| Item |
Information |
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Drug Groups
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approved |
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Description
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A 9,10alpha-dihydro derivative of ergotamine. It is used as a vasoconstrictor, specifically for the therapy of migraine disorders. [PubChem] |
| Indication |
For the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. |
| Pharmacology |
Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. Dihydroergotamine binds with high affinity to 5-HT1Da and 5-HT1Db receptors. It also binds with high affinity to serotonin 5-HT1A, 5-HT2A, and 5-HT2C receptors, noradrenaline a2A, a2B and a receptors, and dopamine D2L and D3 receptors. The therapeutic activity of Dihydroergotamine in migraine is generally attributed to the agonist effect at 5-HT1D receptors. |
| Toxicity |
Side effects include abdominal pain, abnormal speech, coma, confusion, convulsions, hallucinations, increase and/or decrease in blood pressure, nausea, numbness, tingling, pain, and a bluish color of your fingersand toes, slowed breathing, vomiting |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Hepatic |
| Absorption |
Interpatient variable and may be dependent on the administration technique |
| Half Life |
9 hours |
| Protein Binding |
93% (to plasma proteins) |
| Elimination |
The major excretory route of dihydroergotamine is via the bile in the feces.
Only 6%-7% of unchanged dihydroergotamine is excreted in the urine after intramuscular injection. |
| Distribution |
* 800 L |
| Clearance |
* 1.5 L/min |
| External Links |
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