Diazepam

Diazepam – a tranquilizer of anxiolytic, sedative, anticonvulsant, central myorelaxation action.

Form of release and structure

Drug is produced in the following dosage forms:

• Tablets: without cover, round, with the dividing line on one of the parties, white color (on 10 pieces in the blister, on 2 or 10 blisters in a cardboard box);
• Solution for injections: colourless transparent liquid (on 2 ml in dark glass ampoules, on 10 ampoules in a cardboard box).

Is a part of 1 tablet:

• Active ingredient: diazepam – 2, 5 or 10 mg;
• Auxiliary components: monohydrate of lactose, calcium stearate, K-25 povidone, potato starch.

Is a part of 1 ml of injection solution:

• Active ingredient: diazepam – 5 mg;
• Auxiliary component: benzyl alcohol (as the stabilizer).

Indications to use

States/diseases at which Diazepam use is recommended:

• Epileptic status;
• Sleep disorder, motor excitement of various etiology in psychiatry and neurology, an abstinence syndrome owing to an alcoholism;
• Neurosises, borderline cases with elements of tension, alarm, concern, fear;
• The spastic states connected with defeat back or a brain and also miozita, arthritises, bursitis with tension of skeletal muscles;
• Tetanus.

Diazepam is used at anesthesia for carrying out premedication before an anesthesia and/or as a component of the combined anesthesia.

In labor drug is shown for improvement of patrimonial activity, at premature delivery, and also in case of premature placental detachment.

Contraindications

• The expressed chronic hypercapnia;
• Heavy myasthenia;
• Alcohol or medicinal addiction in the anamnesis (except for acute abstinence);
• Hypersensitivity to drug components, and also other medicines of a benzodiazepine row.

In the I trimester of pregnancy use of Diazepam is contraindicated and is allowed only in urgent cases. It is important to consider that use of a tranquilizer at pregnancy can significantly change the heart rate (HR) of a fruit.

In obstetrics use of drug in the doses necessary for simplification of patrimonial activity, can cause a temporary hypomyotonia, a hypothermia, disturbance of breath in newborns (is more often at premature) as they did not completely create fermental system which participates in diazepam metabolism. For the same reason administration of drug is contraindicated to children up to 6 months.

If regular reception of means is necessary during a lactation, it is necessary to stop breastfeeding.

Route of administration and dosage

Diazepam, depending on a release form, is accepted inside, entered intramusculary, intravenously, rektalno.

The daily dose varies with the broad range of 0,5-60 mg. The single dose, frequency and duration of use are established individually.

Side effects

• Nervous system: drowsiness, muscular weakness, dizziness; seldom – a depression, confusion of consciousness, a vision disorder, a dysarthtia, a diplopia, a headache, an ataxy, a tremor; in isolated cases – paradoxical reactions (feeling of alarm, a hallucination, excitement, sleep disorders). After intravenous administration the hiccups can sometimes be observed. In case of prolonged use disturbances of memory and development of medicinal dependence are possible;
• Alimentary system: seldom – nausea, hypersalivation, dryness in a mouth, a lock; in isolated cases – jaundice, increase in activity of an alkaline phosphatase and transaminases in a blood plasma;
• Endocrine system: seldom – decrease or increase in a libido;
• Urinary system: seldom – an inkontinention (an urine incontience);
• Cardiovascular system: perhaps some lowering of arterial pressure at parenteral use;
• Respiratory system: in isolated cases – disturbances of breath at parenteral use;
• Allergic reactions: seldom – skin rashes.

Special instructions

It is necessary to observe extra care to patients with respiratory and heart failure, organic lesions of a brain (it is recommended to avoid parenteral administration), a myasthenia, closed-angle glaucoma and predisposition to it, and also it is long receiving anticoagulants, β-adrenoblockers, anti-hypertensive drugs of the central action, cardiac glycosides (it is preferential at the beginning of therapy).

At treatment cancellation the dose needs to be reduced gradually. In case of sudden cancellation of Diazepam after long use are possible: excitement, concern, spasms, tremor.

If during treatment development of paradoxical reactions, such as uneasiness is observed, acute excitement, hallucinations, sleep disorders, then Diazepam it is necessary to cancel.

After intramuscular injections increase in activity of enzyme of a kreatinfosfokinaza (KFK) in a blood plasma is possible, it should be considered when carrying out differential diagnosis of a myocardial infarction.

It is necessary to avoid intra arterial administration of solution.

To take alcohol during treatment it is inadmissible.

Because of ability of a tranquilizer to cause reduction in the rate of psychomotor reactions, patients who are engaged in potentially dangerous types of activity should show extra care.

Medicinal interaction

At simultaneous use of Diazepam with some medicines there can be following effects:

• Bupivacaine: increase in its concentration in a blood plasma is possible;
• Oral contraceptives: strengthening of effects of diazepam is probable; the risk of development of breakthrough bleeding is increased;
• Diclofenac: strengthening of dizziness is probable;
• Isoniazid: reduces diazepam removal;
• Caffeine: reduces sedative and probably anxiolytic influence of diazepam;
• Clozapine: respiratory depression, the expressed arterial hypotension, a loss of consciousness are possible;
• Rifampicin: increases diazepam removal as considerable is strengthened by his metabolism;
• Levodopa: decrease in protivoparkinsonichesky action is possible;
• The medicines exerting the oppressing impact on the central nervous system (CNS) (including neuroleptics, sedative, hypnagogues, opioid analgetics, anesthetics): the expressed arterial hypotension, and also the oppressing influence on TsNS and on a respiratory center increases;
• Lithium carbonate: there are data on coma development;
• Fluvoksamin: increases side effects and concentration in a diazepam blood plasma;
• Metoprolol: reduction in the rate of psychomotor reactions, deterioration in visual acuity are possible;
• Phenobarbital and Phenytoinum: diazepam metabolism acceleration is possible; in rare instances diazepam strengthens action and metabolism of Phenytoinum oppresses;
• Muscle relaxants: their action amplifies, the risk of developing of an apnoea increases;
• Paracetamol: reduction of removal of diazepam and its metabolite (dezmetildiazepam) is probable;
• The drugs causing induction of enzymes of a liver, including antiepileptic means (carbamazepine, Phenytoinum): are capable to accelerate diazepam removal;
• Risperidon: there are data on development of the malignant antipsychotic syndrome (MAS);
• Theophylline (in low doses): perverts sedative effect of diazepam;
• Tricyclic antidepressants (including with amitriptyline): increase in concentration of antidepressants and increase in cholinergic action, strengthening of their oppressing influence on TsNS is probable;
• Cimetidinum, омепразол, Disulfiramum: increase in intensity and duration of effect of diazepam is possible;
• Ethanol, etanolsoderzhashchy drugs: strengthen the oppressing influence on TsNS (preferential on a respiratory center), can cause a syndrome of pathological intoxication.

To patients who long time received β-adrenoblockers, anti-hypertensive drugs of the central action, anticoagulants, cardiac glycosides, it is impossible to predict mechanisms and extent of medicinal interaction.

Terms and storage conditions

To store in the place, dry, dark, unavailable to children, at a temperature not above 25 °C.

Period of validity – 3 years.