Diazepam (diazepam)
Anxiolytic remedy

Dosage form

Tablets.

Composition

1 tablet contains: Diazepam – 10mg.
Excipients: wheat starch, milk sugar, talc, polyvidone, silicon dioxide colloidal, stearic acid.

Pharmacological svoystvaPreparat refers to benzodiazepine tranquilizers. Has anxiolytic, central miorelaksiruyuschee, anticonvulsant, sedative and a moderate sedative effect. Increases the effects of sleeping pills, narcotic, neuroleptic, analgesic drugs, alcohol.

Pharmacodynamics

The mechanism of action of diazepam related to GABA, an inhibitory neurotransmitter in the CNS. It is known that GABA-ergic neurons inhibit activity of neurons of other types. The drug reduces the activity of the enzyme GABA transaminase, thereby increasing the content of GABA in the brain. On the other hand, increases the sensitivity of receptors to GABA. All this reinforces the inhibitory effect of GABA-ergic neurons in the neurons of other types. Sedative and hypnotic effect of diazepam and other benzodiazepines is associated with inhibition of noradrenergic and dopaminergic neurons. Anticonvulsants and miorelaksiruyuschee effect is due to inhibition of the neurons of the cortical centers and the spinal cord. Inhibition of excitatory processes in the ascending reticular formation leads to the development of anxiolytic effect.

Pharmacokinetics

The drug is well sucked after oral administration – 75%. Maximum plasma concentrations observed after 1-2 hours. 98% of the drug bound to plasma proteins. In the liver, 98-99% of diazepam is metabolized. Main metabolites – nordiazepam (blood plasma), oxazepam (in urine), and temazepam. In the form of glucuronides metabolites are allocated mainly in the urine, 10% – with feces, 0,5-2% – in the urine in unchanged form. The half-life from plasma of adults is 24-72 hours, in old age – 100 hours, the newborn – 31 hours, in infants – 8-14 hours. In acute hepatitis half-life in adults is prolonged to 2-4 days, and in liver cirrhosis – doubled. In case of poisoning diazepam hemodialysis ineffective.

Indications for use

Apply strictly prescribed by a doctor!

The drug is used in a variety of nervous and mental disorders: neuroses, personality disorder, neurosis and psihopodobnyh states in schizophrenia, with organic brain diseases, including those with cerebrovascular lesions, with somatic diseases, accompanied by signs of emotional stress, anxiety, fear, increased irritability, senestoipohondricheskimi and phobic disorders, sleep disorders.

The children are used with neurotic and neurosis-like states, soprovozhayuschihsya the above phenomena, as well as headaches, enuresis, mood disorders and behavior. Also used for relief of psychomotor agitation and agitation in these troubling diseases. The children are used with neurotic and neurosis-like states, accompanied by the above phenomena, as well as headaches, enuresis, mood disorders and behavior.

Diazepam is used to treat epilepsy convulsive paroxysms, mental equivalents. In connection with miorelaksiruyuschim action of the drug is also used in spastic conditions. In combination with other drugs diazepam for the treatment of abstinence syndrome in drug addicts and alcoholics. Can also be used for sedation and ataralgesia in combination with analgesics and other neurotropic drugs. In the clinic of internal diseases: psychosomatic disorders (hypertension, vascular spasm, etc.)

In dermatological practice is used in itching dermatoses. The drug reduces the nocturnal secretion of gastric juice, which may play an important role in appointing him as a calming and soporific patients with gastric ulcer and 12-ultradisperse intestine.

Contraindications

* Idiosyncrasy benzodiazepines;
* Severe myasthenia gravis;
* Acute poisoning by alcohol, hypnotics, analgesics, neuroleptics, antidepressants and lithium;
* Expressed by human liver and kidney;
* Pregnancy (1 term) and breastfeeding. Diazepam should not be used ambulatory persons working at height, transport drivers and others whose profession requires quick psychomotor reactions.

In the treatment of drug use of alcohol is strictly prohibited. With the sudden cancellation of diazepam after prolonged use may concern, excitement tremors, convulsions, sleep disorders. In this connection, the abolition of the drug should be made gradually.

Warnings

Diazepam is not recommended to appoint ambulatory patients involved in activities that require a high concentration of attention and speed of motor responses. With care given to patients with glaucoma!

Interaction with other drugs

In the application of diazepam with other drugs may occur following the reaction of:

* With monoamine oxidase inhibitors, strychnine and Corazol – antagonism against diazepam;
* With hypnotics, sedatives, narcotic analgesics, other tranquilizers, benzodiazepines, antidepressants, a sharp increase in action of diazepam;
* With antacid – may delay (but not decrease) intake of diazepam;
* Premedication with diazepam may decrease dose of fentanyl required for the induction of anesthesia and reduce time loss of consciousness;
* With cimetidine, disulfiram, erythromycin, as well as contraceptives and ekstrogensoderzhaschimi drugs, which inhibit the competitive metabolism in the liver (oxidation) – may slow the excretion of diazepam and its increased plasma levels;
* Dextropropoxyphene, isoniazid, ketoconazole, and metoprolol also slow down the metabolism of diazepam and increased its concentration in the blood plasma;
* Propranolol and valproic acid increase the level of diazepam in blood plasma;
* Rifamycin may increase excretion of diazepam and thus reduce its concentration in blood plasma.

Dosing and Administration

Is inside. Dose determined by the nature of the disease, the patient’s condition and individual sensitivity to the drug. Adults. The dose for adults is – 5-10 mg (1/2-1 tablets) 1-2 times a day. In some cases (when excessive excitement, fear, anxiety), a single dose can be increased to 20 mg (2 tablets). In the treatment in the hospital daily dose may be increased to 30-50 mg (3-5 tablets). The maximum daily dose is 60 mg (6 tablets), divided into 2-3 doses.

In elderly and debilitated patients are used to 5 mg (1 / 2 tablets) 2-3 times a day. Sleep disorders adult appoint 1/2-1 tablet before bedtime.

Children. Do not recommend use of the drug to children under 6 years. Children older than 6 years – 5 mg (1 / 2 tablets) 2 times a day. Older children, if necessary daily dose can be increased to 15 mg.

The drug should not be lifted simultaneously, the dose should be reduced gradually. Due to the possible development of drug dependence treatment should not proceed continuously for more than 1 month. Before re-treatment break – at least 3 weeks.

Side effects

In the course of treatment often complain of fatigue, sleepiness (especially strong in the early days), dizziness. In some cases, the treatment can be observed excitation.

Anticholinergic action of the drug can cause dry mouth, blurred vision, mydriasis, glaucoma, dysuria, constipation, galaktoreyu. Perhaps the development of aplastic anemia as a result of idiosyncrasy. Were noted rare cases of extrapyramidal effects, agranulocytosis, dyscrasia, jaundice, abnormal liver function.

With long-term use may be the development of drug dependence, memory impairment, menstrual cycle, decreased sex drive.

Overdose

Symptoms of overdose: marked drowsiness, disturbances of thinking, weakness, tremors, respiratory depression, slow heartbeat, shortness of breath or difficulty breathing, the suppression of motor and mental reactions until their disappearance, coma.

Treatment: gastric lavage is necessary, the introduction of activated charcoal, intravenous infusion of fluids, and monitoring of respiration, heart rate and blood pressure. Norepinephrine and dopamine cropped hypotension. Possible to conduct forced diuresis. In the presence of excitation should not be used barbiturates. Dialysis is of limited value. In stationary conditions can be used flumazenil – an antagonist of benzodiazepine receptors.

Product

Tablets 10 mg to 20 pieces in one package.

Storage

In dry, dark place at a temperature of 15-25 ° C. List B. Keep out of reach of children! Keep away from direct sunlight!

Expiration

3 years from the date of issue. Do not use after the date specified on the package.

Conditions of supply of pharmacies

Prescription.