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Anticonvulsant, relates to barbiturates. Reduces the excitability of neurons in the epileptogenic focus. It produces a weakly pronounced hypnotic effect.
After oral administration it is quickly and completely absorbed from the gastrointestinal tract. Bioavailability is more than 90%. Tmax - is reached after 3 hours. Vd - 0.64-0.86 l/kg. Primidone is metabolized in the liver to form 2 active metabolites: phenobarbital - 15-25% and phenylethylmalonamide. Binding of primidone to plasma proteins is 20%, phenobarbital - 50%, phenylethylmalonamide - insignificant. T1/2 of primidone, phenobarbital and phenylethylmalonamide is 3-23, 75-126 and 10-25 hours respectively. Excreted by the kidneys as primidone - 64%, phenobarbital - 5.1%, phenylethylmalonamide - 6.6%.
Primidone and its metabolites are excreted with breast milk, where their average concentration is 75% of Css in blood.
Contraindications for use
Liver, kidney and hemopoietic system diseases; pregnancy, lactation; hypersensitivity to primidone.
Usage during pregnancy and lactation
Contraindicated for use during pregnancy and lactation (breast-feeding).
Administration in patients with liver dysfunction
Contraindicated in liver disorders.
Using in patients with impaired renal function.
Contraindicated in kidney disorders.
Administration in children
Caution is recommended when used in children.
Administration in elderly patients
Caution is recommended when used in elderly patients. Long-term use may lead to drug addiction.
Indications of active substances of Mysoline (Primidone)
Epilepsy of various genesis, manifested mainly by grand mal seizures. Less effective in focal, myoclonic, akinetic seizures.
meals, then every 3 days the daily dose is increased by 250 mg for adults and by 125 mg for children under 9 years of age until the desired effect is achieved. The maximum daily dose for adults is 1.5 g, for children 1 g (in 2 doses).