Laropiprant

This MedLibrary.org supplementary page on Laropiprant is provided directly from the open source Wikipedia as a service to our readers. Please see the note below on authorship of this content, as well as the Wikipedia usage guidelines. To search for other content from our encyclopedia supplement, please use the form below:

Related Sponsors

BM Pharmacy Generic pharmaceuticals at unbeatable prices. Insomnia, men's health, hair health, pain control. bmpharmacy.com
Online Pharmacy Carisoprodol, tadalafil, sildenafil, vardenafil and more... xlpharmacy.com
MedBasket.com Discreet. Inexpensive. Fast shipping. Great selection. What more can we say? medbasket.com
Frugalmed 2000 reasons to shop with us first. frugalmed.com
Ads by Tiva

Laropiprant
Systematic (IUPAC) name
(-)-[(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
Identifiers
CAS number 571170-77-9
ATC code  ?
PubChem  ?
Chemical data
Formula C21H19ClFNO4S 
Mol. mass 435.90 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Licence data

EU
Pregnancy cat.

?
Legal status
Routes Oral

Laropiprant (pINN; codenamed MK-0524A) is tested in combination with niacin to reduce blood cholesterol (LDL and VLDL). This combination will be marketed by Merck & Co. under the tradenames Cordaptive and Tredaptive.

Laropiprant itself has no cholesterol lowering effect, but it reduces facial flushes induced by niacin. In a trial with 1613 patients, 10.2% patients stopped taking the medication in the Cordaptive group versus 22.2% under niacin monotherapy.[1]

Method of action

Niacin in cholesterol lowering doses (500-2000 mg per day) causes facial flushes by stimulating biosynthesis of prostaglandin D2, especially in the skin. PG D2 acts as a vasodilator via DP1 receptors, increasing blood flow and thus leading to flushes.

Laropiprant acts as a DP1 antagonist, reducing the vasodilation.

References

  1. ^ E Lai et al (2007). "Suppression of Niacin-induced Vasodilation with an Antagonist to Prostaglandin D2 Receptor Subtype 1". Clinical Pharmacology & Therapeutics 81: 849-857. 
Tablets  This pharmacology-related article is a stub. You can help Wikipedia by expanding it.
v • d • e
Lipid modifying agents (C10)
Statins (HMG-CoA reductase)
Fibrates (PPAR)
Bile acid sequestrants
Niacin and derivatives
CETP inhibitors
Combinations
Other
†Undergoing clinical trials. ‡Withdrawn from market. §Development terminated.

Wikipedia content modification information:

  • This page was last modified on 25 August 2008, at 18:24.

Wikipedia Authorship and Review

Wikipedia content provided here is not reviewed directly by MedLibrary.org. Wikipedia content is authored by an open community of volunteers and is not produced by or in any way affiliated with MedLibrary.org.

Wikipedia Usage Guidelines

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article on "Laropiprant".

The URL for this specific entry is:

All Wikipedia text is available under the terms of the GNU Free Documentation License. (See Copyrights for details). Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc.