Prediction of inter-individual variability on the pharmacokinetics of CYP1A2 substrates in non-smoking healthy volunteers.
Authors: Haraya K, Kato M, Chiba K, Sugiyama Y
Abstract
The activity of CYP1A2, a major drug-metabolizing enzyme, is known to be affected by various environmental factors. Our study aimed to predict inter-individual variability of AUC/Dose of CYP1A2 substrates in non-smoking healthy volunteers using the Monte Carlo simulation. Inter-individual variability in hepatic intrinsic clearance of CYP1A2 substrates (CLint,h,1A2) was estimated using dispersion model based on the inter-individual variability (N = 96) of the AUC of caffeine, a major CYP1A2 substrate. The estimated coefficient of variation (CV) of CL...
Source: Drug Metabolism and Pharmacokinetics - June 20, 2016 Category: Drugs & Pharmacology Tags: Drug Metab Pharmacokinet Source Type: research
Influence of Previous Failed Antispasticity Therapy on the Efficacy and Tolerability of THC:CBD Oromucosal Spray for Multiple Sclerosis Spasticity
Conclusions: THC:CBD oromucosal spray provided consistent relief with good tolerability in MS spasticity patients irrespective of their antispasticity pre-treatment history.Eur Neurol 2016;75:236-243 (Source: European Neurology)
Source: European Neurology - May 9, 2016 Category: Neurology Source Type: research
Alpha2-adrenergic agonists for the management of opioid withdrawal.
CONCLUSIONS: Clonidine and lofexidine are more effective than placebo for the management of withdrawal from heroin or methadone. We detected no significant difference in efficacy between treatment regimens based on clonidine or lofexidine and those based on reducing doses of methadone over a period of around 10 days, but methadone was associated with fewer adverse effects than clonidine, and lofexidine has a better safety profile than clonidine.
PMID: 27140827 [PubMed - as supplied by publisher] (Source: Cochrane Database of Systematic Reviews)
Source: Cochrane Database of Systematic Reviews - May 2, 2016 Category: Journals (General) Authors: Gowing L, Farrell M, Ali R, White JM Tags: Cochrane Database Syst Rev Source Type: research
Haloperidol as an Abortive and Preventative Agent in Status Dystonicus (P2.352)
We present two cases with histories of severe spasms, necessitating intrathecal baclofen pump placement, who both required intubation for status dystonicus. It was not until use of haloperidol as a preventative and abortive agent, that there was significantly decreased spasm frequency and severity in these patients. Cases: Patient 1 is a 40-year-old man with cerebral palsy and spasms controlled with a baclofen pump who was admitted for increasing spasms. Treatment with trihexyphenidyl, increasing amounts of baclofen (oral and intrathecal) and onabotulinumtoxinA injections lessened spasm frequency but did not eliminate them...
Source: Neurology - April 3, 2016 Category: Neurology Authors: George, I., Machado, D. Tags: Movement Disorders: Therapeutics Source Type: research
Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation
Conclusion
In the studied real-life setting, we found a considerable number of MQAB users with additional risk factors for TdP but no ECG monitoring. However, adverse drug reactions were rarely found, and costs vs. benefits of ECG monitoring have to be weighted. In contrast, avoidable risk factors and selected contraindicated pharmacokinetic interactions are clear targets for implementation as automated alerts in electronic prescribing systems. (Source: European Journal of Clinical Pharmacology)
Source: European Journal of Clinical Pharmacology - March 28, 2016 Category: Drugs & Pharmacology Source Type: research
Tizanidine for the management of acute postoperative pain after inguinal hernia repair: A placebo-controlled double-blind trial
BACKGROUND: α2-Agonists are used postoperatively as a component of multimodal analgesia. Tizanidine is a centrally acting α2-agonist with muscle relaxant properties.
OBJECTIVE: The aim of this study was to compare the efficacy of tizanidine with placebo in terms of postoperative pain scores, analgesic consumption, return to daily activity and health-related quality of life.
DESIGN: A randomised double-blind study.
SETTING: Diskapi Yildirim Beyazit Training and Research Hospital.
INTERVENTIONS: After obtaining ethical approval and informed patient consent, 60 patients undergoing inguinal hernia repair under general an...
Source: European Journal of Anaesthesiology - February 3, 2016 Category: Anesthesiology Tags: Postoperative pain Source Type: research
Comparison of Efficacy and Side Effects of Oral Baclofen Versus Tizanidine Therapy with Adjuvant Botulinum Toxin Type A in Children With Cerebral Palsy and Spastic Equinus Foot Deformity
This retrospective study aimed to compare the therapeutic response, including side effects, for oral baclofen versus oral tizanidine therapy with adjuvant botulinum toxin type A in a group of 64 pediatric patients diagnosed with static encephalopathy and spastic equinus foot deformity. Following botulinum toxin A treatment, clinical improvement led to the gradual reduction of baclofen or tizanidine dosing to one-third of the former dose. Gross Motor Functional Measure and Caregiver Health Questionnaire scores were markedly elevated post–botulinum toxin A treatment, with scores for the tizanidine (Gross Motor Function...
Source: Journal of Child Neurology - January 12, 2016 Category: Neurology Authors: Dai, A. I., Aksoy, S. N., Demiryürek, A. T. Tags: Original Articles Source Type: research
Long-term myocardial toxicity in a patient with tizanidine and etizolam overdose
Publication date: Available online 28 November 2015 Source:Journal of Cardiology Cases Author(s): Mari Amino, Koichiro Yoshioka, Yuji Ikari, Sadaki Inokuchi Tizanidine hydrochloride, α2-receptor stimulant, is a central muscle relaxant. Etizolam is a benzodiazepine-based anti-anxiety agent. Both drugs are widely used for the treatment of a variety of muscle pain and frequently used together in Japan. We experienced a case of complicating prolonged myocardial dysfunction in a 56-year-old woman. Six hours after overdose of 48mg tizanidine and 24mg etizolam, she showed sinus bradycardia and peripheral vascular res...
Source: Journal of Cardiology Cases - January 12, 2016 Category: Cardiology Source Type: research
Tizanidine-induced acute severe cystitis in a female taking famotidine.
We report a case of a 26-year-old Asian female on famotidine who presented with acute severe urinary burning after taking tizanidine.
PMID: 26251632 [PubMed] (Source: Clinical Pharmacology: Advances and Applications)
Source: Clinical Pharmacology: Advances and Applications - November 29, 2015 Category: Allergy & Immunology Tags: Clin Pharmacol Source Type: research
Analgesic efficacy of oral gabapentin added to standard epidural corticosteroids in patients with failed back surgery.
CONCLUSION: It was concluded that addition of oral gabapentin to epidural corticosteroid application in patients with failed back surgery syndromes was effective in ameliorating pain at an early stage without significant side effects.
PMID: 22291506 [PubMed] (Source: Clinical Pharmacology: Advances and Applications)
Source: Clinical Pharmacology: Advances and Applications - November 29, 2015 Category: Allergy & Immunology Tags: Clin Pharmacol Source Type: research
Tizanidine and Speech Therapy for Spastic Dysarthria: A Case Study
To evaluate tizanidine with speech therapy for dysarthria associated with spastic tetraplegia. (Source: Archives of Physical Medicine and Rehabilitation)
Source: Archives of Physical Medicine and Rehabilitation - November 23, 2015 Category: Rehabilitation Authors: Jon A. Mukand, Patricia Swift Fulton, Minh Tran, Nita H. Mukand Tags: Research Poster Source Type: research
Spinal antinociceptive action of amiloride and its interaction with tizanidine in the rat formalin test.
PMID: 26357686 [PubMed - as supplied by publisher] (Source: Pain Research and Management)
Source: Pain Research and Management - September 10, 2015 Category: Anesthesiology Authors: Ouyang H, Wang P, Huang W, Li Q, Nie B, Zeng W Tags: Pain Res Manag Source Type: research
Evaluation of tizanidine as a marker of canine CYP1A2 activity
The dog CYP1A2 enzyme is likely an important contributor to the metabolism of veterinary drugs. Dog CYP1A2 is expressed in liver, plus it is inducible and polymorphic, creating the potential for intersubject differences in pharmacokinetics. Hence, the ability to probe dog CYP1A2 activity and inhibition is relevant toward veterinary drug development and drug–drug interaction assessment. Previous studies have relied on human probes with questionable specificity for CYP1A2, so it was hypothesized that recombinant CYP1A2 could be used to find a specific CYP1A2 substrate. Intrinsic clearance experiments demonstrated that tiza...
Source: Journal of Veterinary Pharmacology and Therapeutics - July 30, 2015 Category: Veterinary Research Authors: C. W. Locuson, P. Williams, J. M. Adcock, J. S. Daniels Tags: Scientific Paper Source Type: research
Tizanidine-induced acute severe cystitis in a female taking famotidine
We report a case of a 26-year-old Asian female on famotidine who presented with acute severe urinary burning after taking tizanidine. Keywords: adverse drug reaction, cystitis, famotidine, tizanidine (Source: International Journal of COPD)
Source: International Journal of COPD - July 29, 2015 Category: Respiratory Medicine Tags: Clinical Pharmacology: Advances and Applications Source Type: research
Tizanidine-induced cystitis
Poudel RR, Kafle NK (Source: International Journal of COPD)
Source: International Journal of COPD - July 28, 2015 Category: Respiratory Medicine Source Type: research
