D.H.E. 45, Migranal
Classifications: alpha-adrenergic antagonist; ergot alkaloid; Therapeutic: antimigraine; ergot alkaloid
Pregnancy Category: X
4 mg/mL nasal spray; 1 mg/mL injection
Alpha-adrenergic blocking agent and dihydrogenated ergot alkaloid with direct constricting effect on smooth muscle of peripheral
and cranial blood vessels. Additionally, its ergot properties act as selective serotonin agonists at the 5-HT1 receptors located on intracranial blood vessels, which may also cause vasoconstriction of large intracranial conductance
arteries; this correlates with relief of migraine headaches.
Reduces rate of serotonin-induced platelet aggregation. Has somewhat weaker vasoconstrictor action than ergotamine but greater
adrenergic blocking activity, resulting in relief from migraine headaches.
To prevent or abort vascular headache (e.g., migraine or histaminic cephalalgia) when rapid control is desired or other
routes are not feasible. With low-dose heparin therapy to prevent postoperative deep-vein thrombosis and pulmonary embolism.
To treat postural hypotension.
History of hypersensitivity to ergot preparations; peripheral vascular disease, coronary heart disease, MI, hypertension;
peptic ulcer; severely impaired hepatic or renal function; sepsis; within 48 h of surgery; pregnancy (category X), lactation.
Safe use in children <6 y is not established.
Moderate or mild renal or hepatic impairment; obesity; diabetes mellitus; postmenopausal women; males >40 y; pulmonary heart
disease; valvular heart disease; smokers.
Route & Dosage
Adult: IV/IM/SC 1 mg, may be repeated at 1 h intervals to a total of 3 mg IM or 2 mg IV/SC (max: 6 mg/wk) Intranasal 1 spray (0.5 mg) in each nostril, may repeat with additional spray in 15 min if no relief (max: 4 sprays per attack); wait 68 h before treating another attack (max: 8 sprays per 24 h, 24 sprays/wk)
- Give at first warning of migraine headache.
- Optimum results: Titrate the doses required to bring relief for several headaches to determine the minimal effective dose.
Use the established dose for subsequent attacks.
- Withdraw IM or SC dose directly from ampule. Do not dilute.
- Note: Onset of action is about 20 min; when rapid relief is required, the IV route is prescribed.
PREPARE: Direct: Give undiluted.
ADMINISTER: Direct: Give at a rate of 1 mg/60 sec.
- Store at 15°30° C (59°86° F) unless otherwise directed.
- Protect ampules from heat and light; do not freeze.
- Discard ampule if solution appears discolored.
Adverse Effects (≥1%) CV:
Vasospasm: coldness, numbness and tingling in fingers and toes, muscle pains and weakness of legs, precordial distress and
pain, transient tachycardia or bradycardia, hypertension (large doses). GI: Nausea, vomiting. Body as a Whole:
Dizziness, dysphoria, localized edema and itching;
ergotism (excessive doses).
InteractionsDrug: beta blockers
increase peripheral vasoconstriction with risk of ischemia; increased ergotamine toxicity
with drugs that inhibit CYP3A4 (e.g., protease inhibitors, amprenavir, ritonavir, nelfinavir, indinavir, saquinavir
), macrolide antibiotics (erythromycin, azithromycin, clarithromycin), azole antifungals (ketoconazole, itraconazole, fluconazole, clotrimazole), nefazodone, fluoxetine, fluvoxamine. Food: Grapefruit juice
may increase toxicity
1530 min IM; <5 min IV. Duration:
34 h. Distribution:
Probably distributed into breast milk. Metabolism:
In liver by CYP3A4. Elimination:
Primarily in urine; some in feces. Half-Life:
Assessment & Drug Effects
- Monitor cardiac status, especially when large doses are given.
- Monitor for and report numbness and tingling of fingers and toes, extremity weakness, muscle pain, or intermittent claudication.
Patient & Family Education
- Take at first warning of migraine headache.
- Lie down in a quiet, darkened room for several hours after drug administration for best results.
- Report immediately if any of the following S&S develop: Chest pain, nausea, vomiting, change in heartbeat, numbness, tingling,
pain or weakness of extremities, edema, or itching.