Included in the formulation
АТХ:N.02.C.A.52 Ergotamine in combination with other drugs, excluding psycholeptics
Pharmacodynamics:Combined drug.
Caffeine
The alkaloid contained in coffee seeds, tea leaves, cola nuts, cocoa. Affects the content of intracellular calcium, adenosine receptors and phosphodiesterase, which destroys cAMP.
It inhibits the phosphodiesterase of cAMP, increasing its concentration in the brain tissues. Has psychostimulant activity, increasing mental and physical performance, reducing the need for sleep and removing the feeling of fatigue.
It stimulates the respiratory and vasomotor centers, having an analeptic effect. It inhibits the production of prolactin and the secretion of milk.
Ergotamine
A selective serotonin receptor (5-hydroxytryptamine) agonist of the 5-HT1D and 5-HT1B, located in the vessels. It causes vasoconstriction when interacting with the 5-HT receptors of the intracranial vessels and the sensitive nerve endings of the trigeminovascular system, thereby suppressing the release of CGRP, VIP and substance P, which facilitates the course of migraine attacks by reducing the intensity of pain.Reduction of the release of serotonin and a decrease in its content in the postsynaptic gap by the negative feedback mechanism leads to a decrease in the severity of photo and phonophobia, nausea and vomiting. A stable repeated effect is caused by the action on the brain stem cells responsible for the development of migraine.
Pharmacokinetics:Caffeine
After ingestion, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached in 30-75 minutes. The connection with plasma proteins is 35%.
Metabolism in the liver to paraxanthin (80%), theobromine (10%), theophylline (4%).
Slows the clearance of paracetamol.
The half-life is 5 hours. Elimination by the kidneys.
Accelerates the absorption of ergotamine.
Ergotamine
After ingestion up to 5% absorbed in the gastrointestinal tract.
The therapeutic effect develops 30 minutes after ingestion and lasts for 5-8 hours. Metabolism in the liver.
The elimination half-life is 2 hours. Elimination with feces (90%) and kidneys (10%).
Indications:It is used to stop a migraine attack. Used for arterial hypotension.
VI.G40-G47.G43 Migraine
IX.I95-I99.I95 Hypotension
Contraindications:Diseases of peripheral arteries, severe renal failure, stenocardia Prinzmetal, age 18 years, pregnancy and lactation, individual intolerance.
Carefully:Agoraphobia, sleep disorders, angina pectoris, myocardial infarction, arterial hypertension, glaucoma, ventricular extrasystole, hypersensitivity.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside, 1-2 tablets during a migraine attack, then 1 tablet 2-3 times a day for 2-3 days.
The highest daily dose: 4 tablets.
The highest single dose: 2 tablets.
Side effects:Central and peripheral nervous system: excitation, tremor, convulsions, strengthening tendon reflexes, paresthesia in the tips of the fingers and toes.
Respiratory system: tachypnea, nasal congestion.
The cardiovascular system: cardialgia, arterial hypertension, tachycardia.
Digestive system: nausea, vomiting, diarrhea.
Musculoskeletal system: myalgia, weakness in the legs.
Dermatological reactions: itching.
Allergic reactions.
Overdose:Increased side effects.
Treatment is symptomatic.
Special instructions:If you need long-term use of the drug after a 7-day period, a break is made for 3-4 days.
It is not recommended simultaneous reception with other drugs from the group of agonists 5-HT1Dreceptors.
In the treatment it is not recommended to drive vehicles and work with moving mechanisms.