The active ingredients of the drug Polygot are ergotamine and caffeine. Ergotamine tartrate 1 mg, caffeine 100 mg. It is used for arterial hypotension and migraine. Caffeine causes stimulation of the central nervous system, mainly the cerebral cortex, respiratory and vasomotor centers. It increases mental and physical performance, reduces sleepiness and fatigue. It has a pronounced cardiotonic effect: it increases strength and heart rate, increases blood pressure in hypotension. Ergotamine has a vasoconstrictor effect. Caffeine accelerates absorption of ergotamine.
After oral administration, about 62% of ergotamine is absorbed in the gastrointestinal tract. Maximum plasma concentration is reached 2 hours after oral administration. Binding to plasma proteins is 98%. Ergotamine is metabolized in the liver to form pharmacologically active metabolites. Ergotamine is eliminated mainly with bile both unchanged and as metabolites. Excretion is biphasic, with half-lives of 2.7 hours and 21 hours for I and II phases, respectively. After oral administration, caffeine is absorbed quickly and almost completely. Binding with plasma proteins is 35%. Caffeine is almost completely metabolized in the body. Metabolites are excreted mainly with urine. Half-life period of excretion is about 3.5 hours.
It enhances the pharmacological effects of drugs containing ergot alkaloids and caffeine. Caffeine is an adenosine antagonist (high doses of adenosine may be required). When caffeine and barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin) are used together, metabolism and clearance of caffeine may be increased; cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin reduce caffeine metabolism in liver (slowing its excretion and increasing blood concentrations). Drugs that cause central nervous system stimulation – excessive stimulation of the central nervous system is possible. Mexiletine – reduces caffeine excretion by up to 50%; nicotine – increases caffeine excretion rate. MAO inhibitors, furazolidone, procarbazine, and selegiline – large doses of caffeine can cause dangerous cardiac arrhythmias or marked increases in blood pressure. Caffeine reduces the absorption of calcium preparations in the gastrointestinal tract. Reduces the effect of narcotic and sleeping pills; increases the effect of non-narcotic analgesics (increased absorption). Increases excretion of lithium preparations with urine. Accelerates absorption and enhances the effect of cardiac glycosides, increases their toxicity. Concomitant use of caffeine with beta-adrenoblockers can lead to mutual suppression of therapeutic effects: with adrenergic bronchodilators – additional stimulation of the central nervous system and other additive toxic effects. Caffeine can decrease the clearance of theophylline and possibly other xanthines, increasing the possibility of additive pharmacodynamic and toxic effects. The vasoconstrictor effects of the drug are enhanced by alpha-adrenergic stimulants, beta-adrenoblockers, serotonin agonists (including sumatriptan) and nicotine. Macrolides increase the toxicity of ergotamine (decreased hepatic clearance of caffeine).