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David E Moody, Yueqiao Fu, Wenfang B Fang
The purpose of this study was to test the hypothesis that skeletal muscle relaxants could inhibit the in vitro metabolism of common co-medications opioids buprenorphine, methadone and oxycodone. The compounds (solubility-limited concentration (μM) studied) were: baclofen (1000), carisoprodol (200), its metabolite meprobamate (1000), chlorzoxazone (200), cyclobenzaprine (1000), metaxalone (50), methocarbamol (1000), orphenadrine (1000) and tizanidine (1000). Compounds were first incubated with human liver microsomes (HLM) ± pre-incubation, screened with pathway-specific cDNA-expressed cytochrome P450s (rCYP), and then IC50 values determined using either 8-concentration tests for those where the rCYP screen suggested an IC50 was achievable, or a 3-concentration test with downward extrapolation if screen suggested 50% inhibition was not achievable...
March 5, 2018: Basic & Clinical Pharmacology & Toxicology
Khalid Al Khaja, Husain Ahmed Isa, Sindhan Veeramuthu, Reginald P Sequeira
OBJECTIVES: The aims of the study were to evaluate: a) the prevalence and types of potentially inappropriate prescribing in older adults with hypertension or diabetes mellitus and hypertension; and b) whether or not the differences in training of primary care physicians was associated with the PIP. MATERIALS AND METHODS: Primary care prescriptions issued by family physicians and general practitioners were audited using Screening Tools of Older Person's Prescriptions criteria (version 1) with 18 out of 65 applicable criteria...
March 1, 2018: Medical Principles and Practice: International Journal of the Kuwait University, Health Science Centre
Hanna Bergman, Karla Soares-Weiser
BACKGROUND: Antipsychotic (neuroleptic) medication is used extensively to treat people with serious mental illnesses. However, it is associated with a wide range of adverse effects, including movement disorders. Because of this, many people treated with antipsychotic medication also receive anticholinergic drugs in order to reduce some of the associated movement side-effects. However, there is also a suggestion from animal experiments that the chronic administration of anticholinergics could cause tardive dyskinesia...
January 17, 2018: Cochrane Database of Systematic Reviews
Benjamin W Friedman, David Cisewski, Eddie Irizarry, Michelle Davitt, Clemencia Solorzano, Adam Nassery, Scott Pearlman, Deborah White, E John Gallagher
STUDY OBJECTIVE: In US emergency departments (EDs), patients with low back pain are often treated with nonsteroidal anti-inflammatory drugs and muscle relaxants. We compare functional outcomes among patients randomized to a 1-week course of naproxen+placebo versus naproxen+orphenadrine or naproxen+methocarbamol. METHODS: This was a randomized, double-blind, comparative effectiveness trial conducted in 2 urban EDs. Patients presenting with acute, nontraumatic, nonradicular low back pain were enrolled...
October 28, 2017: Annals of Emergency Medicine
Nick B Polito, Shawn E Fellows
BACKGROUND: Chlorpromazine is the only drug approved by the US Food and Drug Administration for the treatment of hiccups; however, many other pharmacologic treatments have been proposed for intractable and persistent hiccups. Currently, there is little evidence to support the use of one agent over another. OBJECTIVE: This review aims to identify literature concerning the use of pharmacologic treatments for intractable and persistent hiccups with the goal of evaluating therapies in terms of their level of evidence, mechanism of action, efficacy, dosing, onset of action, and adverse effects...
October 2017: Journal of Emergency Medicine
Rafael R Cunha, Michelle M A C Ribeiro, Rodrigo A A Muñoz, Eduardo M Richter
Paracetamol is an active ingredient commonly found in pharmaceutical formulations in combination with one of the following compounds: codeine, orphenadrine, promethazine, scopolamine, and tramadol. In this work, we propose a unique analytical method for determination of these active ingredients in pharmaceutical samples. The method is based on capillary electrophoresis with capacitively coupled contactless conductivity detection. The separation was achieved on a fused silica capillary (50 cm total length, 40 cm effective length, and 50 μm id) using an optimized background electrolyte composed of 20 mmol/L β-alanine/4 mmol/L sodium chloride/4 μmol/L sodium hydroxide (pH 9...
April 2017: Journal of Separation Science
Xin Wang, Sys Stybe Johansen, Marie Katrine Klose Nielsen, Kristian Linnet
A multi-target method that can detect a broad range of drugs in human hair, such as hypnotics, anxiolytics, analgesics, benzodiazepines, antihistamines, antidepressants, antipsychotics, and anticonvulsants, was developed based on ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). The drugs were extracted from 10 mg of washed hair by incubation for 18 h in a 25:25:50 (v/v/v) mixture of methanol/acetonitrile/2 mM ammonium formate (8% acetonitrile, pH 5.3). For 51% of the basic drugs, the lower limits of quantification (LLOQs) were in the range of 0...
August 2017: Drug Testing and Analysis
Seiji Yamasaki, Takuma Fujioka, Katsuhiko Hayashi, Suguru Yamasaki, Mitsuko Hayashi-Nishino, Kunihiko Nishino
A large number of drug efflux transporters have been identified in Salmonella enterica serovar Typhimurium, and increased expression of these transporters confers drug resistance in this organism. Here we compared the respiration activities of the wild-type strain and a mutant with nine deleted transporters by phenotype microarray analysis. The mutant was susceptible to 66 structurally unrelated compounds including many antibiotics, dyes, detergents, antihistamine agents, plant alkaloids, antidepressants, antipsychotic drugs, and antiprotozoal drugs...
November 2016: Journal of Infection and Chemotherapy: Official Journal of the Japan Society of Chemotherapy
Tarek S Belal, Karim M Abdel-Hay, C Randall Clark
A novel simple, direct and selective gas chromatography-mass spectrometry (GC/MS) procedure was developed for the determination of the antihistamine drug dimenhydrinate (DMH) in presence of six of its related substances and potential impurities, namely, diphenylmethane, diphenylmethanol, benzophenone, orphenadrine, caffeine and 8-chlorocaffeine. The method involved resolution of the underivatized compounds using a trifluoropropylmethyl polysiloxane (Rtx-200) capillary column and the mass spectrometric detection was carried out in the electron-impact (EI) mode...
January 2016: Journal of Advanced Research
Ravindra Kumar, Yoichi Hoshimoto, Hayato Yabuki, Masato Ohashi, Sensuke Ogoshi
A highly enantioselective synthesis of 3-aryl-, vinyl-, and alkynyl-2,1-benzoxasiloles (up to 99.9% ee and 99% yield) was achieved via the sequential activation of an aldehyde and a silane by nickel(0). This strategy was applied to a simultaneous generation of carbon- and silicon-stereogenic centers with excellent selectivity (dr = 99:1) via diastereotopic aryl transfer. Initial mechanistic studies revealed the complete switching of an aryl-transfer process from an intermolecular (racemic synthesis in the presence of IPr) to an intramolecular (enantioselective synthesis using chiral NHC, L5) fashion...
September 16, 2015: Journal of the American Chemical Society
Mary Hongying Cheng, Ethan Block, Feizhuo Hu, Murat Can Cobanoglu, Alexander Sorkin, Ivet Bahar
Human dopamine (DA) transporter (hDAT) regulates dopaminergic signaling in the central nervous system by maintaining the synaptic concentration of DA at physiological levels, upon reuptake of DA into presynaptic terminals. DA translocation involves the co-transport of two sodium ions and the channeling of a chloride ion, and it is achieved via alternating access between outward-facing (OF) and inward-facing states of DAT. hDAT is a target for addictive drugs, such as cocaine, amphetamine (AMPH), and therapeutic antidepressants...
2015: Frontiers in Neurology
Yong-Sook Park, Young-Baeg Kim, Jeong-Min Kim
Nefopam, a centrally acting analgesic, has been used to control postoperative pain. Reported adverse effects are anticholinergic, cardiovascular or neuropsychiatric. Neurologic adverse reactions to nefopam are confusion, hallucinations, delirium and convulsions. There are several reports about fatal convulsive seizures, presumably related to nefopam. A 71-year-old man was admitted for surgery for a lumbar spinal stenosis. He was administered intravenous analgesics : ketorolac, tramadol, orphenadrine citrate and nefopam HCl...
November 2014: Journal of Korean Neurosurgical Society
Bassem Sadek, Seyedeh Soha Khanian, Abrar Ashoor, Tatiana Prytkova, Mohammad A Ghattas, Noor Atatreh, Syed M Nurulain, Keun-Hang Susan Yang, Frank Christopher Howarth, Murat Oz
Effects of the histamine H₁ receptor (H1R) antagonists (antihistamines), promethazine (PMZ), orphenadrine (ORP), chlorpheniramine (CLP), pyrilamine (PYR), diphenhydramine (DPH), citerizine (CTZ), and triprolidine (TRP) on the functional properties of the cloned α7 subunit of the human nicotinic acetylcholine receptor expressed in Xenopus oocytes were investigated. Antihistamines inhibited the α7-nicotinic acetylcholine receptor in the order PYR>CLP>TRP>PMZ>ORP≥DPH≥CTZ. Among the antihistamines, PYR showed the highest reversible inhibition of acetylcholine (100 µM)-induced responses with IC₅₀ of 6...
January 5, 2015: European Journal of Pharmacology
Ali M Yehia, Mohamed K Abd El-Rahman
Normalized spectra have a great power in resolving spectral overlap of challenging Orphenadrine (ORP) and Paracetamol (PAR) binary mixture, four smart techniques utilizing the normalized spectra were used in this work, namely, amplitude modulation (AM), simultaneous area ratio subtraction (SARS), simultaneous derivative spectrophotometry (S(1)DD) and ratio H-point standard addition method (RHPSAM). In AM, peak amplitude at 221.6nm of the division spectra was measured for both ORP and PAR determination, while in SARS, concentration of ORP was determined using the area under the curve from 215nm to 222nm of the regenerated ORP zero order absorption spectra, in S(1)DD, concentration of ORP was determined using the peak amplitude at 224nm of the first derivative ratio spectra...
March 5, 2015: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Jessica L Knittel, Shawn P Vorce, Barry Levine, Rhome L Hughes, Thomas Z Bosy
A multidrug fatality involving sumatriptan is reported. Sumatriptan is a tryptamine derivative that acts at 5-HT(1B/1D) receptors and is used for the treatment of migraines. The decedent was a 21-year-old white female found dead in bed by her spouse. No signs of physical trauma were observed and a large number of prescription medications were discovered at the scene. Toxicological analysis of the central blood revealed sumatriptan at a concentration of 1.03 mg/L. Following therapeutic dosing guidelines, sumatriptan concentrations do not exceed 0...
January 2015: Journal of Analytical Toxicology
Yu-Wen Chen, Jann-Inn Tzeng, Yu-Chung Chen, Ching-Hsia Hung, Jhi-Joung Wang
The purpose of this study was to estimate the local anesthetic effect of orphenadrine, an anti-muscarinic agent, in spinal anesthesia and its comparison with the local anesthetic lidocaine. After the rat was injected intrathecally, the spinal block of orphenadrine and lidocaine was constructed in a dosage-dependent fashion. The potency and duration of spinal anesthesia with orphenadrine were compared with that of lidocaine. Our data demonstrated that orphenadrine and lidocaine elicited dose-dependent spinal blockades on the motor function, sensory, and proprioception...
November 5, 2014: European Journal of Pharmacology
Marta Maltese, Giuseppina Martella, Graziella Madeo, Irene Fagiolo, Annalisa Tassone, Giulia Ponterio, Giuseppe Sciamanna, Pierre Burbaud, P Jeffrey Conn, Paola Bonsi, Antonio Pisani
Broad-spectrum muscarinic receptor antagonists have represented the first available treatment for different movement disorders such as dystonia. However, the specificity of these drugs and their mechanism of action is not entirely clear. We performed a systematic analysis of the effects of anticholinergic drugs on short- and long-term plasticity recorded from striatal medium spiny neurons from DYT1 dystonia knock-in (Tor1a(+/Δgag) ) mice heterozygous for ΔE-torsinA and their controls (Tor1a(+/+) mice). Antagonists were chosen that had previously been proposed to be selective for muscarinic receptor subtypes and included pirenzepine, trihexyphenydil, biperiden, orphenadrine, and a novel selective M1 antagonist, VU0255035...
November 2014: Movement Disorders: Official Journal of the Movement Disorder Society
Emmanuela Marchi, Leonardo Furi, Stefania Arioli, Ian Morrissey, Valeria Di Lorenzo, Diego Mora, Luciana Giovannetti, Marco Rinaldo Oggioni, Carlo Viti
Staphylococcus aureus strains harboring QacA, QacB, QacC, QacG transporters and norA promoter up-regulating mutations were characterized by phenotype microarray (PM), standard methods for susceptibility testing, and ethidium bromide efflux assays, in order to increase knowledge on phenotypes associated to efflux pumps and their substrates. PM data and standard susceptibility testing lead to the identification of new potential efflux targets, such as guanidine hydrochloride or 8-hydroxyquinoline for QacA and QacC pumps, respectively...
January 2015: Microbiological Research
Iu I Hubs'kyĭ, T A Bukhtiarova, H H Horiushko, N V Litvinova, H I Paramonova, T M Kurapova, O M Velychko, L P Babenko
Methods of fluorescent probing, spectrophotometry and microcalorimetry were applied to investigate the alterations in biophysical parameters of erythrocytes membranes, and specifically microviscosity, surface charge, molecular organization of lipid bilayer and lipid-protein interactions under conditions of acute pain syndrome produced by experimental chemical lesion. The distinctive features of non-opiod analgesics interactions and binding to the erythrocytes membranes of rats subjected to acute nociceptive pain accompanied with oxidative stress development were investigated...
May 2014: Ukrainian Biochemical Journal
Konrad Rejdak, Dorota Nieoczym, Mirosław Czuczwar, Jacek Kiś, Piotr Wlaź, Waldemar A Turski
BACKGROUND: Identification of new molecular targets as well as the new models recapitulating different aspects of pathophysiology of status epilepticus (SE) in humans might prove essential for the breakthrough in the efforts against pharmacoresistance in epilepsy. Recently, we described a new model of generalized convulsive SE induced with orphenadrine (ORPH) in rats with unique characteristics [5]. The current study was aimed at assessing the efficacy of a new generation antiepileptic drugs (AEDs) and some of the experimental agents in suppressing ORPH-evoked seizures in rats...
June 2014: Pharmacological Reports: PR
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