Summary
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.
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References
Barcroft, H., and H.J. Swan: Sympathetic control of human blood vessels. London: Arnold and Co. 1953.
Brattsand, R., and L. Harthon: Resorbtion, metabolism and excretion of 14-C-pentacrythritoltetranicotinate (Perycit® Bofors) after oral administration to rats. Arzneimittel-Forsch. (in press) 1969.
Bergmeyer, H., and E. Bernt: D-Glucose-Bestimmung mit Glucose-Oxydase und Peroxydase. In: Methoden der Enzymatischen Analyse (H.U. Bergmeyer ed.), p. 123–130. Weinheim: Verlag Chemie 1962.
Carlson, L. A.: Determination of free nicotinic acid in blood plasma. Clin. chim. Acta 13, 349–351 (1966).
L. Orö, and J. Östman: Effect of a single dose of nicotinic acid on plasma lipids in patients with hyperlipoproteinemia. Actamed. scand. 183, 457–465 (1968).
Harthon, L.: Hydrolysis of esters of nicotinic acid by blood and tissues. Arzneimittel-Forsch. (in press) 1969.
— Harthon, L., and J. E. Sigroth: On the absorption and metabolism of pentaerythritoltetranicotinate (Perycit®, Bofors), Arzneimittel-Forsch. (in press 1969).
J. J. E. Sigroth, and A. Sjöbom: Ein Beitrag zur Klärung der Resorption des Hexanicotinsäureesters des meso-Inositols im Organismus. Arzneimittel-Forsch. 14, 126–128 (1964).
Svedmyr, N., and L. Harthon: Comparison between the absorption of nicotinic acid and pentaerythritoltetranicotinate (Perycit®, Bofors) from ordinary and entero-coated tablets. Acta pharmacol. (Kbh.) (in press) 1969.
,, and L. Lundholm: The relationship between the plasma concentration of free nicotinic acid and some of its pharmacological effects in man. Clin. Pharmacol. and Therap. 10, 559–570 (1969).
Trout, D. L., E. H. Estes, and S. J. Friedberg: Titration of free fatty acids of plasma. A study of current methods and a new modification. J. Lipid Res. 1, 199–201 (1960).
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Svedmyr, D.N., Harthon, L. & Lundholm, L. A study of some acute pharmacodynamic effects of pentaerythritoltetranicotinate (Perycit®) in man. Pharmacol. Clin. 2, 13–18 (1969). https://doi.org/10.1007/BF00404179
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DOI: https://doi.org/10.1007/BF00404179