Medication

Diazepam

Structure

1 tablet contains diazepam2 or 5 mg, as auxiliary substances: lactose monohydrate, potato starch, calcium stearate.

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

Release form

  • in a cardboard box in a blister containing 24 tablets;
  • ampoules are produced in blisters of 5 pieces - in one box 2 blisters.

Pharmachologic effect

Tranquilizing, muscle relaxant (relaxing skeletal muscles), hypnosedative and anxiolytic effects.

Pharmacodynamics and pharmacokinetics

Diazepam is tranquilizer benzodiazepine serieswhich is able to potentiate the central action γ-aminobutyric acidas the main inhibitory mediator of the central nervous system, forming a component of the supramolecular unit - the benzodiazepine-γ-aminobutyric acid receptor complex - chlorionophorelocated on the membranes of neurons. It has selective stimulation of the action of γ-aminobutyric acid in the reticular formation of the brain stem, which reduces the excitation of the cerebral cortex, limbic system, thalamus and hypothalamus. The muscle relaxant effect is realized by the inhibitory mechanism of action on polysynaptic reflexes of muscle tension.

Diazepam is characterized by a dose-dependent effect on the central nervous system: small doses (up to 15 mg per day) have a stimulating effect, while high doses (more than 15 mg) have a sedative effect.

With regard to pharmacokinetics, oral administration causes absorption of 75% of the dose in the digestive tract, approximately 98% diazepam binds to proteins plasma, the development of a therapeutic effect occurs on the 2nd-7th day of a course of treatment.

Metabolism occurs in the liver where 99% diazepamconverts to inactive and active metabolitesable to penetrate the hematoplacental barrier and into breast milk. The drug is excreted in two phases mainly by the kidneys (70%), up to 10% is excreted in the feces. The elimination half-life at the first stage is 3 hours, at the second - 48 hours.

Indications for use

Assign with various kinds neuroses, concern and anxiety, psychopathy, schizophrenia, insomnia and others violations sleep, epilepsy, withdrawal syndrome in chronic alcoholism, spastic condition and itchy dermatosesas well as myositis, bursitis, arthritisaccompanied by stress skeletal muscle.

It can be used as a component of combined anesthesia, to facilitate labor, in case of premature birth and with premature placental abruptionat tetanus.

Contraindications

Hypersensitivity to the components of Diazepam and others benzodiazepinesas well as liver and kidney failure, myasthenia gravissevere hypercapnia, angle-closure glaucoma and during pregnancy.

Side effects

Diazepam may cause the following side effects:

  • dizziness;
  • hallucinations;
  • drowsiness;
  • slow reaction;
  • depression of mental and motor activity;
  • muscle weakness or ataxia;
  • dry mouth
  • dyspepsia (violation of the normal functioning of the stomach);
  • nausea;
  • diarrhea;
  • dyspnea(dyspnea);
  • urinary incontinence;
  • bronchospasm;
  • galactorrhea(pathological spontaneous secretion by the mammary glands and expiration of milk);
  • hyperprolactinemia;
  • increase or decrease in libido;
  • allergic reactions.

Long-term use may develop drug addiction, as well as impaired memory.

Diazepam, instructions for use (method and dosage)

Adults take Diazepam IV, IM, rectally (inside) from 4 to 15 mg per day in two divided doses, with a maximum daily dose of not more than 60 mg and only in a hospital setting.

Breasts and children over 6 months of age can be taken in a dose of 0.1-0.8 mg per kg of body weight per day for 3-4 doses.

Instructions for use of diazepam involves intramuscular or intravenous administration of 10-20 mg multiple of the corresponding indications.

A single dose, frequency and duration of the course should be established individually. The duration of the course should be as short as possible, for example, treatment insomniashould not exceed a week, anxiety - 8-12 weeks, suggesting periods of gradual dose reduction.

Overdose

High doses of diazepam may cause development paradoxical arousaldepression of cardiac / respiratory activity, areflexia, apnea and even to whom.

There is a specific antidote - Flumazenil, which by mechanism is an antagonist of benzodiazepines.

Treatment: gastric lavage, enterosorbent agents, mechanical ventilation.

Interaction

With simultaneous use with:

  • Antipsychotics, sedatives, sleeping pills, opioid analgesics - Diazepam enhances the depression of the central nervous system, respiratory center and causes severe arterial hypotension.
  • Tricyclic antidepressants(including Amitriptyline) - it is possible to increase the inhibitory effect on the central nervous system and cholinergic action, an increase in concentration antidepressants.
  • Muscle relaxants- their effect intensifies, however, the risk of development increases apnea.
  • Oral contraceptives the effects of diazepam may be enhanced, increasing the risk of developing bleeding breakthrough type.
  • Bupivacaine, fluvoxamine- It is possible to increase its concentration in blood plasma.
  • Diclofenac - gain dizziness.
  • Isoniazid, Paracetamol - reduced elimination of diazepam.
  • Carbamazepine, Phenytoin, Rifampicin, Phenobarbital- The elimination and metabolism of diazepam is accelerated.
  • Caffeine- a decrease in the sedative and possibly anxiolytic effects of diazepam.
  • Clozapine - reactions of severe arterial hypotension, respiratory depression, loss of consciousness are possible.
  • Levodopa- suppression of antiparkinson action.
  • Lithium carbonate - a case of development is recorded coma.
  • Metoprolol - Possible decreased vision and worsening of psychomotor reactions.
  • Theophyllinein small doses - a perversion of the sedative effect of Diazepam.
  • Cimetidine, Omeprazole, Disulfiram - an increase in the duration of diazepam.
  • Ethanol - ethanol-containing drugs increase central nervous system depression, mainly the effect on the respiratory center, the occurrence of pathological intoxication syndrome.

Terms of sale

In the presence of a prescription.

Storage conditions

In a dry place protected from light rays, with an ambient temperature of 15-25 ° Celsius.

Shelf life

Three years.

Special instructions

During the period of treatment with diazepam, it is unacceptable to use of alcohol.

Regarding driving and operating machinery - there is a danger, since the drug can cause dizziness, hallucinations or general slowdown in psychomotor speed.

Synonyms

Apaurin, Valium, Relanium, Relium, Seduxen, Sibazon.

During pregnancy and lactation

It is not recommended to use Diazepam in the first trimester of pregnancy, the exception is an extreme need, since the drug can significantly change the fetal heart rate. The course of admission at breastfeeding should be discontinued.

Diazepam Analogs

Matches for ATX Level 4 code:BromazepamHelexRudotelReliumNozepamTazepamXanaxEleniumValium RocheAlprazolamTofisopamGrandaxinMezapamSibazonSeduxenRelaniumLorazepam

Synonyms and analogues, generics are substitutes for the drug, among them they are most popular: Relanium, Hyadazepam, Sibazon and other drugs with active substances of the benzodiazepine series.

Diazepam Reviews

Given that self-administration of the drug is categorically unacceptable, especially in pediatric practice, reviews of Diazepam are mostly positive, and note its effectiveness, although many are worried about a large number of side effects and addiction, as well as a fairly complex withdrawal syndrome.

Diazepam price where to buy

The price of Diazepam for 5 mg (20 pcs.) Is 620 rubles. You can buy Diazepam in Moscow by pre-ordering in online pharmacies, delivery by courier - 500 rubles within the Moscow Ring Road, excluding the cost of the order within 2 hours.

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