Acipimox

Acipimox
Clinical data
Trade names	Olbetam
AHFS/Drugs.com	UK Drug Information
Routes of; administration	Oral
ATC code	C10AD06 (WHO) ;
Legal status
Legal status	UK: POM (Prescription only) ;
Pharmacokinetic data
Bioavailability	100%
Protein binding	None
Metabolism	None
Elimination half-life	Phase 1: 2 hrs; Phase 2: 12–14 hrs
Excretion	Renal
Identifiers
	IUPAC name 5-Carboxy-2-methyl-1-oxidopyrazin-1-ium;
CAS Number	51037-30-0 ;
PubChem CID	5310993;
IUPHAR/BPS	1596;
ChemSpider	4470534 ;
UNII	K9AY9IR2SD;
KEGG	D07190 ;
ChEMBL	CHEMBL345714 ;
ECHA InfoCard	100.051.736
Chemical and physical data
Formula	C6H6N2O3
Molar mass	154.13 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES [O-][n+]1c(cnc(C(=O)O)c1)C;
	InChI InChI=1S/C6H6N2O3/c1-4-2-7-5(6(9)10)3-8(4)11/h2-3H,1H3,(H,9,10) ; Key:DJQOOSBJCLSSEY-UHFFFAOYSA-N ;
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Acipimox (trade name Olbetam in Europe) is a niacin derivative used as a lipid-lowering agent. It reduces triglyceride levels and increases HDL cholesterol. It may have less marked adverse effects than niacin, although it is unclear whether the recommended dose is as effective as standard doses of niacin.

Contraindications

Contraindications are peptic ulcers, acute bleeding, fresh myocardial infarction, acute decompensated heart failure, and severe renal insufficiency.^[1]

Adverse effects

As with niacin and related drugs, the most common adverse effects are flushing (associated with prostaglandin D₂^[2]) and gastrointestinal disturbances such as indigestion, which occur in at least 10% of patients.^[1] Flushing can be reduced by taking aspirin 20 to 30 minutes before taking acipimox. Palpitations have also been described. High doses can cause headache,^[3] and precipitate gout. In contrast to niacin, no impairment of glucose tolerance and no disorders of liver function have been found in studies, even under high doses of acipimox.^[1]^[3]

Interactions

No interactions with other drugs are known. Theoretically, combination with statins and fibrates could increase the incidence of myalgia. Alcohol can increase the risk of flushing.^[1]^[3]

Pharmacology

Mechanism of action

Like niacin, acipimox acts on the niacin receptor 1, inhibiting the enzyme triglyceride lipase. This reduces the concentration of fatty acids in the blood plasma and their inflow into the liver. Consequently, VLDL cholesterol production in the liver is reduced, which leads indirectly to a reduction in LDL and increase in HDL cholesterol.^[1]^[2]

Pharmacokinetics

Acipimox is completely absorbed from the gut. It is not bound to blood plasma proteins and not metabolized. Elimination occurs in two phases, the first having a half-life of two hours, the second of 12 to 14 hours. The substance is eliminated via the kidney.^[1]

References

1 2 3 4 5 6 Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
1 2 Benyó, Z; Gille, A; Kero, J; Csiky, M; Suchánková, M. C.; Nüsing, R. M.; Moers, A; Pfeffer, K; Offermanns, S (2005). "GPR109A (PUMA-G/HM74A) mediates nicotinic acid–induced flushing". Journal of Clinical Investigation. 115 (12): 3634–3640. doi:10.1172/JCI23626. PMC 1297235. PMID 16322797.
1 2 3 Dinnendahl, V; Fricke, U, eds. (1989). Arzneistoff-Profile (in German). 1 (6 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.

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[AC-1] 1 2 3 4 5 6 Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.

[Benyo-2] 1 2 Benyó, Z; Gille, A; Kero, J; Csiky, M; Suchánková, M. C.; Nüsing, R. M.; Moers, A; Pfeffer, K; Offermanns, S (2005). "GPR109A (PUMA-G/HM74A) mediates nicotinic acid–induced flushing". Journal of Clinical Investigation. 115 (12): 3634–3640. doi:10.1172/JCI23626. PMC 1297235. PMID 16322797.

[Dinnendahl-3] 1 2 3 Dinnendahl, V; Fricke, U, eds. (1989). Arzneistoff-Profile (in German). 1 (6 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.