Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Tranquilizer from the benzodiazepine group. Has anxiolytic, sedative, hypnotic, anticonvulsant, central muscle relaxant effect. The mechanism of action is associated with increased inhibitory effect of GABA in the central nervous system by increasing the sensitivity of GABA receptors to the mediator as a result of stimulation of benzodiazepine receptors.
PHARMACOKINETICS
After ingestion, chlordiazepoxide is almost completely absorbed from the digestive tract. After the / m introduction, the absorption is slow.
The binding with plasma proteins is high - about 96%.
Chlordiazepoxide penetrates the BBB, is excreted in breast milk, penetrates the placental barrier.
Metabolized with the formation of pharmacologically active metabolites of desmethyldiazepam, desmethylchlorodiazepoxide, demoxepam and oxazepam.
T 1/2 of chlordiazepoxide is variable and is 5-30 h, T 1/2 of the main active metabolite (desmethyldiazepam) is several days. It is excreted in the urine in unchanged form and in the form of conjugated metabolites.
INDICATIONS
Neuroses, sleep disorders, nervous tension, anxiety, irritability, reactive depression, withdrawal syndrome, convulsive state or its threat, NDC, climacteric syndrome, premenstrual tension syndrome, to prepare for surgery.
DOSING MODE
When administered to adults - 5-10 mg 2-4 times / day. In conditions of stress and anxiety in combination with sleep disorders - 10-20 mg 1 time for 1-2 hours before sleep. In psychiatric practice - the initial dose - 50-100 mg / day, then gradually increase the dose to 300 mg / day, the frequency of application - 3-4 times / day.Abstinence syndrome can be used more than 300 mg / day.
Children aged 4-7 years - 5-10 mg / day, 8-14 years - 10-20 mg / day, 15-18 years - 20-30 mg / day; multiplicity of application - 3-4 times / day.
With the / m introduction, a single dose for adults is 50-100 mg.
SIDE EFFECT
From the side of the central nervous system and peripheral nervous system: drowsiness, dizziness, muscle weakness; rarely - confusion, depression, visual impairment, diplopia, dysarthria, headache, tremor, ataxia; in isolated cases, paradoxical reactions (excitement, anxiety, sleep disturbances, hallucinations). After iv introduction hiccups are sometimes observed. With prolonged use, it is possible to develop drug dependence, memory impairment.
From the digestive system: rarely - constipation, nausea, dry mouth, salivation; in isolated cases - an increase in the level of transaminases and alkaline phosphatase in the blood plasma, jaundice.
From the endocrine system: rarely - increased or decreased libido.
From the urinary system: rarely - urinary incontinence.
From the side of the cardiovascular system: with the / m application, some decrease in blood pressure is possible.
On the part of the respiratory system: with parenteral use in isolated cases - breathing disorders.
Allergic reactions: rarely - skin rash.
CONTRAINDICATIONS
Severe myasthenia gravis, acute respiratory failure, severe chronic hypercapnia, phobias, obsessive conditions, chronic psychoses, history of alcohol or drug dependence (except for acute withdrawal), hypersensitivity to chlordiazepoxide and other benzodiazepines.
PREGNANCY AND LACTATION
Do not use chlordiazepoxide in the first trimester of pregnancy, except in cases of extreme necessity. It should be borne in mind that when using chlordiazepoxide in pregnancy, a significant change in the fetal heart rate is possible.
When used in obstetrics in doses recommended for the relief of labor, in newborns, more often in premature babies, temporary hypotension, hypothermia, and respiratory failure are possible.
If it is necessary to use it regularly during lactation, breastfeeding should be discontinued.
It should avoid the use of chlordiazepoxide in newborns.
SPECIAL INSTRUCTIONS
With extreme caution apply in patients with cardiac and chronic respiratory failure, organic changes in the brain (in such cases it is recommended to avoid parenteral administration of chlordiazepoxide), with angle-closure glaucoma and predisposition to it, in myasthenia, chronic kidney and / or liver diseases.
Special care is required when using chlordiazepoxide, especially at the beginning of treatment, in patients who have been receiving long-lasting antihypertensive drugs of central action, beta-adrenoblockers, anticoagulants, cardiac glycosides.
If you cancel therapy, the dose should be reduced gradually. With the sudden withdrawal of chlordiazepoxide after prolonged use, anxiety, agitation, tremors, convulsions are possible.
With prolonged use in high doses, it is possible to develop addiction and drug dependence.
Chlordiazepoxide should be discontinued with the development of paradoxical reactions (acute agitation, anxiety, sleep disturbances and hallucinations).
Avoid ingestion.
During the treatment period, do not drink alcohol.
Impact on the ability to drive vehicles and manage mechanisms
Patients taking chlordiazepoxide should refrain from engaging in potentially hazardous activities requiring increased attention and rapid psychomotor reactions.
DRUG INTERACTION
With simultaneous use with antipsychotic drugs (antipsychotics), antidepressants, sedatives, hypnotics, anesthetics, analgesics, ethanol, the depressing effect on the central nervous system increases, especially with parenteral administration.
Simultaneous use of antacids can delay, but not reduce the absorption of chlordiazepoxide.
With simultaneous ingestion of hormonal contraceptives, the effectiveness of chlordiazepoxide is enhanced. The incidence of development of breakthrough bleeding increases.
With simultaneous use with muscle relaxants, it is possible to increase the effect of muscle relaxants; with levodopa - suppression of antiparkinsonian action is possible.
With the simultaneous use of theophylline in low doses, it distorts the sedative effect of chlordiazepoxide.
With simultaneous use of phenobarbital and phenytoin can accelerate the metabolism of chlordiazepoxide. In rare cases, chlordiazepoxide suppresses metabolism and enhances the action of phenytoin.
In experimental studies, it has been shown that with simultaneous use, chlordiazepoxide can enhance the toxicity of cyclophosphamide.
When used simultaneously with cimetidine, omeprazole, disulfiram, an increase in the intensity and duration of action of chlordiazepoxide is possible.
