Ergotamine

Inhalation/Respiratory
Migraine

Sublingual
Migraine

Contraindicated.

Contraindicated.

May be taken with or without food.

Patient w/ severe or uncontrolled HTN, severe or persistent sepsis, shock, peripheral vascular disease, temporal arteritis, ischaemic heart disease, hyperthyroidism; basilar or hemiplegic migraine. Renal or hepatic impairment. Pregnancy. Concomitant admin w/ potent CYP3A4 inhibitors (e.g. azole antifungals, protease inhibitors, macrolide antibiotics).

Patient w/ anaemia. Lactation.

Nausea and vomiting, abdominal pain, tingling of fingers and toes, weakness, muscle pains in the extremities and numbness, localised oedema, itching, bradycardia, transient tachycardia.

PO/Rectal/SL: X

May cause dizziness and feelings of anxiety, if affected, do not drive or operate machinery.

Evaluate CV status prior to initiation and periodically thereafter.

Symptoms: Numbness, vomiting, tingling, pain, cyanosis of the extremities associated w/ diminished or absent peripheral pulses; HTN or hypotension; stupor, drowsiness, convulsions, shock, coma; reversible bilateral papillitis w/ ring scotomata. Management: Maintain adequate pulmonary ventilation, correction of hypotension and control or BP and convulsions. Keep the extremities warm to treat peripheral vasospasm. Vasodilators may be beneficial.

Increased risk of peripheral vasoconstriction w/ β-blockers. Increased vasoconstrictor effect w/ sympathomimetics (e.g. epinephrine).
Potentially Fatal: Increased risk of ergotism w/ potent CYP3A4 inhibitors (e.g. azole antifungals, protease inhibitors, macrolide antibiotics).

May enhance toxicity w/ grapefruit juice.

Description: Ergotamine has marked vasoconstrictor effects and partial agonistic action at serotonin (5-HT) receptors. It causes constriction of peripheral and cranial blood vessels and produces central vasomotor center depression. It also has a powerful oxytocic action on the uterus.
Pharmacokinetics:
Absorption: Poorly absorbed from the GI tract. Bioavailability: Approx ≤5%. Time to peak plasma concentration: 2 hr (oral).
Distribution: Crosses the blood-brain barrier; enters breast milk. Volume of distribution: 1.85 L/kg. Plasma protein binding: Approx 93-98%.
Metabolism: Undergoes extensive hepatic metabolism, including high first-pass effect.
Excretion: Via faeces (90%, mainly as metabolites); urine (approx 4%). Biphasic elimination half-life: Approx 2 hr (initial phase); 21 hr (terminal phase).

Source: National Center for Biotechnology Information. PubChem Database. Ergotamine, CID=8223, https://pubchem.ncbi.nlm.nih.gov/compound/Ergotamine (accessed on Jan. 22, 2020)

Store between 20-25°C. Protect form heat and light.

Antimigraine Preparations

N02CA02 - ergotamine ; Belongs to the class of ergot alkaloids preparations. Used to relieve migraine.

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Ergomar Tablet, Orally Disintegrating (Rosedale Therapeutics). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/01/2016.

Joint Formulary Committee. Ergotamine Tartrate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/01/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Ergotamine Tartrate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 20/01/2016.

Medihaler Ergotamine Aerosol, Metered (3M Riker). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/01/2016.