A study of some acute pharmacodynamic effects of pentaerythritoltetranicotinate (Perycit�) in man

Abstract

The nicotinic acid ester, pentaerythritol-tetranicotinate orally administered in a dose of 1 g produced a moderate but sustained level (≈ 1 μg/ml) of free nicotinic acid in plasma. The concentration of esterbound nicotinic acid increased in plasma too. The increased nicotinic acid concentration in plasma was accompanied by a significant and protracted increase of the blood-flow of the forearm and hand and a decrease of the FFA-content of plasma. A weak flush of the face and the upper part of the body occurred as long as the nicotinic acid concentration of plasma was increasing. Repeated doses of pentaerythritoltetranicotinate at short intervals (30 min) produced a larger increase of the nicotinic acid concentration in plasma but the pharmacological effects did not increase. This was in agreement with earlier results that already a plasma concentration of 0.3–0.4 μg/ml of nicotinic acid produced almost maximum pharmacological effects. Only the effect on the blood-flow of the forearm was significantly greater when the nicotinic acid dose and nicotinic acid level of plasma was further raised. It was calculated that 1 g pentaerythritoltetranicotinate produced a plasma level of nicotinic acid and pharmacological effects similar to those produced by a continous i.v. infusion of nicotinic acid in a dose of about 0.02 mg/kg/min for 6–7 h.