Phenamine (Phenaminum, Aktedrin, Alentol, Amphamine, Amphedrine, Amphethamini sulfas, Amphetamine sulfate, Benzedrine sulfate, Benzpropamine, Euphodyn, Isoamine; Ortedrine, Psychedrinum, Psychoton, Racephen, Raphetamine, Sympamin, Sympatedrine).
White crystalline powder with a bitter taste. It is soluble in water (1:20 in cold, 1:3 in hot), slightly soluble in alcohol. Phenamine is a Synthetic compound derived from phenylalkylamine. By its chemical structure and some pharmacological properties (mainly by its effect on the peripheral parts of the sympathetic nervous system), it is close to drugs of the adrenaline group. Structurally, it differs from adrenaline and norepinephrine in the absence of hydroxyls in the aromatic cycle and the aliphatic chain, which gives it greater resistance and, moreover, makes it easy to overcome the blood-brain barrier; the branched nature of the aliphatic chain (the presence of a methyl group in the a-position to the amino group) protects its molecule from oxidative deamination by monoamine oxidase. Due to its persistence in the body, the effects of phenamine are long-lasting and manifest themselves when ingested.
Phenamine is a strong central nervous system stimulant. The stimulating effect of the drug is largely due to its effect on the brain stem. In the neurochemical mechanism of action of phenamine, its ability to induce the release of norepinephrine and dopamine from presynaptic nerve endings granules and thus stimulate central noradrenergic and, to a greater extent, dopaminergic receptors plays an important role. It also has a slight inhibitory effect on the activity of monoamine oxidase and inhibits the reverse neuronal uptake of dopamine and norepinephrine. Phenamine also has peripheral adrenergic activity (stimulates a- and b – adrenergic receptors); it causes constriction of peripheral vessels, increased heart contractions, increased blood pressure, relaxation of bronchial muscles, dilation of pupils. These effects are more prolonged, but less pronounced than those of adrenaline.
With proper dosing, phenamine, enhancing the processes of arousal in the central nervous system, reduces the feeling of fatigue, has a general stimulating effect, expressed in improving mood, feeling a surge of strength, cheerfulness, increased efficiency, and reduced need for sleep. Phenamine and its analogues weaken and shorten sleep caused by sleeping pills and drugs, which is why they are sometimes called awakening amines.
The drug has anorexigenic activity, i.e. it reduces appetite and promotes a faster onset of a feeling of satiety with food. For a long time, phenamine was considered one of the main psychostimulants. It has been widely used to improve mental and physical performance, for the treatment of narcolepsy, depressive states, the effects of encephalitis and other diseases accompanied by drowsiness, lethargy, apathy, asthenia, in postencephalitic parkinsonism (together with cholinolytic drugs).
In recent years, due to possible side effects (disorders of higher nervous activity, increased blood pressure, relatively frequent paradoxical reactions – drowsiness and apathy instead of excitement, decreased performance, etc.), and most importantly – due to the possible development of addiction and addiction, phenamine has become extremely rare.
Phenamine is administered orally to adults at 0.005 – 0.01 g (5-10 mg) 1-2 times a day. The effect after a single dose lasts 2 to 8 hours. Doses must be selected individually due to different sensitivity and tolerability. The drug is excreted from the body slowly, accumulation phenomena are possible. Phenamine should be used with caution and only for medical reasons. If the drug is overdosed, dizziness, chills, nausea, loss of appetite, insomnia, tachycardia, arrhythmias may occur. With prolonged uncontrolled use, severe neuropsychological disorders up to schizophrenic-like psychoses are possible. When taking phenamine in the afternoon, sleep may be disturbed.
Contraindications to the use of phenamine are senile age, insomnia, arousal, liver disease, hypertension, atherosclerosis, organic diseases of the cardiovascular system.
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