Dosing and uses of D.H.E. 45 (dihydroergotamine)
Adult dosage forms and strengths
injectable solution
- 1mg/mL
Migraine & Cluster Headaches
Indicated for acute treatment of migraine headaches with or without aura, and acute treatment of cluster headache episodes
1 mg IV/IM/SQ q1hr PRN; not to exceed 2 mg IV or 3 mg IM/SC per 24-hr period
Not to exceed 6 mg qWeek
Do not use for chronic daily administration
Pediatric dosage forms and strengths
Safety and efficacy not established
D.H.E. 45 (dihydroergotamine) adverse (side) effects
Frequency not defined
Common
- Dizziness
- Paresthesia
- Nausea
- Vomiting
- Taste sense altered, Nasal spray
- Nasal irritation
- Throat irritation
Serious
- Peripheral ischemia (rare)
- Vasospasm
- Tachycardia
- Cerebrovascular disease
- Ergotism (rare)
Warnings
Black box warnings
Serious and/or life-threatening peripheral ischemia has been reported with coadministration of this drug with potent CYP 3A4 inhibitors (including protease inhibitors and macrolide antibiotics)
Because CYP3A4 inhibition elevates the serum ergotamine levels, the risk of vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased
Concurrent use of potent CYP3A4 inhibitors is contraindicated
Contraindications
Hypersensitivity
Peripheral vascular disease, severe hepatic/renal impairment, ischemic heart disease, uncontrolled hypertension, sepsis, pregnancy, breastfeeding women
Recent vascular surgery
Hemiplegic or basilar migraine
Coadministration with potent CYP3A4 inhibitors
Peripheral or central vasoconstrictors
Caution
Coadministration with less potent CYP3A4 inhibitors
Fibrotic complications reported (pleural and retroperitoneal fibrosis with prolonged parenteral use)
May cause coronary vasospasm
Avoid in patients with unrecognized CAD (ie, patient with risk factors)
May cause vasospastic reactions including myocardial, peripheral vascular, and colonic ischemia
May elevate blood pressure
Pregnancy and lactation
Pregnancy category: X
Lactation: Contraindicated; excreted in human milk and is known to inhibit prolactin
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of D.H.E. 45 (dihydroergotamine)
Mechanism of action
Binds with high affinity to 5-HT-1Dα and 5-HT-1Dβ; also bind to serotonin 5-HT-1A, -2A, and -2C receptors, noradrenaline α2A, α2B, and alpha receptors, and dopamine D2L and D3 receptors
Therapeutic activity attributed to agonist effect at 5-HT-1D receptors, which includes vasoconstriction of intracranial blood vessels, or activation of 5-HT1D may inhibit proinflammatory neuropeptide release
Pharmacokinetics
Half-Life: 28 hr
Protein Bound: 93%
Metabolism: liver, by CYP3A4
Excretion: mainly in feces; urine: <10%
Onset
- IM: 15-30 min
- IV: <5 minIntranasal: 30 min
Duration
- IM: 3-4 hr
- SC/IV: 8 hr
Administration
IV/IM Administration
Administer by IM, IV, or SC injection
IV: 1 mg or fraction thereof over 1 min
After the initial dose is administered, patient should lie down & relax in a quiet, darkened room
Should not be used for chronic daily administration
Storage
Store below 25°C (77°F)
Do not refrigerate or freeze
