Diazepam

Диазепам Drug photo

The description is actual on 16.12.2014

  • Latin name: Diazepam
  • ATH code: N05BA01
  • Active ingredient: Diazepam (Diazepam)
  • Producer: Alkaloid (Macedonia)

Structure

Contains in 1 dragee mg diazepam 2 or 5, as excipients: monohydrate of lactose, potato starch, calcium stearate.

1 ampoule contains 2 ml of solution, the content of substance diazepam — 10 mg.

Release form

  • in a cardboard box in the blister containing 24 tablets;
  • ampoules release in blisters on 5 pieces — in one box 2 blisters.

Pharmacological action

Tranquilizing, myorelaxation (weakening skeletal muscles), gipnosedativny and anksiolitichesky action.

Pharmacodynamics and pharmacokinetics

Diazepam is a tranquilizer of a benzodiazepine row which is capable to exponentiate the central action γ - aminobutyric acid as the main brake mediator of TsNS, creating a component of supramolecular unit – a receptor complex бензодиазепин-γ-аминомаслянной acids – the chlorionophore which is placed on membranes of neurons. It possesses selective stimulation of effect of γ-aminobutyric acid of acid in a reticular formation of a brainstem that reduces excitement of a cerebral cortex, limbic system, a thalamus and hypothalamus. The myorelaxation effect is implemented on the brake mechanism of action on polisinaptichesky reflexes of a muscular tension.

Diazepam is characterized by dozozavisimy influence on TsNS: small doses (to 15 mg a day) render the stimulating effect while high (it is more than 15 mg) – sedative.

As for pharmacokinetics, oral administration causes absorption of 75% of a dose in a digestive tract, about 98% of diazepam contact plasma proteins, development of therapeutic effect happens for 2-7 day of a course of treatment.

The metabolism occurs in a liver where 99% of diazepam are transformed to the inactive and active metabolites capable to get through a gematoplatsentarny barrier and into breast milk. Drug in two phases mainly is excreted by kidneys (70%), to 10% it is removed with a stake. The elimination half-life at the first stage makes 3 hours, on the second – 48 hours.

Indications to use

Appoint at different neurosises, concern and alarm, a psychopathy, schizophrenia, sleeplessness and other sleep disorders, epilepsy, an abstinence syndrome at an alcoholism, a spastic state and a pruritic dermatosis, and also at miozita, a bursitis, arthritises which are followed by tension of skeletal muscles.

It can be used as a component of the combined anesthesia, for simplification of patrimonial activity, in case of premature births and at premature placental detachment, at tetanus.

Contraindications

Hypersensitivity to the making components of Diazepam and other benzodiazepines, and also at a liver and renal failure, the myasthenia expressed to a chronic hypercapnia, closed-angle glaucoma and during pregnancy.

Side effects

Diazepam can cause the following side effects:

Prolonged use can develop medicinal dependence, and also memory disturbance.

Diazepam, application instruction (Way and dosage)

Adults accept Diazepam in/in, in oil, rektalno (in) from 4 to 15 mg a day in two steps, at the same time the maximum daily dose can make no more than 60 mg and only in the conditions of a hospital.

To babies and children 6 months are more senior it is possible to take in a dose 0,1–0,8 mg on weight kg a day for 3–4 receptions.

The application instruction of Diazepam assumes intramuscular or intravenous administration on 10–20 mg multiple to the corresponding indications.

The single dose, frequency and duration of a course have to be established individually. Duration of a course has to be as little as possible, for example, treatment of sleeplessness should not exceed weeks, a condition of alarm — 8-12 weeks, assuming the periods of a gradual dose decline.

Overdose

The overestimated doses of Diazepam can cause development of paradoxical excitement, oppression of cordial/respiratory activity, an areflexia, an apnoea and even to whom.

There is a specific antidote — Flumazenil who on the mechanism is an antagonist of benzodiazepines.

Treatment: gastric lavage, enterosorbentny means, artificial ventilation of the lungs.

Interaction

At simultaneous use with:

  • Neuroleptics, sedative, hypnagogues, opioid analgetics — Diazepam strengthens oppression of TsNS, respiratory center and causes the expressed arterial hypotension.
  • Tricyclic antidepressants (including Amitriptyline) — increase of the oppressing effect on TsNS and cholinergic action, increase in concentration of antidepressants is possible.
  • Muscle relaxants — their action amplifies, however, the risk of development of an apnoea increases.
  • Oral contraceptives effects of Diazepam can amplify, increasing risk of development of bleeding of breakthrough type.
  • Bupivacaine, fluvoksaminy — increase of its concentration in a blood plasma is possible.
  • Diclofenac — strengthening of dizziness.
  • Isoniazid, Paracetamol — decrease in removal of Diazepam.
  • Carbamazepine, Phenytoinum, Rifampicin, Phenobarbital — removal and a metabolism of Diazepam accelerates.
  • Caffeine — reduction sedative and, perhaps, anksiolitichesky effect of Diazepam.
  • Clozapine — reactions of the expressed arterial hypotension, respiratory depression, a loss of consciousness are possible.
  • Levodopa — suppression of protivoparkinsonovy action.
  • Lity the carbonate — recorded a case of development of a coma.
  • Metoprolol — decrease in sight and deterioration in psychomotor reactions is possible.
  • Theophylline in small doses — a perversion of sedative effect of Diazepam.
  • Cimetidinum, Omeprazol, Disulfiramum — increase in duration of effect of Diazepam.
  • Ethanol — etanolsoderzhashchy drugs strengthen oppression of TsNS, generally influence on a respiratory center, emergence of a syndrome of pathological intoxication is possible.

Terms of sale

In the presence of the recipe.

Storage conditions

In the dry, protected from rays of light place, with ambient temperature 15–25 ° Celsius.

Period of validity

Three years.

Special instructions

During treatment by Diazepam alcohol intake is inadmissible.

Concerning driving by motor transport and controls of mechanisms – danger exists as drug can cause dizziness, hallucinations or the general delay of speed of a psychomotor system.

Synonyms

Apaurinum, Valium, Relanium, Relium, Seduxenum, Sibazonum.

Synonyms and analogs, generics are substitutes of drug, among them most of all enjoy popularity: Relanium, Giadazepam, Sibazonum and other drugs with active agents of a benzodiazepine row.

About Diazepam

Considering that independent administration of drug is categorically inadmissible, especially — in children's practice, About Diazepam are generally positive, and note its efficiency though many are disturbed by a big number of side effects and accustoming, and also rather difficult withdrawal.

The Diazepam price where to buy

The Diazepam price for 5 mg (20 pieces) makes 620 rubles. It is possible to buy Diazepam in Moscow, in advance having ordered in Internet drugstores, delivery with the courier — 500 rubles within MKAD without order cost within 2 hours.

Section: For a nervous system
in more detail

Education: Graduated from the Nikolaev national university of V. A. Sukhomlinsky, gained the diploma of the specialist with honors as "An embryologist, a cytologist, a histologist". Also, the human physiology and animals, the teacher of biology" graduated from a magistracy majoring in ". The course on discipline "Pharmacology" is with honors passable.

Experience: Worked as the senior laboratory assistant of department of Physiology and biochemistry of the Nikolaev national university of V. A. Sukhomlinsky in 2010 - 2011.

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