Current Issue : July - September Volume : 2020 Issue Number : 3 Articles : 5 Articles
This study investigates the pharmacokinetic (PK) and pharmacodynamic (PD) consequences\nof shifting from Quetiapine fumarate immediate-release (IR) to extended-release (XR) formulation in\nnon-adherent schizophrenia patients. Monte-Carlo simulations using population PK and PD models\nwere implemented to predict the time course of plasma concentration and Brief Psychiatric Rating\nScale (BPRS) scores following the oral administration of 200 mg Seroquel® every 12 h and 400 mg\nSeroquel XR® every 24 h in patients experiencing dose delay, omission or doubling. Parameters\nwere computed and their distributions were compared using the Kolmogorovâ??Smirnov test. Dose\nirregularities with both formulations had different effects on plasma concentration and %reduction in\nBPRS scores from baseline. However, the odds ratio of getting a %reduction in BPRS below 14%, or\nplasma concentration exceeding 500..................
(1S,5R)-4-((E)-3,4-dihydroxy-5-methoxystryryl)-6,6-dimethylbicylco[3.1.1]hept-3-en-2-one\n(SP-8356) is a novel (1S)-(-)-verbenone derivative that is currently in preclinical development for\nthe treatment of ischemic stroke and atherosclerosis. This report aimed at characterization of the\nmetabolism and pharmacokinetic properties of SP-8356. Following intravenous dose in rats and dogs,\nplasma concentrations of SP-8356 declined rapidly with high clearance (CL) and short half-life; after\noral administration in both species, its plasma levels were below the quantitation limit. Fourteen\ncirculating metabolites, formed by mono-oxygenation, demethylation, glucuronidation, catechol\nO-methylation, sulfation and oxidation (bioactivation) followed by glutathione (GSH) conjugation,\nwere tentatively identified in both species. Urinary excretion of SP-8356 appeared to be minimal in\nrats, compared to its metabolites.................
Betahistine dihydrochloride is widely used to reduce the severity and frequency of vertigo\nattacks associated with Ménièreâ??s disease. Betahistine is an analogue of histamine, and is a weak\nhistamine H1 receptor agonist and potent histamine H3 receptor antagonist. The recommended\ntherapeutic dose for adults ranges from 24 to 48 mg given in doses divided throughout the day.\nBetahistine undergoes extensive first-pass metabolism to the major inactive metabolite 2-pyridyl\nacetic acid (2PAA), which can be considered a surrogate index for quantitation of the parent drug\ndue to extremely low plasma levels of betahistine. The aim of the present investigation was to\nassess the pharmacokinetics and dose proportionality of betahistine in Arabic healthy adult male\nsubjects under fasting conditions. A single dose of betahistine in the form of a 8, 16, or 24 mg tablet\nwas administered to 36 subjects in randomized, cross-over, three-period, three-sequence design\nseparated by a one week washout period between dosing......................
The phytocannabinoid-based medicine Sativex® is currently marketed for the treatment\nof spasticity and pain in multiple sclerosis patients and is being investigated for other central and\nperipheral pathological conditions. It may also serve in Veterinary Medicine for the treatment of\ndomestic animals, in particular for dogs affected by different pathologies, including human-like\npathological conditions. With the purpose of assessing different dosing paradigms for using Sativex\nin Veterinary Medicine, we investigated its pharmacokinetics when administered to naïve dogs\nvia sublingual delivery. In the single dose arm of the study, adult Beagle dogs were treated with\n3 consecutive sprays of Sativex, and blood samples were collected at 12 intervals up to 24 h later.\nIn the multiple dose arm of the study, Beagle dogs received 3 sprays daily for 14 days, and blood\nsamples were collected for 24 h post final dose. Blood was used to obtain plasma samples and.....................
The aim of this study was to develop a population pharmacokinetic model for piperacillin\n(PIPC)/tazobactam (TAZ) in late elderly patients with pneumonia and to optimize the administration\nplanning by applying pharmacokinetic/pharmacodynamic (PK/PD) criteria. PIPC/TAZ (total dose\nof 2.25 or 4.5 g) was infused intravenously three times daily to Japanese patients over 75 years\nold. The plasma concentrations of PIPC and TAZ were determined using high-performance liquid\nchromatography and modeled using the NONMEM program. PK/PD analysis with a random\nsimulation was conducted using the final population PK model to estimate the probability of\ntarget attainment (PTA) profiles for various PIPC/TAZ-regimenâ??minimum-inhibitory-concentration\n(MIC) combinations..................
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