HMG-CoA reductase inhibitor (statin)
ATC code: C10AA02 (Lovastatin)
Brand names
Mevacor, Altoprev
Lovastatin is a prodrug; after hydrolysis of the lactone ring it becomes an active HMG-CoA reductase inhibitor. It reduces hepatic cholesterol synthesis and upregulates receptor expression on hepatocytes. About 98% of lovastatin is metabolised by CYP3A4, so interaction risks mirror those of simvastatin: combination with strong CYP3A4 inhibitors (itraconazole, clarithromycin, grapefruit juice) raises concentrations several-fold and increases the risk of myopathy and rhabdomyolysis. Current guidelines use lovastatin less often because its outcome data are shorter than for atorvastatin and rosuvastatin.
Third line
First-generation statin for reduction. SEC and AEMPS prefer atorvastatin or rosuvastatin for greater efficacy and fewer CYP3A4 interactions. Lovastatin remains an option for patients intolerant to newer statins.
Third line
Treats Fredrickson type IIa and IIb primary hypercholesterolaemia. SEC prefers atorvastatin and rosuvastatin for high-intensity statin therapy.
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FDA Category X. AEMPS and EMA contraindicate statins in pregnancy due to the theoretical risk of impaired cholesterol synthesis required for embryogenesis. Discontinued before planned pregnancy and not resumed until breastfeeding ends.
Not compatible. Hale L4. No human milk transfer data; theoretical concern about disruption of infant cholesterol synthesis. AEMPS contraindicates statins during breastfeeding.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Lovastatin is evaluated for the following indications with varying evidence strength: Dyslipidemia (evidence tier A), Primary hypercholesterolemia (evidence tier B). See the full indication matrix with dosing and citations above on this page.
Common side effects of Lovastatin (≥ 1 in 100): Myalgia, Elevated transaminases, Headache, Constipation and flatulence. See the Safety section for uncommon and serious reactions.
FDA category X. FDA Category X. AEMPS and EMA contraindicate statins in pregnancy due to the theoretical risk of impaired cholesterol synthesis required for embryogenesis. Discontinued before planned pregnancy and not resumed until breastfeeding ends.
Not compatible. Hale L4. No human milk transfer data; theoretical concern about disruption of infant cholesterol synthesis. AEMPS contraindicates statins during breastfeeding.
Lovastatin is contraindicated in: Hypersensitivity to lovastatin; Active liver disease or transaminases >3× ULN; Pregnancy and lactation; Co-administration with potent CYP3A4 inhibitors (itraconazole, ketoconazole, clarithromycin, ritonavir). Full list in the Safety section.