[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Statins](https://durgical.com/en/pharmacology/classes/statins/) › Lovastatin [Pharmacology](https://durgical.com/en/pharmacology/) · [Statins](https://durgical.com/en/pharmacology/classes/statins/) # Lovastatin A statin derived from a fungus. A lactone prodrug metabolized by CYP3A4, so strong CYP3A4 inhibitors are contraindicated. Updated 2026-11-01 - Class: [Statins](https://durgical.com/en/pharmacology/classes/statins/) - Enzyme: HMG-CoA reductase - ATC code: C10AA02 - WHO Model List of Essential Medicines ✂**HMG-CoA reductase**Lovastatin ⓘ 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. **Target in 3D:** HMG-CoA reductase. PDB structure 1HW8 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/1HW8) · Drag to rotate · pinch to zoom ## 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 →](https://durgical.com/en/conditions/atherosclerosis-and-dyslipidaemia/) - Heterozygous familial hypercholesterolemia in adolescents [Familial hypercholesterolemia →](https://durgical.com/en/conditions/familial-hypercholesterolemia/) ## Adverse effects ### Common - Muscle aches - Headache, abdominal pain, constipation, flatulence - Raised liver transaminases ### Serious (rare, important) - Myopathy and rhabdomyolysis, more with CYP3A4 inhibitors - Immune-mediated necrotizing myopathy (rare) - Liver injury (rare) ## 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. ## Memory aid «Lova loves 3A4 and dinner»: a lactone prodrug, cleared by CYP3A4, taken with the evening meal. Block 3A4 and the muscles pay. ## 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. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/lovastatin/) ## Related drugs - [Simvastatin](https://durgical.com/en/pharmacology/simvastatin/) - [Pravastatin](https://durgical.com/en/pharmacology/pravastatin/) - [Fluvastatin](https://durgical.com/en/pharmacology/fluvastatin/) ## Related conditions - [Atherosclerosis and dyslipidaemia](https://durgical.com/en/conditions/atherosclerosis-and-dyslipidaemia/) - [Familial hypercholesterolemia](https://durgical.com/en/conditions/familial-hypercholesterolemia/) [← Back to the class: Statins](https://durgical.com/en/pharmacology/classes/statins/) 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](https://medlineplus.gov/druginfo/meds/a688006.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [DailyMed - LOVASTATIN tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7b86160d-74a9-4774-b5b3-5641e686991f) (DailyMed (U.S. National Library of Medicine), 2026); [COMPLEX OF THE CATALYTIC PORTION OF HUMAN HMG-COA REDUCTASE WITH COMPACTIN (ALSO KNOWN AS MEVASTATIN)](https://www.rcsb.org/structure/1HW8) (RCSB Protein Data Bank, 2001); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 37 (McGraw Hill, 2023). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/lovastatin/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/lovastatin/