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Dihydroergotamine: profile and news
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May 2, 2005 Abbott Receives FDA Approval for a Once-Daily Kaletra(R)-Based ... May 2, 2005 Intranasal delivery Mar 11, 2005 Other information 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. Mechanism Of Action Two theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in migraine: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release. Drug Category Analgesics; Vasoconstrictor Agents; Sympatholytics; ATC:N02CA01 Brand Names/Synonyms Ergotamine, 9,10-dihydro-; Dihydroergotaminum [INN-Latin]; Dihidroergotamina [INN-Spanish]; D.H.E.; D.H.E. 45; Agit; Angionorm; D.H.E. 45; DET MS; DHE-45; Dergotamine; Diergo; Dihydergot; Dihydroergotamine; Dihydroergotamine mesylate; Dihydroergotamine methanesulfonate; Dihydroergotamine monomethanesulfonate; Dirgotarl; Endophleban; Ergomimet; Ergont; Ergotonin; Ikaran; Migranal; Morena; Orstanorm; Tonopres; Verladyn Dosage Forms LIQUID Absorption Interpatient variable and may be dependent on the administration technique Interactions Interactions for Dihydroergotamine: Vasoconstrictors: D.H.E. 45 (dihydroergotamine mesylate) injection, USP should not be used with peripheral vasoconstrictors because the combination may cause synergistic elevation of blood pressure. Sumatriptan: Sumatriptan has been reported to cause coronary artery vasospasm, and its effect could be additive with D.H.E. 45 (dihydroergotamine mesylate) injection, USP. Sumatriptan and D.H.E. 45 (dihydroergotamine mesylate) injection, USP should not be taken within 24 hours of each other. Beta Blockers: Although the results of a clinical study did not indicate a safe problem associated with the administration of D.H.E. 45 (dihydroergotamine mesylate) injection, USP to subjects already receiving propranolol, there have been reports that propranolol may potentiate the vasoconstrictive action of ergotamine by blocking the vasodilating property of epinephrine. Nicotine: Nicotine may provoke vasoconstriction in some patients, predisposing to a greater ischemic response to ergot therapy. Macrolide Antibiotics (e. g. erythromycin and troleandomycin): Agents of the ergot alkaloid class, of which D.H.E. 45 (dihydroergotamine mesylate) injection, USP is a member, have been shown to interact with antibiotics of the macrolide class, resulting in increased plasma levels of unchanged alkaloids and peripheral vasoconstriction. Vasospastic reactions have been reported with therapeutic doses of ergotamine-containing drugs when co-administered with these antibiotics. SSRI's: Weakness hyperreflexia, and incoordination have been reported rarely when 5-HT1 agonists have been co-administered with SSRI's (e.g. fluoxetine, fluvoxamine, paroxetine, sertraline). There have been no reported cases from spontaneous reports of drug interaction between SSRI's and D.H.E. 45 (dihydroergotamine mesylate) injection, USP. Oral Contraceptives: The effect of oral contraceptives on the pharmacokinetics of D.H.E. 45 (dihydroergotamine mesylate) injection, USP has not been studied. Chemical IUPAC Name Not Available Chemical Formula C33H37N5O5 Half Life 9 hours Drug Type Approved Drug # Accession No APRD00476 CAS Registry Number 6190-39-2 |
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