Overview
11 DESCRIPTION Niacin extended-release tablets USP, contain niacin, USP, which at therapeutic doses is an antihyperlipidemic agent. Niacin USP (nicotinic acid, or 3-pyridinecarboxylic acid) is white crystals or crystalline powder, sparingly soluble in water, soluble in boiling alcohol, freely soluble in boiling water and in solutions of alkali hydroxides and carbonates.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism by which niacin alters lipid profiles has not been well defined. It may involve several actions including partial inhibition of release of free fatty acids from adipose tissue, and increased lipoprotein lipase activity, which may increase the rate of chylomicron triglyceride removal from plasma. Niacin decreases the rate of hepatic synthesis of VLDL and LDL, and does not appear to affect fecal excretion of fats, sterols, or bile acids. 12.3 Pharmacokinetics Absorption Due to extensive and saturable first-pass metabolism, niacin concentrations in the general circulation are dose dependent and highly variable. Time to reach the maximum niacin plasma concentrations was about 5 hours following niacin extended-release tablets.
Indications
- 1 INDICATIONS AND USAGE Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hyperlipidemia. Niacin therapy is indicated as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate. Niacin extended-release tablets are indicated to reduce elevated TC, LDL-C, Apo B and TG levels, and to increase HDL-C in patients with primary hyperlipidemia and mixed dyslipidemia.
Common Doses
- 500 mg
- 000 mg
- 750 mg
- 325 mg
Dosage
2 DOSAGE AND ADMINISTRATION Niacin extended-release tablets should be taken at bedtime with a low-fat snack. ( 2.1 ) Dose range: 500 mg to 2,000 mg once daily. ( 2.1 ) Therapy with niacin extended-release tablets must be initiated at 500 mg at bedtime in order to reduce the incidence and severity of side effects which may occur during early therapy and should not be increased by more than 500 mg in any 4-week period. ( 2.1 ) Maintenance dose: 1,000 mg to 2,000 mg once daily. ( 2.2 ) Doses greater than 2,000 mg daily are not recommended. ( 2.2 ) 2.
Contraindications
- 4 CONTRAINDICATIONS Niacin extended-release tablets are contraindicated in the following conditions: Active liver disease or unexplained persistent elevations in hepatic transaminases [see Warnings and Precautions (5.3) ] Patients with active peptic ulcer disease Patients with arterial bleeding Hypersensitivity to niacin or any component of this medication [see Adverse Reactions (6.1) ] Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels. ( 4 , 5.3 ) Active peptic ulcer disease. ( 4 ) Arterial bleeding.
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the labeling: Mortality and Coronary Heart Disease Morbidity [see Warnings and Precautions (5.1) ] Skeletal Muscle (rhabdomyolysis) [see Warnings and Precautions (5.2) ] Liver Dysfunction [see Warnings and Precautions (5.3) ] Laboratory Abnormalities [see Warnings and Precautions (5.4) ] Most common adverse reactions (incidence >5% and greater than placebo) are flushing, diarrhea, nausea, vomiting, increased cough, and pruritus. ( 6.
Interactions
- 7 DRUG INTERACTIONS Statins: Caution should be used when prescribing niacin with statins as these agents can increase risk of myopathy/rhabdomyolysis. ( 5.2 , 7.1 ) Bile Acid Sequestrants: Bile acid sequestrants have a high niacin-binding capacity and should be taken at least 4 to 6 hours before niacin extended-release tablets administration. ( 7.2 ) 7.1 Statins Caution should be used when prescribing niacin (≥1 gm/day) with statins as these drugs can increase risk of myopathy/rhabdomyolysis [see Warnings and Precautions (5) and Clinical Pharmacology (12.3) ] . 7.