Adult: Initially, 250 mg once daily in the evening. Increase dose every 4-7 days until desired LDL cholesterol and/or triglyceride level is achieved or dose of 1.5-2 g/day is reached. If hyperlipidaemia is not adequately controlled after 2 mth w/ this dose, it can be increased at 2- to 4-wk intervals to 1 g tid. Max: 6 g daily. As extended-release tab: Initially, 500 mg at night, gradually increased according to response to a maintenance of 1-2 g at bedtime.
Oral Vasodilation
Adult: 100-150 mg 3-5 times daily. As extended-release tab: 300-400 mg 12 hrly.
Oral Treatment and prophylaxis of nicotinic acid deficiency
Adult: For treatment of pellagra: 300-500 mg daily in divided doses. For management of Hartnup disease: 50-200 mg daily. Child: For treatment of pellagra: 100-300 mg daily in divided doses.
Topical/Cutaneous Mild to moderate inflammatory acne
Adult: As 4% gel: Apply to affected area bid.
Administration
Should be taken with food. Take at bedtime after a low-fat snack.
Contraindications
Patient w/ active liver disease or unexplained persistent elevations of serum transaminases, active peptic ulcer disease, arterial bleeding.
Special Precautions
Patient w/ unstable angina, acute MI, CHD, DM, gout, history of peptic ulceration. Patient who consume large amount of alcohol. Patient undergoing surgery. Renal or hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Flushing, sensation of heat, faintness, pounding in the head, tingling, itching, headache, dizziness, tachycardia, palpitations, dyspnoea, sweating, chills, oedema; dryness of skin, pruritus, hyperpigmentation, rash, cramps, cough, diarrhoea, nausea and vomiting, anorexia, activation of peptic ulcer, eye disorders including cystoid macular oedema and toxic amblyopia; decreased glucose tolerance, hyperglycaemia, hyperuricaemia; abnormal LFTs, jaundice; hypophosphataemia, reduced platelet counts, prolonged prothrombin time, arrhythmias, hypersensitivity reactions including angioedema; insomnia, myalgia and hypotension.
Increased risk of myopathy and rhabdomyolysis w/ concomitant HMG-CoA reductase inhibitors. Reduced bioavailability w/ colestyramine or colestipol. Decreased metabolic clearance w/ aspirin. May potentiate effects of ganglionic blocking agents and vasoactive drugs resulting in postural hypotension.
Food Interaction
Avoid alcohol or hot drinks and spicy foods as it may increase risk of flushing and pruritus.
Lab Interference
May produce false elevations in some fluorometric determinations of plasma or urinary catecholamines. May give false-positive results w/ cupric sulfate soln (Benedict's reagent) in urine glucose determination.
Action
Description: Mechanism of Action: Nicotinic acid is a derivative of vitamin B3 and is incorporated into coenzymes nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP), which are involved in multiple cellular metabolic pathways. Nicotinic acid also reduces total serum cholesterol, LDL, VLDL, apolipoprotein B and triglycerides, and increases HDL cholesterol. Pharmacokinetics: Absorption: Readily absorbed from the GI tract. Distribution: Widely distributed in body tissues and appears in breast milk. Metabolism: Converted to N-methylnicotinamide, 2-pyridone and 4-pyridone derivatives. Excretion: Via urine in small amounts as unchanged drug. Plasma elimination half-life: 20-45 min.
Chemical Structure
Nicotinic acid Source: National Center for Biotechnology Information. PubChem Database. Nicotinic acid, CID=938, https://pubchem.ncbi.nlm.nih.gov/compound/Nicotinic-acid (accessed on Jan. 22, 2020)
C10AD02 - nicotinic acid ; Belongs to the class of nicotinic acid and derivatives. Used in the treatment of hyperlipidemia. C04AC01 - nicotinic acid ; Belongs to the class of nicotinic acid agents. Used as peripheral vasodilators.
References
Anon. Niacin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/10/2014.Buckingham R (ed). Nicotinic acid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/10/2014.Joint Formulary Committee. Nicotinic acid. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/10/2014.McEvoy GK, Snow EK, Miller J et al (eds). Niacin, Niacinamide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 10/10/2014.McEvoy GK, Snow EK, Miller J et al (eds). Niacin. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 10/10/2014.Niacor-Niacin Tablet (Upsher-Smith Laboratories Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/10/2014.Niaspan-Niacin Tablet, Film Coated, Extended Release. DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 26/08/2015.
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