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Sample records for promazine

  1. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride with promazine... RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222b Ketamine.... Ketamine hydrochloride, (±),-2-(o-chlorophenyl)-2-(methylamino) cyclohexanone hydrochloride, with promazine...

  2. In vitro cross-linking of bovine lens proteins photosensitized by promazines

    Merville, M.P.; Decuyper, J.; Piette, J.; Calberg-Bacq, C.M.; Van de Vorst, A.

    1984-01-01

    Promazine derivatives induce cross-linking of bovine lens crystallins in vitro by irradiation with near-ultraviolet (UV) light in the presence of O 2 , as revealed by electrophoresis after denaturation. With the five derivatives tested (promazine [PZ], chlorpromazine [CPZ], triflupromazine [TFPZ], methoxypromazine [MTPZ], and acepromazine [ACPZ]), single-hit kinetics are observed. Evidence implicating the cation radicals of the PZ derivatives as the causative agent of this in vitro effect is presented. Hydroxyl radicals do not appear to be involved in the photo-cross-linking reaction. Sodium ascorbate protects against damage induced either by PZ derivatives plus light or by PZ cation radicals in the dark. These findings are discussed with respect to development of cataracts induced by these drugs in vivo

  3. Photophysical and computational investigation of the intermolecular interactions of pyrene with phenothiazine and promazine

    Güloğlu, Pınar; Acar, Nursel, E-mail: nursel.acar@ege.edu.tr

    2016-10-20

    Highlights: • Intermolecular interactions of pyrene with phenothiazine/promazine were investigated. • All investigated systems were optimized at ωB97XD/6-31G(d,p) level in gas phase. • The electronic transitions were determined using frontier orbitals. • Both Py–Pheno and Py–Prom are potential candidates for charge transfer systems. - Abstract: The intermolecular interactions between the pyrene (Py) (as acceptor) and phenothiazine (Pheno), promazine (Prom) (as donors) were investigated using UV/Vis absorption and fluorescence spectroscopy. Fluorescence quenching rate constants for Py–Pheno and Py–Prom systems have been calculated approximately 10{sup 10} M{sup −1} s{sup −1}, indicating diffusion controlled processes. A computational investigation has also been carried out in gas phase at ωB97XD/6-31G(d,p) level. Time-dependent density functional theory (TDDFT) was used to calculate the electronic transitions of molecules at B3LYP/6-311++G(d,p) level. Total electronic energies, complexation energies, free energy differences, excitation wavelengths, and HOMO–LUMO energy gaps are discussed in gas phase. Analyses of first excited singlet states have indicated charge transfers transitions between Py and Pheno, Prom through π–π stacking in gas phase at 433 nm and 466 nm, respectively. Due to its charge transfer character, Py–Pheno and Py–Prom systems seem to be appropriate models to investigate and design photosensitive materials.

  4. Aggregation and phase separation behavior of an amphiphilic drug promazine hydrochloride under the influence of inorganic salts and ureas

    Rub, Malik Abdul, E-mail: malikrub@gmail.com [Center of Excellence for Advanced Materials Research, King Abdulaziz University, Jeddah 21589 (Saudi Arabia); Chemistry Department, King Abdulaziz University, Jeddah 21589 (Saudi Arabia); Asiri, Abdullah M.; Azum, Naved; Khan, Anish; Khan, Aftab Aslam Parwaz; Khan, Sher Bahadar; Rahman, Mohammed M. [Center of Excellence for Advanced Materials Research, King Abdulaziz University, Jeddah 21589 (Saudi Arabia); Chemistry Department, King Abdulaziz University, Jeddah 21589 (Saudi Arabia); Kabir-ud-Din [Department of Chemistry, Aligarh Muslim University, Aligarh 202002 (India)

    2013-12-20

    Highlights: • Aggregation and clouding behavior of PMZ-additive (salts/ureas) mixtures have been investigated. • Both urea and thiourea, at low concentrations, decrease the cmc but, at high concentrations, increase it. • However, ΔH{sub m}° for pure drug/drug–additive systems is negative at low temperature and positive at higher temperature. • The ΔS{sub m}° values are positive, their magnitude being more at T = 303.15 K and above. - Abstract: Self-association and phase separation phenomena of an amphiphilic phenothiazine drug promazine hydrochloride (PMZ) in the absence and presence of inorganic salts (NaF, NaCl and NaBr) and ureas (urea and thiourea) have been investigated in the present study. By the increase in temperature the critical micelle concentration (cmc) of drug PMZ first increases then decreases. Maximum cmc values were obtained at 303.15 K in presence or absence of additives (salts/ureas). Decrease in cmc occurs by the addition of the inorganic salts which is explained on the basis of nature and ion size. Ureas (urea and thiourea) decreased the cmc at low concentration; however, at higher concentrations, increase in cmc was observed with both the additives. Increasing inorganic salt concentrations caused an increase in the cloud point (CP) of PMZ, whereas urea decreased the CP. Significant thermodynamic parameters were also evaluated and discussed.

  5. Aggregation and phase separation behavior of an amphiphilic drug promazine hydrochloride under the influence of inorganic salts and ureas

    Rub, Malik Abdul; Asiri, Abdullah M.; Azum, Naved; Khan, Anish; Khan, Aftab Aslam Parwaz; Khan, Sher Bahadar; Rahman, Mohammed M.; Kabir-ud-Din

    2013-01-01

    Highlights: • Aggregation and clouding behavior of PMZ-additive (salts/ureas) mixtures have been investigated. • Both urea and thiourea, at low concentrations, decrease the cmc but, at high concentrations, increase it. • However, ΔH m ° for pure drug/drug–additive systems is negative at low temperature and positive at higher temperature. • The ΔS m ° values are positive, their magnitude being more at T = 303.15 K and above. - Abstract: Self-association and phase separation phenomena of an amphiphilic phenothiazine drug promazine hydrochloride (PMZ) in the absence and presence of inorganic salts (NaF, NaCl and NaBr) and ureas (urea and thiourea) have been investigated in the present study. By the increase in temperature the critical micelle concentration (cmc) of drug PMZ first increases then decreases. Maximum cmc values were obtained at 303.15 K in presence or absence of additives (salts/ureas). Decrease in cmc occurs by the addition of the inorganic salts which is explained on the basis of nature and ion size. Ureas (urea and thiourea) decreased the cmc at low concentration; however, at higher concentrations, increase in cmc was observed with both the additives. Increasing inorganic salt concentrations caused an increase in the cloud point (CP) of PMZ, whereas urea decreased the CP. Significant thermodynamic parameters were also evaluated and discussed

  6. 21 CFR 522.1962 - Promazine hydrochloride.

    2010-04-01

    ... for tetanus. (B) For use as a tranquilizer and preanesthetic. (iii) Limitations. Not for use in horses... (c)(1)(iii) of this section. (c) Conditions of use—(1) Horses—(i) Amount—(A) 0.2 to 0.5 milligrams... conjunction with local anesthesia, as adjunctive therapy for tetanus, and as an antiemetic prior to worming...

  7. Electrochemical, Chemical and Enzymatic Oxidations of Phenothiazines

    Blankert, B.; Hayen, H.; van Leeuwen, S.M.; Karst, U.; Bodoki, E.; Lotrean, S.; Sandulescu, R.; Mora Diaz, N.; Dominguez, O.; Arcos, J.; Kauffmann, J.-M.

    2005-01-01

    The oxidation of several phenothiazine drugs (phenothiazine, promethazine hydrochloride, promazine hydrochloride, trimeprazine hydrochloride and ethopropazine hydrochloride) has been carried out in aqueous acidic media by electrochemical, chemical and enzymatic methods. The chemical oxidation was

  8. Interaction of solutions containing phenothiazines exposed to laser radiation with materials surfaces, in view of biomedical applications

    Simon, A.; Alexandru, T.; Boni, M.; Damian, V.; Stoicu, A.; Dutschk, Victoria; Pascu, M.L.

    2014-01-01

    Phenothiazine drugs - chlorpromazine (CPZ), promazine (PZ) and promethazine (PMZ) - were exposed to 266 nm (fourth harmonic of the Nd:YAG pulsed laser radiation) in order to be modified at molecular level and to produce an enhancement of their antibacterial activity. The irradiated samples were

  9. Comparison of TiO2 photocatalysis, electrochemically assisted Fenton reaction and direct electrochemistry for simulation of phase I metabolism reactions of drugs

    Ruokolainen, Miina; Gül, Turan; Permentier, Hjalmar; Sikanen, Tiina; Kostiainen, Risto; Kotiaho, Tapio

    2016-01-01

    The feasibility of titanium dioxide (TiO2) photocatalysis, electrochemically assisted Fenton reaction (EC-Fenton) and direct electrochemical oxidation (EC) for simulation of phase I metabolism of drugs was studied by comparing the reaction products of buspirone, promazine, testosterone and

  10. Medication-related risks of CT-procedures in neonates and young infants

    Abel, M.

    1985-01-01

    In very young pediatric patients CT-investigations require sedative-hypnotic drug treatment to ensure complete immobilisation during scanning. The case report of a neonate with respiratory arrest after a repeated CT-premedication underlines the high risk of these procedures, especially in patients with central nervous system disorders. We compared organisational requirements, risks and complication rates of 146 oral and intramuscular promazine medications for CT-scanning of the head in 146 infants and neonates (93,8% adequate sedation response) to those of reported alternative methods. Oral promazine proved to be a very effective and safe medication (average dosage in 57 patients without complications: 5,2 mg/kg body weight/90 minutes before CT-scanning; 96% successful sedation procedures) in comparison to 89 patients with i.m. promazine (average dosage: 2,3 mg/kg body weight/45 min before CT with 92% adequate sedations but a complication rate of 7,9%). For neuropediatric examinations of outpatients fast recovery and EEG-compatibility are further important advantages of oral promazine CT-medication. (orig.) [de

  11. Skin Bioengineering: Noninvasive Transdermal Monitoring

    2005-01-01

    chloroquine , promazine, tetracaine and metoclopramide) were administered iontophoretically (figure 6). Then, the anodal extraction of PGE2 from the site of... analogue of human colour this apparent thermo-optical response of the perception. Unlike the classical NIR approach skin can also provide an

  12. Photoreactivity of chlorpromazine with native DNA in an aqueous solution

    Fujita, Hitoshi; Yanagisawa, Fukuko; Endo, Akira; Suzuki, Kenshi

    1980-01-01

    Near-UV irradiation of a mixture of chlorpromazine and native DNA caused irreversible binding of the drug or its photoproduct(s) to DNA and double strand break of DNA. When the irradiation was performed in a reaction mixture with a low salt concentration, much more photobinding occurred. Accompanying these effects, the maximum hyperchromicity of DNA at a high temperature was decreased. This can be explained by either a partial denaturation or an inhibition of melting by a formation of complex between double helical DNA and a promazine polymer. (author)

  13. Interaction of amphiphilic drugs with human and bovine serum albumins.

    Khan, Abbul Bashar; Khan, Javed Masood; Ali, Mohd Sajid; Khan, Rizwan Hasan; Kabir-Ud-Din

    2012-11-01

    To know the interaction of amphiphilic drugs nortriptyline hydrochloride (NOT) and promazine hydrochloride (PMZ) with serum albumins (i.e., human serum albumin (HSA) and bovine serum albumin (BSA)), techniques of UV-visible, fluorescence, and circular dichroism (CD) spectroscopies are used. The binding affinity is more in case of PMZ with both the serum albumins. The quenching rate constant (k(q)) values suggest a static quenching process for all the drug-serum albumin interactions. The UV-visible results show that the change in protein conformation of PMZ-serum albumin interactions are more prominent as compared to NOT-serum albumin interactions. The CD results also explain the conformational changes in the serum albumins on binding with the drugs. The increment in %α-helical structure is slightly more for drug-BSA complexes as compared to drug-HSA complexes. Copyright © 2012 Elsevier B.V. All rights reserved.

  14. Research related to boron neutron capture therapy at The Ohio State University

    Barth, R.F.; Soloway, A.H.; Alam, F.

    1986-01-01

    Research in the area of boron neutron capture therapy (BNCT) at The Ohio State University is a highly multidisciplinary effort involving approximately twenty investigators in nine different departments. Major areas of interest include: (1) Boronation of monoclonal antibodies directed against tumor-associated antigens for the delivery of 10 B; (2) Synthesis of 10 B-containing derivatives of promazines and porphyrins that possess tumor-localizing properties; (3) Development of a rat model for the treatment of glioblastoma by BNCT; (4) Quantitation and microdistribution of 10 B in tissues by means of a solid state nuclear track detector. The ultimate goal of this research is to carry out the extensive preclinical studies that are required to bring BNCT to the point of a clinical trial. 13 references

  15. Sol-gel-immobilized Tris(2,2'-bipyridyl)ruthenium(II) electrogenerated chemiluminescence sensor for high-performance liquid chromatography

    Choi, Han Nim; Cho, Sung-Hee; Park, Yu-Jin; Lee, Dai Woon; Lee, Won-Yong

    2005-01-01

    The sol-gel-immobilized Tris(2,2'-bipyridyl)ruthenium(II) [Ru(bpy) 3 2+ ] electrogenerated chemiluminescence (ECL) sensor was applied to the reversed-phase high-performance liquid chromatography (HPLC) determination of phenothiazine derivatives (promazine, chlorpromazine, triflupromazine, thioridazine, and trifluoperazine) and erythromycin in human urine samples. In this method, Ru(bpy) 3 2+ was immobilized in sol-gel-derived titania (TiO 2 )-Nafion nanocomposite films coated on a dual platinum electrode. This method eliminates an extra pump needed for the delivery of Ru(bpy) 3 2+ reagent into a reaction/observation zone in front of photomultiplier tube because the immobilized-Ru(bpy) 3 2+ is recycled on the electrode surface by an applied potential at +1.3 V versus Ag/AgCl (3 M NaCl) reference electrode. The resulting analytical performances such as detection limit, working range, sensitivity, and measurement precision were slightly worse than those obtained with the conventional post-column Ru(bpy) 3 2+ addition approach. The lack of significant interferences and the low detection limits for phenothiazine derivatives and erythromycin indicate that the proposed HPLC-Ru(bpy) 3 2+ ECL detection method is suitable for the determination of those compounds in biological fluids

  16. Self-aggregation of bio-surfactants within ionic liquid 1-ethyl-3-methylimidazolium bromide: A comparative study and potential application in antidepressants drug aggregation

    Banjare, Manoj Kumar; Behera, Kamalakanta; Kurrey, Ramsingh; Banjare, Ramesh Kumar; Satnami, Manmohan L.; Pandey, Siddharth; Ghosh, Kallol K.

    2018-06-01

    Aggregation behavior of bio-surfactants (BS) sodium cholate (NaC) and sodium deoxycholate (NaDC) within aqueous solution of ionic liquid (IL) 1-ethyl-3-methylimidazolium bromide [Emim][Br] has been investigated using surface tension, conductivity, steady state fluorescence, FT-IR and dynamic light scattering (DLS) techniques. Various interfacial and thermodynamic parameters are determined in the presence of different wt% of IL [Emim][Br]. Information regarding the local microenvironment and size of the aggregates is obtained from fluorescence and DLS, respectively. FT-IR spectral response is used to reveal the interactions taking place within aqueous NaC/NaDC micellar solutions. It is noteworthy to mention that increasing wt% of [Emim][Br] results in an increase in the spontaneity of micelle formation and the hydrophilic IL shows more affinity for NaC as compared to NaDC. Further, the micellar solutions of BS-[Emim][Br] are utilized for studying the aggregation of antidepressants drug promazine hydrochloride (pH). UV-vis spectroscopic investigation reveals interesting outcomes and the results show changes in spectral absorbance of PH drug on the addition of micellar solution (BS-[Emim][Br]). Highest binding affinity and most promising activity are shown for NaC as compared to NaDC.

  17. [Application of HPLC-UV method for aripiprazole determination in serum].

    Synowiec, Anna; Gomółka, Ewa; Zyss, Tomasz; Zieba, Andrzej; Florek, Ewa; Piekoszewski, Wojciech

    2012-01-01

    Aripiprazole is a new drug applied in schizophrenia treatment. There are not strict indications for aripiprazole therapeutic drug monitoring. Despite, serum aripiprazole measuring would help control the drug doses effectiveness. The drug monitoring can eliminate overdosing, adverse effects and let control proper drug ingestion. The aim of the paper was to develop a simple method for aripiprazole determination in serum for therapeutic drug monitoring. High performance liquid chromatography with spectrophotometric detection (HPLC-UV) was used. Resolution was performed on LC-8 column; moving phase was solution 0,025M trimethylammonium buffer: acetonitrile (62:38). Isocratic flow was 1,2 ml/min; internal standard (IS) was promazine; monitored wavelength was lambda=214 nm. The validation parameters were: limits of linearity (LOL) 100-800 ng/ml, limit of detection (LOD) 10 ng/ml, limit of quantity (LOQ) 100 ng/ml. Coefficient of variation (CV) describing accuracy and precision didn't cross 10%. The method was useful for therapeutic drug monitoring in serum of patients treated with aripiprazole.

  18. Sequential cloud-point extraction for toxicological screening analysis of medicaments in human plasma by high pressure liquid chromatography with diode array detector.

    Madej, Katarzyna; Persona, Karolina; Wandas, Monika; Gomółka, Ewa

    2013-10-18

    A complex extraction system with the use of cloud-point extraction technique (CPE) was developed for sequential isolation of basic and acidic/neutral medicaments from human plasma/serum, screened by HPLC/DAD method. Eight model drugs (paracetamol, promazine, chlorpromazine, amitriptyline, salicyclic acid, opipramol, alprazolam and carbamazepine) were chosen for the study of optimal CPE conditions. The CPE technique consists in partition of an aqueous sample with addition of a surfactant into two phases: micelle-rich phase with the isolated compounds and water phase containing a surfactant below the critical micellar concentration, mainly under influence of temperature change. The proposed extraction system consists of two chief steps: isolation of basic compounds (from pH 12) and then isolation of acidic/neutral compounds (from pH 6) using surfactant Triton X-114 as the extraction medium. Extraction recovery varied from 25.2 to 107.9% with intra-day and inter-day precision (RSD %) ranged 0.88-1087 and 5.32-17.96, respectively. The limits of detection for the studied medicaments at λ 254nm corresponded to therapeutic or low toxic plasma concentration levels. Usefulness of the proposed CPE-HPLC/DAD method for toxicological drug screening was tested via its application to analysis of two serum samples taken from patients suspected of drug overdosing. Published by Elsevier B.V.

  19. The effects of microsphere injections into the left atrium on the myocardial blood supply measured by thermal conductance probes

    Hahn, N.; Eichelkraut, W.; Kropp, J.; Bonn Univ.

    1990-01-01

    210 measurements made during experiments on 66 dogs under propionyl-promazine/pentobarbital narcosis were newly analysed to verify a possible influence of microspheres (9 μm diameter) injected into the left atrium on microcirculation. Using 20 additional dogs in identically performed experiments, the myocardial perfusion was measured using thermal conductance probes, following injections of isotonic NaCl solution, Ringer's solution, 5% glucose, the subject's blood, and isotonic NaCl solution mixed with the surface-active substance Tween 80 R . These supension media were injected both with and without unlabelled microspheres (8.6 μm diameter). The results led to the following conclusions. An obligatory decrease in the blood supply as the result of a mechanical blocking of capillaries by microspheres can be ruled out. The particles, the suspension media, and a suspension temperature not sufficiently adjusted to the body temperature induce reactive negative or positive changes in the microcirculation of the myocardium. Solutions containing particles cause, in the majority of cases, a decrease. The suspension medium with the smallest effect proved to be isotonic NaCl solution. From the results one can conclude that artefacts may arise from the application of the heat conductance probe method when the temperatures are not perfectly matched. However, the injected solution itself can often lead to various reactions in microcirculation which may last up to 5 min. It is advisable to allow at least 6 min to elapse after reactive changes have faded before administering the next injection. (orig./MG)

  20. [Augmented antipsychotic therapy with pantogam active in patients with schizophrenia].

    Medvedev, V E; Frolova, V I; Gushanskaya, E V; Ter-Israelyan, A U

    2015-01-01

    to study the efficacy of the GABA-ergic drug pantogam active (D-, L-gopantenic acid) in patients with schizophrenia treated with typical neuroleptics and to assess the rate of treatment response and tolerability of the drug. A sample consisted of 70 patients with schizophrenia stratified into main (n=35) and control (n=35) groups. All patients received one of typical antipsychotics (haloperidol, zuclopenthixol, promazine or perphenazine). Patients of the main group received in addition pantogam active in dose of 1200-1800 mg daily. The maximum allowed dose of 1800 mg daily was used in 62.9% of the patients. The long-term combined therapy with the addition of D-, L-gopantenic acid (pantogam activ) allowed to achieve clinical improvement earlier (on 8th week in the main group versus 16th week in the control group). The frequency and severity of secondary negative symptoms associated with antipsychotic therapy were decreased as well. The high efficacy and tolerability of the combined therapy allow to improve quality of life in patients with schizophrenia and their compliance to treatment as well as to reduce costs of medical care.

  1. Comparison of TiO2 photocatalysis, electrochemically assisted Fenton reaction and direct electrochemistry for simulation of phase I metabolism reactions of drugs.

    Ruokolainen, Miina; Gul, Turan; Permentier, Hjalmar; Sikanen, Tiina; Kostiainen, Risto; Kotiaho, Tapio

    2016-02-15

    The feasibility of titanium dioxide (TiO2) photocatalysis, electrochemically assisted Fenton reaction (EC-Fenton) and direct electrochemical oxidation (EC) for simulation of phase I metabolism of drugs was studied by comparing the reaction products of buspirone, promazine, testosterone and 7-ethoxycoumarin with phase I metabolites of the same compounds produced in vitro by human liver microsomes (HLM). Reaction products were analysed by UHPLC-MS. TiO2 photocatalysis simulated the in vitro phase I metabolism in HLM more comprehensively than did EC-Fenton or EC. Even though TiO2 photocatalysis, EC-Fenton and EC do not allow comprehensive prediction of phase I metabolism, all three methods produce several important metabolites without the need for demanding purification steps to remove the biological matrix. Importantly, TiO2 photocatalysis produces aliphatic and aromatic hydroxylation products where direct EC fails. Furthermore, TiO2 photocatalysis is an extremely rapid, simple and inexpensive way to generate oxidation products in a clean matrix and the reaction can be simply initiated and quenched by switching the UV lamp on/off. Copyright © 2015 Elsevier B.V. All rights reserved.

  2. A "Light Meal" Three Hours Preoperatively Decreases the Incidence of Gastro-Esophageal Reflux in Dogs.

    Savvas, Ioannis; Raptopoulos, Dimitrios; Rallis, Timoleon

    Emerging evidence from veterinary and medical clinical research shows that reducing preoperative fasting time may reduce the incidence of gastro-esophageal reflux (GER) intraoperatively. In order to evaluate the effect of two different preoperative fasting times on the incidence of GER during general anesthesia, 120 dogs were randomly assigned to two groups: administration of canned food 3 h before premedication (group C3, n = 60) and administration of canned food 10 h before premedication (group C10, n = 60). The animals were premedicated with propionyl-promazine. Anesthesia was induced with thiopental sodium and maintained with halothane. A pH electrode was introduced into the esophagus, and the esophageal pH was constantly monitored. Esophageal pH of less than 4 or greater than 7.5 was taken as an indication of GER. Three of the 60 dogs of group C3 and 12 of the 60 dogs of group C10 experienced a GER episode, the difference being statistically significant (P = .025). Feeding the dog 3 h before anesthesia at a half daily rate reduces significantly the incidence of GER during anesthesia, compared to the administration of the same amount and type of food 10 h before anesthesia. The administration of a half daily dose of an ordinary canine diet may be useful in clinical practice.

  3. Models of treatment with antipsychotics of the schizophrenic patients

    Svjetlana Loga-Zec

    2005-11-01

    Full Text Available The aim of this study were to determine which antipsychotic are currently in use, to establish which doses are administrated to patients, to find out is there a practice of proscribing simultaneously more then one antipsychotic drug, to determine whether antipsychotic are proscribed in divided doses, to establish whether there is, besides antipsychotics, treatment with other medicaments (co-administration, especially with antiparkinsonics. The research (study is epidemiological-clinical prospective, descriptive and analytical and it was conducted at University hospitals in Sarajevo, Tuzla and Mostar. Criteria for inclusion, non-inclusion and exclusion from the study were precisely defined as a mean for formation of sample. Based on this hypothesis were established, zero and alterative. According to zero hypothesis in the treatment of schizophrenia at University hospitals in FBiH new antipsychotic drugs are in use, small doses are proscribed (up to 20 mg, not more then one antipsychotic drug is used simultaneously, antipsychotics are administrated once a day and alongside with antipsychotics other medicaments are not co-administrated, especially antiparkinsons. The results of our study are showing that majority of patients are treated with classical antipsychotics. Minority of patients is treated with atypical neuroleptics like olanzapine, which is proscribed only in Sarajevo. Use of risperidone and ziprasidone is registered also only in Sarajevo, but only small number of patients is treated with these drugs. Most frequent antipsychotics were promazine and haloperidol. The range between minimal and maximal daily dose of promazine was from 50 to 450 mg/daily, and for haloperidol from 1 to 75 mg/daily. Above-mentioned drugs were administrated in an average from two to three times a day. Alongside with antipsychotics, other drugs were used. Most frequent was the use of biperidine in oral and parenteral formulation, as

  4. Exposure of Chlorpromazine to 266 nm Laser Beam Generates New Species with Antibacterial Properties: Contributions to Development of a New Process for Drug Discovery

    Pascu, Mihail Lucian; Danko, Balazs; Martins, Ana; Jedlinszki, Nikoletta; Alexandru, Tatiana; Nastasa, Viorel; Boni, Mihai; Militaru, Andra; Andrei, Ionut Relu; Staicu, Angela; Hunyadi, Attila; Fanning, Seamus; Amaral, Leonard

    2013-01-01

    Introduction Phenothiazines when exposed to white light or to UV radiation undergo a variety of reactions that result in degradation of parental compound and formation of new species. This process is slow and may be sped up with exposure to high energy light such as that produced by a laser. Methods Varying concentrations of Chlorpromazine Hydrochloride (CPZ) (2–20 mg/mL in distilled water) were exposed to 266 nm laser beam (time intervals: 1–24 hrs). At distinct intervals the irradiation products were evaluated by spectrophotometry between 200–1500 nm, Thin Layer Chromatography, High Pressure Liquid Chromatography (HPLC) - Diode Array Detection, HPLC tandem mass spectrometry, and for activity against the CPZ sensitive test organism Staphylococcus aureus ATCC 25923. Results CPZ exposure to 266 nm laser beam of given energy levels yielded species, whose number increased with duration of exposure. Although the major species produced were Promazine (PZ), hydroxypromazine or PZ sulfoxide, and CPZ sulfoxide, over 200 compounds were generated with exposure of 20 mg/mL of CPZ for 24 hrs. Evaluation of the irradiation products indicated that the bioactivity against the test organism increased despite the total disappearance of CPZ, that is due, most probably, to one or more new species that remain yet unidentified. Conclusions Exposure of CPZ to a high energy (6.5 mJ) 266 nm laser beam yields rapidly a large number of new and stable species. For biological grade phenothiazines (in other words knowing the impurities in the samples: solvent and solute) this process may be reproducible because one can control within reasonably low experimental errors: the concentration of the parent compound, the laser beam wavelength and average energy, as well as the duration of the exposure time. Because the process is “clean” and rapid, it may offer advantages over the pyrogenically based methods for the production of derivatives. PMID:23405212

  5. The effect of pre-anaesthetic fasting time and type of food on gastric content volume and acidity in dogs.

    Savvas, Ioannis; Rallis, Timoleon; Raptopoulos, Dimitris

    2009-11-01

    To investigate the effect of pre-anaesthetic fasting time and variety of food on gastric content (GC) volume and pH in dogs. Randomized, cross-over, prospective experimental study. Fifteen mongrel dogs (nine females and six males 1-4 years old, weighing 10-24.5 kg). Each dog received the same seven treatments in random order: dry food 3 hours before anaesthesia (BA) (treatment 3D), canned food (half daily rate) 3 hours BA (treatment 3C), 0% fat cow milk 3 hours BA (treatment 3M), dry food 10 hours BA (treatment 10D), canned food 10 hours BA (treatment 10C), low fat canned food 10 hours BA (treatment 10F) and low protein canned food 10 hours BA (treatment 10P). All animals were pre-medicated with propionyl promazine and anaesthesia was induced with thiopental sodium and maintained with halothane. GC was aspirated using an orogastric catheter and its volume and pH were measured. Treatment 10F had significantly lower GC pH than all the 3-hour treatments. Treatments 10D and 10P had significantly lower pH than treatments 3D and 3C. Treatment 3M had significantly lower pH than the other 3-hour treatments. Treatment 3D had significantly greater gastric volume than treatments 3M, 10C, 10F and 10P. Canned food at half the daily rate administered 3 hours before anaesthesia did not increase significantly the GC volume compared to the other types of food used. The GC pH was also high. This type of food fed 3 hours before induction of anaesthesia may be of benefit in reduction of the incidence of gastro-oesophageal reflux during anaesthesia in dogs.

  6. Novel and versatile solid-state chemiluminescence sensor based on TiO2-Ru(bpy)32+ nanoparticles for pharmaceutical drugs detection

    Al-Hetlani, Entesar; Amin, Mohamed O.; Madkour, Metwally

    2018-02-01

    This work describes a novel and versatile solid-state chemiluminescence sensor for analyte detection using TiO2-Ru(bpy)32+-Ce(IV). Herein, we report the synthesis, characterization, optimization and application of a new type of hybrid nanoparticles (NPs). Mesoporous TiO2-Ru(bpy)32+ NPs were prepared using a modified sol-gel method by incorporating Ru(bpy)32+ into the initial reaction mixture at various concentrations. The resultant bright orange precipitate was characterized via transmission electron microscopy, N2 sorpometry, inductively coupled plasma-optical emission spectrometer (ICP-OES), Raman and UV-Vis spectroscopy techniques. The concentration of Ru(bpy)32+ complex in the NPs was quantified using ICP-OES, and its chemiluminescence (CL) response was measured and compared with the same concentration in the liquid phase using oxalate as model analyte. The results showed that this type of hybrid material exhibited a higher CL signal compared with the liquid phase due to the enlarged surface area of the hybrid NPs ( 149.6 m2/g). The amount of TiO2-Ru(bpy)32+ NPs and the effect of the analyte flow rate were also investigated to optimize the CL signal. The optimized system was further used to detect oxalate and two pharmaceutical drugs, namely, imipramine and promazine. The linear range for both drugs was 1-100 pm with limits of detection (LOD) of 0.1 and 0.5 pm, respectively. This approach is considered to be simple, low cost and facile and can be applied to a wide range of analytes.

  7. Novel and versatile solid-state chemiluminescence sensor based on TiO2-Ru(bpy32+ nanoparticles for pharmaceutical drugs detection

    Al-Hetlani Entesar

    2018-02-01

    Full Text Available This work describes a novel and versatile solid-state chemiluminescence sensor for analyte detection using TiO2-Ru(bpy32+-Ce(IV. Herein, we report the synthesis, characterization, optimization and application of a new type of hybrid nanoparticles (NPs. Mesoporous TiO2-Ru(bpy32+ NPs were prepared using a modified sol-gel method by incorporating Ru(bpy32+ into the initial reaction mixture at various concentrations. The resultant bright orange precipitate was characterized via transmission electron microscopy, N2 sorpometry, inductively coupled plasma-optical emission spectrometer (ICP-OES, Raman and UV-Vis spectroscopy techniques. The concentration of Ru(bpy32+ complex in the NPs was quantified using ICP-OES, and its chemiluminescence (CL response was measured and compared with the same concentration in the liquid phase using oxalate as model analyte. The results showed that this type of hybrid material exhibited a higher CL signal compared with the liquid phase due to the enlarged surface area of the hybrid NPs (~149.6 m2/g. The amount of TiO2-Ru(bpy32+ NPs and the effect of the analyte flow rate were also investigated to optimize the CL signal. The optimized system was further used to detect oxalate and two pharmaceutical drugs, namely, imipramine and promazine. The linear range for both drugs was 1–100 pm with limits of detection (LOD of 0.1 and 0.5 pm, respectively. This approach is considered to be simple, low cost and facile and can be applied to a wide range of analytes.

  8. Antibacterial activity of antipsychotic agents, their association with lipid nanocapsules and its impact on the properties of the nanocarriers and on antibacterial activity.

    Hassan Nehme

    Full Text Available Bacterial antibiotic resistance is an emerging public health problem worldwide; therefore, new therapeutic strategies are needed. Many studies have described antipsychotic compounds that present antibacterial activity. Hence, the aims of this study were to evaluate the in vitro antibacterial activity of antipsychotics belonging to different chemical families, to assess the influence of their association with lipid nanocapsules (LNCs on their antimicrobial activity as well as drug release and to study the uptake of LNCs by bacterial cells. Antibacterial activity was evaluated against Gram-positive Staphylococcus aureus and Gram negative Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Acinetobacter baumannii by minimum inhibitory concentration (MIC assay, and the capability of killing tested microorganisms was evaluated by time kill assay. LNCs were prepared by phase inversion method, and the antipsychotic agents were incorporated using pre-loading and post-loading strategies. Only phenothiazines and thioxanthenes showed antibacterial activity, which was independent of antibiotic-resistance patterns. Loading the nanocarriers with the drugs affected the properties of the former, particularly their zeta potential. The release rate depended on the drug and its concentration-a maximum of released drug of less than 40% over 24 hours was observed for promazine. The influence of the drug associations on the antibacterial properties was concentration-dependent since, at low concentrations (high nanocarrier/drug ratio, the activity was lost, probably due to the high affinity of the drug to nanocarriers and slow release rate, whereas at higher concentrations, the activity was well maintained for the majority of the drugs. Chlorpromazine and thioridazine increased the uptake of the LNCs by bacteria compared with blank LNCs, even below the minimum inhibitory concentration.

  9. Micellar and analytical implications of a new potentiometric PVC sensor based on neutral ion-pair complexes of dodecylmethylimidazolium bromide-sodium dodecylsulfate.

    Sanan, Reshu; Mahajan, Rakesh Kumar

    2013-03-15

    With an aim to characterize the micellar aggregates of imidazolium based ionic liquids, a new potentiometric PVC sensor based on neutral ion-pair complexes of dodecylmethylimidazolium bromide-sodium dodecylsulfate (C12MeIm(+)DS(-)) has been developed. The electrode exhibited a linear response for the concentration range of 7.9×10(-5)-9.8×10(-3) M with a super-Nernstian slope of 92.94 mV/decade, a response time of 5 s and critical micellar concentration (cmc) of 10.09 mM for C12MeImBr. The performance of the electrode in investigating the cmc of C12MeImBr in the presence of two drugs [promazine hydrochloride (PMZ) and promethazine hydrochloride (PMT)] and three triblock copolymers (P123, L64 and F68) has been found to be satisfactory on comparison with conductivity measurements. Various micellar parameters have been evaluated for the binary mixtures of C12MeImBr with drugs and triblock copolymers using Clint's, Rubingh's, and Motomura's approach. Thus the electrode offers a simple, straightforward and relatively fast technique for the characterization of micellar aggregates of C12MeImBr, complementing existing conventional techniques. Further, the analytical importance of proposed C12MeIm(+)-ISE as end point indicator in potentiometric titrations and for direct determination of cationic surfactants [cetylpyridinium chloride (CPC), tetradecyltrimethylammonium bromide (TTAB), benzalkonium chloride (BC)] in some commercial products was judged by comparing statistically with classical two-phase titration methods. Copyright © 2013 Elsevier Inc. All rights reserved.

  10. Immunoassay detection of drugs in racing horses. IX. Detection of detomidine in equine blood and urine by radioimmunoassay

    Wood, T.; Tai, C.L.; Taylor, D.G.

    1989-01-01

    Detomidine is a potent non-narcotic sedative agent which is currently in the process of being approved for veterinary clinical use in the United States. Since no effective screening method in horses is available for detomidine, we have developed an 125 I radioimmunoassay for detomidine in equine blood and urine as part of a panel of tests for illegal drugs in performance horses. Our 125 I radioimmunoassay has an I-50 for detomidine of approximately 2 ng/ml. Our assay shows limited cross-reactivity with the pharmacodynamically similar xylazine, but does not cross-react with acepromazine, epinephrine, haloperidol or promazine. The plasma kinetic data from clinical (greater than or equal to 5 mg/horse) as well as sub-clinical doses indicate first-order elimination in a dose-dependent manner. Within the first 30 minutes after intravenous (IV) administration of 30 mg/horse, plasma levels peak at approximately 20 ng/ml and then decline with an apparent plasma half-life of 25 minutes. Diuresis can occur with administration of clinical doses of detomidine and this effect was accounted for in the analysis of urine samples. Using this method, administration of 30 mg/horse can be readily detected in equine urine for up to 8 hours after IV injection. Additionally, doses as low as 0.5 mg/horse can be detected for short periods of time in blood and urine with use of this assay. Utilization of this assay by research scientists and forensic analysts will allow for the establishment of proper guidelines and controls regarding detomidine administration to performance horses and assurance of compliance with these guidelines

  11. Human serum albumin unfolding pathway upon drug binding: A thermodynamic and spectroscopic description

    Cheema, Mohammad Arif; Taboada, Pablo; Barbosa, Silvia; Juarez, Josue; Gutierrez-Pichel, Manuel; Siddiq, Mohammad; Mosquera, Victor

    2009-01-01

    The interest on phenothiazine drugs has been increased during last years due to their proved utility in the treatment of several diseases and biomolecular processes. In the present work, the binding of the amphiphilic phenothiazines promazine and thioridazine hydrochlorides to the carrier protein human serum albumin (HSA) has been examined by ζ-potential, isothermal titration calorimetry (ITC), fluorescence and circular dichorism (CD) spectroscopies, and dynamic light scattering (DLS) at physiological pH with the aim of analyzing the role of the different interactions in the drug complexation process with this protein. The ζ-potential results were used to check the existence of complexation. This is confirmed by a progressive screening of the protein charge up to a reversal point as a consequence of drug binding. On the other hand, binding causes alterations on the tertiary and secondary structures of the protein, which were observed by fluorescence and CD spectroscopies, involving a two-step, three-state transition. The thermodynamics of the binding process was derived from ITC results. The binding enthalpies were negative, which reveal the existence of electrostatic interactions between protein and drug molecules. In addition, increases in entropy are consistent with the predominance of hydrophobic interactions. Two different classes of binding sites were detected, viz. Binding to the first class of binding sites is dominated by an enthalpic contribution due to electrostatic interactions whereas binding to a second class of binding sites is dominated by hydrophobic bonding. In the light of these results, protein conformational change resembles the acid-induced denaturation of HSA with accumulation of an intermediate state. Binding isotherms were derived from microcalorimetric results by using a theoretical model based on the Langmuir isotherm. On the other hand, the population distribution of the different species in solution and their sizes were determined

  12. Human serum albumin unfolding pathway upon drug binding: A thermodynamic and spectroscopic description

    Cheema, Mohammad Arif [Grupo de Fisica de Coloides y Polimeros, Departamento de Fisica de la Materia Condensada, Facultad de Fisica, Universidad de Santiago de Compostela, E-15782, Santiago de Compostela (Spain); Department of Chemistry, Quaid-i-Azam University, Islamabad 45320 (Pakistan); Taboada, Pablo [Grupo de Fisica de Coloides y Polimeros, Departamento de Fisica de la Materia Condensada, Facultad de Fisica, Universidad de Santiago de Compostela, E-15782, Santiago de Compostela (Spain); Department of Chemistry, Quaid-i-Azam University, Islamabad 45320 (Pakistan)], E-mail: pablo.taboada@usc.es; Barbosa, Silvia; Juarez, Josue; Gutierrez-Pichel, Manuel [Grupo de Fisica de Coloides y Polimeros, Departamento de Fisica de la Materia Condensada, Facultad de Fisica, Universidad de Santiago de Compostela, E-15782, Santiago de Compostela (Spain); Department of Chemistry, Quaid-i-Azam University, Islamabad 45320 (Pakistan); Siddiq, Mohammad [Department of Chemistry, Quaid-i-Azam University, Islamabad 45320 (Pakistan); Mosquera, Victor [Grupo de Fisica de Coloides y Polimeros, Departamento de Fisica de la Materia Condensada, Facultad de Fisica, Universidad de Santiago de Compostela, E-15782, Santiago de Compostela (Spain); Department of Chemistry, Quaid-i-Azam University, Islamabad 45320 (Pakistan)

    2009-04-15

    The interest on phenothiazine drugs has been increased during last years due to their proved utility in the treatment of several diseases and biomolecular processes. In the present work, the binding of the amphiphilic phenothiazines promazine and thioridazine hydrochlorides to the carrier protein human serum albumin (HSA) has been examined by {zeta}-potential, isothermal titration calorimetry (ITC), fluorescence and circular dichorism (CD) spectroscopies, and dynamic light scattering (DLS) at physiological pH with the aim of analyzing the role of the different interactions in the drug complexation process with this protein. The {zeta}-potential results were used to check the existence of complexation. This is confirmed by a progressive screening of the protein charge up to a reversal point as a consequence of drug binding. On the other hand, binding causes alterations on the tertiary and secondary structures of the protein, which were observed by fluorescence and CD spectroscopies, involving a two-step, three-state transition. The thermodynamics of the binding process was derived from ITC results. The binding enthalpies were negative, which reveal the existence of electrostatic interactions between protein and drug molecules. In addition, increases in entropy are consistent with the predominance of hydrophobic interactions. Two different classes of binding sites were detected, viz. Binding to the first class of binding sites is dominated by an enthalpic contribution due to electrostatic interactions whereas binding to a second class of binding sites is dominated by hydrophobic bonding. In the light of these results, protein conformational change resembles the acid-induced denaturation of HSA with accumulation of an intermediate state. Binding isotherms were derived from microcalorimetric results by using a theoretical model based on the Langmuir isotherm. On the other hand, the population distribution of the different species in solution and their sizes were

  13. Rapid method for the determination of tranquilizers and a beta-blocker in porcine and bovine kidney by liquid chromatography with tandem mass spectrometry

    Mitrowska, Kamila [National Veterinary Research Institute, Department of Pharmacology and Toxicology, al. Partyzantow 57, 24-100 Pulawy (Poland)], E-mail: kamitro@piwet.pulawy.pl; Posyniak, Andrzej; Zmudzki, Jan [National Veterinary Research Institute, Department of Pharmacology and Toxicology, al. Partyzantow 57, 24-100 Pulawy (Poland)

    2009-04-01

    A fast and simple liquid chromatography with tandem mass spectrometry method for detection and confirmation of tranquilizers (chlorpromazine, propionylpromazine, acepromazine, triflupromazine, promazine, azaperone and its metabolite, azaperol) and beta-blocker (carazolol) in porcine and bovine kidney has been presented. The method relies on the extraction with acetonitrile followed by centrifugation. After evaporation of acetonitrile, the residue was reconstituted in a mobile phase and filtrated. The separation of analytes was performed on a C18 column using a mobile phase of acetonitrile and ammonium formate buffer (0.05 M, pH 4.5) with gradient elution. The electrospray ionization was used to obtain the protonated molecules [M+H]{sup +} and two product ions were monitored for each compound. For quantification deutered internal standards were used. The whole method has been validated according to the European Union requirements. Specificity, decision limit (CC{alpha}), detection capability (CC{beta}), trueness and precision were determined. The results showed good trueness ranged from 73.2% to 110.6% with a good R.S.D., less than 13.0% under within-laboratory reproducibility conditions. The calculated critical concentrations of CC{alpha} for phenothiazines were between 5.8 and 6.6 {mu}g kg{sup -1} while for azaperone CC{alpha} was 105.5 {mu}g kg{sup -1} and for azaperol was 121.4 {mu}g kg{sup -1}. CC{alpha} for carazolol was 16.7 {mu}g kg{sup -1} in bovine and 21.9 {mu}g kg{sup -1} in porcine kidney. CC{beta} for phenothiazines were between 6.3 and 7.6 {mu}g kg{sup -1}, for azaperone was 119.0 {mu}g kg{sup -1} and for azaperol was 140.0 {mu}g kg{sup -1}. For carazolol in bovine kidney CC{beta} was 18.6 {mu}g kg{sup -1} whereas in porcine kidney was 24.4 {mu}g kg{sup -1}.

  14. Sorption of structurally different ionized pharmaceutical and illicit drugs to a mixed-mode coated microsampler.

    Peltenburg, Hester; Timmer, Niels; Bosman, Ingrid J; Hermens, Joop L M; Droge, Steven T J

    2016-05-20

    The mixed-mode (C18/strong cation exchange-SCX) solid-phase microextraction (SPME) fiber has recently been shown to have increased sensitivity for ionic compounds compared to more conventional sampler coatings such as polyacrylate and polydimethylsiloxane (PDMS). However, data for structurally diverse compounds to this (prototype) sampler coating are too limited to define its structural limitations. We determined C18/SCX fiber partitioning coefficients of nineteen cationic structures without hydrogen bonding capacity besides the charged group, stretching over a wide hydrophobicity range (including amphetamine, amitriptyline, promazine, chlorpromazine, triflupromazine, difenzoquat), and eight basic pharmaceutical and illicit drugs (pKa>8.86) with additional hydrogen bonding moieties (MDMA, atenolol, alprenolol, metoprolol, morphine, nicotine, tramadol, verapamil). In addition, sorption data for three neutral benzodiazepines (diazepam, temazepam, and oxazepam) and the anionic NSAID diclofenac were collected to determine the efficiency to sample non-basic drugs. All tested compounds showed nonlinear isotherms above 1mmol/L coating, and linear isotherms below 1mmol/L. The affinity for C18/SCX-SPME for tested organic cations without Hbond capacities increased with longer alkyl chains, ranging from logarithmic fiber-water distribution coefficients (log Dfw) of 1.8 (benzylamine) to 5.8 (triflupromazine). Amines smaller than benzylamine may thus have limited detection levels, while cationic surfactants with alkyl chain lengths >12 carbon atoms may sorb too strong to the C18/SCX sampler which hampers calibration of the fiber-water relationship in the linear range. The log Dfw for these simple cation structures closely correlates with the octanol-water partition coefficient of the neutral form (Kow,N), and decreases with increased branching and presence of multiple aromatic rings. Oxygen moieties in organic cations decreased the affinity for C18/SCX-SPME. Log Dfw values of