Disease relevance of Metaclazepam

• Tilting experiments in dogs did not show any risk for postural hypotension due to metaclazepam [1].
• At intravenous, intraduodenal and repeated oral administration of metaclazepam in anesthetized cats and dogs and RHR arterial hypotension, if any, occurred only at rather high dosages [1].

High impact information on Metaclazepam

• Higher GH stimulation occurred after diazepam (10 mg i.v.) than after diazepam (10 mg p.o.). No dose-dependent difference in GH stimulation after metaclazepam (10 and 30 mg p.o.) was apparent [2].
• The therapeutic efficacy and tolerance of metaclazepam and diazepam were compared in a double-blind study of outpatients suffering from a generalized anxiety syndrome [3].
• Double-blind randomized trial of the benzodiazepine derivative metaclazepam as compared with placebo treatment of outpatients with anxiety syndromes [4].
• A single-centre, open, Phase I-study comparison of the pharmacokinetics of a single dose of metaclazepam 10 mg, a new 1,4-benzodiazepine has been done in 10 older and 20 younger volunteers [5].
• No important age-related effect was found on the kinetics of metaclazepam or its N-desmethyl derivative, the principal metabolite in man [5].

Biological context of Metaclazepam

• Qualitative and quantitative differences in the biotransformation products of metaclazepam in comparison with the well known metabolites of other drugs in the 1,4-benzodiazepine class could be demonstrated [6].

Anatomical context of Metaclazepam

• In guinea pig papillary muscles and in anesthetized dogs (i.v.), metaclazepam had a moderate negative inotropic effect [1].
• Transfer of metaclazepam and its metabolites into breast milk [7].

Associations of Metaclazepam with other chemical compounds

• DMI thus causes reliable GH stimulation in healthy male subjects, whereas GH stimulation could only be measured in some of the subjects after diazepam and metaclazepam [2].
• Plasma levels of metaclazepam and its major biotransformation product, N-desmethylmetaclazepam, were determined [8].

Gene context of Metaclazepam

• Metabolism and pharmacokinetics of metaclazepam (Talis), Part III: Determination of the chemical structure of metabolites in dogs, rabbits and men [6].

Analytical, diagnostic and therapeutic context of Metaclazepam

• Two dosage regimens were compared by a randomized two-way crossover design: a once-a-day dosing (15 mg metaclazepam in the evening, = A) versus a twice-a-day dosing (5 mg in the morning plus 10 mg in the evening, = B) over ten days in twelve healthy male volunteers [8].

References