Ji, Wenjin; Liang, Jiexian; Zhang, Zhiwei
Endothelin B receptor agonists exert antipruritic effects on itching induced via endothelin-1 (ET-1) and compound 48/80. Peripheral µ- and κ-opioid receptors (MORs and KORs, respectively) are reported to be involved in the anti-nociceptive properties triggered by ETB agonists. Therefore, we investigated the role of peripheral opioid receptors in the scratching response induced by ET-1. ETA and ETB antagonists and non-selective and selective opioid receptor antagonists were co-injected with ET...
Perilla (Perilla frutescens L.) leaves have shown therapeutic efficacy in the treatment of inflammatory disorders, allergies, bronchial asthma, and systemic damage due to free radicals. In the present study we analyzed the active constituents in perilla leaves using high-performance liquid chromatography (HPLC) and isolated luteolin, a polyphenolic flavonoid. We investigated the anti-inflammatory and antipruritic properties of luteolin. Luteolin inhibited the secretion of inflammatory cytokin...
Itch is a sensation that provokes a desire to scratch. Mast-cell histamine was thought to be a key itch mediator. However, histamine and mast-cell degranulation were reported not to elicit scratching in animals. It was difficult to investigate the pathophysiology of itching and to evaluate the antipruritic efficacy of chemical agents in the early 1990 s. We showed that hind-paw scratching and biting were elicited by stimulation with pruritogenic agents in mice. Those results demonstrated for the first time that cutaneous itching could be evaluated behaviorally in animals. We established various animal models of pathological itch of the skin (dry skin, mosquito allergy, surfactant-induced pruritus, and herpes zoster) and mucus membranes (pollen allergy). Mast-cell histamine did not play a key role in itching in any animal model examined except for the pollen allergy model. Histamine is not an exclusive itch mediator of mast cells; tryptase and leukotriene B4 released from mast cells also act as itch mediators. Epidermal keratinocytes release several itch mediators, such as leukotriene B4, sphingosylphosphorylcholine, thromboxane A2, nociceptin, nitric oxide, and histamine, which may play important roles in pathological itching. Appropriate animal models of pathological itching are needed for pharmacological evaluation of the antipruritic efficacy of chemical agents. PMID:25947907
Yesilyurt, Ozgur; Cayirli, Mutlu; Sakin, Yusuf Serdar; Seyrek, Melik; Akar, Ahmet; Dogrul, Ahmet
The increase of endocannabinoid tonus by inhibiting fatty acid amide hydrolase (FAAH) or monoacylglycerol lipase (MAGL) represents a promising therapeutic approach in a variety of disease to overcome serious central side effects of exocannabinoids. Recent studies reported that systemic administration of FAAH and MAGL inhibitors produce antipruritic action. Dual FAAH/MAGL inhibitors have also been described to get enhanced endocannabinoid therapeutic effect. In this study, we examined and compared dose-related antipruritic effects of systemic (intraperitoneal; ip) or intrathecal (it) administration of selective FAAH inhibitor PF-3845 (5, 10, and 20 mg/kg, i.p.; 1, 5, and 10 µg, i.t.), MAGL inhibitor JZL184 (4, 20, and 40 mg/kg, i.p.; 1, 5, and 10 µg, i.t.) and dual FAAH/MAGL inhibitor JZL195 (2, 5, and 20 mg/kg, i.p.; 1, 5, and 10 µg, i.t.) on serotonin (5-HT)-induced scratching model. Serotonin (25 μg) was injected intradermally in a volume of 50 μl into the rostral part of skin on the back of male Balb-C mice. Both systemic or intrathecal administration of PF-3845, JZL184 or JZL195 produced similar dose-dependent antipruritic effects. Our results suggest that endocannabinoid-degrading enzymes FAAH and MAGL are involved in pruritic process at spinal level. FAAH, MAGL or dual FAAH/MAGL inhibitors have promising antipruritic effects, at least, in part through spinal site of action. PMID:27126057
In Hwa Jeon
Full Text Available Perilla (Perilla frutescens L. leaves have shown therapeutic efficacy in the treatment of inflammatory disorders, allergies, bronchial asthma, and systemic damage due to free radicals. In the present study we analyzed the active constituents in perilla leaves using high-performance liquid chromatography (HPLC and isolated luteolin, a polyphenolic flavonoid. We investigated the anti-inflammatory and antipruritic properties of luteolin. Luteolin inhibited the secretion of inflammatory cytokines such as interleukin-1β (IL-1 β and tumor necrosis factor-α (TNF-α from human mast cells (HMC-1 stimulated with phorbol myristate acetate plus calcium ionophore A23187 in a dose-dependent manner. Luteolin also significantly reduced the histamine release from rat peritoneal mast cells stimulated by compound 48/80, a potent histamine liberator. Furthermore, the administration of luteolin markedly inhibited the scratching behavior and vascular permeability induced by pruritogens, such as compound 48/80 or serotonin, in ICR mice. These results suggested that luteolin has potential as a therapeutic agent against inflammation and itch-related skin diseases.
Andersen, Hjalte H.; Melholt, Camilla; Hilborg, Sigurd D.; Jerwiarz, Anne; Randers, Amalie; Simoni, Amalie; Elberling, Jesper; Arendt-Nielsen, Lars
A frequent empirical observation is that cold-induced counter-irritation may attenuate itch. The aim of this randomized, single-blinded, exploratory study was to evaluate the counter-irritation effects of cold-stimulation and topical application of transient receptor potential TRPA1/M8-agonists...... (trans-cinnamaldehyde/L-menthol, respectively), on histamine-induced itch, wheal and neurogenic inflammation in 13 healthy volunteers. Histamine 1% was applied to the volar forearms using skin prick-testing lancets. Recorded outcome-parameters were itch intensity, wheal reactions and neurogenic......-menthol and trans-cinnamaldehyde had antipruritic efficacy similar to doxepin (p < 0.05). Cold-induced counter-irritation had an inhibitory effect on histaminergic itch, suggesting that agonists of cold transduction receptors could be of potential antipruritic value....
Scott, D W; Rothstein, E; Beningo, K E; Miller, W. H.
Cyproheptadine hydrochloride was administered to 20 presumed or proven allergic cats to determine its efficacy in controlling pruritus. Each cat received 2 mg, orally, every 12 h. The pruritus was satisfactorily controlled in 9 cats. Side effects were seen in 8 cats, and included polyphagia, sedation, vocalization, affectionate behavior, and vomiting.
Gupta, Achla; Gomes, Ivone; Bobeck, Erin N; Fakira, Amanda K; Massaro, Nicholas P; Sharma, Indrajeet; Cavé, Adrien; Hamm, Heidi E; Parello, Joseph; Devi, Lakshmi A
Among the opioid receptors, the κ-opioid receptor (κOR) has been gaining considerable attention as a potential therapeutic target for the treatment of complex CNS disorders including depression, visceral pain, and cocaine addiction. With an interest in discovering novel ligands targeting κOR, we searched natural products for unusual scaffolds and identified collybolide (Colly), a nonnitrogenous sesquiterpene from the mushroom Collybia maculata. This compound has a furyl-δ-lactone core similar to that of Salvinorin A (Sal A), another natural product from the plant Salvia divinorum Characterization of the molecular pharmacological properties reveals that Colly, like Sal A, is a highly potent and selective κOR agonist. However, the two compounds differ in certain signaling and behavioral properties. Colly exhibits 10- to 50-fold higher potency in activating the mitogen-activated protein kinase pathway compared with Sal A. Taken with the fact that the two compounds are equipotent for inhibiting adenylyl cyclase activity, these results suggest that Colly behaves as a biased agonist of κOR. Behavioral studies also support the biased agonistic activity of Colly in that it exhibits ∼10-fold higher potency in blocking non-histamine-mediated itch compared with Sal A, and this difference is not seen in pain attenuation by these two compounds. These results represent a rare example of functional selectivity by two natural products that act on the same receptor. The biased agonistic activity, along with an easily modifiable structure compared with Sal A, makes Colly an ideal candidate for the development of novel therapeutics targeting κOR with reduced side effects. PMID:27162327
Full Text Available The study was an attempt to determine the possibilities of using ovocystatin, a component of a new generation product of natural origin, in local therapy of atopic dermatitis in dogs by suppressing pruritus during illness. Chicken egg cystatin was used locally in the interdigital spaces of forelimbs of dogs used in the experiment. The degree of pruritus and clinical changes in the animals were defined using CADESI-03 scale before and after the beginning of the experiment. The results obtained proved that ovocystatin may be used as a substance suppressing pruritus in atopic dermatitis.
Schilling, J; Mueller, R S
Shampoo therapy is frequently used on pruritic dogs. However, there are few double-blinded, placebo-controlled studies of this form of therapy. This randomised, double-blinded, placebo-controlled study evaluated the efficacy of a commercial medicated shampoo (DermaTopic; Almapharm) containing chlorhexidine, lactoferrin, piroctone olamine, chitosan and essential fatty acids in 27 dogs with mild to moderate allergic pruritus without secondary skin infections. All dogs received shampoo therapy with either DermaTopic or a shampoo vehicle as placebo twice weekly for four weeks. The extent of pruritus was evaluated before the study and then on a daily basis by the owners using a visual analogue scale. Before beginning the treatment and after four weeks, the skin lesions were evaluated by an experienced clinician with a validated lesion score (Canine Atopic Dermatitis Extent and Severity Index - CADESI). The pruritus was reduced significantly by both DermaTopic and placebo. However, there was no significant difference between both groups. There was no statistically significant difference in the CADESI scores pre- and post-treatment in either group or between the two types of treatment. This study provides further evidence of the benefit of shampoo therapy for pruritic dogs. PMID:22678620
A comparison of dexamethasone, ondansetron, and dexamethasone plus ondansetron as prophylactic antiemetic and antipruritic therapy in patients receiving intrathecal morphine for major orthopedic surgery.
In a prospective, double-blinded, randomized trial, we evaluated the efficacy of IV (a) dexamethasone 8 mg, (b) ondansetron 8 mg, and (c) dexamethasone 8 mg plus ondansetron 4 mg for the prevention of postoperative nausea, vomiting (PONV), and pruritus in 130 (ASA physical status I to III) patients undergoing elective major orthopedic surgery after spinal anesthesia with hyperbaric 0.5% bupivacaine and intrathecal morphine. After spinal anesthesia, patients were randomized to one of three groups. Failure of PONV prophylaxis in the 24-h postoperative period occurred more frequently in patients who received dexamethasone alone (29 of 40; 73%) compared with those who received either ondansetron alone (23 of 47; 49%) (P = 0.02) or dexamethasone plus ondansetron together (19 of 43; 44%)(P = 0.01). There was no difference in the incidence of failure of prophylaxis of pruritus (70%, 72%, and 70% in dexamethasone 8 mg, ondansetron 8 mg, and dexamethasone 8 mg plus ondansetron 4 mg, respectively) (P > 0.1) in the 24-h postoperative period. We conclude that the administration of dexamethasone 8 mg with ondansetron 4 mg has no added benefit compared with ondansetron 8 mg alone in the prophylaxis of PONV and pruritus. IMPLICATIONS: Postoperative nausea and vomiting (PONV) and pruritus are common side effects after spinal opioid administration. In this study, dexamethasone 8 mg plus ondansetron 4 mg was as effective as ondansetron 8 mg. The administration of dexamethasone alone was associated with a frequent incidence of PONV, demonstrating a lack of efficacy. This has important cost implications.
李成; 颜晗; 罗意文; 曾繁涛; 路伟; 陈连剑
目的 建立复方达克罗宁薄荷脑润肤止痒水中达克罗宁的含量测定方法 .方法 采用高效液相色谱法,色谱柱为Phenomenex lune(4.6 mm ×250 mm,5 μm),流动相为乙睛-水-三乙胺-冰醋酸(55:43.5:1.0:0.5),流速为0.5 ml/min,检测波长为279 nm,柱温30℃.结果 盐酸达克罗宁的检测线性范围为20.13-120.78 μg/ml,r=0.9995,平均回收率为99.6%,RSD为0.43%(n=6).结论 本法简便、准确、灵敏度高、重复性好,可作为复方达克罗宁薄荷脑润肤止痒水中达克罗宁的含量测定方法 .
谢志强; 杨高云; 姜薇; 徐敏丽
目的 探讨吡美莫司乳膏对成年女性面部皮炎快速抗瘙痒机制.方法 采用研究者总体评估(IGA)、瘙痒程度(SP)评分及参照由温度敏感瞬时受体电位通道建立的痛痒觉基本规则和分子底物方法,评估外用1%吡美莫司乳膏治疗前、后成年女性患者面部皮炎临床体征、SP及皮肤感觉变化.结果 所有患者治疗后第4天和第11天的IGA评分,治疗后第1天、第4天和第11天的SP评分均显著低于治疗前(P均<0.05).52例患者中.有28例(53.8%)在用药数分钟后出现辣椒素样效应,12例(23.1%)出现樟脑样效应,12例(23.1%)未出现辣椒素样效应或樟脑样效应.结论 外用吡美莫司可迅速缓解成年女性面部皮炎的症状和体征,其可能是通过激活皮肤感觉神经上的瞬时受体电位香草类受体1诱导辣椒素样效应或樟脑样效应来达到快速抗瘙痒作用.
Full Text Available D07195 Drug Chloropyramine (INN) C16H20ClN3 289.1346 289.8031 D07195.gif ATC code: D04AA09 R06AC ... ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC . D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHE ... TICS, ETC . D04AA Antihistamines for topical use D04AA09 Chlo ...
Full Text Available D07196 Drug Tolpropamine (INN) C18H23N 253.1831 253.3819 D07196.gif ATC code: D04AA12 Anatomical ... ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC . D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHE ... TICS, ETC . D04AA Antihistamines for topical use D04AA12 Tolp ...
Full Text Available D03285 Drug Diphenhydramine tannate (JP16); Restamin A (TN) Antihistaminic Therapeutic category: ... ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC . D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHE ... TICS, ETC . D04AA Antihistamines for topical use D04AA32 Diph ...
Full Text Available D07679 Drug Chloropyramine hydrochloride; Avapena (TN) C16H20ClN3. HCl 325.1113 326.264 D07679.g ... ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC . D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHE ... TICS, ETC . D04AA Antihistamines for topical use D04AA09 Chlo ...
Full Text Available D07194 Drug Thenalidine (INN) C17H22N2S 286.1504 286.435 D07194.gif ATC code: D04AA03 R06AX03 An ... ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC . D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHE ... TICS, ETC . D04AA Antihistamines for topical use D04AA03 Then ...
Jang, Yongwoo; Lee, Wook-Joo; Hong, Gyu-Sang; Shim, Won-Sik
Background: Korean Red Ginseng—a steamed root of Panax ginseng Meyer—has long been used as a traditional medicine in Asian countries. Its antipruritic effect was recently found, but no molecular mechanisms were revealed. Thus, the current study focused on determining the underlying molecular mechanism of Korean Red Ginseng extract (RGE) against histamine-induced itch at the peripheral sensory neuronal level. Methods: To examine the antipruritic effect of RGE, we performed in vivo scratching b...
Full Text Available D03959 Drug Efalizumab (USAN/INN); Raptiva (TN) Treatment of transplant rejections; Antipruritic ... onoclonal antibody which decreases the activation, migration , and adhesion of T-cells] ATC code: L04AA21 anti-C ... toxicity hsa04670(3683) Leukocyte transendothelial migration ... hsa04810(3683) Regulation of actin cytoskeleton An ...
Chantal Frigon; Joëlle Desparmet
The case of a seven-year-old boy with chronic pruritus secondary to a giant congenital melanocytic nevus is presented. The pruritus did not respond to conventional antipruritic drug treatment, but responded to ondansetron, a selective antagonist of 5-hydroxytryptamine type 3 receptors.
Full Text Available The case of a seven-year-old boy with chronic pruritus secondary to a giant congenital melanocytic nevus is presented. The pruritus did not respond to conventional antipruritic drug treatment, but responded to ondansetron, a selective antagonist of 5-hydroxytryptamine type 3 receptors.
Neurologic itch is defined as pruritus resulting from any dysfunction of the nervous system. Itch arising due to a neuroanatomic pathology is seen to be neuropathic. Causes of neuropathic itch range from localized entrapment of a peripheral nerve to generalized degeneration of small nerve fibers. Antipruritic medications commonly used for other types of itch such as antihistamines and corticosteroids lack efficacy in neuropathic itch. Currently there are no therapeutic options that offer relief in all types of neuropathic pruritus, and treatment strategies vary according to etiology. It is best to decide on the appropriate tests and procedures in collaboration with a neurologist during the initial work-up. Treatment of neuropathic itch includes general antipruritic measures, local or systemic pharmacotherapy, various physical modalities, and surgery. Surgical intervention is the obvious choice of therapy in cases of spinal or cerebral mass, abscess, or hemorrhagic stroke, and may provide decompression in entrapment neuropathies. Symptomatic treatment is needed in the vast majority of patients. General antipruritic measures should be encouraged. Local treatment agents with at least some antipruritic effect include capsaicin, local anesthetics, doxepin, tacrolimus, and botulinum toxin A. Current systemic therapy relies on anticonvulsants such as gabapentin and pregabalin. Phototherapy, transcutaneous electrical nerve stimulation, and physical therapy have also been of value in selected cases. Among the avenues to be explored are transcranial magnetic stimulation of the brain, new topical cannabinoid receptor agonists, various modes of acupuncture, a holistic approach with healing touch, and cell transplantation to the spinal cord. PMID:27578080
Full Text Available Alexandru DP Papoiu,1 Hunza Chaudhry,2 Erin C Hayes,2 Yiong-Huak Chan,3 Kenneth D Herbst4 1Independent contractor, San Diego, CA, USA: 2Cosmederm Bioscience, Inc., San Diego, CA, USA; 3Biostatistics Unit, Yong Loo Lin School of Medicine, National University of Singapore, Singapore; 4Department of Medicine, University of California, San Diego, San Diego, CA, USA Background: Itch is one of the most frequent skin complaints and its treatment is challenging. From a neurophysiological perspective, two distinct peripheral and spinothalamic pathways have been described for itch transmission: a histaminergic pathway and a nonhistaminergic pathway mediated by protease-activated receptors (PAR2 and 4. The nonhistaminergic itch pathway can be activated exogenously by spicules of cowhage, a tropical plant that releases a cysteine protease named mucunain that binds to and activates PAR2 and PAR4. Purpose: This study was conducted to assess the antipruritic effect of a novel over-the-counter (OTC steroid-free topical hydrogel formulation, TriCalm®, in reducing itch intensity and duration, when itch was induced with cowhage, and compared it with two other commonly used OTC anti-itch drugs. Study participants and methods: This double-blinded, vehicle-controlled, randomized, crossover study recorded itch intensity and duration in 48 healthy subjects before and after skin treatment with TriCalm hydrogel, 2% diphenhydramine, 1% hydrocortisone, and hydrogel vehicle, used as a vehicle control. Results: TriCalm hydrogel significantly reduced the peak intensity and duration of cowhage-induced itch when compared to the control itch curve, and was significantly superior to the two other OTC antipruritic agents and its own vehicle in antipruritic effect. TriCalm hydrogel was eight times more effective than 1% hydrocortisone and almost six times more effective than 2% diphenhydramine in antipruritic action, as evaluated by the reduction of area under the curve
Katsunori Yamaura; Ayana Tomono; Eriko Suwa; Koichi Ueno
Background: Royal jelly is widely used as a health tonic, especially in Asia. Royal jelly is commonly used in cosmetics as well as in dietary supplements and beverages. Little is known, however, about the pharmacologic efficacy of topical royal jelly. Therefore, we investigated the antipruritic activity of topical royal jelly on chronic pruritus in experimental allergic contact dermatitis in mice. Materials and Methods: Hairless mice (HOS: HR-1), with chronic allergic contact dermatitis induc...
Gibson, Rachel A.; Jon Robertson; Harshna Mistry; Stewart McCallum; Disala Fernando; Melody Wyres; Gil Yosipovitch
BACKGROUND: Transient receptor potential vanilloid type 1 (TRPV1) is a non-selective cation channel widely expressed in skin tissues, and peripheral sensory nerve fibres. Activation of TRPV1 releases neuropeptides; the resulting neurogenic inflammation is believed to contribute to the development of pruritus. A TRPV1 antagonist has the potential to perform as an anti-pruritic agent. SB705498 is a TRPV1 antagonist that has demonstrated in vitro activity against cloned TRPV1 human receptors and...
Gibson, Rachel A.; Robertson, Jon; Mistry, Harshna; McCallum, Stewart; Fernando, Disala; Wyres, Melody; Yosipovitch, Gil
Background Transient receptor potential vanilloid type 1 (TRPV1) is a non-selective cation channel widely expressed in skin tissues, and peripheral sensory nerve fibres. Activation of TRPV1 releases neuropeptides; the resulting neurogenic inflammation is believed to contribute to the development of pruritus. A TRPV1 antagonist has the potential to perform as an anti-pruritic agent. SB705498 is a TRPV1 antagonist that has demonstrated in vitro activity against cloned TRPV1 human receptors and ...
Özge Gündüz Çınar; Hasan Kırmızıbekmez; Galip Akaydın; Erdem Yesilada
Kappa Opioid Peptide Receptor (KOPr) activation produces analgesic, psychotomimetic, diuretic and antipruritic effects. KOPr ligands are investigated for their potential roles in the treatment of addiction, depression, feeding behavior, psychosis and schizophrenia. In this study the methanolic extracts of a number of Salvia species which are native to Turkey (S. tomentosa, S. tchihatcheffii , S. rosifolia, S. dichroantha and S. sclarea) were tested for their potential binding to opioid recept...
Selvåg, E; Holm, J O; Thune, P
Ethereal oils are widely used, in food, toothpaste, as flavouring agents in perfumes and cosmetics, and in dermatological treatment, as antiseptics, adstringenta, antipruritic tinctures, lotions and pomades. The use of ethereal oils seems to have increased in recent years, probably due to a growing interest in alternative medicine, and especially aromatherapy. By describing the cases of three patients with allergic contact dermatitis, we wish to point out possible unwanted side effects of using ethereal oils. PMID:7491578
BACKGROUND: The incidence of pruritus after elective caesarean section under spinal anaesthesia with subarachnoid morphine may be 60-100%, and is a common cause of maternal dissatisfaction. Ondansetron has been shown to reduce pruritus but the effect is short-lived. The objective of this randomized double-blind trial was to evaluate the anti-pruritic efficacy of granisetron compared with ondansetron. METHODS: Eighty ASA I or II women undergoing elective caesarean section received spinal anaesthesia with 0.5% hyperbaric bupivacaine 10 mg, fentanyl 25 microg and preservative-free morphine 150 microg. After delivery of the baby and clamping of the umbilical cord, they were randomised to receive granisetron 3mg i.v. (group G) or ondansetron 8 mg i.v. (group O). RESULTS: The two groups were similar for age, gestational age, height and weight. According to visual analogue pruritus scores, patients in group G experienced less pruritus at 8h (P=0.003) and 24h (P=0.01). Fewer patients in group G (n=8) than group O (n=18) required rescue anti-pruritic medication (P=0.03). Satisfaction scores were also higher in group G than in group O (P=0.03). There was no difference in overall incidence of pruritus, nausea and vomiting, and visual analogue pain scores between the two groups. CONCLUSIONS: Administration of granisetron 3mg i.v. reduces the severity of pruritus and the use of rescue anti-pruritic medication, and improves satisfaction but does not reduce the overall incidence of pruritus in women who have received subarachnoid morphine 150 microg compared to ondansetron 8 mg i.v.
Objective:To observe the efficacy and safety of Shu Antipruritic Skin Cream combined with Cetirizine oral liquid in treatment of children with eczema. Methods:60 cases were randomly divided into the treatment group and 62 cases in the control group,.The treatment group was treated with Shu Antipruritic Skin Cream with Cetirizine oral liquid ,and the control group with Cetirizine oral liquid and Hydrocortisone Butyrate. The response was evaluated at 1 month .Results:The effective rate of the treatment group was 83.05%, 66.67% in the control group. There was a significant difference between the two groups’ effective rate (P=0.034) .Conclusion:The effective rate of Shu Antipruritic Skin Cream combined with Cetirizine oral liquid is high in treatment of children with eczema , and has no side effect of steroids.%目的：观察肤舒止痒膏联合西替利嗪口服液治疗儿童湿疹的疗效和安全性。方法：随机分为治疗组60例和对照组62例，两组均口服西替利嗪口服液，治疗组外用肤舒止痒膏，对照组外用丁酸氢化可的松软膏，治疗1月后判效。结果：治疗组有效率为83.05%，对照组为66.67%，二者差异有统计学意义（P=0.034）。结论：肤舒止痒膏联合西替利嗪口服液治疗儿童湿疹临床痊愈率高，且无激素副作用。
Full Text Available OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE C05AD Local anesthetics C05AD04 Cinchocaine D02220 Dibucain... ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AB Anesthetics for topical use D04AB02 Cinchoca... ANESTHETICS, LOCAL N01BB Amides N01BB06 Cinchocaine D02220 Dibucaine hydrochloride (JP16/USP) S SENSORY ORG...ANS S01 OPHTHALMOLOGICALS S01H LOCAL ANESTHETICS S01HA Local anesthetics S01HA06 Cinchocaine D02220 Dibucain...s and anesthetics S02DA04 Cinchocaine D02220 Dibucaine hydrochloride (JP16/USP) Target-based classification
Full Text Available D00733 Drug Dibucaine (USP); Cinchocaine (INN); Nupercaine (TN) C20H29N3O2 343.226 ...l anesthetics C05AD04 Cinchocaine D00733 Dibucaine (USP); Cinchocaine (INN) D DERMATOLOGICALS D04 ANTIPRURIT...AB Anesthetics for topical use D04AB02 Cinchocaine D00733 Dibucaine (USP); Cinchocaine (INN) N NERVOUS SYSTE...M N01 ANESTHETICS N01B ANESTHETICS, LOCAL N01BB Amides N01BB06 Cinchocaine D00733...l anesthetics S01HA06 Cinchocaine D00733 Dibucaine (USP); Cinchocaine (INN) S02 OTOLOGICALS S02D OTHER OTOLO
Tekin, Hande Gazeteci; Gökben, Sarenur; Serdaroğlu, Gül
Camphor is a cyclic ketone of the hydro aromatic terpene group. Today it is frequently used as a prescription or non-prescription topical antitussive, analgesic, anesthetic and antipruritic agent. Camphor which is considered an innocent drug by parents and physicians is a common household item which can lead to severe poisoning in children even when taken in small amounts. Neurotoxicity in the form of seizures can ocur soon after ingestion. A two-year old female patient who presented with a complaint of generalized tonic-clonic seizures after oral ingestion of camphor is presented. PMID:26884696
Kamo, Atsuko; Tominaga, Mitsutoshi; Kamata, Yayoi; Kaneda, Kazuyuki; Ko, Kyi C; Matsuda, Hironori; Kimura, Utako; Ogawa, Hideoki; Takamori, Kenji
Epidermal hyperinnervation, which is thought to underlie intractable pruritus, has been observed in patients with atopic dermatitis (AD). The epidermal expression of axonal guidance molecules has been reported to regulate epidermal hyperinnervation. Previously, we showed that the excimer lamp has antihyperinnervative effects in nonpruritic dry-skin model mice, although epidermal expression of axonal guidance molecules was unchanged. Therefore, we investigated the antipruritic effects of excimer lamp irradiation and its mechanism of action. A single irradiation of AD model mice significantly inhibited itch-related behavior 1 day later, following improvement in the dermatitis score. In addition, irradiation of nerve fibers formed by cultured dorsal root ganglion neurons increased bleb formation and decreased nerve fiber expression of nicotinamide mononucleotide adenylyl transferase 2, suggesting degenerative changes in these fibers. We also analyzed whether attaching a cutoff excimer filter (COF) to the lamp, thus decreasing cytotoxic wavelengths, altered hyperinnervation and the production of cyclobutane pyrimidine dimer (CPD), a DNA damage marker, in dry-skin model mice. Irradiation with COF decreased CPD production in keratinocytes, as well as having an antihyperinnervative effect, indicating that the antipruritic effects of excimer lamp irradiation with COF are due to induction of epidermal nerve degeneration and reduced DNA damage. PMID:24940652
Yang, Niu-Niu; Shi, Hao; Yu, Guang; Wang, Chang-Ming; Zhu, Chan; Yang, Yan; Yuan, Xiao-Lin; Tang, Min; Wang, Zhong-Li; Gegen, Tana; He, Qian; Tang, Kehua; Lan, Lei; Wu, Guan-Yi; Tang, Zong-Xiang
Osthole, an active coumarin isolated from Cnidium monnieri (L.) Cusson, has long been used in China as an antipruritic herbal medicine; however, the antipruitic mechanism of osthole is unknown. We studied the molecular mechanism of osthole in histamine-dependent itch by behavioral test, Ca(2+) imaging, and electrophysiological experiments. First, osthole clearly remitted the scratching behaviors of mice induced with histamine, HTMT, and VUF8430. Second, in cultured dorsal root ganglion (DRG) neurons, osthole showed a dose-dependent inhibitory effect to histamine. On the same neurons, osthole also decreased the response to capsaicin and histamine. In further tests, the capsaicin-induced inward currents were inhibited by osthole. These results revealed that osthole inhibited histamine-dependent itch by modulating TRPV1 activity. This study will be helpful in understanding how osthole exerts anti-pruritus effects and suggests that osthole may be a useful treatment medicine for histamine-dependent itch. PMID:27160770
Matsuda, Kazuki M; Sharma, Divya; Schonfeld, Ariel R; Kwatra, Shawn G
Chronic pruritus is a distressing symptom that is often refractory to treatment. Patients frequently fail topical therapies and oral over-the-counter antihistamines, prompting the clinician to consider alternative therapies such as neuroactive agents. Herein, the use of gabapentin and pregabalin, 2 medications well known for treating neuropathic pain and epilepsy that are occasionally used for relieving chronic pruritus is explored. The findings from original sources published to date to evaluate the use of gabapentin and pregabalin as antipruritic agents are explored. They are found to be promising alternative treatments for the relief of several forms of chronic pruritus, particularly uremic pruritus and neuropathic or neurogenic itch, in patients who fail conservative therapies. PMID:27206757
Sultana, Nighat; Ata, Athar
Oleanolic acid has been isolated from chloroform extract of Olea ferruginea Royle after removal of organic bases and free acids. The literature survey revealed it to be biologically very important. In this review the biological significance of oleanolic acid and its derivatives has been discussed. The aim of this review is to update current knowledge on oleanolic acid and its natural and semisynthetic analogs, focussing on its cytotoxic, antitumer, antioxidant, anti-inflamatory, anti-HIV, acetyl cholinesterase, alpha-glucosidase, antimicrobial, hepatoprotective, anti-inflammatory, antipruritic, spasmolytic activity, anti-angiogenic, antiallergic, antiviral and immunomodulatory activities. We present in this review, for the first time, a compilation of the most relevant scientific papers and technical reports of the chemical, pre-clinical and clinical research on the properties of oleanolic acid and its derivatives. PMID:18618318
Roelofzen, J.H.J.; Aben, K.K.H.; Van Der Valk, P.G.M.; Van Houtum, J.L.M.; Van De Kerkhof, P.C.M.; Kiemeney, L.A.L.M. [Radboud University Nijmegen Medical Center, Nijmegen (Netherlands). Dept. of Dermatology
Coal tar is one of the oldest treatments for psoriasis and eczema. It has anti-inflammatory, antibacterial, antipruritic and antimitotic effects. The short-term side effects are folliculitis, irritation and contact allergy. Coal tar contains carcinogens. The carcinogenicity of coal tar has been shown in animal studies and studies in occupational settings. There is no clear evidence of an increased risk of skin tumors or internal tumors. Until now, most studies have been fairly small and they did not investigate the risk of coal tar alone, but the risk of coal tar combined with other therapies. New, well-designed, epidemiological studies are necessary to assess the risk of skin tumors and other malignancies after dermatological use of coal tar.
Ward, L; Wright, E; McMahon, S B
We have studied experimentally induced itch (using histamine iontophoresis) and pain (using topical mustard oil) in healthy human volunteers, measured using visual analogue scale (VAS) ratings. The effects of the following counterstimuli were evaluated: innocuous vibration; innocuous transcutaneous electrical nerve stimulation (TENS); innocuous warming of skin; noxious heating of skin; noxious chemical skin stimulation (using mustard oil); mildly noxious constant current transdermal electrical stimulation. Innocuous stimuli applied 2 min after histamine or mustard oil challenge produced a modest reduction of itch and pain ratings (20-30%), which did not persist for more than 20 sec when the counterstimuli were removed. These changes may well be due to distraction. The same stimuli (in some cases applied for periods of up to 1 h) given prior to the histamine or mustard oil, produced no significant reduction in evoked itch or pain. Noxious stimuli of all types applied 2 min after histamine or mustard oil challenge produced a consistent and significant inhibition of itch (22.8-52.7%) which outlasted the period of counterstimulation application. In contrast, these stimuli had no significant effects on chemically induced pain. The anti-pruritic state produced by brief noxious stimuli were effective for periods of more than 30 min. The differential effects of noxious counterstimuli on itch and pain do not support the suggestion that itch is a subliminal form of pain. Noxious counterstimuli are likely to act via a central rather than peripheral mechanism. The novel finding that a persistent anti-pruritic state can be induced by transdermal constant current may be useful in conditions of clinical itch. PMID:8867255
止痒洗剂联合妇炎消生物敷料栓治疗妊娠合并外阴阴道假丝酵母菌病的临床观察%Clinical observation on the effect of anti -itching lotion combined with Fuyanxiao biological dressing supposi-tory in treatment of pregnancy and vulvovaginal candidiasis
目的：观察止痒洗剂联合妇炎消生物敷料栓治疗妊娠合并外阴阴道假丝酵母菌病（VVC）的临床疗效及复发率。方法选择妊娠合并 VVC 患者236例，将患者以随机数字表法分为两组：治疗组、对照组，各118例。治疗组采用止痒洗剂联合妇炎消生物敷料栓治疗，对照组单独采用妇炎消生物敷料栓治疗，疗程结束后比较两组的临床疗效及复发率。结果治疗组治愈率90．68％，高于对照组的57．62（χ2＝10．731，P ＜0．01）；治疗组复发率3．39％，低于对照组的13．56％，差异有统计学意义（χ2＝10．733，P ＜0．05）。结论止痒洗剂联合妇炎消生物敷料栓治疗妊娠合并 VVC 可有效改善患者的临床症状，降低复发率。%Objective To observe the effect of antipruritic lotion combined Fuyanxiao with biological dress-ing suppository in the treatment of vulvovaginal candidiasis in pregnancy(VVC)the clinical curative effect and the recurrence rate.Methods 236 patients with pregnancy complicated with VVC,would be in community were randomly divided into the two groups:combination treatment group,single drug group,118 cases in each.Combination therapy using antipruritic lotion combined Fuyanxiao biological dressing suppository combined treatment,the control group was treated by Fuyanxiao biological dressing suppository treatment,two groups of clinical efficacy and recurrence rate after the end of treatment were compared.Results The cure rate in the combined treatment group was 90.68%,which was higher than 57.62 % in the control group(χ2 =10.731,P <0.01);The recurrence rate in the combined treatment group was 3.39%,which was lower than 13.56% in the control group(χ2 =10.733,P <0.05).Conclusion The antipruritic lotion combined Fuyanxiao biological dressing suppository in the treatment of pregnancy with VVC can effectively improve the clinical symptoms of patients,reduce the recurrence rate.
Basith, Shaherin; Cui, Minghua; Hong, Sunhye; Choi, Sun
Capsaicin is the most predominant and naturally occurring alkamide found in Capsicum fruits. Since its discovery in the 19th century, the therapeutic roles of capsaicin have been well characterized. The potential applications of capsaicin range from food flavorings to therapeutics. Indeed, capsaicin and few of its analogues have featured in clinical research covered by more than a thousand patents. Previous records suggest pleiotropic pharmacological activities of capsaicin such as an analgesic, anti-obesity, anti-pruritic, anti-inflammatory, anti-apoptotic, anti-cancer, anti-oxidant, and neuro-protective functions. Moreover, emerging data indicate its clinical significance in treating vascular-related diseases, metabolic syndrome, and gastro-protective effects. The dearth of potent drugs for management of such disorders necessitates the urge for further research into the pharmacological aspects of capsaicin. This review summarizes the historical background, source, structure and analogues of capsaicin, and capsaicin-triggered TRPV1 signaling and desensitization processes. In particular, we will focus on the therapeutic roles of capsaicin and its analogues in both normal and pathophysiological conditions. PMID:27455231
Objective: To investigate the efficacy of lavender in treating recurrent Keloids pretreated with triamcinolone acetonide local blocking.Methods:184 cases of recurrent Keloid were treated in this way for 2 years.Results: The curative rate was 90.2 ％ and total effective rate 95.1％.Conclusion:lavender has good effect for curing Keloid and preventing recurrence.It also has anti-pruritic and pain relieving effects.%目的:观察薰衣草精油防治瘢痕疙瘩局封后复发的疗效.方法:对184例瘢痕疙瘩患者用曲安奈德局部封闭后外涂薰衣草精油.结果:两年后治愈率达90.2%、有效率达95.1%.结论:薰衣草精油对防治瘢痕疙瘩增生与复发有较好的疗效.
Yamaura, Katsunori; Oda, Manabu; Suwa, Eriko; Suzuki, Masahiko; Sato, Hiromi; Ueno, Koichi
Many medicines exist which can cause pruritus (itching) as "serious adverse events." Many severe pruritic conditions respond poorly to histamine H1 receptor antagonists; there is no generally accepted antipruritic treatment. Recently described histamine H4 receptors are expressed in haematopoietic cells and have been linked to the pathology of allergy and asthma. We previously reported their expression in human dermal fibroblasts; in this study we have investigated H4 receptor expression in human epidermal tissue and found it to be greater in keratinocytes in the epidermal upper layer than in the lower layer. We have also investigated the effect of histamine H4 receptor antagonists on histamine H1 receptor antagonist-resistant pruritus using a mouse model. Scratching behavior was induced by histamine (300 nmol) or substance P (100 nmol) injected intradermally into the rostral part of the back of each mouse. Fexofenadine, a histamine H1 receptor antagonist, reduced scratching induced by histamine but not by substance P, whereas JNJ7777120, a histamine H4 receptor antagonist, significantly reduced both histamine- and substance P-induced scratching. These results suggest that H4 receptor antagonists may be useful for treatment of H1 receptor antagonist-resistant pruritus. PMID:19652466
Li, Yi-Min; Jia, Min; Li, Hua-Qiang; Zhang, Nai-Dan; Wen, Xian; Rahman, Khalid; Zhang, Qiao-Yan; Qin, Lu-Ping
Cnidium monnieri (L.) Cuss., an annual plant of the Umbelliferae species is one of the most widely used traditional herbal medicines and its fruits have been used to treat a variety of diseases in China, Vietnam, and Japan. The aim of this review is to provide an up-to-date and comprehensive analysis of the botany, traditional uses, phytochemistry, pharmacology, toxicity and contraindication of Cnidium monnieri (L.) Cuss. and to provide future directions of research on this plant. To date, 350 compounds have been isolated and identified from Cnidium monnieri (L.) Cuss., including the main active constituent, coumarins. In vitro and in vivo studies suggest that osthole and other coumarin compounds possess wide range of pharmacological properties for the treatment of female genitals, male impotence, frigidity, skin-related diseases, and exhibit strong antipruritic, anti-allergic, antidermatophytic, antibacterial, antifungal, anti-osteoporotic effects. Although coumarins have been identified as the main active constituents responsible for the observed pharmacological effects, the molecular mechanisms of their actions are still unknown. Therefore, further studies are still required to reveal the structure-activity relationship of these active constituents. In addition, toxicological and clinical studies are also required to provide further data for pharmaceutical use. PMID:26243582
Full Text Available Background: Royal jelly is widely used as a health tonic, especially in Asia. Royal jelly is commonly used in cosmetics as well as in dietary supplements and beverages. Little is known, however, about the pharmacologic efficacy of topical royal jelly. Therefore, we investigated the antipruritic activity of topical royal jelly on chronic pruritus in experimental allergic contact dermatitis in mice. Materials and Methods: Hairless mice (HOS: HR-1, with chronic allergic contact dermatitis induced by 5 weeks of repeated application of 2,4,6-trinitro-1-chlorobenzene (TNCB to the entire back skin were treated topically with royal jelly (0.01% or 1% for 5 weeks after sensitization with TNCB. The effects of royal jelly on pruritus and inflammation were evaluated by measurement of scratching behavior and skin inflammation score, respectively. Results: Repeated application of TNCB to the back skin of mice elicited frequent scratching behavior immediately and 24h after challenge. Topical royal jelly (0.01% or 1% and betamethasone (0.01% significantly ameliorated this chronic pruritus throughout the experimental period. The level of nerve growth factor mRNA in back skin was increased in the mice with dermatitis and reduced by betamethasone, but not by royal jelly. Conclusion: The inhibitory effect of royal jelly on chronic pruritus may occur through different mechanisms from those of betamethasone. Topical application of royal jelly, as used in cosmetics, might be beneficial for the alleviation of chronic pruritus.
Full Text Available Capsaicin is the most predominant and naturally occurring alkamide found in Capsicum fruits. Since its discovery in the 19th century, the therapeutic roles of capsaicin have been well characterized. The potential applications of capsaicin range from food flavorings to therapeutics. Indeed, capsaicin and few of its analogues have featured in clinical research covered by more than a thousand patents. Previous records suggest pleiotropic pharmacological activities of capsaicin such as an analgesic, anti-obesity, anti-pruritic, anti-inflammatory, anti-apoptotic, anti-cancer, anti-oxidant, and neuro-protective functions. Moreover, emerging data indicate its clinical significance in treating vascular-related diseases, metabolic syndrome, and gastro-protective effects. The dearth of potent drugs for management of such disorders necessitates the urge for further research into the pharmacological aspects of capsaicin. This review summarizes the historical background, source, structure and analogues of capsaicin, and capsaicin-triggered TRPV1 signaling and desensitization processes. In particular, we will focus on the therapeutic roles of capsaicin and its analogues in both normal and pathophysiological conditions.
Thomas, Jackson; Carson, Christine F; Peterson, Greg M; Walton, Shelley F; Hammer, Kate A; Naunton, Mark; Davey, Rachel C; Spelman, Tim; Dettwiller, Pascale; Kyle, Greg; Cooper, Gabrielle M; Baby, Kavya E
Globally, scabies affects more than 130 million people at any time. In the developed world, outbreaks in health institutions and vulnerable communities result in a significant economic burden. A review of the literature demonstrates the emergence of resistance toward classical scabicidal treatments and the lack of effectiveness of currently available scabicides in reducing the inflammatory skin reactions and pyodermal progression that occurs in predisposed patient cohorts. Tea tree oil (TTO) has demonstrated promising acaricidal effects against scabies mites in vitro and has also been successfully used as an adjuvant topical medication for the treatment of crusted scabies, including cases that did not respond to standard treatments. Emerging acaricide resistance threatens the future usefulness of currently used gold standard treatments (oral ivermectin and topical permethrin) for scabies. The imminent development of new chemical entities is doubtful. The cumulative acaricidal, antibacterial, antipruritic, anti-inflammatory, and wound healing effects of TTO may have the potential to successfully reduce the burden of scabies infection and the associated bacterial complications. This review summarizes current knowledge on the use of TTO for the treatment of scabies. On the strength of existing data for TTO, larger scale, randomized controlled clinical trials are warranted. PMID:26787146
Neff, Guy W; O'Brien, Christopher B; Reddy, K Rajender; Bergasa, Nora V; Regev, Arie; Molina, Enrique; Amaro, Rafael; Rodriguez, Miguel J; Chase, VeEtta; Jeffers, Lennox; Schiff, Eugene
Pruritus due to cholestatic liver disease can be particularly difficult to manage and frequently is intractable to a variety of medical therapies. The aim of our study is to evaluate the efficacy of delta-9-tetrahydrocannabinol (delta-9-THC) for intractable cholestatic related pruritus (ICRP) that has failed conventional (and unconventional) remedies. Three patients were evaluated for plasmapheresis because of ICRP. All 3 patients had previously been extensively treated with standard therapies for ICRP including: diphenhydramine, chlorpheniramine, cholestyramine, rifampicin, phenobarbital, doxepin, naltrexone, UV therapy, and topical lotions. Even multiple courses of plasmapheresis were performed without any benefit for the intractable pruritus. All patients reported significant decreases in their quality of life, including lack of sleep, depression, inability to work, and suicidal ideations. All patients were started on 5 mg of delta-9-THC (Marinol) at bedtime. All 3 patients reported a decrease in pruritus, marked improvement in sleep, and eventually were able to return to work. Resolution of depression occurred in two of three. Side effects related to the drug include one patient experiencing a disturbance in coordination. Marinol dosage was decreased to 2.5 mg in this patient with resolution of symptoms. The duration of antipruritic effect is approximately 4-6 hrs in all three patients suggesting the need for more frequent dosing. Delta-9-tetrahydrocannabinol may be an effective alternative in patients with intractable cholestatic pruritus. PMID:12190187
Alexandru D P Papoiu
Full Text Available BACKGROUND: Histamine is the prototypical pruritogen used in experimental itch induction. However, in most chronic pruritic diseases, itch is not predominantly mediated by histamine. Cowhage-induced itch, on the other hand, seems more characteristic of itch occurring in chronic pruritic diseases. OBJECTIVES: We tested the validity of cowhage as an itch-inducing agent by contrasting it with the classical itch inducer, histamine, in healthy subjects and atopic dermatitis (AD patients. We also investigated whether there was a cumulative effect when both agents were combined. METHODS: Fifteen healthy individuals and fifteen AD patients were recruited. Experimental itch induction was performed in eczema-free areas on the volar aspects of the forearm, using different itch inducers: histamine, cowhage and their combination thereof. Itch intensity was assessed continuously for 5.5 minutes after stimulus application using a computer-assisted visual analogue scale (COVAS. RESULTS: In both healthy and AD subjects, the mean and peak intensity of itch were higher after the application of cowhage compared to histamine, and were higher after the combined application of cowhage and histamine, compared to histamine alone (p<0.0001 in all cases. Itch intensity ratings were not significantly different between healthy and AD subjects for the same itch inducer used; however AD subjects exhibited a prolonged itch response in comparison to healthy subjects (p<0.001. CONCLUSIONS: Cowhage induced a more intense itch sensation compared to histamine. Cowhage was the dominant factor in itch perception when both pathways were stimulated in the same time. Cowhage-induced itch is a suitable model for the study of itch in AD and other chronic pruritic diseases, and it can serve as a new model for testing antipruritic drugs in humans.
张岳花; 曾平; 谢维跃; 汤志球; 李帜红; 黄向辉
Objective To develop a low-alcohol floral water with long repellent time and low irritation. Meth-ods Using dimethyl phthalate 1,2- Benzenedicarboxylic acid ( BAAPE) as a mosquito repellent with addition of extracts from mugwort, mint and lavender in order to give the products antipruritic effect. The mixed problem was resolved with introduction of the PEG - 40 hydrogenated castor oil as a solubilizer. Results A low-alcohol floral water mixed with mugwort and the ethanol content below 25% was prepared. Tests showed that the mosquito repellent time of the product was more than 4. 7 hours,and the physical and chemical properties were in line with our company' s enterprise standards. Conclusion The product is suitable for using in home and travel because of its long repellent time and high safety.%目的 开发一种驱蚊时效长、刺激性低的低醇驱蚊露产品.方法 使用驱蚊酯作为蚊虫驱避剂,同时添加艾叶、薄荷、薰衣草天然植物提取物以赋予产品止痒健肤的功效,在配方中引入PEG-40氢化蓖麻油作为增溶剂解决混溶问题.结果 研制出一款乙醇含量在25％以下的复合型艾叶低醇驱蚊露,有效驱蚊时间达4.7h以上,各项理化指标均符合已制定的企业标准.结论 产品具有驱蚊时间长、安全性高的优点,适合各类人群居家及旅行使用.
Kremer, Andreas E; Namer, Barbara; Bolier, Ruth; Fischer, Michael J; Oude Elferink, Ronald P; Beuers, Ulrich
Pruritus is a preeminent symptom in patients with chronic cholestatic liver disorders such as primary biliary cirrhosis and primary sclerosing cholangitis. More than two-thirds of these patients experience itching during the course of their disease. This symptom is also frequently observed in patients with other causes of cholestasis such as cholangiocarcinoma, inherited forms of cholestasis and intrahepatic cholestasis of pregnancy, but may accompany almost any other liver disease. The pathogenesis of pruritus of cholestasis remains largely elusive. Increased concentrations of bile salts, histamine, serotonin, progesterone metabolites and endogenous opioids have been controversially discussed as potential pruritogens. However, for these molecules, neither a correlation with itch intensity nor a causative link could be established. The G protein-coupled receptor for bile salts, TGR5, has been shown to be expressed in dorsal root ganglia and give rise to itch in rodents, albeit upon stimuli with suprapathological concentrations of bile salts. The potent neuronal activator lysophosphatidic acid (LPA) and its forming enzyme, autotaxin (ATX), could be identified in the serum of patients with cholestatic pruritus. ATX activity correlated with itch severity and effectiveness of several anti-pruritic therapeutic interventions in cholestatic patients. Thus, the ATX-LPA-axis may represent a key element in the pathogenesis of this agonizing symptom. Treatment options for pruritus of cholestasis remain limited to a few evidence-based and several experimental medical and interventional therapies. The current guideline-based recommendations include the anion exchange resins colestyramine, the pregnane X receptor-agonist and enzyme inducer rifampicin, the μ-opioid antagonist naltrexone, and the selective serotonin reuptake inhibitors sertraline. Still, a considerable part of patients is unresponsive to these drugs and requires experimental approaches including phototherapy
Full Text Available Stephanie Vanterpool, Randall Coombs, Karamarie FechoDepartment of Anesthesiology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC, USABackground: This study retrospectively compared the continuous epidural infusion of morphine with a single epidural injection of extended-release morphine for postoperative pain control after arthroplasty.Methods: Medical records were reviewed for subjects who had total knee or hip arthroplasty (THA under spinal anesthesia and received either a continuous epidural infusion of morphine (Group EPID; n = 101 or an extended-release epidural morphine (Group EREM; n = 109 for postoperative pain. Data were collected for three postoperative days (POD on: pain scores; supplemental opioids; medications for respiratory depression, nausea, and pruritus, and distance ambulated during physical therapy.Results: Pain scores were similar until subjects were transitioned to another analgesic approach on POD 2; after that time, pain scores increased in Group EPID, although they decreased in Group EREM. Supplemental opioids were used more on POD1 in Group EREM than in Group EPID, although time to first opioid and total daily morphine equivalents were similar. Naloxone and antiemetics, not antipruritics, were used more in Group EREM. Distance ambulated after THA was greater in Group EREM than in Group EPID.Conclusions: These results suggest that EREM is associated with better postoperative ambulation and analgesia during the transition to oral or intravenous analgesics, although a higher incidence of side-effects was evident.Keywords: continuous epidural morphine infusion, extended-release epidural morphine, lower extremity arthroplasty, ambulation, postoperative pain, side-effects
Parikh, Nisha R; Mandal, Animesh; Bhatia, Deepak; Siveen, Kodappully Sivaraman; Sethi, Gautam; Bishayee, Anupam
Breast cancer is one of the most frequently diagnosed cancers and major cause of death in women in the world. Emerging evidence underscores the value of dietary and non-dietary phytochemicals, including triterpenoids, in the prevention and treatment of breast cancer. Oleanolic acid, an oleanane-type pentacyclic triterpenoid, is present in a large number of dietary and medicinal plants. Oleanolic acid and its derivatives exhibit several promising pharmacological activities, including antioxidant, anti-inflammatory, hepatoprotective, cardioprotective, antipruritic, spasmolytic, antiallergic, antimicrobial and antiviral effects. Numerous studies indicate that oleanolic acid and other oleanane triterpenoids modulate multiple intracellular signaling pathways and exert chemopreventive and antitumor activities in various in vitro and in vivo model systems. A series of novel synthetic oleanane triterpenoids have been prepared by chemical modifications of oleanolic acid and some of these compounds are considered to be the most potent anti-inflammatory and anticarcinogenic triterpenoids. Accumulating studies provide extensive evidence that synthetic oleanane derivatives inhibit proliferation and induce apoptosis of various cancer cells in vitro and demonstrate cancer preventive or antitumor efficacy in animal models of blood, breast, colon, connective tissue, liver, lung, pancreas, prostate and skin cancer. This review critically examines the potential role of oleanolic acid, oleanane triterpenoids and related synthetic compounds in the chemoprevention and treatment of mammary neoplasia. Both in vitro and in vivo studies on these agents and related molecular mechanisms are presented. Several challenges and future directions of research to translate already available impressive preclinical knowledge to clinical practice of breast cancer prevention and therapy are also presented. PMID:25395898
Kamatou, Guy P P; Vermaak, Ilze; Viljoen, Alvaro M; Lawrence, Brian M
Menthol is a cyclic monoterpene alcohol which possesses well-known cooling characteristics and a residual minty smell of the oil remnants from which it was obtained. Because of these attributes it is one of the most important flavouring additives besides vanilla and citrus. Due to this reason it is used in a variety of consumer products ranging from confections such as chocolate and chewing gum to oral-care products such as toothpaste as well as in over-the-counter medicinal products for its cooling and biological effects. Its cooling effects are not exclusive to medicinal use. Approximately one quarter of the cigarettes on the market contain menthol and small amounts of menthol are even included in non-mentholated cigarettes. Natural menthol is isolated exclusively from Mentha canadensis, but can also be synthesised on industrial scale through various processes. Although menthol exists in eight stereoisomeric forms, (-)-menthol from the natural source and synthesised menthol with the same structure is the most preferred isomer. The demand for menthol is high and it was previously estimated that the worldwide use of menthol was 30-32,000 metric tonnes per annum. Menthol is not a predominant compound of the essential oils as it can only be found as a constituent of a limited number of aromatic plants. These plants are known to exhibit biological activity in vitro and in vivo such as antibacterial, antifungal, antipruritic, anticancer and analgesic effects, and are also an effective fumigant. In addition, menthol is one of the most effective terpenes used to enhance the dermal penetration of pharmaceuticals. This review summarises the chemical and biological properties of menthol and highlights its cooling effects and toxicity. PMID:24054028
Ogata, Ikuko; Kawanai, Takuya; Hashimoto, Erika; Nishimura, Yumiko; Oyama, Yasuo; Seo, Hakaru
German chamomile (Matricaria recutita L.), one of the popular ingredients in herbal teas, has been traditionally used for medicinal purposes. Bisabololoxide A (BSBO) is one of the main constituents in this herb. BSBO is supposed to be principle in some bioactivities of German chamomile such as anti-inflammatory, gastrointestinal, and antipruritic actions. Although the use of German chamomile has spread, the information related to toxicity of BSBO is very limited. In present study, the cytotoxic effect of micromolar BSBO was cytometrically examined on rat thymocytes by using appropriate fluorescent dyes. When the cells were incubated with BSBO for 24 h, BSBO at concentrations of 30 microM or more significantly increased populations of dead cells, shrunken cells, and cells with phosphatidylserine exposed on membrane surface. Both cell shrinkage and externalization of membrane phosphatidylserine are general features in an early stage of apoptosis. In addition, BSBO significantly increased population of cells containing hypodiploid DNA, and the increase was completely attenuated by Z-VAD-FMK, a pan-inhibitor for caspases, indicating an involvement of caspase activation. Thus, it is likely that the type of cell death induced by BSBO is apoptosis. The significant changes in cellular parameters of rat thymocytes by BSBO were not observed when the concentration was 10 microM or less. Furthermore, the short incubation (3 h) of cells even with 30-100 microM BSBO did not significantly affect the cells. Therefore, it may be suggested that BSBO is practically safe when German chamomile is conventionally used. PMID:19834689
Full Text Available Salsola is one of the largest and most important genera in the family Chenopodiaceae. Salsola species are used for their anti-inflammatory, antinociceptive, anthelmintic and antipruritic effects and also as diuretic in traditional medicines worldwide. The aim of the present study is to assess the activity potential of the extracts, subextracts and isolated compounds from the aerial parts of and Salsola grandis, an endemic species in Turkey in a scientific platform. The effects of the extracts, subextracts and isolated compounds were investigated using in vivo experimental models of inflammation and pain in mice, and also total phenolic content of the plant was determined. For the evaluation of the anti-inflammatory activity, carrageenan-induced paw edema and for the assessment of antinociceptive activity, p-benzoquinone-induced nociception tests in mice were employed. The crude ethanol extract of the plant was sequentially fractionated into five subextracts, namely n-hexane, CHCl 3, EtOAc, n-BuOH and remaining water subextracts. Further studies were carried out on the bioactive n -BuOH subextract. Through bioassay-guided fractionation and isolation procedures from active fraction , ten flavonoids, i sorhamnetin-3-O-rutinoside(1, quercetin-3-O-rutinoside (2,quercetin-3-O-metylether (3,tiliroside (4, isorhamnetin-3-glucuronide (5, isorhamnetin-3-O-glucoside (6,quercetin-3-O-galactoside (7, quercetin-3-O-rhamnoside (8,quercetin (9 and manghaslin (10, and two oleanane-type saponins, momordin II b (11 andmomordin II c (12, and one amino acid derivative compound, N-acetyltryptophan (13 were isolated, and their structures were established on the basis of spectroscopic techniques. The anti-inflammatory and antinociceptive activities of 1 , 4, 6, 7 and 12 were investigated firstly in this study, and 4 and 7 were found to have the most potent inhibitory activity in used models. The present study demonstrates the anti-inflammatory and antinociceptive
Thurmond, Robin L
The histamine H4 receptor (H4R) was first noted as a sequence in genomic databases that had features of a class A G-protein coupled receptor. This putative receptor was found to bind histamine consistent with its homology to other histamine receptors and thus became the fourth member of the histamine receptor family. Due to the previous success of drugs that target the H1 and H2 receptors, an effort was made to understand the function of this new receptor and determine if it represented a viable drug target. Taking advantage of the vast literature on the function of histamine, a search for histamine activity that did not appear to be mediated by the other three histamine receptors was undertaken. From this asthma and pruritus emerged as areas of particular interest. Histamine has long been suspected to play a role in the pathogenesis of asthma, but antihistamines that target the H1 and H2 receptors have not been shown to be effective for this condition. The use of selective ligands in animal models of asthma has now potentially filled this gap by showing a role for the H4R in mediating lung function and inflammation. A similar story exists for chronic pruritus associated with conditions such as atopic dermatitis. Antihistamines that target the H1 receptor are effective in reducing acute pruritus, but are ineffective in pruritus experienced by patients with atopic dermatitis. As for asthma, animal models have now suggested a role for the H4R in mediating pruritic responses, with antagonists of the H4R reducing pruritus in a number of different conditions. The anti-pruritic effect of H4R antagonists has recently been shown in human clinical studies, validating the preclinical findings in the animal models. A selective H4R antagonist inhibited histamine-induced pruritus in health volunteers and reduced pruritus in patients with atopic dermatitis. The history to date of the H4R provides an excellent example of the deorphanization of a novel receptor and the translation
Rachel A Gibson
Full Text Available BACKGROUND: Transient receptor potential vanilloid type 1 (TRPV1 is a non-selective cation channel widely expressed in skin tissues, and peripheral sensory nerve fibres. Activation of TRPV1 releases neuropeptides; the resulting neurogenic inflammation is believed to contribute to the development of pruritus. A TRPV1 antagonist has the potential to perform as an anti-pruritic agent. SB705498 is a TRPV1 antagonist that has demonstrated in vitro activity against cloned TRPV1 human receptors and when orally administered has demonstrated pharmacodynamic activity in animal models and clinical studies. OBJECTIVES: To select a topical dose of SB705498 using the TRPV1 agonist capsaicin; to confirm engagement of the TRPV1 antagonistic action of SB705498 and assess whether the dose selected has an effect on itch induced by two challenge agents. METHODS: A clinical study was conducted in 16 healthy volunteers to assess the effects of 3 doses of SB705498 on skin flare induced by capsaicin. Subjects with a robust capsaicin response were chosen to determine if the selected topical formulation of SB705498 had an effect on challenge agent induced itch. RESULTS: Following capsaicin challenge the greatest average reduction in area of flare was seen for the 3% formulation. This dose was selected for further investigation. Itch intensity induced by two challenge agents (cowhage and histamine was assessed on the Computerised Visual Analogue Scale. The difference in average itch intensity (Weighted Mean Over 15 Mins between the 3% dose of SB705498 and placebo for the cowhage challenge was -0.64, whilst the histamine challenge showed on average a -4.65 point change. CONCLUSIONS: The 3% topical formulation of SB705498 cream was clinically well tolerated and had target specific pharmacodynamic activity. However there were no clinically significant differences on pruritus induced by either challenge agent in comparison to placebo. SB705498 is unlikely to be of symptomatic
翁德会; 毛淑芳; 程弘夏; 许腊英
目的：厚朴酚性成分具有杀菌、消炎、燥湿、止痒等作用，通过制备乳膏对其提取物进行开发利用。方法根据厚朴酚、和厚朴酚的特点及乳膏基质的特点，筛选处方组成，并对制备工艺进行研究，通过对乳膏的外观性状、透皮、稠度和稳定性等指标进行考察，筛选最佳的处方组成，并制备厚朴乳膏。结果由该比例的组成制备的厚朴乳膏，重现性好，乳膏色泽较纯正，均匀细腻，稠度适宜，易涂布，稳定性好、透皮吸收等均较好，可以作为最佳配比来制备厚朴乳膏。结论厚朴乳膏可以作为一种新制剂进行开发利用。%Abstracts:Objective Puepose honokiol components has bactericidal, anti -inflammatory, eliminating dampness, antipruritic effect, through the preparation of cream on the extract was developed using.Methods on the basis of characteristics and cream base of magnolol and honokiol, the prescription composition, screening, and the preparation technology was studied, through the inspection of appearance, the drug transdermal, consistency and stability index, screening the best prescription composition, and preparation of Magnolia officinalis cream. Results Magnolia cream consists of the proportion of preparation, good reproducibility, cream Kizawa Jung, even delicate, consistency is appropriate, easy coating, good stability, absorption through the skin is good, can be regarded as the best proportion to prepare the Magnolia cream.Conclusions It can be used as a new preparation for the development and utilization.
Robin L. Thurmond
Full Text Available The histamine H4 receptor (H4R was first noted as a sequence in genomic databases that had features of a G-protein coupled receptor. This putative receptor was found to bind histamine consistent with its homology to other histamine receptors and thus became the fourth member of the histamine receptor family. Due to the previous success of drugs that target the H1 and H2 receptors, an effort was made to understand the function of this receptor and determine if it represented a drug target. Taking advantage of the vast literature on histamine, a search for histamine activity that did not appear to be mediated by the other three histamine receptors was undertaken. From this asthma and pruritus emerged as areas of particular interest. Histamine has long been suspected to play a role in the pathogenesis of asthma, but antihistamines that target the H1 and H2 receptors have not been shown to be effective for this condition. The use of selective ligands in animal models of asthma has now potentially filled this gap by showing a role for the H4R in mediating lung function and inflammation. A similar story exists for chronic pruritus associated with conditions such as atopic dermatitis. Antihistamines that target the H1 receptor are effective in reducing acute pruritus, but are ineffective in pruritus experienced by patients with atopic dermatitis. As for asthma, animal models have now suggested a role for the H4R in mediating pruritic responses, with antagonists to the H4R reducing pruritus in a number of different conditions. The anti-pruritic effect of H4R antagonists has recently been shown in human clinical studies, validating the preclinical findings in the animal models. A selective H4R antagonist inhibited histamine-induced pruritus in health volunteers and reduced pruritus in patients with atopic dermatitis. The history to date of the H4R provides an excellent example of the deorphanization of a novel receptor and the translation of this into
H R Jerajani
Full Text Available Background : Sertaconazole is a new, broad spectrum, fungicidal and fungistatic imidazole with added antipruritic and anti-inflammatory activity that would provide greater symptomatic relief and hence would be beneficial in improving the quality of life for the patient with dermatophytoses. Aims and Objectives : To compare efficacy and safety of sertaconazole, terbinafine and luliconazole in patients with dermatophytoses. Materials and Methods : 83 patients with tinea corporis and tinea cruris infections were enrolled in this multicentre, randomized, open label parallel study. The initial ′Treatment Phase′ involved three groups receiving either sertaconazole 2% cream applied topically twice daily for four weeks, terbinafine 1% cream once daily for two weeks, luliconazole 1% cream once daily for two weeks. At the end of treatment phase, there was a ′Follow-up Phase′ at end of 2 weeks, where the patients were assessed clinically and mycologically for relapse. Results : Of the 83 patients, 62 completed the study, sertaconazole (n = 20, terbinafine (n = 22 and luliconazole (n = 20. The primary efficacy variables including change in pruritus, erythema, vesicle, desquamation and mycological cure were significantly improved in all the three groups, as compared to baseline, in the Treatment and Follow-up phase. Greater proportion of patients in sertaconazole group (85% showed resolution of pruritus as compared to terbinafine (54.6%; and luliconazole (70%, (P < 0.05 sertaconazole vs terbinafine. There was a greater reduction in mean total composite score (pruritus, erythema, vesicle and desquamation in sertaconazole group (97.1% as compared to terbinafine (91.2% and luliconazole (92.9%. All groups showed equal negative mycological assessment without any relapses. All three study drugs were well tolerated. Only one patient in sertaconazole group withdrew from the study due to suspected allergic contact dermatitis. Conclusion : Sertaconazole was
Ana Cristina Gomes Barros Salgado
Full Text Available Dermatological inflammatory diseases such as atopic dermatitis, psoriasis and seborrhoeic dermatitis often affect the scalp and the eyebrows. Although there are many dosage forms available, these are particularly critical anatomic regions for application of topical formulations because of the presence of hair. Lotions are therefore the recommended type of drug delivery system for these areas. The presence of hair may limit the application and thus the acceptability of the formulation and its compliance. Because of its low apparent viscosity, lotion application is unpleasant. Gels, given their consistency and adhesiveness, are a suitable alternative to lotions in this situation. The aim of this study was to formulate a stable gel containing mometasone furoate, which is an anti-inflammatory and anti-pruritic corticosteroid, in order to improve topical treatment of scalp dermatitis. In this study, pharmaceutical development, physical-chemical characterization, stability and in vitro permeation studies were performed. In terms of the pH, viscosity, assay and macroscopic and microbiological properties, the gel was stable over the period of study. The in vitro permeation studies allowed the characterization of the mometasone furoate permeation profile for the gel through different membranes. Mometasone furoate presented a slow permeation through the skin. This gel appears safe for topical application.Afecções dermatológicas do tipo inflamatório como a dermatite atópica, psoríase e dermatite seborreica, afetam freqüentemente o couro cabeludo e sobrancelhas. Apesar de existirem várias formas farmacêuticas para o seu tratamento, apenas as loções são indicadas para estas zonas, mas devido à baixa viscosidade, a aplicação de loções torna-se desagradável. Os geles, pela maior consistência e capacidade de adesão, apresentam-se como alternativa nesta situação. Neste trabalho procedeu-se ao desenvolvimento galênico de um gel com furoato
杨素清; 安月鹏; 闫景东
目的 探讨氟芬那酸丁酯软膏治疗日光皮炎的疗效及安全性.方法 日光皮炎患者64例,随机分为观察组和对照组,每组32例.观察组外用氟芬那酸丁酯软膏,对照组外用双氯芬酸钠乳膏,疗程为3周.采用疾病情况评分和瘙痒视觉模拟评分比较氟芬那酸丁酯软膏和双氯芬酸乳膏的疗效.结果 观察组临床痊愈4例,显效19例,有效7例,无效2例,总有效率93.8％;对照组临床痊愈2例,显效11例,有效14例,无效5例,总有效率84.4％.观察组总有效率高于对照组,两者差异有统计学意义(P＜0.05).从瘙痒评分构成比来看,观察组瘙痒评分显著低于对照组,两者差异有统计学意义(P＜0.05).结论 氟芬那酸丁酯治疗日光皮炎疗效优于双氯芬酸,能较好地改善患者瘙痒症状.%Objective To evaluate the efficacy and safety of butyl flufenamate ointment for the treatment of solar dermatitis.Methods Sixty-four patients with solar dermatitis were randomly divided into the observation group (n =32) and control group (n =32) to topically apply butyl flufenamate ointment and diclofenac sodium cream,respectively,for 3 weeks.The efficacy was evaluated by lesion scores and a visual analog scale for pruritus.Results At the end of the treatment,4 patients in the observation group were clinically cured,19 markedly improved,17 improved,and 2 showed no improvement; meanwhile,2 patients in the control group were clinically cured,11 markedly improved,14 improved,and 5 showed no improvement.The total response rate was significantly higher (93.8％ vs.84.4％,P ＜ 0.05),while the pruritus score was significantly lower (P ＜ 0.05) in the observation group than in the control group.Conclusion Butyl flufenamate ointment is superior to dicofenac sodium cream in terms of both efficacy and anti-pruritic effect.
Fisara, Petr; Sargent, Roger M; Shipstone, Michael; von Berky, Andrew; von Berky, Janet
Background Canine flea-allergy dermatitis (FAD), a hypersensitivity response to antigenic material in the saliva of feeding fleas, occurs worldwide and remains a common presentation in companion animal veterinary practice despite widespread availability of effective systemic and topical flea-control products. Hypothesis/Objectives To evaluate the clinical response in dogs with FAD treated topically with indoxacarb, a novel oxadiazine insecticide. Animals Twenty-five client-owned dogs in Queensland, Australia diagnosed with pre-existing FAD on the basis of clinical signs, flea-antigen intradermal and serological tests. Methods An open-label, noncontrolled study, in which all dogs were treated with topical indoxacarb at 4 week intervals, three times over 12 weeks. Results Twenty-four dogs completed the study. Complete resolution of clinical signs of FAD was observed in 21 cases (87.5%), with nearly complete resolution or marked improvement in the remaining three cases. Mean clinical scores (Canine Atopic Dermatitis Extent and Severity Index-03) were reduced by 93.3% at week 12. Mean owner-assessed pruritus scores were reduced by 88% by week 12. Mean flea counts reduced by 98.7 and 100% in weeks 8 and 12, respectively. Conclusions and clinical importance Topical indoxacarb treatment applied every 4 weeks for 12 weeks, without concomitant antipruritic or ectoparasiticide therapy, completely alleviated flea infestations in all dogs and associated clinical signs of FAD in a high proportion of this population of dogs in a challenging flea-infestation environment. Résumé Contexte La dermatite par allergie aux piqures de puces (FAD), une hypersensibilité aux antigènes salivaires des puces, est décrite dans le monde entier et reste une présentation fréquente en médicine vétérinaire des animaux de compagnie malgré une large gamme d'antiparasitaires topiques et systémiques efficaces disponibles. Hypothèses/Objectifs Estimer la réponse clinique des chiens