Dihydroergotamine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IV/IM/SC Migraine; Acute attack of cluster headache Initial: 1 mg via IV/IM/SC inj, repeat dose at 1 hr interval, as needed. Max: 2 mg/day (IV); 3 mg/day (IM/SC); 6 mg/wk. Nasal Acute Migraine attacks As 0.4% soln: 0.5 mg/nostril, then an additional 0.5 mg/nostril after 15 min. Max: 2 mg/attack.
Dosage Details
Intravenous
Acute attack of cluster headache, Migraine
Adult: Initially, 1 mg via slow IV inj over 2-3 min, repeat dose at 1 hr interval, as needed. Max: 2 mg daily; 6 mg wkly.

Nasal
Acute migraine attacks
Adult: As 0.4% soln: 0.5 mg sprayed into each nostril, then an additional 0.5 mg into each nostril after 15 min. Max: 2 mg/attack.

Parenteral
Acute attack of cluster headache, Migraine
Adult: Initially, 1 mg via SC/IM inj, repeat dose at 1 hr interval, as needed. Max: 3 mg daily; 6 mg wkly.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
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.
Special Precautions
Patients w/ risk factors predictive of coronary artery disease (e.g. HTN, hypercholesterolemia, angina), history of drug induced fibrotic disorders, severe orthostatic hypotension.
Adverse Reactions
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
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor CV status prior to and periodically during therapy.
Overdosage
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.
Drug Interactions
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.
Action
Description: 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.
Chemical Structure

Chemical Structure Image

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

Storage
Store below 25°C. Do not refrigerate or freeze. Soln for inj: Protect from light.
ATC Classification
N02CA01 - dihydroergotamine ; Belongs to the class of ergot alkaloids preparations. Used to relieve migraine.
References
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.

Disclaimer: This information is independently developed by MIMS based on Dihydroergotamine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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