axert medication

axert medication AXERT® (almotriptan malate) Tablets contain almotriptan malate, a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist. Firstly, Almotriptan malate is chemically designated as 1-[[[3-[2-(Dimethylamino)ethyl]-1H-indol5-yl]methyl]sulfonyl]pyrrolidine (±)-hydroxybutanedioate (1:1), and its structural formula is: Its empirical formula is C17H25N3O2S-C4H6O5, representing a molecular weight of 469.56. Almotriptan is a white to slightly yellow crystalline powder that is soluble in water.Secondly,  AXERT® for oral administration contains almotriptan malate equivalent to 6.25 or 12.5 mg of almotriptan. Thirdly, and most importantly, Each compressed tablet contains the following inactive ingredients: mannitol, cellulose, povidone, sodium starch glycolate, sodium stearyl fumarate, titanium dioxide, hypromellose, polyethylene glycol, propylene glycol, iron oxide (6.25 mg only), FD&C Blue No. 2 (12.5 mg only), and carnauba wax.

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CLINICAL PHARMACOLOGY
Mechanism of Action
Moreover, Almotriptan binds with high affinity to 5-HT1D, 5-HT1B, and 5-HT1F receptors. Almotriptan has weak affinity for 5-HT1A and 5-HT7 receptors, but has no significant affinity or pharmacological activity at 5-HT2, 5-HT3, 5-HT4, 5-HT6; alpha or beta adrenergic; adenosine (A1, A2); angiotensin (AT1, AT2); dopamine (D1, D2); endothelin (ETA, ETB); or tachykinin (NK1, NK2, NK3) binding sites. Current theories on the etiology of migraine headaches.

suggest that symptoms are due to local cranial vasodilatation and/or to the release of vasoactive and pro-inflammatory peptides from sensory nerve endings in an activated trigeminal system. The therapeutic activity of almotriptan in migraine can most likely be 1 attribute to agonist effects at 5-HT1B/1D receptors on the extracerebral, intracranial blood vessels that become dilated during a migraine attack, and on nerve terminals in the trigeminal system. Activation of these receptors results in cranial vessel constriction, inhibition of neuropeptide release, and reduced transmission in trigeminal pain pathways.

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Pharmacokinetics
General
However,  Almotriptan is well absorbe after oral administration (absolute bioavailability about 70%) with peak plasma levels 1 to 3 hours after administration; food does not affect pharmacokinetics. Almotriptan has a mean half-life of 3 to 4 hours.
It is eliminate primarily by renal excretion (about 75% of the oral dose).
In conclusion, Almotriptan is minimally protein bound (approximately 35%) and the mean apparent
volume of distribution is approximately 180 to 200 liters.