dihydroergotamine mesylate

dihydroergotamine mesylate

[dīhī′drō·ərgot′əmēn me′si lāt]

an ergot alkaloid causing vasoconstriction through stimulation of several types of receptors, including alpha-adrenergic receptors and serotonin receptors.

indications It is prescribed for the treatment of migraine and vascular headache.

contraindications Cardiovascular disease, hypertension, liver or kidney dysfunction, sepsis, pregnancy, or known hypersensitivity to this drug prohibits its use.

adverse effects Among the more serious adverse reactions are gangrene and the toxicity of the ergot alkaloids.

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dihydroergotamine mesylate

D.H.E. 45, Dihydroergotamine-Sandoz (CA), Migranal

Pharmacologic class: Alpha-adrenergic blocker

Therapeutic class: Vasoconstrictor, vascular headache suppressant

Pregnancy risk category X

FDA Boxed Warning

• Serious or life-threatening peripheral ischemia may occur when drug is given concurrently with potent CYP3A4 inhibitors (including protease inhibitors and macrolide antibiotics). Interaction increases risk of vasospasm leading to cerebral ischemia or ischemia of extremities. Concurrent use is contraindicated.

Action

Stimulates alpha-adrenergic receptors, causing intracranial and peripheral vasoconstriction. Also activates 5-hydroxytryptamine-1D receptors to inhibit release of proinflammatory neuropeptides.

Availability

Injection: 1 mg/ml

Nasal spray: 4 mg/ml in ampule with applicator

⊘Indications and dosages

➣ Vascular headaches, including migraine and cluster headaches

Adults: 1 mg I.M. or subcutaneously; may repeat in 1 hour to a total dosage of 3 mg (not to exceed 3 mg/day or 6 mg/week). Or 1 mg I.V.; may repeat in 1 hour (not to exceed 2 mg/day or 6 mg/week). Or one spray (0.5 mg) in each nostril, repeated after 15 minutes to a total dosage of 2 mg (not to exceed 3 mg/24 hours or 4 mg/week).

Off-label uses

• Intracranial hypertension
• Prevention of orthostatic hypotension
• Deep-vein thrombosis, pulmonary embolism

Contraindications

• Hypersensitivity to drug
• Cardiovascular disease, hypertension, peripheral vascular disease
• Severe renal or hepatic disease
• Concurrent use of potent vasoconstrictors
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• diabetes mellitus
• concurrent use of beta-adrenergic blockers, macrolide antibiotics, or nitrates
• children younger than age 6.

Administration

• Give at first sign of migraine or as soon as possible after symptom onset.
• For I.V. use, drug may be given undiluted over 1 minute.

Route	Onset	Peak	Duration
I.V.	<5 min	15 min-2 hr	8 hr
I.M., subcut.	15-30 min	15 min-2 hr	8 hr
Nasal	Within 30 min	Unknown	Unknown

Adverse reactions

CNS: dizziness, fatigue, numbness or tingling in fingers or toes

CV: angina pectoris, intermittent claudication, sinus tachycardia, sinus bradycardia, myocardial infarction

EENT: rhinitis, throat irritation

GI: nausea, vomiting, diarrhea, abdominal pain

Musculoskeletal: stiffness or weakness of arms, legs, neck, or shoulders; muscle pain

Other: altered taste, polydipsia

Interactions

Drug-drug . Beta-adrenergic blockers, macrolides, vasoconstrictors: increased risk of peripheral vasoconstriction

Nitrates: antagonism of antianginal effects

Drug-behaviors. Smoking: increased risk of peripheral vasoconstriction

Patient monitoring

• Monitor cardiac status, especially when giving large doses.
• Assess for and report numbness and tingling of fingers and toes, arm or leg weakness, muscle pain, and intermittent claudication.

Patient teaching

• Advise patient to take drug at first sign of migraine.
• Instruct patient to lie down in dark, quiet room for several hours after taking dose.
☞ Tell patient to immediately report chest pain, nausea, vomiting, change in heartbeat, numbness, tingling, or pain or weakness in arms or legs.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and behaviors mentioned above.