HMG-CoA reductase inhibitor (statin)
Brand names: Mevacor, Altoprev
Updated · Methodology
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.
Sources
ICD-10: E78 · ICD-11: 5C80
Third line
Treats Fredrickson type IIa and IIb primary hypercholesterolaemia. SEC prefers atorvastatin and rosuvastatin for high-intensity statin therapy.
Sources
ICD-10: E78.0 · ICD-11: 5C80.00
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.
AEMPS summary of product characteristics (section 4.6): lovastatin is contraindicated in pregnancy, and no controlled clinical trials have been done in pregnant women. There have been rare reports of congenital anomalies after intrauterine exposure to HMG-CoA reductase inhibitors, but in an analysis of about 200 prospectively followed pregnancies exposed in the first trimester to lovastatin or a closely related HMG-CoA reductase inhibitor, the rate of anomalies was comparable to that in the general population; this number was statistically enough to exclude a 2.5-fold or greater increase. Maternal lovastatin may lower fetal levels of mevalonate, a precursor of cholesterol synthesis, and because atherosclerosis is a chronic process, stopping lipid-lowering drugs during pregnancy should have little impact on the long-term risk of primary hypercholesterolaemia. Lovastatin is not taken by women who are pregnant, trying to conceive or suspect pregnancy; treatment is stopped for the whole pregnancy or until pregnancy has been ruled out.
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.
Grapefruit juice blocks intestinal CYP3A4, the main route by which lovastatin is broken down. In the Colesvir SmPC, more than a litre of juice a day clearly raised statin activity in plasma. The excess damages muscle: pain and weakness in the thighs and shoulders, dark urine, raised creatine kinase. The SmPC says to avoid grapefruit juice during treatment. Pravastatin, rosuvastatin, fluvastatin and pitavastatin barely depend on CYP3A4.
Source: AEMPS: Ficha técnica de Colesvir 20 mg comprimidos (lovastatina) (2024)
6 pairs found. Sorted from critical to minor.
Mechanism
Clarithromycin inhibits CYP3A4 – lovastatin (sensitive substrate) rises 8-fold. Rhabdomyolysis risk.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Combination contraindicated. Switch lovastatin to pravastatin or rosuvastatin during the course.
Sources
Mechanism
Lovastatin is a CYP3A4 sensitive substrate (like simvastatin). Cobicistat causes 30-fold rise. Tybost Section 4.3.
Symptoms
Rhabdomyolysis within 5–10 days.
Management
Combination contraindicated. Pravastatin or rosuvastatin.
Sources
Mechanism
CYP3A4 inhibition – lovastatin rises 5-fold. Rhabdomyolysis.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Combination contraindicated.
Sources
Mechanism
Strong CYP3A4 inhibitor – lovastatin rises 20+ fold. contraindication.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Combination contraindicated.
Sources
Mechanism
Strong CYP3A4 inhibitor. Lovastatin rises 10+ fold.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Combination contraindicated.
Sources
Mechanism
Amiodarone inhibits CYP3A4. Lovastatin rises 2-3 fold. recommends capping lovastatin at 40 mg/day with amiodarone.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Cap lovastatin at 40 mg/day. Better – pravastatin or rosuvastatin.
Sources
Verbatim lines from the interaction sections, in the language of the label
«?? Administració n concomitante de inhibidores potentes de la CYP3A4 (p. ej., itraconazol, ketoconazol, inhibidores de la proteasa del HIV, eritromicina, claritromicina, telitromicina y nefazodona)…»AEMPS, section 4.3 · Open on CIMA
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«?? Administració n concomitante de inhibidores potentes de la CYP3A4 (p. ej., itraconazol, ketoconazol, inhibidores de la proteasa del HIV, eritromicina, claritromicina, telitromicina y nefazodona)…»AEMPS, section 4.3 · Open on CIMA
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«?? Administració n concomitante de inhibidores potentes de la CYP3A4 (p. ej., itraconazol, ketoconazol, inhibidores de la proteasa del HIV, eritromicina, claritromicina, telitromicina y nefazodona)…»AEMPS, section 4.3 · Open on CIMA
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«?? Administració n concomitante de inhibidores potentes de la CYP3A4 (p. ej., itraconazol, ketoconazol, inhibidores de la proteasa del HIV, eritromicina, claritromicina, telitromicina y nefazodona)…»AEMPS, section 4.3 · Open on CIMA
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«Amiodarona y verapamilo: Por tanto, el uso combinado de lovastatina no debe superar los 40mg al día en pacientes que reciben medicación concomitante con amiodarona o verapamilo, a menos que sea…»AEMPS, section 4.5 · Open on CIMA
«Interacciones que afectan a la CYP3A4: Por tanto, la combinación con itraconazol, ketoconazol, inhibidores de la proteasa del HIV, eritromicina, claritromicina, telitromicina y nefazodona está…»AEMPS, section 4.5 · Open on CIMA
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«Mientras dure el tratamiento: La dosis de lovastatina no debe superar los 20mg al día en pacientes que reciben medicación concomitante con ciclosporina, danazol, gemfibrozilo, o dosis hipolipemiantes…»AEMPS, section 4.4 · Open on CIMA
«?? Administració n concomitante de inhibidores potentes de la CYP3A4 (p. ej., itraconazol, ketoconazol, inhibidores de la proteasa del HIV, eritromicina, claritromicina, telitromicina y nefazodona)…»AEMPS, section 4.3 · Open on CIMA
«Interacciones que afectan a la CYP3A4: Por tanto, la combinación con itraconazol, ketoconazol, inhibidores de la proteasa del HIV, eritromicina, claritromicina, telitromicina y nefazodona está…»AEMPS, section 4.5 · Open on CIMA
«Derivados cumarínicos: Cuando se administran concomitantemente lovastatina y anticoagulantes cumarínicos, el tiempo de protrombina puede aumentar en algunos pacientes. Se recomienda determinar el…»AEMPS, section 4.5 · Open on CIMA
«CONTRAINDICATIONS: Lipid-Modifying Agents: Lomitapide, lovastatin, simvastatin»FDA, section 4 · Open on DailyMed
«Claritromicina no se debe usar concomitantemente con los inhibidores de la HMG-CoA reductasa (estatinas) que son ampliamente metabolizados por la CYP3A4 (lovastatina o simvastatina), debido al…»AEMPS, section 4.3 · Open on CIMA
«CONTRAINDICATIONS: Lomitapide, lovastatin, and simvastatin (4.5)»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Lipid-modifying Agents: lomitapide, lovastatin, simvastatin»FDA, section 4 · Open on DailyMed
«INHIBIDORES DE LA HMG CO-A REDUCTASA: El aumento de las concentraciones plasmáticas de lovastatina o simvastatina puede provocar miopatía e incluso rabdomiólisis. Por tanto, está contraindicada la…»AEMPS, section 4.5 · Open on CIMA
«CONTRAINDICATIONS: • Alpha 1-adrenoreceptor antagonist: alfuzosin • Anti-gout: colchicine, in patients with renal and/FDA, section 4 · Open on DailyMed
«Tratamiento simultáneo con astemizol, terfenadina, disopiramida, cisaprida, pimocida, alcaloides del cornezuelo (como la ergotamina y la dihidroergotamina), simvastatina, atorvastatina o lovastatina.»AEMPS, section 4.3 · Open on CIMA
«Drug Interactions: Additionally, the following other drugs are contraindicated with ketoconazole tablets: methadone, disopyramide, dronedarone, ergot alkaloids such as dihydroergotamine, ergometrine…»FDA, section 4 · Open on DailyMed
«Inhibidores de la HMG-CoA reductasa p.ej., simvastatina, lovastatina, ya que el incremento de las concentraciones plasmáticas de estos fármacos puede producir rabdomiolisis.»AEMPS, section 4.3 · Open on CIMA
«Administración concomitante con los inhibidores de la HMG-CoA reductasa simvastatina, lovastatina y atorvastatina (ver sección 4.5).»AEMPS, section 4.3 · Open on CIMA
«HMG-CoA Reductase Inhibitors Primarily Metabolized Through CYP3A4: Coadministration with the HMG-CoA reductase inhibitors that are primarily metabolized through CYP3A4 (e.g., atorvastatin…»FDA, section 4 · Open on DailyMed
«Inhibidores de la HMG Co-reductasa: Los inhibidores de la HMG-Co-reductasa, como lovastatina y simvastatina, son altamente dependientes del metabolismo por CYP3A, se espera que presenten un marcado…»AEMPS, section 4.5 · Open on CIMA
«CONTRAINDICATIONS: HMG-CoA Reductase Inhibitors: lovastatin, simvastatin»FDA, section 4 · Open on DailyMed
«Sustratos CYP P450 3A4: Estatinas: el riesgo de toxicidad muscular aumenta con la administración concomitante de amiodarona con estatinas metabolizadas por el CYP 3A4, tales como simvastatina…»AEMPS, section 4.5 · Open on CIMA
«DRUG INTERACTIONS: HMG-CoA Reductase Inhibitors simvastatin, lovastatin, atorvastatin Increased plasma concentration of HMGCoA reductase inhibitor. Limit the dose of lovastatin to 40 mg. Limit the…»FDA, section 7 · Open on DailyMed
«Effects of Ranolazine on Other Drugs: Drugs Metabolized by CYP3A Limit the dose of simvastatin in patients on any dose of ranolazine extended-release tablets to 20 mg once daily, when ranolazine is…»FDA, section 7 · Open on DailyMed
«Medicamentos metabolizados por CYP3A4: Simvastatina: la administración concomitante de ticagrelor y simvastatina aumentó la C max de la simvastatina en un 81% y el AUC en un 56%, y también aumentó la…»AEMPS, section 4.5 · Open on CIMA
«Simvastatin, Lovastatin, Rosuvastatin: Ticagrelor increases serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4. Avoid simvastatin and lovastatin doses…»FDA, section 7 · Open on DailyMed
«El tratamiento con inhibidores de HMG CoA reductasa (por ejemplo simvastatina, atorvastatina o lovastatina) en un paciente que tome verapamilo debe iniciarse con la dosis más baja posible y valorarse…»AEMPS, section 4.5 · Open on CIMA
«Fármacos hipolipemiantes/AEMPS, section 4.5 · Open on CIMA
«Table 4. Other Potentially Significant Drug Interactions Concomitant Drug Class or Food Noted or Anticipated Outcome Clinical Comment HMG-Co A Reductase Inhibitors: atorvastatin, fluvastatin…»FDA, section 7 · Open on DailyMed
«Estatinas (simvastatina, lovastatina): diltiazem es un inhibidor de la CYP3A4 y ha demostrado que aumenta significativamente el AUC de algunas estatinas. El riesgo de miopatía y rabdomiolísis por…»AEMPS, section 4.5 · Open on CIMA
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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.
AEMPS summary of product characteristics (section 4.6): lovastatin is contraindicated in pregnancy, and no controlled clinical trials have been done in pregnant women. There have been rare reports of congenital anomalies after intrauterine exposure to HMG-CoA reductase inhibitors, but in an analysis of about 200 prospectively followed pregnancies exposed in the first trimester to lovastatin or a closely related HMG-CoA reductase inhibitor, the rate of anomalies was comparable to that in the general population; this number was statistically enough to exclude a 2.5-fold or greater increase. Maternal lovastatin may lower fetal levels of mevalonate, a precursor of cholesterol synthesis, and because atherosclerosis is a chronic process, stopping lipid-lowering drugs during pregnancy should have little impact on the long-term risk of primary hypercholesterolaemia. Lovastatin is not taken by women who are pregnant, trying to conceive or suspect pregnancy; treatment is stopped for the whole pregnancy or until pregnancy has been ruled out.
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.
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Omega-3 triglycerides (EPA and DHA), Pitavastatin, Pravastatin, Rosuvastatin, Simvastatin, Atorvastatin + Ezetimibe, Fluvastatin, Rosuvastatin + Ezetimibe