$200.00 – $450.00
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.
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.
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.
30 TABLETS, 60 TABLETS, 90 TABLETS, 120 TABLETS