose adjustments. PMID:10174757
Full Text Available Vitamin K antagonists (VKA are among the most widely prescribed drugs in the industrialized world. In fact, for decades, VKA have been the only orally available anticoagulant for the primary and secondary prevention of venous and arterial thrombotic events. Their efficacy has been widely demonstrated in a series of studies carried out in the 1990s. Since the incidences of atrial fibrillation and venous thromboembolism increase exponentially with age, the number of anticoagulated patients is destined to increase. This paper examines anticoagulation therapy management with particular attention to the use of VKA.
Wu, Songmei; Zuber, Flavia; Brugger, Juergen; Maniura-Weber, Katharina; Ren, Qun
We present here a technological platform for engineering Au nanotopographies by templated electrodeposition on antibacterial surfaces. Three different types of nanostructures were fabricated: nanopillars, nanorings and nanonuggets. The nanopillars are the basic structures and are 50 nm in diameter and 100 nm in height. Particular arrangement of the nanopillars in various geometries formed nanorings and nanonuggets. Flat surfaces, rough substrate surfaces, and various nanostructured surfaces were compared for their abilities to attach and kill bacterial cells. Methicillin-resistant Staphylococcus aureus, a Gram-positive bacterial strain responsible for many infections in health care system, was used as the model bacterial strain. It was found that all the Au nanostructures, regardless their shapes, exhibited similar excellent antibacterial properties. A comparison of live cells attached to nanotopographic surfaces showed that the number of live S. aureus cells was technological platform for engineering Au nanotopographies by templated electrodeposition on antibacterial surfaces. Three different types of nanostructures were fabricated: nanopillars, nanorings and nanonuggets. The nanopillars are the basic structures and are 50 nm in diameter and 100 nm in height. Particular arrangement of the nanopillars in various geometries formed nanorings and nanonuggets. Flat surfaces, rough substrate surfaces, and various nanostructured surfaces were compared for their abilities to attach and kill bacterial cells. Methicillin-resistant Staphylococcus aureus, a Gram-positive bacterial strain responsible for many infections in health care system, was used as the model bacterial strain. It was found that all the Au nanostructures, regardless their shapes, exhibited similar excellent antibacterial properties. A comparison of live cells attached to nanotopographic surfaces showed that the number of live S. aureus cells was information (ESI) available. See DOI: 10.1039/c5nr06157a
Chirag Modi; Shailesh Mody; Hitesh Patel; Ghanshyam Dudhatra; Avinash Kumar; Madhavi Awale
Plants are rich source of antibacterial agents because they produce wide array of bioactive molecules, most of which probably evolved as chemical defense against predation or infection. A major part of the total population in developing countries still uses traditional folk medicine obtained from plant resources With an estimation of WHO that as many as 80% of world population living in rural areas rely on herbal traditional medicines as their primary health care, the study on properties and...
Antibacterial activity of leaf and stem bark of Pterocarpus santalinus (Fabaceae) was investigated. The antibacterial activity was tested against both Gram-positive and Gram-negative organisms. Among the two extracts tested, stem bark extract exhibited broad-spectrum antibacterial activity against the tested organisms. The stem bark extract showed maximum activity against Enterobacter aerogenes, Alcaligenes faecalis, Escherichia coli, Pseudomonas aeruginosa, Proteus vulgaris, Bacillus cere...
Bungard, Tammy J; Gardner, Leslie; Archer, Stephen L.; Hamilton, Peter; Ritchie, Bruce; Tymchak, Wayne; Tsuyuki, Ross T.
Background Anticoagulation management services (AMSs) are widely used for anticoagulation management in many countries. Our AMS is a pharmacist-run ambulatory clinic with a physician advisory committee that manages patients referred with complicated anticoagulation histories. This paper assesses the adequacy of anticoagulation, rates of anticoagulant-related events and associated health care resource utilization for patients before and after referral to our AMS. Methods Consecutive patients r...
Full Text Available Background: The use of thrombolytic agents in the treatment of hemodynamically stable patients with acute submassive pulmonary embolism (PTE remains controversial. We, therefore, conducted this study to compare the effect of thrombolytic plus anticoagulation versus anticoagulation alone on early death and adverse outcome following submassive PTE.Methods: We conducted a study of patients with acute pulmonary embolism and pulmonary hypertension or right ventricular dilatation/dysfunction but without arterial hypotension or shock. The patients were randomly assigned in a single-blind fashion to receive an anticoagulant [Enoxaparin (1 mg/kg twice a day] plus a thrombolytic [Alteplase (100 mg or Streptokinase (1500000 u/2 hours] or an anticoagulant [Enoxaparin (1 mg/kg twice a day] alone. The primary endpoint was in-hospital death or clinical deterioration requiring an escalation of treatment. The secondary endpoints of the study were major bleeding, pulmonary hypertension, right ventricular dilatation at the end of the first week, and exertional dyspnea at the end of the first month.Results: Of 50 patients enrolled, 25 patients were randomly assigned to receive an anticoagulant plus a thrombolytic and the other 25 patients were given an anticoagulant alone. The incidence of the primary endpoints was significantly higher in the anticoagulant-alone group than in the thrombolytic-plus-anticoagulant group (p value = 0.022. At the time of discharge, pulmonary artery pressure was significantly higher in the anticoagulant-alone group than in the thrombolytic- plus-anticoagulant group (p value = 0.018; however, reduction in the right ventricular size or normalization of the right ventricle showed non-significant differences between the two groups. There was no significant difference regarding the New York Heat Association (NYHA functional class between the two groups at the end of the first month (p value = 0.213. No fatal bleeding or cerebral bleeding
Lassen, Michael R
For many years, vitamin K antagonists, unfractionated heparins, low-molecular-weight heparins and a pentasaccharide were the only anticoagulant drugs available for the prevention of venous thromboembolism after surgery. However, their benefits were associated with disadvantages, such as their...
von Samson-Himmelstjerna, G; Harder, A; Sangster, N C; Coles, G C
Resistance against the major currently available anthelmintics has reached a critical level in many small ruminant herds world-wide, and is increasingly becoming a problem in horses and cattle. Therefore, new products with different modes of action are urgently needed. Recently, such a new class of compounds, the anthelmintically active cyclooctadepsipeptides, was described. Here, the effects of cyclooctadepsipeptides on benzimidazole-, levamisole- and ivermectin-resistant populations of Haemonchus contortus in sheep as well as an ivermectin-resistant Cooperia oncophora population in cattle were studied. Experimentally infected sheep and cattle were used. Animals were treated orally, subcutaneously, or intravenously with cyclooctadepsipeptides. The anthelmintic effects were assessed by means of fecal egg count reductions and/or worm count reductions. Both, PF1022A and emodepside were found to be fully effective against these parasite populations. These findings confirm that this new class of compounds acts by a different mode of action compared to the above-mentioned anthelmintics. PMID:15796017
Dimova, Cena; Evrosimovska, Biljana; Pandilova, Maja; Kovacevska, Ivona; Zabokova-Bilbilova, Efka
Aim of this study is to review the evidence of different therapy approach, to highlight the areas of major concern and to suggest specific oral surgery treatment for patients on oral anticoagulants. The aim of operative treatment is to minimize the risk of hemorrhage while continuing to protect the patient against thromboembolism formation. The ordinary treatment includes the interruption of anticoagulant therapy for oral surgery interventions to prevent hemorrhage. However, this practice may...
Dimova, Cena; Papakoca, Kiro; Kovacevska, Ivona; Kamceva, Gordana
INTRODUCTIONS: The oral surgeons are frequently asked to manage patients who are receiving oral anticoagulants. The goal of treatment is to minimize the risk of hemorrhage while continuing to protect the patient against thromboembolism formation. The ordinary treatment includes the interruption of anticoagulant therapy for oral surgery interventions to prevent hemorrhage. AIM:However, this practice may logically increase the risk of a potentially life-threatening thromboembolism. Thus, thi...
The oral and maxillofacial surgeons are frequently asked to manage patients who are receiving oral anticoagulants. The goal of treatment is to minimize the risk of hemorrhage while continuing to protect the patient against thromboembolism formation. The ordinary treatment includes the interruption of anticoagulant therapy for oral surgery interventions to prevent hemorrhage. However, this practice may logically increase the risk of a potentially life-threatening thromboembolism. Thus, this is...
The oral and maxillofacial surgeons are frequently asked to manage patients who are receiving oral anticoagulants. The goal of treatment is to minimize the risk of hemorrhage while continuing to protect the patient against thromboembolism formation. The ordinary treatment includes the interruption of anticoagulant therapy for oral surgery interventions to prevent hemorrhage. However, this practice may logically increase the risk of a potentially life-threatening thromboembolism. Thus, this is...
Marcelo Kropf; Cleidson Alves Bergami; Felipe Dias Leal; Claudia Oliveira Dias Passos; Zilda de Santana Gonsalves; Isabela Laudares Marques; Isabela Azevedo Mota; Marcele Lima Monte Gonçalves
Anticoagulant therapy is essential for the prevention of risks associated with the formation of thrombus in patients after surgery, especially in orthopedics. Recently, new oral anticoagulants were introduced in the therapeutic arsenal. This fact is important, because the current drug of choice in clinical practice is enoxaparin, a low molecular weight heparin. As all injecting drugs, enoxaparin may reduce patients' adherence to treatment by dissatisfaction with and resistance to the administ...
Dimova, Cena; Evrosimovska, Biljana; Papakoca, Kiro; Georgiev, Zlatko; Angelovska, Bistra; Ristoska, Sonja
Introduction:The ordinary treatment of anticoagulated patients includes the interruption of anticoagulant therapy for oral surgery interventions to prevent hemorrhage. However, this practice may logically increase the risk of a potentially life-threatening thromboembolism, so this issue is still controversial. The aim of the study was to evaluate the antifibrinolitic mouthwash solution (tranexamic acid) as a local haemostatic modality after oral surgery interventions. Methods:To realize the a...
Barrios, Annette C.; Ventura, Hector O.; Milani, Richard V.
Clinical privileging of pharmacists and the effective use of support staff and information technology have helped create an efficient pharmacist-operated anticoagulation clinic at Ochsner Clinic Foundation that will support future growth efforts for improved patient care. Developed by Ochsner's Department of Cardiology, the pharmacist-operated anticoagulation clinic cares for 2000 patients with a clinical pharmacist, staff pharmacist, registered nurse, and medical assistants. Patients are man...
VALCHEV, Ivan; Binev, Rumen; YORDANOVA, Veska; Nikolov, Yordan
The newest measures for the control of harmful rodent populations are from the anticoagulant rodenticide group, which are divided into 2 subgroups: first and second generations, and indandione derivatives. Non-target organisms are potentially at risk of direct consumption of baits (primary hazard) and of eating poisoned rodents (secondary hazard). Anticoagulant rodenticides inhibit the enzyme vitamin K-dependent carboxylase and thus impair the reactivation of vitamin K1, indirectly affecting ...
Prashanth Panduranga; Mohammed El-Deeb; Chitra Jha
Choosing the best anticoagulant therapy for a pregnant patient with a mechanical prosthetic valve is controversial and the published international guidelines contain no clear-cut consensus on the best approach. This is due to the fact that there is presently no anticoagulant which can reliably decrease thromboembolic events while avoiding damage to the fetus. Current treatments include either continuing oral warfarin or substituting warfarin for subcutaneous unfractionated heparin or low-mole...
Fadi Shamoun; Hiba Obeid; Harish Ramakrishna
Atrial fibrillation continues to be a significant source of morbidity and mortality worldwide. Effective anticoagulation remains the cornerstone of outpatient and inpatient treatment. The use of the new generation of anticoagulants (NOACs) continues to grow. Recently published data indicate their cost-effectiveness and overall safety in stroke prevention; compared to vitamin K antagonists, they can be prescribed in fixed doses for long-term therapy without the need for coagulation monitoring....
Full Text Available L Bellamy1, N Rosencher1, BI Eriksson21Anaesthesiology Department, Hôpital Cochin (AP-HP, René Descartes University, Paris 75014 France; 2Orthopaedic Department, University Hospital Sahlgrenska/Ostra, Gothenburg, SwedenAbstract: The recent development of new oral anticoagulants, of which dabigatran etexilate is currently at the most advanced stage of development, is the greatest advance in the provision of convenient anticoagulation therapy for many years. A new oral anticoagulation treatment, dabigatran etexilate, is already on the market in Europe. The main interest probably will be to improve the prescription and the adherence to an effective thromboprophylaxis in medical conditions such as atrial fibrillation without bleeding side effects, without the need for monitoring coagulation, and without drug and food interactions such as vitamin K anticoagulant (VKA treatment. Dabigatran is particularly interesting for extended thromboprophylaxis after major orthopedic surgery in order to avoid daily injection for a month. However, oral long-term treatments such as VKA are not systematically associated with a higher compliance level than injected treatments such as low-molecular-weight heparins. Indeed, adherence to an oral treatment, instead of the usual daily injection in major orthopedic surgery, is complex, and based not only on the frequency of dosing but also on patient motivation, understanding, and socio-economic status. New oral anticoagulants may be useful in this way but education and detection of risk factors of nonadherence to treatment are still essential.Keywords: oral anticoagulant, adherence, compliance, education, dabigatran
Becattini, Cecilia; Lignani, Alessandra; Agnelli, Giancarlo
Anticoagulant drugs have an essential role in the prevention and treatment of thromboembolic diseases. Currently available anticoagulants substantially reduce the incidence of thromboembolic events in a number of clinical conditions. However, these agents have limitations that strengthen the case for the development of new anticoagulants. An ideal anticoagulant should be at least as effective as those currently in use, as well as safe, simple to use, and widely applicable. The majority of new anticoagulants currently under investigation are small molecules with a selective and direct anti-Xa or antithrombin action, allowing oral administration in fixed doses. These new agents are in different phases of clinical development. The anti-Xa agent rivaroxaban and the antithrombin agent dabigatran are already available for the prophylaxis of venous thromboembolism in some countries. Apixaban is in an advanced phase of clinical development and several anti-Xa agents are currently approaching phase III clinical trials. Promising results in terms of efficacy and safety profiles have been obtained with these agents in different clinical conditions. Differences in pharmacokinetics and pharmacodynamics could offer the potential for individualized anticoagulant therapies in the near future. PMID:20531960
Kuznetsov, M R; Leontyev, S G; Neskhodimov, L A; Tolstikhin, V Yu; Khotinskiy, A A
Adequate anticoagulant therapy is a general approach to treatment of deep vein thrombosis. However, the duration of anticoagulant therapy is not strictly specified in everyday clinical practice. The present article deals with various approaches to selecting the duration of therapy with anticoagulants based on the findings of studies, national and foreign clinical guidelines. The minimal duration of therapy for deep vein thrombosis and pulmonary thromboembolism amounts to 3 months in accordance with the national and American recommendations. For some cohorts of patients, continuation of therapy above 3 months is considered: patients with idiopathic thrombosis (the recommended duration of therapy of not less than 6 months), patients having persisting risk factor for relapse of thrombosis on termination of the main therapeutic course, oncological patients (6 month therapy followed by assessing the risk and benefit of continuing therapy with anticoagulants). Prolonged therapy of venous thromboembolism using unfractionated heparin or low-molecular-weight heparin followed by changing over to vitamin K antagonists is associated with decreased risk for thrombosis relapse approximately by 90%, however increasing the risk of haemorrhage. Currently, as an alternative, it is possible to consider administration of novel oral anticoagulants (rivaroxaban, dabigatran, apixaban) which beside high efficacy are associated with less risk of bleeding. The route of administration, no necessity to control the INR, and the minimal number of drug and food interactions make administration of new oral anticoagulants an attractive alternative to therapy with heparins and vitamin K antagonists. PMID:27100556
Norton, J L; Gibson, D L
The establishment of a pharmacist-managed out-patient anticoagulation clinic in a private community hospital is described. Discussions by pharmacy with office-based physicians at a 187-bed, private, nonprofit community medical center indicated that the traditional system of anticoagulation management was not ideal for the physicians or their patients. Development of a pharmacist-managed anticoagulation clinic began in fall 1993; operations began in spring 1994. Planning included analyzing existing practices, reviewing the relevant literature, obtaining physician input, visiting an established anticoagulation clinic, formulating a business plan, and developing clinical protocols. Collaborative relationships were established with the hospital laboratory, business office, and risk management, information services, and medical records departments. Two pharmacists were trained to work in the clinic and provide coverage 24 hours a day. Services include patient assessment, monitoring of anticoagulation, warfarin dosage adjustment, medication management, patient education, follow-up care, and providing feedback to referring and attending physicians. The clinic has met with physician and patient satisfaction, has reduced the number of admissions to treat warfarin-related bleeding, and has been able to cover its direct costs. A pharmacist-managed anti-coagulation clinic was successfully established in a private community hospital. PMID:8734675
Bodet, C A; Jorgensen, J H; Drutz, D J
Fourteen antineoplastic agents were examined for in vitro antibacterial activity against 101 aerobic and anaerobic bacterial isolates representing indigenous human microflora and selected opportunistic pathogens. Only 5-fluorouracil, mitomycin, and etoposide demonstrated inhibitory effects at achievable plasma concentrations, while the remaining drugs lacked appreciable antibacterial activities.
Williams, Andrew R; Peña-Espinoza, Miguel A; Boas, Ulrik; Simonsen, Henrik T; Enemark, Heidi L; Thamsborg, Stig M
Chicory is a perennial crop that has been investigated as a forage source for outdoor-reared ruminants and pigs, and has been reported to have anthelmintic properties. Here, we investigated in vitro anthelmintic effects of forage chicory-extracts against the highly prevalent swine parasites Ascaris suum and Oesophagostomum dentatum. Methanol extracts were prepared and purified from two different cultivars of chicory (Spadona and Puna II). Marked differences were observed between the anthelmintic activity of extracts from the two cultivars. Spadona extracts had potent activity against A. suum third (L3) and fourth (L4) - stage larvae, as well as O. dentatum L4 and adults, whereas Puna II extracts had less activity against A. suum and no activity towards O. dentatum L4. Transmission-electron microscopy of A. suum L4 exposed to Spadona extracts revealed only subtle changes, perhaps indicative of a specific anthelmintic effect rather than generalized toxicity. Ultra-high liquid chromatography-mass spectrometry analysis revealed that the purified extracts were rich in sesquiterpene lactones (SL), and that the SL profile differed significantly between cultivars. This is the first report of anthelmintic activity of forage chicory towards swine nematodes. Our results indicate a significant anthelmintic effect, which may possibly be related to SL composition. PMID:26935644
Maryam Taherkhani; Adineh Taherkhani; SeyedReza Hashemi; Taraneh Faghihi-Langroodi; Roxana Sadeghi; Mohammadreza Beyranvand
Background: The use of thrombolytic agents in the treatment of hemodynamically stable patients with acute submassive pulmonary embolism (PTE) remains controversial. We, therefore, conducted this study to compare the effect of thrombolytic plus anticoagulation versus anticoagulation alone on early death and adverse outcome following submassive PTE.Methods: We conducted a study of patients with acute pulmonary embolism and pulmonary hypertension or right ventricular dilatation/dysfunction but w...
Full Text Available Carbon nanomaterials like graphene, carbon nanotubes, fullerenes and the various forms of diamond have attracted great attention for their vast potential regarding applications in electrical engineering and as biomaterials. The study of the antibacterial properties of carbon nanomaterials provides fundamental information on the possible toxicity and environmental impact of these materials. Furthermore, as a result of the increasing prevalence of resistant bacteria strains, the development of novel antibacterial materials is of great importance. This article reviews current research efforts on characterizing the antibacterial activity of carbon nanomaterials from the perspective of colloid and interface science. Building on these fundamental findings, recent functionalization strategies for enhancing the antibacterial effect of carbon nanomaterials are described. The review concludes with a comprehensive outlook that summarizes the most important discoveries and trends regarding antibacterial carbon nanomaterials.
Enriquez, Andres; Lip, Gregory Y H; Baranchuk, Adrian
In recent years, non-vitamin K oral anticoagulants (NOACs) have emerged as an alternative to warfarin for the prevention and treatment of thrombo-embolic disease. Large randomized trials have demonstrated that these agents, which act by directly targeting thrombin (dabigatran) and factor Xa....... New specific antidotes (e.g. idarucizumab, andexanet alfa, and ciraparantag) show promising data, and may soon become available for clinical use. In this article, we review the pharmacology of these agents, the incidence and outcomes of haemorrhagic complications, the available strategies for...
Turnidge, John; PATERSON, DAVID L.
Clinical microbiology laboratories need to communicate results of antibacterial susceptibility testing to prescribers. Sophisticated prescribers who are knowledgeable of the pharmacokinetics and pharmacodynamics of antibacterials may desire no more information than the MIC of the drug in question. However, most prescribers require interpretation of antibacterial susceptibility testing results. Breakpoints can assist in determining if an antibacterial is potentially useful in the treatment of ...
Desrues, Oliver; Enemark, Heidi L.; Mueller-Harvey, I.;
Some plant secondary metabolites as tannins have direct anthelminthic properties and may play a role in the control of nematodes in livestock. However, their great diversity in structural characteristics and different levels of content in plants are responsible for a highly variable response in...... anthelmintic activity, as measured in vitro. The aim of the present study was to assess the relationship between tannin structure and anthelmintic activity using an in vitro assay. We used a series of purified tannins (from 65% to 100% of purity) characterized for their degree of polymerization (m......DP), prodelphinidin/procyanidin (PC/PD) ratio and cis/trans ratio by thiolytic degradation. Tannins diluted in two concentrations in water, epigallocatechin gallate (EGCG), positive (ivermectin) and negative (water) controls were examined by the Larval Feeding Inhibition Assay (LFIA) with first stage larvae (L1) of...
Full Text Available The aim of the present study was to evaluate the anthelmintic potential of ethanolic and aqueous extract of bark of Holoptelea integrifolia using Eisenia foetida. Various concentrations (10, 25, 50 and 100 mg/ml of ethanolic and aqueous extract were tested in the bioassay, which involved determination of time of paralysis (P and time of death (D of the worms. Piperazine Citrate (10 mg/ml was included as standard. The results indicated that the ethanolic and aqueous extract significantly demonstrated paralysis and also caused death of worms especially at higher concentration as compared to standard references. In conclusion, the use of bark of Holoptelea integrifolia as an anthelmintic have been confirmed and further studies are suggested to isolate the active principles responsible for the activity.
T. Srinath Reddy
Full Text Available Gymnema sylvestre has been used as a traditional medicinal plant to prevent diabetes. The present study was undertaken to evaluate anthelmintic activity of hot and cold hydroalcoholic extracts of Gymnema sylvestre leaves against Pheretima posthuma. Various concentrations (25-500 mg/ml of hot and cold hydroalcoholic extracts of Gymnema sylvestre were evaluated in the bioassay involving determination of time of paralysis (P and time of death (D of the worms. Albendazole was used as standard anthelmintic drug and distilled water was used as control. The results of present study indicated that the hydroalcoholic extracts significantly exhibited the paralysis in worms and also caused death of worms in dose dependent manner, among which hot maceration extract showing more significant results when compared with the cold maceration extract. Further studies have to be done to isolate the active principles responsible for the activity.
Full Text Available Tabernaemontana coronaria is a potential non cultivated medicinal plant widely distributed in waste lands and open forests in India. The alcoholic, ethereal and chloroform extracts were obtained from the plant Tabernaemontana coronaria by soxhlet extraction or continuous hot percolation method and the extracts were evaluated for their anthelmintic activity, against locally available earth worms (Pheretima posthuma. Three concentrations (10, 30, 60 mg/ml were prepared from each extract and were used for the study over earth worms. The study involves the determination of time of paralysis and time for death of the earth worms tested. The results obtained from the study revealed that all the extracts of Tabernaemontana coronaria possess significant anthelmintic effect at highest concentration (60 mg/ml. A solution of Albendazole was prepared in same concentration as that of extract and was used as standard. A 5% tween-80 suspension prepared using normal saline solution was used as control or blank.
Liu, Tian-Ming; Wu, Xing-Ze; Qiu, Yun-Ren
Citric acid (CA) and chitosan (CS) were covalently immobilized on polyurethane (PU) materials to improve the biocompatibility and antibacterial property. The polyurethane pre-polymer with isocyanate group was synthesized by one pot method, and then grafted with citric acid, followed by blending with polyethersulfone (PES) to prepare the blend membrane by phase-inversion method so that chitosan can be grafted from the membrane via esterification and acylation reactions eventually. The native and modified membranes were characterized by attenuated total reflectance-Fourier transform infrared spectroscope, X-ray photoelectron spectroscopy, scanning electron microscopy, water contact angle measurement, and tensile strength test. Protein adsorption, platelet adhesion, hemolysis assay, activated partial thromboplastin time, prothrombin time, thrombin time, and adsorption of Ca(2+) were executed to evaluate the blood compatibility of the membranes decorated by CA and CS. Particularly, the antibacterial activities on the modified membranes were evaluated based on a vitro antibacterial test. It could be concluded that the modified membrane had good anticoagulant property and antibacterial property. PMID:27102367
Rasmussen, Rasmus V; Snygg-Martin, Ulrika; Olaison, Lars;
-hospital mortality was 23% (95% CI: 17-29%), and there was no significant difference between those with or without anticoagulation. CONCLUSIONS: We found no increased risk of cerebral haemorrhage in S. aureus IE patients receiving anticoagulation. Anticoagulation was associated with a reduced risk of cerebral events...... before initiation of antibiotics. Data support the continuance of anticoagulation in S. aureus IE patients when indicated.......OBJECTIVES: To study the impact of anticoagulation on major cerebral events in patients with left-sided Staphylococcus aureus infective endocarditis (IE). METHODS: A prospective cohort study; the use of anticoagulation and the relation to major cerebral events was evaluated separately at onset...
Schurer, Janna M.; McKenzie, Christina; Dowling, Patricia M.; Bouchard, Emilie; Jenkins, Emily J.
Animal shelters have limited resources and must accommodate large numbers of animals at unpredictable intake rates. These dogs and cats are often parasitized, which can adversely affect the health of animals and expose shelter workers and adoptive owners to zoonoses. We analyzed survey responses from rural (n = 32) and urban (n = 50) companion animal shelters across Canada, and compared the wholesale cost of commercially available anthelmintics to identify cost-effective methods of managing p...
Pedersen, Amy B.; Antonovics, Janis
Individuals are often co-infected with several parasite species, yet the consequences of drug treatment on the dynamics of parasite communities in wild populations have rarely been measured. Here, we experimentally reduced nematode infection in a wild mouse population and measured the effects on other non-target parasites. A single oral dose of the anthelmintic, ivermectin, significantly reduced nematode infection, but resulted in a reciprocal increase in other gastrointestinal parasites, spe...
Ikeda, Haruo; Nonomiya, Tomoko; Usami, Masayo; Ohta, Toshio; Ōmura, Satoshi
Analysis of the gene cluster from Streptomyces avermitilis that governs the biosynthesis of the polyketide anthelmintic avermectin revealed that it contains four large ORFs encoding giant multifunctional polypeptides of the avermectin polyketide synthase (AVES 1, AVES 2, AVES 3, and AVES 4). These clustered polyketide synthase genes responsible for avermectin biosynthesis together encode 12 homologous sets of enzyme activities (modules), each catalyzing a specific round of polyketide chain el...
Ali Niaz; Ali Shah Syed; Shah Ismail; Ahmed Ghayour; Ghias Mehreen; Khan Imran; Ali Waqar
Abstract Background Verbascum thapsus is used in tribal medicine as an antispasmodic, anti-tubercular agent and wormicide. In this study, we investigated the antispasmodic and anthelmintic activities of crude aqueous methanolic extract of the plant. Methods V. thapsus extracts were tested against roundworms (Ascaridia galli) and tapeworms (Raillietina spiralis). Each species of worm was placed into a negative control group, an albendazole treatment group, or a V. thapsus treatment group, and ...
S.Ushasri; Ch.Gireesh kumar; M.Sarath Chandra Sekhar; Ramesh, N.; Satyanarayana, M.
Tabernaemontana coronaria is a potential non cultivated medicinal plant widely distributed in waste lands and open forests in India. The alcoholic, ethereal and chloroform extracts were obtained from the plant Tabernaemontana coronaria by soxhlet extraction or continuous hot percolation method and the extracts were evaluated for their anthelmintic activity, against locally available earth worms (Pheretima posthuma). Three concentrations (10, 30, 60 mg/ml) were prepared from each extract and w...
A. MAHFOOZ, M. Z. MASOOD, A. YOUSAF, N. AKHTAR AND M. A. ZAFAR
The prevalence and anthelmintic efficacy of Abamectin against gastrointestinal parasites under field conditions in Faisalabad (Punjab, Pakistan) was studied in 100 horses. The overall prevalence of gastrointestinal parasites was 75%, including Strongylus spp. (50%), Oxyuris equi (12%), Parascaris equorum (8%) and mixed infection (5%). Among these naturally infected animals, 15 were selected. These horses were assigned to three groups on the basis of prevalent species of gastrointestinal paras...
Full Text Available The water extract of Trigonella foenum graecum stem and leaves was tested for lethal activity against Hymenolepis nana, Syphacia obvelata, and Moniezia expansa. The plant extract demonstrated good anthelmintic activity in vitro which is directly related to the concentration of the extract used. The extract also prevents the formation of Ascaris larvae from the eggs of Ascaris lumbrico- ides (human. Department of Pharmacology and Department of Pathobiology, School of Medicine, Universety of Isfahan, Isfahan IRAN.
Bartley, David Jon
The studies within this thesis have made a valuable contribution to our understanding of anthelmintic resistance in Scotland and in particular to the prevalence of benzimidazole (BZ) and ivermectin (IVM) resistance, the expression of multiple resistance and its management. Parasitic gastroenteritis (PGE) is a major welfare issue not only for Scottish, UK and European farmers but also for livestock producers throughout the world. Parasites such as Haemonchus, Trichostrongylus ...
Nellickal Subramanyan Jayamohan
Full Text Available Introduction: Herbal medicines have been used for treating various diseases from ancient times. Even in the era of advanced modern medicine, natural sources of antioxidants and pharmaceutical compounds are of great importance, many of such rich sources are still unearthed.Materials and methods: Methanolic extract of Jamun (Syzygium cumini tree bark was screened for in vitro- antioxidant activity. Preliminary phytochemical screening results showed S. cumini was positive for flavonoids, saponins, tannins and terpenoids. Antioxidant studies includes DPPH scavenging activity, reducing capacity assessment, reducing effect, scavenging of hydrogen peroxide and nitrous oxide scavenging activity against ascorbic acid (ASA standard.Results: The phenolic content was 480 mg % of gallic acid equivalents, tannin 1.9 mg % of gallic acid equivalents, tannin was 250 mg % of catechine equivalents on ferric chloride estimation and flavon content 66.17 µg/ ml was considerable. Anthelmintic property of methanolic and aqueous extract of S. cumini bark showed promising activity against control.Discussion: S. cumini could be a promising agent in antioxidant and anthelmintic research and could lead in development of new drug molecule. To the best of our knowledge this is the first report on the antioxidant and anthelmintic activity of S. cumini bark.
Fouche, Gerda; Sakong, Bellonah M; Adenubi, Olubukola T; Pauw, Elizabeth; Leboho, Tlabo; Wellington, Kevin W; Eloff, Jacobus N
The nematode, Haemonchus contortus, is responsible for major economic losses in the livestock industry. The management of parasites such as H. contortus has been through the use of synthetic parasiticides. This has resulted in the presence of residues in meat and milk, which affects food safety. The development of resistance to available anthelmintics coupled with their high cost has further complicated matters. This has led to the investigation of alternative methods to manage nematodes, including the use of plants and plant extracts as a potential source of novel anthelmintics. Acetone extracts were prepared from 15 South African plant species and their anthelmintic activity determined using the egg hatch assay (EHA). The leaf extract of Cleome gynandra had the best inhibitory activity (68% ± 3%) at a concentration of 2.5 mg/mL, followed by the stem extract of Maerua angolensis (65% ± 5%). The extracts had a relatively low toxicity on Vero cells determined by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) cellular assay. PMID:27543148
Islam Md. Shamsul
Full Text Available This study describes the biological investigations of Clerodendrum viscosum – a plant belonging to the family Verbenaceae. The leaf of Clerodendrum viscosum was extracted with methanol and water. The crude extract of methanol of Clerodendrum viscosum was screened for cytotoxic activity using brine shrimp lethality bioassay. A reputed cytotoxic agent vincristine sulphate was used as a positive control. From the result of the brine shrimp lethality bioassay it can be well predicted that methanol extract possess cytotoxic principles (with LC50 3.696 µg/ml comparison with positive control vincristine sulphate (with LC50 0.773 µg /ml. Both methanolic and aqueous extracts from the leaves of Clerodendrum viscosum were investigated for their anthelmintic activity against Pheretima posthuma and five concentrations (10, 20, 30, 40 and 50 mg/ml of each extracts were studied in activity, which involved the determination of time of paralysis and time of death of the worm. Both the extracts exhibited significant anthelmintic activity at highest concentration of 50 mg/ml. Albendazole in 20mg/ml concentration extract was used as standard reference and saline solution as control. All the extracts showed significant anthelmintic activity in dose dependent manner.
Stepek, Gillian; Lowe, Ann E; Buttle, David J; Duce, Ian R; Behnke, Jerzy M
Infections with gastrointestinal (GI) nematodes are amongst the most prevalent worldwide, especially in tropical climates. Control of these infections is primarily through treatment with anthelmintic drugs, but the rapid development of resistance to all the currently available classes of anthelmintic means that alternative treatments are urgently required. Cysteine proteinases from plants such as papaya, pineapple and fig are known to be substantially effective against three rodent GI nematodes, Heligmosomoides polygyrus, Trichuris muris and Protospirura muricola, both in vitro and in vivo. Here, based on in vitro motility assays and scanning electron microscopy, we extend these earlier reports, demonstrating the potency of this anthelmintic effect of plant cysteine proteinases against two GI helminths from different taxonomic groups - the canine hookworm, Ancylostoma ceylanicum, and the rodent cestode, Rodentolepis microstoma. In the case of hookworms, a mechanism of action targeting the surface layers of the cuticle indistinguishable from that reported earlier appears to be involved, and in the case of cestodes, the surface of the tegumental layers was also the principal location of damage. Hence, plant cysteine proteinases have a broad spectrum of activity against intestinal helminths (both nematodes and cestodes), a quality that reinforces their suitability for development as a much-needed novel treatment against GI helminths of humans and livestock. PMID:18005461
Full Text Available Antibacterial activity of leaf and stem bark of Pterocarpus santalinus (Fabaceae was investigated. The antibacterial activity was tested against both Gram-positive and Gram-negative organisms. Among the two extracts tested, stem bark extract exhibited broad-spectrum antibacterial activity against the tested organisms. The stem bark extract showed maximum activity against Enterobacter aerogenes, Alcaligenes faecalis, Escherichia coli, Pseudomonas aeruginosa, Proteus vulgaris, Bacillus cereus, Bacillus subtilis, Staphylococcus aureus . The leaf extract showed maximum activity against Escherichia coli, Alcaligenes faecalis, Enterobacter aerogenes and Pseudomonas aeruginosa . Both extracts exhibited concentration dependent activity.
Jang, Yongjun; Park, Geun-Young; Park, Jihye; Choi, Asayeon; Kim, Soo Yeon; Boulias, Chris; Phadke, Chetan P.; Ismail, Farooq
Objective To evaluate Korean physiatrists' practice of performing intramuscular botulinum toxin injection in anticoagulated patients and to assess their preference in controlling the bleeding risk before injection. Methods As part of an international collaboration survey study, a questionnaire survey was administered to 100 Korean physiatrists. Physiatrists were asked about their level of experience with botulinum toxin injection, the safe international normalized ratio range in anticoagulated patients undergoing injection, their tendency for injecting into deep muscles, and their experience of bleeding complications. Results International normalized ratio <2.0 was perceived as an ideal range for performing Botulinum toxin injection by 41% of the respondents. Thirty-six respondents replied that the international normalized ratio should be lowered to sub-therapeutic levels before injection, and 18% of the respondents reported that anticoagulants should be intentionally withheld and discontinued prior to injection. In addition, 20%–30% of the respondents answered that they were uncertain whether they should perform the injection regardless of the international normalized ratio values. About 69% of the respondents replied that they did have any standardized protocols for performing botulinum toxin injection in patients using anticoagulants. Only 1 physiatrist replied that he had encountered a case of compartment syndrome. Conclusion In accordance with the lack of consensus in performing intramuscular botulinum toxin injection in anticoagulated patients, our survey shows a wide range of practices among many Korean physiatrists; they tend to avoid botulinum toxin injection in anticoagulated patients and are uncertain about how to approach these patients. The results of this study emphasize the need for formulating a proper international consensus on botulinum toxin injection management in anticoagulated patients. PMID:27152278
Muscarella, Marilena; Armentano, Antonio; Iammarino, Marco; Palermo, Carmen; Amorena, Michele
This study evaluates the presence of anticoagulant rodenticides in animals with a diagnosis of suspected poisoning and in bait samples. The survey was carried out from 2010 to 2012, in 2 regions of South Italy (Puglia and Basilicata) on 300 organs of animals and 90 suspected bait samples. The qualitative and quantitative analyses were conducted using an analytical method based on high‑performance liquid chromatography (HPLC) with fluorimetric detection (FLD) for the simultaneous determination of 8 anticoagulant rodenticides (bromadiolone, brodifacoum, coumachlor, coumafuryl, coumatetralyl, difenacoum, flocoumafen, and warfarin). The presence of anticoagulant rodenticides was detected in 33 organs of animals (11% of the total) and 6 bait samples (7% of the total). The most commonly detected compound was coumachlor (47% of 39 positive samples) followed by bromadiolone (24%), and brodifacoum (11%). The species mostly involved in anticoagulant rodenticide poisoning were dogs and cats. This study emphasizes the relevance of the determinations of anticoagulant rodenticides in cases of suspected poisoning in veterinary practice. PMID:27393877
Garabedian-Ruffalo, S M; Gray, D R; Sax, M J; Ruffalo, R L
The effectiveness of a pharmacist-managed warfarin anticoagulation clinic in maintaining therapeutic prothrombin times and preventing hospitalizations secondary to inadequate control of anticoagulation was evaluated. Patients who had received warfarin sodium for at least one year before being referred to the anticoagulation clinic were studied using retrospective chart reviews. Clinical pharmacists provided patient education, monitored patients for hemorrhagic and thromboembolic complications, and adjusted warfarin sodium dosage to maintain therapeutic prothrombin times. The patients' primary physicians retained responsibility for overall care and were consulted by pharmacists regarding complications of anticoagulation and patient unreliability. The percentage of patients requiring hospitalization (39% versus 4%) and the percentage of prothrombin times outside the therapeutic range (35.8% versus 14.4%) were significantly higher during the preclinic phase (before referral to the clinic) than during the clinic phase. Eight patients were hospitalized for hemorrhagic complications and four for thromboembolism during the preclinic phase; only one hospitalization for hemorrhage occurred during the clinic phase. The warfarin anticoagulation clinic staffed by specially trained pharmacists provided improved therapy compared with treatment received by patients before their referral to the clinic. PMID:3976675
Full Text Available Due to their mechanism of action, the new oral anticoagulants are named direct oral anticoagulants (DOACs. Dabigatran is a selective, competitive, direct inhibitor of thrombin (Factor IIa while rivaroxaban, apixaban and edoxaban act by directly inhibiting the activated Factor X (FXa in a selective and competitive manner. DOACs have a relatively short half-life and almost immediate anticoagulant activity, and rapidly reach the plasma peak concentration. Therefore, they do not need a phase of overlapping with parenteral anticoagulants. After their withdrawal, their removal is sufficiently rapid, although influenced by renal function. Dabigatran is the only DOACs to be administered as a pro-drug and becomes active after drug metabolization. The route of elimination of dabigatran is primarily renal, whereas FXa inhibitors are mainly eliminated by the biliary-fecal route. The drug interactions of DOACs are mainly limited to drugs that act on P-glycoprotein for dabigatran and on P-glycoprotein and/or cytochrome P3A4 for anti-Xa. DOACs have no interactions with food. Given their linear pharmacodynamics, with a predictable dose/response relationship and anticoagulant effect, DOACs are administered at a fixed dose and do not require routine laboratory monitoring.
Full Text Available Abstract Background Saponins isolated from plant sources have a number of traditional and industrial applications. Saponins have pharmacological effects like anti-inflammatory, molluscicidal, antimicrobial, antispasmodic, antidiabetic, anticancer, anticonvulsant, anthelmintic, antitussive and cytotoxic activities. The current work describes the anthelmintic and cytotoxic activities of crude saponins of Achillea Wilhelmsii and Teucrium Stocksianum as these plants are rich with saponins. Methods Brine shrimp cytotoxic activity of crude saponins was determined by Meyer et al. (1982 at test concentrations of 1000 μg/ml, 100 μg/ml, 10 μg/ml, 7.5 μg/ml, 5.0 μg/ml, 2.5 μg/ml and 1.25 μg/ml. Percentage mortality of test concentrations was determined. Similarly, in vitro anthelmintic activity was determined against roundworms, tapeworms and earthworms. Albendazole and piperazine citrate at concentration 10 mg/ml were used as standard anthelmintic drugs. Results Crude saponins of Achillea wilhelmsii (CSA and Teucrium stocksianum (CST had, respectively, cytotoxic activity with LC50 values 2.3 ± 0.16 and 5.23 ± 0. 34 μg/ml. For in vitro anthelmintic activity, time for paralysis and death of parasites (parasiticidal activity was noted. At concentration 40 mg/ml, crude saponins of Achillea wilhelmsii are 1.96 and 2.12 times more potent than albendazole against Pheretima posthuma and Raillietina spiralis, respectively. Similarly, at concentration 40 mg/ml, crude saponins of Teucrium stocksianum (CST has 1.89, 1.96 and 1.37 times more parasiticidal activity than albendazole against Pheretima posthuma, Raillietina spiralis and Ascardia galli, respectively. Conclusion Crude saponins of Achillea wilhelmsii and Teucrium stocksianum have cytotoxic and anthelmintic activity. The crude saponins may be excellent sources of cytotoxic and anthelmintic constituents that warrant its isolation and purification for new drug development.
Full Text Available Sebastian Luger,1 Carina Hohmann,2 Daniela Niemann,1 Peter Kraft,3 Ignaz Gunreben,3 Tobias Neumann-Haefelin,2 Christoph Kleinschnitz,3 Helmuth Steinmetz,1 Christian Foerch,1 Waltraud Pfeilschifter1 1Department of Neurology, University Hospital Frankfurt, Frankfurt am Main, 2Department of Neurology, Klinikum Fulda gAG, Fulda, 3Department of Neurology, University Hospital Würzburg, Würzburg, Germany Background: Oral anticoagulant therapy (OAT potently prevents strokes in patients with atrial fibrillation. Vitamin K antagonists (VKA have been the standard of care for long-term OAT for decades, but non-VKA oral anticoagulants (NOAC have recently been approved for this indication, and raised many questions, among them their influence on medication adherence. We assessed adherence to VKA and NOAC in secondary stroke prevention. Methods: All patients treated from October 2011 to September 2012 for ischemic stroke or transient ischemic attack with a subsequent indication for OAT, at three academic hospitals were entered into a prospective registry, and baseline data and antithrombotic treatment at discharge were recorded. At the 1-year follow-up, we assessed the adherence to different OAT strategies and patients’ adherence to their respective OAT. We noted OAT changes, reasons to change treatment, and factors that influence persistence to the prescribed OAT. Results: In patients discharged on OAT, we achieved a fatality corrected response rate of 73.3% (n=209. A total of 92% of these patients received OAT at the 1-year follow-up. We observed good adherence to both VKA and NOAC (VKA, 80.9%; NOAC, 74.8%; P=0.243 with a statistically nonsignificant tendency toward a weaker adherence to dabigatran. Disability at 1-year follow-up was an independent predictor of lower adherence to any OAT after multivariate analysis, whereas the choice of OAT did not have a relevant influence. Conclusion: One-year adherence to OAT after stroke is strong (>90% and patients
Dilute Russell's viper venom (DRVV) testing and activated partial thromboplastin time (APTT) have been effectively used in combination for lupus anticoagulant testing. The purpose of our study was to evaluate the role of mixing in activated partial thromboplastin and dilute Russell's viper venom testing for evaluation of lupus anticoagulants. Citrated blood from patients who were not on oral anticoagulant therapy was studied. Mixing study with 1 : 1 normal plasma for elevated APTT and also few samples with elevated screen time was carried out. Elevated APTT was seen in only 48.1% of patients with lupus anticoagulant. Correction of APTT was seen in 27.8% of lupus anticoagulant-positive patients. DRVV test on mixing resulted in 83.8% false-negative values. Integrated DRVV test could be a standalone test for testing lupus anticoagulant. Mixing study may be restricted for patients on oral anticoagulants or patients with strong lupus anticoagulant. PMID:26626041
Haustein, K O
Anticoagulants of the cumarin-type (warfarin, phenprocoumon, and acenocoumarol) are drugs for the long-term treatment and prevention of thromboembolic disorders. Because of their narrow therapeutic range, many patients have bleedings of variable severity or have recurrent thrombotic events. For this reason, the study of the pharmacokinetic parameters of phenprocoumon (PPC), considering its influence on blood clotting factors, is of high interest. The elimination kinetics of PPC, its interaction with phytomenadion (vitamin K), and the pharmacokinetic behavior of the anticoagulant under steady-state conditions have been investigated in studies with healthy volunteers and patients taking anticoagulants. The maintenance dose and the plasma levels of PPC were correlated with prothrombin time (PT) in 89 patients treated with PPC. Varying parameters in each patient (e.g., elimination kinetics of PPC, activity of the cumarin-dependent blood-clotting factors, endogenous phytomenadion stores), render it impossible to use a different means of monitoring than that of PT determination. PMID:10327214
Nutescu, Edith A; Shapiro, Nancy L; Chevalier, Aimee; Amin, Alpesh N
For over 50 years, anticoagulant options for the treatment and prevention of thrombosis have been limited mainly to traditional agents such as unfractionated heparin and oral vitamin K antagonists such as warfarin. These traditional agents are fraught with limitations that complicate their clinical use. A variety of novel anticoagulants with improved pharmacologic and clinical profiles have recently been introduced or are in development, offering benefits over traditional therapies. Specifically, progress has been made in the development of low-molecular-weight heparins, factor Xa inhibitors, and direct thrombin inhibitors. Because of their convenience and ease of use, some of these novel compounds are competing with the traditional anticoagulants and are needed additions to the antithrombotic arsenal. PMID:15853173
Full Text Available Amber L Beitelshees,1,* Deepak Voora,2,* Joshua P Lewis,1,* 1Program for Personalized and Genomic Medicine and Division of Endocrinology, Diabetes, and Nutrition, University of Maryland School of Medicine, Baltimore, MD, USA; 2Center for Applied Genomics & Precision Medicine, Department of Medicine, Duke School of Medicine, Durham, NC, USA*All authors contributed equally to this work Abstract: In recent years, substantial effort has been made to better understand the influence of genetic factors on the efficacy and safety of numerous medications. These investigations suggest that the use of pharmacogenetic data to inform physician decision-making has great potential to enhance patient care by reducing on-treatment clinical events, adverse drug reactions, and health care-related costs. In fact, integration of such information into the clinical setting may be particularly applicable for antiplatelet and anticoagulation therapeutics, given the increasing body of evidence implicating genetic variation in variable drug response. In this review, we summarize currently available pharmacogenetic information for the most commonly used antiplatelet (ie, clopidogrel and aspirin and anticoagulation (ie, warfarin medications. Furthermore, we highlight the currently known role of genetic variability in response to next-generation antiplatelet (prasugrel and ticagrelor and anticoagulant (dabigatran agents. While compelling evidence suggests that genetic variants are important determinants of antiplatelet and anticoagulation therapy response, significant barriers to clinical implementation of pharmacogenetic testing exist and are described herein. In addition, we briefly discuss development of new diagnostic targets and therapeutic strategies as well as implications for enhanced patient care. In conclusion, pharmacogenetic testing can provide important information to assist clinicians with prescribing the most personalized and effective antiplatelet and
Full Text Available The short-comings of current anticoagulants have led to the development of newer, albeit more expensive, oral alternatives.Objective: To explore the potential impact the new anticoagulants dabigatran and rivaroxaban in the local hospital setting, in terms of utilisation and subsequent costing.Method: A preliminary costing analysis was performed based on a prospective 2-week clinical audit (29th June - 13th July 2009. Data regarding current anticoagulation management were extracted from the medical files of patients admitted to Ryde Hospital. To model potential costing implications of using the newer agents, the reported incidence of VTE/stroke and bleeding events were obtained from key clinical trials.Results: Data were collected for 67 patients treated with either warfarin (n=46 or enoxaparin (n=21 for prophylaxis of VTE/stroke. At least two-thirds of all patients were deemed suitable candidates for the use of newer oral anticoagulants (by current therapy: warfarin: 65.2% (AF, 34.8% (VTE; enoxaparin: 100%, (VTE. The use of dabigatran in VTE/stroke prevention was found to be more cost-effective than warfarin and enoxaparin due to significantly lower costs of therapeutic monitoring and reduced administration costs. Rivaroxaban was more cost-effective than warfarin and enoxaparin for VTE/stroke prevention when supplier-rebates (33% were factored into costing.Conclusion: This study highlights the potential cost-effectiveness of newer anticoagulants, dabigatran and rivaroxaban, compared to warfarin and enoxaparin. These agents may offer economic advantages, as well as clinical benefits, in the hospital-based management of anticoagulated patients.
E. I. Mayboroda
Full Text Available The literature data about antibacterial properties of benzimidazole 2-thio-, 2-aminoderivatives and benzimidazole complexes have been generalized and systematized in the review. Today prevention and treatment of diseases caused by microorganisms is an actual problem of modern therapy. Therefore, the search for active molecules, the based on them development of some new, more effective antimicrobial agents is an important task of modern pharmaceutical chemistry. Promising compounds for solving these problems are benzimidazole derivatives. They are available, functionally capable, stable and have a wide spectrum of biological activities (antiviral, anthelmintic, antibacterial, anticancer, antidiabetic.The purpose of this paper is to generalize and systematize information about the antimicrobial action of 2-thio-, 2-amino-substituted benzimidazoles and benzimidazole derivatives complexes with transition metals.These compounds and their complexes with transition metals are active against pathogenic strains Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhimurium, Proteus vulgaris, Bacillus cereus, Micrococcus luteus, Helicobacter рylori and others.
Dillon Carla; Twells Laurie; Bishop Lisa; Young Stephanie; Hawboldt John; O'Shea Patrick
Abstract Background The beneficial outcomes of oral anticoagulation therapy are dependent upon achieving and maintaining an optimal INR therapeutic range. There is growing evidence that better outcomes are achieved when anticoagulation is managed by a pharmacist with expertise in anticoagulation management rather than usual care by family physicians. This study compared a pharmacist managed anticoagulation program (PC) to usual physician care (UC) in a family medicine clinic. Methods A retros...
Feher, G; Illes, Z; Komoly, S; Hargroves, D
(NOACs) have been extensively studied in patients with deep vein thrombosis (DVT), pulmonary embolism (PE) and non-valvular atrial fibrillation (NVAF). The aim of our work to review the available evidence for NOACs in the treatment of CVT. Based on our literature search there is insufficient evidence to......Cerebral venous thrombosis (CVT) is an uncommon cause of stroke with extremely diverse clinical features, predisposing factors, brain imaging findings, and outcome. Anticoagulation is the cornerstone of CVT management, however, it is not supported by high-quality evicence. Novel oral anticoagulants...
Feher, Gergely; Illes, Zsolt; Komoly, Samuel; Hargroves, David
Cerebral venous thrombosis (CVT) is an uncommon cause of stroke with extremely diverse clinical features, predisposing factors, brain imaging findings, and outcome. Anticoagulation is the cornerstone of CVT management, however, it is not supported by high-quality evicence. Novel oral anticoagulants (NOACs) have been extensively studied in patients with deep vein thrombosis, pulmonary embolism and non-valvular atrial fibrillation. The aim of our work was to review the available evidence for NOACs in the treatment of CVT. Based on our literature search there is insufficient evidence to support the use of NOACs in CVT, although case series with rivaroxaban and dabigatran have showed promising results. PMID:25994451
Hankey, Graeme J; Norrving, Bo; Hacke, Werner; Steiner, Thorsten
Each year, 1·0–2·0% of individuals with atrial fibrillation and 0·1–0·2% of those with venous thromboembolism who are receiving one of the novel oral anticoagulants (dabigatran, rivaroxaban, or apixaban) can be expected to experience an acute ischemic stroke. Additionally, 0·2–0·5% of individuals with atrial fibrillation who are receiving one of the novel oral anticoagulants can be expected to experience an intracranial hemorrhage. This opinion piece addresses the current literature and offer...
Soltysiak, Jolanta; Warzywoda, Alfred; Kociński, Bartłomiej; Ostalska-Nowicka, Danuta; Benedyk, Anna; Silska-Dittmar, Magdalena; Zachwieja, Jacek
Background Regional citrate anticoagulation (RCA) is one of the methods used to prevent clotting in continuous renal replacement therapy (CRRT). The aim of this study was to describe the outcomes and complications of RCA-CRRT in comparison to heparin anticoagulation (HA)-CRRT in critically ill children. Methods This study was a retrospective review of 30 critically ill children (16 on RCA- and 14 on HA-CRRT) who underwent at least 24 h of CRRT. The mean body weight of the children was 8.69 ± ...
Pitrák, V; Hadacová, I; Hochová, I; Hoch, J
Chronic anticoagulant treatment is administered mostly for cardiological reasons. Cumarin derivatires are used in the majority of cases (Warfarin, Pelentan). It is necessary to monitor this treatment regularly and to control the dose according to the INR value. Different complications can occur; the haemorrhage represents a serious one. The authors discuss several aspects of anticoagulant therapy and possible prevention of the complications. The importance of the problems is demonstrated on the authors' clinical experience--two cases of haemorrhage after Warfarin administration simulating an acute surgical event. PMID:11482149
Full Text Available Combretum mucronatum Schumach. & Thonn. is a medicinal plant widely used in West African traditional medicine for wound healing and the treatment of helminth infections. The present study aimed at a phytochemical characterization of a hydroalcoholic leaf extract of this plant and the identification of the anthelmintic compounds by bioassay-guided fractionation. An EtOH-H2O (1:1 extract from defatted leaves was partitioned between EtOAc and H2O. Further fractionation was performed by fast centrifugal partition chromatography, RP18-MPLC and HPLC. Epicatechin (1, oligomeric proanthocyanidins (OPC 2 to 10 (mainly procyanidins and flavonoids 11 to 13 were identified as main components of the extract. The hydroalcoholic extract, fractions and purified compounds were tested in vitro for their anthelmintic activity using the model nematode Caenorhabditis elegans. The bioassay-guided fractionation led to the identification of OPCs as the active compounds with a dose-dependent anthelmintic activity ranging from 1 to 1000 μM. Using OPC-clusters with a defined degree of polymerization (DP revealed that a DP ≥ 3 is necessary for an anthelmintic activity, whereas a DP > 4 does not lead to a further increased inhibitory effect against the helminths. In summary, the findings rationalize the traditional use of C. mucronatum and provide further insight into the anthelmintic activity of condensed tannins.
D. A. Sychev
Full Text Available The clinical significance of the patient genetic characteristics in the individual pharmacological response to oral anticoagulants is considered. Possible tactics of warfarin dosing and new oral anticoagulants choice on the basis of pharmacogenetic testing as well as indications for this approach in clinical practice are discussed. It should increase efficacy and safety of anticoagulant therapy.
Ali Niaz; Shah Syed; Shah Ismail; Ahmed Ghayour; Ghias Mehreen; Khan Imran
Abstract Background Saponins isolated from plant sources have a number of traditional and industrial applications. Saponins have pharmacological effects like anti-inflammatory, molluscicidal, antimicrobial, antispasmodic, antidiabetic, anticancer, anticonvulsant, anthelmintic, antitussive and cytotoxic activities. The current work describes the anthelmintic and cytotoxic activities of crude saponins of Achillea Wilhelmsii and Teucrium Stocksianum as these plants are rich with saponins. Method...
Stormorken, H; Gjemdal, T; Bjøro, K
Lupus anticoagulants (LA) are associated with various forms of thrombotic events. Of particular interest to obstetrics is the association with placental infarcts and habitual abortion. In the case described a near full-term viable infant was delivered subsequent to four early miscarriages. However, the mother had then developed an antifactor II antibody leading to grave hypoprothrombinemia with bleeding tendency, indicating efficient autoanticoagulation. This natural experiment indicates that these patients should receive anticoagulation during pregnancy, possibly in combination with steroids to depress the LA level. PMID:3139508
Rees, P; Grech, V
The insertion of a mechanical heart valve predisposes to thrombosis and embolism, and for this reason, individuals with mechanical valves who undergo dental/surgical procedures must take special precautions. In this article, we illustrate a protocol for anticoagulation during such procedures in individuals with mechanical valves. PMID:22368581
Feher, G; Illes, Z; Hargroves, D; Komoly, S
INTRODUCTION: Cerebral venous thrombosis (CVT) is a rare form of venous thromboembolism (VTE). Although anticoagulation is recommended for the initial and long term treatment with regards to thrombotic risks for patients with CVT, the role of anticogalution has not been fully elucidated. The aim of...
Allione, Alessandra; Di Gaetano, Cornelia; Dani, Nadia; Barberio, Davide; Sieri, Sabina; Krogh, Vittorio; Matullo, Giuseppe
Obesity is an important health problem worldwide. Adipose tissue acts as an endocrine organ that secretes various bioactive substances, called adipokines, including pro-inflammatory biomarkers such as TNF-α, IL-6, leptin and C-reactive protein (CRP) and anti-inflammatory molecules such as adiponectin. The deregulated production of adipokines in obesity is linked to the pathogenesis of various disease processes and monitoring their variation is critical to understand metabolic diseases. The aim of this study was to determine the plasma concentration of adipokines in healthy subjects by multiplexed measurements and the effect of anticoagulants on their levels. Plasma samples from 10 healthy donors were collected in two different anticoagulants (sodium citrate or heparin). All markers, excluding TNF-α, showed significantly higher concentrations in heparinized compared to citrate plasma. However, levels of adipokines in different plasma samples were highly correlated for most of these markers. We reported that different anticoagulants used in the preparation of the plasma samples affected the measurements of some adipokines. The importance of the present results in epidemiology is relevant when comparing different studies in which blood samples were collected with different anticoagulants. PMID:26945995
Bobek, M.; Boubelík, Michael; Fišerová, Anna; Luptovcová, Martina; Vannucci, Luca; Kacprzak, G.; Kolodzej, J.; Majewski, A.M.; Hoffman, R. M.
Roč. 47, č. 2 (2005), s. 215-223. ISSN 0169-5002 Institutional research plan: CEZ:AV0Z5052915 Keywords : anticoagulant drugs * lung cancer * NK cells Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 3.172, year: 2005
Becattini, Cecilia; Agnelli, Giancarlo
Venous thromboembolism (VTE) is a common disease associated with high risk for recurrences, death, and late sequelae, accounting for substantial health care costs. Anticoagulant agents are the mainstay of treatment for deep vein thrombosis and pulmonary embolism. The recent availability of oral anticoagulant agents that can be administered in fixed doses, without laboratory monitoring and dose adjustment, is a landmark change in the treatment of VTE. In Phase III trials, rivaroxaban, apixaban, edoxaban (antifactor Xa agents), and dabigatran (an antithrombin agent) were noninferior and probably safer than conventional anticoagulation therapy (low-molecular-weight heparin followed by vitamin K antagonists). These favorable results were confirmed in specific patient subgroups, such as the elderly and fragile. However, some patients, such as those with cancer or with intermediate- to high-risk pulmonary embolism, were underrepresented in the Phase III trials. Further clinical research is required before new oral anticoagulant agents can be considered standard of care for the full spectrum of patients with VTE. PMID:27102510
We report a patient who experienced a severe vertiginous episode with bilateral tinnitus and progressive right-sided hearing loss. She had Marfan's disease and was on anticoagulant treatment. The fluid in the labyrinth gave higher signal than cerebrospinal fluid on T1-weighted images, suggesting haemorrhage. The radiological follow-up is discussed. (orig.)
PAVÃO MAURO S. G.
Full Text Available Dermatan sulfates and heparin, similar to the mammalian glycosaminoglycans, but with differences in the degree and position of sulfation were previously isolated from the body of the ascidian Styela plicata and Ascidia nigra. These differences produce profound effects on their anticoagulant properties. S. plicata dermatan sulfate composed by 2-O-sulfatedalpha-L-iduronic acid and 4-O-sulfated N-acetyl-beta-D-galactosamine residues is a potent anticoagulant due to a high heparin cofactor II activity. Surprisingly, it has a lower potency to prevent thrombus formation on an experimental model and a lower bleeding effect in rats than the mammalian dermatan sulfate. In contrast, A. nigra dermatan sulfate, also enriched in 2-O-sulfated alpha-L-iduronic acid, but in this case sulfated at O-6 of the N-acetyl-beta-D-galactosamine units, has no in vitro or in vivo anticoagulant activity, does not prevent thrombus formation but shows a bleeding effect similar to the mammalian glycosaminoglycan. Ascidian heparin, composed by 2-O-sulfated alpha-L-iduronic acid, N- and 6-O-sulfated glucosamine (75% and alpha-L-iduronic acid, N- and 6-O-sulfated glucosamine (25% disaccharide units has an anticoagulant activity 10 times lower than the mammalian heparin, is about 20 times less potent in the inhibition of thrombin by antithrombin, but has the same heparin cofactor II activity as mammalian heparin.
Sara Nicole Fernández
Full Text Available Regional anticoagulation with citrate is an alternative to heparin in continuous renal replacement therapies, which may prolong circuit lifetime and decrease hemorrhagic complications. A retrospective comparative cohort study based on a prospective observational registry was conducted including critically ill children undergoing CRRT. Efficacy, measured as circuit survival, and secondary effects of heparin and citrate were compared. 12 patients on CRRT with citrate anticoagulation and 24 patients with heparin anticoagulation were analyzed. Median citrate dose was 2.6 mmol/L. Median calcium dose was 0.16 mEq/kg/h. Median heparin dose was 15 UI/kg/h. Median circuit survival was 48 hours with citrate and 31 hours with heparin (P=0.028. 66.6% of patients treated with citrate developed mild metabolic alkalosis, which was directly related to citrate dose. There were no cases of citrate intoxication: median total calcium/ionic calcium index (CaT/I of 2.16 and a maximum CaT/I of 2.33, without metabolic acidosis. In the citrate group, 45.5% of patients developed hypochloremia and 27.3% hypomagnesemia. In the heparin group, 27.8% developed hypophosphatemia. Three patients were moved from heparin to citrate to control postoperatory bleeding. In conclusion citrate is a safe and effective anticoagulation method for CRRT in children and it achieves longer circuit survival than heparin.
Fernández, Sara Nicole; Santiago, Maria José; López-Herce, Jesús; García, Miriam; Del Castillo, Jimena; Alcaraz, Andrés José; Bellón, Jose María
Regional anticoagulation with citrate is an alternative to heparin in continuous renal replacement therapies, which may prolong circuit lifetime and decrease hemorrhagic complications. A retrospective comparative cohort study based on a prospective observational registry was conducted including critically ill children undergoing CRRT. Efficacy, measured as circuit survival, and secondary effects of heparin and citrate were compared. 12 patients on CRRT with citrate anticoagulation and 24 patients with heparin anticoagulation were analyzed. Median citrate dose was 2.6 mmol/L. Median calcium dose was 0.16 mEq/kg/h. Median heparin dose was 15 UI/kg/h. Median circuit survival was 48 hours with citrate and 31 hours with heparin (P = 0.028). 66.6% of patients treated with citrate developed mild metabolic alkalosis, which was directly related to citrate dose. There were no cases of citrate intoxication: median total calcium/ionic calcium index (CaT/I) of 2.16 and a maximum CaT/I of 2.33, without metabolic acidosis. In the citrate group, 45.5% of patients developed hypochloremia and 27.3% hypomagnesemia. In the heparin group, 27.8% developed hypophosphatemia. Three patients were moved from heparin to citrate to control postoperatory bleeding. In conclusion citrate is a safe and effective anticoagulation method for CRRT in children and it achieves longer circuit survival than heparin. PMID:25157369
Rombouts, Eva Karolien
One of the causes of unstable anticoagulation is a variable vitamin K intake. The main objective of this thesis was to test the hypothesis that the INR is particularly sensitive to changes in vitamin K intake when vitamin K status is low, and that patients with a low vitamin K intake would therefore
Callonnec, F.; Gerardin, E.; Thiebot, J. [Department of Radiology, Rouen University Hospital, 1 rue de Germont, F-76031 Rouen cedex (France); Marie, J.P.; Andrieu Guitrancourt, J. [Department of Otolaryngology, Rouen University Hospital (France); Marsot-Dupuch, K. [Department of Radiology, St. Antoine, Paris University Hospital (France)
We report a patient who experienced a severe vertiginous episode with bilateral tinnitus and progressive right-sided hearing loss. She had Marfan`s disease and was on anticoagulant treatment. The fluid in the labyrinth gave higher signal than cerebrospinal fluid on T1-weighted images, suggesting haemorrhage. The radiological follow-up is discussed. (orig.) With 2 figs., 11 refs.
Verheugt Freek WA
Full Text Available Abstract Thrombosis plays a major role in acute vessel closure both after coronary balloon angioplasty and after stenting. This review will address the role of antiplatelet and anticoagulant therapy in preventing early thrombotic complications after percutaneous coronary intervention. The focus will be on agents that are routinely available and commonly used.
Eerenberg, E.S.; Kamphuisen, P.W.; Sijpkens, M.K.; Meijers, J.C.; Büller, H.R.; Levi, M.
Background: Rivaroxaban and dabigatran are new oral anticoagulants that both have been licensed worldwide for the treatment of atrial fibrillation and rivaroxaban also for venous thrombosis. Both drugs specifically inhibit one coagulation factor, factor Xa and thrombin, respectively, and both compou
Grech, Victor E.; Rees, P.
The insertion of a mechanical heart valve predisposes to thrombosis and embolism, and for this reason, individuals with mechanical valves who undergo dental/surgical procedures must take special precautions. In this article, we illustrate a protocol for anticoagulation during such procedures in individuals with mechanical valves.
Middleberg, Robert A; Homan, Joseph
Rodenticide anticoagulants are used in the control of rodent populations. In addition to accidental ingestions in humans, such agents have also been used for homicidal and suicidal purposes. There are two major groups of rodenticide anticoagulants - hydroxycoumarins and indanediones. Before the advent of LC-MS/MS, analysis for such agents was relegated to such techniques as TLC and HPLC with nonspecific modes of detection. LC-MS/MS has been used to determine any given number of rodenticide anticoagulants in animal tissues, foods, plasma, etc. Use of this technique allows for the simultaneous identification of individual compounds within both classes of rodenticide anticoagulants. The LC-MS/MS method presented allows for simultaneous qualitative identification of brodifacoum, bromadiolone, chlorphacinone, dicumarol, difenacoum, diphacinone, and warfarin in blood, serum, and plasma using ESI in the negative mode. Two transitions are monitored for each analyte after a simple sample preparation. Chromatographic separation is accomplished using a gradient of ammonium hydroxide in water and ammonium hydroxide in methanol. Chloro-warfarin is used as internal standard. PMID:22767114
Jespersen, Stine Funder; Christensen, Louisa M; Christensen, Anders;
Background. The knowledge is still sparse about patient related factors, influencing oral anticoagulation therapy (OAC) rates, in stroke patients with atrial fibrillation (AF). Aims. To assess the use of OAC in ischemic stroke patients diagnosed with AF and to identify patient related factors...
Coumarin derivatives such as acenocoumarol, phenprocoumon and warfarin are frequently used for the prevention of stroke and systemic embolism in patients with atrial fibrillation or for the treatment of venous thromboembolism. These oral anticoagulants have a narrow therapeutic range and a large var
Harder, Achim; Schmitt-Wrede, Hans-Peter; Krücken, Jürgen; Marinovski, Predrag; Wunderlich, Frank; Willson, James; Amliwala, Kiran; Holden-Dye, Lindy; Walker, Robert
There are three major classes of anthelmintics for veterinary use: the benzimidazoles/prebenzimidazoles, the tetrahydropyrimidines/imidazothiazoles, and the macrocyclic lactones. In nematodes, there are five targets for the existing anthelmintics: the nicotinergic acetylcholine receptor which is the target of tetrahydropyrimidines/imidazothiazoles and indirectly that of the acetylcholineesterase inhibitors; the GABA receptor which is the target of piperazine, the glutamate-gated chloride channel as the target of the macrocyclic lactones, and beta-tubulin as the target of prebenzimidazoles/benzimidazoles. All these anthelmintics are now in serious danger because of the worldwide spread of resistant nematodes in sheep, cattle, horses and pigs. The class of cyclooctadepsipeptides has entered the scene of anthelmintic research in the early 1990s. PF1022A, the first anthelmintically active member, is a natural compound from the fungus Mycelia sterilia that belongs to the microflora of the leaves of the Camellia japonica. PF1022A contains 4 N-Methyl-L-leucines, 2 D-lactic acids and 2-D-phenyllactic acids arranged as a cyclic octadepsipeptide with an alternating L-D-L-configuration. Emodepside is a semisynthetic derivative of PF1022A with a morpholine ring at each of the two D-phenyllactic acids in para position. The anthelmintic activity is directed against gastrointestinal nematodes in chicken, mice, rats, meriones, dogs, cats, sheep, cattle and horses. Moreover, emodepside is active against Trichinella spiralis larvae in muscles, microfilariae and preadult filariae and Dictyocaulus viviparus. PF1022A and emodepside are fully effective against benzimidazole-, levamisole or ivermectin-resistant nematodes in sheep and cattle. In Ascaris suum both cyclooctadepsipeptides lead to paralysis indicating a neuropharmacological action of these compounds. Using a PF1022A-ligand immunoscreening of a cDNA library from Haemonchus contortus a cDNA clone of 3569 base pairs could be
At present, goat farming, either as a full-time or part-time activity, is in increasingly being recognized as an economically beneficial livestock enterprise in tropical and sub tropical countries. Despite this popularity of goat industry, several constraints have limited the full potential of this farming activity in these countries. Among the multitude of impediments, which limit the development of the goat industry, gastrointestinal nematode infection represents a major constraint in Sri Lanka like in other parts of the tropics. Recent studies in Sri Lanka have shown, gastrointestinal nematode infections decrease the productivity, particularly weight gain in meat goats in the dry zone. The work done in dry zone of Sri Lanka has indicated that an overwhelming majority (99%) of goats were affected by a moderate to high gastrointestinal nematode infection. Successful control gastrointestinal nematodiasis infection is important for the sustainable productivity of the goat industry. The control of gastrointestinal nematodiasis is usually performed using synthetic anthelmintics. The appearance of nematode resistance to these anthelmintics and several other factors highlight the need to developing alternatives. This stimulated the research of alternatives, such as medicinal plants to control gastrointestinal nematodiasis. According to circumstances and depending on their efficacy, naturally produced plant anthelmintics offer an alternative that can overcome some of these problems and is both sustainable and environmentally acceptable. Fifteen plant extracts were screened using an in vitro larval migration inhibition (LMI) assay. Out of the fifteen crude extracts Azadiractha indica (neem) seed (NS), Areca catechu(areca-nut) unripe fruit kernel(AUFK), Adhatoda vasica (pavatta-adathoda) leaves (PL), caused a significant(P 0.05). ANUFK and PL extracts at the dose rates used was effective in controlling the GI nematodiasis in goats. ANUFK and PL could be used in control
Fischer, Juliane K; Hinney, Barbara; Denwood, Matthew J; Traversa, Donato; von Samson-Himmelstjerna, Georg; Clausen, Peter-Henning
Cyathostomins are currently the most common internal parasites of horses. With the intensive use of anthelmintic drugs over the past decades, resistance of cyathostomins to anthelmintics is becoming a growing problem in many countries. The aim of this study was to assess the current situation on horse farms in the German federal state of Brandenburg. A pre-selected population of horses from 24 premises that had shown a prevalence of cyathostomins higher than the average in a previous study was examined for anthelmintic efficacy. Faecal egg count reduction tests (FECRTs) were performed for ivermectin (IVM) and pyrantel (PYR). For IVM, the egg reappearance period (ERP) was also examined, as a shortened ERP can be indicative of developing resistance. The efficacy of IVM on cyathostomins was high: 99.1 % of 224 horses had a zero egg count 14 days after treatment. No shortening of the ERP was detected. For the data of the FECRT for PYR, three different methods of calculation were employed: (a) the method as recommended by the World Association for the Advancement of Veterinary Parasitology (WAAVP), (b) a bootstrapping method and (c) a Markov chain Monte Carlo method. Two methods of interpretation for these data were used: Resistance was declared (a) when FECR was <90 % and the lower 95 % confidence interval (LCL) <80 % and (b) when additionally the upper 95 % confidence level (UCL) was <95 %. When applying the first interpretation, resistance against PYR was found on four yards, while, when considering the UCL, all three methods for calculation only detected resistance on one single yard. Twelve species of cyathostomins were detected in larval cultures derived from strongyle egg positive faecal samples collected 14 days after treatment with PYR by reverse line blot hybridization (RLB). In order to generate comparable data, it is suggested to establish international standards for the calculation of FECRT data. PMID:26337266
Walker, R S; Miller, J E; Monlezun, C J; LaMay, D; Navarre, C; Ensley, D
Gastrointestinal nematode (GIN) parasite control recommendations are in a state of flux because of the increase in anthelmintic resistant cattle parasites, such as Cooperia spp. In addition, Cooperia spp. infection is typically high in warm-season grass pastures and can affect growth performance of grazing stocker calves in the Gulf Coast Region. This study evaluated the effects of moxidectin pour-on, oxfendazole oral suspension, or a combination of the two given at separate times on infection and performance of weaned beef calves grazing summer forages. Steers (n=42) and heifers (n=31) were stratified by sex, d-11 fecal egg count (FEC), and d-1 shrunk body weight (BW) to one of 10 pastures with four anthelmintic treatments and one control. Treatments included: (1) oxfendazole given on d 0 and moxidectin on d 73 (O+M), (2) moxidectin given on d 0 and oxfendazole on d 73 (M+O), (3) moxidectin given on d 0 (M), (4) oxfendazole given on d 0 (O) and (5) no anthelmintic given (CON). Calves grazed for d-110 beginning May 27th. Response variables were FEC (collected on d-11, 14, 31, 45, 59, 73, 87 and 108), coprocultures (evaluated for d 87 and 108), final shrunk BW, shrunk BW gain, average daily gain (ADG), and full BW gain (collected on d 31, 59, 73, 87, and 108). Calves treated with either oxfendazole (O+M and O) or moxidectin (M+O and M) on d 0 had significantly lower (Pparasite control and improve animal gains for stocker calves grazing warm-season grass pastures. PMID:23953143
Muhammad Arfan Zaman*§, Zafar Iqbal, Muhammad Nisar Khan and Ghulam Muhammad1
Full Text Available This study was carried out to evaluate the anthelmintic activity of a herbal formulation (HF based on aqueous extracts of leaves of Azadirachta indica and Nicotiana tabacum, flowers of Calotropis procera and seeds of Trachyspermum ammi. In vitro, eggs and adult Haemonchus contortus were exposed to different concentrations of HF following the standard procedures of egg hatch test (EHT; 50 to 0.024414 mg ml-1 and adult motility assay (AMA; 200-0.1953125mg ml-1, respectively. The reference drugs used in the study were oxfendazole (0.0056704 to 0.0000027 mg ml-1 and levamisole (1.50 mg ml-1 for EHT and AMA, respectively. In vivo, pre and post-treatment (4 mg, 2 mg and 500 µg kg-1 body weight fecal egg counts were determined following standard fecal egg count reduction test in sheep naturally parasitized with mixed species of gastrointestinal nematodes. In EHT, LC50 values of HF and oxfendazole (reference drug were 275.1 and 0.016 µg ml-1, respectively. In AMA, 100% mortality of H. contortus was observed 6 hr post-exposure to 3.125-200 mg ml-1 concentrations of HF and 2 hr post-exposure to levamisole. In vivo, maximum (96.2% fecal egg count (EPG reduction was recorded in sheep treated with HF @ 4 mg kg-1 body weight; whereas, 89.3% reduction in EPG was recorded in sheep treated with levamisole @ 7.5 mg kg-1 body weight. A graded dose response was noted in all the tests used in the present study to evaluate the anthelmintic activity of HF. Therefore, HF seems to be promising as an anthelmintic for animals. Large scale trials on efficacy and safety, however, are recommended before the HF is considered for commercialization in crude form.
Hernandez, Pablo Mejia; Salem, Abdelfattah Z M; Elghandour, Mona M M Y; Cipriano-Salazar, Moisés; Cruz-Lagunas, Blas; Camacho, Luis Miguel
Twenty Katahdin × Pelibuey crossbreed male lambs, 3 to 4 months of age and 24 ± 0.3 kg of body weight, were used to study the anthelmintic effects of administering extracts of Salix babylonica L. (SB) and Leucaena leucocephala Lam. (LL). Lambs had not been treated with anthelmintics previously and were randomly allocated into four groups of five lambs each in a completely randomized design. Treatments were as follows: control (lambs fed on total mixed ration without extracts), SB (as control plus S. babylonica L. extract at 30 ml/day), LL (as control plus L. leucocephala Lam. extract at 30 ml/day), and SBLL (as control plus 30 ml/day of S. babylonica L. and L. leucocephala Lam. extracts in a 1:1 (v/v) mixture) for 63 days. Extracts were orally administered before the 8:00 a.m. feeding to each lamb. Rectal fecal samples were collected from each lamb at day 22 (P1), day 43 (P2), and day 63 (P3) of the experiment. Adult worm and egg counts were determined in each fecal sample immediately after collection. Plant secondary metabolites of total phenolics, saponins, and the aqueous fraction were 50 % lower in the SB versus LL extracts. Overall, the oral administration of extracts has improved the egg and worm count reductions in lamb feces by 54, 47, and 40 % for LL, SB, and SBLL, respectively, versus the control lambs. Reductions of worm egg counts in lamb feces were higher (P < 0.05) in P2 and P3 versus P1. Extracts of SB and LL or possibly isolated bioactive compounds could be a promising alternative to conventional anthelmintics to treat gastrointestinal parasites of small ruminants. Such treatments could be used in control strategies against gastrointestinal nematodes in organic and conventional production systems. PMID:24077919
Full Text Available General Practitioners (GPs provide first contact care of children and pregnant mothers in the community. This study ascertained the prescribing pattern of anthelmintics to children and pregnant women by a sample of GPs from the district of Colombo. Two hundred medical practitioners engaged in full-time General Practice (100 urban and 100 rural, were selected randomly. A pre-tested interviewer-administered questionnaire was used to collect data. A total of 183 GPs aged between 26 and 72 years (median 38 participated with 94 coming from urban areas. Seventy percent of the GPs were male. Almost 13% of GPs from urban areas had a Postgraduate degree in comparison to 4.5% from the rural areas ( P < 0.05. Over 50% of GPs had 6-20 years of service and over 30% treated 16-30 patients daily. Seventy-three percent of GPs from rural areas accessed health-related reading material either daily or weekly in contrast to only 40% from urban areas ( P < 0.001. All GPs prescribed anthelmintics to children. Pyrantel pamoate was the preferred anthelmintic used for children by both groups. Approximately 55% and 64% of GPs from urban and rural areas, respectively, prescribed anthelmintics during pregnancy. A majority of GPs prescribed drugs after the first trimester. However, 25% from urban areas gave drugs during any trimester ( P < 0.001. Regression analysis revealed that GPs with postgraduate qualifications, those having frequent access to health-related material and those seeing more than 30 patients daily, prescribed anthelmintics to pregnant women more often. Although routine de-worming of pregnant women and children should occur through government antenatal and well-baby clinics, and through the schools de-worming programme, it may not happen due to various reasons. Thus, GPs play a vital role in achieving good coverage of anthelmintics among children and pregnant women. Making available clear national guidelines on prescribing anthelmintics in Sri Lanka would
Full Text Available Abstract Background Despite the high frequency with which adverse drug events (ADEs occur in outpatient settings, detailed information regarding these events remains limited. Anticoagulant drugs are associated with increased safety concerns and are commonly involved in outpatient ADEs. We therefore sought to evaluate ambulatory anticoagulation ADEs and the patient population in which they occurred within the Duke University Health System (Durham, NC, USA. Methods A retrospective chart review of ambulatory warfarin-related ADEs was conducted. An automated trigger surveillance system identified eligible events in ambulatory patients admitted with an International Normalized Ratio (INR >3 and administration of vitamin K. Event and patient characteristics were evaluated, and quality/process improvement strategies for ambulatory anticoagulation management are described. Results A total of 169 events in 167 patients were identified from December 1, 2006-June 30, 2008 and included in the study. A median supratherapeutic INR of 6.1 was noted, and roughly half of all events (52.1% were associated with a bleed. Nearly 74% of events resulted in a need for fresh frozen plasma; 64.8% of bleeds were classified as major. A total of 59.2% of events were at least partially responsible for hospital admission. Median patient age was 68 y (range 36-95 y with 24.9% initiating therapy within 3 months prior to the event. Of events with a prior documented patient visit (n = 157, 73.2% were seen at a Duke clinic or hospital within the previous month. Almost 80% of these patients had anticoagulation therapy addressed, but only 60.0% had a follow-up plan documented in the electronic note. Conclusions Ambulatory warfarin-related ADEs have significant patient and healthcare utilization consequences in the form of bleeding events and associated hospital admissions. Recommendations for improvement in anticoagulation management include use of information technology to assist
Charles H Greenberg
Full Text Available The mechanism for hemorrhage enlargement in the brain, a key determinant of patient outcome following hemorrhagic stroke, is unknown. We performed computer-based stochastic simulation of one proposed mechanism, in which hemorrhages grow in "domino" fashion via secondary shearing of neighboring vessel segments. Hemorrhages were simulated by creating an initial site of primary bleeding and an associated risk of secondary rupture at adjacent sites that decayed over time. Under particular combinations of parameters for likelihood of secondary rupture and time-dependent decay, a subset of lesions expanded, creating a bimodal distribution of microbleeds and macrobleeds. Systematic variation of the model to simulate anticoagulation yielded increases in both macrobleed occurrence (26.9%, 53.2%, and 70.0% of all hemorrhagic events under conditions simulating no, low-level, and high-level anticoagulation and final hemorrhage size (median volumes 111, 276, and 412 under the same three conditions, consistent with data from patients with anticoagulant-related brain hemorrhages. Reversal from simulated high-level anticoagulation to normal coagulation was able to reduce final hemorrhage size only if applied relatively early in the course of hemorrhage expansion. These findings suggest that a model based on a secondary shearing mechanism can account for some of the clinically observed properties of intracerebral hemorrhage, including the bimodal distribution of volumes and the enhanced hemorrhage growth seen with anticoagulation. Future iterations of this model may be useful for elucidating the effects of hemorrhage growth of factors related to secondary shearing (such as small vessel pathology or time-dependent decay (such as hemostatic agents.
Pengo, Vittorio; Pegoraro, Cinzia; Cucchini, Umberto; Iliceto, Sabino
A multicenter, observational, retrospective, cross-sectional study of patients, receiving oral anticoagulation therapy (OAT) for stroke prophylaxis in chronic non-valvular atrial fibrillation (NVAF) was conducted in the US, Canada, France, Italy and Spain according to their predominant model of care [routine medical care (RMC) or Anticoagulation Clinic care (ACC)]. The study objectives were to assess anticoagulation control (time in target range), and to describe the features of the local model of care. Consecutive patients were recruited on the basis of a minimum of 60 days of oral anticoagulant treatment over a 12 month period, and clinic and physician details were captured by means of a structured face-to-face or telephone interview. Time in therapeutic range (TTR) was calculated by using linear interpolation between INR values. A total of 1511 patients were recruited, of whom 1445 were included in the analysis of TTR. TTR was higher in ACC (69.5% and 64.9% for Italy and Spain, respectively) with respect to RMC (58.1%, 62.8% and 59.3% for the US, Canada and France, respectively). Mean intervals between INR determinations were between 3 and 4 weeks. Dose changes in case of INR outside therapeutic range were more frequent in Spain and less frequent in France. Striking differences were observed in type of VKA used, specialists involved in patient management, and dosage instructions. Studying of anticoagulation management based on local models of care highlights important discrepancies among countries and suggests further standardization of the management of this important therapy is necessary. PMID:16475046
Keegan, Jemma Louise
Several surface plasmon resonance (SPR) biosensor assays were developed and validated for the detection of anthelmintic veterinary drugs in liver tissue and milk using a QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) extraction procedure. The first screening assay was developed to detect 11 benzimidazole carbamates in milk and liver. In bovine milk the assay showed a limit of detection (LOD) of 2.7 μg kg-1 and a detection capability (CCβ) of 5 μg kg-1. Analyte recovery was in th...
Prashant Tiwari; Bimlesh Kumar; Manoj Kumar; Mandeep Kaur; Pardeep Sharma; Jiban Debnath
The present study aimed at the in-vitro evaluation of anthelmintic activity of aqueous and ethanolic extracts of stem of Tinospora cordifolia using Eisenia foetida at four different concentrations (10, 25, 50 and 100 mg/ml) respectively. The study involved the determination of time of paralysis (P) and time of death (D) of the worms. At the concentration of 100 mg/ml both the ethanolic and the aqueous extracts exhibited very significant activities as compared to the standard drug piperazine c...
D'Souza, Marina G.; Bheemappa, Eswarappa; Pai, Vasantakumar K.; Byahatti, Vivek V.; Tule, Chandramouli
The present study has been undertaken to screen the anthelmintic potential of aqueous root extracts of Aristolochia indica Linn. and A. tagala Cham. against adult Indian earthworm Pheritima posthuma and round worms Ascaridia galli. Different concentrations of the extracts ranging from 2-8 mg/mL were screened. Piperazine citrate was used as reference standard. Extract of A. tagala was found to be more potent and effective at the dose level of 2 mg/mL compared to the extract of A. indica. Extra...
Li NAN; Weichao YANG; Yongqian LIU; Hui XU; Ying LI; Manqi L(U); Ke YANG
A preliminary study was made on the antibacterial mechanism of copper-bearing antibacterial stainless steels against E.coli through experiments of microbiology such as EDTA (ethylenediaminetetraacetic acid) complex- ing, DNA smearing and AFM (atomic force microscope) observation. It was measured that the antibacterial stainless steels showed excellent antibacterial functions with antibacterial rate to E.coli over 99.99%. The antibacterial rate was weak if the bacteria solution was complexed by EDTA, indicating that the copper ions play a dominant role in the antibacterial effect of the antibacterial stainless steels. The electrophoresis experi- ment did not show the phenomenon of DNA smearing for E.coli after contacting antibacterial stainless steels, which meant that DNA of E.coli was not obviously damaged. It was observed by AFM that the morphology of E.coli changed a lot after contacting antibacterial stainless steels, such as cell walls being seriously changed and lots of contents in the cells being leaked.
Aiello, Allison E.; Marshall, Bonnie; Levy, Stuart B.; Della-Latta, Phyllis; Lin, Susan X.; Larson, Elaine
We examined whether household use of antibacterial cleaning and hygiene products is an emerging risk factor for carriage of antimicrobial drug–resistant bacteria on hands of household members. Households (N = 224) were randomized to use of antibacterial or nonantibacterial cleaning and hygiene products for 1 year. Logistic regression was used to assess the influence of antibacterial product use in homes. Antibacterial product use did not lead to a significant increase in antimicrobial drug re...
Ke YANG; Manqi L(U)
An austenitic antibacterial stainless steel is reported in this paper. The very fine and dispersive ε-Cu precipitations in the matrix of the antibacterial steel after the antibacterial treatment endow the steel with antibacterial function. The antibacterial function is strong, long-term and broad-spectrum, and can be maintained even after repeated wear and long time dipping in water. The steel is safe for human body and could be used widely in daily application.
Chambers, Henry F.; Bartlett, John G.; Bonomo, Robert A.; Chiou, Christine; Cosgrove, Sara E.; CROSS, HEATHER R.; Daum, Robert S.; Downing, Michele; Evans, Scott R.; Knisely, Jane; Kreiswirth, Barry N.; Lautenbach, Ebbing; Mickley, Brenda S.; Patel, Robin; Pettigrew, Melinda M.
The Antibacterial Resistance Leadership Group (ARLG) is tasked with prioritizing, designing, implementing, and conducting clinical studies to address antibacterial resistance. This article outlines clinical research resources and opportunities made available by ARLG and encourages submission of proposals that address antibacterial resistance.
Keyyu, J D; Kyvsgaard, N C; Kassuku, A A; Willingham, A L
Worm control practices and anthelmintic usage in 177 cattle farms in Iringa district in the southern highlands of Tanzania was determined through a questionnaire survey. A total of 76 traditional, 92 small-scale dairy and 9 large-scale dairy cattle farms were included in the survey. Results indicated that 87.7% traditional, 97.8% small-scale dairy and 100% large-scale farmers relied solely on the use of anthelmintics, 2.7% traditional farmers used traditional medicines while 9.6% traditional farmers had not any form of worm control practice. Worm infection was ranked the second most important constraint of productivity in cattle in the three production systems. Most farms (57.6% traditional, 35.8% small-scale dairy, 66.7% large-scale dairy) used anthelmintics with a combination of levamisole and oxyclozanide. Benzimidazoles were used only in traditional (25.4%) and small-scale dairy (32.1%) farms while nitroxynil (Trodax) was mostly used in large-scale dairy farms (33.3%). Generally, 40% of farmers treated three or four times a year and the frequency in some farms was surprisingly high for resource poor small-scale farmers. The frequency of anthelmintic treatment was mostly the same regardless of the management system. Treatments in most farms depended on availability of money and drugs and not the epidemiology of parasites. A significant proportion (46.3%, P=0.007) of farmers especially in rural areas failed to follow their pre-planned treatment schedules due to lack of money (86%) and unavailability of drugs (6.6%). Many farmers (58.9%) had used the same type of anthelmintic for four or more consecutive years and 85.3% of them would continue with the same anthelmintic. Farmers in all management systems mostly purchased anthelmintics from private veterinary drug shops and about 43% traditional and 33.3% small-scale dairy farmers mostly in rural areas obtained anthelmintics from village extension officers. Despite the fact that all farmers were aware of worm
Full Text Available Abstract Background Soil-transmitted helminth (STH infections are responsible for a huge public health burden, however treatment options are limited. The discovery and development of novel efficacious drugs or drug combinations for the treatment of STH infections therefore has a high research priority. Methods We studied drug combination effects using the main standard anthelmintics, albendazole, mebendazole, levamisole, pyrantel pamoate and ivermectin in the Trichuris muris model. Drug combinations were first tested in vitro and additive and synergistic combinations investigated further in vivo in female mice using ratios based on the ED50 of the respective drugs. Results In vitro all 10 combinations of the standard anthelmintics tested against T. muris revealed synergistic behavior. We identified three drug combinations in vivo as strongly synergistic, namely mebendazole-ivermectin (Combination index (CI=0.16, mebendazole-levamisole (CI=0.17 and albendazole-mebendazole (CI=0.23. For albendazole-ivermectin, moderate synergism was observed (CI=0.81 and for albendazole-levamisole a nearly additive effect was documented (CI=0.93 in vivo. Five combinations (albendazole-pyrantel pamoate, mebendazole-pyrantel pamoate, levamisole-pyrantel pamoate, levamisole-ivermectin and pyrantel pamoate-ivermectin were antagonistic in vivo. Conclusion Our results strengthen the evidence that combination chemotherapy might play a role in the treatment of Trichuris infections. Albendazole-mebendazole should be studied in greater detail in preclinical studies.
Full Text Available The present study aimed at the in-vitro evaluation of anthelmintic activity of aqueous and ethanolic extracts of stem of Tinospora cordifolia using Eisenia foetida at four different concentrations (10, 25, 50 and 100 mg/ml respectively. The study involved the determination of time of paralysis (P and time of death (D of the worms. At the concentration of 100 mg/ml both the ethanolic and the aqueous extracts exhibited very significant activities as compared to the standard drug piperazine citrate (10 mg/ml. The time of paralysis and death was recorded as 9 ± 0.57 and 15.83 ± 0.60 in case of aqueous extract, on the other hand it was recorded as 4.16 ± 0.30 and 10.83 ± 0.60 in case of ethanolic extracts. In conclusion, the use of stem of Tinospora cordifolia as an anthelmintic have been confirmed and further studies are suggested to isolate the active principles responsible for the activity
Full Text Available Pineapple is a favorite for the lovers of fruit in its fresh forms as well as in preserves like jams, jellies and squashes. Two varieties of Pineapples (Queen and Kew are available in Tripura during mid-May to mid-September. The plant is well known for its different folk medicines like the root and fruit are either eaten or applied topically as an anti-inflammatory, digestive and anthelmintic. It was observed that the people of Tripura especially the Tribes are use the juice of matured root or fruit in worm. Research shows that, mainly bromelain is responsible for all its therapeutic activity.The agriculture of Tripura, each year, gets a special boost from pineapple production between the middle of May and middle of September, both inclusive. Pineapple’s leaves are used as the source of a textile fiber and are employed as a component of wall paper and furnishings, amongst other uses. This allows the crop to contribute a significant proportion in the economy of the state.The present study was carried out to evaluate the anthelmintic activity of fruit extract (Aqueous of Pineapple using Indian earthworm (Pheretima posthuma.All the extracts were found not only to paralysis (vermifuge but also to kill the earthworms (vermicidal. But the concentration of 40mg/ml fruit extract showed the maximum effect in respect of 20 and 10 mg/ml.
Luoga, W; Mansur, F; Buttle, D J; Duce, I R; Garnett, M C; Lowe, A; Behnke, J M
We examined the in vitro and in vivo efficacy of plant cysteine proteinases (CPs) derived from pineapple (Ananas comosus) and kiwi fruit (Actinidia deliciosa), and compared their efficacy as anthelmintics to the known effects of CPs from the latex of papaya (Carica papaya) against the rodent intestinal nematode, Heligmosomoides bakeri. Both fruit bromelain and stem bromelain had significant in vitro detrimental effects on H. bakeri but in comparison, actinidain from kiwi fruit had very little effect. However, in vivo trials indicated far less efficacy of stem bromelain and fruit bromelain than that expected from the in vitro experiments (24.5% and 22.4% reduction in worm burdens, respectively) against H. bakeri. Scanning electron microscopy revealed signs of cuticular damage on worms incubated in fruit bromelain, stem bromelain and actinidain, but this was far less extensive than on those incubated in papaya latex supernatant. We conclude that, on the basis of presently available data, CPs derived from pineapples and kiwi fruits are not suitable for development as novel anthelmintics for intestinal nematode infections. PMID:24176056
Mansur, F; Luoga, W; Buttle, D J; Duce, I R; Lowe, A; Behnke, J M
Hymenolepis diminuta is a natural parasite of the common brown rat Rattus norvegicus, and provides a convenient model system for the assessment of the anthelmintic activity of novel drugs against cestodes. The experiments described in this paper indicate that treatment of rats infected with H. diminuta with a supernatant extract of papaya latex, containing a mixture of four cysteine proteinases, was moderately efficacious, resulting in a significant, but relatively small, reduction in worm burden and biomass. However, faecal egg output was not affected by treatment. In our experiments these effects were only partially dose-dependent, although specific inhibition by E-64 confirmed the role of cysteine proteinases as the active principles in papaya latex affecting worm growth but not statistically reducing worm burden. Data collected for a further 7 days after treatment indicated that the effects of papaya latex supernatant on worm loss and on worm growth were not enhanced. Our findings provide a starting point for further refinement in formulation and delivery, or assessment of alternative natural plant-derived cysteine proteinases in efforts to develop these naturally occurring enzymes into broad-spectrum anthelmintics, with efficacy against cestodes as well as nematodes. PMID:25761568
Donnan Alison A
Full Text Available Abstract Background The cysteine proteinases in papaya latex have been shown to have potent anthelmintic properties in monogastric hosts such as rodents, pigs and humans, but this has not been demonstrated in ruminants. Methods In two experiments, sheep were infected concurrently with 5,000 infective larvae of Haemonchus contortus and 10,000 infective larvae of Trichostrongylus colubriformis and were then treated with the supernatant from a suspension of papaya latex from day 28 to day 32 post-infection. Faecal egg counts were monitored from a week before treatment until the end of the experiment and worm burdens were assessed on day 35 post-infection. Results We found that the soluble fraction of papaya latex had a potent in vivo effect on the abomasal nematode H. contortus, but not on the small intestinal nematode T. colubriformis. This effect was dose-dependent and at tolerated levels of gavage with papaya latex (117 μmol of active papaya latex supernatant for 4 days, the H. contortus worm burdens were reduced by 98%. Repeated treatment, daily for 4 days, was more effective than a single dose, but efficacy was not enhanced by concurrent treatment with the antacid cimetidine. Conclusions Our results provide support for the idea that cysteine proteinases derived from papaya latex may be developed into novel anthelmintics for the treatment of lumenal stages of gastro-intestinal nematode infections in sheep, particularly those parasitizing the abomasum.
Tsiboukis, D; Sazakli, E; Jelastopulu, E; Leotsinidis, M
Anthelmintics, such as benzimidazoles and probenzimidazoles, are veterinary drugs used against endoparasites in food producing animals. A number of these drugs are considered responsible for embryotoxicity and teratogenicity. The residue levels of Albendazole, Febantel, Fenbendazole, Mebendazole and some of their metabolites (Albendazole sulphoxide, Albendazole sulphone, Fenbendazole sulfone) were assessed in 123 (42 goat, 69 sheep, 12 bovine) raw milk samples collected from all farms throughout Southern Greece. Sample analysis was performed by HPLC with Diode Array Detector. A high percentage (27.6%) of the samples examined was found to be positive for the investigated compounds. In 14 samples (11.4%), the residues' concentration exceeded the established Maximum Residue Limits. Estimated Daily Intakes were calculated for a population of 723 children aged 10-12 years. Data on milk consumption were obtained by personal interview through a 7-day food frequency questionnaire. The maximum Estimated Daily Intakes for the anthelmintic residues, concerning raw milk, did not exceed the current Acceptable Daily Intake. PMID:23691580
Full Text Available Intestinal worms affect a host of individuals resulting in malnutrition, stunted growth, intellectual retardation and cognitive deficits. The aim of this study is to investigate the antihelminthic activity of Alstonia boonei De Wild (Apocynaceae and Vernonia amygdalina (Asteraceae using earth-worms (Lumbricus terretris. The worms were directly exposed to 50, 100, and 200 mg/ml of aque-ous and ethanolic bark extracts of Alstonia boonei and leaf extract of Vernonia amygdalina and piperazine citrate in a petri dish and in an organ bath. The control group was exposed to distilled water. The time of paralysis and death were determined within a period of 6 h in the petri dish method whiles spontaneous movements of the worms before and after drug administration were recorded on a slow moving kymograph drum in the organ bath method. All doses of the aqueous and ethanolic extracts significantly (P ≤ 0.001 reduced the time of paralysis and time of death compared to the vehicle treated group. The time of paralysis and time of death in the tissue bath method corresponded to that obtained by direct exposure. The extracts exhibited anthelmintic ac-tivity and thus could be an inexpensive and readily available source of anthelmintic treatment.
Andrew C. Kotze
Full Text Available Anthelmintic resistance has a great impact on livestock production systems worldwide, is an emerging concern in companion animal medicine, and represents a threat to our ongoing ability to control human soil-transmitted helminths. The Consortium for Anthelmintic Resistance and Susceptibility (CARS provides a forum for scientists to meet and discuss the latest developments in the search for molecular markers of anthelmintic resistance. Such markers are important for detecting drug resistant worm populations, and indicating the likely impact of the resistance on drug efficacy. The molecular basis of resistance is also important for understanding how anthelmintics work, and how drug resistant populations arise. Changes to target receptors, drug efflux and other biological processes can be involved. This paper reports on the CARS group meeting held in August 2013 in Perth, Australia. The latest knowledge on the development of molecular markers for resistance to each of the principal classes of anthelmintics is reviewed. The molecular basis of resistance is best understood for the benzimidazole group of compounds, and we examine recent work to translate this knowledge into useful diagnostics for field use. We examine recent candidate-gene and whole-genome approaches to understanding anthelmintic resistance and identify markers. We also look at drug transporters in terms of providing both useful markers for resistance, as well as opportunities to overcome resistance through the targeting of the transporters themselves with inhibitors. Finally, we describe the tools available for the application of the newest high-throughput sequencing technologies to the study of anthelmintic resistance.
Kotze, Andrew C.; Hunt, Peter W.; Skuce, Philip; von Samson-Himmelstjerna, Georg; Martin, Richard J.; Sager, Heinz; Krücken, Jürgen; Hodgkinson, Jane; Lespine, Anne; Jex, Aaron R.; Gilleard, John S.; Beech, Robin N.; Wolstenholme, Adrian J.; Demeler, Janina; Robertson, Alan P.; Charvet, Claude L.; Neveu, Cedric; Kaminsky, Ronald; Rufener, Lucien; Alberich, Melanie; Menez, Cecile; Prichard, Roger K.
Anthelmintic resistance has a great impact on livestock production systems worldwide, is an emerging concern in companion animal medicine, and represents a threat to our ongoing ability to control human soil-transmitted helminths. The Consortium for Anthelmintic Resistance and Susceptibility (CARS) provides a forum for scientists to meet and discuss the latest developments in the search for molecular markers of anthelmintic resistance. Such markers are important for detecting drug resistant worm populations, and indicating the likely impact of the resistance on drug efficacy. The molecular basis of resistance is also important for understanding how anthelmintics work, and how drug resistant populations arise. Changes to target receptors, drug efflux and other biological processes can be involved. This paper reports on the CARS group meeting held in August 2013 in Perth, Australia. The latest knowledge on the development of molecular markers for resistance to each of the principal classes of anthelmintics is reviewed. The molecular basis of resistance is best understood for the benzimidazole group of compounds, and we examine recent work to translate this knowledge into useful diagnostics for field use. We examine recent candidate-gene and whole-genome approaches to understanding anthelmintic resistance and identify markers. We also look at drug transporters in terms of providing both useful markers for resistance, as well as opportunities to overcome resistance through the targeting of the transporters themselves with inhibitors. Finally, we describe the tools available for the application of the newest high-throughput sequencing technologies to the study of anthelmintic resistance. PMID:25516826
Komuniecki, Richard; Law, Wen Jing; Jex, Aaron; Geldhof, Peter; Gray, John; Bamber, Bruce; Gasser, Robin B
This review is designed to summarize the information on monoamine-dependent paralysis as a target for anthelmintic development, examine the conservation of monoamine receptors in the genomes of both free-living and parasitic nematodes, and highlight the utility of the Caenorhabditis elegans model system for dissecting the monoaminergic modulation of locomotory decision-making. PMID:22343182
Golam Sarwar Raju
Conclusion: Since S. violaceum have shown antimicrobial, antioxidant, and anthelmintic activities, more studies such as anti-inflammatory, analgesic, antipyretic, and other pharmacological activities should be carried out to justify its traditional use, as the plant is available and used broadly in the rural areas for folkloric remedies.
WANG Jing; ZHANG Quanbin; ZHANG Zhongshan; HOU Yun; ZHANG Hong
Fucoidan, a group of sulfated heteropolysaccharides, was extracted from Laminariajaponica,an important economic alga species in China. The anticoagulant activity of fucoidan and its derivatives (including sulfated, phosphorylated, and aminated fucoidan) was examined using in-vitro anticoagulant systems. The correlation between chemical variations within the fucoidan group and anticoagulant activity was determined. The in-vitro anticoagulant properties of fucoidan and its derivatives were determined by measuring activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT).The results indicate anticoagulant activity in all samples using APTT and TT assays; however, only the fucoidan derivatives affected the PT assay. Thus, the fucoidan derivatives were able to inhibit both intrinsic and extrinsic blood coagulants. Fucoidan (FPS) and its derivatives presented better anticoagulant activity than low molecular weight fucoidan (DFPS) and its derivatives, suggesting that molecular weight and proper conformation are contributing factors for anticoagulant activity of polysaccharides. Amino groups have a positive charge and can thus change the charge density of fucoidan. Accordingly, among the tested samples, aminated fucoidan (NF) was the most active reflecting the importance of charge density for anticoagulant activity. Available data obtained using in-vitro models suggest that the sulfate content,sulfate/total-sugar ratio, molecular weight, and the substituted group of fucoidan are important factors for anticoagulant activity but that the influence of sulfate, phosphate and amino groups on anticoagulant activity was different.
Wang, Jing; Zhang, Quanbin; Zhang, Zhongshan; Hou, Yun; Zhang, Hong
Fucoidan, a group of sulfated heteropolysaccharides, was extracted from Laminaria japonica, an important economic alga species in China. The anticoagulant activity of fucoidan and its derivatives (including sulfated, phosphorylated, and aminated fucoidan) was examined using in-vitro anticoagulant systems. The correlation between chemical variations within the fucoidan group and anticoagulant activity was determined. The in-vitro anticoagulant properties of fucoidan and its derivatives were determined by measuring activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT). The results indicate anticoagulant activity in all samples using APTT and TT assays; however, only the fucoidan derivatives affected the PT assay. Thus, the fucoidan derivatives were able to inhibit both intrinsic and extrinsic blood coagulants. Fucoidan (FPS) and its derivatives presented better anticoagulant activity than low molecular weight fucoidan (DFPS) and its derivatives, suggesting that molecular weight and proper conformation are contributing factors for anticoagulant activity of polysaccharides. Amino groups have a positive charge and can thus change the charge density of fucoidan. Accordingly, among the tested samples, aminated fucoidan (NF) was the most active reflecting the importance of charge density for anticoagulant activity. Available data obtained using in-vitro models suggest that the sulfate content, sulfate/total-sugar ratio, molecular weight, and the substituted group of fucoidan are important factors for anticoagulant activity but that the influence of sulfate, phosphate and amino groups on anticoagulant activity was different.
Mickley, Frank; Geigenmüller, Grit; Schinköthe, Claudia
Equal safety and efficacy of direct oral anticoagulants as compared to vitamin K antagonists have been shown in elderly and very old patients. The use of these seem to have certain advantages in this special patient cohort: higher drug safety, no need for lab monitoring, less drug-drug interactions and a lower rate of intracranial hemorrhages. However, more data is needed to quantify the exact bleeding risk for geriatric patients. Elderly patients suffer quite frequently from significant comorbidities, such as renal failure, dementia, vision loss etc., which might put them at higher risk to suffer from medication side effects, especially bleeding complications. Routine clinical examinations combined with monitoring of renal function are therefore of paramount importance. Regarding these precautions the use of the new oral anticoagulants in the elderly is hence quite justified and rising. PMID:26625228
Summers, Richard L; Sterling, Sarah A
Direct oral anticoagulants (DOACs) offer clinical advantages over warfarin, such as minimal medication and food interactions and fixed dosing without the need for routine monitoring of coagulation status. As with all anticoagulants, bleeding, either spontaneous or provoked, is the most common complication. The long-term use of these drugs is increasing, and there is a crucial need for emergency medicine service professionals to understand the optimal management of associated bleeding. This review aims to describe the indications and pharmacokinetics of available DOACs; to discuss the risk of bleeding; to provide a treatment algorithm to manage DOAC-associated emergency bleeding; and to discuss future directions in bleeding management, including the role of specific reversal agents, such as the recently approved idarucizumab for reversal of the direct thrombin inhibitor dabigatran. Because air medical personnel are increasingly likely to encounter patients receiving DOACs, it is important that they have an understanding of how to manage patients with emergent bleeding. PMID:27255877
Amara, Walid; Larsen, Torben B; Sciaraffia, Elena; Hernández Madrid, Antonio; Chen, Jian; Estner, Heidi; Todd, Derick; Bongiorni, Maria G; Potpara, Tatjana S; Dagres, Nikolaos; Sagnol, Pascal; Blomstrom-Lundqvist, Carina
The purpose of this European Heart Rhythm Association survey was to assess the attitude, level of education, and knowledge concerning oral anticoagulants (OACs) among patients with atrial fibrillation (AF) taking vitamin K antagonists (VKAs), non-VKA oral anticoagulants (NOACs) or antiplatelets. A...... total of 1147 patients with AF [mean age 66 ± 13 years, 529 (45%) women] from 8 selected European countries responded to this survey. The overall use of OACs and antiplatelets was 77 and 15.3%, respectively. Of the patients taking OACs, 67% were on VKAs, 33% on NOACs, and 17.9% on a combination of OACs...... and antiplatelets. Among patients on VKAs, 91% correctly stated the target international normalized ratio (INR) level. The proportion of patients on VKA medication who were aware that monthly INR monitoring was required for this treatment and the proportion of patients on NOAC who knew that renal...
Menapace, Laurel A; McCrae, Keith R; Khorana, Alok A
The impact of venous thromboembolism (VTE) in the cancer population remains substantial despite significant advances in detecting and treating thrombotic events. While there is extensive literature regarding predictors of first VTE event in cancer patients as well as a validated predictive score, less data exist regarding recurrent VTE in cancer cohorts and associated predictive variables. A similar paucity of data in regard to bleeding events in cancer patients receiving anticoagulation has been observed. This review article will highlight clinical risk factors as well as predictive biomarkers associated with recurrent VTE and bleeding in cancer patients receiving therapeutic anticoagulation. Predictive risk assessment models for cancer-associated recurrent VTE and bleeding are also discussed. PMID:27067987
Nilsson, Hanna; Grove, E; Larsen, Torben Bjerregaard;
endpoints: all-cause mortality, major thromboembolism and bleeding events, percentage of time within therapeutic International Normalized Ratio (INR) target range (TTR) and variance of the INR value. Patient data was obtained from two databases in the two centers, where all data had been prospectively......Self-management of oral anticoagulant therapy in two centers: 11.000 patient-years of follow-up H Nilsson1,2,3, EL Grove2, TB Larsen3, M Maegaard1, TD Christensen1 1Department of Cardiothoracic and Vascular Surgery & Institute of Clinical Medicine, Aarhus University Hospital, Aarhus; 2Department of...... registered. Results: Results are pending but baseline characteristics (age, gender, indication for anticoagulant therapy) and data on all-cause mortality, major thromboembolism and bleeding events, TTR, INR-variance will be presented at the meeting. Conclusions: We hope to find a good quality of treatment...
Lee, C R; Thrasher, K A
The clinical significance of rifampin's induction of warfarin metabolism is well documented, but no published studies or case reports have quantified this interaction with respect to the international normalized ratio (INR). A patient receiving concomitant rifampin and warfarin to treat a mycobacterial infection and intraventricular thrombus, respectively, underwent routine INR testing at a pharmacist-managed anticoagulation clinic to assess his anticoagulation regimen. A 233% increase in warfarin dosage over 4 months proved insufficient to attain a therapeutic INR during long-term rifampin therapy More aggressive titration of the warfarin dosage was needed. In addition, a gradual 70% reduction in warfarin dosage over 4-5 weeks was necessary to maintain a therapeutic INR after rifampin discontinuation, demonstrating the clinically significant offset of this drug interaction. Extensive changes in warfarin dosage are required to attain and maintain a therapeutic INR during the initiation, maintenance, and discontinuation of rifampin. PMID:11601670
Cohen, I A; Hutchison, T A; Kirking, D M; Shue, M E
Medical records were retrospectively analyzed to evaluate the success of a pharmacist-managed Anticoagulation Surveillance Clinic (ASC). The 78 patients in group I were followed by the ASC. The 17 patients in Group II were followed by other Veterans Administration Medical Center clinics. Demographic characteristics, warfarin indication and potentially complicating conditions were comparable between the groups. Group I patients had shorter intervals between visits to the clinic than Group II patients. Although not statistically different compared to Group II, Group I patients had better prothrombin time control. Group I patients also had fewer complications per treatment year (6.9% vs 9.0%) and received fewer potentially interacting drugs. The ASC was at least as successful as the other clinics in managing patients on warfarin, and results compared very favorably to those reported in the literature for other anticoagulation clinics. PMID:4019790
Saeed, Wajeeha; Burke, James F; Mirrani, Ghazi; Sirinivasa, Minisha; Nabi, Usman; Hayat, Umar; Khan, Zubair; Sardar, Muhammad Rizwan
Atrial fibrillation (AF) is the most common arrhythmia and represents one-third of the arrhythmia-related hospital admissions in the developed countries. Embolic strokes associated with AF are more severe and disabling. Thromboembolic stroke prevention is a major goal in treatment of AF and Warfarin has successfully served this purpose for many years. Drug-drug interaction and regular monitoring with Warfarin pose a significant challenge where health care system has limited resources; and lack of a well-structured health system, hinders regular International Normalized Ratio (INR) monitoring. Novel oral anticoagulants (NOACs) have opened up a new exciting chapter in the field of anticoagulation in non-valvular atrial fibrillation (NVAF). This review discussed the landmark trials that led to the development of NOACs and explored the potentials of these new agents with simultaneous comparison of Warfarin. PMID:27504556
Dimova, Cena; Kovacevska, Ivona; Angelovska, Bistra
Aim of this study is to review the evidence of different therapy approach, to highlight the areas of major concern, and to suggest specific oral surgery treatment for patients on new oral anticoagulants. A Medline and an extensive hand search were performed on English-language publications beginning in 1971 till now. The pertinent literature and clinical protocols of hospital dentistry departments have been extensively reviewed, presented and discussed. Several evolving clinical practic...
Fontana, Pierre; Robert-Ebadi, Helia; Bounameaux, Henri; Boehlen, Françoise; Righini, Marc
In recent years, small oral compounds that specifically block activated coagulation factor X (FXa) or thrombin (FIIa) have become alternatives to the anticoagulants that had been used for several decades. As of today, these direct oral anticoagulants (DOACs) include dabigatran etexilate (thrombin inhibitor) and apixaban, edoxaban and rivaroxaban (inhibitors of FXa). While there is no doubt that DOACs represent a major step forward in the management of patients with venous thromboembolic disease and atrial fibrillation, new challenges have arisen. They need to be addressed with the necessary pragmatism on the basis of evidence. Indeed, a better understanding of the management of these last-generation antithrombotics will favour safer use and increase confidence of the practitioner for the prescription of these drugs. The aim of this article is to present practical suggestions for the prescription and use of these drugs in everyday clinical practice, based on clinical experience and recently updated recommendations of the European Heart Rhythm Association and the American College of Chest Physicians among other scientific organisations. We address issues such as pharmacokinetics, dosing, side effects, limitations of use, drug interactions, switching from and to other anticoagulants, renal function, concomitant administration of antiplatelet agents and perioperative use. We also address the issue of monitoring and reversal, taking advantage of the most recent development in this latter area. Rather than being one additional set of recommendations, our narrative review aims at assisting the practicing physician in his or her daily handling of these novel anticoagulant compounds, based on frequently asked questions to the authors, a group of experienced specialists in the field who have, however, no commitment to issue guidelines. PMID:26964028
Walmsley, T. A.; George, P M; Fowler, R. T.
AIMS: To determine if the iron in EDTA anticoagulated plasma samples can be measured by colorimetric assays using Ferrozine. METHODS: Paired samples of serum and EDTA plasma were obtained from 24 patients and analysed by three commercial iron methods. The EDTA plasmas were also analysed using methods modified by the addition of zinc sulphate or with different concentrations of Ferrozine. The iron contamination of EDTA sample tubes was measured by atomic absorption spectroscopy. RESULTS: Two c...
Hughes, Stephen; Szeki, Iren; Nash, Michael J; Thachil, Jecko
There is an increasing awareness about the risks of arterial and venous thromboembolism (TE) in hospital patients and general public which has led to consideration of thrombosis prevention measures in earnest. Early recognition of the symptoms of TE disease has led to timely administration of antiplatelet and anticoagulant drugs, translating to better outcome in many of these patients. In this respect, patients with chronic kidney disease (CKD) represent a special group. They indeed represent...
Konrad Jarząbek; Dawid Bąkowski; Beata Wożakowska-Kapłon
Atrial fibrillation is associated with a few folds higher risk of stroke. Traditional vitamin K antagonists used in the prevention of stroke in patients with non-valvular atrial fibrillation are often not efficient enough due to their interactions with a broad range of substances including medicines or food ingridients and problems with monitoring the treatment. New oral anticoagulants pose an alternative for the vitamin K antagonists. They are equally efficient in the prevention of stroke, ...
Akkari, Hafidh; Hajaji, Soumaya; B'chir, Fatma; Rekik, Mourad; Gharbi, Mohamed
Phenolic content, antioxidant and anthelmintic activities of herbal extracts are of particular interest to drug industry; plant extracts with significant anthelmintic activity have the potential to be used as alternatives to conventional chemical drugs. In the present study, Rubus ulmifolius fruit extracts obtained using solvents of increasing polarity (water, methanol, chloroform and hexane) were examined for their antioxidant and anthelmintic activities in correlation with their polyphenolic content. In vitro antioxidant activity of all extracts was carried out using free radical-scavenging activity by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethilenebenzotiazolin)-6-sulfonic acid (ABTS) radical cation. In vitro anthelmintic activities were investigated on the egg and adult worms of Haemonchus contortus from sheep in comparison to albendazole. Total polyphenol content of R. ulmifolius was higher in more polar extract, ranging from 64.5 in aqueous extract to 1.57mg gallic acid equivalents per gram of dry weight (GAE/g DW) in hexanic extract. Likewise, highest amounts of flavonoids and condensed tannins were found in aqueous extract (28.06mg QE/g and 7.42mg CE/g DW, respectively) compared to hexanic extract (0.71mg QE/g and 0.29mg CE/g DW, respectively) (ptannins content with scavenging of either DPPH (r=0.722, 0.764 and 0.752, p<0.01, respectively) or ABTS radicals (r=0.893, 0.765 and 0.722, p<0.01, respectively) and with inhibition of egg hatching (r=0.874, 0.883 and 0.862, p<0.01, respectively). Highest inhibition of motility (100%) of worms was observed 8h post-exposure in aqueous and methanolic extract at 8mg/mL. To our knowledge, these results depict for the first time that R. ulmifolius possesses in vitro anthelmintic properties. PMID:27084470
Wondu Dagnaw; Alemayehu Mekonnen
Objective:To investigate phytochemicals constituents and check the anthelmintic activities of Maesa lanceolata (M. lanceolata) solvent extracts against aquatic leech. Methods: Several phytochemicals were tested and screened from petroleum ether, chloroform and methanol extracts ofM. lanceolata extracts and their anthelmintic activities were done based on the standard procedure against aquatic leech. Piperazine citrate (20 mg/mL) was used as a reference standard while distilled water was used as a control. Results:Qualitative phytochemical analysis of different solvent (petroleum ether, chloroform and methanol) extracts ofM. lanceolata revealed the presence of flavonoids and alkaloids in chloroform extracts and alkaloids in methanol extracts. In addition to the qualitative analysis of the plant extracts, the anthelmintic effects were also evaluated against aquatic leech (Lymnatis nilotica). Accordingly, various concentrations (10, 20, 40 and 60 mg/mL) of each solvent (petroleum ether, chloroform and methanol) extracts and 20 mg/mL of standard drug were prepared and tested against the selected leech. All the tested concentrations showed anthelmintic activities in a dose-dependent manner. From petroleum ether, chloroform and methanol extracts, chloroform extracts with 60 mg/mL concentration was effective with the paralytic time of (29.00 ± 1.06) min and death time of (65.00 ± 2.00) min in gradient extraction method. But in the case of extraction without gradient method, methanol extracts with 60 mg/mL concentration showed effective paralysis and death time (26.00 ± 1.73) and (56.00 ± 1.56) min, respectively, against the selected aquatic leech. Conclusions:The present study revealed thatM. lanceolata extracts have magic anthelmintic activities which are helpful to treat aquatic leeches (Lymnatis nilotica) which are associated with the nasal cavities of animals and human beings.
Full Text Available Gastrointestinal nematodes resistant to anthelmintics have been reported in several regions of Brazil, and they may be associated with economic losses for the cattle industry. This study aimed to evaluate the resistance status of gastrointestinal nematodes from naturally infected beef cattle to several commercially available anthelmintics, as well as to test the efficacy of combinations of anthelmintics against multi-resistant gastrointestinal nematodes. Ten farms located in Rio Grande do Sul state were selected by: farmers' consent; extensive raising system; availability of calves aged from 7 to 9 months naturally infected by gastrointestinal nematodes; absence of anthelmintic treatment for 60 days before the study; and presence of 70–100 calves or more of both genders with ≥200 eggs per gram of feces (EPG (sensitivity of 50 EPG. These calves were distributed into 10 groups (of 7–10 animals per farm and treated with ivermectin, doramectin, eprinomectin, fenbendazole, closantel, nitroxynil, disophenol, levamisole, albendazole, or moxidectin. Feces were collected 2 days before treatment and 14 days after treatment. Additional groups of 7–10 calves were used to test six different two-drug combinations at four of the studied farms. In general terms, fenbendazole was the most effective drug, followed by levamisole, disophenol, and moxidectin. However, parasite resistance to multiple drugs was found in all herds, especially in the genera Cooperia spp., Trichostrongylus spp., and Haemonchus spp.. Some of the two-drug combinations were effective against nematode populations identified as resistant to the same compounds when used as single drugs. The most effective combinations were moxidectin + levamisole, doramectin + fenbendazole, and levamisole + closantel. In this study, parasites resistant to the main commercially available anthelmintics were found in all herds, and some combinations of two active components belonging to different
Ramos, Fernanda; Portella, Luiza Pires; Rodrigues, Fernando de Souza; Reginato, Caroline Zamperete; Pötter, Luciana; Cezar, Alfredo Skrebsky; Sangioni, Luís Antônio; Vogel, Fernanda Silveira Flores
Gastrointestinal nematodes resistant to anthelmintics have been reported in several regions of Brazil, and they may be associated with economic losses for the cattle industry. This study aimed to evaluate the resistance status of gastrointestinal nematodes from naturally infected beef cattle to several commercially available anthelmintics, as well as to test the efficacy of combinations of anthelmintics against multi-resistant gastrointestinal nematodes. Ten farms located in Rio Grande do Sul state were selected by: farmers' consent; extensive raising system; availability of calves aged from 7 to 9 months naturally infected by gastrointestinal nematodes; absence of anthelmintic treatment for 60 days before the study; and presence of 70-100 calves or more of both genders with ≥200 eggs per gram of feces (EPG) (sensitivity of 50 EPG). These calves were distributed into 10 groups (of 7-10 animals) per farm and treated with ivermectin, doramectin, eprinomectin, fenbendazole, closantel, nitroxynil, disophenol, levamisole, albendazole, or moxidectin. Feces were collected 2 days before treatment and 14 days after treatment. Additional groups of 7-10 calves were used to test six different two-drug combinations at four of the studied farms. In general terms, fenbendazole was the most effective drug, followed by levamisole, disophenol, and moxidectin. However, parasite resistance to multiple drugs was found in all herds, especially in the genera Cooperia spp., Trichostrongylus spp., and Haemonchus spp.. Some of the two-drug combinations were effective against nematode populations identified as resistant to the same compounds when used as single drugs. The most effective combinations were moxidectin + levamisole, doramectin + fenbendazole, and levamisole + closantel. In this study, parasites resistant to the main commercially available anthelmintics were found in all herds, and some combinations of two active components belonging to different chemical groups were
Ramos, Fernanda; Portella, Luiza Pires; Rodrigues, Fernando de Souza; Reginato, Caroline Zamperete; Pötter, Luciana; Cezar, Alfredo Skrebsky; Sangioni, Luís Antônio; Vogel, Fernanda Silveira Flores
Gastrointestinal nematodes resistant to anthelmintics have been reported in several regions of Brazil, and they may be associated with economic losses for the cattle industry. This study aimed to evaluate the resistance status of gastrointestinal nematodes from naturally infected beef cattle to several commercially available anthelmintics, as well as to test the efficacy of combinations of anthelmintics against multi-resistant gastrointestinal nematodes. Ten farms located in Rio Grande do Sul state were selected by: farmers' consent; extensive raising system; availability of calves aged from 7 to 9 months naturally infected by gastrointestinal nematodes; absence of anthelmintic treatment for 60 days before the study; and presence of 70–100 calves or more of both genders with ≥200 eggs per gram of feces (EPG) (sensitivity of 50 EPG). These calves were distributed into 10 groups (of 7–10 animals) per farm and treated with ivermectin, doramectin, eprinomectin, fenbendazole, closantel, nitroxynil, disophenol, levamisole, albendazole, or moxidectin. Feces were collected 2 days before treatment and 14 days after treatment. Additional groups of 7–10 calves were used to test six different two-drug combinations at four of the studied farms. In general terms, fenbendazole was the most effective drug, followed by levamisole, disophenol, and moxidectin. However, parasite resistance to multiple drugs was found in all herds, especially in the genera Cooperia spp., Trichostrongylus spp., and Haemonchus spp.. Some of the two-drug combinations were effective against nematode populations identified as resistant to the same compounds when used as single drugs. The most effective combinations were moxidectin + levamisole, doramectin + fenbendazole, and levamisole + closantel. In this study, parasites resistant to the main commercially available anthelmintics were found in all herds, and some combinations of two active components belonging to different chemical groups
Pollack, Charles V
Long-term oral anticoagulant (OAC) therapy is used for the treatment and prevention of thrombosis and thromboembolism. As OAC use is so widespread, emergency physicians are likely to encounter patients on anticoagulant therapy in the emergency department (ED) on a regular basis, either for the same reasons as the population in general or as a result of the increased bleeding risk that OAC use entails.The vitamin K antagonist warfarin has been the standard OAC for several decades, but recently, the newer agents dabigatran etexilate, rivaroxaban and apixaban (collectively, novel OACs, non-vitamin K OACs, or simply 'NOACs') have become available for long-term use. Protocols for assessing and managing warfarin-treated patients in the ED are well established and include international normalised ratio (INR) testing, which helps guide patient management. However, the INR does not give an accurate evaluation of coagulation status with NOACs, and alternative tests are therefore needed for use in emergency settings. This paper discusses what information the INR provides for a patient taking warfarin and which coagulation tests can guide the physician when treating patients on one of the NOACs, as well as other differences in emergency anticoagulation management. PMID:25987596
Fucoidan (FC),an effective anticoagulant constituent extracted from brown algae,was introduced into silk fibroin (SF) for improving its blood compatibility.The SF and SF/FC blend films were characterized by attenuated total reflectance Fourier-transform infrared (ATR-FTIR),X-ray photoelectron spectroscopy (XPS),scanning electron microscopy (SEM) and dynamic contact angle determinator (CA).The in vitro anticoagulant activities of the films were evaluated by activated partial thromboplastin time (APTT),thrombin time (TT) and prothrombin time (PT) measurements.The endothelial cell attachment and proliferation viability on the film were assessed by micropipette aspiration technique and MTT assay,respectively.The testing results indicated that the introduction of FC increased the roughness,hydrophilicity and sulfate component of the film surface without impeding the formation of β-sheet conformation in SF.More important,FC brought excellent anticoagulant activity and better endothelial cell affinity to SF.The SF/FC blend film was hopeful to be used as blood-contacting biomaterials.
Skelley, Jessica W; Kyle, Jeffrey A; Roberts, Rachel A
To review the use of the novel oral anticoagulant (NOAC) agents for the treatment of heparin-induced thrombocytopenia (HIT) from relevant clinical trial data. A MEDLINE, International Pharmaceutical Abstracts, ClinicalTrials.gov, and Google-Scholar searches (1966-March 2016) were conducted using the keywords: thrombocytopenia, NOACs, dabigatran, apixaban, rivaroxaban, edoxaban, Xa inhibitor, direct thrombin inhibitor. Articles evaluating the new oral anticoagulants for thrombocytopenia published in English and using human subjects were selected. Eight clinical trials were identified. References cited in identified articles were used for additional citations. Approximately 12 million hospitalized patients each year are exposed to heparin for thromboprophylaxis. HIT, an immune-mediated, prothrombotic adverse reaction is a potential complication of heparin therapy. As a result, heparin products must be immediately withdrawn and replaced by alternative anticoagulants to compensate for the thrombotic risk associated with HIT. Limitations exist with the only currently FDA approved heparin alternative, argatroban. NOACs have been considered as potential alternatives to traditional agents based on their pharmacologic activity. Case reports have indicated positive results in patients, with clinical outcomes and tolerability supporting the use of the NOACs as alternative agents in the treatment of HIT. Positive results have been reported for the use of NOACs in the treatment of HIT. Further robust studies are needed for definitive decision making by clinicians. PMID:27102287
Jennifer A Martin
Full Text Available Adverse drug reactions, including severe patient bleeding, may occur following the administration of anticoagulant drugs. Bivalirudin is a synthetic anticoagulant drug sometimes employed as a substitute for heparin, a commonly used anticoagulant that can cause a condition called heparin-induced thrombocytopenia (HIT. Although bivalrudin has the advantage of not causing HIT, a major concern is lack of an antidote for this drug. In contrast, medical professionals can quickly reverse the effects of heparin using protamine. This report details the selection of an aptamer to bivalirudin that functions as an antidote in buffer. This was accomplished by immobilizing the drug on a monolithic column to partition binding sequences from nonbinding sequences using a low-pressure chromatography system and salt gradient elution. The elution profile of binding sequences was compared to that of a blank column (no drug, and fractions with a chromatographic difference were analyzed via real-time PCR (polymerase chain reaction and used for further selection. Sequences were identified by 454 sequencing and demonstrated low micromolar dissociation constants through fluorescence anisotropy after only two rounds of selection. One aptamer, JPB5, displayed a dose-dependent reduction of the clotting time in buffer, with a 20 µM aptamer achieving a nearly complete antidote effect. This work is expected to result in a superior safety profile for bivalirudin, resulting in enhanced patient care.
Krupa, Mariusz; Moskała, Marek; Składzień, Tomasz; Grzywna, Ewelina
In recent years in the Department of Neurotraumatology in Cracow it has been noticed the frequent connection between appearance of chronic subdural hematoma (CSDH) and treatment by anticoagulant medications. The aim of this study is to draw attention to the problem of insufficient control of anticoagulants consumption, especially by patients treated for cardiovascular system diseases that increases the risk of bleeding and CSDH development. The paper is based on data from questionnaires that was sent to patients with CSDH, cured in the Department of Neurotraumatology form 2004 to 2005. Analyzed was the group of 51 patients with chronic subdural hematoma; 37 individuals (72.5%) confirmed taking acetylsalicylic acid in the period of 3 months before admission to the Department, 9 (17.6%) patients answered that they were taking low-molecular weight heparin. One patient (1.9%) was taking chronically derivative of cumarin. The authors would inform that anticoagulant treatment might favour increase of chronic subdural hematoma incidence. It's especially important, because the average life expectancy has been prolonged in Poland and there are more people taking acetylsalicylic acid. This can be an epidemiological problem in future. PMID:20043584
Emre Kumral; Tuba Cerraho(g)lu (S)irin
Recent evidence is leading to the replacement of vitamin K antagonists,the efficacy of which in preventing stroke in patients with atrial fibrillation (AF) is well established,with better tolerated and more manageable new anticoagulant drugs,with a lower risk of intracranial bleeding,no clear interactions with food,fewer interactions with medications,and no need for frequent laboratory monitoring and dose adjustments.Among new anticoagulants,dabigatran etexilate is a direct,competitive inhibitor of thrombin.It was evaluated for patients with AF in the RE-LY trial,showing lower rates of stroke and systemic embolism at a dose of 150 mg twice daily with similar rates of major hemorrhage compared with warfarin; and non-inferiority compared with warfarin for the prevention of stroke and systemic embolism at a dose of 110 mg twice daily,with lower rates of major bleeding.Beside dabigatran,oral factor X a inhibitors are also emerging for the prevention of thromboembolic events in AF.Despite the obvious advantages of these new oral anticoagulants over vitamin K antagonists,further information is still needed on how to prioritize the patients deriving the greatest benefit from these novel agents on the basis of patient characteristics or drug pharmacokinetics.There is also a need for assessing their long-term efficacy and safety over decades in the real-world setting.
Julio Cesar Lazaro
Full Text Available Introduction Electroconvulsive therapy (ECT is considered the most effective treatment for catatonia regardless its underlying condition. The rigid fixed posture and immobility observed in catatonia may lead to several clinical complications, of which, pulmonary embolism (PE is one of the most severe. The rapid improvement of the psychiatric condition in catatonia-related PE is essential, since immobility favors the occurrence of new thromboembolic events and further complications. In that scenario, ECT should be considered, based on a risk-benefit analysis, aiming at the faster resolution of the catatonia. Methods Case report and literature review. Results A 66-years-old woman admitted to the psychiatric ward with catatonia due to a depressive episode presented bilateral PE. Clinically stable, but still severely depressed after a trial of antidepressants, she was treated with ECT in the course of full anticoagulation with enoxaparin. After five ECT sessions, her mood was significantly better and she was walking and eating spontaneously. She did not present complications related either to PE or to anticoagulation. After the eighth ECT session, she evolved with hypomania, which was managed with oral medication adjustments. The patient was completely euthymic at discharge. Conclusion The case we presented provides further evidence to the anecdotal case reports on the safety of ECT in the course of concomitant full anticoagulant therapy after PE, and illustrates how, with the proper precautions, the benefits of ECT in such condition might outweigh its risks.
Full Text Available Recently, there has been growing interest in the traditional cures of livestock diseases. This is because industrially produced drugs are too expensive for some sectors of the farming community especially in the developing world. Medicinal plants are often cheaper and more easily available than the commercially produced drugs. The self-help study in form of traditional medicines (especially from medicinal plants, offer a way out by making use of resources available within the communities themselves. Despite the steady increase in demand for herbal medicines over the past decade worldwide, a great majority of herbal products are not pharmacologically assessed for their quality, safety and efficacy, nor are they licensed as medicine. In this study some of the medicinal plants used by the Banyankole (an ethnic group with a long history of cattle-keeping and the use of medicinal plants have been tested in vitro using the Ascaris model. Seven plants were studied (Vernonia amygdalina, Cassia didymobotrya, Rhoicissus tridentata, Phytolacca dodecandra, Euphorbia hirta, Aspilla africana and Cymbopogon nardus. Aspillia africana and Cymbopogon nardus did not show anthelmintic activity in this test system. The other five showed anthelmintic activity (Vernonia amygdalina, Cassia didymobotrya, Rhoicissus tridentata, Phytolacca dodecandra and Euphorbia hirta. Extracts of Vernonia amygdalina, Rhoicissus tridentata and Cassia didymobotrya showed higher activity than Euphorbia hirta and Phytolacca dodecandra (Vernonia amygdalina (ED50 of 3.533 mg mL 1, Rhoicissus tridentata (ED50 of 4.355 mg mL 1 and Cassia didymobotrya (ED50 of 4.880 mg mL 1; Euphorbia hirta (ED50 of 5.866 mg mL 1 and Phytolacca dodecandra (ED50 of 7.151 mg mL 1. Further studies on the five plants are needed. Phytochemical analysis to determine the active principles that are responsible for anthelmintic activity are urgently called for. This would help in identifying the spectrum of activity of
Ezekowitz, Michael D; Spahr, Judy; Ghosh, Pradeepto; Corelli, Kathryn
Anticoagulation for stroke prevention in atrial fibrillation (AF) is effective. Pivotal trials RE-LY, ROCKET AF, ARISTOTLE, and ENGAGE-AF TIMI 48 tested novel agents against warfarin (W). In RE-LY, an open-label trial, dabigatran 150 mg BID (D150) was superior (35%) and 110 mg BID (D110) was noninferior to W. D150 reduced ischemic strokes by 25% and intracerebral bleeds by 74%, but increased major GI bleeds by 0.5 % per year. In ROCKET AF, a double-blind study, rivaroxaban 20 mg daily, downtitrated to 15 mg daily (if CrCl was 80; weight, 1.5 mg) was superior for safety (31%), efficacy (21%), and all-cause mortality (11%). In ENGAGE-AF TIMI 48, edoxaban 60 mg once daily (30 mg once daily if CrCl 30-50 ml/min, weight <60 kg, or concomitant verapamil or quinidine) was noninferior to W for efficacy, but reduced major bleeding (20%). To translate clinical trials to practice, understanding the disease and each anticoagulant is essential. For all novel agents, rapid anticoagulation, absence of monitoring, and a short half-life differentiate them from W. Bleed rates were either noninferior or lower than for W, without an antidote. Patient compliance is critical. Knowledge of renal function is essential and maintaining patients on therapy is key. PMID:24880227
Parry, D; Bryan, S; Gee, K; Murray, E.; Fitzmaurice, D
BACKGROUND: The demand for anticoagulation management is increasing. This has led to care being provided in non-hospital settings. While clinical studies have similarly demonstrated good clinical care in these settings, it is still unclear as to which alternative is the most efficient. AIM: To determine the costs borne by patients when attending an anticoagulation management clinic in either primary or secondary care and to use this information to consider the cost-effectiveness of anticoagul...
Kozik-Jaromin, Justyna; Nier, Volker; Heemann, Uwe; Kreymann, Bernhard; Böhler, Joachim
Background. Regional citrate anticoagulation is a very effective anticoagulation method for haemodialysis. However, it is not widely used, primarily due to the risk of hypocalcaemia. We studied citrate and calcium kinetics to better understand safety aspects of this anticoagulation method. Methods. During 15 haemodialysis treatments with a calcium-free dialysis solution, citrate was infused pre-dialyser and calcium was substituted post-dialyser. Systemic and extracorporeal citrate and calcium...
The anthelmintic activity of chicory (Cichorium intybus L.) herbage has been attributed to sesquiterpene lactones. Chicory leaves contain significant amounts of lactucin (LAC), 8-deoxylactucin (DOL), and lactucopicrin (LPIC), but the proportions of these three sesquiterpene lactones vary among fora...
E. A. Belikov; K. V. Davtyan; O. N. Tkacheva
Prevention of thromboembolic complications in patients with atrial fibrillation during catheter pulmonary veins isolation is discussed. This subject review is presented with special consideration to new anticoagulants.
Singer, D E
Nonrheumatic atrial fibrillation (AFib) is the most potent common risk factor for stroke, raising the risk of stroke 5-fold. Six randomized trials of anticoagulation in AFib consistently demonstrated a reduction in the risk of stroke by about two-thirds. In these trials, anticoagulation in AFib was quite safe. In contrast, randomized trials indicate that aspirin confers only a small reduction in risk of stroke, at best. Pooled data from the first set of randomized trials indicate that prior stroke, hypertension, diabetes, and increasing age are independent risk factors for future stroke with AFib. Individuals AFib increases greatly at INR levels AFib depend on maintaining the INR between 2.0-3.0. Cost-effectiveness studies indicate that anticoagulation for AFib is among the most efficient preventive interventions in adults. Importantly, the benefits of anticoagulation in AFib accrue immediately. The implications for managed care organizations are that anticoagulation for AFib should be encouraged in their covered populations, and that dedicated anticoagulation services should be developed to promote system-wide control of anticoagulation intensity. Quality measures would include the proportion of patients with AFib who are anticoagulated, and the percentage of time patients' INR levels are between 2.0-3.0. Managed care organizations can benefit from recent research on anticoagulation for AFib; they have a responsibility to support future research and development efforts. PMID:9525571
Nirmal, S A; Girme, A S; Bhalke, R D
The major volatile constituents of leaves and flowers of Cymbopogon martini from the volatile oil obtained by steam distillation were identified by GC/MS. Five constituents were identified from the volatile oil of leaves and flowers, which constituted about 82.49 and 75.63% of the total amount, respectively. A monoterpene, piperitone (6.00%), was identified in the flowers of C. martini; in addition, flowers were found to contain more olefinic terpenes, namely geraniol (69.63%), compared with leaves (53.41%). Leaves contain bicyclic monoterpene, nerol (24.76%) and alpha-pinene (4.32%). Anthelmintic activity of these oils was evaluated on adult Indian earthworms Pheretima posthuma and results showed that the volatile oil of C. martini flower required less time to cause paralysis and death of the earthworms. PMID:17987504
A. MAHFOOZ, M. Z. MASOOD, A. YOUSAF, N. AKHTAR AND M. A. ZAFAR
Full Text Available The prevalence and anthelmintic efficacy of Abamectin against gastrointestinal parasites under field conditions in Faisalabad (Punjab, Pakistan was studied in 100 horses. The overall prevalence of gastrointestinal parasites was 75%, including Strongylus spp. (50%, Oxyuris equi (12%, Parascaris equorum (8% and mixed infection (5%. Among these naturally infected animals, 15 were selected. These horses were assigned to three groups on the basis of prevalent species of gastrointestinal parasites. Each group had five animals, comprising four treatment horses and a control horse. Abamectin was evaluated against these gastrointestinal parasites with a single shot at the dose rate of 0.2 mg/kg body weight administered through subcutaneous route which resulted in 98% reduction in faecal egg count after day 14 post-treatment. Non-treated horses remained positive for gastrointestinal parasites. No adverse reactions were observed during the experimental period. It was concluded that Abamectin is highly effective against gastrointestinal parasites in horses.
Desrues, Olivier; Enemark, Heidi L.; Thamsborg, Stig Milan
The use of tannin-rich plants against gastro-intestinal nematodes is an alternative currently investigated to avoid the exclusive use of anthelmintic (AH) synthetic drugs and prevent the spread of resistance among these nematode populations. Studies of AH effects on cattle nematodes using tannin......-rich legumes such as Onobrychis viciifolia have been carried out in vitro but the contribution of all structural parameters from their condensed tannins has not been yet completely elucidated. The aim of this study was to investigate the relationship between structure and AH activity in vitro. A series of...... activity using the Larval Feeding Inhibition Assay (LFIA) and the Larval Exsheathment Inhibition Assay on Cooperia oncophora. Preliminaries results with the LFIA showed that high AH activity was due to tannins with increasing prodelphinidin/procyanidin and cis/trans ratios. The variation in mDP between...
Borges, Fernando A; Almeida, Gabriel D; Heckler, Rafael P; Lemes, Raul T; Onizuka, Marcel K V; Borges, Dyego G L
The performance of grazing cattle in tropical areas is deeply influenced by parasitism, and the increasing reports of resistance are a threat to effective nematode control. The present study aimed to evaluate the effect of avermectins on the performance of weaned calves naturally infected by ivermectin-resistant gastrointestinal nematodes. The effect of four commercial endectocides (ivermectin 2.25 % + abamectin 1.25 %, ivermectin 3.15 %, doramectin 3.15 %, and doramectin 1 %) on parasitism and performance of a hundred weaned Nellore calves were evaluated during 112 days. The most effective anthelmintic showed efficacy of 84 % and resulted in an increase (P parasites in beef cattle in the weaning phase may not result in increased productivity when carried out without technical criteria. PMID:23076819
Pradip Kumar Kar
Full Text Available Exploring a green chemistry approach, this study brings to the fore, the anthelmintic efficacy of gold nanoparticles, highlighting the plausible usage of myconanotechnology. Gold nanoparticles of ∼6 to ∼18 nm diameter were synthesized by treating the mycelia-free culture filtrate of the phytopathogenic fungus with gold chloride. Their size and morphology were confirmed by UV-Vis spectroscopy, DLS data, AFM and TEM images. The XRD studies reveal a crystalline nature of the nanoparticles, which are in cubic phase. The FTIR spectroscopic studies before and after the formation of nanoparticles show the presence of possible functional groups responsible for the bio-reduction and capping of the synthesized gold nanoparticles. The latter were tested as vermifugal agents against a model cestode Raillietina sp., an intestinal parasite of domestic fowl. Further, ultrastructural and biochemical parameters were used to corroborate the efficacy study.
Nielsen, Martin Krarup; Vidyashankar, Anand N.; Hanlon, Bret;
contribute to cause this high variability and these must be taken into account to accurately identify a reduction in anthelmintic efficacy. To address this problem, we developed a hierarchical statistical model for analysis of FECRT data from multiple farms. The model includes animal effect and farm clusters...... (48.4 %) testing positive. The efficacy of pyrantel was unaffected by the presence of S. vulgaris on the farm. The cutoff LCL values used for classifying farms as pyrantel resistant were: >92%: no resistance, 88-92%: suspect resistance, and <88%: resistance. Using model-adjusted LCLs, we classified 7...... as random effects. Resistance classifications are based on model adjusted lower confidence limit (LCL) values of predicted mean efficacies on each farm. The model was used to evaluate the efficacy of pyrantel embonate paste from 64 Danish horse farms. On these farms 614 out of 1644 horses had egg...
Rezaul Haque; Wahedul Islam; Selina Parween
Objective: To conduct the antibacterial potency and minimum inhibitory concentration of extracts (n-hexane, acetone, chloroform and methanol) obtained from the root, leaf and stem of Capparis zeylanica. Methods: The powdered leaf, root and stem samples were Soxhlet extracted sequentially in n-hexane, acetone, chloroform and methanol. Antibacterial potency was evaluated by following the agar diffusion method and amoxicillin disc was used as a control. Results: In vitro antibacterial activity against 12 bacteria was performed with crude extracts. Among them, all the bacteria showed the moderate activity but chloroform and methanolic extracts showed promising antibacterial potency against Staphylococcus aureus, Sarcina lutea, Bacillus megaterium, Bacillus subtilis, Salmonella typhi and Shigella dysenteriae (leaf > root > stem). This activity was evaluated using disc diffusion method with a standard antibiotic, 30 µg/disc of amoxicillin. Conclusions: Strong antibacterial potency of chloroform and methanolic extracts provides new antibacterial compounds.
Ashish Kant Jain
Full Text Available Plants are rich source of antibacterial agents, which could be control human diseases. Present investigation was an undertaken to evaluate the antibacterial of Harsinger (Nyctanthes arbortristis Linn against five important human pathogenic bacteria i.e. Escherichia coli, Staphylococcus aureus, Proteus vulgaris, Salmonella typhimurium and Pseudomonas aueruginosa by filter paper disc diffusion method. Dried leaves of Nyctanthes arbortristis were collected, washed, shade dried and powdered. Aqueous and methanol extracts were prepared and evaluate their antibacterial activity. The significant result of antibacterial activity was observed in aqueous as well as methanol leaves extract. The strongest antibacterial activity of aqueous leaves extract was observed in Pseudomonas aeruginosa with (22.00 mm zone of inhibition while the methanol leaves extract showed strongest antibacterial activity against Staphylococcus aureus with (28.00 mm maximum zone of inhibition.
Maggiore, Marina A; Albanese, Adriana A; Gende, Liesel B; Eguaras, Martín J; Denegri, Guillermo M; Elissondo, María Celina
The aim of the present work was to determine the in vitro effect of Mentha piperita and Mentha pulegium essential oils against Echinococcus granulosus and to compare the effectiveness of both oils according to the exposure time and concentration. Although both treatments had a protoscolicidal effect, M. pulegium had a considerably stronger effect than M. piperita. Essential oil of M. pulegium produced dose- and time-dependent effects. Maximal protoscolicidal effect was observed after 12 days of incubation and reached 0% after 18 days. This lack of viability was proved during the determination of infectivity into mice. Essential oil of M. piperita produced only a time-dependent effect. At 24 days p.i., the viability of protoscoleces decreased to approximately 50%. Scanning and transmission electron microscopy (SEM and TEM) demonstrated the drug-induced ultrastructural damage. On the other hand, a loss of turgidity was detected in all M. pulegium-treated cysts respective of the drug concentration. There was a correlation between the intensity of damage and the concentration of the essential oil assayed. Studies by SEM revealed that the germinal layer of treated cysts lost the feature multicellular structure. M. pulegium essential oil showed piperitone oxide as main compound in their composition, and we suggest that this component could be responsible of the markedly anthelmintic effect detected. Our data suggest that essential oils of Mentha spp. can be a promising source of potential protoscolicidal agents. The isolation of active anthelmintic constituents is in progress and may lead to the discovery of compounds with improved therapeutic value. PMID:21845411
Bazh, Eman K A; El-Bahy, Nasr M
Intestinal helmintic infection, continue to be a cause of major concern in several parts of the world, particularly in the developing nations. The use of plant extracts to control poultry helminths is increasing in different rearing systems. The anthelmintic activity of ginger and curcumin was studied on the nematode Ascaridia galli. In vitro and in vivo studies were allocated. Live parasites for in vitro studies were collected from the intestine of naturally infected chickens. Some living worms were incubated at 37 °C in media containing ginger at three concentration levels (25, 50, and 100 mg/ml), and others were incubated in media containing curcumin at the same concentration levels. Another living worm group was incubated in media containing albendazole at a dose of 7.5 mg/ml. The extracts' efficacy was exhibited in a concentration-time-dependent manner mainly at 100 mg/ml and after 48 h. The in vivo study takes place on experimentally infected chickens. Group of infected chickens was treated with ginger extract at dose of 100 mg, another group was treated with curcumin extract at dose of 100 mg, and a third group was treated with albendazole at dose of 7.5 mg. In vivo study of ginger and curcumin recorded lower mortality rates than the in vitro study. It is concluded that ginger and curcumin extracts have potential anthelmintic properties against A. galli. Ginger in all concentrations used exhibited a higher death rate observed than curcumin. Their wormicidal effect is concentration-time dependent. PMID:24046262
Kliks, M M
Infusions and decoctions of the leaves, roots and inflorescences of the herbaceous shrub Chenopodium ambrosioides (American wormseed, goosefoot, epazote, paico) and related species indigenous to the New World have been used for centuries as dietary condiments and as traditional anthelmintics by native peoples for the treatment of intestinal worms. Commercial preparations of oil of chenopodium and its active constituent, ascaridol, obtained by steam distillation, have been and continue to be, used with considerable success in mass treatment campaigns. Ethnopharmacological studies in a community of Mayan subsistence farmers in Chiapas, Mexico, confirmed that decoctions containing up to 300 mg of dry plant material per kg body weight (MGKGW) were widely used and traditionally highly regarded in the treatment of ascariasis. However, therapeutic doses of up to 6000 MGKGW of powdered, dried plant had no significant anthelmintic effect on the adults of Necator, Trichuris of Ascaris. Gas-liquid chromatographic analyses of plant samples used consistently demonstrated the presence of ascaridol in the expected amounts. Possible origins of subjective belief in the efficacy of C. ambrosioides as used, may be related to the positive association of spontaneous, or peristalsis-induced passage of senescent worms immediately following a therapeutic episode. It is also possible that in the past varieties of the plant containing much more ascaridol were used. The results of these controlled field studies did not sustain widely held traditional beliefs, nor the value of therapeutic practices regarding this plant. It is, therefore, essential that all indigenous ethnomedical practices be objectively evaluated for efficacy and safety using appropriate protocols before being considered for adoptation or promotion in health care programs.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:3906906
Wu, Chia-Chen; Hu, Yan; Miller, Melanie; Aroian, Raffi V; Sailor, Michael J
The ability of nano- and microparticles of partially oxidized mesoporous silicon (pSi) to sequester, protect, and deliver the anthelmintic pore-forming protein Cry5B to nematodes is assessed in vitro and in vivo. Thermally oxidized pSi particles are stable under gastric conditions and show relatively low toxicity to nematodes. Fluorescence images of rhodamine-labeled pSi particles within the nematodes Caenorhabditis elegans and Ancylostoma ceylanicum show that ingestion is dependent on particle size: particles of a 0.4 ± 0.2 μm size are noticeably ingested by both species within 2 h of introduction in vitro, whereas 5 ± 2 μm particles are excluded from C. elegans but enter the pharynx region of A. ceylanicum after 24 h. The anthelmintic protein Cry5B, a pore-forming crystal (Cry) protein derived from Bacillus thuringiensis, is incorporated into the pSi particles by aqueous infiltration. Feeding of Cry5B-loaded pSi particles to C. elegans leads to significant intoxication of the nematode. Protein-loaded particles of size 0.4 μm display the highest level of in vitro toxicity toward C. elegans on a drug-mass basis. The porous nanostructure protects Cry5B from hydrolytic and enzymatic (pepsin) degradation in simulated gastric fluid (pH 1.2) for time periods up to 2 h. In vivo experiments with hookworm-infected hamsters show no significant reduction in worm burden with the Cry5B-loaded particles, which is attributed to slow release of the protein from the particles and/or short residence time of the particles in the duodenum of the animal. PMID:25950754
Kamaraj, Chinnaperumal; Rahuman, Abdul Abdul; Elango, Gandhi; Bagavan, Asokan; Zahir, Abdul Abduz
The source of chemical anthelmintics (levamisole, flubendazole, and thiabendazole) had limited the success of gastrointestinal nematodiasis control in sheep and goats and thus awakened interest in the study of medicinal plant extracts as alternative sources of anthelmintics. The egg hatching and larvicidal effect of indigenous plant extracts were investigated against the sheep parasite, Haemonchus contortus. The purpose of the present study was to assess the efficacy of leaf, bark, and seed ethyl acetate, acetone and methanol extracts of Andrographis paniculata (Burm.f.) Wall. ex Nees., Anisomeles malabarica (L.) R. Br., Annona squamosa L., Datura metel L., and Solanum torvum Swartz were tested against the parasitic nematode of small ruminants H. contortus using egg hatch assay (EHA) and larval development assay (LDA). The assays were run in 24-well cell culture plates at room temperature with five replicates. All plant extracts showed moderate parasitic effects after 48 and exposure for egg hatching and LDA, respectively; however, 100% egg hatching and larvicidal inhibition were found in the methanol extracts of A. paniculata, A. squamosa, D. metel, and S. torvum at 25 mg/ml and the effect was similar to positive control of Albendazole (0.075 mg/ml) and Ivermectin (0.025mg/ml) against H. contortus, respectively. The EHA result showed the ED(50) of methanol extracts of A. paniculata and D. metel, which were 2.90 and 3.08 mg/ml, and in larval development assay, the ED(50) was 4.26 and 3.86 mg/ml, respectively. These effects remain to be confirmed through in vivo studies. PMID:21161270
Anthrax is one of the oldest threats to humankind, and remains endemic in animals in many parts of the world. Human cases are infrequent, and some result from biological warfare. This review summarizes the current knowledge on the antibacterial activity of available antibiotics. For potential use in the most severe cases of anthrax, antibacterials need to exhibit potent in vitro activity, intracellular bioactivity, and suitable locations in lymph nodes. In animal models, it has been shown that doxycycline and fluoroquinolones are the most active compounds. There is a lack of data for animal models for macrolides and ketolides, some of them exhibiting good in vitro activity. However, systemic anthrax (inhalation or gastrointestinal) is mainly due to anthrax toxin, and therapy directed against intoxication is needed as basic treatment. PMID:12197869
Ou, Junfei; Wang, Zhile; Wang, Fajun; Xue, Mingshan; Li, Wen; Amirfazli, Alidad
Inspired by the high adherence of mussel and the excellent water repellency of lotus leaf, superhydrophobic fabric is fabricated via the sequential deposition of polydopamine, Ag2O, and 1H,1H,2H,2H-perfluorodecanethiol, which shows excellent washability and high anti-bacterial activity due to the strong interfacial interaction and the surface silver species as well as the non-wettability, respectively.
Beranová, Jana; Seydlová, Gabriela; Kozak, Halyna; Benada, Oldřich; Fišer, Radovan; Artemenko, Anna; Konopásek, Ivo; Kromka, Alexander
Ostrava: Tanger, 2014. ISBN 978-80-87294-55-0. [International Conference NANOCON /6./. 05.11.2014-07.11.2014, Brno] R&D Projects: GA ČR GAP108/12/0910 Institutional support: RVO:68378271 ; RVO:61388971 Keywords : diamond nanoparticles * antibacterial properties * Escherichia coli * Bacillus subtilis * DLS * XPS Subject RIV: BM - Solid Matter Physics ; Magnetism; EE - Microbiology, Virology (MBU-M)
Pešić-Mikulec Dragana M.; Dugalić-Vrndić Nada; Baltić Milan Ž.
Honey was used as a medicine in traditional medicine of the Ancient Times ever since the age of Hippocrates. Scientifically based investigations of the medicinal qualities of honey date back to the 19th century. There have been constant polemics, about the medicinal characteristics of honey and parameters that cause them, among scientists and apiculture experts. In this paper, we processed much data from literature, which indicate the antibacterial characteristics of honey through the experim...
Sawai, J; Doi, R; Maekawa, Y; Yoshikawa, T; Kojima, H
The applicability of indirect conductimetric assays for evaluation of antibacterial activity was examined. The minimal inhibitory concentration (MIC) obtained by the indirect method was consistent with that by the direct conductimetric assay and the turbidity method. The indirect assay allows use of growth media, which cannot be used in the direct conductimetric assay, making it possible to evaluate the antibacterial activity of insoluble or slightly soluble materials with high turbidity, such as antibacterial ceramic powders. PMID:12407467
DeSouza, L.; Wahidullah, S.; PrabhaDevi
and antifungal assays were performed using Agar well diffusion method2, 3 and MIC was determined by tube dilution method using Himedia Mueller-Hinton broth4. Streptomycin and nystatin were used as antibacterial and antifungal positive controls while solvent... reported the enhancement of antibacterial activity on mixing of quercetin with quercitrin, morin or rutin. There are conflicting reports on the antibacterial activity of quercetin probably owing to inter and intra-assay variation in susceptibility...
Lijian Xu; Wei Meng; Cong Cao; Jian Wang; Wenjun Shan; Qinggui Wang
This paper reviews 116 new compounds with antifungal or antibacterial activities as well as 169 other known antimicrobial compounds, with a specific focus on January 2010 through March 2015. Furthermore, the phylogeny of the fungi producing these antibacterial or antifungal compounds was analyzed. The new methods used to isolate marine fungi that possess antibacterial or antifungal activities as well as the relationship between structure and activity are shown in this review.
Kiristi, Melek; Singh, Virendra V; Esteban-Fernández de Ávila, Berta; Uygun, Murat; Soto, Fernando; Aktaş Uygun, Deniz; Wang, Joseph
An effective and rapid bacterial killing nanotechnology strategy based on lysozyme-modified fuel-free nanomotors is demonstrated. The efficient antibacterial property of lysozyme, associated with the cleavage of glycosidic bonds of peptidoglycans present in the bacteria cell wall, has been combined with ultrasound (US)-propelled porous gold nanowire (p-AuNW) motors as biocompatible dynamic bacteria nanofighters. Coupling the antibacterial activity of the enzyme with the rapid movement of these p-AuNWs, along with the corresponding fluid dynamics, promotes enzyme-bacteria interactions and prevents surface aggregation of dead bacteria, resulting in a greatly enhanced bacteria-killing capability. The large active surface area of these nanoporous motors offers a significantly higher enzyme loading capacity compared to nonporous AuNWs, which results in a higher antimicrobial activity against Gram-positive and Gram-negative bacteria. Detailed characterization studies and control experiments provide useful insights into the underlying factors controlling the antibacterial performance of the new dynamic bacteria nanofighters. Rapid and effective killing of the Gram-positive Micrococcus lysodeikticus bacteria (69-84% within 1-5 min) is demonstrated. PMID:26308491
Jacob A Udell
Full Text Available BACKGROUND: Survivors of anterior MI are at increased risk for stroke with predilection to form ventricular thrombus. Commonly patients are discharged on dual antiplatelet therapy. Given the frequency of early coronary reperfusion and risk of bleeding, it remains uncertain whether anticoagulation offers additional utility. We examined the effectiveness of anticoagulation therapy for the prevention of stroke after anterior MI. METHODS AND FINDINGS: We performed a population-based cohort analysis of 10,383 patients who survived hospitalization for an acute MI in Ontario, Canada from April 1, 1999 to March 31, 2001. The primary outcome was four-year ischemic stroke rates compared between anterior and non-anterior MI patients. Risk factors for stroke were assessed by multivariate Cox proportional-hazards analysis. Warfarin use was determined at discharge and followed for 90 days among a subset of patients aged 66 and older (n = 1483. Among the 10,383 patients studied, 2,942 patients survived hospitalization for an anterior MI and 20% were discharged on anticoagulation therapy. Within 4 years, 169 patients (5.7% were admitted with an ischemic stroke, half of which occurred within 1-year post-MI. There was no significant difference in stroke rate between anterior and non-anterior MI patients. The use of warfarin up to 90 days was not associated with stroke protection after anterior MI (hazard ratio [HR], 0.68; 95% confidence interval [CI], 0.37-1.26. The use of angiotensin-converting-enzyme inhibitors (HR, 0.65; 95% CI, 0.44-0.95 and beta-blockers (HR, 0.60; 95% CI, 0.41-0.87 were associated with a significant decrease in stroke risk. There was no significant difference in bleeding-related hospitalizations in patients who used warfarin for up to 90 days post-MI. CONCLUSION: Many practitioners still consider a large anterior-wall MI as high risk for potential LV thrombus formation and stroke. Among a cohort of elderly patients who survived an anterior
Werder, Gabriel M. [William Beaumont Hospital, Department of Radiology, 3600 West Thirteen Mile Road, Royal Oak, MI 48073 (United States); St Christopher Iba Mar Diop College of Medicine, Luton (United Kingdom)], E-mail: firstname.lastname@example.org; Razdan, Rahul S.; Gagliardi, Joseph A.; Chaddha, Shashi K.B. [St Vincent' s Medical Center, Bridgeport, CT (United States)
We present a case of pineal apoplexy in an anticoagulated and hypertensive 56-year-old Hispanic male. At presentation, the patient's international normalized ratio (INR) was 10.51 and his blood pressure was 200/130 mmHg. His presenting symptoms included acute onset of headache, chest pain, nausea, vomiting, vertigo, and visual disturbance. Neuroimaging demonstrated hemorrhage into a morphologically normal pineal gland. Under conservative management, the patient experienced gradual resolution of all symptoms excluding the disturbance of upward gaze.
Just, Søren Andreas; Nybo, Mads; Laustrup, Helle;
Inflammation is strongly associated with lupus anticoagulant positivity, indepentent of know autoimmune disease and recent venous or arterial thrombosis......Inflammation is strongly associated with lupus anticoagulant positivity, indepentent of know autoimmune disease and recent venous or arterial thrombosis...
Full Text Available Sport and leisure horses in Morocco are treated with several anthelmintics, organophosphates (dichlorvos, benzimidazoles (mostly thiabendazole or tetrahydropyrimidines (mostly pyrantel pamoate against nematodes. We studied three horse stables in Rabat, one in Meknes and one in Bouznika. Two of the Rabat and Bouznika stables had introduced a large number of horses from countries (Argentina or Europe where resistance to benzimidazoles is frequent, whereas the Meknes stud farm remained without foreign introduction. The number of treatments was not very frequent (twice a year in adult horses but the same anthelmintics were used repeatedly. No resistance to dichlorvos was detected whereas benzimidazole and pyrantel pamoate resistances were detected for the first time in African horses, outside South Africa.
Williams Andrew R.
Full Text Available Ascariasis affects more than 1 billion people worldwide, mainly in developing countries, causing substantial morbidity. Current treatments for Ascaris infection are based on mass drug administration (MDA with synthetic anthelmintic drugs such as albendazole, however continual re-infection and the threat of drug resistance mean that complementary treatment options would be highly valuable. Here, we screened ethanolic extracts from 29 medicinal plants used in Africa (Ghana and the Caribbean (US Virgin Islands for in vitro anthelmintic properties against Ascaris suum, a swine parasite that is very closely related to the human A. lumbricoides. A wide variety of activities were seen in the extracts, from negligible to potent. Extracts from Clausena anisata, Zanthoxylum zanthoxyloides and Punica granatum were identified as the most potent with EC50 values of 74, 97 and 164 μg/mL, respectively. Our results encourage further investigation of their use as complementary treatment options for ascariasis, alongside MDA.
Kinung'hi, Safari M.; Magnussen, Pascal; Kishamawe, Coleman; Todd, Jim; Vennervald, Birgitte J
BACKGROUND: Some studies have suggested that helminth infections increase the risk of malaria infection and are associated with increased number of malaria attacks and anaemia. Thus interventions to control helminth infections may have an impact on incidence of clinical malaria and anaemia. The...... current study assessed the impact of two anthelmintic treatment approaches on malaria infection and on anaemia in school and pre-school children in Magu district, Tanzania. METHODS: A total of 765 children were enrolled into a prospective randomized anthelmintic intervention trial following a baseline...... study of 1546 children. Enrolled children were randomized to receive either repeated treatment with praziquantel and albendazole four times a year (intervention group, 394 children) or single dose treatment with praziquantel and albendazole once a year (control group, 371 children). Follow up...
Diet composition is one of the factors that may contribute to intraindividual variability in the anticoagulant response to warfarin. The aim of this study was to determine the associations between food pattern and anticoagulant response to warfarin in a group of Brazilian patients with vascular dis...
Williams, Andrew R.; Aina Ramsay; Hansen, Tina V. A.; Ropiak, Honorata M; Helena Mejer; Peter Nejsum; Irene Mueller-Harvey; Thamsborg, Stig M.
Cinnamon (Cinnamomum verum) has been shown to have anti-inflammatory and antimicrobial properties, but effects on parasitic worms of the intestine have not been investigated. Here, extracts of cinnamon bark were shown to have potent in vitro anthelmintic properties against the swine nematode Ascaris suum. Analysis of the extract revealed high concentrations of proanthocyanidins (PAC) and trans-cinnamaldehyde (CA). The PAC were subjected to thiolysis and HPLC-MS analysis which demonstrated tha...
Gastrointestinal (GI) nematodes are important helminth pathogens responsible for severe losses to livestock industries and human health throughout the world. Control of these infections relies primarily on chemotherapy; however there is rapid development of resistance to all available classes of anthelmintic drugs, and therefore new alternative treatments are urgently required. Plant cysteine proteinases (CPs) from papaya latex, pineapple fruit and stem extracts have been demonstrated to b...
Gunawardena GSA; Siriwardana C; Paranavitane S; Ismail M; Fernando S.
General Practitioners (GPs) provide first contact care of children and pregnant mothers in the community. This study ascertained the prescribing pattern of anthelmintics to children and pregnant women by a sample of GPs from the district of Colombo. Two hundred medical practitioners engaged in full-time General Practice (100 urban and 100 rural), were selected randomly. A pre-tested interviewer-administered questionnaire was used to collect data. A total of 183 GPs aged between 26 and 72 year...
John N. Kateregga; Maria Nabayunga; Patrick Vudriko; James G. Ndukui
Background: Cassia occidentalis is traditionally used to treat helminth infestations in poultry. We investigated the in-vitro anthelmintic activity of the methanolic leaf extract of this plant against Heterakis gallinarum and Ascaridia galli worms and its acute toxicity. Methods: Leaves of the plant were air dried, ground into powder and extracted with 70% methanol, filtered and dried at 50℃ into a dark green semi-solid mass. The worms were isolated from fresh intestines of local chi...
R. G. Shrimali
Full Text Available Aim: Fasciolosis is a parasitic disease caused by Fasciola spp. of the family Fasciolidae (trematodes characterized by bottle jaw, anemia, progressive debility, and potbelly condition. There are many aspects of fasciolosis remaining unknown thus hemato-biochemical alterations in closantel, triclabendazole + ivermectin, and oxyclozanide + levamisole treated goats were studied. Materials and Methods: A total of 40 naturally fasciolosis infected goats having egg per gram more than 100 were randomly divided into four groups. Goats of Group I-III were treated with three different anthelmintics, whereas, goats of Group-IV were kept as control or untreated. Whole blood, serum, and fecal samples were collected on 0, 7th, and 30th day of treatment. Results: During the study, values of hemoglobin, total erythrocyte count, pack cell volume, and total protein were significantly elevated to their normal levels in anthelmintics treated groups. Whereas, values of total leukocyte count, aspartate transaminase (AST, lactate dehydrogenase (LDH, and gamma-glutamyl transferase (GGT were significantly reduced to their normal level in anthelmintics treated groups. The efficacy of closantel (T1, triclabendazole + ivermectin (T2, and oxyclozanide + levamisole (T3 was 99.63%, 100%, and 94.74% and 100%, 100%, and 97.38% on 7th and 30th day of treatment, respectively. Conclusions: Fasciolosis in goats can be diagnosed on the basis of fecal sample examination, but alterations in important biomarkers such as AST, GGT, and LDH are also helpful for early diagnosis. The use of newer anthelmintic either alone or in combination showed a higher therapeutic response in fasciolosis of goats.
Cappelleri, Gianluca; Fanelli, Andrea
The use of direct oral anticoagulants including apixaban, rivaroxaban, and dabigatran, which are approved for several therapeutic indications, can simplify perioperative and postoperative management of anticoagulation. Utilization of regional neuraxial anesthesia in patients receiving anticoagulants carries a relatively small risk of hematoma, the serious complications of which must be acknowledged. Given the extensive use of regional anesthesia in surgery and the increasing number of patients receiving direct oral anticoagulants, it is crucial to understand the current clinical data on the risk of hemorrhagic complications in this setting, particularly for anesthesiologists. We discuss current data, guideline recommendations, and best practice advice on effective management of the direct oral anticoagulants and regional anesthesia, including in specific clinical situations, such as patients undergoing major orthopedic surgery at high risk of a thromboembolic event, or patients with renal impairment at an increased risk of bleeding. PMID:27290980
Vinholt, Pernille J; Nybo, Mads
We present a case concerning a patient with splenic marginal zone lymphoma (SMZL) and isolated prolonged activated partial thromboplastin time (aPTT) caused by lupus anticoagulant. Von Willebrand factor (VWF) activity and antigen were immeasurable by latex particle immunoturbidimetric assays, and...... several coagulation factor levels were decreased. However, VWF activity and antigen were normal when analyzed by other methods. Also, coagulation factor levels were normal if an aPTT reagent with low lupus anticoagulant sensitivity or a chromogenic method was applied. Altogether, the initial findings were...... because of lupus anticoagulant interference and in fact, the patient had normal VWF activity and coagulation status. Interference of lupus anticoagulant in clot-based assays is well known but has not previously been described in VWF assays. This is furthermore the first report in which lupus anticoagulant...
Zacharski, Leo R
Numerous studies have shown that elements of coagulation reactions mediate tumor cell proliferation, motility (invasiveness), tissue remodeling and metastasis. Coagulation activation is virtually a universal feature of human malignancy that differs from the clotting response to injury in that it is self-perpetuating rather than self-attenuating. Coagulation activation participates in tumor matrix deposition and local inflammation, and predicts subsequent cancer risk and adverse cancer outcomes. Several clinical trials of anticoagulants have shown improved outcomes in small cell carcinoma of the lung (SCCL) that have been correlated with assembly on the tumor cells of an intact coagulation pathway. However, variable efficacy of anticoagulant therapy has raised doubts about the coagulation hypothesis. Recently, initiators of coagulation and fibrinolytic pathways have been identified that mediate tumor inception and progression. Notable among these is oxidative stress driven by iron-catalyzed reactive oxygen species that may be the basis for local coagulation activation, tumor matrix deposition, inflammation and aberrant properties characteristic of the malignant phenotype. Recognition of important biological characteristics of individual tumor types, disease stage, choice of standard therapy including chemotherapy and the iron status of the host may clarify mechanisms. All of these are subject to modification based on controlled clinical trial design. Further tests of the coagulation hypothesis may lead to novel, low cost and relatively non-toxic approaches to treatment of malignancy including lung cancer that contrast with certain current cancer treatment paradigms. PMID:27413710
Full Text Available In intrauterine life, hemostasis is maintained by the same components as in extrauterine life (blood platelets, coagulation and fibrinolysis systems, involvement of the vascular wall; in the fetus, however, these components show significant differences of a quantitative/qualitative nature. In the present study, we surveyed the literature on the coagulation system in the fetus. We focused on the velocity of development of the coagulation system, being reflected in the increased concentration of all procoagulants and anticoagulants (a rise from approximately 20% in the middle of pregnancy to about 60% or more in the period of labor; exceptions: factors V, VIII and XIII which in the labor period reach the adult level and screening test results (prothrombin time, aPTT - activated prothrombin time, and thrombin time. Reference values were given for the 19-38 weeks of pregnancy and the labor term. Biochemical features of fetal fibrinogen and PIVKA factors were also discussed. The role of activated protein C (APC in the maintenance of balance between procoagulants and anticoagulants was postulated as well as the role of APC in the formation of thrombin activatable fibrinolysis inhibitor (TAFI.
Numerous studies have shown that elements of coagulation reactions mediate tumor cell proliferation, motility (invasiveness), tissue remodeling and metastasis. Coagulation activation is virtually a universal feature of human malignancy that differs from the clotting response to injury in that it is self-perpetuating rather than self-attenuating. Coagulation activation participates in tumor matrix deposition and local inflammation, and predicts subsequent cancer risk and adverse cancer outcomes. Several clinical trials of anticoagulants have shown improved outcomes in small cell carcinoma of the lung (SCCL) that have been correlated with assembly on the tumor cells of an intact coagulation pathway. However, variable efficacy of anticoagulant therapy has raised doubts about the coagulation hypothesis. Recently, initiators of coagulation and fibrinolytic pathways have been identified that mediate tumor inception and progression. Notable among these is oxidative stress driven by iron-catalyzed reactive oxygen species that may be the basis for local coagulation activation, tumor matrix deposition, inflammation and aberrant properties characteristic of the malignant phenotype. Recognition of important biological characteristics of individual tumor types, disease stage, choice of standard therapy including chemotherapy and the iron status of the host may clarify mechanisms. All of these are subject to modification based on controlled clinical trial design. Further tests of the coagulation hypothesis may lead to novel, low cost and relatively non-toxic approaches to treatment of malignancy including lung cancer that contrast with certain current cancer treatment paradigms.
Stöllberger, Claudia; Finsterer, Josef
Dabigatran, rivaroxaban, and apixaban are the new oral anticoagulants (NOAC) which have been investigated in patients with atrial fibrillation (AF) for primary and secondary prevention of stroke and thromboembolism. In these trials NOAC had a similar efficacy and safety profile compared to traditional vitamin-K-antagonists such as warfarin. We advise caution in the use of NOAC in patients with stroke or cerebral hemorrhage because of the following reasons: 1) Patients with cerebral bleeding were excluded from the trials. 2) Stroke within 14 days and severe stroke within 6 months before screening were exclusion criteria in the trials investigating dabigatran and rivaroxaban. 3) There is no antidote for reversal and no reliable laboratory monitoring of the anticoagulant effect for emergency situations. 4) NOAC are either substrates of the P-glycoprotein (P-gp) or are metabolized by the cytochrome P450 (CYP) system, or both. Drug-drug interactions between NOAC and P-gp and CYP-affecting drugs are largely unknown. 5) Long-term effects of thrombin generation inhibition on the occurrence of infections, malignancies, dementia, and other diseases are unknown. Based on these considerations it is our opinion that studies of NOAC in patients with stroke compared with other prevention strategies, as well as more post marketing surveillance data, are required. PMID:23628464
Robben, J H; Mout, H C; Kuijpers, E A
The occurrence, the diagnosis, and the treatment of anticoagulant rodenticide poisoning in dogs in the Netherlands was evaluated by a survey among Dutch veterinarians carried out by the National Poisons Control Center (NPCC). The survey included information on 54 dogs, 32 being treated by veterinarians who consulted the NPCC and 22 that were admitted to the Utrecht University Clinic for Companion Animals (UUCCA). The poisons that were suspected were brodifacoum (n = 19), bromadiolone (n = 14), difenacoum (n = 8), difethialone (n = 6) and chlorophacinone (n = 1). In 6 dogs the identity of the poison was unknown. Of 31 dogs with hemorrhages, 2 died shortly after presentation to practitioners and 2 died shortly after admission to the UUCCA. Signs of bleeding occurred especially in poisoning by brodifacoum (n = 16). In all but one of the dogs without hemorrhages, the intake of poison had taken place within 24 hours before presentation. The method of treatment varied, with the induction of vomiting and the use of vitamin K mentioned most. The choice of therapy was determined by the length of time after intake of the poison, the clinical signs and whether or not an anticoagulant toxicosis was suspected at the time of the initial examination. These findings provide the basis for discussion of several aspects of diagnosis and treatment. PMID:9534772
Barrios, Annette C; Ventura, Hector O; Milani, Richard V
Clinical privileging of pharmacists and the effective use of support staff and information technology have helped create an efficient pharmacist-operated anticoagulation clinic at Ochsner Clinic Foundation that will support future growth efforts for improved patient care. Developed by Ochsner's Department of Cardiology, the pharmacist-operated anticoagulation clinic cares for 2000 patients with a clinical pharmacist, staff pharmacist, registered nurse, and medical assistants. Patients are managed by face-to-face and telephone encounters. The pharmacists are privileged by medical staff to write prescriptions for warfarin, adjust warfarin doses, and conduct appropriate laboratory monitoring. Patients attend a mandatory initial visit where they are given medication instructions and educational materials. The pharmacist determines the treatment dose and schedules follow-up appointments. A software system developed by Ochsner's Information Services Department imports patient data from the institution's central computer system, allowing for a limited electronic patient record. Once fully implemented, this program will allow for more specific patient tracking and assist with quality improvement efforts. At present, approximately 68% of our patient population is within therapeutic range. PMID:22822313
Ciurus, Tomasz; Cichocka-Radwan, Anna
Introduction The risk of complications in anticoagulation therapy can be reduced by maximising the percentage of time spent by the patient in the optimal therapeutic range (TTR). However, little is known about the predictors of anticoagulation control. The aim of this paper was to assess the quality of anticoagulant therapy in patients on warfarin and to identify the factors affecting its deterioration. Material and methods We studied 149 patients who required anticoagulant therapy with warfarin due to non-valvular atrial fibrillation and/or venous thromboembolism. Each patient underwent proper training regarding the implemented treatment and remained under constant medical care. Results The mean age of the patients was 68.8 ± 12.6 years, and 59% were male. A total of 2460 international normalised ratio (INR) measurements were collected during the 18-month period. The mean TTR in the studied cohort was 76 ± 21%, and the median was 80%. The level at which high-quality anticoagulation was recorded for this study was based on TTR values above 80%. Seventy-five patients with TTR ≥ 80% were included in the stable anticoagulation group (TTR ≥ 80%); the remaining 74 patients constituted the unstable anticoagulation group (TTR < 80%). According to multivariate stepwise regression analysis, the independent variables increasing the risk of deterioration of anticoagulation quality were: arterial hypertension (OR 2.74 [CI 95%: 1.06-7.10]; p = 0.038), amiodarone therapy (OR 4.22 [CI 95%: 1.30-13.70]; p = 0.017), and obesity (OR 1.11 [CI 95%: 1.02-1.21]; p = 0.013). Conclusions The presence of obesity, hypertension, or amiodarone therapy decreases the quality of anticoagulation with warfarin. High quality of anticoagulation can be achieved through proper monitoring and education of patients. PMID:26855650
Thirteen plants which are traditionally used for the treatment of dysentery and diarrhoea in Myanmar were selected and tested for antibacterial activity by using agar disc diffusion technique. Polar and nonpolar solvents were employed for extraction of plants. The minimum inhibitory concentration (MIC) of the extracts with the most significant predominant activity were evaluated by plate dilution method. The plants Eugenia jambolana, Quisqualis indica, Leucaena glauca and Euphorbia splendens var. 1 were found to show significant antibacterial activity. It was also observed that extracts using nonpolar solvents did not show any antibacterial activity and extracts using polar solvents showed antibacterial activity on tested bacteria, indicating that the active chemical compound responsible for the antibacterial action must be a polar soluble compound. (author)
van Krimpen, M M; Binnendijk, G P; Borgsteede, F H M; Gaasenbeek, C P H
Two experiments were performed to determine the anthelmintic effect of some phytogenic feed additives on a mild infection of Ascaris suum in growing and finishing pigs. Usually, an infection of A. suum is controlled by using conventional synthetic drugs. Organic farmers, however, prefer a non-pharmaceutical approach to worm control. Therefore, phytotherapy could be an appropriate alternative. In the first experiment, a commercial available organic starter diet was supplemented with 3% of a herb mixture, adding 1% Thymus vulgaris, 1% Melissa officinalis and 1% Echinacea purpurea to the diet, or with 4% of a herb mixture, thereby adding the mentioned herbs plus 1% Camellia sinensis (black tea). A negative control group (no treatment) and a positive control group (treatment with conventional synthetic drug flubendazole) were included. In the second experiment, the anthelmintic properties against A. suum of three individual herbs, Carica papaya, Peumus boldus and Artemisia vulgaris, each in a dose of 1%, were tested. Pigs were infected with 1000 infective worm eggs each. Each experiment was performed with 32 individually housed growing pigs (8 replicates/treatment), which were monitored for 67 days. It was hypothesized that the herbs would block the cycles of the larvae, thereby preventing the development of adult worms. Therefore, phytogenic feed additives were not supplied during the whole experimental period, but only from the start until D39. Pigs were inoculated with infective worm eggs during five consecutive days (D17-D21). At D67 all pigs were dissected, whereafter livers were checked for the presence of white spots. Also numbers of worms in the small intestine were counted. In experiment 1, the numbers of worm-infected pigs were similar for both the herb supplemented (groups 3 and 4) and the unsupplemented (group 1) treatments (5-6 pigs of 8), while the treatment with flubendazole (group 2) resulted in 0 infected pigs. In experiment 2, herb addition (groups 2
Gauly, M; Duss, C; Erhardt, G
In the present study, the effects of an experimental Ascaridia galli infection and anthelmintic treatment on the behaviour and social status of laying hens of two different lines were studied. Sixty white (Lohmann LSL; LSL) and 60 brown (Lohmann Brown; LB) hens were reared under helminth-free conditions. The hens of each line were divided into four groups. The birds in two of the groups were artificially infected with 250 embryonated A. galli eggs at an age of 27 weeks. The other two groups were kept as uninfected controls. One infection and control group was dewormed at 38 weeks of age and slaughtered 4 weeks later, contemporary with the other animals. Individual faecal Ascaridia egg counts (FEC) were performed 11 weeks post-infection (p.i.). Body weights, laying performance and egg weights were recorded regularly. Blood was taken to measure testosterone levels. The worm burdens established in the intestines were counted in the infected not treated group after slaughtering. In addition, 15 behavioural parameters were recorded by focal animal observation (n=10 per group) of one infection (plus anthelmintic treatment) and one control group, according to the time-sampling method throughout the experiment. All agonistic interactions within the groups were recorded simultaneously on an ongoing basis, thereby allowing the calculation of an individual social rank index. The following results were obtained: Mean FEC and worm burden were higher (p 0.05) from the controls. Infections with A. galli resulted in significant behavioural changes in both lines as the infected birds showed a higher food intake and lower locomotion activity during the prepatent and patent periods. After anthelmintic treatment, food intake decreased and locomotion increased. Behavioural changes were more pervasive in the infected LSL hens, as these hens also showed changes in ground pecking and nesting activity not only during the prepatent and patent periods, but also after anthelmintic treatment
Elmeros, Morten; Christensen, Thomas Kjær; Lassen, Pia
Anticoagulant rodenticides are widely used to control rodent populations but they also pose a risk of secondary poisoning in non-target predators. Studies on anticoagulant rodenticide exposure of non-target species have mainly reported on frequency of occurrence. They have rarely analyzed variations in residue concentrations. We examine the occurrence and concentrations of five anticoagulant rodenticides in liver tissue from 61 stoats (Mustela erminea) and 69 weasels (Mustela nivalis) from Denmark. Anticoagulant rodenticides were detected in 97% of stoats and 95% of weasels. 79% of the animals had detectable levels of more than one substance. Difenacoum had the highest prevalence (82% in stoats and 88% in weasels) but bromadiolone was detected in the highest concentrations in both stoat (1.290 μg/g ww) and weasel (1.610 μg/g ww). Anticoagulant rodenticide concentrations were highest during autumn and winter and varied with sampling method. Anticoagulant rodenticide concentrations were higher in stoats and weasels with unknown cause of death than in specimens killed by physical trauma. There was a negative correlation between anticoagulant rodenticide concentrations and body condition. Our results suggest that chemical rodent control in Denmark results in an extensive exposure of non-target species and may adversely affect the fitness of some stoats and weasels. PMID:21477845
Sim, Won-Jin; Kim, Hee-Young; Choi, Sung-Deuk; Kwon, Jung-Hwan; Oh, Jeong-Eun
We investigated 33 pharmaceuticals and personal care products (PPCPs) with emphasis on anthelmintics and their metabolites in human sanitary waste treatment plants (HTPs), sewage treatment plants (STPs), hospital wastewater treatment plants (HWTPs), livestock wastewater treatment plants (LWTPs), river water and seawater. PPCPs showed the characteristic specific occurrence patterns according to wastewater sources. The LWTPs and HTPs showed higher levels (maximum 3000 times in influents) of anthelmintics than other wastewater treatment plants, indicating that livestock wastewater and human sanitary waste are one of principal sources of anthelmintics. Among anthelmintics, fenbendazole and its metabolites are relatively high in the LWTPs, while human anthelmintics such as albendazole and flubendazole are most dominant in the HTPs, STPs and HWTPs. The occurrence pattern of fenbendazole's metabolites in water was different from pharmacokinetics studies, showing the possibility of transformation mechanism other than the metabolism in animal bodies by some processes unknown to us. The river water and seawater are generally affected by the point sources, but the distribution patterns in some receiving water are slightly different from the effluent, indicating the influence of non-point sources. PMID:23357510
Full Text Available Anthelmintics used for intestinal helminthiasis treatment are generally effective; however, their effectiveness in tissue parasitosis (i.e. visceral toxocariasis is moderate. The aim of this study was to evaluate the in vitro activity of lapachol, β-lapachone and phenazines in relation to the viability of Toxocara canis larvae. A concentration of 2 mg/mL (in duplicate of the compounds was tested using microculture plates containing Toxocara canis larvae in an RPMI-1640 environment, incubated at 37 °C in 5% CO2 tension for 48 hours. In the 2 mg/mL concentration, four phenazines, lapachol and three of its derivatives presented a larvicide/larvistatic activity of 100%. Then, the minimum larvicide/larvistatic concentration (MLC test was conducted. The compounds that presented the best results were nor-lapachol (MLC, 1 mg/mL, lapachol (MLC 0.5 mg/mL, β-lapachone, and β-C-allyl-lawsone (MLC, 0.25 mg/mL. The larvae exposed to the compounds, at best MLC with 100% in vitro activity larvicide, were inoculated into healthy BALB/c mice and were not capable of causing infection, confirming the larvicide potential in vitro of these compounds.
Rajendraprasad, N.; Basavaiah, K.
Oxfendazole (OFA) is a broad spectrum benzimidazole anthelmintic medication used to treat veterinary diseases. Two new, simple, rapid, precise and accurate, and sensitive spectrophotometric methods have been developed and validated for the assay of OFA in its pure form and in its boluses. The first method (method A) is based on the measurement of green colored manganate obtained due to oxidation of OFA by permanganate in an alkaline medium at 610 nm. In the second method (Method B), the chromophoric activity of OFA is measured at 290 nm in the acetic acid-water (1:1) solvent system. OFA has been quantified over the linear ranges of 1.25-12.5 and 1.25-10 μg/mL in method A and method B, respectively, with apparent molar absorptivity values of 2.54 × 104 and 2.13 × 104 L·mol-1·cm-1. The limit of detection (LOD), limit of quantification (LOQ), and Sandell sensitivity values are 0.15 u 0.18 μg/mL, 0.46 and 0.56 μg/mL, and 0.0124 and 0.0148 μg/cm2. The developed methods were successfully applied to determine OFA in the bolus. No interference from adjuvants was observed.
Luis Javier Mendoza-Estrada
Full Text Available Parasitic agents, such as helminths, are the most important biotic factors affecting aquaculture, and the fluke Centrocestus formosanus is considered to be highly pathogenic in various fish species. There have been efforts to control this parasite with chemical helminthicides, but these efforts have had unsuccessful results. We evaluated the anthelmintic effect of 37 strains of Bacillus thuringiensis against C. formosanus metacercariae in vitro using two concentrations of total protein, and only six strains produced high mortality. The virulence (CL50 on matacercariae of three strains was obtained: the GP308, GP526, and ME1 strains exhibited a LC50 of 146.2 μg/mL, 289.2 μg/mL, and 1721.9 μg/mL, respectively. Additionally, these six B. thuringiensis strains were evaluated against the cercariae of C. formosanus; the LC50 obtained from the GP526 strain with solubilized protein was 83.8 μg/mL, and it could be considered as an alternative control of the metacercariae and cercariae of this parasite in the productivity systems of ornamental fishes.
Mendoza-Estrada, Luis Javier; Hernández-Velázquez, Víctor Manuel; Arenas-Sosa, Iván; Flores-Pérez, Fernando Iván; Morales-Montor, Jorge; Peña-Chora, Guadalupe
Parasitic agents, such as helminths, are the most important biotic factors affecting aquaculture, and the fluke Centrocestus formosanus is considered to be highly pathogenic in various fish species. There have been efforts to control this parasite with chemical helminthicides, but these efforts have had unsuccessful results. We evaluated the anthelmintic effect of 37 strains of Bacillus thuringiensis against C. formosanus metacercariae in vitro using two concentrations of total protein, and only six strains produced high mortality. The virulence (CL50) on matacercariae of three strains was obtained: the GP308, GP526, and ME1 strains exhibited a LC50 of 146.2 μg/mL, 289.2 μg/mL, and 1721.9 μg/mL, respectively. Additionally, these six B. thuringiensis strains were evaluated against the cercariae of C. formosanus; the LC50 obtained from the GP526 strain with solubilized protein was 83.8 μg/mL, and it could be considered as an alternative control of the metacercariae and cercariae of this parasite in the productivity systems of ornamental fishes. PMID:27294137
Kalaiselvan, R; Mohanta, G P; Madhusudan, S; Manna, P K; Manavalan, R
The objective of this study was to improve the oral bioavailability and therapeutic efficacy of albendazole (ABZ) employing solid dispersion and cyclodextrin complexation techniques. Solid dispersion (dispersion) was prepared using ABZ and polyvinylpyrrolidone (PVP) polymer (1:1 weight ratio). Ternary inclusion complex (ternary complex) was prepared using ABZ, hydroxypropyl beta-cyclodextrin (HPbetaCD) and L-tartaric acid (1:1:1 molar ratio). In rabbits with high gastric acidity (gastric pH approximately 1), ternary complex and solid dispersion showed a bioavailability enhancement of 3.2 and 2.4 fold respectively, compared to a commercial suspension (p 5) caused a 62% reduction in AUC (area under the plasma level curve) for the commercial suspension, whereas the reduction in case of PVP dispersion and ternary complex was only 43% and 37% respectively. The rapid absorption of the drug from solid dispersion and ternary complex was reflected in improved anthelmintic efficacy against the systemic phases of Trichinella spiralis. The ternary complex was significantly more efficient than solid dispersion and exhibited the highest larvicidal activity (90%) at a dose of 50 mg x kg(-1) (p < 0.05). These results suggest that the bioavailability and therapeutic efficacy of the ternary complex might be high even if there is a great variation in the gastric pH. PMID:17867556
Full Text Available Breast carcinoma is the most common female cancer with considerable metastatic potential. Discovery of new therapeutic approaches for treatment of metastatic breast cancer is still needed. Here, we reported our finding with niclosamide, an FDA approved anthelmintic drug. The potency of niclosamide on breast cancer was assessed in vitro and in vivo. In this investigation, we found that niclosamide showed a dramatic growth inhibition against breast cancer cell lines and induced apoptosis of 4T1 cells in a dose-dependent manner. Further, Western blot analysis demonstrated the occurrence of its apoptosis was associated with activation of Cleaved caspases-3, down-regulation of Bcl-2, Mcl-1 and Survivin. Moreover, niclosamide blocked breast cancer cells migration and invasion, and the reduction of phosphorylated STAT3(Tyr705, phosphorylated FAK(Tyr925 and phosphorylated Src(Tyr416 were also observed. Furthermore, in our animal experiments, intraperitoneal administration of 20 mg/kg/d niclosamide suppressed 4T1 tumor growth without detectable toxicity. Histological and immunohistochemical analyses revealed a decrease in Ki67-positive cells, VEGF-positive cells and microvessel density (MVD and an increase in Cleaved caspase-3-positive cells upon niclosamide. Notably, niclosamide reduced the number of myeloid-derived suppressor cells (MDSCs in tumor tissues and blocked formation of pulmonary metastases. Taken together, these results demonstrated that niclosamide may be a promising candidate for breast cancer.
Dal Mas, C; Moreira, J T; Pinto, S; Monte, G G; Nering, M B; Oliveira, E B; Gazarini, M L; Mori, M A; Hayashi, M A F
Despite the unquestionable importance of the highly cationic feature of several small polypeptides with high content of positively charged amino acids for their biological activities, positively charged peptides do not necessarily have the capacity to cross the cell membranes. Interestingly, we found that crotamine, a positively charged amphiphilic peptide from the South American rattlesnake venom, has a unique cell-penetrating property with affinity for acidic vesicles, besides a well-characterized antimicrobial and antitumoral activities. In spite of a remarkable in vitro antifungal activity of crotamine against Candida spp., no significant effect of this peptide could be observed in the course of Candida albicans and Candida krusei infection on Caenorhabditis elegans asssed in vivo. These experiments, in which the nematode C. elegans was used as a living host, suggested, however, the potential anthelmintic activity of crotamine because of its uptake by the worms and accumulation in their acidic compartments. As described in the present work, this lysosomotropic property is consistent with a previously proposed mechanism of toxicity of crotamine on mammalian tumoral cell lines. This study also allowed us to propose the cationic peptides with lysosomotropic property, as crotamine, as a potential new class of anthelmentics with ability to overcome the challenging problems of drug resistance. PMID:26713409
Full Text Available Gastrointestinal helminthiasis infections are considerate one of the main limiting factors in sheep production worldwide. The development of parasite resistance to anthelmintics has caused significant losses of small ruminant production. In the search for new alternatives for effective control of gastrointestinal nematodes in small ruminants, phytotherapy is a promising field of research in an attempt to reduce the usage of chemical treatments, aimed at ecological production. Many plants play a crucial role in maintaining animal and human life. During human evolution many interactions with other organisms were established and they have affected each other in many ways. Plants have developed biochemical mechanisms to defend themselves from biological antagonists that act as their natural enemies. This principle has led scientists to search for bio-active compounds produced by plants against pathogens. Since these discovers their metabolites are evaluated against diseases of importance not only in public health, but also in animal production. This article presents a review of studies with tanniniferous plants scientifically tested worldwide for the control of gastrointestinal parasites in ruminants.
Mendoza-Estrada, Luis Javier; Hernández-Velázquez, Víctor Manuel; Arenas-Sosa, Iván; Flores-Pérez, Fernando Iván; Morales-Montor, Jorge; Peña-Chora, Guadalupe
Parasitic agents, such as helminths, are the most important biotic factors affecting aquaculture, and the fluke Centrocestus formosanus is considered to be highly pathogenic in various fish species. There have been efforts to control this parasite with chemical helminthicides, but these efforts have had unsuccessful results. We evaluated the anthelmintic effect of 37 strains of Bacillus thuringiensis against C. formosanus metacercariae in vitro using two concentrations of total protein, and only six strains produced high mortality. The virulence (CL50) on matacercariae of three strains was obtained: the GP308, GP526, and ME1 strains exhibited a LC50 of 146.2 μg/mL, 289.2 μg/mL, and 1721.9 μg/mL, respectively. Additionally, these six B. thuringiensis strains were evaluated against the cercariae of C. formosanus; the LC50 obtained from the GP526 strain with solubilized protein was 83.8 μg/mL, and it could be considered as an alternative control of the metacercariae and cercariae of this parasite in the productivity systems of ornamental fishes. PMID:27294137
Bin Karim, Mohammed Faisal; Imam, Hasan; Sarker, Md Moklesur-Rahman; Uddin, Nizam; Hasan, Nahid; Paul, Nirmala; Haque, Tahmina
In this phyto-pharmacological screening of Pistia stratiotes L leaf and root extracts each separately in two different solvents demonstrated its potential medicinal value. Apparent antioxidant value is demonstrated by DPPH, Nitric oxide scavenging and Ferric ion reducing method. Additionally, total flavonoid and phenolic compounds were measured. The leaf methanolic extract scavenged both nitric oxide (NO) and DPPH radical with a dose dependent manner. But the pet ether fraction of root was found to have highest efficacy in Fe(3±) reducing power assay. Flavonoid was found to contain highest in the pet ether fraction of root (411.35mg/g) in terms of quercetin equivalent, similarly highest amount (34.96mg/g) of total phenolic compounds (assayed as gallic acid equivalents) were found to contain in the same fraction. The methanolic fractions appeared less cytotoxic compared to pet ether extracts. The plant extracts caused a dose dependent decrease in faecal droppings in both castor oil and magnesium sulphate induced diarrhea, where as leaf extracts in each solvent appeared most effective. Also, the plant extracts showed anthelmintic activity in earthworm by inducing paralysis and death in a dose dependent manner. At highest doses (50 mg/ml) all fractions were almost effective as the positive control piperazine citrate (10 mg/ml). Thus, besides this cytotoxic effect it's traditional claim for therapeutic use can never be overlooked. PMID:26004725
Madubuike U. ANYANWU; Chah, Kennedy F.
Antibacterial resistance (AR) is currently one of the greatest threats to mankind as it constitutes health crisis. Extensive use of antibacterial agents in human and veterinary medicine, and farm crops have resulted in emergence of antibacterial-resistant organisms in different environmental settings including aquaculture. Antibacterial resistance in aquaculture is a serious global concern because antibacterial resistance genes (ARGs) can be transferred easily from aquaculture setting to othe...
We induced 3 cell lines that were in vitro cultured from Lepidoptera with heat inactivated Escherichia coil DH5α to stimulate the antibacterial peptide followed by antibacterial activity assay,induction dynamic research and Tricine sodium dodecyl sulfate-polyacrylamide gel electrophoresis (Tricine SDS-PAGE) experiment.The antibacterial activity of the induced BTI-Tn-5B1 cell line was the highest,and the antibacterial activity increased gradually to the highest level in 16 hours after stimulation.A new antibacterial peptide with a molecular weight of about 8000 Da was preferentially induced in Trichoplusia ni BTI-Tn-5B1 ceils in 16 hours after stimulation.Antibacterial activity assays indicated that it had inhibition against Staphylococcus aureus,Escherichia coli K12D31 and Salmonella derby.It has especially strong inhibition against Gram-negative bacteria such as Escherichia coli KI2D31 and Salmonella derby.
Full Text Available Abstract Background The prevention of venous thromboembolism has been identified as a leading priority in hospital safety. Recommended parenteral anticoagulant agents with different indications for the prevention and treatment of venous thromboembolism include unfractionated heparin, low-molecular-weight heparins and fondaparinux. Prescribing decisions in venous thromboembolism management may seem complex due to the large range of clinical indications and patient types, and the range of anticoagulants available. Methods MEDLINE and EMBASE databases were searched to identify relevant original articles. Results Low-molecular-weight heparins have nearly replaced unfractionated heparin as the gold standard antithrombotic agent. Low-molecular-weight heparins currently available in the US are enoxaparin, dalteparin, and tinzaparin. Each low-molecular-weight heparin is a distinct pharmacological entity with different licensed indications and available clinical evidence. Enoxaparin is the only low-molecular-weight heparin that is licensed for both venous thromboembolism prophylaxis and treatment. Enoxaparin also has the largest body of clinical evidence supporting its use across the spectrum of venous thromboembolism management and has been used as the reference standard comparator anticoagulant in trials of new anticoagulants. As well as novel oral anticoagulant agents, biosimilar and/or generic low-molecular-weight heparins are now commercially available. Despite similar anticoagulant properties, studies report differences between the branded and biosimilar and/or generic agents and further clinical studies are required to support the use of biosimilar low-molecular-weight heparins. The newer parenteral anticoagulant, fondaparinux, is now also licensed for venous thromboembolism prophylaxis in surgical patients and the treatment of acute deep-vein thrombosis; clinical experience with this anticoagulant is expanding. Conclusions Parenteral
Full Text Available Thyroid storm is a life-threatening condition that occurs secondary to an uncontrolled hyperthyroid state. Atrial fibrillation is a cardiovascular complication occurring in up to 15% of patients experiencing thyroid storm, and if left untreated this condition could have up to a 25% mortality rate. Thyroid storm with stroke is a rare presentation. This case report details a left middle cerebral artery (MCA stroke with global aphasia and thyroid storm in a 53-year-old Hispanic male patient. Although uncommon, this combination has been reported in multiple case series. Although it is well documented that dysfunctional thyroid levels promote a hypercoagulable state, available guidelines from multiple entities are unclear on whether anticoagulation therapy is appropriate in this situation.
Carazo, Matthew; Berger, Jeffrey S; Reyentovich, Alex; Katz, Stuart D
Heart failure continues to be a leading cause of morbidity and mortality throughout the United States. The pathophysiology of heart failure involves the activation of complex neurohormonal pathways, many of which mediate not only hypertrophy and fibrosis within ventricular myocardium and interstitium, but also activation of platelets and alteration of vascular endothelium. Platelet activation and vascular endothelial dysfunction may contribute to the observed increased risk of thromboembolic events in patients with chronic heart failure. However, current data from clinical trials do not support the routine use of chronic antiplatelet or oral anticoagulation therapy for ambulatory heart failure patients without other indications (atrial fibrillation and/or coronary artery disease) as the risk of bleeding seems to outweigh the potential benefit related to reduction in thromboembolic events. In this review, we consider the potential clinical utility of targeting specific pathophysiological mechanisms of platelet and vascular endothelial activation to guide clinical decision making in heart failure patients. PMID:26501990
Mamdani, M M; Racine, E; McCreadie, S; Zimmerman, C; O'Sullivan, T L; Jensen, G; Ragatzki, P; Stevenson, J G
We conducted a prospective cohort study to evaluate clinical and economic end points achieved by a pharmacist-managed anticoagulation service compared with usual care (50 patients/group). The primary therapeutic end point was the time between starting heparin therapy and surpassing the activated partial thromboplastin time therapeutic threshold. The primary economic end point was the direct variable cost of hospitalization from admission to discharge. No significant differences between groups were noted for the primary therapeutic end point. Total hospital costs were significantly lower for patients receiving pharmacist-managed care than for those receiving usual care ($1594 and $2014, respectively, 1997 dollars, p=0.04). Earlier start of warfarin (p=0.05) and shorter hospital stay (5 and 7 days, p=0.05) were associated with the pharmacist-managed group. PMID:10610013
Kang, K H; Jang, S K; Kim, B K; Park, M K
The butanol extract of Paulownia tomentosa stem showed antibacterial activity against Staphylococcus aureus (SG511, 285 and 503), Streptococcus pyogenes (A308 and A77) and Streptococcus faecium MD8b etc. The most active compound of the extract was identified to be campneoside I, which had a minimal inhibitory concentration (MIC) of 150 micrograms/ml against Streptococcus and Staphylococcus species. From such antibacterial activity, the methoxy group of campneoside I was postulated to be the essential element for the antibacterial activity. PMID:10319161
Muschin, Tegshi; Budragchaa, Davaanyam; Kanamoto, Taisei; Nakashima, Hideki; Ichiyama, Koji; Yamamoto, Naoki; Shuqin, Han; Yoshida, Takashi
Naturally occurring galactomannans were sulfated to give sulfated galactomannans with degrees of substitution of 0.7-1.4 per sugar unit and molecular weights of M¯n=0.6×10(4)-2.4×10(4). Sulfated galactomannans were found to have specific biological activities in vitro such as anticoagulant, anti-HIV and anti-Dengue virus activities. The biological activities were compared with those of standard dextran and curdlan sulfates, which are polysaccharides with potent antiviral activity and low cytotoxicity. It was found that sulfated galactomannans had moderate to high anticoagulant activity, 13.4-36.6unit/mg, compared to that of dextran and curdlan sulfates, 22.7 and 10.0unit/mg, and high anti-HIV and anti-Dengue virus activities, 0.04-0.8μg/mL and 0.2-1.1μg/mL, compared to those curdlan sulfates, 0.1μg/mL, respectively. The cytotoxicity on MT-4 and LCC-MK2 cells was low. Surface plasmon resonance (SPR) of sulfated galactomannans revealed strong interaction with poly-l-lysine as a model compound of virus proteins, and suggested that the specific biological activities might originate in the electrostatic interaction of negatively charged sulfate groups of sulfated galactomannans and positively charged amino groups of surface proteins of viruses. These results suggest that sulfated galactomannans effectively prevented the infection of cells by viruses and the degree of substitution and molecular weights played important roles in the biological activities. PMID:27154517
WANG Jian-qi; SHI Xu-bo; YANG Jin-gang; HU Da-yi
Background Although low-molecular-weight heparin has replaced unfractionated heparin to become the primary anticoagulation drug for treatment of acute coronary syndrome, there is no convenient bedside monitoring method. We explored the best laboratory monitoring method of low-molecular-weight heparins (enoxapadn, dalteparin, and nadroparin) by use of the Sonoclot coagulation analyzer to monitor the activated clotting time.Methods Atotal of 20 healthy volunteers were selected and 15 ml of fasting venous blood samples were collected and incubated. Four coagulants, kaolin, diatomite, glass bead, and magnetic stick, were used to determine the activated clotting time of the low-molecular-weight heparins at different in vitro anti-Xa factor concentrations. A correlation analysis was made to obtain the regression equation. The activated clotting time of the different low-molecular-weight heparins with the same anti-Xa factor concentration was monitored when the coagulant glass beads were applied. Results The activated clotting time measured using the glass beads, diatomite, kaolin, and magnetic stick showed a linear correlation with the concentration of nadroparin (r= 0.964, 0.966, 0.970, and 0.947, respectively). The regression equation showed that the linear slopes of different coagulants were significantly different (glass beads 230.03 s/IU,diatomite 89.91 s/IU, kaolin 50.87 s/IU, magnetic stick could not be calculated). When the concentration of the anti-Xa factor was the same for different low-molecular-weight heparins, the measured activated clotting time was different after the application of the glass bead coagulant.Conclusions The glass bead coagulant is most feasible for monitoring the in vitro anticoagulation activity of nadroparin.The different effects of different low-molecular-weight heparins on the activated clotting time may be related to the different anti-Ila activities.
Wilke, Thomas; Groth, Antje; Pfannkuche, Matthias;
Oral anticoagulation (OAC) with either new oral anticoagulants (NOACs) or Vitamin-K antagonists (VKAs) is recommended by guidelines for patients with atrial fibrillation (AF) and a moderate to high risk of stroke. Based on a claims-based data set the aim of this study was to quantify the stroke...... have been recommended for 56.1/62.9 % of the patients (regarding factors disfavouring VKA/NOAC use). For 38.88/39.20 % of the patient-days in 2010 we could not observe any coverage by anticoagulants. Dementia of patients (OR 2.656) and general prescription patterns of the treating physician (OR 1...
Rahmat, Nur A; Lip, Gregory Y H
In the last decade, we have witnessed the emergence of the oral non-vitamin K oral anticoagulants (NOACs), which have numerous advantages compared with the vitamin K antagonists, particularly their lack of need for monitoring; as a result their use is increasing. Nonetheless, the NOACs face two...... major challenges: the need for reliable laboratory assays to assess their anticoagulation effect, and the lack of approved antidotes to reverse their action. This article provides an overview of monitoring the anticoagulant effect of NOACs and their potential specific antidotes in development....
Velema, Willem A.; van der Berg, Jan Pieter; Hansen, Mickel J.; Szymanski, Wiktor; Driessen, Arnold J. M.; Feringa, Ben L.
Bacterial resistance is a major problem in the modern world, stemming in part from the build-up of antibiotics in the environment. Novel molecular approaches that enable an externally triggered increase in antibiotic activity with high spatiotemporal resolution and auto-inactivation are highly desirable. Here we report a responsive, broad-spectrum, antibacterial agent that can be temporally activated with light, whereupon it auto-inactivates on the scale of hours. The use of such a ‘smart’ antibiotic might prevent the build-up of active antimicrobial material in the environment. Reversible optical control over active drug concentration enables us to obtain pharmacodynamic information. Precisely localized control of activity is achieved, allowing the growth of bacteria to be confined to defined patterns, which has potential for the development of treatments that avoid interference with the endogenous microbial population in other parts of the organism.
Alwar Vidyalakshmi; Kandaswamy Kruthika
Objective: To test efficacy of Parmelia perlata (P. perlata), which is used in traditional medicine for rapid wound healing against test bacteria that cause wound infections. Methods: Different solvents such as methanol, ethyl acetate and acetone were used for extraction of P. perlata. The sensitivity of the test bacteria to solvent extracts of P. perlata was tested by measuring the zone of inhibition on growth media and by determining the minimal inhibitory concentration and minimal bactericidal concentration. Results: Methanol, ethyl acetate and acetone extracts of P.perlata have shown inhibitory activity against Staphylococcus aureus (S.aureus). Conclusions: The results of the present study indicate that P. perlata has potential antibacterial compounds againstS.aureus that causes multitude of skin infections among human beings. Development of drugs from natural compounds can help us to combat antibiotic-resistant bacteria.
Alessandro Morotti; Mauro Felice Frascisco
Life-threatening bleeding in anticoagulation with Warfarin is an emergency challenging issue. Several approaches are available to treat bleeding in either over-anticoagulation or proper-anticoagulation, including vitamin K, fresh frozen plasma and prothrombin complex concentrates (PCC) administration. In coexisting trauma-induced bleeding and anticoagulation, reversal of anticoagulation must be a rapid and highly effective procedure. Furthermore the appropriate treatment must be directly avai...
Pureti Madhu Kumar; PSrinivasa Babu; Shaik Rasheed; Ramadoss Karthikeyan
Objective: To develop and explore the use of PEGylated poly (propylene imine) dendritic architecture for the delivery of an anti bacterial bioactive, Trimethoprim. Methods: For this study, PEGylated poly(propylene imine) dendritic architecture was synthesized and loaded with Trimethoprim and targeted to the resistant producing strains of both gram positive and gram negative. The antibacterial activity was carried out by agar well-diffusion method to compare zone of inhibition with standard drug and plain PPI dendrimer. Results: The study showed that the Trimethoprim loaded dendrimer has significant antibacterial activity than the plain PPI dendrimer, but standard drug was not shown zone of inhibition upon both microorganisms butKlebsiella pneumoniae (K. pneumoniae) the pure drug showed activity. Conclusions: In this study antibacterial activity of synthesized system is also relatively safer and holds potential to deliver any other antibacterial agent to the resistant producing strains.
Lakshmi, C.; K Akshaya Kumar; T J Dennis; T. S. S. P. N. S. Sanath Kumar
The aim of present work is to study the antibacterial activity of polyphenols isolated from the ethyl acetate soluble of methanol extract of stem bark of Garcinia indica against Staphylococcus aureus, Salmonella typhi and Escherichia coli by paper disc method. The results showed good antibacterial activity against S. aureus at higher concentrations, moderate at lower concentrations, against S. typhi moderate at higher concentrations but no activity against E. coli even at higher concentration...
Lakshmi, C.; Kumar, K. Akshaya; T J Dennis; Kumar, T. S. S. P. N. S. Sanath
The aim of present work is to study the antibacterial activity of polyphenols isolated from the ethyl acetate soluble of methanol extract of stem bark of Garcinia indica against Staphylococcus aureus, Salmonella typhi and Escherichia coli by paper disc method. The results showed good antibacterial activity against S. aureus at higher concentrations, moderate at lower concentrations, against S. typhi moderate at higher concentrations but no activity against E. coli even at higher concentration...
Kashani, L. (MD; Okhly, M. (BSc); Ghaemi, EA. (PhD); N. Behnampour; Kashani, E. (MD; Okhly, HO. (BSc); Fendereski, S. (BSc); Bazoori, M. (BSc; Falsafi, L. (MSc)
Background and Objective: Along with antibiotics, the use of biological methods to combat bacteria is notably considered. A natural barrier such as amniotic membrane is one of the ways of dealing with bacterial infections. The aim of this study was to determine the antibacterial effect of human amniotic membrane. Materials and Methods: This descriptive study was performed in Dezyani teaching Hospital of Gorgan University of Medical Sciences, Iran. To evaluate the antibacterial activity agains...
Wright, H. Tonie; Reynolds, Kevin A.
The fatty acid biosynthesis pathway is an attractive but still largely unexploited target for development of new anti-bacterial agents. The extended use of the anti-tuberculosis drug isoniazid and the antiseptic triclosan, which are inhibitors of fatty acid biosynthesis, validates this pathway as a target for anti-bacterial development. Differences in subcellular organization of the bacterial and eukaryotic multi-enzyme fatty acid synthase systems offer the prospect of inhibitors with host vs...
Full Text Available The petroleum ether, chloroform, acetone and water extracts of mushroom Osmoporus odoratus were selected for examine the antibacterial activity against Staphylococcus aureus, Streptococcus pyogenes, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa by disc diffusion method using Muller Hinton agar media. And the extracts were compared with that of standard ampicillin (30 µg and chloramphenicol (30 µg. The water extract alone showed antibacterial activity against the tested organisms and the results were comparable with that of ampicillin rather than chloramphenicol.
Bonneau, Stephane; Maynard, Laurence; Tomczuk, Krzysztof; Kok, Dawid; Eun, Hyone-Myong
In this blinded randomized and controlled study, the anthelmintic efficacy of a tablet formula of ivermectin-praziquantel was evaluated in horses experimentally infected with three species of Strongylus larvae. Eighteen previously dewormed horses were inoculated on study day 0 with third-stage larvae of Strongylus vulgaris, Strongylus equinus, and Strongylus edentatus. The horses were randomly allocated to three groups (n = 6): test-drug (tablet formula), positive-control (reference gel), and negative-control (placebo tablet). On day 56, the horses were treated once with the respective drugs. On day 95, the horses were sacrificed, and necropsy examinations were performed to assess the status of the parasite burden (L4 and immature L5) and pathological lesions on selected organs and tissues. By the criteria of worm counts, the test-drug and positive-control showed, respectively, 100% and 97.3% anthelmintic efficacies on S. vulgaris, 100% and 81.4% on S. equinus, and equally 100% on S. edentatus. However, the efficacies on S. equinus and S. edentatus should be taken only as face values considering their respective low worm counts in the placebo group. The S. vulgaris-induced arterial lesions were also reduced in the test-drug and positive-control groups with efficacies of 73.9% and 62.9%, respectively. No adverse reactions were observed with either of the drugs. Our data demonstrate that the Equimax tablet formula was as safe and efficacious as the gel formula anthelmintic on large strongyles in horses. PMID:19488785
Mwale, Marizvikuru; Masika, Patrick Julius
The study was conducted to determine the anthelmintic efficacy of Aloe ferox, Agave sisalana, and Gunnera perpensa against Heterakis gallinarum in village chickens. The chickens naturally infected with H. gallinarum were randomly divided into 14 groups of eight chickens and orally administered distilled water (negative control), mebendazole (positive control), and graded levels (50-, 100-, 200-, and 400-mg/kg doses) of the three plant extracts. At days 0, 7, and 14, the floatation technique was used to determine fecal egg counts and H. gallinarum worms from chicken ceca were counted at days 0 and 14. Egg count reduction percentage (ECR%) was high at day 7 for all the test materials except for A. sisalana (100 mg/kg) that had 33%. At day 14, ECR% was high for all the other test materials save for A. ferox (200 mg/kg), mebendazole, and distilled water which was 50, 32, and 50%, respectively. A. ferox (200 mg/kg), G. perpensa (200 and 400 mg/kg), and A. sisalana (50 and 100 mg/kg) had the highest (85, 78, 74, 86, and 73%, respectively) worm count reduction percentage. The plants had anthelmintic properties. Advocacy and utilization of these plants in improving the health of village chickens could lead to increased productivity, boosting profits for the poultry industry thereby enabling it to meet the supply of animal protein and enhance livelihoods. It is imperative to determine compounds in the crude extracts of these medicinal plants which are responsible for the anthelmintic activities and their mechanism of action. PMID:25311442
Full Text Available Intraoral hematoma secondary to systemic anticoagulant therapy is rare, but it is a potentially fatal condition requiring immediate medical management. Case report: Here we report a case of self-inflicted hematoma in the anterior maxillary gingival region in a 65year old female cardiac patient who was on systemic anticoagulant therapy with a poor periodontal condition, manifesting as a periodontal swelling for a period of one week. Oral anticoagulant therapy is considerably imperative to prevent thromboembolic complications in various medical conditions, in such patients there are chances for spontaneous bleeding or hematoma by means of minor trauma due to sharp teeth or dental prosthesis in the mouth leading to life threatening complications such as partial or complete airway blockage. Therefore,directives about possible bleeding complications secondary to anticoagulant drugs in the oral cavity and the importance of maintaining oral health hygiene are necessary for the patient.
Heiberg, Ann-Charlotte; Leirs, Herwig; Siegismund, Hans Redlef
Resistance to anticoagulant rodenticides in brown rats (Rattus norvegicus Berk.) is associated with pleiotropic effects, notably with an increased dietary vitamin K requirement. Owing to this disadvantage, resistance is believed to be selected against if anticoagulant selection is absent. In small...... experimental populations of wild brown rats, an investigation was carried out to establish whether tolerance to anticoagulant exposure changed over a period of 2 years. In the same populations, DNA microsatellite markers were used to infer parentage, and this made it possible to estimate reproductive success...... of sensitive and resistant rats and estimate effective population size, Ne. Even though there was evidence for a selection against resistant rats with high vitamin K requirement, anticoagulant tolerance was not seen to be significantly influenced in the absence of bromadiolone selection. As the...
Nielsen, Henriette Svarre; Christiansen, Ole Bjarne
BACKGROUND: Anticardiolipin antibodies (ACA) are found with increased prevalence in women with unexplained recurrent miscarriage (RM) but their impact on future pregnancy outcome in lupus anticoagulant (LAC) negative patients needs better quantification. METHODS: The impact of a repeatedly positive...
Werth, Sebastian; Breslin, Tomás; NiAinle, Fionnuala; Beyer-Westendorf, Jan
Modern direct-acting anticoagulants are rapidly replacing vitamin K antagonists (VKA) in the management of millions of patients worldwide who require anticoagulation. These drugs include agents that inhibit activated factor X (FXa) (such as apixaban and rivaroxaban) or thrombin (such as dabigatran), and are collectively known today as non-VKA oral anticoagulants (NOACs). Since bleeding is the most common and most dangerous side effect of long-term anticoagulation, and because NOACs have very different mechanisms of action and pharmacokinetics compared with VKA, physicians are naturally concerned about the lack of experience regarding frequency, management and outcome of NOAC-associated bleeding in daily care. This review appraises trial and registry (or "real-world") data pertaining to bleeding complications in patients taking NOACs and VKA and provides practical recommendations for the management of acute bleeding situations. PMID:25940651
Spivak, Inna E
Anticoagulation is an important strategy for the prevention of stroke associated with atrial fibrillation. Development of new oral agents has created a need to educate nurses to administer these medications and provide patient education. PMID:26306367
Felice, L J; Chalermchaikit, T; Murphy, M J
A sensitive liquid chromatographic method was developed for the analysis of 4-hydroxycoumarin anticoagulant rodenticides in blood serum. The method can simultaneously measure the serum levels of five anticoagulant rodenticides: brodifacoum, bromadiolone, coumatetralyl, difenacoum, and warfarin. Serum proteins are precipitated with acetonitrile and the supernatant is mixed with ethyl ether. The organic phase is separated, evaporated to dryness, and the residue subjected to chromatographic analysis. The anticoagulants are separated by reversed-phase gradient chromatography with fluorescence detection at an excitation wavelength of 318 nm and emission wavelength of 390 nm. Extraction efficiencies of 68.1 to 98.2% were obtained. The within-run precision (CV) ranged from 2.19 to 3.79% and the between-run precision (CV) from 3.72 to 9.57%. The anticoagulants can be quantitated at serum levels of 10 to 20 ng/mL. PMID:1943055
Fauconnet, V; Pouliquen, H; Pinault, L
A reversed-phase high-performance liquid chromatographic method was developed for the analysis of eight anticoagulant rodenticides in animal liver. Coumarinic anticoagulant rodenticides (brodifacoum, bromadiolone, coumachlor, coumatetralyl, difenacoum, and warfarin) were detected by using a gradient elution and a fluorimetric detection. Indanedione anticoagulant rodenticides (chlorophacinone and diphacinone) were detected by using an isocratic elution and an UV detection. Anticoagulants were extracted from liver with mixtures of acetone/diethylether and acetone/chloroform. Extracts were applied to solid-phase extraction cartridges. Linearity was checked over the concentration range 0.1-0.6 microgram/g. Relative standard deviations of within-run and between-run variability were all between 5.7 and 10.3%. Recoveries from spiked liver samples were between 51.7 (difenacoum) and 78.2% (warfarin). Limits of detection were between 0.01 (difenacoum and warfarin) and 0.11 microgram/g (chlorophacinone). PMID:9399124
Riva, Nicoletta; Ageno, Walter
Anticoagulant treatment can be currently instituted with two different classes of drugs: the vitamin K antagonists (VKAs) and the newer, "novel" or non-vitamin K antagonist oral anticoagulant drugs (NOACs). The NOACs have several practical advantages over VKAs, such as the rapid onset/offset of action, the lower potential for food and drug interactions, and the predictable anticoagulant response. However, the VKAs currently have a broader spectrum of indications, a standardized monitoring test, and established reversal strategies. The NOACs emerged as alternative options for the prevention and treatment of venous thromboembolism and for the prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. Nevertheless, there remain some populations for whom the VKAs remain the most appropriate anticoagulant drug. This article discusses the advantages and disadvantages of VKAs and NOACs. PMID:25703519
Although therapeutic anticoagulation improves early (within 1 month) outcomes after ischemic stroke in hospital-admitted patients with atrial fibrillation, no information exists on late outcomes in unselected population-based studies, including patients with all stroke (ischemic and hemorrhagic).
Full Text Available Vitamin K antagonists, such as warfarin, used in oral anticoagulation therapy currently represent the standard drugs for the primary and secondary prevention of stroke in non-valvular atrial fibrillation (AF, with a relative risk reduction close to 70%. Newer oral anticoagulants, such as direct thrombin inhibitors (i.e., dabigatran and direct factor Xa inhibitors (i.e., apixaban and rivaroxaban have been recently compared with warfarin in large randomized trials for stroke prevention in AF. The new oral anticoagulants showed, compared with warfarin, no statistically significant difference in the rate of stroke or systemic embolism in secondary prevention (patients with previous transient ischemic attack or stroke subgroups. With regard to safety, the risk of intracranial bleeding was reduced with new anticoagulants compared with warfarin. Indirect treatment comparisons of clinical trials on secondary prevention cohorts showed no significant difference in efficacy among apixaban, rivaroxaban, and dabigatran; but dabigatran 110 mg was associated with less intracranial bleedings than rivaroxaban.
This review discusses the basic pharmacology of new oral anticoagulants that are used for prevention of thromboembolism in patients with atrial fibrillation. It presents available evidence, and provides recommendations for the management of patients requiring invasive procedures in dental practice.
Ami M Karkar
Full Text Available Thromboembolism continues to be a major concern in patients with mechanical heart valves, especially in those with unsatisfactory anticoagulation levels. The new On-X valve (On-X Life Technologies, Austin, TX, USA has been reported as having unique structural characteristics that offer lower thrombogenicity to the valve. We report a case where the patient received no or minimal systemic anticoagulation after placement of On-X mitral and aortic valves due to development of severe mucosal arterio-venous malformations yet did not show any evidence of thromboembolism. This case report reinforces the findings of recent studies that lower anticoagulation levels may be acceptable in patients with On-X valves and suggests this valve may be particularly useful in those in whom therapeutic levels of anticoagulation cannot be achieved due to increased risk of bleeding.
Full Text Available Four anthelmintic preparations were tested against some of the most important parasites of reindeer, i.e. warble fly (Oedemagena tarandi, nostril fly (Cephenemyia trompe, brainworm (Elaphostrongylus rangiferi, and lungworm (Dictyocaulus viviparus. Their efficacy against intestinal nematodes was also registered. Test drugs were Fenthion (Bayer, Fenbendazole (Hoechst, Mebendazole (Janssen, and Ivermectin (Merk Sharp & Dohme. Against O. tarandi and C. trompe Ivermectin was 100% effective and Fenthion 86 and 100% respectively. The efficacy of Fen- and Mebendazole against these parasites was not significant. Against E. rangiferi the benzimidazole compounds were highly effective, with Mebendazole a bit ahead. Ivermectin had a moderate effect and Fenthion had no effect on this parasite. Against D. viviparus Fenbendazole, Mebendazole and Ivermectin were of equal, moderate-high effectiveness. No drug had a complete effect on the «arrested» larvae of D. viviparus. Fenthion had no effect at all. Fenbendazole and Ivermectin were both 100% effective against intestinal nematodes. Mebendazole was less effective and Fenthion had no effects. Ivermectin is considered to be the overall most effective anthelmintic in this test.En jamforande studie av effekten av fyra anthelmintika mot några betydelsesfulla parasiter hos ren.Abstract in Swedish / Sammandrag: Fyra antiparasitmedel har prôvats mot några av renens viktigaste parasiter, nàmligen hudkorm (Oedemagena tarandi, svalgkorm (Cephenemyia trompe, hjårnmask (Elaphostrongylus rangiferi och lungmask (Dictyocaulus viviparus. Vidare har medlens effekt på mag- tarmnematoder (Trichostongylider också noterats. De prôvade medicinerna var Fenthion (Bayer, Mebendazole (Leo/Janssen, Fenbendazole (Hoechst och Ivermectin (Merck Sharp & Dohme. Mot hud- och svalgkorm var Ivermectin 100% effektivt medan for Fenthion effekten var 86 resp 100%. Effekten av Fen- och Mebendazole mot de båda parasiterna var inte
Nielsen, Martin Krarup; Vidyashankar, Anand N.; Hanlon, Bret;
Anthelmintic resistance is an increasing challenge for the control of parasites in livestock. The faecal egg count reduction test (FECRT) is the practical gold standard method for evaluating resistance, but the interpretation is complicated due to high levels of variability. A hierarchical...... arithmetic calculations classified nine farms (14.1 %) as resistant and 11 farms (17.2 %) as suspect resistant. Using 10000 Monte Carlo simulated data sets, our methodology provides a reliable classification of farms into different resistance categories with a false discovery rate of 1.02 %. The methodology...
Full Text Available BACKGROUND: Two platyhelminths of biomedical and commercial significance are Schistosoma mansoni (blood fluke and Fasciola hepatica (liver fluke. These related trematodes are responsible for the chronic neglected tropical diseases schistosomiasis and fascioliasis, respectively. As no vaccine is currently available for anti-flukicidal immunoprophylaxis, current treatment is mediated by mono-chemical chemotherapy in the form of mass drug administration (MDA (praziquantel for schistosomiasis or drenching (triclabendazole for fascioliasis programmes. This overreliance on single chemotherapeutic classes has dramatically limited the number of novel chemical entities entering anthelmintic drug discovery pipelines, raising significant concerns for the future of sustainable blood and liver fluke control. METHODOLOGY/ PRINCIPLE FINDINGS: Here we demonstrate that 7-keto-sempervirol, a diterpenoid isolated from Lycium chinense, has dual anthelmintic activity against related S. mansoni and F. hepatica trematodes. Using a microtiter plate-based helminth fluorescent bioassay (HFB, this activity is specific (Therapeutic index = 4.2, when compared to HepG2 cell lines and moderately potent (LD50 = 19.1 μM against S. mansoni schistosomula cultured in vitro. This anti-schistosomula effect translates into activity against both adult male and female schistosomes cultured in vitro where 7-keto-sempervirol negatively affects motility/behaviour, surface architecture (inducing tegumental holes, tubercle swelling and spine loss/shortening, oviposition rates and egg morphology. As assessed by the HFB and microscopic phenotypic scoring matrices, 7-keto-sempervirol also effectively kills in vitro cultured F. hepatica newly excysted juveniles (NEJs, LD50 = 17.7 μM. Scanning electron microscopy (SEM evaluation of adult F. hepatica liver flukes co-cultured in vitro with 7-keto-sempervirol additionally demonstrates phenotypic abnormalities including breaches in tegumental
Naveen Gautam; Abhilasha Yadav; Nishidha Khandelwal; D C Gautam
A series of novel fluorinated 10-phenothiazines were synthesized via Smiles rearrangement. 10-phenothiazines on refluxing with 30% hydrogen peroxide in glacial acetic acid gave 10-phenothiazines-5, 5-dioxides (sulphones). These synthesized 10-phenothiazines were then used as base to prepare ribofuranosides by treating them with sugar (-D-ribofuranosyl- 1-acetate-2, 3, 5-tribenzoate). The synthesized compounds were screened for antimicrobial activity and anthelmintic activity. The structural assignments of compounds were made on the basis of spectroscopic data and elemental analysis.
Hosmane, Sharath R.; Tucker, Johanna; Osman, Dave; Williams, Steve; Waterworth, Paul
Background Warfarin prescription for anticoagulation after cardiac surgery has always been a challenge for junior medical staff. Methods A prospective study was carried out to assess the quality of anticoagulation control by junior doctors compared with clinical pharmacists at South Manchester University hospitals NHS Trust. The junior medical staff prescribed warfarin for 50 consecutive patients from April to September 2006 (group A, n = 50) and experienced clinical pharmacists dosed 46 cons...
Dimova, Cena; Kovacevska, Ivona; Angelovska, Bistra
During the past 20 years, the approval of anticoagulants such as low-molecular-weight heparins (LMWHs), indirect factor Xa inhibitors and direct thrombin inhibitors has signaled a growing interest in antithrombotic compounds that have relatively discrete targets within the coagulation pathway. Aim of this study is to review the evidence of different therapy approach, to highlight the areas of major concern, and to suggest specific oral surgery treatment for patients on new oral anticoagul...
Luca Masotti; Mario Di Napoli; Walter Ageno; Davide Imberti; Cecilia Becattini; Maurizio Paciaroni; Daniel Augustin Godoy; Roberto Cappelli; Giancarlo Landini; Grazia Panigada; Ido Iori; Domenico Prisco; Giancarlo Agnelli
The patients with non-valvular atrial fibrillation (NVAF), both permanent and paroxysmal, and history of previous transient ischemic attack (TIA) or stroke represent a category of patients at high risk of new embolic events, independently of the presence of other risk factors. In these patients, national and international guidelines recommend oral anticoagulants as first choice for antithrombotic prevention. Direct oral anticoagulants (DOACs) have been demonstrated to be not inferior to warfa...
Hanninen, Mikael; Cassagneau, Romain; Manlucu, Jaimie; Yee, Raymond
Lead extraction is becoming increasingly common as indications for pacing and ICD insertion expand. Periop management varies between extraction centers, and no clinical guidelines have addressed the need for perioperative anticoagulation. We report a case of massive thrombosis which occurred shortly after laser lead extraction and is undoubtedly related to the trauma of the extraction and ensuing hypercoagulabiilty. Routine post-operative anticoagulation has been advocated as a means to preve...
Bergen, P. F. van; Deckers, J.W.; Jonker, J. J.; van Domburg, R. T.; Azar, A J; Hofman, A.
OBJECTIVE--To investigate the efficacy of long term oral anticoagulant treatment in subgroups of patients after myocardial infarction. DESIGN--Analysis of the effect of anticoagulant treatment in subgroups of hospital survivors of myocardial infarction based upon age, gender, history of hypertension, previous myocardial infarction, smoking habits, diabetes mellitus, Killip class, anterior location of infarction, thrombolytic therapy, and use of beta blockers. SUBJECTS--Participants of a multi...
Mankee, Anil; Petri, Michelle; Magder, Laurence S.
Introduction Multiple factors, including proteinuria, antiphospholipid syndrome, thrombocytopenia and hypertension, are predictive of pregnancy loss in systemic lupus erythematosus (SLE). In the PROMISSE study of predictors of pregnancy loss, only a battery of lupus anticoagulant tests was predictive of a composite of adverse pregnancy outcomes. We examined the predictive value of one baseline lupus anticoagulant test (dilute Russell viper venom time) with pregnancy loss in women with SLE. Me...
Cappello, M; Vlasuk, G P; Bergum, P W; Huang, S.; Hotez, P. J.
Human hookworm infection is a major cause of gastrointestinal blood loss and iron deficiency anemia, affecting up to one billion people in the developing world. These soil-transmitted helminths cause blood loss during attachment to the intestinal mucosa by lacerating capillaries and ingesting extravasated blood. We have isolated the major anticoagulant used by adult worms to facilitate feeding and exacerbate intestinal blood loss. This 8.7-kDa peptide, named the Ancylostoma caninum anticoagul...
A. A. Rumyantsev; I. A. Pokataev; T.V. Kozlov; N.A. Rumyantsev
Despite large number of known risk factors of venous thromboembolism (VTE) in cancer patients existing prediction models do not allow definite identification of cancer patients that have indications for anticoagulant prevention. Besides, heparin and warfarin use for VTE prevention in cancer is accompanied by some problems. New oral anticoagulants (NOAC) are promising drugs for use in oncology practice; however their use is complicated by the lack of data on efficacy and safety in these patien...
Raj Patel Department of Haematological Medicine, King's Thrombosis Centre, King's College Hospital, London, UK Abstract: Anticoagulation therapy is essential for the effective treatment and secondary prevention of venous thromboembolism (VTE). For many years, anticoagulation for acute VTE was limited to the use of initial parenteral heparin, overlapping with and followed by a vitamin K antagonist. Although highly effective, this regimen has several limitations and is particularly cha...
Raj Patel Department of Haematological Medicine, King's Thrombosis Centre, King's College Hospital, London, UK Abstract: Anticoagulation therapy is essential for the effective treatment and secondary prevention of venous thromboembolism (VTE). For many years, anticoagulation for acute VTE was limited to the use of initial parenteral heparin, overlapping with and followed by a vitamin K antagonist. Although highly effective, this regimen has several limitations and is particul...
Full Text Available BACKGROUND AND AIM OF THE STUDY Optimal duration of oral anticoagulant therapy (OAT in idiopathic venous thromboembolism (VTE is unknown. Indefinite OAT carries an unacceptable risk of major bleeding and prospective studies have demonstrated that OAT is no longer protective after its withdrawal. How to identify the patients at risk for recurrence? D-dimer is a marker of thrombin activity. Early prospective studies showed that elevated D-dimer levels after anticoagulation had a highly predictive value for a recurrent episode. Does D-dimer assay have a role in gauging the appropriate duration of anticoagulant therapy? The PROLONG study tries to answer this question. METHOD D-dimer assay was performed one month after stopping anticoagulation. Patiens with normal D-dimer levels did not resume anticoagulation while patients with elevated D-dimer levels were randomized to discontinue or resume anticoagulation. Study end-points was the composite of recurrent VTE and major bleeding during an average follow-up of 1.4 years. RESULTS The rate of recurrence is significantly higher in patients with elevated D-dimer levels who discontinued anticoagulation. Resuming anticoagulation in this cohort of patients markedly reduces recurrent events without increasing major bleeding. DISCUSSION AND CONCLUSIONS PROLONG study is provocative, because D-dimer assay is simple, thus not requiring dedicated laboratory facilities. D-dimer test has otherwise high sensitivity but low specificity in VTE diagnosis. Aspecifically elevated D-dimer levels are available in the elderly and the majority of patients included in the study were > 65 years old, thus introducing a possible selection bias. Nonetheless the results of the study are useful for the clinician. Prolongation of vitamin K antagonists in patients with elevated D-dimer levels one month after discontinuation of OAT for a first unprovoked episode of VTE results in a favourable risk-benefit relationship. Probably this
Acute mesenteric venous thrombosis is potentially lethal because it can result in mesenteric ischemia and, ultimately, bowel infarction requiring surgical intervention. Systemic anticoagulation for the prevention of thrombus propagation is a well-recognized treatment modality and the current mainstay therapy for patients with acute mesenteric venous thrombosis. However, the decision between prompt surgical exploration vs conservative treatment with anticoagulation is somewhat difficult in pat...
OBJECTIVE: Atrial fibrillation (AF) substantially increases risk of stroke. Evidence suggests that anticoagulation to reduce risk is underused (a "care gap"). Our objectives were to clarify measures of this gap in care by including data from family physicians and to determine why eligible patients were not receiving anticoagulation therapy. DESIGN: Telephone survey of family physicians regarding specific patients in their practices. SETTING: Nova Scotia. PARTICIPANTS: Ambulatory AF patients n...
Drozd, N N; Kuznetsova, S A; Kalinina, T B; Vasilieva, N Yu
Experiments on rabbits showed that increasing the dose of intravenously administered cellulose sulfate from wheat straw (dynamic viscosity 3.4 cP, sulfur content 14.1%) increased plasma clotting time in some coagulation tests and plasma anticoagulant activity. When cellulose sulfate was administered in the dose of 1 mg/kg, plasma clotting time in the presence of the anticoagulant (5 min after administration) was ~3-fold higher than after saline administration. PMID:27165079
Schmid, K; Rohdich, N; Zschiesche, E; Kok, D J; Allan, M J
The efficacy, safety and palatability of a new flavoured chewable anthelmintic tablet were investigated in dogs. The efficacy, based on worm counts, of a single recommended therapeutic dose (RTD) of 5 mg pyrantel + 20 mg oxantel + 5 mg praziquantel/kg bodyweight was assessed in experimental infections (EI) and natural infections (NI) with Trichuris vulpis, Echinococcus granulosus and Toxocara canis. For T vulpis, the efficacy of the treatment was 99.3 per cent in EI (comparing groups of six treated and six control dogs) and 100 per cent in NI (nine treated and nine control dogs). For E granulosus, the efficacy was more than 99.9 per cent in EI (11 treated and 11 control dogs). For T canis, the efficacy was 94.3 per cent in EI (10 treated and 10 control dogs) and 100 per cent in NI (12 treated and 13 control dogs). In a field study, Ancylostoma caninum (11 dogs) and T canis (11 dogs) faecal egg counts were reduced by more than 99 per cent, and in eight dogs with Dipylidium caninum proglotides in the faeces the efficacy was 100 per cent. The tablets were readily consumed by 56 of 64 (87.5 per cent) privately owned dogs. Safety was assessed in groups of six dogs treated either once with twice the RTD, once with six times the RTD, with twice the RTD on three consecutive days, or untreated. There were no significant differences in blood parameters between the groups, and no abnormal clinical findings. Two dogs treated with six times the RTD vomited, but no vomiting was observed when administration was repeated two days later. PMID:21257464
AlGusbi, Salha; Krücken, Jürgen; Ramünke, Sabrina; von Samson-Himmelstjerna, Georg; Demeler, Janina
Effects of the cytochrome P450 inhibitor piperonyl butoxide and the P-glycoprotein inhibitor verapamil on the efficacy of ivermectin and thiabendazole were studied in vitro in susceptible and resistant isolates of the cattle parasitic nematodes Cooperia oncophora and Ostertagia ostertagi. The effects of combined use of drug and piperonyl butoxide/verapamil, respectively, were investigated in the Egg Hatch Assay, the Larval Development Assay and the Larval Migration Inhibition Assay. The effects of piperonyl butoxide and verapamil as inhibitors of thiabendazole and ivermectin responses were particularly marked for larval development, where both inhibitors were able to completely eliminate all differences between susceptible and resistant isolates. Even the lowest concentrations of anthelmintics used in combination with inhibitors caused complete inhibition of development. Differences and/or similarities among responses in different isolates were only obtained in the two other assays: in the Egg Hatch Assay piperonyl butoxide caused a shift in concentration-response curves obtained with thiabendazole to the left for all isolates tested, changing relative differences between isolates. In contrast, an effect of verapamil in the Egg Hatch Assay was only apparent for benzimidazole-resistant isolates. In the Larval Migration Inhibition Assay only ivermectin was tested and piperonyl butoxide shifted the concentration-response curves for all isolates to the left, again eliminating differences in EC50 values between susceptible and resistant isolates. This was not the case using verapamil as an inhibitor, where curves for both susceptible and benzimidazole-resistant isolates shifted to the left in Ostertagia isolates. In Cooperia the picture was more complex with ivermectin-resistant isolates showing a larger shift than the susceptible isolate. Single nucleotide polymorphisms in the β-tubulin isotype 1 gene were investigated. Significantly increased frequencies of
the identification of ligands for a host of potential anthelmintic targets.
Agnelli, Giancarlo; Becattini, Cecilia
The management of patients with acute pulmonary embolism is made challenging by its wide spectrum of clinical presentation and outcome, which is mainly related to patient haemodynamic status and right ventricular overload. Mechanical embolic obstruction and neurohumorally mediated pulmonary vasoconstriction are responsible for right ventricular overload. The pathophysiology of acute pulmonary embolism is the basis for risk stratification of patients as being at high, intermediate and low risk of adverse outcomes. This risk stratification has been advocated to tailor clinical management according to the severity of pulmonary embolism. Anticoagulation is the mainstay of the treatment of acute pulmonary embolism. New direct oral anticoagulants, which are easier to use than conventional anticoagulants, have been compared with conventional anticoagulation in five randomised clinical trials including >11 000 patients with pulmonary embolism. Patients at high risk of pulmonary embolism (those with haemodynamic compromise) were excluded from these studies. Direct oral anticoagulants have been shown to be as effective and at least as safe as conventional anticoagulation in patients with pulmonary embolism without haemodynamic compromise, who are the majority of patients with this disease. Whether these agents are appropriate for the acute-phase treatment of patients at intermediate-high risk pulmonary embolism (those with both right ventricle dysfunction and injury) regardless of any risk stratification remains undefined. PMID:25700388
Full Text Available Several studies have reported underprescription of anticoagulants in atrial fibrillation (AF. We conducted an observational study on 142 out of a total of 995 consecutive ≥75 years old patients presenting AF (14% when admitted in an emergency unit of a general hospital, in search of geriatric characteristics that might be associated with the underprescription of anticoagulation therapy (mostly antivitamin K at the time of the study. The following data was collected from patients presenting AF: medical history including treatment and comorbidities, CHADS2 score, ISAR scale (frailty, Lawton’s scale (ADL, GDS scale (mood status, MUST (nutrition, and blood analysis (INR, kidney function, and albumin. Among those patients for who anticoagulation treatment was recommended (73%, only 61% were treated with it. In the group with anticoagulation therapy, the following characteristics were observed more often than in the group without such therapy: a recent (≤6 months hospitalization and medical treatment including digoxin or based on >3 different drugs. Neither the value of the CHADS2 score, nor the geriatric characteristics could be correlated with the presence or the absence of an anticoagulation therapy. More research is thus required to identify and clarify the relative importance of patient-, physician-, and health care system-related hurdles for the prescription of oral anticoagulation therapy in older patients with AF.
Ofosu, F A; Modi, G J; Blajchman, M A; Buchanan, M R; Johnson, E A
Heparan sulphate and dermatan sulphate have both antithrombotic and anticoagulant properties. These are, however, significantly weaker than those of a comparable amount of standard pig mucosal heparin. Antithrombotic and anticoagulant effects of glycosaminoglycans depend on their ability to catalyse the inhibition of thrombin and/or to inhibit the activation of prothrombin. Since heparan sulphate and dermatan sulphate are less sulphated than unfractionated heparin, we investigated whether the decreased sulphation contributes to the lower antithrombotic and anticoagulant activities compared with standard heparin. To do this, we compared the anticoagulant activities of heparan sulphate and dermatan sulphate with those of their derivatives resulphated in vitro. The ratio of sulphate to carboxylate in these resulphated heparan sulphate and dermatan sulphate derivatives was approximately twice that of the parent compounds and similar to that of standard heparin. Anticoagulant effects were assessed by determining (a) the catalytic effects of each glycosaminoglycan on the inhibition of thrombin added to plasma, and (b) the ability of each glycosaminoglycan to inhibit the activation of 125I-prothrombin in plasma. The least sulphated glycosaminoglycans were least able to catalyse the inhibition of thrombin added to plasma and to inhibit the activation of prothrombin. Furthermore, increasing the degree of sulphation improved the catalytic effects of glycosaminoglycans on the inhibition of thrombin by heparin cofactor II in plasma. The degree of sulphation therefore appears to be an important functional property that contributes significantly to the anticoagulant effects of the two glycosaminoglycans. Images Fig. 1. Fig. 2. Fig. 3. Fig. 4. PMID:2963622
Gómez-Canela, Cristian; Barata, Carlos; Lacorte, Silvia
Anticoagulants are biocides widely used as pest control agents in agriculture, urban infrastructures, and domestic applications for the control of rodents. Other anticoagulants such as warfarin and acenocoumarol are also used as drugs against thrombosis. After use, anticoagulants are discharged to sewage grids and enter wastewater treatment plants (WWTPs). Our hypothesis is that WWTP effluents can be a source of anticoagulants to receiving waters and that these can affect aquatic organisms and other nontarget species. Therefore, the objective of the present study was to determine the occurrence of 11 anticoagulants in WWTPs receiving urban and agricultural wastewaters. Warfarin was the most ubiquitous compound detected in influent waters and was partially eliminated during the activated sludge treatment, and low nanograms per liter concentration were found in the effluents. Other detected compounds were coumatetralyl, ferulenol, acenocoumarol, flocoumafen, brodifacoum, bromadiolone, and difenacoum at concentrations of 0.86-87.0 ng L(-1). Considering water volumes of each WWTP, daily emissions were estimated to be 0.02 to 21.8 g day(-1), and thus, WWTPs contribute to the loads of anticoagulants to receiving waters. However, low aquatic toxicity was observed using Daphnia magna as a model aquatic organism. PMID:24622989
Mehlberg, J; Wittkowsky, A K; Possidente, C
A national survey of pharmacist-managed anticoagulation clinics was conducted to determine how pharmacists are trained to provide care in such clinics. In June 1996 a survey was mailed to 177 pharmacist-managed anticoagulation clinics in the United States. A total of 128 surveys were returned (response rate, 72%). One hundred ten surveys representing 42 states and a variety of institutions were usable. Twenty-five (23%) of the 110 clinics offered an anticoagulation training program for their pharmacists. Most training programs had both didactic and experiential components and had been in existence for one to five years. Thirty-two (29%) of the 110 responding clinics had at least one pharmacist who had completed the ASHP Research and Education Foundation's Anticoagulation Service Traineeship. Twenty-three of the 25 clinics with a training program required successful completion of the program before a pharmacist could practice in the clinic. The overall quality of pharmacists' performance was regularly assessed by 22 of the 25 clinics. Most pharmacist-managed anticoagulation clinics in the United States do not offer formal training in anticoagulation therapy to pharmacists who practice in that setting. PMID:9606455
In this paper, novel multiaction antibacterial nanofibrous membranes containing apatite, Ag, AgBr and TiO2 as four active components were fabricated by an electrospinning technique. In this antibacterial membrane, each component serves a different function: the hydroxyapatite acts as the adsorption material for capturing bacteria, the Ag nanoparticles act as the release-active antibacterial agent, the AgBr nanoparticles act as the visible sensitive and release-active antibacterial agent, and the TiO2 acts as the UV sensitive antibacterial material and substrate for other functional components. Using E. coli as the typical testing organism, such multicomponent membranes exhibit excellent antimicrobial activity under UV light, visible light or in a dark environment. The significant antibacterial properties may be due to the synergetic action of the four major functional components, and the unique porous structure and high surface area of the nanofibrous membrane. It takes only 20 min for the bacteria to be completely (99.9%) destroyed under visible light. Even in a dark environment, about 50 min is enough to kill all of the bacteria. Compared to the four component system in powder form reported previously, the addition of the electrospun membrane could significantly improve the antibacterial inactivation of E. coli under the same evaluation conditions. Besides the superior antimicrobial capability, the permanence of the antibacterial activity of the prepared free-standing membranes was also demonstrated in repeated applications.
Full Text Available Anticoagulant therapy is essential for the prevention of risks associated with the formation of thrombus in patients after surgery, especially in orthopedics. Recently, new oral anticoagulants were introduced in the therapeutic arsenal. This fact is important, because the current drug of choice in clinical practice is enoxaparin, a low molecular weight heparin. As all injecting drugs, enoxaparin may reduce patients' adherence to treatment by dissatisfaction with and resistance to the administration. This article reviews the available literature on the overall utility of these innovative medicines, approaching the pharmacology, the compared efficacy in relation to current agents, and the potential targets for new agents, as well as points to new trends in research and development. The article also contributes with a practical guide for use and recommendations to health professionals, especially focusing on the reversibility of hemorrhagic events, and discusses the importance of convenience/satisfaction of use, the cost of treatment, and the risk-benefit profile for patients.A terapia anticoagulante é fundamental para a prevenção de riscos associados à formação de trombos em pacientes pós-cirúrgicos, principalmente em ortopedia. Recentemente, novos anticoagulantes orais foram introduzidos no arsenal terapêutico. Tal fato é importantíssimo, visto que o atual medicamento de primeira escolha na prática clínica é a enoxaparina, uma heparina de baixo peso molecular. Por ser de uso injetável, a enoxaparina pode diminuir a adesão do paciente ao tratamento, devido à insatisfação e à resistência quanto à via de administração. Este artigo revisa a literatura disponível sobre a utilidade total desses medicamentos inovadores ao abordar a farmacologia, a eficácia em comparação com os agentes atuais e os alvos potenciais para novos agentes, bem como aponta as novas tendências em pesquisa e desenvolvimento. O artigo também contribui
Paraish Misra, MD
Full Text Available Guidelines strongly recommend long-term anticoagulation with warfarin for patients with newly recognized AF who have high embolic risk by virtue of a CHADS2 (Congestive Heart Failure, Hypertension, Age >65, Diabetes, History of Stroke score ≥ 2. The goal of this study was to determine patterns of emergency department-initiated anticoagulation among eligible patients discharged from Canadian centers with an episode of recent-onset atrial fibrillation and flutter (RAFF and determine if decision-making is driven by the CHADS2 score or other factors. This was accomplished by examining health records using uniform case identification and data abstraction as well as centralized quality control; it was conducted in 8 Canadian university emergency departments over a 12-month period. Eligible patients for this analysis demonstrated RAFF requiring emergency management, were not already taking warfarin and were not admitted to hospital. Univariate analyses were conducted using T-test or Chi-square to select factors associated with anticoagulation initiation at a significance level of p < 0.15 and multiple logistic regression was employed to evaluate independent predictors after adjustment for confounders. Among 633 eligible patients, only 21 out of 120 patients (18% with a CHADS2 score ≥ 2 received anticoagulation and among 70 patients who were given anticoagulation only 21 (30% had a CHADS2 score ≥ 2. Independent predictors of anticoagulation included age by 10-year strata: (OR = 1.7; 95% CI 1.3 – 2.1, heparin use in the anticoagulation (OR = 9.6; 95% CI 4.9 – 18.9, a new prescription for metoprolol (OR = 9.6; 95% CI 4.9 – 18.9 and being referred to cardiology for follow-up (OR = 5.6; 95% CI 2.6 – 12.0. CHADS2 ≥ 2 doubled the likelihood of being prescribed anticoagulation (OR= 2.0; 95% CI 1.5 – 3.5 but was not an independent predictor. It was thus determined that patients discharged from the emergency department in this study were not
Full Text Available Piperlonguminine (PL, an important component of Piperlongum fruits, is known to exhibit anti-hyperlipidemic, antiplateletand anti-melanogenic activities. Here, the anticoagulantactivities of PL were examined by monitoring activatedpartial-thromboplastin-time (aPTT, prothrombin-time (PT, andthe activities of thrombin and activated factor X (FXa. Theeffects of PL on the expressions of plasminogen activatorinhibitor type 1 (PAI-1 and tissue-type plasminogen activator(t-PA were also tested in tumor necrosis factor-α (TNF-αactivated HUVECs. The results showed that PL prolonged aPTTand PT significantly and inhibited the activities of thrombin andFXa. PL inhibited the generation of thrombin and FXa inHUVECs. In accordance with these anticoagulant activities, PLprolonged in vivo bleeding time and inhibited TNF-α inducedPAI-1 production. Furthermore, PAI-1/t-PA ratio was significantlydecreased by PL. Collectively, our results suggest that PLpossesses antithrombotic activities and that the current studycould provide bases for the development of new anticoagulantagents. [BMB Reports 2013; 46(10: 484-489
Poposka, Lidija; Boskov, Vladimir; Risteski, Dejan; Taleski, Jane; Georgievska-Ismail, Ljubica
INTRODUCTION: In patients with an implanted pacemaker, asymptomatic atrial fibrillation (AF) is associated with an increased risk of thrombo-embolic complications. There is still no consensus which duration of episodes of atrial fibrillation should be taken as an indicator for inclusion of oral anticoagulation therapy (OAC). MATERIAL AND METHODS: A total of 104 patients who had no AF episodes in the past and have an indication for permanent pacing were included in the study. RESULTS: During an average follow-up of 18 months, 33 of the patients developed episodes of AF. Inclusion of OAC was performed in 17 patients, in whom AF was recorded, although in all patients CHA2DS2-VASc score was ≥ 1. The inclusion of OAC showed a statistically significant correlation with increasing duration of episodes of AF (r = 0.502, p = 0.003). During the follow-up period none of the patients developed thrombo-embolic complication. CONCLUSION: Considering that our group of patients had no thrombo-embolic events, we could conclude that dividing the AF episodes in less than 1% in 24 hours and longer than 1% within 24 hours could be an indicator for decision-making to include OAK if the CHA2DS2-VASc score is ≥ 1. PMID:27335594
Dr. J. David Spence
Full Text Available Patients in atrial fibrillation may have left atrial thrombi or strokes despite adequate anticoagulation. It is important to consider elevated plasma total homocysteine (tHcy as a treatable clotting factor that may explain such cases. Metabolic B12 deficiency is common even in patients with a “normal” serum B12. Measurement of holotranscobalamin, methylmalonic acid or, in folate-replete patients, tHcy are necessary to diagnose metabolic B12 deficiency when the serum B12 is below 400 pmol/L. Elevated tHcy quadruples the risk of stroke in atrial fibrillation, and is far more common than the usual clotting factors for which testing is commonly performed: among patients attending a secondary stroke prevention clinic, tHcy > 14 mmol/L is present in 20% at age 40, and in 40% at age 80. B vitamin therapy does reduce the risk of stroke; key issues are renal impairment and adequacy of vitamin B12. This intervention should be considered routinely in patients with AF.
Vitor Hugo Pomin
Full Text Available Marine sulfated polysaccharides (MSP, such as sulfated fucans (SF, sulfated galactans (SG and glycosaminoglycans (GAG isolated from either algae or invertebrate animals, are highly anionic polysaccharides capable of interacting with certain cationic proteins, such as (co-factors of the coagulation cascade during clotting-inhibition processes. These molecular complexes between MSP and coagulation-related proteins might, at first glance, be assumed to be driven mostly by electrostatic interactions. However, a systematic comparison using several novel sulfated polysaccharides composed of repetitive oligosaccharides with clear sulfation patterns has shown that these molecular interactions are regulated essentially by the stereochemistry of the glycans (which depends on a conjunction of anomericity, monosaccharide, conformational preference, and glycosylation and sulfation sites, rather than just a simple consequence of their negative charge density (mainly the number of sulfate groups. Here, we present an overview of the structure-function relationships of MSP, correlating their structures with their potential anticoagulant and antithrombotic actions, since pathologies related to the cardiovascular system are one of the major causes of illness and mortality in the world.
To evaluate the complications and outcome of anticoagulation therapy in pregnant females with valvular heart diseases. All pregnant females with prosthetic heart valves admitted in Armed Forces Institute of Cardiology from Jan 2004 to Dec 2004 were included in this study Basic demographic data including age, duration of pregnancy and complications observed were recorded. Warfarin was replaced with un-fractionated heparin (UFH) in first trimester and after that warfarin was continued with a targeted INR between 2.0-3.0. At 36 weeks warfarin was stopped and UFH was added; however, if patient went into spontaneous labour before this then immediate caesarian section was performed and UFH was restarted 4-6 hours after delivery along with oral warfarin. Out of 21 patients, sixteen (76.1%) had mitral valve diseases and five (23.9%) had both mitral and atrial. Majority (42.3%)of patients were in age group 26-30 years. Eleven (52.2%) reported in 9th month of gestation. Complications observed were hypertension (1), transient ischaemic attacks (1), pulmonary embolism (1), haemoptysis (1) and abortion (1). All patients, except one had successful completion of pregnancy. No case of foetal abnormality was seen. In 76% patients, daily dose of warfarin was <5 mg. Thrombo-prophylaxis in pregnancy with warfarin and UFH with an INR of 2.0-3.0 is effective in preventing thrombotic complications in females with mechanical valves without resulting in increase hemorrhagic complications. (author)
Prats, Guillem; Rossi, Vilma; Salvatori, Enrica; Mirelis, Beatriz
In the last few years, the antimicrobial activity, efficacy and relative safety of fluoroquinolones have made them attractive for the treatment of community-acquired and nosocomial infections. Prulifloxacin is a new fluoroquinolone antibacterial agent with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is available for oral use, and after absorption is metabolized in to the active form, ulifloxacin. It exhibits good penetration in target tissues and a long elimination half-life, allowing once-daily administration. A number of randomized, controlled clinical trials carried out in Europe demonstrated the efficacy of prulifloxacin in the treatment of urinary tract (acute uncomplicated and complicated) and respiratory tract infections (acute exacerbations of chronic bronchitis), in comparison with the most widely used drugs such as ciprofloxacin, co-amoxiclav and pefloxacin. Prulifloxacin was generally well tolerated. The most frequent adverse reactions observed in clinical trials were gastric pain, diarrhea, nausea and skin rash. This review focuses on the characteristics of prulifloxacin, summarizing the relevant preclinical and clinical data. PMID:16441207
Bakalli, Aurora; Kamberi, Lulzim; Dragusha, Gani; Zeqiri, Nexhmi; Gashi, Fitim; Prekpalaj, Lazer
Background Despite the indisputable role of anticoagulation therapy for atrial fibrillation (AF) patients at risk for stroke, anticoagulants remain under-used in everyday clinical practice. We assumed that by performing trans-oesophageal echocardiography (TEE) on patients with AF who were not on anticoagulation treatment prior to the procedure, and by explaining to them the TEE images obtained, as well as the possible consequences of these findings, we could convince patients to start anticoa...
Khan, Madiha F; Zepeda-Velazquez, Laura; Brook, Michael A
Silicone surfactants are used in a variety of applications, however, limited data is available on the relationship between surfactant structure and biological activity. A series of seven nonionic, silicone polyether surfactants with known structures was tested for in vitro antibacterial activity against Escherichia coli BL21. The compounds varied in their hydrophobic head, comprised of branched silicone structures with 3-10 siloxane linkages and, in two cases, phenyl substitution, and hydrophilic tail of 8-44 poly(ethylene glycol) units. The surfactants were tested at three concentrations: below, at, and above their Critical Micelle Concentrations (CMC) against 5 concentrations of E. coli BL21 in a three-step assay comprised of a 14-24h turbidometric screen, a live-dead stain and viable colony counts. The bacterial concentration had little effect on antibacterial activity. For most of the surfactants, antibacterial activity was higher at concentrations above the CMC. Surfactants with smaller silicone head groups had as much as 4 times the bioactivity of surfactants with larger groups, with the smallest hydrophobe exhibiting potency equivalent to sodium dodecyl sulfate (SDS). Smaller PEG chains were similarly associated with higher potency. These data link lower micelle stability and enhanced permeability of smaller silicone head groups to antibacterial activity. The results demonstrate that simple manipulation of nonionic silicone polyether structure leads to significant changes in antibacterial activity. PMID:26057244
Kashani, L. (MD
Full Text Available Background and Objective: Along with antibiotics, the use of biological methods to combat bacteria is notably considered. A natural barrier such as amniotic membrane is one of the ways of dealing with bacterial infections. The aim of this study was to determine the antibacterial effect of human amniotic membrane. Materials and Methods: This descriptive study was performed in Dezyani teaching Hospital of Gorgan University of Medical Sciences, Iran. To evaluate the antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli bacteria, 20 amniotic membranes were obtained from postpartum mothers and examined by repeated dilution, diffusion and extraction techniques. Data were collected by observation method and described by mean and standard deviation. Results: The antibacterial activity was found in 15% of the samples against Staphylococcus Aureus and Pseudomonas aeruginosa, while no antibacterial activity was found against E. coli. Given the 15% positive responses, "Diffusion" and "repeated dilution" techniques were more effective in investigating the antibacterial effect of amniotic membrane. Conclusion: The results show the probability of antimicrobial effect of amniotic membrane tissue and it seems that this property can be affected by many factors.
Full Text Available Antimicrobial resistance is a natural biological phenomenon of response of microbes to the selective pressure of an antimicrobial drug. Resistance may be inherent, which explains the phenomenon of opportunistic infection or acquired. Concern about the resistance increased in the late 1990′s and since then, many governmental and agency reports have been published regarding the agricultural use of antibacterials, advising less use of antibacterials, appropriate choice of antibacterials and regimens, prevention of cross-infection and development of new antibacterials. The emergence of multidrug resistant strains of Gram-negative bacteria (Pseudomonas, Klebsiella, Enterobacter, Acinetobacter, Salmonella species and Gram-positve organisms (Staphylococcus, Enterococcus, Streptococcus species is the more worrisome in the present therapeutic scenario. Multidrug - resistant tuberculosis is another serious public health problems. Resistance to some agents can be overcome by modifying the dosage regimens (e.g., using high-dose therapy or inhibiting the resistance mechanism (e.g., beta-lactamase inhibitors, whereas other mechanisms of resistance can only be overcome by using an agent from a different class. It is urgently required to ban the sale of antibiotics without prescription, to use antibiotics more judiciously in hospitals by intensive teaching of the principles of the use of antibiotics and to establish better control measures for nosocomial infections. Thus, it is highly recommended that practicing physicians should become aware of the magnitude of existing problem of antibacterial resistance and help in fighting this deadly threat by rational prescribing.
Williams, Andrew Richard; Ropiak, Honorata M.; Fryganas, Christos;
. Oesophagostomum dentatum is an economically important parasite of pigs, as well as serving as a useful laboratory model of helminth parasites due to the ability to culture it in vitro for long periods through several life-cycle stages. Here, we investigated the anthelmintic effects of CT on multiple life cycle...
Haemonchus contortus is a blood-sucking abomasal parasite responsible for major losses to small ruminant producers worldwide. The recent increase in populations of anthelmintic resistant parasites has produced a demand for alternative control methods. An orange oil emulsion that has shown activity...
A liquid chromatographic-tandem mass spectrometric (LC-MS/MS) multi-residue method for the simultaneous quantification and identification of 38 residues of the most widely used anthelmintic veterinary drugs (including benzimidazoles, macrocyclic lactones, and flukicides) in milk and liver has been d...
Hennessy, D.R.; Bauer, C.; Boray, J.C.;
Guidelines are provided for evaluating the efficacy of anthelmintics in swine which, in conjunction with other sets of guidance such as those of the International Cooperation on Harmonization of Technical Requirements for Registration of Veterinary Medicinal Products (VICH GL7 and VICH GL16), sho...
Ayaz, Muhammad; Junaid, Muhammad; Subhan, Fazal; Ullah, Farhat; Sadiq, Abdul; Ahmad, Sajjad; Imran, Muhammad; Kamal, Zul; Hussain, Sajid; Shah, Syed Majid
Background Polygonum hydropiper L decoctions are traditionally used in the treatment of various ailments including inflammation, dyspepsia, diarrhea, menorrhagia, hemorrhoids, helminthiasis and CNS disorders. Present study was undertaken to investigate P. hydropiper L. for heavy metals content, phytoconstituents, Phytotoxic and anthelmintic activities to explore its toxicological and pharmacological potentials and rationalize its ethnomedicinal uses. Methods Plant crude powder, methanolic ext...
Tummala, Ramyashree; Kavtaradze, Ana; Gupta, Anjan; Ghosh, Raktim Kumar
The Vitamin K antagonist warfarin was the only oral anticoagulant available for decades for the treatment of thrombosis and prevention of thromboembolism until Direct Oral Anticoagulants (DOACs); a group of new oral anticoagulants got approved in the last few years. Direct thrombin inhibitor: dabigatran and factor Xa inhibitors: apixaban, rivaroxaban, and edoxaban directly inhibit the coagulation cascade. DOACs have many advantages over warfarin. However, the biggest drawback of DOACs has been the lack of specific antidotes to reverse the anticoagulant effect in emergency situations. Activated charcoal, hemodialysis, and activated Prothrombin Complex Concentrate (PCC) were amongst the nonspecific agents used in a DOAC associated bleeding but with limited success. Idarucizumab, the first novel antidote against direct thrombin inhibitor dabigatran was approved by US FDA in October 2015. It comprehensively reversed dabigatran-induced anticoagulation in a phase I study. A phase III trial on Idarucizumab also complete reversal of anticoagulant effect of dabigatran. Andexanet alfa (PRT064445), a specific reversal agent against factor Xa inhibitors, showed a complete reversal of anticoagulant activity of apixaban and rivaroxaban within minutes after administration without adverse effects in two recently completed parallel phase III trials ANNEXA-A and ANNEXA-R respectively. It is currently being studied in ANNEXA-4, a phase IV study. Aripazine (PER-977), the third reversal agent, has shown promising activity against dabigatran, apixaban, rivaroxaban, as well as subcutaneous fondaparinux and LMWH. This review article summarizes pharmacological characteristics of these novel antidotes, coagulation's tests affected, available clinical and preclinical data, and the need for phase III and IV studies. PMID:27082776
Wei Lai; Shi-Chun Lu; Guan-Yin Li; Chuan-Yun Li; Ju-Shan Wu; Qing-Liang Guo; Meng-Long Wang; Ning Li
AIM:To compare the incidence of early portal or splenic vein thrombosis (PSVT) in patients treated with irregular and regular anticoagulantion alter splenectomy with gastroesophageal devascularization.METHODS:We retrospectively analyzed 301 patients who underwent splenectomy with gastroesophageal devascularization for portal hypertension due to cirrhosis between April 2004 and July 2010.Patients were categorized into group A with irregular anticoagulation and group B with regular anticoagulation,respectively.Group A (153 patients) received anticoagulant monotherapy for an undesignated time period or with aspirin or warfarin without low-molecular-weight heparin (LMWH) irregularly.Group B (148 patients) received subcutaneous injection of LMWH routinely within the first 5 d after surgery,followed by oral warfarin and aspirin for one month regularly.The target prothrombin time/international normalized ratio (PT/INR) was 1.25-1.50.Platelet and PT/INR were monitored.Color Doppler imaging was performed to monitor PSVT as well as the effectiveness of thrombolytic therapy.RESULTS:The patients' data were collected and analyzed retrospectively.Among the patients,94 developed early postoperative mural PSVT,including 63patients in group A (63/153,41.17％) and 31 patients in group B (31/148,20.94％).There were 50 (32.67％)patients in group A and 27 (18.24％) in group B with mural PSVT in the main trunk of portal vein.After the administration of thrombolytic,anticoagulant and antiaggregation therapy,complete or partial thrombus dissolution achieved in 50 (79.37％) in group A and 26 (83.87％) in group B.CONCLUSION:Regular anticoagulation therapy can reduce the incidence of PSVT in patients who undergo splenectomy with gastroesophageal devascularization,and regular anticoagulant therapy is safer and more effective than irregular anticoagulant therapy.Early and timely thrombolytic therapy is imperative and feasible for the prevention of PSVT.
Full Text Available Abstract Background The beneficial outcomes of oral anticoagulation therapy are dependent upon achieving and maintaining an optimal INR therapeutic range. There is growing evidence that better outcomes are achieved when anticoagulation is managed by a pharmacist with expertise in anticoagulation management rather than usual care by family physicians. This study compared a pharmacist managed anticoagulation program (PC to usual physician care (UC in a family medicine clinic. Methods A retrospective cohort study was carried out in a family medicine clinic which included a clinical pharmacist. In 2006, the pharmacist assumed anticoagulation management. For a 17-month period, the PC group (n = 112 of patients on warfarin were compared to the UC patients (n = 81 for a similar period prior to 2006. The primary outcome was the percentage of time patients' INR was in the therapeutic range (TTR. Secondary outcomes were the percentage of time in therapeutic range within ± 0.3 units of the recommended range (expanded TTR and percentage of time the INR was >5.0 or Results The baseline characteristics were similar between the groups. Fifty-five percent of the PC group was male with a mean age of 67 years; 51% of the UC group was male with a mean age of 71 years. The most common indications for warfarin in both groups were atrial fibrillation, mechanical heart valves and deep vein thrombosis. The TTR was 73% for PC and 65% for UC (p 5 were 0.3% for PC patients and 0.1% for UC (p Conclusion The pharmacist-managed anticoagulation program within a family practice clinic compared to usual care by the physicians achieved significantly better INR control as measured by the percentage of time patients' INR values were kept in both the therapeutic and expanded range. Based on the results of this study, a collaborative family practice clinic using pharmacists and physicians may be an effective model for anticoagulation management with these results verified in future
Tang, Zhen-Xing, E-mail: email@example.com [Department of Food Science, Anqing, Vocational and Technical College, Anqing, Anhui (China); Lv, Bin-Feng [Date Palm Research Center, King Faisal University, (Saudi Arabia)
Bacterial pollution is a great risk for human health. Nanotechnology offers a way to develop new inorganic antibacterial agents. Nano-inorganic metal oxide has a potential to reduce bacterial contamination. MgO is an important inorganic oxide and has been widely used in many fields. Many studies have shown that MgO nanoparticles have good antibacterial activity. Therefore, in this paper, the main synthesis methods, antibacterial activity and antibacterial mechanisms of MgO nanoparticles are reviewed. (author)
Gene-encoded antibacterial peptides are multifunctional effector molecules and play an important role in host innate immunity. Upon stimulation, the mature active peptides are released from inactive precursors. Cathelicidins constitute a family of antibacterial peptides, which share a conserved N-terminal cathelin-like region followed by a variable C-terminal antibacterial domain. In addition to its antibacterial activity, LL-37, the only cathelicidin found in human, is ...
Full Text Available Bacterial pollution is a great risk for human health. Nanotechnology offers a way to develop new inorganic antibacterial agents. Nano-inorganic metal oxide has a potential to reduce bacterial contamination. MgO is an important inorganic oxide and has been widely used in many fields. Many studies have shown that MgO nanoparticles have good antibacterial activity. Therefore, in this paper, the main synthesis methods, antibacterial activity and antibacterial mechanisms of MgO nanoparticles are reviewed.
White, Anthony R
The original and successful business model of return on investment being sufficiently attractive to the pharmaceutical industry to encourage development of new antibacterial molecules and related diagnostics has been compromised by increasing development costs and regulatory hurdles, resulting in a decreasing chance of success and financial return. The supply of new effective agents is diminishing along with the number of companies engaged in antibacterial research and development. The BSAC Working Party on The Urgent Need:Regenerating Antibacterial Drug Discovery and Development identified the need to establish, communicate and apply the true health and economic value of antibacterials, along with the adoption of meaningful incentives, as part of the future model for antibacterial development. Robust data are needed on the cost of resistance and ineffective treatment of bacterial infection, along with national and local holistic analyses of the cost-benefit of antibacterials. An understanding of the true health and economic value of antibacterials and the cost of resistance across healthcare systems needs to be generated, communicated and used in order to set a pricing and reimbursement structure that is commensurate with value. The development and economic model of antibacterial use needs to be rebuilt based on this value through dialogue with the various stakeholders, including the pharmaceutical industry, and alternative incentives from 'push' to 'pull' and funding models, such as public/private partnerships, agreed. A research and development model that succeeds in developing and delivering new antibacterial agents that address the health needs of society from start to finish, 'from cradle to grave', must be established. PMID:21700625
Full Text Available In this study, it was investigated that the extracts (ethanol, aceton, methanol, ethyl acetat obtained from fruit peels of the plant to whether has antibacterial effect against Streptococcus mitis CNCTC 4/77, Streptococcus salivarius CNCTC 64/59, Streptococcus mutans CNCTC 8/77, Staphylococcus epidermidis ATCC 12228, Staphylococcus aureus ATCC 29213, Escherichia coli ATCC 25922, Salmonella abony NCTC 6017, Salmonella typhimurium ATCC 14028, Enterococcus faecalis ATCC 29212, Bacillus subtilis ATCC 6633 bacteria strains in vitro. The antibacterial activity of extracts was evaluated according to disc diffusion method. It has been determined that pomegranate peel's extract had the highest inhibition zone diameters ( 18-30 mm against S. epidermidis and S. aureus bacteria strains. The antibacterial activity of plant against Streptococcus mitis is determined in this study for the first time.
Full Text Available Actinopyga lecanora, a type of sea cucumber commonly known as stone fish with relatively high protein content, was explored as raw material for bioactive peptides production. Six proteolytic enzymes, namely alcalase, papain, pepsin, trypsin, bromelain and flavourzyme were used to hydrolyze A. lecanora at different times and their respective degrees of hydrolysis (DH were calculated. Subsequently, antibacterial activity of the A. lecanora hydrolysates, against some common pathogenic Gram positive bacteria (Bacillus subtilis and Staphylococcus aureus and Gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Pseudomonas sp. were evaluated. Papain hydrolysis showed the highest DH value (89.44%, followed by alcalase hydrolysis (83.35%. Bromelain hydrolysate after one and seven hours of hydrolysis exhibited the highest antibacterial activities against Pseudomonas sp., P. aeruginosa and E. coli at 51.85%, 30.07% and 30.45%, respectively compared to the other hydrolysates. Protein hydrolysate generated by papain after 8 h hydrolysis showed maximum antibacterial activity against S. aureus at 20.19%. The potent hydrolysates were further fractionated using RP-HPLC and antibacterial activity of the collected fractions from each hydrolysate were evaluated, wherein among them only three fractions from the bromelain hydrolysates exhibited inhibitory activities against Pseudomonas sp., P. aeruginosa and E. coli at 24%, 25.5% and 27.1%, respectively and one fraction of papain hydrolysate showed antibacterial activity of 33.1% against S. aureus. The evaluation of the relationship between DH and antibacterial activities of papain and bromelain hydrolysates revealed a meaningful correlation of four and six order functions.
Thoracic radiographs and clinical records from 14 dogs with confirmed anticoagulant rodenticide toxicity were reviewed. Twelve of the 14 dogs were presented with a chief complaint of respiratory distress, and 12 had elevated prothrombin and activated partial thromboplastin times consistent with a coagulopathy secondary to a clotting factor deficiency. Thoracic radiographs of the 14 dogs were reviewed and abnomalities included increased mediastinal soft tissue opacity with extra and intrathoracic tracheal narrowing (4/14), increased mediastinal soft tissue opacity without tracheal narrowing (8/14), variable degrees of pleural effusion (13/14) and generalized, patchy interstitial/alveolar pulmonary infiltrates (8/14). Radiographic evidence of cardiomegaly and pulmonary artery abnormalities consistent with concurrent heartworm infestation were detected in one dog. In four dogs, dramatic tracheal narrowing was identified on the lateral thoracic radiograph caused by either mediastinal hemorrhage compressing the trachea or submucosal hemorrhage within the tracheal lumen. The trachea was displaced in a ventral direction in two dogs, and extra and intrathoracic luminal diameter narrowing was evident cranially in all four dogs. Two of these four dogs had soft tissue opacity within the dorsal trachea that extended from the larynx to the intrathoracic trachea. Twelve of the 14 dogs survived with standard treatment protocols utilizing injectable and oral vitamin K1. One dog died from pancreatitis and disseminated intravascular coagulopathy. The other dog died soon after presentation due to severe, disseminated hemorrhage. Follow-up thoracic radiographs were made in four dogs that survived and showed resolution of the mediastinal, pleural and pulmonary changes within one to five days after the initiation of vitamin K1 therapy
Başaran, Özcan; Dogan, Volkan; Beton, Osman; Tekinalp, Mehmet; Aykan, Ahmet Cağri; Kalaycioğlu, Ezgi; Bolat, Ismail; Taşar, Onur; Şafak, Özgen; Kalcik, Macit; Yaman, Mehmet; İnci, Sinan; Altintaş, Bernas; Kalkan, Sedat; Kirma, Cevat; Biteker, Murat
Abstract This study aimed to investigate the potential misuse of novel oral anticoagulants (NOACs) and the physicians’ adherence to current European guideline recommendations in real-world using a large dataset from Real-life Multicenter Survey Evaluating Stroke Prevention Strategies in Turkey (RAMSES Study). RAMSES study is a prospective, multicenter, nationwide registry (ClinicalTrials.gov identifier NCT02344901). In this subgroup analysis of RAMSES study, patients who were on NOACs were classified as appropriately treated (AT), undertreated (UT), and overtreated (OT) according to the European Society of Cardiology (ESC) guidelines. The independent predictors of UT and OT were determined by multivariate logistic regression. Of the 2086 eligible patients, 1247 (59.8%) received adequate treatment. However, off-label use was detected in 839 (40.2%) patients; 634 (30.4%) patients received UT and 205 (9.8%) received OT. Independent predictors of UT included >65 years of age, creatinine clearance ≥50 mL/min, urban living, existing dabigatran treatment, and HAS-BLED score of <3, whereas that of OT were creatinine clearance <50 mL/min, ongoing rivaroxaban treatment, and HAS-BLED score of ≥3. The suboptimal use of NOACs is common because of physicians’ poor compliance to the guideline recommendations in patients with nonvalvular atrial fibrillation (NVAF). Older patients who were on dabigatran treatment with good renal functions and low risk of bleeding were at risk of UT, whereas patients who were on rivaroxaban treatment with renal impairment and high risk of bleeding were at risk of OT. Therefore, a greater emphasis should be given to prescribe the recommended dose for the specified patients. PMID:27583892
Bernard, A; Fauchier, L; Pellegrin, C; Clementy, N; Saint Etienne, C; Banerjee, A; Naudin, D; Angoulvant, D
In patients with atrial fibrillation (AF) undergoing coronary stent implantation, the optimal antithrombotic strategy is unclear. We evaluated whether use of oral anticoagulation (OAC) was associated with any benefit in morbidity or mortality in patients with AF, high risk of thromboembolism (TE) (CHA2DS2-VASC score ≥ 2) and coronary stent implantation. Among 8,962 unselected patients with AF seen between 2000 and 2010, a total of 2,709 (30%) had coronary artery disease and 417/2,709 (15%) underwent stent implantation while having CHA2DS2-VASC score ≥ 2. During follow-up (median=650 days), all TE, bleeding episodes, and major adverse cardiac events (i.e. death, acute myocardial infarction, target lesion revascularisation) were recorded. At discharge, 97/417 patients (23%) received OAC, which was more likely to be prescribed in patients with permanent AF and in those treated for elective stent implantation. The incidence of outcome event rates was not significantly different in patients treated and those not treated with OAC. However, in multivariate analysis, the lack of OAC at discharge was independently associated with increased risk of death/stroke/systemic TE (relative risk [RR] =2.18, 95% confidence interval [CI] 1.02-4.67, p=0.04), with older age (RR =1.12, 1.04-1.20, p=0.003), heart failure (RR =3.26, 1.18-9.01, p=0.02), and history of stroke (RR =18.87, 3.11-111.11, p=0.001). In conclusion, in patients with AF and high thromboembolic risk after stent implantation, use of OAC was independently associated with decreased risk of subsequent death/stroke/systemic TE, suggesting that OAC should be systematically used in this patient population. PMID:23846210
Truong, Teresa; Armor, Becky L
Warfarin is considered a high-risk drug because of its narrow therapeutic window, variability in dose response, and multitude of drug and food interactions. Although travel advice is available for patients who are taking warfarin, it is geared toward patients who are traveling to developed countries and tends to be lacking in detail. We describe a 53-year-old woman with two mechanical heart valves and chronic atrial fibrillation who was taking warfarin for thromboembolism prophylaxis and had plans to travel to Vietnam for 10 weeks. Three days before her departure, she was prescribed amiodarone for long-term use. As a result of the extended duration of her travel and the complexities of warfarin use, the pharmacists who managed the patient's anticoagulation reviewed several aspects of a comprehensive management approach with the patient for a safe international trip. They assessed the patient's thromboembolic and hemorrhagic risks, and determined which other drugs (e.g., enoxaparin, phytonadione), dosages, and adequate supplies would be required along with warfarin, as well as how to safely transport these drugs during travel. In addition, the logistics of effectively monitoring international normalized ratio (INR) levels were evaluated, and methods of managing multiple potential scenarios were carefully planned out. Contact with the patient was made through pharmacist-directed telephone visits throughout the travel period. A total of 12 telephone visits were conducted with the patient during the 10 weeks of travel. Her INR was supratherapeutic on three occasions and was subtherapeutic once; however, neither enoxaparin nor phytonadione were needed during the travel period, and the patient returned safely to the United States. Effective and safe use of high-risk drugs for patients leaving the United States requires extensive pretravel planning, and pharmacists can play a central role in optimizing therapeutic outcomes for these patients during international travel
Wilt, V M; Gums, J G; Ahmed, O I; Moore, L M
The primary objective of this study was to determine if a pharmacist-managed anticoagulation monitoring service (AMS) improved the outcomes of patients receiving warfarin in a family practice setting and was cost effective in treating and preventing thromboembolic disorders. A retrospective chart review was performed on all patients at the University of Florida's Family Practice Residency Program who received warfarin pharmacotherapy between October 1, 1988, and December 15, 1993. The outcomes of patients followed by AMS were compared with those of a control group consisting of patients receiving warfarin but followed only by their physician. Outcomes were evaluated based on the number of thromboembolic and hemorrhagic events, as well as unplanned clinic visits, emergency room visits, and hospital admissions. Cost of hospital admissions, emergency room visits, and participation in the AMS were analyzed. During 28 person-years of treatment, control subjects sustained 12 thromboembolic events (2 pulmonary embolisms, 1 cerebrovascular accident, and 9 deep venous thromboses) and 2 minor and 5 major hemorrhagic events. The study group reported two minor hemorrhagic events during a total of 60 person-years. The control group was 20 times more likely than the study group to experience any event (rate ratio 20, 95% CI 5-87). In addition, hospitalization and emergency room charges indicated an actual cost of $119,074.95 for the control group's events. The cost to this group for 28 person-years of participation in the AMS would have been $5040.00. A potential cost avoidance of $4072.68 per person-year of follow-up may have been possible if these patients had been followed by the AMS. A pharmacist-managed AMS in a family practice setting can result in improved outcomes for patients receiving warfarin and is cost effective. PMID:8602380
Böttger, Björn; Thate-Waschke, Inga-Marion; Bauersachs, Rupert; Kohlmann, Thomas; Wilke, Thomas
Since the introduction of new oral anticoagulants (NOACs), besides vitamin-K antagonists, an additional option for stroke prevention of patients with atrial fibrillation (AF) is available. The objective of this study was to assess AF patients' preferences with regard to the attributes of these different treatment options. We conducted a multicenter study among randomly selected physicians. Preferences were assessed by computer-assisted telephone interviews. We used a discrete-choice-experiment (DCE) with four convenience-related treatment dependent attributes (need of bridging: yes/no, interactions with food/nutrition: yes/no, need of INR controls/dose adjustment: yes/no; frequency of intake: once/twice daily) and one comparator attribute (distance to practitioner: 15 km). Preferences measured in the interviews were analyzed descriptively and based on a conditional logit regression model. A total of 486 AF patients (age: 73.9 ± 8.2 years; 43.2 % female; mean CHA2DS2-VASc: 3.7 ± 1.6; current medication: 48.1 % rivaroxaban, 51.9 % VKA) could be interviewed. Regardless of type of medication, patients significantly preferred the attribute levels (in order of patients' importance) "once daily intake" (Level: once = 1 vs. twice = 0; Coefficient = 0.615; p 15 km = 0 vs. ≤1 km = 1; 0.494; p important OAC-attribute for patients' choice followed by "no bridging necessary" and "no interactions with food/nutrition". Thus, patients with AF seem to prefer treatment options which are easier to administer. PMID:26260625
Full Text Available The use of non-vitamin K antagonist oral anticoagulants (NOACs has become a breakthrough in anticoagulant treatment and it is expected to rise significantly in upcoming years. The use of conventional anticoagulants have several limitations: subcutaneous administration of heparin, or close monitoring of INR during application of vitamin K antagonists. In the last decade, target-specific oral anticoagulants (TSOAC including dabigatran, rivaroxaban, apixaban, edoxaban have been marketed for prophylaxis and treatment. Therefore, it is crucial to understand the potential uses, side effects, and management of these agents in routine practice. NOACs have major pharmacologic advantages, including a rapid onset and offset of action, fewer drug interactions than conventional anticoagulants, and predictable pharmacokinetics. These agents are gaining popularity among both physicians and patients because of their easiness of administration and the eliminating the requirement for regular coagulation monitoring. In this review, we focus on discussing practical recommendations for the use of NOACs and the risks and benefits of incorporating them into routine practice.
Full Text Available In order to search for sulfated polysaccharides in different invertebrate connective tissues and to examine their biological activities, we have isolated three types of polysaccharides from the body wall of the three sea cucumbers Holothuria edulis, Apostichopus japonicas and Holothuria nobilis. The physicochemical properties and anticoagulant activities of these polysaccharides were examined and compared. The chemical composition analysis and nuclear magnetic resonance (NMR analysis indicate that two types of polysaccharides, sulfated fucan and fucosylated chondroitin sulfate (FuCS, were found in all of the three species and in addition a neutral glycan was observed in H. edulis. The neutral α-glucan was firstly obtained from sea cucumber. The same type of polysaccharides from different species of sea cucumbers have similar physicochemical properties and anticoagulant activities, but those of different types of glycans are significantly different, possibly due to their different monosaccharide compositions, electric charges and average molecular weights. The FuCSs have stronger anticoagulant activities than the sulfated fucans, although the molecular sizes of the FuCSs are lower than those of the sulfated fucans, whereas the neutral glucan has no activity, as expected from the absence of sulfate. Thus, anticoagulant activities of the different type of polysaccharides are likely to relate to monosaccharide composition and sulfate content. Preliminary analysis suggests that the sulfation patterns of the FuCSs may result in the difference in anticoagulant activities. Our data could help elucidate the structure-activity relationship of the sea cucumber polysaccharides.
Menssen, H D; Melber, K; Brandt, N; Thiel, E
Undesirable interactions between anticoagulants and diagnostic test kit procedures so far have prevented the development of a single uniform blood sampling tube. Contrary to K2-EDTA, heparin and other anticoagulants, hirudin only minimally alters blood cells and dissolved blood constituents, thus qualifying as a universal anticoagulant for diagnostic purposes. Automated complete blood counts, automated analyses of clinical chemistry analytes and immunohaematology were performed from hirudinised and routinely processed blood obtained from healthy volunteers (n=35) and hospitalised patients (n=45). Hirudin (400 ATU/ml blood) sufficiently anticoagulated blood for diagnostic purposes. The measurements of automated complete blood counts obtained from K2-EDTA-anticoagulated and hirudinised blood correlated significantly as did the measurements of 24 clinical chemistry analytes from hirudinised plasma and serum. Regression analysis revealed that the results of complete blood counts and clinical chemistry tests were predictable from the respective measurements from hirudinised blood (p=0.001). Immunohaematological tests and cross-matching from hirudinised and native blood of the same donors gave identical results. Single clotting factors, but not global coagulation analytes, could be measured from hirudinised blood. Therefore, a universal hirudin-containing blood sampling tube could be designed for automated analysis of haematological, serological and clinical chemistry analytes. PMID:11798089
Romero Guardeño, Araceli; Pérez Lucena, Dolores Amalia
A significant increase during recent years in the number of patients who need Oral Anticoagulant Treatment has meant a greater role for nurses, especially in Primary Health Care Centers, since nurses, along with doctors, are the professionals responsible for treating those patients. This control is carried out by measuring the levels of anticoagulants in the blood, regulating the anticoagulant medicine doses, and providing patients with the essential health education so patients participate in the treatment of their illness. To a large degree, the preponderance of Primary Health Care Centers in the aforementioned control has developed hand-in-hand with the availability of portable, simple and low cost coagulation measuring systems which permit a direct reading of a patient's anticoagulation level with one drop of capillary blood. The objective of this article is introduce the reader to a measuring system appropriate for outpatient clinic control of anticoagulant levels in blood by mans of the CoaguChek XS System, which is described. The authors specify the sample extraction procedure, how to measure coagulant levels, and recommendations to keep in mind while carrying out this procedure. The authors sketch the importance of health education and finally, they describe some advantages and inconveniences this system has. PMID:19462604
Abdou, John K; Auyeung, Vivian; Patel, Jignesh P; Arya, Roopen
Adherence to medication, commonly reported as being 50% in chronic diseases, is of great concern in healthcare. Medication non-adherence is particularly apparent in chronic diseases, where treatment is often preventative and may provide little or no symptomatic relief or feedback for the patient. A lot of research has been undertaken to describe the extent of non-adherence to long-term anticoagulation therapy, particularly with vitamin K antagonists and more recently with direct oral anticoagulants. However, the literature is scarce with respect to describing adherence to anticoagulation in terms of the behavioural aspects that influence medicine use. Utilizing the COM-B (capability, opportunity, motivation and behaviour) psychological model of non-adherence, we present the available evidence, not only in terms of describing the extent of the non-adherence problem, but also describing why patients do not adhere, offering theory-driven and evidence-based solutions to improve long-term adherence to chronic anticoagulation therapy. Lessons learned are not only applicable within the field of anticoagulation but throughout haematology. PMID:27173746
Obamiro, Kehinde O; Chalmers, Leanne; Bereznicki, Luke R E
Atrial fibrillation (AF) is a growing public health concern and remains an independent risk factor for ischemic stroke. Warfarin, a commonly used oral anticoagulant, is associated with a 60-70 % relative reduction in stroke risk and a reduction in mortality of 26 %. However, warfarin has several limitations, including a narrow therapeutic window, variable dose response, multiple interactions with other drugs and concurrent illnesses, and the need for frequent laboratory monitoring. In recent years, the direct acting oral anticoagulants (DOACs), including dabigatran, rivaroxaban, apixaban and edoxaban, have been developed to overcome the limitations of warfarin therapy. These treatment strategies are either comparable or superior to warfarin in stroke prevention in AF. Despite the documented effectiveness of oral anticoagulants in AF, patients may not derive optimal benefit if they fail to adhere or fail to continue with their medication. This may lead to treatment failure, increased hospitalization and mortality. This review summarizes the literature regarding adherence and persistence (or discontinuation) rates with oral anticoagulants in the management of AF; the impact of non-adherence and non-persistence on treatment outcomes; and the effectiveness of strategies to improve adherence and persistence with oral anticoagulant therapy. PMID:27262433
Wellman, Jessica C; Kraus, Peggy S; Burton, Bradley L; Ensor, Christopher R; Nesbit, Todd W; Ross, Patricia A; Thomas, Michelle L; Streiff, Michael B
PURPOSE. A stepwise approach to development and implementation of a program to standardize and increase pharmacists' involvement in anticoagulation therapy at a large academic medical center is described. SUMMARY. In response to the Joint Commission's national goal of improved patient safety in anticoagulation therapy, a work group of pharmacy administrators, educators, clinical specialists, and decentralized pharmacists at the hospital developed the structure for a comprehensive inpatient anticoagulation program (IAP); the work group also developed a list of required competencies, educational materials, assessment methods, and mechanisms for eliciting feedback from IAP pharmacists and other patient care staff. After completion of training that included structured case-review sessions, a one-on-one shadowing experience, and competency assessment, IAP pharmacists began reviewing clinical and laboratory data on patients receiving warfarin and low-molecular-weight heparins and providing recommendations to physicians, nurse practitioners, and other health care team members. Feedback from other clinicians was generally positive, with a majority of those surveyed indicating that increased pharmacist involvement in anticoagulation monitoring and dosage adjustment resulted in improved patient care; about 80% indicated that they concurred with pharmacists' recommendations at least 75% of the time. Results of a survey of IAP pharmacists indicated increased satisfaction with their daily duties but also a need for improved pharmacist-to-pharmacist communication. CONCLUSION. Case-based advanced training and implementation of an IAP in a tertiary care hospital increased pharmacists' involvement in the management of inpatients receiving anticoagulants. PMID:21546645
Battinelli, Elisabeth M; Markens, Beth A; Kulenthirarajan, Rajesh A; Machlus, Kellie R; Flaumenhaft, Robert; Italiano, Joseph E
Platelets are a reservoir for angiogenic proteins that are secreted in a differentially regulated process. Because of the propensity for clotting, patients with malignancy are often anticoagulated with heparin products, which paradoxically offer a survival benefit by an unknown mechanism. We hypothesized that antithrombotic agents alter the release of angiogenesis regulatory proteins from platelets. Our data revealed that platelets exposed to heparins released significantly decreased vascular endothelial growth factor (VEGF) in response to adenosine 5'-diphosphate or tumor cells (MCF-7 cells) and exhibited a decreased angiogenic potential. The releasate from these platelets contained decreased proangiogenic proteins. The novel anticoagulant fondaparinux (Xa inhibitor) demonstrated a similar impact on the platelet angiogenic potential. Because these anticoagulants decrease thrombin generation, we hypothesized that they disrupt signaling through the platelet protease-activated receptor 1 (PAR1) receptor. Addition of PAR1 antagonists to platelets decreased VEGF release and angiogenic potential. Exposure to a PAR1 agonist in the presence of anticoagulants rescued the angiogenic potential. In vivo studies demonstrated that platelets from anticoagulated patients had decreased VEGF release and angiogenic potential. Our data suggest that the mechanism by which antithrombotic agents increase survival and decrease metastasis in cancer patients is through attenuation of platelet angiogenic potential. PMID:24065244
Full Text Available BACKGROUND: Hookworm infections are one of the most important parasitic infections of humans worldwide, considered by some second only to malaria in associated disease burden. Single-dose mass drug administration for soil-transmitted helminths, including hookworms, relies primarily on albendazole, which has variable efficacy. New and better hookworm therapies are urgently needed. Bacillus thuringiensis crystal protein Cry5B has potential as a novel anthelmintic and has been extensively studied in the roundworm Caenorhabditis elegans. Here, we ask whether single-dose Cry5B can provide therapy against a hookworm infection and whether C. elegans mechanism-of-action studies are relevant to hookworms. METHODOLOGY/PRINCIPAL FINDINGS: To test whether the C. elegans invertebrate-specific glycolipid receptor for Cry5B is relevant in hookworms, we fed Ancylostoma ceylanicum hookworm adults Cry5B with and without galactose, an inhibitor of Cry5B-C. elegans glycolipid interactions. As with C. elegans, galactose inhibits Cry5B toxicity in A. ceylanicum. Furthermore, p38 mitogen-activated protein kinase (MAPK, which controls one of the most important Cry5B signal transduction responses in C. elegans, is functionally operational in hookworms. A. ceylanicum hookworms treated with Cry5B up-regulate p38 MAPK and knock down of p38 MAPK activity in hookworms results in hypersensitivity of A. ceylanicum adults to Cry5B attack. Single-dose Cry5B is able to reduce by >90% A. ceylanicum hookworm burdens from infected hamsters, in the process eliminating hookworm egg shedding in feces and protecting infected hamsters from blood loss. Anthelmintic activity is increased about 3-fold, eliminating >97% of the parasites with a single 3 mg dose (∼30 mg/kg, by incorporating a simple formulation to help prevent digestion in the acidic stomach of the host mammal. CONCLUSIONS/SIGNIFICANCE: These studies advance the development of Cry5B protein as a potent, safe single
A. P. Momot
Full Text Available The anticoagulants of indirect action during many years serve drugs of basic prophylaxis and therapy of thromboembolic episodes at cardiovascular , neurological, oncology, orthopaedic and other diseases, after surgical interventions and traumas, and also large bunch of the generically caused and acquired (secondary thrombophilie. The contents of vitamin К1 in nutrition depend on a method of product preparation. The highest concentrations are found in dark green vegetables and grass: parsley, spinach, green turnip, and also in cabbage and lettuce. For achievement stable hypocoagulation at assignment of anticoagulants of indirect action the daily entering with nutrition of constant amounts of vitamin K (at a level 65-80 mkg/day is necessary. Thus, a doctor at assignment of anticoagulants, is obliged to pay attention to character of a food and to inform patient about possible undesirable consequences at the use of products keeping high levels of vitamin К1.
Christensen, Thomas D; Attermann, Jørn; Hjortdal, Vibeke E.;
complications requiring doctoral intervention. All the patients and their parents expressed full satisfaction with the treatment. Conclusion: Selfmanagement of oral anticoagulation provides a good quality of treatment, which is feasible and safe in selected children with congenital cardiac disease.......Objective: The concept of self – management of oral anticoagulation has been shown to entail better quality of treatment than conventional management when assessed in selected adults. We have extended the concept of self – management to include children with congenital cardiac disease......, hypothesizing self-management of oral anticoagulation is also possible in this subset of patients. Our aim was to assess the quality of self-management. Methods: We trained 14 children aged from 2.2 to 15.6 years, with a mean age of 9.7 years, and their parents, in domiciliary analysis of the International...
Heiberg, A.C.; Leirs, H.; Siegismund, Hans Redlef
how bromadiolone-resistant phenotypes are manifested when bromadiolone selection is absent. Experimental populations were established under semi-natural conditions with wild rats trapped at two Danish farms. The individuals caught on each of the two farms were divided into two experimental groups. One......Resistance to anticoagulant rodenticides in Norway rats (Rattus norvegicus) is documented to be associated with pleiotropic effects, notably with an increased dietary vitamin K requirement. The aim of this study was to quantify these effects in small populations of Norway rat in Denmark and to see...... against resistance in the two non-treatment populations was found to be insignificant. Thus, absence of anticoagulant, under the environmental conditions provided, did not lead to a selection favouring anticoagulant-sensitive rats. However, we found some evidence of selection against presumed homozygous...
Stabile, Eugenio; Izzo, Raffaele; Rozza, Francesco; Losi, Maria Angela; Coscioni, Enrico; Trimarco, Bruno
Vitamin K-dependent antagonists (VKAs) are the most commonly used oral anticoagulants. Non-VKA oral anticoagulants (NOACs), directly target factor IIa (dabigatran) or Xa (rivaroxaban, apixaban, and edoxaban) have predictable pharmacological effects and relatively few drug and food interactions compared with VKA. Among NOACs, dabigatran has been extensively tested for stroke prevention in patients with non-valvular atrial fibrillation eligible for oral anticoagulation with VKA. Dabigatran is at least as effective as warfarin at preventing stroke with advantages of less serious bleeding except for gastrointestinal bleeding, which occurs more often than with warfarin. The findings of dabigatran use in randomized trials, post market registries and specific clinical settings are discussed in this article. PMID:27207360
Maas, Angela H E M; Euler, Mia von; Bongers, Marlies Y; Rolden, Herbert J A; Grutters, Janneke P C; Ulrich, Lian; Schenck-Gustafsson, Karin
A growing number of premenopausal women are currently using antithrombotic and/or (dual) antiplatelet therapy for various cardiovascular indications. These may induce or exacerbate abnormal uterine bleeding and more awareness and knowledge among prescribers is required. Heavy and irregular menstrual bleeding is common in women in their forties and may have a variety of underlying causes that require different treatment options. Thus using anticoagulants in premenopausal women demands specific expertise and close collaboration between cardiovascular physicians and gynecologists. In this article we summarize the scope of the problem and provide practical recommendations for the care for young women taking anticoagulants and/or (dual) antiplatelet therapy. We also recommend that more safety data on uterine bleeding with novel anticoagulants in premenopausal women should be obtained. PMID:26358933
The European Food Safety Authority (EFSA) asked the Panel on Dietetic Products, Nutrition and Allergies to provide a scientific statement on the safety of glucosamine for patients receiving coumarin anticoagulants. More than 40 case reports have been collected by drug-monitoring agencies that...... showed in some patients being prescribed coumarin anticoagulants, especially warfarin, that the International Normalised Ratio (INR) increased after they began taking glucosamine, which indicated an increase in the coagulation time. In most cases the increased INR values were symptomless but in some...... cases haemorrhage occurred in a variety of organs, and in one case this resulted in a persistent vegetative state. The evidence for an interaction between glucosamine and coumarin anticoagulants is strengthened by the observation that in the majority of cases the INR began to fall to normal values when...
Greaves, J H; Rehman, A B
Three South-Asian rodent past species were tested for susceptibility to anticoagulant rodenticides. Wheat fluor containing 0-025% warfarin 0-0375% coumatetralyl or 0-005% difenacoum was fed to 260 Tatera indica, 140 Nesokia indica and 81 Bandicota bengalensis for 1-56 days. Tatera was about as susceptible to anticoagulants as Rattus has been reported to be. Nesokia and Bandicota were extremely variable: though the majority were highly susceptible, the slopes of the dose-mortality curves were close to zero. The difenacoum diet appeared to be more toxic than the warfarin diet to all three species, but less toxic than the coumatetralyl diet to Tatera and Nesokia. All of the anticoagulants were eventually lethal to all of the animals tested. PMID:264500
Amartya Kundu; Partha Sardar; Jessica Huston; Parijat Sen; Saurav Chatterjee; Ramez Nairooz; John J. Ryan; Wilbert S. Aronow
Full Text Available Novel Oral Anticoagulants (NOACs such as Dabigatran, Rivaroxaban, Apixaban and Edoxaban are becoming increasingly popular choices for anticoagulation in place of oral Vitamin K Antagonists in various clinical settings. However, they are thought to be associated with an increased risk of gastrointestinal bleeding. Moreover, no specific antidote is available which can rapidly reverse the anti-coagulant action of NOACs raising concern that gastrointestinal bleeding with NOACs could carry a worse prognosis than that associated with conventional agents. In this review, we describe a case of gastrointestinal bleeding in the setting of NOAC use, followed by a brief overview of the pivotal trials involving NOACs. Clinical issues such as pathophysiology, diagnosis and management of NOAC induced GI bleeding have been described. Future trials will help elucidate the true incidence, risk factors and preventive strategies for NOAC associated gastrointestinal bleeding.
Martin, Karlyn; Key, Nigel S
Situations that ordinarily necessitate consideration of anticoagulation, such as arterial and venous thrombotic events and prevention of stroke in atrial fibrillation, become challenging in patients with inherited bleeding disorders such as hemophilia A, hemophilia B, and von Willebrand disease. There are no evidence-based guidelines to direct therapy in these patients, and management strategies that incorporate anticoagulation must weigh a treatment that carries a risk of hemorrhage in a patient who is already at heightened risk against the potential consequences of not treating the thrombotic event. In this paper, we review atherothrombotic disease, venous thrombotic disease, and atrial fibrillation in patients with inherited bleeding disorders, and discuss strategies for using anticoagulants in this population using cases to illustrate these considerations. PMID:27106121
Albert, Nancy M
Atrial fibrillation (AF), a common arrhythmia, increases the risk of ischemic stroke. Stroke and bleeding scores for patients with AF can help to stratify risk and determine the need for antithrombotic therapy, for which warfarin has been the gold standard. Although highly effective, warfarin has several limitations that can lead to its underuse. Data from randomized, Phase III clinical trials of the novel oral anticoagulants, dabigatran, a direct thrombin inhibitor, and rivaroxaban and apixaban, both factor Xa inhibitors, indicate these drugs are at least noninferior to warfarin for the prevention of stroke and systemic embolism. They are easier to administer, and have an equivalent or lower risk of bleeding versus warfarin. A better understanding of the risks and benefits of the novel oral anticoagulants, and their use in clinical practice, will prepare clinicians to anticipate and address educational and clinical needs of AF patients and their families, and promote evidence-based prescription of appropriate and safe anticoagulation therapy. PMID:24373340
Markussen, Mette Drude Kjær; Heiberg, Ann-Charlotte; Fredholm, Merete;
Background: Anticoagulant resistance in Norway rats, Rattus norvegicus (Berk.), has been suggested to be conferred by mutations in the VKORC1 gene, encoding the target protein of anticoagulant rodenticides. Other factors, e.g. pharmacokinetics, may also contribute to resistance, however. To examine...
Mahmoud, W; Redfern, R
The response of Acomys cahirinus to three anticoagulant rodenticides was investigated in the laboratory. In contrast to the other commensal rodents Rattus rattus and R. norvegicus, this species appears to be naturally very resistant to warfarin, difenacoum and brodifacoum. It is considered unlikely that anticoagulant poisons would be effective in the field for the control of A. cahirinus. PMID:7240734
Taki Galanis, MD
Conclusions: These novel, oral anticoagulant agents are legitimate options for the treatment of VTE. A careful assessment of a patient׳s comorbidities, medication use, and laboratory results should be undertaken before prescribing the new oral anticoagulant agents for patients with VTE.