Laropiprant
Encyclopedia
Laropiprant 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. Tredaptive was approved by the European Medicines Agency
(EMA) on July 3, 2008.
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.
Tredaptive contains 1000 mg of niacin and 20 mg of laropiprant in each tablet.
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.
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, but this medication also increases the risk of gastrointestinal bleeding
, though the increased risk is less than 1 percent.
Niacin
"Niacin" redirects here. For the neo-fusion band, see Niacin .Niacin is an organic compound with the formula and, depending on the definition used, one of the forty to eighty essential human nutrients.Niacin is one of five vitamins associated with a pandemic deficiency disease: niacin deficiency...
to reduce blood cholesterol (LDL and VLDL). Merck & Co.
Merck & Co.
Merck & Co., Inc. , also known as Merck Sharp & Dohme or MSD outside the United States and Canada, is one of the largest pharmaceutical companies in the world. The Merck headquarters is located in Whitehouse Station, New Jersey, an unincorporated area in Readington Township...
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. Tredaptive was approved by the European Medicines Agency
European Medicines Agency
The European Medicines Agency is a European agency for the evaluation of medicinal products. From 1995 to 2004, the European Medicines Agency was known as European Agency for the Evaluation of Medicinal Products.Roughly parallel to the U.S...
(EMA) on July 3, 2008.
Laropiprant itself has no cholesterol lowering effect, but it reduces facial flushes
Flushing (physiology)
For a person to flush is to become markedly red in the face and often other areas of the skin, from various physiological conditions. Flushing is generally distinguished, despite a close physiological relation between them, from blushing, which is milder, generally restricted to the face, cheeks or...
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.
Tredaptive contains 1000 mg of niacin and 20 mg of laropiprant in each tablet.
Mechanism of action
Niacin in cholesterol lowering doses (500–2000 mg per day) causes facial flushes by stimulating biosynthesis of prostaglandinProstaglandin
A prostaglandin is any member of a group of lipid compounds that are derived enzymatically from fatty acids and have important functions in the animal body. Every prostaglandin contains 20 carbon atoms, including a 5-carbon ring....
D2, especially in the skin. PG D2 acts as a vasodilator via DP1 receptors
Prostaglandin D2 receptor
Prostaglandin D2 receptor is a G-protein coupled receptor, encoded by the PTGDR gene, for prostaglandin D2.-Mechanism:DP1 is a G-protein-coupled receptor...
, increasing blood flow and thus leading to flushes.
Laropiprant acts as a DP1 antagonist, reducing the vasodilation.
Taking 650 mg of aspirin
Aspirin
Aspirin , also known as acetylsalicylic acid , is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. It was discovered by Arthur Eichengrun, a chemist with the German company Bayer...
20–30 minutes prior to taking niacin has also been proven to prevent flushing in 90% of patients, presumably by suppressing prostaglandin synthesis, but this medication also increases the risk of gastrointestinal bleeding
Gastrointestinal bleeding
Gastrointestinal bleeding or gastrointestinal hemorrhage describes every form of hemorrhage in the gastrointestinal tract, from the pharynx to the rectum. It has diverse causes, and a medical history, as well as physical examination, generally distinguishes between the main forms...
, though the increased risk is less than 1 percent.