Sibazonum

General characteristics. Structure:

Active ingredient: 5 mg of diazepam.

Excipients: lactose (sugar milk), potato starch, calcium stearate.

The drug rendering anxiolytic, antiarrhytmic, myorelaxation, moderate and somnolent, spasmolytic, exponential and anticonvulsant action.

Pharmacological properties:

Pharmacodynamics. Tranquilizer, derivative benzodiazepine. Renders anxiolytic, sedative, anticonvulsant, central myorelaxation action. The mechanism of action is connected with strengthening of brake influence of GABA in TsNS. Myorelaxation action is caused also by inhibition of spinal reflexes. Can cause anticholinergic effect.

Pharmacokinetics. Absorption is bystry. Cmax in plasma is noted in 90 min. Linkng with proteins of plasma makes 98%. Gets through a placental barrier, into cerebrospinal fluid, it is allocated with breast milk. It is metabolized in a liver. It is removed by kidneys - 70%.

Indications to use:

Neurosises, borderline cases with the phenomena of tension, concern, alarm, fear; sleep disorders, motive excitement of various etiology in neurology and psychiatry, an abstinence syndrome at an alcoholism; the spastic states connected with damage of a head or spinal cord, and also a miozita, the bursitis, arthritises which are followed by tension of skeletal muscles; epileptic status; premedication before an anesthesia; as a component of the combined anesthesia; simplification of patrimonial activity, premature birth, premature placental detachment, tetanus.

Route of administration and doses:

Accept inside, enter in oil, in/in, rektalno. The daily dose varies from 500 mkg to 60 mg. The single dose, frequency and duration of use are established individually.

Features of use:

With extra care apply at patients with heart and respiratory failure, organic changes of a brain (in such cases it is recommended to avoid parenteral administration of diazepam), at closed-angle glaucoma and predisposition to it, at a myasthenia.

Extra care at diazepam use is required, especially in an initiation of treatment, from patients, it is long receiving anti-hypertensive drugs of the central action, beta adrenoblockers, anticoagulants, cardiac glycosides.

At therapy cancellation the dose should be reduced gradually. At sudden cancellation of diazepam after prolonged use the concern, excitement, a tremor, spasms are possible.

Diazepam should be cancelled at development of paradoxical reactions (acute excitement, uneasiness, sleep disorders and hallucinations).

After an injection of diazepam in oil increase in activity of KFK in a blood plasma is possible (that should be considered at differential diagnosis of a myocardial infarction).

To avoid in / and introductions.

During treatment not to allow alcohol intake.

Influence on ability to driving of motor transport and to control of mechanisms

Diazepam can cause delay of speed of psychomotor reactions that should be considered to the patients who are engaged in potentially dangerous types of activity.

It is not necessary to apply diazepam in the I trimester of pregnancy, except for emergency cases. It must be kept in mind that at use of diazepam at pregnancy perhaps essential change of ChSS of a fruit.

At use in obstetrics in the doses recommended for simplification of childbirth at newborns, is more often at premature, the temporary hypomyotonia, a hypothermia, breath disturbance are possible.

At regular inclusion in the lactation period breastfeeding should be stopped.

It is necessary to avoid use of diazepam for newborns as at them the fermental system participating in diazepam metabolism was not completely created.

Side effects:

From a nervous system: drowsiness, dizziness, muscular weakness; seldom - confusion of consciousness, a depression, vision disorders, a diplopia, a dysarthtia, a headache, a tremor, an ataxy; in isolated cases - paradoxical reactions: excitement, feeling of alarm, sleep disorder, hallucination. Later in/in introductions the hiccups is sometimes observed. At prolonged use development of medicinal dependence, memory disturbance is possible.

From the alimentary system: seldom - a lock, nausea, dryness in a mouth, hypersalivation; in isolated cases - increase in activity of transaminases and ShchF in a blood plasma, jaundice.

From endocrine system: seldom - increase or decrease in a libido.

From an urinary system: seldom - an urine incontience.

From cardiovascular system: at parenteral use perhaps some decrease in the ABP.

From respiratory system: at parenteral use in isolated cases - breath disturbances.

Allergic reactions: seldom - skin rash.

Interaction with other medicines:

At simultaneous use with the medicines exerting the oppressing impact on TsNS (including with neuroleptics, sedative, hypnagogues, opioid analgetics, anesthetics), the oppressing influence on TsNS, on a respiratory center, the expressed arterial hypotension amplifies.

At simultaneous use with tricyclic antidepressants (including with amitriptyline) strengthening of the oppressing influence on TsNS, increase in concentration of antidepressants and strengthening of cholinergic action is possible.

At patients, it is long receiving anti-hypertensive drugs of the central action, beta adrenoblockers, anticoagulants, cardiac glycosides, degree and mechanisms of medicinal interaction are unpredictable.

At simultaneous use with muscle relaxants action of muscle relaxants amplifies, increases risk of developing of an apnoea.

At simultaneous use with oral contraceptives strengthening of effects of diazepam is possible. The risk of development of breakthrough bleeding increases.

At simultaneous use with bupivacaine increase in concentration of bupivacaine in a blood plasma is possible; with diclofenac - strengthening of dizziness is possible; with an isoniazid - reduction of removal of diazepam from an organism.

The drugs causing induction of enzymes of a liver, including antiepileptic means (carbamazepine, Phenytoinum) can accelerate diazepam removal.

At simultaneous use with caffeine anxiolytic effect of diazepam decreases sedative and, perhaps.

At simultaneous use with clozapine are possible the expressed arterial hypotension, respiratory depression, a loss of consciousness; with a levodopa - suppression of protivoparkinsonichesky action is possible; from lithium the carbonate - described a coma development case; with metoprololy - decrease in visual acuity, deterioration in psychomotor reactions are possible.

At simultaneous use with paracetamol reduction of removal of diazepam and its metabolite (dezmetildiazepam) is possible; with risperidony - cases of development of ZNS are described.

At simultaneous use with rifampicin removal of diazepam owing to considerable strengthening of his metabolism under the influence of rifampicin increases.

Theophylline in low doses, perverts sedative effect of diazepam.

At simultaneous use in rare instances diazepam suppresses metabolism and strengthens action of Phenytoinum. Phenobarbital and Phenytoinum can accelerate diazepam metabolism.

At simultaneous use флувоксамин increases concentration in a blood plasma and side effects of diazepam.

At simultaneous use with Cimetidinum, omeprazoly, Disulfiramum increase in intensity and duration of effect of diazepam is possible.

At a concomitant use of ethanol, etanolsoderzhashchy drugs the oppressing influence on TsNS amplifies (mainly on a respiratory center), and also there can be a syndrome of pathological intoxication.

Contraindications:

Heavy myasthenia, the expressed chronic hypercapnia. Instructions in the anamnesis on alcohol or medicinal addiction (except acute abstinence). Hypersensitivity to diazepam and other benzodiazepines.

Overdose:

Symptoms: drowsiness, oppression of consciousness of various stepenityazhesta, paradoxical excitement, decrease in reflexes to an areflexia, reduced reaction to pain stimulations, a dysarthtia, an ataxy, a vision disorder (nystagmus), a tremor, bradycardia, decrease in the ABP, a collapse, oppression cordial idykhatelny (up to an apnoea) activity, a lump.

Treatment: artificial diuresis, symptomatic therapy (maintenance of breath and ABP), artificial ventilation of the lungs. In the kachestvespetsifichesky antagonist use flumazenit (in the conditions of a hospital). The hemodialysis – is ineffective. The antagonist of benzodiazepines flumazenit not pokazanbolny epilepsy which received treatment by benzodiazepines. At such bolnykhantagonistichesky action in relation to benzodiazepines can sprovotsirovatrazvity epileptic seizures.

Storage conditions:

The list III of the list of the drugs, psychotropic substances and their precursors which are subject to control in the Russian Federation. To store in the unavailable to children, protected from light place, at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

20 pieces - banks of dark glass (1) - a pack cardboard.
20 pieces - banks polymeric (1) - packs cardboard.
20 pieces - planimetric strip packagings (1) - packs cardboard.