PHENAMINUM (Phenaminum, Aktedrin, Alentol, Amphamine, Amphedrine, Amphethamini sulfas, Amphetamine sulfate, Benzedrine sulfate, Benzpropamin, Euphodyn, Isoamin; Ortedrine, Psychedrinum, Psychoton, Racephen, Raphetamin, Sympamin, Sympatedrine).
Crystalline powder, white color, bitter taste. Let’s easily dissolve in water, it is badly alcohol-soluble. Phenaminum is the synthetic bond derivative of a fenilalkilamin. On a chemical structure and some pharmacological properties (mainly on influence on peripheric departments of a sympathetic nervous system) it is close to drugs of group of an adrenaline. On a structure differs from an adrenaline and Noradrenalinum in lack of hydroxyls in an aromatic cycle and an aliphatic chain that gives it larger firmness and, besides, allows to break a hematoencephalic barrier easily; branched character of an aliphatic chain (existence of metilny group in a-situation to an amino group) protects its molecule from an oxidizing deamination monoamine oxidase. Thanks to firmness in an organism effects of Phenaminum are long and are shown at its reception inside.
Phenaminum is a strong stimulator of a CNS. The stimulating effect of drug is bound considerably to its influence on a stem part of a brain. In the neurochemical mechanism of action of Phenaminum the large role is played by its ability to cause release from granules of the presynaptic nervous terminations of Noradrenalinum and Dofaminum and to stimulate, thus central noradrenergichesky and more dofaminergichesky receptors. It exerts also small inhibiting impact on activity of monoamine oxidase and slows down the return neyronalny capture of Dofaminum and Noradrenalinum. Phenaminum has also peripheric adrenergic activity (stimulates a-and b – adrenoreceptors); it causes narrowing of peripheric vessels, intensifying of reductions of heart, rising of arterial pressure, relaxation of a musculation of bronchi, expansion of pupils. These effects are more long, but are less expressed, than at an adrenaline.
At the correct dosage Phenaminum, strengthening processes of exaltation in a CNS, reduces feeling of a fatigue, exerts the general exciting impact which is expressed in improvement of mood, feeling of inflow of forces, cheerfulness, working capacity rising, decrease of need for a dream. Phenaminum and its analogs weaken and shorten the dream caused by hypnotic drugs and narcotics in this connection they are called sometimes the awakening amines.
Drug has anorexigenic activity, i.e. reduces appetite and promotes more bystry offensive of feeling of saturation by a nutrition. The long time Phenaminum was considered one of the fixed psychogogic assets. Widely used it for rising of mental and physical working capacity, for the treatment of a narcolepsy, depressions, consequences of an encephalitis and other diseases which are followed by a sleepiness, slackness, apathy, an asthenia at a postencephalitic parkinsonism (together with cholinolytic drugs).
In recent years in connection with possible by-effects (disturbances of higher nervous activity, rising of arterial pressure, rather frequent paradoxical reactions – drowsiness and apathy instead of exaltation, working capacity dropping, etc.), and, above all – in connection with possible development of accustoming and addiction by Phenaminum began to use extremely seldom.
Prescribe Phenaminum inside the adult on 0,005 – 0,01 g (5 – 10 mg) of 1 – 2 time a day. Action after a single dose lasts 2 – 8 h. Doses need to be selected individually because of various sensitivity and an acceptability. Drug is removed from an organism slowly, the cumulation phenomena are possible. Phenaminum has to be applied with care and only on medical indications. At an overdosage of drug there can be a giddiness, a cold fit, nausea, appetite loss, sleeplessness, tachycardia, arrhythmias. At prolonged uncontrolled use serious psychological disorders up to the shizofrenopodobnykh of psychoses are possible. At reception of Phenaminum in the second half of day the sleep can be interrupted.
As contraindications to use of Phenaminum serve the senile age, sleeplessness, a condition of exaltation, a liver disease, a hypertensia, atherosclerosis, organic diseases of cardiovascular system.