Acipimox C₆H₆N₂O₃

Pharmacodynamic properties

Acipimox inhibits the release of fatty acids from adipose tissue and reduces the blood concentrations of very low density lipoproteins (VLDL or Pre-beta) and low density lipoproteins (LDL or beta) with a subsequent overall reduction in triglyceride and cholesterol levels.

Acipimox also has a favourable effect on high density lipoproteins (HDL or alpha) which increase during treatment.

Pharmacokinetic properties

Acipimox is rapidly and completely absorbed orally, reaching peak plasma levels within two hours. The half-life is about two hours. It does not bind to plasma proteins; it is not significantly metabolised and is eliminated almost completely intact by the urinary route.

Preclinical safety data

Nonclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology and repeat-dose toxicity, carcinogenicity and mutagenicity.

There is no evidence from the animal studies that acipimox is teratogenic. However, a higher incidence of immature and underweight foetuses was seen in pregnant animals given higher doses of acipimox. This effect may be due to maternal toxicity.

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