アルモトリプタン

Pharmaceuticals -> Listed in ZINC15

Pharmaceuticals

1.6

1.6

Breast Feeding; Lactation; Milk, Human; Serotonin Receptor Agonists; Serotonin 5-HT1 Receptor Agonists; Triptans; Vasoconstrictor Agents

Pharmaceuticals

Warning

H373 (100%): May causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]

P260, P319, and P501 (click each P-code to see the statement)

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Gastrointestinal decontamination (i.e., gastric lavage followed by activated charcoal) should be considered in patients suspected of an overdose with Almotriptan. Clinical and electrocardiographic monitoring should be continued for at least 20 hours, even if clinical symptoms are not observed. (L1712)

The common adverse effects of almotriptan are drowsiness, dizziness, headache, nausea, vomiting, chest pain, and fatigue. The drug is associated with a similar incidence of nausea or vomiting compared to other classes of triptans (eg, sumatriptan). However, it shows a decreased incidence of common adverse effects, especially compared to first-generation triptans.

There are no associated toxicities with almotriptan due to the limited data, although studies demonstrate increased preterm birth rates in pregnant women who were prescribed triptans for migraine relief.

Almotriptan binds with high affinity to human 5-HT_1B and 5-HT_1D receptors leading to cranial blood vessel constriction.

N02CC05

N - Nervous system

QN - Nervous system

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-HT_1D family) having only a weak affinity for 5-HT_1A, 5-HT_5A, 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.

Almotriptan has known human metabolites that include 2-hydroxy-almotriptan and methyl(2-{5-[(pyrrolidine-1-sulfonyl)methyl]-1H-indol-3-yl}ethyl)amine.

Hepatic. Route of Elimination: Almotriptan is eliminated primarily by renal excretion (about 75% of the oral dose), with approximately 40% of an administered dose excreted unchanged in urine. Approximately 13% of the administered dose is excreted via feces, both unchanged and metabolized. Half Life: 3-4 hours