Valium is a drug of the benzodiazepine group that has found wide application in medical practice. The drug has a sedative, hypnotic, anti-anxiety, anticonvulsant, muscle relaxant and amnestic action.
Other names: Diazepam
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Anxiolytic of the benzodiazepine group, has an anxiolytic, sedative, muscle relaxant, anticonvulsant effect. Anxiolytic action is associated with increased GABAergic inhibition in the central nervous system. The GABAA receptor-C1~ channel complex contains a benzodiazepine receptor, stimulation of which leads to conformational changes in the GABAA receptor, resulting in an increase in its sensitivity to GABA. This leads to an increase in the permeability of the GABAA receptor channel for chloride ions. The entry of negatively charged chloride ions into the neuron leads to membrane hyperpolarization and inhibition of neuronal activity.
The anticonvulsant effect of diazepam is associated with the inhibition of epileptogenic activity due to the enhancement of inhibitory GABAergic processes in the central nervous system.
The muscle relaxant effect is associated with the inhibition of spinal polysynaptic reflexes and a violation of their supraspinal regulation.
In small doses, it has a sedative effect, with an increase - a hypnotic effect.
With prolonged use, drug dependence is formed. After the end of taking the drug, manifestations of the withdrawal syndrome are possible.
After ingestion on an empty stomach, up to 75% is absorbed in the gastrointestinal tract. The maximum plasma concentration is reached after 90 minutes. Communication with plasma proteins is 98%. deposited in adipose tissue. Penetrates through the blood-brain and placental barrier, enters breast milk.
Metabolism in the liver with the formation of active metabolites (desmethyldiazepam) with a half-life of 40 to 200 hours.
The half-life is 24-48 hours. Elimination of the drug by the kidneys.
It is used for neurosis-like and neurotic conditions, accompanied by fear and anxiety. It is used for sedation before surgery and for induction into anesthesia. It is used to relieve status epilepticus and in diseases manifested by increased muscle tone: epilepsy, schizophrenia, psychopathic agitation, specific personality disorders, insomnia.
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Hypersensitivity to the drug, coma, shock, acute alcohol intoxication with a weakening of vital functions, acute intoxication of drugs that have a depressing effect on the central nervous system (including narcotic analgesics and hypnotic drugs), myasthenia gravis, angle-closure glaucoma (acute attack or predisposition); severe COPD (danger of progression of the degree of respiratory failure), acute respiratory failure, absence or Lennox-Gastaut syndrome (with intravenous administration contributes to the onset of tonic status epilepticus), pregnancy (especially the first trimester), lactation, children under 6 months of age (with ingestion), up to 30 days inclusive (with i / m and / in the introduction).
With caution. History of epilepsy or epileptic seizures (initiation of treatment or its abrupt withdrawal may accelerate the development of seizures or status epilepticus), hepatic and / or renal failure, cerebral and spinal ataxia, hyperkinesis, history of drug dependence, tendency to abuse psychoactive drugs, organic diseases of the brain brain, hypoproteinemia, sleep apnea (established or suspected), old age.
As an anxiolytic drug, it is prescribed orally, 2.5-10 mg 2-4 times a day.
Psychiatry: with neurosis, hysterical or hypochondriacal reactions, dysphoria of various origins, phobias - 5-10 mg 2-3 times a day. If necessary, the dose can be increased to 60 mg / day. With alcohol withdrawal syndrome - 10 mg 3-4 times a day for the first 24 hours, followed by a decrease to 5 mg 3-4 times a day. Elderly, debilitated patients, as well as patients with atherosclerosis at the beginning of treatment - orally, 2 mg 2 times a day, if necessary, increase until the optimal effect is obtained. Working patients are recommended to take 2.5 mg 1-2 times a day or 5 mg (basic dose) in the evening.
Neurology: spastic conditions of central origin in degenerative neurological diseases - orally, 5-10 mg 2-3 times a day.
Cardiology and rheumatology: angina - 2-5 mg 2-3 times a day; arterial hypertension - 2-5 mg 2-3 times a day, vertebral syndrome in bed rest - 10 mg 4 times a day; as an additional drug in physiotherapy for rheumatic pelvis spondyloarthritis, progressive chronic polyarthritis, arthrosis - 5 mg 1-4 times a day. As part of the complex therapy of myocardial infarction: initial dose - 10 mg / m, then inside, 5-10 mg 1-3 times a day; premedication in case of defibrillation - 10-30 mg IV slowly (in separate doses); spastic conditions of rheumatic origin, vertebral syndrome - the initial dose of 10 mg / m, then inside, 5 mg 1-4 times a day.
Anesthesiology, surgery: premedication - on the eve of surgery, in the evening - 10-20 mg orally; preparation for surgery - 1 hour before the start of anesthesia in / m for adults - 10-20 mg, for children - 2.5-10 mg; introduction to anesthesia - in / in 0.2-0.5 mg / kg; for a short-term narcotic sleep during complex diagnostic and therapeutic interventions in therapy and surgery - in / in adults - 10-30 mg, children - 0.1-0.2 mg / kg.
Pediatrics: psychosomatic and reactive disorders, spastic states of central origin - are prescribed with a gradual increase in dose (starting with low doses and slowly increasing them to the optimal dose well tolerated by the patient), daily dose (can be divided into 2-3 doses, with the main dose the largest dose, taken in the evening): inside, it is not recommended to use up to 6 months, from 6 months and older - 1-2.5 mg, or 40-200 mcg / kg, or 1.17-6 mg / sq.m, 3- 4 times a day.
For elderly and senile patients treatment should begin with half the usual adult dose, gradually increasing it, depending on the effect achieved and tolerability. Parenterally, in case of anxiety, it is administered intravenously at an initial dose of 0.1-0.2 mg / kg, injections are repeated every 8 hours until the symptoms disappear, then they switch to oral administration.
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Most often - lethargy, drowsiness and muscle weakness (usually depends on the dose); rarely - confusion, constipation, depression, dullness of emotions, decreased attention, diplopia, dysarthria, headache, arterial hypotension, urinary incontinence, increased or decreased sexual desire, nausea, xerostomia or increased salivation, skin rash, slurred speech, tremor, delay urine, headache, dizziness, blurred vision; very rarely - increased activity of transaminases and alkaline phosphatase, as well as jaundice.
Paradoxical reactions such as acute agitation, anxiety, sleep disturbances, and hallucinations have been described; when they appear, diazepam should be discontinued. With parenteral use - thrombosis and thrombophlebitis, local irritation (especially after rapid intravenous administration). Diazepam solution should not be injected into very small veins; it is unacceptable to / and the introduction and ingress of the solution into the adjacent tissues. IM injections may be accompanied by soreness and erythema.
Symptoms: drowsiness, confusion, paradoxical arousal, decreased reflexes, areflexia, stupor, reduced response to painful stimuli, deep sleep, dysarthria, ataxia, visual disturbance (nystagmus), tremor, bradycardia, shortness of breath or shortness of breath, apnea, severe weakness, decrease in blood pressure, collapse, depression of cardiac and respiratory activity, coma.
Treatment: gastric lavage, forced diuresis, activated charcoal. Symptomatic therapy (maintenance of breathing and blood pressure), mechanical ventilation. Flumazenil is used as a specific antagonist (in a hospital setting). Hemodialysis is ineffective.
Enhances the inhibitory effect on the central nervous system of ethanol, sedative and antipsychotic drugs (neuroleptics), antidepressants, narcotic analgesics, drugs for general anesthesia, muscle relaxants.
Inhibitors of microsomal oxidation (including cimetidine, oral contraceptives, erythromycin, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, propranolol, propoxyphene, valproic acid) lengthen T1 / 2 and enhance the action of diazepam.
Inducers of microsomal liver enzymes reduce the effectiveness.
Narcotic analgesics increase euphoria, leading to an increase in psychological dependence.
Antacids reduce the rate of absorption of diazepam from the gastrointestinal tract, but not its completeness.
Antihypertensive drugs may increase the severity of lowering blood pressure.
Against the background of the simultaneous appointment of clozapine, it is possible to increase respiratory depression.
With simultaneous use with low-polarity cardiac glycosides, an increase in the concentration of the latter in the blood serum and the development of digitalis intoxication (as a result of competition for binding to plasma proteins) is possible.
Reduces the effectiveness of levodopa in patients with parkinsonism.
Omeprazole prolongs the elimination time of diazepam.
MAO inhibitors, analeptics, psychostimulants - reduce activity.
Premedication with Valium reduces the dose of fentanyl required for induction of general anesthesia and reduces the time required to "turn off" consciousness with induction doses.
May increase zidovudine toxicity.
Rifampin may increase the excretion of diazepam and decrease its plasma concentrations.
Theophylline (used in low doses) can reduce or even reverse the sedative effect.
In the process of treatment, patients are strictly prohibited from using ethanol.
In case of renal / hepatic insufficiency and long-term treatment, it is necessary to control the pattern of peripheral blood and "liver" enzymes.
The risk of developing drug dependence increases with the use of large doses, a significant duration of treatment, in patients who have previously abused ethanol or drugs. Without special instructions should not be used for a long time.
It is unacceptable to abruptly stop treatment due to the risk of "withdrawal" syndrome (headache, myalgia, anxiety, tension, confusion, irritability; in severe cases, derealization, depersonalization, hyperacusis, photophobia, tactile hypersensitivity, paresthesias in the extremities, hallucinations and epileptic seizures), however, due to the slow T1 / 2 of diazepam, its manifestation is much weaker than that of other benzodiazepines.
If patients experience such unusual reactions as increased aggressiveness, acute states of arousal, anxiety, fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, superficial sleep, treatment should be discontinued.
The initiation of treatment or its abrupt withdrawal in patients with epilepsy or with a history of epileptic seizures may accelerate the development of seizures or status epilepticus.
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