Anxiolytic medicine (tranquilizer) of the group of benzodiazepines of medium duration of action, also has sedative-hypnotic effect. Farmapram enhances inhibitory effects of endogenous GABA (mediator of pre- and postsynaptic inhibition in the CNS). Stimulates benzodiazepine receptors located in allosteric center of postsynaptic GABA receptors of ascending activating reticular formation of brain stem and insertion neurons of lateral horns of spinal cord; reduces excitability of subcortical structures of brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes. Anxiolytic effect is manifested by reduction of emotional tension, easing of anxiety, fear and restlessness. Sedative and sedative effect is manifested by reduction of symptomatology of neurotic origin (anxiety, fear). Expressed anxiolytic activity is combined with moderate soporific action; it shortens the period of falling asleep, increases the duration of sleep, reduces the number of night awakenings. The mechanism of hypnotic action is inhibition of the reticular formation cells of the brain stem. It reduces the effect of emotional, vegetative and motor stimuli, which disturb the mechanism of falling asleep.
Absorption after oral administration is fast and complete. TCmax is 1-2 hours. Binding with plasma proteins – 80%. Can cross the placenta, the HEB and penetrate into breast milk. Css in plasma is usually reached within a few (2-3) days. Metabolized in the liver to inactive or inactive metabolites. CYP3A4, CYP3A5 and CYP3A7 isoenzymes are involved in metabolism of the drug. T1/2 is 11-16 hours. The drug is excreted mainly by the kidneys as compounds with glucuronic acid. Accumulation after repeated administration is minimal (relates to benzodiazepines with medium T1/2), excretion after discontinuation of treatment is rapid.
Anxiety and neuroses with anxiety, tension, restlessness, irritability, sleep disturbance and somatic disorders.
Anxiety associated with depression (as part of complex therapy).
Panic disorders (treatment).
Tremor (senile, essential).
Hypersensitivity, coma, shock, myasthenia gravis, closed-angle glaucoma (acute attack or predisposition), acute alcohol poisoning (with impairment of vital functions), narcotic analgesics, sleeping pills and psychoactive drugs; severe COPD (progressive degree of respiratory failure), acute respiratory failure; severe depression (suicidal tendencies may manifest); pregnancy (especially trimester I), lactation, age less than 18 years (safety and efficacy not determined).
Caution. Liver failure, CKD, cerebral and spinal ataxia, drug addiction in anamnesis, predisposition to abuse of psychoactive drugs, hyperkinesis, organic brain diseases, psychosis (paradoxical reactions possible), hypoproteinemia, nocturnal apnea (established or suspected), elderly age.
Fetal Action Category. D