Suppression of Niacin-induced Vasodilation with an Antagonist to Prostaglandin D2 Receptor Subtype 1
| Autor: | Fang Liu, Eseng Lai, E Vets, Larissa Wenning, Gary P. O'Neill, Nicole Michiels, Tami Crumley, I De Lepeleire, Keith Gottesdiener, John A. Wagner |
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| Rok vydání: | 2007 |
| Předmět: |
Adult
Male medicine.medical_specialty Indoles Adolescent Vasodilator Agents Receptors Prostaglandin Prostaglandin Vasodilation Pharmacology Niacin chemistry.chemical_compound Internal medicine medicine Humans Pharmacology (medical) Receptors Immunologic Skin Prostaglandin D2 receptor Cross-Over Studies Aspirin Dose-Response Relationship Drug Chemistry digestive oral and skin physiology Antagonist food and beverages nutritional and metabolic diseases Middle Aged Prostaglandin antagonist B vitamins Endocrinology Regional Blood Flow Delayed-Action Preparations Female Laropiprant |
| Zdroj: | Clinical Pharmacology & Therapeutics. 81:849-857 |
| ISSN: | 1532-6535 0009-9236 |
| Popis: | Niacin (nicotinic acid) reduces cardiovascular events in patients with dyslipidemia. However, symptoms associated with niacin-induced vasodilation (e.g., flushing) have limited its use. Laropiprant is a selective antagonist of the prostaglandin D(2) receptor subtype 1 (DP1), which may mediate niacin-induced vasodilation. The aim of this proof-of-concept study was to evaluate the effects of laropiprant (vs placebo) on niacin-induced cutaneous vasodilation. Coadministration of laropiprant 30, 100, and 300 mg with extended-release (ER) niacin significantly lowered flushing symptom scores (by approximately 50% or more) and also significantly reduced malar skin blood flow measured by laser Doppler perfusion imaging. Laropiprant was effective after multiple doses in reducing symptoms of flushing and attenuating the increased malar skin blood flow induced by ER niacin. In conclusion, the DP1 receptor antagonist laropiprant was effective in suppressing both subjective and objective manifestations of niacin-induced vasodilation. |
| Databáze: | OpenAIRE |
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