Valproic acid (valproic acid)
VALPROEVAYA ACID (Valproic acid)
Chemical name : 2-Propilvalerianovaya acid (and a limestone, magnesium or sodium salt)
Description : White melkokristallichesky powder. The easily soluble in water and alcohol.
Pharmacology : The drugs act-protivoepilepticheskoe, miorelaksiruyuschee, sedative.
Ingibiruya GAMK- transferazu enhances content in the CNS gamma aminomaslyanoy acid, which makes lower threshold level of excitability and convulsant to motor areas brain. When administered to valproat- ion dissociation, which is absorbed in the blood plasma. Food reduces the absorption. Cmax plasma determined by 1-4 h. Therapeutic concentrations in the blood of 50-100 ug / ml (may be much higher or lower depending on the permeability of the patient GEB). Linking blood plasma proteins of about 90%. Metabolised in the liver : most glyukuronidiruetsya, less-oxidized with a mikrosomalnyh enzymes in mitochondria or hepatocytes (beta-oxidation). T1 / 2 ranges from 6 to 16 h, and depends largely on the activity of liver enzymes mikrosomalnyh. Metabolites and Algae kidney removed. A few valproevoy acid out of milk.
Application : Various forms of generalized fits : small (absansy), large (apnoea) and polymorphic; Used focal fits, child-tice.
Contraindications : Giperchuvstvitelnost, incl. "Family" (death of close relatives in the face of admission valproevoy acid), liver disease and pancreas (a portion of patients may significantly decrease metabolism in the liver), hemorrhagic diathesis, pregnancy (I term), breast-feeding.
Restrictions apply to : Children's age (the simultaneous appointment of several convulsants) aplaziya bone marrow, pregnancy (postponed).
Application of pregnancy and breastfeeding : Protivopokazano I trimester of pregnancy. Perhaps in II and III trimester of pregnancy if the expected effect of treatment outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.
Side effects : Nausea, vomiting, diarrhoea, stomach pains, anorexia or increased appetite, disruption of the liver, drowsiness, tremor, parestezii, sputannost consciousness, peripheral oedema, hemorrhage, radiation, thrombocytopenia. When long-time admission hair loss.
Networking : The effect reinforces the other convulsants, sedatives and pain medication. Diarrhoeal disorders develop less in the face spazmolitikov and coating means. Alcohol and other means of increasing the likelihood gepatotoksichnye to liver, anticoagulants or acetylsalicylic acid, the risk of bleeding.
Dosing and Administration : inside, during or immediately after eating. Daily intake for adults in the early treatment of 0,3-0,6 g, in the 1-2 weeks it has gradually increased until 0,9-1,5 g single dose for adults 0,3-0,45 city Daily intake for children 15-50 mg / kg (in the early 15 mg / kg, followed by a gradual increase of 5-10 mg / kg per week).
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