Drug reference

Lovastatin

Statin · Cholesterol-lowering agent

StatinCholesterol-lowering agent

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

AtazanavirSevereTextbook-citedKDT 7e · p948
ClarithromycinSevereTextbook-citedKDT 7e · p948
DarunavirSevereTextbook-citedKDT 7e · p948
ErythromycinSevereTextbook-citedKDT 7e · p948

Mechanism

Lovastatin, a statin, is administered as an inactive prodrug with a lactone ring, which is converted to its active acid form. It reversibly inhibits HMG-CoA reductase, an enzyme that catalyzes a rate-limiting step in cholesterol biosynthesis. This inhibition occurs primarily in the liver, which is the main target organ for its cholesterol-lowering effects.

Indications

HypercholesterolemiaReduction of LDL-C levelsTreat dyslipidemias, especially elevated LDL-CChildren aged 11 years and older with heterozygous FHPrimary hyperlipidaemias with raised LDL and total CH levels, with or without raised TG levels (Type IIa, IIb, V)Secondary hypercholesterolaemia (e.g., in diabetes, nephrotic syndrome)

Dosing

Adult: than 20 mg/24 hr and lovastatin at doses greater than 40 mg/24 hr. Serious symptomatic. Proposed therapeutic level with chronic oral use: 1e2.5 mg/L. Intravenous continuous infusion concentration for peripheral administration should not exceed 2 mg/. Tabs: 10, 25, 50, 75, 100, 150 mg. Oral suspension: 10 mg/mL , 20 mg/mL

Pharmacokinetics

Half-life

1 to 4 h

Bioavailability

Absorption is increased when taken with food.

Protein binding

>95%

Metabolism

Administered as an inactive prodrug (lactone ring) that is converted to an active form. It is a substrate of CYP3A4. It undergoes efficient first-pass hepatic uptake, mediated by uptake transporters such as OATP1B1, and undergoes enterohepatic circulation.

Excretion

10%

Contraindications

Pregnancy

Side effects

Common

MyalgiaMuscle sorenessWeaknessGastrointestinal complaintsHeadacheRashes (uncommon)Sleep disturbances (uncommon)Muscle aches (10%)

Serious

Rhabdomyolysis (increased risk when used with amiodarone at doses greater than 40 mg/24 hr)
Myopathy
Rhabdomyolysis
Hepatotoxicity
Rise in serum transaminase
Liver damage (rare)
Myopathy (rare, < 1 per 1000)
Rhabdomyolysis (fatalities on record)

Drug interactions

Atazanavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Clarithromycin

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Darunavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Erythromycin

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Fluconazole

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Gemfibrozil

Severe

Textbook-cited

Increased risk of myopathy and rhabdomyolysis.

Use with caution; monitor for muscle symptoms and CK levels

Source: KDT 7e · p949

Itraconazole

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Ketoconazole

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Lopinavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Nicotinic Acid

Severe

Textbook-cited

Increased risk of myopathy and rhabdomyolysis

Use with caution; monitor for muscle symptoms and CK levels

Source: KDT 7e · p949

Ritonavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Azole Antifungals

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736