COFFETAMINUM

General characteristics. Structure:

Active ingredients: tartrate ergotamine – 0,001g; caffeine anhydrous – 0,0915 g. Excipients: starch potato-0,0238, talc-0,0031g, calcium stearate — 0,0006g cover Excipients; refined sugar (sucrose) — 0,1346 g, Dextrosums monohydrate-0,0207g, potato starch-0,0647, talc of-0,0072 g, calcium stearate — 0,0028 g. Description: Round, biconvex tablets, coated, the easy mramornost is allowed. On cross section two layers are visible: cover of white color, kernel of color, white or white with a creamy shade.

Pharmacological properties:

Pharmacodynamics. The combined drug. Caffeine causes stimulation of the central nervous system, mainly, of a cerebral cortex, the respiratory and vasomotor centers. Increases intellectual and physical effeciency, reduces drowsiness, feeling of fatigue. Has the expressed cardiotonic effect: increases force and heart rate, increases arterial pressure at hypotension. Ergotamine causes vasoconstrictive action. Caffeine accelerates ergotamine absorption.  

Pharmacokinetics. After intake about 62% of ergotamine are soaked up in digestive tract. The maximum concentration in plasma is reached in 2 h after intake. Linkng with proteins of plasma – 98%. Ergotamine is metabolized in a liver with formation pharmacological of active metabolites. Ergotamine preferential with bile both in an invariable look, and in the form of metabolites is removed. Removal has two-phase character, elimination half-lives of 2,7 h and 21 h for I and II phases respectively. After administration of drug inside caffeine is soaked up quickly and almost completely. Linkng with proteins of plasma makes 35%. Caffeine is almost completely metabolized in an organism. Metabolites are removed, mainly, with urine. The elimination half-life makes about 3,5 h.

Indications to use:

Migraine, arterial hypotension.

Route of administration and doses:

Inside, to adults and children 12 years on 1-2 tablet on inclusion in headache attack time, then on 1 tablet 2-3 times a day within several days are more senior. The maximum single dose – 2 tablets, daily – 4 tablets. It is not recommended to apply it is long (in avoidance of the phenomenon of an ergotism): after 7 days of use in the cases demanding more prolonged treatment do a break (for 3-4 days).

Features of use:

Use at pregnancy and during breastfeeding: Use at pregnancy and during breastfeeding is contraindicated.

Side effects:

From a nervous system: excitement, uneasiness, a tremor, concern, a headache, dizziness, spasms, paresthesias in extremities, strengthening of reflexes, tachypnea, sleeplessness; at sudden cancellation – strengthening of braking of the central nervous system, increased fatigue, drowsiness. From cardiovascular system: heartbeat, tachycardia, cardialgia, increase in arterial pressure. From the alimentary system: nausea, vomiting, diarrhea. Allergic reactions: hypostases, skin itch. Other: at prolonged use – accustoming, medicinal dependence, weakness in legs, a mialgiya, Lerish's syndrome (sharp cyanosis, lack of pulse on the lower extremities, pain, disturbance of sensitivity on distal type).

Interaction with other medicines:

Strengthens pharmacological effect of other medicines containing alkaloids of an ergot and caffeine. Caffeine is an antagonist of adenosine (high doses of adenosine can be required). At combined use of caffeine and barbiturates, Primidonum, anticonvulsant medicines (hydantoin derivatives, especially Phenytoinum) strengthening of metabolism and increase in clearance of caffeine is possible; Cimetidinum, peroral contraceptive means, Disulfiramum, ciprofloxacin, norfloxacin – decrease in metabolism of caffeine in a liver (delay of its allocation and increase in concentration in blood). The means causing stimulation of the central nervous system – excessive stimulation of the central nervous system is possible. Meksiletin – reduces removal of caffeine to 50%; nicotine – increases caffeine removal speed. Monoamine oxidase inhibitors, furasolidone, Procarbazinum and селегилин – high doses of caffeine can cause development of dangerous arrhythmias of heart or the expressed increase in arterial pressure. Caffeine reduces absorption of drugs of calcium in digestive tract. Reduces effect narcotic and hypnagogues; raises – non-narcotic analgesics (increase in absorbability). Increases removal of drugs of lithium with urine. Accelerates absorption and strengthens effect of cardiac glycosides, increases their toxicity. Combined use of caffeine with beta adrenoblockers can lead to mutual suppression of therapeutic effects: with adrenergic bronchodilatory medicines – additional stimulation of the central nervous system and other additive toxic effects. Caffeine can reduce clearance of theophylline and, perhaps, other xanthines, increasing a possibility of the additive pharmakodinamichesky and toxic effects. Vasoconstrictive effect of drug is strengthened alpha адреностимуляторы, by beta adrenoblockers, serotonin agonists (including суматриптан) and nicotine. Macroleads increase toxicity of ergotamine (decrease in hepatic clearance of caffeine). Influence on ability to control of vehicles during treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding concentration of attention and speed of psychomotor reactions.

Contraindications:

Individual intolerance of components of drug, children's age up to 12 years. With care - sleep disorders, alarming frustration (an agoraphobia, panic frustration), organic diseases of cardiovascular system (including an acute myocardial infarction, stenocardia, the expressed atherosclerosis, a Bouveret's disease, frequent ventricular premature ventricular contraction, arterial hypertension, obliterating diseases of peripheral vessels), a liver and/or renal failure, glaucoma, advanced age.

Overdose:

Symptoms: strengthening of expressiveness of side effects, including nausea, vomiting, numbness of fingers of hands and legs, block, drowsiness, epileptic seizures, stupor, coma.

Treatment: a gastric lavage, reception of absorbent carbon, if necessary – performing symptomatic therapy.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated. On 10 tablets in a blister strip packaging. 1 or 2 blister strip packagings together with the application instruction place in a pack cardboard.