Tolerability and effects of high doses acipimox as additional lipid-lowering therapy in familial hypercholesterolemia

Stuyt, P.M.J.; Kleinjans, H. A. J.; Stalenhoef, Anton F. H.

doi:10.1016/s0300-2977(98)00076-x

Cited by 7 publications

(6 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Acipimox, a nicotinic acid analog and a potent inhibitor of lipolysis, is an established available therapy for dyslipidemia outside the United States, with known efficacy in the setting of familial hypercholesterolemia (17) and in association with type II diabetes mellitus (18,19). For example, Fulcher et al (18) showed improvement in lipids, as well as insulin action, in nonobese type 2 diabetics with acipimox.…”

mentioning

confidence: 99%

Improved Triglycerides and Insulin Sensitivity with 3 Months of Acipimox in Human Immunodeficiency Virus-infected Patients with Hypertriglyceridemia

Hadigan

Liebau

Torriani

et al. 2006

The Journal of Clinical Endocrinology &Amp; Metabolism

View full text Add to dashboard Cite

show abstract

mentioning

confidence: 99%

Improved Triglycerides and Insulin Sensitivity with 3 Months of Acipimox in Human Immunodeficiency Virus-infected Patients with Hypertriglyceridemia

Hadigan

Liebau

Torriani

et al. 2006

The Journal of Clinical Endocrinology &Amp; Metabolism

View full text Add to dashboard Cite

show abstract

“…Several studies show that short-term Acipimox treatment (250 mg, two-to-three times per day) for up to 2 weeks can reduce fasting plasma free fatty acids and increase insulin sensitivity and glucose control in obese and T2D individuals (Bajaj et al, 2005;Daniele et al, 2014;Phielix et al, 2014;van de Weijer et al, 2015). Furthermore, 8 weeks of Acipimox treatment lowers plasma free fatty acids, cholesterol and triglyceride concentrations in obese individuals and T2D patients (Crepaldi et al, 1988;Stuyt, Kleinjans and Stalenhoef, 1998). Lower plasma free fatty acid levels reduce the availability of FA for uptake into skeletal muscle, potentially minimising the accumulation of lipid in this tissue.…”

Section: Anti-lipolytic Drug Therapymentioning

confidence: 99%

High intramuscular triglyceride turnover rates and the link to insulin sensitivity: influence of obesity, type 2 diabetes and physical activity

Barrett

Whytock

Strauss

et al. 2022

Appl. Physiol. Nutr. Metab.

View full text Add to dashboard Cite

Large intramuscular triglyceride (IMTG) stores in sedentary, obese individuals have been linked to insulin resistance, yet well-trained athletes exhibit high IMTG levels whilst maintaining insulin sensitivity. Contrary to previous assumptions, it is now known that IMTG content per se does not result in insulin resistance. Rather, insulin resistance is caused, at least in part, by the presence of high concentrations of harmful lipid metabolites, such as diacylglycerols and ceramides in muscle. Several mechanistic differences between obese sedentary individuals and their highly-trained counterparts have been identified, that determine the differential capacity for IMTG synthesis and breakdown in these populations. In this review, we first describe the most up-to-date mechanisms by which a low IMTG turnover rate (both breakdown and synthesis) leads to the accumulation of lipid metabolites and results in skeletal muscle insulin resistance. We then explore current and potential exercise and nutritional strategies which target IMTG turnover in sedentary obese individuals, to improve insulin sensitivity. Overall, improving IMTG turnover should be an important component of successful interventions which aim to prevent the development of insulin resistance in the ever-expanding sedentary, overweight and obese populations. Novelty Bullet points • A description of the most up-to-date mechanisms regulating turnover of the IMTG pool. • An exploration of current and potential exercise/nutritional strategies to target and enhance IMTG turnover in obese individuals • Overall, highlights the importance of improving IMTG turnover to prevent the development of insulin resistance

show abstract

“…, 1992). Like niacin, it is also effective in reducing circulating levels of Lp(a) (Stuyt et al. , 1998).…”

Section: Niacin Receptor Agonistsmentioning

confidence: 99%

“…In addition to its effects on plasma lipids, acipimox has been shown to cause regression of atherosclerosis (Stuyt et al, 1998), and it has also proved particularly useful in treating dyslipidaemias associated with high levels of LDL or TGs (Crepaldi et al, 1988;O'Kane et al, 1992). Like niacin, it is also effective in reducing circulating levels of Lp(a) (Stuyt et al, 1998).…”

Section: Acipimoxmentioning

confidence: 99%

Niacin: a re‐emerging pharmaceutical for the treatment of dyslipidaemia

Vosper

2009

British J Pharmacology

View full text Add to dashboard Cite

Dyslipidaemias, particularly those characterized by the 'atherogenic profile' of high low-density lipoprotein-cholesterol and triglycerides and low high-density lipoprotein-cholesterol, are the major modifiable risk factor for atherosclerosis. The search for drugs to favourably alter such lipid profiles, reducing the associated morbidity and mortality, remains a major research focus. Niacin (nicotinic acid) is the most effective agent available for increasing high-density lipoprotein-cholesterol, but its use is associated with side effects that negatively affect patient compliance: these appear to arise largely as a result of production of prostaglandin D2 and its subsequent activation of the DP1 receptor. Desire to reduce the side effects (and improve pharmacokinetic parameters) has led to the development of a number of agonists that have differing effects, both in terms of clinical potency and the severity of adverse effects. The recent discovery of the niacin G-protein-coupled receptor HM74A (GPR109A) has clarified the distinction between the mechanism whereby niacin exerts its therapeutic effects and the mechanisms responsible for the generation of side effects. This has allowed the development of new drugs that show great potential for the treatment of dyslipidaemia. However, recent advances in understanding of the contribution of prostaglandin metabolism to vascular wall health suggest that some of the beneficial effects of niacin may well result from activation of the same pathways responsible for the adverse reactions. The purpose of this review is to emphasize that the search for agonists that show higher tolerability must take into account all aspects of signalling through this receptor.

show abstract

Tolerability and effects of high doses acipimox as additional lipid-lowering therapy in familial hypercholesterolemia

Cited by 7 publications

References 19 publications

Improved Triglycerides and Insulin Sensitivity with 3 Months of Acipimox in Human Immunodeficiency Virus-infected Patients with Hypertriglyceridemia

Improved Triglycerides and Insulin Sensitivity with 3 Months of Acipimox in Human Immunodeficiency Virus-infected Patients with Hypertriglyceridemia

High intramuscular triglyceride turnover rates and the link to insulin sensitivity: influence of obesity, type 2 diabetes and physical activity

Niacin: a re‐emerging pharmaceutical for the treatment of dyslipidaemia

Contact Info

Product

Resources

About