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Drug Detailed Description (Generic name) - Dihydroergotamine Mesylate


DIHYDROERGOTAMINE MESYLATE

Pharmacology

Dihydroergotamine (DHE) is a semisynthetic ergot alkaloid that is hypothesized to exert its antimigraine effect via its agonist activity at the sero-tonin 5-HT1D receptor, resulting in vasoconstriction of intracranial blood vessels and inhibition of inflammatory neuropeptide release.The drug also binds with high affinity to adrenergic and dopamine receptors; however, the antimigraine ef-fect of these events is unknown. Compared with ergotamine, DHE is a weaker vasoconstrictor, is less active as an emetic, and is less oxytocic.

Administration and Adult Dosage

IM 1 mg initially, then 1 mg q 1 hr prn, to a maximum of 3 mg/day or 6 mg/week. IV (for rapid effect) 0.5–1 mg, may repeat in 1 hr to a maximum of 2 mg/day or 6 mg/week. Consider administering meto-clopramide 10 mg IV before DHE to treat nausea due to migraine and prevent nausea due to the drug.Intranasal one spray (0.5 mg) into each nostril; may re-peat in 15 min to a maximum of 2 mg over 24 hr.

Special Populations

Pediatric Dosage

Safety and efficacy not established.

Geriatric Dosage

Same as adult dosage.

Dosage Forms

Inj 1 mg/mL; Nasal Spray 4 mg/mL.

Patient Instructions

This drug can cause numbness and tingling in fingers, toes, or face. Notify your physician if you are pregnant or have heart disease or high blood pressure. Do not exceed the maximum dosage. The nasal spray can cause local irritation. Do not reuse the applicator; use the solution right after opening. Review training materials with your health care provider and report the use of all cold or allergy medications and all over-the-counter medications.

Pharmacokinetics

Onset and Duration. Onset under 5 min IV, within 15–30 min after IM or intranasal spray; duration 3–4 hr. Intranasal 50–70% of patients respond in 4 hr.

Fate

The drug is absorbed directly into the systemic circulation when administered intranasally, but it undergoes extensive first-pass metabolism if given orally. Bio-availability of the nasal spray is 38 ± 16%, variable depending on self-administration technique.Protein binding is 93%. After administration of 1 mg, peak levels are 1 ± 0.4 µg/L (intranasal) and 4.4 µg/L (IM), occurring at 0.9 ± 0.6 hr (intranasal) and 0.4 ± 0.3 hr (IM).After IM administration, Vc is 12 ± 4 L/kg, and Vd is 33 ± 0.2 L/kg, suggesting distribution into deep tissue compartments. Cl is 1.6 ± 0.17 L/hr/kg. The drug is metabolized to at least 5 metabolites, 3 of which are active. The major route of excretion for DHE and its metabolites is in the feces via the bile. t¹/2. phase (intranasal) 1 ± 0.5 hr, (IM) 0.9 ± 0.3 hr; phase (intranasal) 7.9 ± 4 hr, (IM) 7.2 ± 2.2 hr.

Adverse Reactions

The most frequently reported adverse events with intranasal administration are rhinitis, pharyngitis, altered sense of taste, application site reac-tions, nausea, vomiting, and dizziness. With all routes of administration, nausea, vomiting, diarrhea, and localized edema occur frequently.Numbness and tingling of fingers and toes, muscle pain in extremities, weakness in legs, pruritus, rash, and infection occur occasionally. Pleural and retroperitoneal fibrosis occur rarely with prolonged use.

Contraindications

Pregnancy and lactation; peripheral vascular disease; coro-nary artery disease; ischemic heart disease; hemiplegic or basilar migraine; sepsis; recent history of vascular surgery; severely impaired hepatic or renal function; hy-persensitivity to ergot alkaloids.

Precautions

Use caution to avoid overuse by patients with chronic vascular headaches. Patients with risk factors for coronary artery disease should undergo periodic cardiovascular evaluation.

Drug Interactions

is worsened with co-administration of DHE. Macrolides in-cluding erythromycin can increase the risk of ergot toxicity. Sumatriptan can ex-acerbate coronary artery vasospasm and should not be taken within 24 hr of DHE. SSRIs can cause weakness, hyperreflexia, or incoordination.

Notes

IV DHE is used when oral agents have failed to abort migraine and for ter-minating cluster or migraine headache in an emergency setting. It is not intended for prophylaxis or the management of hemiplegic or basilar migraine. The in-tranasal preparation is a noninvasive option for outpatients. Intranasal administra-tion also results in improved bioavailability over the oral form because it does not undergo a first-pass effect in the liver. DHE does not cause physical dependence and is associated with a more favorable side effect profile than ergotamine, espe-cially with regard to GI and peripheral vascular effects. In one study, subcuta-neously administered sumatriptan appeared to be more effective than DHE nasal spray; however, DHE was better tolerated.
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