Pharmaceutical Form and Formulation
Each tablet contains:
Ergotamine tartrate 1 mg
50 mg caffeine
Aspirin 400 mg
Excipient c.b.p. 1 tablet.
Oral. Take 1-2 tablets as soon as the first symptoms of painful access arise, if the pain persists continue with a tablet every half hour until symptoms disappear, not to exceed 6 tablets per day. As a prophylactic crisis or subsequent attacks an average dose of one tablet every 12 hours, according to the severity of symptoms is recommended.
INDICATIONS: Indicated for the relief or prevention of vascular headaches known as migraines, tension, headaches and jaquecoides mixed syndromes.
Pharmacokinetics: The ergotamine acts as a vasoconstrictor if the vessel tone is poor and acts as a vasodilator if the pitch is high. Ergotamine is a partial agonist or antagonist at alpha adrenergic receptors causes vasoconstriction of arteries and veins, especially in the arterial bed when the external carotid is dilated. Also has a central effect on the serotonin (5-hydroxytryptamine) of serotonergic neurons, thereby breaking amines after nerve stimulation is avoided, thereby reducing the extracranial ergotamine and decreases blood flow in certain regions hyperfusion without decreasing the cerebral hemispheric flow.
Ergotamine slowly and incompletely absorbed in the digestive tract, so their bioavailability is low, about 97% is degraded in the first absorption step. But if ergotamine is administered concurrently with caffeine, increases its absorption and plasma concentration doubled.
Ergotamine is rapidly distributed in tissues is metabolized in the liver, eliminated as metabolites through the bile ducts by 90%, and 3-4% in urine, its half-life is 96 + - 24 minutes and its metabolites can last for up to 21-34 hours.
Caffeine has stimulant action on the CNS, in addition to action on the circulatory system, producing decreased peripheral vascular resistance without producing changes on blood pressure. At the central level increases cerebrovascular resistance with consequent decrease in cerebral blood flow also produces decrease in cerebrospinal fluid pressure and thereby hypertensive headache. Caffeine also increases the absorption of ergotamine. Slightly increased (10%) basal metabolic rate, its absorption is rapid in the digestive tract; is metabolized in the liver and eliminated almost entirely via feces, only 1% can be recovered in the urine.
Aspirin is the drug of choice in the treatment of mild to moderate pain, and that relieves pain by central and peripheral effect by direct inhibition of prostaglandin synthesis, is known to place central action is the hypothalamus (for it also has an antipyretic effect), acetylsalicylic acid biotransformation occurs in many tissues, particularly in the endoplasmic reticulum and mitochondria liver, excretion via the kidney is as metabolites of salicylate and 85% other acids by 5 %. The half-life of acetylsalicylic acid is about 23 hours at low and 15 to 30 hours at high dose. This is because the possibility of producing salicylates and other metabolites in the liver.