Dihydroergotamine

Intravenous
Acute attack of cluster headache, Migraine

Nasal
Acute migraine attacks

Parenteral
Acute attack of cluster headache, Migraine

Severe: Contraindicated.

Severe: Contraindicated.

May be taken with or without food.

Ischaemic heart disease (i.e. angina pectoris, silent ischaemia, history of MI), coronary artery vasospasm (e.g. Prinzmetal’s variant angina), vasospastic coronary artery disease, uncontrolled HTN, haemiplegic or basilar migraine, peripheral vascular disease, sepsis. Patient following vascular surgery. Concomitant use w/ potent CYP3A4 inhibitors. Severe hepatic or renal impairment. Pregnancy and lactation.

Patients w/ risk factors predictive of coronary artery disease (e.g. HTN, hypercholesterolemia, angina), history of drug induced fibrotic disorders, severe orthostatic hypotension.

Significant: Nausea, vomiting. Rarely, pleural, retroperitoneal, and cardiac valvular fibrosis, increase in BP.
Nervous: Paraesthesia, numbness of fingers and toes, tingling sensation, dizziness, headache.
CV: HTN, vasospasm.
GI: Abdominal pain, diarrhoea, taste disturbance, throat irritation.
Resp: Dyspnoea, nasal irritation.
Muscoloskeletal: Muscle spasm.
Dermatologic: Facial oedema, urticaria, rash, increased sweating.
Potentially Fatal: Rarely, coronary artery vasospasm, transient myocardial ischaemia, acute MI, ventricular tachycardia, ventricular fibrillation, cerebrovascular events (e.g. cerebral or subarachnoid haemorrhage, stroke), gangrene.

IM/IV/Nasal/Parenteral/SC: X

This drug may cause dizziness, if affected, do not drive or operate machinery.

Monitor CV status prior to and periodically during therapy.

Symptoms: Nausea, vomiting, numbness, tingling, pain, cyanosis of the extremities, abdominal pain, resp depression, increase and/or decrease in BP, confusion, delirium, convulsions, and coma. Management: Apply warmth to affected area. Provide nursing care to prevent tissue damage. Admin of vasodilators may be beneficial.

Enhanced vasoconstriction w/ other ergot alkaloids, sumatriptan, β-blockers, nicotine, and other vasoconstrictors. May lead to serotonin-like syndrome (e.g. weakness, incoordination, hyperreflexia) when used w/ SSRIs.
Potentially Fatal: Concurrent use of potent CYP3A4 inhibitors (e.g protease inhibitors, macrolides, azole antifungals) may cause vasospasm that may lead to cerebral ischaemia.

Description:
Mechanism of Action: Dihydroergotamine, an ergot alkaloid, is an α-adrenergic blocker that directly stimulates vascular smooth muscle to constrict peripheral and cerebral vessels. Additionally, it stimulates 5-HT plasma level to counteract the loss of tone of the extracranial vasculature.
Onset: 15-30 min (IM).
Duration: 3-4 hr (IM).
Pharmacokinetics:
Absorption: Bioavailability: 43% (nasal). Time to peak plasma concentration: 1-2 min (IV); 24 min (IM); 15-45 min (SC); 30-60 min (nasal).
Distribution: Volume of distribution: Approx 800 L. Plasma protein binding: 90-95%.
Metabolism: Extensively metabolised to the active metabolite, 8'-β-hydroxydihydroergotamine; and further metabolised via oxidation to the active metabolite, 8',10'-dihydroxydihydroergotamine; undergoes extensive hepatic first-pass metabolism.
Excretion: Mainly via faeces; and urine (6-7% as unchanged drug). Elimination half-life: Approx 9-10 hr.

Source: National Center for Biotechnology Information. PubChem Database. Dihydroergotamine, CID=10531, https://pubchem.ncbi.nlm.nih.gov/compound/Dihydroergotamine (accessed on Jan. 21, 2020)

Store below 25°C. Do not refrigerate or freeze. Soln for inj: Protect from light.

Antimigraine Preparations

Anon. Dihydroergotamine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 22/02/2017.

Buckingham R (ed). Dihydroergotamine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/02/2017.

Dihydroergotamine Mesylate Injection, Solution (Paddock Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 22/02/2017.

Dihydroergotamine Mesylate Spray (Oceanside Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 22/02/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Dihydroergotamine Mesylate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 22/02/2017.