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Almotriptan
drug data and news
Almotriptan 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 | Almotriptan | ||
| Brand Names/Synonyms | Almotriptan; Axert; Eletriptan | ||
| Indication | For the treatment of acute migraine headache in adults | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT1D family) having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almotriptan in humans. | ||
| Mechanism Of Action | Almotriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. | ||
| Almotriptan News (When available) |
Switching 'triptans' may improve migraine response Sep 9, 2005 Tripos’ program accelerates drug discovery Aug 15, 2005 Triptan Nonresponder Studies: Implications for Clinical Practice Mar 7, 2005 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Anti-migraine Agents; Anti-inflammatory Agents; Vasoconstrictor Agents; Selective Serotonin Agonists; ATC:N02CC05 | ||
| Absorption | Not Available | ||
| Interactions |
-->Interactions for Almotriptan: Ergot-Containing Drugs These drugs have been reported to cause prolonged vasospastic reactions. Because there is a theoretical basis that these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and AXERT® within 24 hours of each other should be avoided. Monoamine Oxidase Inhibitors Coadministration of moclobemide resulted in a 27% decrease in almotriptan clearance and an increase in Cmax of approximately 6%. No dose adjustment is necessary. Other 5-HT1B/1D Agonists Concomitant use of other 5-HT1B/1D agonists within 24 hours of treatment with AXERT® is contraindicated. Propanolol The pharmacokinetics of almotriptan were not affected by coadministration of propranolol. Selective Serotonin Reuptake Inhibitors (SSRIs) SSRIs (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline) have been rarely reported to cause weakness, hyperreflexia, and incoordination when coadministered with 5-HT1 agonists. If concomitant treatment with AXERT® and an SSRI is clinically warranted, appropriate observation of the patient is advised. Verapamil Coadministration of almotriptan and verapamil resulted in a 24% increase in plasma concentrations of almotriptan. No dose adjustment is necessary. Ketoconazole and Other Potent CYP3A4 Inhibitors Coadministration of almotriptan and the potent CYP3A4 inhibitor ketoconazole (400 mg q.d. for 3 days) resulted in an approximately 60% increase in the area under the plasma concentration-time curve and maximal plasma concentrations of almotriptan. Although the interaction between almotriptan and other potent CYP3A4 inhibitors (e.g., itraconazole, ritonavir, and erythromycin) has not been studied, increased exposures to almotriptan may be expected when almotriptan is used concomitantly with these medications. Drug/Laboratory Test Interactions AXERT® is not known to interfere with commonly employed clinical laboratory tests. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]-ethanamine | ||
| Chemical Formula | C17H25N3O2S | ||
| Molecular Weight | 335.465 g/mol | ||
| Smiles String | CN(C)CCC1=CNC2=C1C=C(C=C2)CS(=O)(=O)N3CCCC3 | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 1.87 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 3-4 hours | ||
| Protein Binding [%] | 35% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Almotriptan.html http://www.rxlist.com/cgi/generic2/almotriptan.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00169 | ||
| CAS Registry Number | 181183-52-8 | ||
| KEGG Compound ID | Not Available | ||
| PubChem ID | SID:700325 | ||
| PharmGKB ID | PA10246 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2248128 |
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