Inhibition of lipolysis by nicotinic acid and by acipimox

Fuccella, L. M.; Goldaniga, Giancarlo; Lovisolo, P. P.; Maggi, E.; Musatti, L.; Mandelli, V.; Sirtori, Cesare R.

doi:10.1038/clpt.1980.236

Cited by 122 publications

(45 citation statements)

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“…Several pharmaceutical companies began developing selective agonists of GPR109A (42)(43)(44)(45)(46)(47). Walters et al ( 48 ) suggested that the effects of niacin on FFAs and fl ushing could be segregated.…”

Section: Niacin Receptormentioning

confidence: 99%

Niacin, an old drug with a new twist

Song

FitzGerald

2013

Journal of Lipid Research

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This article is available online at http://www.jlr.org the only approved drug with such an effect ( 1 ). It has proven to be an attractive option for those intolerant of statin treatment. It has been demonstrated to reduce risk of atherosclerotic cardiovascular disease ( 4 ). The clinical use of niacin has been markedly limited by cutaneous fl ushing. The molecular target of niacin responsible for lipid metabolic changes and fl ushing was unknown until 2003 ( 5-7 ), when the niacin receptor, namely HM74A in humans and PUMA-G in mice, was discovered. The niacin receptor, also known as GPR109A, was shown to be activated by niacin and to mediate its antilipolytic effect as well as the fl ushing effect ( 8-10 ). Interest in niacin has risen because there is still signifi cant residual risk in patients with intensive statin therapy ( 11 ). However, recent outcome trials ( 11, 12 ) failed to show niacin's benefi t on top of statin therapy in lipid-targeted approaches to reduce major cardiovascular events in high-risk patients. In this review we will summarize the pharmacology of niacin, with a particular emphasis on recent outcome trials, including discussion of their limitations . NIACIN'S LIPID EFFECTSNiacin has long been shown to have effects on lipids ( 13 ). Niacin increases high density lipoprotein cholesterol (HDLc), but reduces low density lipoprotein cholesterol (LDLc), VLDL cholesterol, and triglycerides (TGs) ( 14 ) Niacin is also known as vitamin B3. Chronic dietary defi ciency of niacin can cause pellagra ( 1 ). It is a precursor to NAD+/NADH and NADP+/NADPH, both of which play essential metabolic roles in living cells ( 2 ). Niacin has been used for more than half a century in the treatment of dyslipidemia. When Altschul, Hoffer, and Stephen ( 3 ) discovered that niacin could lower plasma levels of cholesterol, it was

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Section: Niacin Receptormentioning

confidence: 99%

Niacin, an old drug with a new twist

Song

FitzGerald

2013

Journal of Lipid Research

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“…Following an experimental protocol, previously designed by our group to investigate the interplay GH/FFA in normal subjects (27,28), the first eight acromegalic subjects (group 1 of Table 1) received (per os, on two different days, at a 3 day-interval, and in a random order) placebo or 250 mg acipimox (Olbetam, Pharmacia & Upjohn, Inc., Milan, Italy) at 0700 h and at 1100 h. Acipimox is an inhibitor of lipolysis analogous to nicotinic acid that is known to act only on the adipose tissue (32,33). In both tests, GHRH (1-29 NH 2 ), 50 g iv, was administered at 1300 h.…”

Section: Subjects and Experimental Proceduresmentioning

confidence: 99%

The Control on Growth Hormone Release by Free Fatty Acids Is Maintained in Acromegaly

Lanzi¹,

Losa²,

Mignogna³

et al. 1999

The Journal of Clinical Endocrinology & Metabolism

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Free fatty acids (FFA) physiologically regulate GH release via a negative feedback. The aim of this study was to examine whether such feedback is preserved in acromegaly, a condition in which alterations in other regulatory mechanisms of GH release occur. Eight acromegalic patients (group 1: five women and three men, 43.0 Ϯ 4.2 yr old, mean Ϯ SE) received per os on two different days, at a 3 day-interval, in a random order, placebo or 250 mg of acipimox,

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“…Nicotinic acid reduces lipolysis in adipose tissue and inhibits the release of fatty acids into the circulation (29). Less fatty acids therefore reach the liver for synthesis of VLDL and subsequently LDL.…”

Section: Nicotinic Acid a N D Derivativesmentioning

confidence: 99%

“…It is often fortuitous that many patients who require these drugs are already on low-dose aspirin for vascular disease. Acipimox also seems to be more potent than nicotinic acid in suppressing fatty acid release (29), although less effective in reducing LDL-cholesterol (30).…”

Section: Nicotinic Acid a N D Derivativesmentioning

confidence: 99%