降血脂 (其他) Hypercholesterolemia, primary (heterozygous familial and non-familial) and mixed dyslipidemia (Fredrickson types IIa and IIb) (Not US FDA approved).

Niacin decreases the rate of hepatic synthesis of VLDL-C and LDL-C.
Lovastatin is a specific inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, a precursor to cholesterol.
The mechanism of the LDL lowering effect of lovastatin may involve both reduction of VLDL-C concentration and induction of the LDL receptor, leading to reduced production and/or increased catabolism of LDL-C.

Absorption:
Systemic: Niacin: 72%; food increases bioavailability 22 to 30%; Lovastatin: Incompletely absorbed; food decreases bioavailability, grapefrutijuice increases bioavailability
Metabolism:
Systemic: Niacin- Hepatic: Rapid and extensive dose dependent first pass metabolism; Metabolite: nicotinamide adenine dinucleotide (NAD); Lovastatin- Hepatic: rapid extensive first-pass metabolism; via CYP3A4 pathway; Active metabolite: beta-hydroxyacid derivative.
Excretion:
Systemic: Niacin- Renal: 60%; Lovastatin- Fecal: 83%; Renal: 10%
Elimination Half Life:
Niacin: 20 to 48 min; Lovastatin: 4.5 h.

Arterial bleeding.
Concomitant use with strong CYP3A4 inhibitors (eg, boceprevir, clarithromycin, erythromycin, HIV protease inhibitors, itraconazole, ketoconazole, nefazodone, posaconazole, telaprevir, telithromycin), or cobicistat/elvitegravir/emtricitabine/tenofovir.
Hypersensitivity to lovastatin, niacin, or any component of the product.
Liver disease, active.
Nursing women.
Peptic ulcer disease, active.
Serum transaminase elevations, unexplained persistent.
Women who are pregnant or may become pregnant; may cause fetal harm.

X (FDA)

Infant risk has been demonstrated.

Common:
Dermatologic: Flushing (up to 83%), Pruritus (7%).
Gastrointestinal: Diarrhea (6%), Nausea (7%).
Neurologic: Headache (9%).
Other: Infectious disease (20%).
Serious:
Dermatologic: Dermatomyositis.
Hepatic: Hepatic necrosis, Increased liver enzymes, Liver failure.
Immunologic: Autoimmune disease, Systemic lupus erythematosus.
Musculoskeletal: Disorder of muscle (0.2%), Rhabdomyolysis

Initial, niacin 500 mg/lovastatin 20 mg orally once daily at bedtime; may increase by no more than 500 mg of niacin and not more frequently than every 4 weeks; Max niacin 2000 mg/lovastatin 40 mg daily.

Severe (CrCl less than 30 mL/min): avoid doses of lovastatin greater than 20 mg/day

Use is contraindicated in patients with significant or unexplained hepatic dysfunction.