Laropiprant

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Laropiprant
File:Laropiprant.png
Systematic (IUPAC) name
(-)-[(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]
Routes of
administration		 Oral
Identifiers
CAS Number 571170-77-9
ATC code C10AD52 (WHO)
(combination with niacin)
Synonyms MK-0524A
Chemical data
Formula C21H19ClFNO4S
Molar mass 435.90 g/mol[[Script error: No such module "String".]]
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Laropiprant (INN) is used in combination with niacin to reduce blood cholesterol (LDL and VLDL). Merck & Co. planned to market this combination under the trade names Cordaptive and Tredaptive. On April 28, 2008, the U.S. Food and Drug Administration (FDA) issued a "not approved" letter for Cordaptive.[1] Tredaptive was approved by the European Medicines Agency (EMA) on July 3, 2008.[2]

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.[3]

Tredaptive contains 1000 mg of niacin and 20 mg of laropiprant in each tablet.[4]

Mechanism 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.[4][5]

Laropiprant acts as a DP1 antagonist, reducing the vasodilation.[4]

Taking 650 mg of aspirin 20–30 minutes prior to taking niacin has also been proven to prevent flushing in 90% of patients, presumably by suppressing prostaglandin synthesis,[6] but this medication also increases the risk of gastrointestinal bleeding,[7] though the increased risk is less than 1 percent.[8]

References

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GI tract
Liver
Niacin and derivatives (HDL and LDL)
Blood vessels
Combinations
Other

M: MET

mt, a/u/y/n/h, r/g/c/p/i, f/s/l/o, m

au/y/n/h, rgcp/i, f/s/l/o, m, epon

meds(A16, C10),intm(a/u/y/n/h, r/g/c/p/i, f/s/o)


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da:Tredaptive
  1. Jump up ↑ Carey, John (April 29, 2008). "FDA Rejects Merck's Cordaptive". BusinessWeek. Retrieved 2009-11-13. 
  2. Jump up ↑ "Tredaptive European Public Assessment Report". European Medicines Agency. Retrieved November 13, 2009. 
  3. Jump up ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  4. ↑ Jump up to: 4.0 4.1 4.2 "Tredaptive Prescribing Information" (PDF). Merck & Co. Retrieved 2009-11-14. 
  5. Jump up ↑ Sood, A.; Arora, R. (2009). "Mechanisms of Flushing Due to Niacin and Abolition of These Effects". The Journal of Clinical Hypertension. 11 (11): 685. doi:10.1111/j.1559-4572.2008.00050.x. PMID 19878384.  edit
  6. Jump up ↑ Richard A. Kunin (1976). "The Action of Aspirin in Preventing the Niacin Flush and its Relevance to the Antischizophrenic Action of Megadose Niacin" (PDF). Orthomolecular Psychiatry. 5 (2): 89–100. Retrieved 2009-11-14. 
  7. Jump up ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  8. Jump up ↑ [1][dead link]
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