| Indication |
For the treatment of acute migraine headache in adults |
| Pharmacodynamics |
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. |
| Absorption |
Not Available |
| Volume of distribution |
|
| Protein binding |
35% |
| Metabolism |
Not Available |
| 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 |
| Clearance |
- 57 L/h [healthy]
- 34.2 L/h [moderate renal impairment (creatinine clearance between 31 and 71 mL/min)]
- 9.8 L/h [severe renal impairment (creatinine clearance between 10 and 30 mL/min)]
|
| Toxicity |
Not Available |
