Ergotamine information from DrugsUpdate
P - Contraindicated in pregnancy
L - Contraindicated in lactation
FI - Food *
Ergotamine is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It possesses structural similarity to several neurotransmitters, and has biological activity as a vasoconstrictor. It is used medicinally for treatment of acute migraine attacks (sometimes in combination with caffeine), and to induce childbirth and prevent post-partum haemorrhage.
Pharmacodynamics
Pharmacokinetics
Ergotamine has marked vasoconstrictor effects and partial agonistic action at serotonin receptors. It causes constriction of peripheral and cranial blood vessels and also has powerful oxytocic action on the uterus. It also reduces hyperperfusion in the basilar artery territory.
Absorption
Poorly absorbed from the GI tract (oral, sublingual), decreased further by gastric stasis.
Distribution
Enters breast milk
Metabolism
Extensive hepatic first-pass effect.
Excretion
Via bile (as metabolites), via urine (4%); elimination T1/2 (biphasic): 2 hr (initial phase), 21 hr (terminal phase).
Ergotamine Indications / Ergotamine Uses
Information Not Available
Ergotamine Adverse Reactions / Ergotamine Side Effects
Muscle cramps, stiffness, tiredness. Numbness and tingling of extremities. Nausea, vomiting, diarrhoea. Ergotism consisting of hypotension and gangrene of extremities, anginal pain and transient tachycardia or bradycardia.
Potentially Fatal: Severe peripheral vasoconstriction, CV disturbances. Due to vascular occlusions causing gangrene, MI, bowel necrosis, renal failure. Simultaneous use of oral contraceptives or β-blockers increases the risk.
Precautions
Information Not Available
Special Precautions
Anaemia. Monitor for signs of ergotism such as numbness or tingling of the extremities.
Other Drug Interactions
Vasoconstrictor effects enhanced by sympathomimetic agents e.g. adrenaline. Caffeine potentiates the action of ergotamine.
Potentially Fatal: Administration within 6 hr of taking serotonin agonist may lead to increased and prolonged vasopastic reactions. May have increased risk of peripheral vasoconstriction with β-blockers. Erythromycin increases plasma conc of ergotamine which may lead to ergotism.
Other Interactions
Food Interactions
Beverages containing caffeine e.g. tea, cola and coffee.
Dosage
Oral
Migraine
Adult: As tartrate: 1-2 mg, repeated after 30 minutes if needed. Max:: 6 mg/24 hr, 12 mg/wk. Ensure an interval of at least 4 days between successive 24-hr courses. Not more than 2 courses/mth. May also be given sublingually.
Rectal
Migraine
Adult: As tartrate: 2 mg repeated after 1 hr, if needed. Max: 4 mg/24 hr, 8 mg/wk with an interval of at least 4 days between successive 24-hr courses.
Inhalation
Migraine
Adult: As tartrate: 360 mcg inhaled at the onset of attack and repeated at 5-min intervals, if needed. Max: 6 inhalations/24 hr, 12 inhalations/wk with an interval of at least 4 days between successive 24-hr courses.
Food(before/after)
May be taken with or without food
List of Contraindications
Ergotamine and Pregnancy
Contraindicated in pregnancy.
Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Ergotamine and Lactation
Contraindicated in lactation
Ergotamine and Children
Information Not Available
Ergotamine and Geriatic
Information Not Available
Ergotamine and Other Contraindications
Severe or uncontrolled hypertension, peripheral vascular disease, pregnancy, lactation, septic conditions, ischaemic heart disease, hyperthyroidism, impaired hepatic or renal function, hypersensitivity, cachexia, collagen disease and fibrotic conditions.
Storage
Inhalation
Store below 25°C.
Oral
Store below 25°C.
Rectal
Store below 25°C.
Lab interference
Inhalation
Store below 25°C.
Oral
Store below 25°C.
Rectal
Store below 25°C.
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