Rizatriptan Chemical Properties

Melting point:

178-180°C

Boiling point:

504.8±60.0 °C(Predicted)

Density 

1.21±0.1 g/cm3(Predicted)

storage temp. 

under inert gas (nitrogen or Argon) at 2-8°C

pka

16.98±0.30(Predicted)

Water Solubility 

42 mg/mL

CAS DataBase Reference

144034-80-0(CAS DataBase Reference)

EPA Substance Registry System

Acetonitrile, 2,2-dibromo-2-chloro- (144034-80-0)

Rizatriptan Usage And Synthesis

Uses

Rizatriptan is reported to be a very effective acute migraine drug. It is reported to display high agonist activity at mainly the serotonin 5-HT1B and 5-HT1D receptor subtypes.

Uses

Ca channel blocker

Definition

ChEBI: Rizatriptan is a member of tryptamines. It has a role as a serotonergic agonist, a vasoconstrictor agent and an anti-inflammatory drug. It is functionally related to a N,N-dimethyltryptamine.

brand name

Maxalt (Merck).

General Description

Rizatriptan, approved in 1998, is a fast-acting triptan becauseof its moderate lipophilicity yet has a very shortelimination half-life similar to sumatriptan (i.e., like sumatriptan,it is mainly metabolized by MAO-A). The only advantagesof this drug when compared with sumatriptan arethat it has a slightly faster onset and that it has an orallydisintegrating tablet formulation which can be taken withoutwater.

Clinical Use

5HT1 receptor agonist:
Acute treatment of migraine

Drug interactions

Potentially hazardous interactions with other drugs
Antidepressants: increased risk of CNS excitation with citalopram - avoid; risk of CNS toxicity with MAOIs, moclobemide and linezolid - avoid for 2 weeks after discontinuation of MAOI and moclobemide; possibly increased serotonergic effects with duloxetine and venlafaxine; increased serotonergic effects with St John’s wort - avoid.
Dapoxetine: possible increased risk of serotonergic effects - avoid for 2 weeks after stopping 5HT1 agonists.
Ergot alkaloids: increased risk of vasospasm - avoid.
Propranolol: rizatriptan levels increased, reduce dose of rizatriptan to 5 mg (max 10 mg in 24 hours).

Metabolism

The main route of rizatriptan metabolism is via oxidative deamination by monoamine oxidase-A (MAO-A) to the indole acetic acid metabolite, which is not pharmacologically active. N-monodesmethyl-rizatriptan, a metabolite with activity similar to that of parent compound, is formed to a minor degree, but does not contribute significantly to the pharmacodynamic activity of rizatriptan.
Less than 1% is excreted in the urine as active N-monodesmethyl metabolite.

Rizatriptan(144034-80-0)Related Product Information

• Zolmitriptan
• Dacthal
• Dimethyl fumarate
• Dimethyl sulfate
• Dimethyl sulfoxide
• Almotriptan
• Dimethyl disulfide
• 1H-Benzotriazole
• Indole
• Dimethyl ether
• 5-Methyl-1H-benzotriazole
• Sumatriptan
• ETHANE
• Dimethyl phthalate
• Dimethyl carbonate
• N,N-Dimethylformamide
• 1,2,4-Triazole
• Voriconazole