Nocturnal inhibition of lipolysis in man by nicotinic acid and derivatives

Abstract

The effect of nicotinic acid and several derivatives on the nocturnal level of free fatty acids was studied in 12 healthy young women and men. Free fatty acids are an important precursor of plasma triglycerides and their concentration is highest at night. The drugs used were nictinic acid, beta-pyridyl-carbinol, mesoinositol hexanicotinate and xantinol nicotinate. The highest plasma nicotinic acid level was observed with beta-pyridyl-carbinol, but significant reduction in free fatty acids during the entire night was only achieved with inositolhexanicotinate and xantinol nicotinate. There was no correlation between the plasm levels of free fatty acids and nicotinic acid at any sampling time. If prolonged reduction in free fatty acid concentration is desired in the therapy of hyperlipidemias, the inositol and xantinol esters of nicotinic acid appear to be superior to the other preparations.

Niacin: chemical forms, bioavailability, and health effects

“…This compound is marketed as “no‐flush niacin.” 24 The small amount of data available that suggests IHN does not produce a flushing reaction is consistent with the modest NA plasma response following IHN intake 23,24,40 . Few other adverse effects have been reported in clinical trials studying the use of dosages of IHN up to 4,000 mg/day 40–43 .…”

“…Interestingly, the peak plasma levels of NA after oral doses of IHN are dramatically lower when compared with those obtained after oral doses of NA; for example, a single oral dose of 1,000 mg NA resulted in a peak plasma level of 30 µg/mL NA, 21 while 1,000 mg of IHN (weight equivalent to ∼910 mg NA) resulted in a peak plasma level of 0.2 µg/mL NA 22 . Similarly, Kruse et al 23 . gave 12 healthy young women 2,400 mg of IHN orally over a 3‐hour period and achieved a peak plasma NA level of 0.1 µg/mL.…”

“…Some reports indicate IHN produces a slight increase in the plasma level of NA but does not have any significant effects on plasma lipid profiles 22–24 . If IHN is, in fact, absorbed intact and hydrolyzed in the body with the release of NA and inositol, the extent of hydrolysis appears to be very low, as evidenced by the low levels of NA found in plasma after IHN ingestion.…”

“…IHN has been discussed as a better tolerated and safer alternative to NA and ER‐NA, 44,45 but data on the efficacy of IHN for lowering serum lipids do not support the hypothesis that the chemical forms are clinically interchangeable 14,23–25 …”

“…Humans given oral doses of IHN obtain peak plasma levels of NA at 6-12 h, 19,20 while oral doses of NA result in peak plasma levels of NA at 0.5-1 h. 21 Interestingly, the peak plasma levels of NA after oral doses of IHN are dramatically lower when compared with those obtained after oral doses of NA; for example, a single oral dose of 1,000 mg NA resulted in a peak plasma level of 30 mg/mL NA, 21 while 1,000 mg of IHN (weight equivalent tõ 910 mg NA) resulted in a peak plasma level of 0.2 mg/mL NA. 22 Similarly, Kruse et al 23 gave 12 healthy young women 2,400 mg of IHN orally over a 3-hour period and achieved a peak plasma NA level of 0.1 mg/ mL. Another experiment conducted in dogs compared the bioavailability of oral doses of 1 g of NA to the same amount of IHN and pentaerythritol tetranicotinate.…”