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Acipimox is a synthetic derivative of nicotinic acid (niacin) used as a lipid-lowering medication. It is prescribed mainly to lower elevated triglycerides and, to a lesser degree, to raise HDL cholesterol in people with certain forms of hyperlipidemia. Marketed in parts of Europe under the trade name Olbetam, it is generally regarded as having a milder side-effect profile than niacin itself.
- Strongly lowers triglycerides
- Cuts free fatty acid release from fat tissue
- Can improve insulin sensitivity
- Less flushing than standard niacin
- Studied in diabetes and metabolic syndrome
- May improve overall lipid profile
- Facial flushing and warmth, a class effect shared with niacin
- Itching or a prickling sensation of the skin
- Mild stomach upset such as nausea or indigestion
- Headache in some users
- Generally gentler effects on glucose and liver than niacin
Overview
Acipimox is a niacin analogue belonging to the pyrazine carboxylic acid family and is classed pharmacologically as an antilipolytic, lipid-lowering agent. Like the parent vitamin nicotinic acid, it suppresses the release of fatty acids from fat tissue, which in turn lowers the raw material the liver uses to manufacture triglyceride-rich lipoproteins [1][2]. Its small, water-soluble molecule is almost completely absorbed after oral intake, is not appreciably bound to plasma proteins, and is cleared largely unchanged by the kidneys [4].
The drug is used chiefly to treat high triglycerides and mixed dyslipidemias, where it reduces circulating triglycerides and free fatty acids and can modestly increase HDL cholesterol [2][4]. Because lowering the supply of free fatty acids to muscle and liver also changes how the body handles glucose, acipimox has been studied as a tool for probing insulin sensitivity and fuel selection; short, intensified dosing has been shown to lower fasting free fatty acids, triglycerides, and blood glucose in people with type 2 diabetes, although a rebound rise in fatty acids can blunt any sustained benefit [1][4]. These metabolic actions have made it a frequent experimental probe in human physiology research as well as a therapeutic agent [1].
Compared with immediate-release niacin, acipimox is often described as better tolerated, with reports of little impairment of glucose tolerance or liver function even at higher intakes, though whether ordinary doses match the full efficacy of standard niacin remains debated [4]. It is taken by mouth and is marketed in several European countries, notably under the name Olbetam, where it is a prescription medicine; it has not been widely marketed in some other regions [2]. The characteristic facial flushing shared by niacin-type drugs is produced through the same receptor pathway and remains a recognized effect [3].
Mechanism
Acipimox acts chiefly by activating the hydroxycarboxylic acid receptor 2, also known as niacin receptor 1 or GPR109A, a G-protein-coupled receptor found abundantly on fat cells [3]. Stimulating this receptor lowers cyclic AMP inside adipocytes and thereby restrains hormone-sensitive lipase, the enzyme that breaks stored triglyceride down into free fatty acids; the result is reduced release of fatty acids into the blood [1][3].
With fewer free fatty acids arriving at the liver, production of very-low-density lipoprotein and the triglycerides it carries falls, which indirectly lowers circulating triglycerides and can shift the lipoprotein profile toward higher HDL cholesterol [2]. The same drop in fatty acid supply alters fuel use in skeletal muscle, increasing reliance on intramuscular fat and glycogen stores and improving apparent sensitivity, effects that underlie the drug's use as a research probe of metabolism [1]. Activation of the same receptor on immune cells in the skin triggers prostaglandin release, which accounts for the flushing sensation associated with acid and its analogues [3]. A practical limitation is that sustained suppression of lipolysis can provoke a counter-regulatory rebound, with free fatty acids climbing again during prolonged exposure [4].
receptor fingerprint
Adipose lipolysisInhibitor
sensitivityEnhancer
Plasma lipidsReducer
Safetyrisks and cautions, not medical advice
Acipimox is a nicotinic acid analog and its most characteristic adverse effect is prostaglandin-mediated cutaneous flushing, often with warmth or itching, which can be blunted by pre-dosing aspirin. Other reported effects include headache, rash, palpitations, and gastrointestinal upset such as nausea, dyspepsia, diarrhea, and upper abdominal pain. It is generally better tolerated than niacin and, unlike niacin, does not worsen insulin sensitivity, making it more suitable in dyslipidemic patients with diabetes. Because it is cleared renally, caution and dose adjustment are warranted in renal impairment.
Subjective profileweighing the evidence above
A real lipid drug worth having where triglycerides are the actual problem, and a sensible one in diabetes, since unlike niacin it does not worsen insulin sensitivity. It is a European prescription medicine, not a supplement to add for general heart health, and flushing is still the main complaint.
Resources
This entry is here for reference.
Research
- 1993first citedLipoprotein structure in male subjects during in vivo lipolysis: effect of an anti-lipolytic tr…
- 2005most recentInhibition of adipose tissue lipolysis increases intramuscular lipid and glycogen use in vivo i…
- 1.Inhibition of adipose tissue lipolysis increases intramuscular lipid and glycogen use in vivo in humans
- 2.Lipoprotein structure in male subjects during in vivo lipolysis: effect of an anti-lipolytic treatment with acipimox
- 3.GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing
- 4.Pronounced blood glucose-lowering effect of the antilipolytic drug acipimox in noninsulin-dependent diabetes mellitus patients during a 3-day intensified treatment period
4 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
How is acipimox different from niacin?
It is a niacin analog that lowers fatty acids and triglycerides with generally less flushing and a lighter effect on blood sugar.
Why is it dosed several times a day?
Its short half-life means fatty acids can rebound between doses, so it is spread out to keep the antilipolytic effect steady.
Is it a general supplement?
No; it is a prescription lipid-lowering drug in the countries where it is sold, so it should be used with medical guidance.
Adverse effects
- Facial flushing and warmth, a class effect shared with niacin
- Itching or a prickling sensation of the skin
- Mild stomach upset such as nausea or indigestion
- Headache in some users
- Generally gentler effects on glucose and liver than niacin