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Dihydroergotamine
drug data and news
Dihydroergotamine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Dihydroergotamine | ||
| 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 | ||
| Indication | For the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Dihydroergotamine News (When available) |
Mechanically stimulating the heart Feb 23, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... Feb 9, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... 09 Feb 2006 New Data Show a Kaletra(R) (Lopinavir/Ritonavir)-Based Regimen ... Nov 18, 2005 Boehringer Ingelheim Announces 48-Week Results from Aptivus(R) ... Nov 21, 2005 Kaletra ® may provide convenient dosages in HIV treatment regime Jul 31, 2005 Abbott Statement on Agreement With Brazilian Government for ... 11 Jul 2005 Valeant Pharmaceuticals Introduces Redesigned Migranal Delivery ... Jun 27, 2005 Valeant Pharmaceuticals Introduces Redesigned Migranal Delivery ... Jun 27, 2005 Valeant Pharmaceuticals Introduces Redesigned Migranal Delivery ... 13 Sep 2002 Research Seeking To Prevent Menstrually-Related Migraine Headaches May 31, 2005 Ergot Compound Not as Effective as Triptans for Migraine May 5, 2005 Abbott Receives FDA Approval for a Once-Daily Kaletra(R)-Based ... May 2, 2005 Abbott Receives FDA Approval for a Once-Daily Kaletra(R)-Based ... May 2, 2005 Intranasal delivery Mar 11, 2005 | ||
| Dosage Forms | LIQUID | ||
| Drug_Category | Analgesics; Vasoconstrictor Agents; Sympatholytics; ATC:N02CA01 | ||
| 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. | ||
| 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 | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C33H37N5O5 | ||
| Molecular Weight | 583.678 g/mol | ||
| Smiles String | CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | Not Available | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 9 hours | ||
| Protein Binding [%] | 93% (to plasma proteins) | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mig1267.shtml http://www.drugs.com/cons/Dihydroergotamine.html http://www.rxlist.com/cgi/generic2/dihyergmes.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00476 | ||
| CAS Registry Number | 6190-39-2 | ||
| KEGG Compound ID | C07798 | ||
| PubChem ID | SID:153817 | ||
| PharmGKB ID | PA449327 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2241163 |
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