Rizatriptan Property

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)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H319Causes serious eye irritation

H336May cause drowsiness or dizziness

H361Suspected of damaging fertility or the unborn child

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P281Use personal protective equipment as required.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P308+P313IF exposed or concerned: Get medical advice/attention.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P314Get medical advice/attention if you feel unwell.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

Rizatriptan Chemical Properties,Usage,Production

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.