Lovastatin !
A statin derived from a fungus. A lactone prodrug metabolized by CYP3A4, so strong CYP3A4 inhibitors are contraindicated.
Updated 2026-11-01
The figure shows compactin (mevastatin), which differs from lovastatin's active acid by a single methyl group, in the HMG-CoA pocket of human HMG-CoA reductase; lovastatin occupies the same site.
Mechanism of action
Lovastatin is an inactive lactone that is hydrolyzed in the body to its β-hydroxy acid. The acid competitively inhibits HMG-CoA reductase, lowers hepatic cholesterol synthesis and, through SREBP-2, raises LDL receptors so LDL falls.
- Inactive lactone is opened to the active hydroxy acid
- The acid blocks HMG-CoA reductase in the liver
- More LDL receptors clear LDL from the blood
Pharmacokinetics
- Absorption
- Oral; the immediate-release tablet is taken with the evening meal, since food increases its absorption.
- Distribution
- Lovastatin and its active acid are highly bound to plasma proteins; it crosses the blood–brain and placental barriers in animals.
- Metabolism
- Extensive first-pass metabolism by CYP3A4.
- Half-life
- Short, which is why it is given in the evening, when cholesterol synthesis peaks.
Indications
- High LDL cholesterol and prevention of coronary events Atherosclerosis and dyslipidaemia →
- Heterozygous familial hypercholesterolemia in adolescents Familial hypercholesterolemia →
Adverse effects
Common
- Muscle aches
- Headache, abdominal pain, constipation, flatulence
- Raised liver transaminases
Contraindications
- Strong CYP3A4 inhibitors: itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, erythromycin, clarithromycin, nefazodone, cobicistat products
- Active liver disease or unexplained persistent transaminase rises
- Pregnancy and breastfeeding
- Hypersensitivity to a component
Key interactions
- Strong CYP3A4 inhibitors
- Large rise in lovastatin levels and rhabdomyolysis risk; contraindicated.
- Gemfibrozil, cyclosporine
- Raise myopathy risk; the combinations are avoided.
- Danazol, diltiazem, verapamil, dronedarone, amiodarone
- More myopathy, especially at higher lovastatin doses; the dose is limited.
- Large amounts of grapefruit juice
- Inhibit CYP3A4 and raise levels; avoided.
What is monitored
- Lipid panel
- Liver enzymes
- Creatine kinase if there are muscle symptoms
Administration and safety
- Oral tablet, usually with the evening meal.
- Before starting, the list is screened for strong CYP3A4 inhibitors and for grapefruit juice habits.
- Look-alike name risk with other «-statins»: the drug and strength are checked.
Nursing care
- Before: lipid panel, liver enzymes, full medication list.
- Teach to report muscle pain, weakness or dark urine.
- Teach to avoid large amounts of grapefruit juice.
- Ask about pregnancy plans.
Pregnancy and breastfeeding
Contraindicated in pregnancy and breastfeeding.
Test yourself
Think of the answer, then tap the question to see it.
Why is lovastatin called a prodrug?
It is given as an inactive lactone that is hydrolyzed to the active β-hydroxy acid.
Which group of drugs is contraindicated with lovastatin?
Strong CYP3A4 inhibitors such as clarithromycin, itraconazole and HIV protease inhibitors (also erythromycin, ketoconazole, nefazodone).
Why is lovastatin taken with the evening meal?
Food increases its absorption, and its short half-life fits the night-time peak of cholesterol synthesis.
Related drugs
Related conditions
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Lovastatin: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); DailyMed - LOVASTATIN tablet (DailyMed (U.S. National Library of Medicine), 2026); COMPLEX OF THE CATALYTIC PORTION OF HUMAN HMG-COA REDUCTASE WITH COMPACTIN (ALSO KNOWN AS MEVASTATIN) (RCSB Protein Data Bank, 2001); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 37 (McGraw Hill, 2023).
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Representative model, for educational purposes only.