Lovastatin

Selected IR labeling covers dietary adjunct treatment of primary hypercholesterolemia, including heterozygous familial/nonfamilial forms, coronary primary prevention in the specified at-risk phenotype, and slowing coronary atherosclerosis in coronary heart disease. Archived Altoprev label covers adult primary hyperlipidemia including HeFH, slowing coronary atherosclerosis and reducing MI, unstable angina and revascularization in adults at high CHD risk. These labels do not supply a complete contemporary ASCVD treatment algorithm.

Selected IR covers boys ages 10–17 and girls ages 10–17 at least 1 year after menarche following adequate diet trial, with LDL-C >189 mg/dL, or >160 mg/dL plus family history of premature cardiovascular disease or at least two other cardiovascular risk factors. Prepubertal/below 10 use is not studied. Altoprev pediatric safety/effectiveness is unestablished; do not transplant IR age approval to ER.

IR dosing uses the evening meal. The archived ER PI specifies evening administration and whole tablets; its PK shows food lowers exposure, so do not copy IR meal instructions onto ER. ER missed dose: take as soon as possible, never double. Assess LDL response as early as 4 weeks for ER; if high-intensity treatment is required or goals unmet at 60 mg, its label calls for alternative LDL-lowering therapy. No automatic IR/ER substitution, universal LDL goal or current ER availability is inferred.

Selected IR: hypersensitivity, active liver disease or unexplained persistent transaminase elevations, strong CYP3A inhibitors, and retained pregnancy/lactation contraindication wording. Archived March 2024 ER: hypersensitivity, acute liver failure/decompensated cirrhosis, and strong CYP3A inhibitors including erythromycin; pregnancy/lactation contraindications were removed. FDA 2021 requests removal of blanket pregnancy contraindications for the class. Do not use retained IR wording as an unqualified current class rule; reconcile exact product with prescriber/pharmacist.

Selected IR and archived ER labels have no boxed warning. The FDA pregnancy communication concerns removal of a contraindication, not removal of a boxed warning.

IR trials reported gastrointestinal symptoms, headache, myalgia/cramps, rash and dizziness. ER trials most commonly reported infection, headache and accidental injury; trial reports do not prove drug causality or permit direct product comparisons. Postmarketing reports include serious hypersensitivity, hepatic failure, reversible cognitive symptoms, IMNM and, in ER labeling, new/worsened myasthenia gravis. No specific overdose antidote is known; contact Poison Help/medical toxicology. IR label says human dialyzability is unknown; do not invent an effective dialysis regimen.

Check prothrombin time/INR before and frequently after initiation or dose changes with coumarin anticoagulants; archived ER also specifies after discontinuation. Once stable, return to usual monitoring intervals. Review all prescriptions, OTC products and supplements rather than relying on a short interaction list.

CrCl <30 mL/min: >20 mg/day requires careful risk/benefit consideration and monitoring; ER has no mild/moderate renal adjustment recommendation. IR contraindicates active liver disease/persistent unexplained transaminase elevation; ER contraindicates acute liver failure/decompensated cirrhosis. Older age raises muscle risk; use cautious dose selection and interaction assessment rather than a fixed percentage dose reduction.

Selected current IR repack retains older pregnancy/lactation contraindications. FDA 2021 and archived ER March 2024 remove a blanket pregnancy contraindication: most pregnant patients discontinue statins, while rare very-high-risk cases require individualized ongoing-need assessment. Notify prescriber promptly about suspected pregnancy; inadvertent early exposure is not proof of fetal harm. Breastfeeding is not recommended when statin therapy is required; consider clinician-directed temporary interruption or alternative feeding. These changes do not establish unrestricted pregnancy use.

IR is bounded to the labeled adolescent HeFH group, with maximum 40 mg/day; no prepubertal or below 10 regimen. Counsel adolescent females about pregnancy planning. ER pediatric efficacy/safety unestablished; no dose is inferred from adult ER or adolescent IR.

The active β-hydroxyacid inhibits HMG-CoA reductase, reducing hepatic cholesterol synthesis and increasing LDL-receptor-mediated clearance. LDL-C falls; maximal effect develops over weeks rather than immediately after a single dose.

Extensive hepatic first-pass extraction produces low/variable systemic active-inhibitor availability. Lovastatin and its hydroxyacid are >95% protein-bound; CYP3A4 metabolism explains major interactions. IR active/total inhibitory activity peaks about 2–4 hours, with lower exposure fasting than after a meal. ER prolongs absorption and lowers peaks relative to IR; food reduces ER exposure. Severe renal insufficiency increases inhibitory-activity exposure. No universal half-life or bioequivalence assumption is supplied.

Obtain baseline lipids and liver assessment; reassess lipids after initiation/titration at the product-specific interval and liver enzymes when clinically indicated. Assess muscle symptoms, renal risk, interacting drugs, thyroid disease and glucose risk. CK testing is driven by clinical concern rather than a universal monthly panel. Follow INR closely when warfarin therapy and lovastatin change.

Report new muscle pain/weakness, dark urine, jaundice, severe fatigue or persistent symptoms after stopping. Avoid grapefruit and review new antibiotics or antifungals before use. IR with evening meal; archived ER whole in evening, separate instructions. Do not increase dose above an interaction ceiling to compensate for LDL response. Discuss pregnancy and feeding promptly and retain exact-product label.

Tablet

20 mg, light green, round, uncoated; LU on one side, G02 on the other.

Selected repack

RemedyRepack from Lupin; NDC 70518-2009-00 bottle 90, -01 blister 30.

Status

Prescription oral statin; verify exact manufacturer/strength/release type.

IR label regimen

10–80 mg/day labeled adult range; representative repack reviewed is 20 mg, not a claim that every package contains every tablet strength.

Altoprev historical ER

March 2024 label lists 20,40,60 mg; Andrx logo plus strength on orange/peach/light-peach round convex tablets.

Current FDA record

NDA 021316 lists 10,20,40,60 mg ER products Discontinued. Last listed full PI is March 14,2024; historical 10 mg listing is not a current PI dosing option.

Selected IR 25°C, excursions 15–30°C, well-closed light-resistant container. Archived ER 20–25°C, excursions 15–30°C, avoid excess heat/humidity; do not crush/chew/split. Current FDA discontinued listing is retained, with no new-stock or interchangeable-product claim.