Benzodiazepine
The benzodiazepines are a class of Médicament S with the properties Hypnotique S, Anxiolytique S, Antiépileptique S, Amnésiant be and Myorelaxant be. Benzodiazepines are often used to relieve with short-term the Anxiété, the Insomnie severe or stun. The use with the long-term can be problematic because of the appearance of a tolerance and a Addiction (dependence). It is thought that they act on the GABAA, receiver of the GABA whose activation moderates the activity of the Neuron S. They appeared in the Années 1960 and 1970.
GABA is a inhibiting Neurotransmetteur. While being fixed at its receiver which is an ionic channel, it opens this channel to allow the passage of ions chloride. Scientifically, it is said that benzodiazepines are positive modulators allosteric of the inhibiting neurotransmission GABAergique: they act on a site different from that of the GABA and increase the affinity of that Ci for its receiver. For the same quantity of GABA, the ionic channel will be open in a more important way, which will allow the passage of more than ions chlorides and a stronger inhibition.
History
August 1st
Representatives of this family
The table which follows gives the list, of the principal molecules benzodiazepines. For each molecule, are indicated moreover:- Trade name of the “French-speaking” specialities using this molecule. Certain molecules benzodiazepines are available in generic form; trade name is then a couple molecule-laboratory, for example Alprazolam-Alter® is credits of the molecule alprazolam distributed by the Alter® Laboratory; the indication Générique at the beginning of the list of the specialities announces the existence of one or more credits for the corresponding molecule, indication followed then of the list of the other specialities not credits .
- duration of Half-life; various benzodiazepines have rather comparable effects, with this close the duration of action can be very short, a few hours, or relatively long, several days. In the first case, the molecule is in general used like Hypnotique (soporific), in the second like Anxiolytique (tranquillizing). But the border between these two classes cannot be precisely defined.
- the most frequent use:
- has = Anxiolytique.
- H = Hypnotic.
- M = Myorelaxant.
- S = Antispasmodique.
The patients are not always informed generally when one prescribes chlordiazépoxide (Librax®) to them, like antispasmodic, or tétrazépam (Myolastan®), not prescribed like myorelaxant, that they are in fact benzodiazepines possibly combined with other molecules.
The following substances are not benzodiazepines, but have similar effects:
- Zolpidem
- Zopiclone
- Zaléplon
- Méprobamate
Indications
Benzodiazepines are a Anesthésiant of the anxious state. The anxious state is not pathological in oneself, it is a response of the organization to a situation of alarm in a very broad direction. The symptoms which are the consequence can be invalidating, and benzodiazepines by anaesthetizing this anxious state make it possible to decrease or remove whole or part of these symptoms. Benzodiazepines can in no way of treating the causes of the anxiety.The use of benzodiazepines as “Antidépresseur” is unsuited: on the simplified scale: depressive state -- normal state -- anxious state; benzodiazepines are located like a corrector of an anxious state and thus direct rather towards the depressive state. The english-speaking say that benzodiazepines are in particular “removing pressure from” (Dépresseur S).
Benzodiazepines are sometimes used also to cause a Amnésie at the time of procedures traumatisantes (for example Cardioversion S, intubation S, inspection).
Benzodiazepines are some times diverted for their effects Myorelaxant S by marksmen.
Side effects
- Hypotonia of the muscles of the throat being able to involve a gene of breathing,
- respiratory depression when they are managed by intravenous way and with strong amounts,
- Somnolence,
- turbid of the memory,
- confusion,
- falls.
The use of benzodiazepines is delicate because of the risks of dependence and tolerance. The installation of the dependence and/or the tolerance is very variable from one patient to another. The stop must be progressive and under medical supervision. The symptoms of weaning include/understand nervousness, irritability, syndrome of panic, Agoraphobie, Insomnie, muscular, turbid pains of the digestive system in particular turbid intestinal, etc
The correlation with the duration of the “treatment” and the appearance of symptoms of weaning would be strong. American disadvises a regulation over one duration of more than one month. In France, a benzodiazepine should not be prescribed more than three months the regular use of benzodiazepine is not effective any more after a few weeks in a few months.
Professor Edouard Zarifiant deplores the fact that these drugs “are distributed to the users who all are not inevitably reached of psychiatric disease, any time, anyhow and for anything”. According to him, the persons in charge of this situation in France are the doctors.
Weaning can be carried out in a rather short time, a few days the best cases, until a rather long time, several years. It is carried out via a progressive reduction in the benzodiazepine amount. The Anglo-Saxons set up groups “Tranx”, comparable with the groups of support for the Alcoolique S or the drug addicts.
Prolonged syndrome of weaning to benzodiazepines
At 10 to 15% of the patients, the demonstrations of weaning disappear only after several months, even several years. The principal symptoms of weaning of long life are the anguish, insomnia, the depression, various sensory and driving symptoms, of the gastro-intestinal disorders, as well as disorders of the memory and cognitive disorders. According to professor M. Lader. : Some of these groups of victims of tranquillizing can document on people who still have symptoms of weaning ten years after the stop. The prolonged syndrome of weaning to benzodiazepines is a iatrogenic disease.The studies anglosaxones show that approximately 50% of the dependant patients to benzodiazepines find their health after weaning. Approximately 25% note a very substantial benefit after weaning, although certain after-effects almost always psychological or neurological remain more or less present.
The frequency of appearance of a syndrome of weaning in the chronic benzodiazepine consumers ranges between 15 and 26%, but the frequencies increase with the seniority of the treatment (around 80% for treatments higher than 3 years).
Intoxication
More or less pronounced respiratory depression, it is antagonisable with the Flumazénil (Anexate). They are much surer than the Barbiturique S, the Méthaqualone or the anesthetic halogenous ones thanks to the existence of this antidote.
Legal statute
With the the United States, the Flunitrazépam (Rohypnol®) and the Bromazépam (Lexotan®) are Stupéfiant S and are not available.In Belgium, the benzodiazepine delivery is subjected to ordinance. The Flunitrazépam (Rohypnol®) is a regulated substance compared to the Stupéfiant S. Seule the form with 1 Mg is still authorized (that to 2 Mg is prohibited).
French regulation concerning the hypnotic ones and tranquillizing them: Stopped of October 7th, 1991 fixing the list of the substances of list I of the poisonous substances at hypnotic and/or anxiolytic properties of which the duration of regulation is reduced.
References
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