Diazepam is a drug of the benzodiazepine group, which has been widely used in medical practice. The drug has sedative, hypnotic , anti-anxiety, anticonvulsant, muscle relaxant and amnestic effects. Enhances the effect of sleeping pills, narcotic, antipsychotic, analgesic drugs, alcohol. Taking diazepam for a long time can lead to drug dependence .
| Diazepam | |
|---|---|
| Diazepam | |
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| Chemical compound | |
| IUPAC | 7-chloro-1-methyl-5-phenyl-1,3-dihydro-2 H -1,4-benzodiazepin-2-one |
| Gross formula | C 16 H 13 ClN 2 O |
| Molar mass | 284.7 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| ATX | |
| Pharmacokinetics | |
| Bioavailable | 93% |
| The half-life. | 20-36 hours |
| Dosage Forms | |
| dragees, solution for intravenous and intramuscular administration, tablets, coated tablets | |
| Route of administration | |
| , , and | |
| Other names | |
| Apaurin, Assival, Valium, Relanium, Relium, Seduxen, Sibazon, Bruzepam. | |
Diazepam is part of the WHO list of essential medicines that defines the minimum set of medicines needed in the health system. The drug is used, in particular, for the treatment of anxiety , insomnia , epileptic seizures, muscle cramps , alcohol addiction . In preparation for certain medical procedures, such as endoscopy , diazepam is used to calm the patient or for anesthesia.
Content
Properties
Fine crystalline powder, white or white with a slight yellowish tint, is practically insoluble in water, and it is difficult to dissolve in alcohol. The drug and its main metabolites are excreted mainly in the urine.
Application
Diazepam is prescribed for various neuropsychiatric diseases: neuroses , personality disorders (psychopathies), as well as for neurosis-like and psychopathic conditions, for schizophrenia , organic brain lesions, including cerebrovascular diseases , for somatic diseases accompanied by signs of emotional stress, anxiety , fear, increased irritability, senesto - hypochondriac , obsessive and phobic disorders, with sleep disorders. It is also used to stop psychomotor agitation and anxiety agitation in these diseases.
It has a general anxiolytic (anti-anxiety) effect, which manifests itself in relieving emotional stress, suppressing feelings of anxiety , anxiety and fear [1] .
In children's psychoneurological practice, diazepam is prescribed for neurotic and neurosis-like conditions, accompanied by the above phenomena, as well as headaches, enuresis , mood and behavior disorders.
Diazepam is used for epilepsy to treat convulsive paroxysms , mental equivalents, and to stop epileptic status. In connection with the muscle relaxant effect, the drug is also used for various spastic conditions.
In combination with other drugs, diazepam is prescribed for the treatment of withdrawal syndrome in alcoholism.
In anesthetic practice is used for preoperative preparation of patients.
In dermatological practice, it is used for pruritic dermatoses .
The drug reduces the nighttime secretion of gastric juice, which can play an important role in appointing it as a sedative and sleeping pill for patients with gastric ulcer.
The drug also has an antiarrhythmic effect.
Diazepam is used for premedication and ataralgesia before endoscopy and surgery in combination with analgesics and other neurotropic drugs .
Diazepam is a component of the sleeping pill drug reladorm (see Cyclobarbital ).
Diazepam is administered orally, intravenously or intramuscularly. Sedation is observed within a few minutes after intravenous and 30-40 minutes after intramuscular injection of diazepam, therapeutic effect - after 3-10 days. After removing the acute manifestations of the disease, diazepam is prescribed orally.
Possible complications, contraindications and precautions are basically the same as for chlozepide . With intravenous administration of a diazepam solution, local inflammatory processes can be observed, in connection with which it is recommended to change the injection site. Diazepam has a teratogenic effect : when used during pregnancy, the fetus may develop hypothermia , hypotension , bifurcation and anomalies of the limbs [2] ; possible depression of the central nervous system in the fetus (lasting up to several days), respiratory depression, apnea , risk of aspiration, increased jaundice . A single dose of a low dose of diazepam (up to 20 mg) is harmless to the fetus, but with large doses and with repeated administration of the drug, a toxic effect may develop [3] .
Interaction
With the simultaneous use of diazepam with some other psychotropic or antispasmodic drugs (drugs for anesthesia , barbiturates , phenothiazines , analgesics , ethanol ), the effect of diazepam is enhanced . With the simultaneous use of diazepam with muscle relaxants , the risk of apnea increases.
Diazepam potentiates the effect of analgesics , antihypertensive drugs , muscle relaxants, tricyclic antidepressants , drugs that depress the central nervous system , antiepileptic drugs ; when combined with alcohol-containing drugs, the inhibitory effect on the central nervous system is enhanced [3] .
MAO inhibitors , respiratory analeptics , psychostimulants reduce the activity of diazepam [3] .
With prolonged use of cimetidine or omeprazole, the clearance of diazepam decreases. Drugs that cause induction of liver enzymes, including antiepileptic drugs ( carbamazepine , phenytoin ), can accelerate the elimination of diazepam.
Diazepam solution is incompatible in the same syringe with any other drugs (sediment formation is possible).
Non-medical use
Due to the relative availability of diazepam (despite the prescription of the medicine), drug addicts very often use this drug along with tramadol ( tramal retard ), when withdrawal symptoms develop, to stop “breaking”. In addition, it is taken to exclude cases of epileptic seizures caused by the use of large doses (over 400 mg) of tramadol - containing drugs.
People with alcoholism often use diazepam to enhance the effects of ethanol on their bodies.
Legal Status
Since August 1, 2013, diazepam has been included in Schedule III of psychotropic substances , the circulation of which in the Russian Federation is limited and for which the exclusion of certain control measures is allowed. Previously, he was on the list of potent substances.
In the United States, diazepam is controlled as a Schedule IV substance, in accordance with the 1970 Controlled Substances Act.
Diazepam is a Schedule IV drug in the UN Convention on Psychotropic Substances .
History
The drug was invented by Leo Sternbach from Hoffman-La Roche . It appeared on the market in 1963 and immediately gained great popularity. From 1969 to 1982, diazepam had the largest sales of all pharmaceutical products in America. In 1978, its record amount was sold - 2.3 billion tablets. The drugs of the benzodiazipam group were widely used for non-medical purposes: according to 2011 studies, there were 28.7% of them. By this indicator, they are second only to opiates. For example, in Sweden in 26% of cases of drunk driving in the blood of drivers diazepam was found, and in Northern Ireland this figure reached 87%. [four]
Notes
- ↑ Mashkovsky M.D. Medicines. - 16th ed. - M .: New Wave, 2012 .-- S. 78. - 1216 p. - ISBN 978-5-7864-0218-7 .
- ↑ Chapter 5. Medicine and age. 4.1. Pregnancy and drugs // Zmushko E.I., Belozerov E.S. Medical complications . - St. Petersburg: Peter, 2001 .-- 448 p. - (Quick Reference). - 3000 copies. - ISBN 5-272-00168-0 .
- ↑ 1 2 3 Drug Interactions and Pharmacotherapy Effectiveness / L. V. Derimedved, I. M. Pertsev, E. V. Shuvanova, I. A. Zupanets, V. N. Khomenko; under the editorship of prof. I. M. Pertseva. - Kharkov: Publishing house "Megapolis", 2001. - 784 p. - 5,000 copies. - ISBN 996-96421-0-X.
- ↑ Diazepam (Valium) [LifeBio.wiki ] . lifebio.wiki. Date of treatment December 20, 2018.