MEDAZEPAM (Medazepam)

     Chemical name : 7-Chloro-2, 3-digidro-1- metil-5- fenil-1H-1, 4-benzodiazepine (as hydrochloride)

     Description : Zelenovato- melkokristallichesky yellow powder. Almost nerastvorim water easily in alcohol.

     Pharmacology : The drugs act-acid, sedative.

Benzodiazapine receptor interacts with the limbic system and upstream activating the brain stem structures, contributes to the formation of channels for chlorine ions, which leads to greater braking effect of GABA in the CNS.

When ingestion absorbed 50-75%. Cmax in plasma achieved in 1-2 hours While associated with plasma proteins. Metabolised in the liver by gidroksilirovaniya, N-demethylation and oxidation. Forms active metabolites : Oxazepam (7% of dose), desmetilmedazepam, diazepam and desmetildiazepam, the latter has long T1 / 2, and probably has sedative effect. T1 / 2 medazepama is 20-176 hours Metabolites are great T1 / 2, after receiving medazepama even during 3-14 days determined by their significant concentrations in plasma. Provided in the form of metabolites (mainly glyukuronidy) through the kidneys (63-85%) and the intestines (15-37%).

It removes anxiety, fear, psihonevroticheskogo voltage motor concern over bustle. Restores critical assessment of their own illness. Protivosudorozhnoe central miorelaksiruyuschee, sedative and sleeping pills effect is less widespread than the typical benzodiazapine tranquilizers. SLEEPING combined with a certain trigger properties, slightly violates working during the day (it lies within the "daily" tranquilizers). Recommended for therapy weakened patients, older patients and children (for lack expressed miorelaksiruyuschih and sedative properties). Appointed for a short time, because a long reception, especially at high doses, may develop mental Drug Dependence (Physical dependence occurs infrequently). In practice, child assigned strictly on the grounds (reduced ability to memorize). For patients with chronic obstructive respiratory diseases with high doses may gipoventilyatsii alveolar development.

     Application : U-adult concerns and fears of aggressive character disorders, neuroses, state TV (including functional nervousness in the cardiovascular system, migraines, menopause syndrome), withdrawal syndrome in chronic alcoholism. In children, excessive anxiety, "school" neuroses, mental lability.

     Contraindications : Giperchuvstvitelnost (including from other benzodiazepines), male.

     Restrictions : To Serious liver and kidney functions, I trimester of pregnancy (should strictly adhere to the use of evidence), breast-feeding (should abandon breastfeeding).

     Side Effects : The sense of fatigue, headache (first reaction to the reception, disappears after lower doses), drowsiness, weakness, a violation of accommodation, tachycardia, increased muscle fatigue, loss of libido, impotence, menstrual irregularities, allergic skin reactions, drug dependency; A Older patients and children, the loss of orientation, lack of braking aggressiveness.

     Networking : Usilivaet (mutually) effect hypnotics, Neuroleptics, antidepressants, alcohol and etanolsoderzhaschih preparations for narcosis and analgesics.

     Overdosing : Symptoms : a sense of fatigue, ataxy, tachycardia, hypotension, diminished muscle tone; In severe cases, coma, convulsions, respiratory depression.

Treatment : washing stomach reception activated carbon and sodium sulphate; Correction respiratory and circulatory, symptomatic therapy. Forced Diurez and hemodialysis little.

     Dosing and Administration : inside, the food, squeezed small amounts of liquid. Early treatment for the 5 mg 2-3 times a day, then gradually increase the dose to 30-40 mg per day. In outpatient settings recommended by the morning of 5 mg and 10 mg day and night. Older patients and adolescents appoint 10-20 mg; Children 2 mg / kg / day. The maximum daily intake for adults 60-70 mg. When treating chronic alcoholism drug use in the average daily dose for 1-2 weeks.

     Precautions : Do not apply during the drivers of transport operators and those professions that require rapid mental and motor responses. During treatment should refrain from accepting alcohol. To prevent cramping syndrome should be lifted gradually preparation.

Materials allowed to copy only with the active hyperlink to the handbook of medicines