Halazepam
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| Non-proprietary name | Halazepam | ||||||||||||||||||
| other names |
7-chloro-5-phenyl-1- (2,2,2-trifluoroethyl) -3 H -1,4-benzodiazepin-2-one |
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| Molecular formula | C 17 H 12 ClF 3 N 2 O | ||||||||||||||||||
| Brief description |
crystalline solid |
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| Molar mass | 352.74 g mol −1 | ||||||||||||||||||
| Physical state |
firmly |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||||||||||||
Halazepam belongs to the group of long and powerful benzodiazepine derivatives. The effect is strongly sedative (calming) to hypnotic (sleep-promoting), muscle-relaxing , anxiolytic (anxiolytic) and anticonvulsive (anticonvulsant). While taking halazepam one can in a short time depending arise.
field of use
Halazepam is indicated for symptomatic relief of anxiety and transient anxiety disorders.
Pharmacodynamics
Halazepam acts, like all benzodiazepines by the neurotransmission of the main inhibitory neurotransmitter γ-aminobutyric acid influences (GABA). Benzodiazepines bind to the GABA A receptor and act as an allosteric modulator of the neurotransmitter. This can be explained pharmacodynamically by the fact that benzodiazepines bind to the protein subunit of the receptor and change the permeability of the chloride channel . This leads to an increase in conductivity in the channel and the influx of chloride ions into the interior of the nerve cell. As a result, there is a short circuit across the excitatory postsynaptic potential (EPSP) and hyperpolarization of downstream neurons.
Pharmacokinetics
Halazepam is well and quickly absorbed after oral administration and is mainly excreted in the urine. The maximum plasma concentration after administration of a single dose is reached after approximately two hours. In two studies with 12 healthy volunteers, the median half-life of halazepam was 13.9 hours. The main biotransformation pathway is demethylation to N- desmethyldiazepam , which occurs as the main metabolite in plasma. In humans, N- desmethyldiazepam is also an important plasma metabolite of diazepam ; its elimination half-life is 76 to 90 hours.
Side effects and interactions
Halazepam has the typical side effects of the benzodiazepines. First and foremost, fatigue, dizziness , visual impairment, double vision , confusion and a "hangover" can occur. While the effectiveness of Halazepam is comparable to that of Diazepam, the side effect profile is said to be more favorable.
In the case of simultaneous use with other psychotropic drugs or anticonvulsants , the pharmacology of these substances should be taken into account. Phenothiazines , barbiturates , MAO inhibitors , antidepressants , antihistamines or anesthetics, for example, can increase the effect, as can alcohol consumption. Substances that inhibit cytochrome P450 can also increase the effects of halazepam.
Web links
- Halazepam on drugs.com
Individual evidence
- ↑ a b c caymanchem.com: Halazepam (PDF) accessed December 11, 2017.
- ↑ a b c Resumo das Características do Medicamento - Pacinone Comprimido 40 mg / 120 mg ( Technical Information Pacinone Tablets, Schering-Plow Farma, Lda., Portugal), June 2009.
- ↑ WE Fann, WM Pitts, JC Wheless: Pharmacology, efficacy, and adverse effects of halazepam, a new benzodiazepine. Pharmacotherapy 2 (2), 1982, pp. 72-79. PMID 6152591 .