pharmacopeia
GET
/api/v1/drug/lovastatin
2D structure
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] (2S)-2-methylbutanoate
SMILES CC[C@H](C)C(=O)O[C@H]1C[C@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@@H]3C[C@H](CC(=O)O3)O)C
InChIKey PCZOHLXUXFIOCF-BXMDZJJMSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Cytochrome P450 3A4 Inhibitors; HIV Protease Inhibitors; Hydroxymethylglutaryl-CoA Reductase Inhibitors.

Cytochrome P450 3A4HIV ProteaseHydroxymethylglutaryl-CoA Reductase

Indications

Sourced from openFDA
  • Therapy with Lovastatin Tablets USP should be a component of multiple risk factor intervention in those individuals with dyslipidemia at risk for atherosclerotic vascular disease. Lovastatin Tablets USP should be used in addition to a diet restricted in saturated fat and cholesterol as part of a treatment strategy to lower total-C and LDL-C to target levels when the response to diet and other nonpharmacological measures alone has been inadequate to reduce risk.

Contraindications

Sourced from openFDA
  • Hypersensitivity to any component of this medication. Active liver disease or unexplained persistent elevations of serum transaminases (see WARNINGS ).contraindicated

Dosage & administration

Sourced from openFDA

The patient should be placed on a standard cholesterol-lowering diet before receiving lovastatin tablets and should continue on this diet during treatment with lovastatin tablets (see NCEP Treatment Guidelines for details on dietary therapy). Lovastatin tablets should be given with meals. Adult Patients The usual recommended starting dose is 20 mg once a day given with the evening meal. The recommended dosing range of lovastatin is 10 to 80 mg/day in single or two divided doses; the maximum recommended dose is 80 mg/day. Doses should be individualized according to the recommended goal of therapy (see NCEP Treatment Guidelines and CLINICAL PHARMACOLOGY ). Patients requiring reductions in LDL-C of 20% or more to achieve their goal (see INDICATIONS AND USAGE ) should be started on 20 mg/day of lovastatin tablets. A starting dose of 10 mg of lovastatin may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more. Cholesterol levels should be monitored periodically and consideration should be given to reducing the dosage of lovastatin tablets if cholesterol levels fall significantly below the targeted range. Dosage in Patients Taking Danazol, Diltiazem, Dronedarone or Verapamil In patients taking danazol, diltiazem, dronedarone or verapamil concomitantly with lovastatin, therapy should begin with 10 mg of lovastatin and should not exceed 20 mg/day (see CLINICAL PHARMACOLOGY , Pharmacokinetics , WARNINGS , Myopathy/Rhabdomyolysis , PRECAUTIONS , Drug Interactions , Other Drug Interactions ).

Warnings & precautions

Sourced from openFDA

Myopathy/Rhabdomyolysis Lovastatin, like other inhibitors of HMG-CoA reductase, occasionally causes myopathy manifested as muscle pain, tenderness or weakness with creatine kinase (CK) above ten times the upper limit of normal (ULN). Myopathy sometimes takes the form of rhabdomyolysis with or without acute renal failure secondary to myoglobinuria, and rare fatalities have occurred. The risk of myopathy is increased by high levels of HMG-CoA reductase inhibitory activity in plasma. The risk of myopathy/rhabdomyolysis is dose related. In a clinical study (EXCEL) in which patients were carefully monitored and some interacting drugs were excluded, there was one case of myopathy among 4933 patients randomized to lovastatin 20 to 40 mg daily for 48 weeks, and 4 among 1649 patients randomized to 80 mg daily. There have been rare reports of immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, associated with statin use. IMNM is characterized by: proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuation of statin treatment; muscle biopsy showing necrotizing myopathy without significant inflammation; improvement with immunosuppressive agents. All patients starting therapy with lovastatin, or whose dose of lovastatin is being increased, should be advised of the risk of myopathy and told to report promptly any unexplained muscle pain, tenderness or weakness particularly if accompanied by malaise or fever or if muscle signs and symptoms persist after discontinuing lovastatin.

Adverse reactions

Sourced from openFDA

Phase III Clinical Studies In Phase III controlled clinical studies involving 613 patients treated with lovastatin, the adverse experience profile was similar to that shown below for the 8,245 patient EXCEL study (see Expanded Clinical Evaluation of Lovastatin [EXCEL] Study ). Persistent increases of serum transaminases have been noted (see WARNINGS, Liver Dysfunction ). About 11% of patients had elevations of CK levels of at least twice the normal value on one or more occasions. The corresponding values for the control agent cholestyramine were 9 percent. This was attributable to the noncardiac fraction of CK. Large increases in CK have sometimes been reported (see WARNINGS , Myopathy/Rhabdomyolysis ). Expanded Clinical Evaluation of Lovastatin (EXCEL) Study Lovastatin was compared to placebo in 8,245 patients with hypercholesterolemia (total-C 240 to 300 mg/dL [6.2 to 7.8 mmol/L]) in the randomized, double-blind, parallel, 48 week EXCEL study. Clinical adverse experiences reported as possibly, probably or definitely drug-related in ≥ 1% in any treatment group are shown in the table below. For no event was the incidence on drug and placebo statistically different. Placebo (N = 1663) % Lovastatin 20 mg q.p.m. (N = 1642) % Lovastatin 40 mg q.p.m. (N = 1645) % Lovastatin 20 mg b.i.d. (N = 1646) % Lovastatin 40 mg b.i.d.

Use in specific populations

Sourced from openFDA

Pregnancy Teratogenic Effects Pregnancy Category X See CONTRAINDICATIONS . Safety in pregnant women has not been established. Lovastatin has been shown to produce skeletal malformations in offspring of pregnant mice and rats dosed during gestation at 80 mg/kg/day (affected mouse fetuses/total: 8/307 compared to 4/289 in the control group; affected rat fetuses/total: 6/324 compared to 2/308 in the control group). Female rats dosed before mating through gestation at 80 mg/kg/day also had fetuses with skeletal malformations (affected fetuses/total: 1/152 compared to 0/171 in the control group). The 80 mg/kg/day dose in mice is 7 times the human dose based on body surface area and in rats results in 5 times the human exposure based on AUC.

Overdosage

Sourced from openFDA

After oral administration of lovastatin to mice, the median lethal dose observed was > 15 g/m 2 . Five healthy human volunteers have received up to 200 mg of lovastatin as a single dose without clinically significant adverse experiences. A few cases of accidental overdosage have been reported; no patients had any specific symptoms, and all patients recovered without sequelae. The maximum dose taken was 5 to 6 g. Until further experience is obtained, no specific treatment of overdosage with lovastatin can be recommended. The dialyzability of lovastatin and its metabolites in man is not known at present.

Approval history

Sourced from openFDA
  • Dec 17, 2001ANDAANDA075551Teva
  • Jun 5, 2002ANDAANDA075991Carlsbad
  • Nov 1, 2007ANDAANDA078296Lupin

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
25,355 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective1,6746.6%
  2. 2Fatigue1,5336.0%
  3. 3Nausea1,3985.5%
  4. 4Diarrhoea1,2615.0%
  5. 5Dyspnoea1,2194.8%
  6. 6Dizziness1,1544.6%
  7. 7Pain1,0644.2%
  8. 8Headache1,0094.0%
  9. 9Asthenia9773.9%
  10. 10Fall8973.5%
  11. 11Arthralgia8173.2%
  12. 12Off Label Use8103.2%
  13. 13Death7883.1%
  14. 14Pain In Extremity7513.0%
  15. 15Vomiting7513.0%

Literature

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Recent PubMed references pinned to Lovastatin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 632 ClinicalTrials.gov registrations naming Lovastatin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Lovastatin. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Lovastatin work?
Mechanism-of-action classes: Cytochrome P450 3A4 Inhibitors; HIV Protease Inhibitors; Hydroxymethylglutaryl-CoA Reductase Inhibitors.
What is Lovastatin used for?
According to FDA labeling, Lovastatin carries indications including: Therapy with Lovastatin Tablets USP should be a component of multiple risk factor intervention in those individuals with dyslipidemia at risk for atherosclerotic vascular disease. Lovastatin Tablets USP should be used in addition to a diet restricted in saturated fat and cholesterol as part of a treatment strategy to lower total-C and LDL-C to target levels when the response to diet and other nonpharmacological measures alone has been inadequate to reduce risk.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Lovastatin?
Lovastatin is classified as HMG CoA reductase inhibitors, HMG-CoA Reductase Inhibitor, Cytochrome P450 3A4 Inhibitors, HIV Protease Inhibitors, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Decreased Cholesterol Synthesis.
What are the brand names for Lovastatin?
Lovastatin is marketed under brand names including Altoprev.
What are the contraindications for Lovastatin?
Lovastatin labeling lists contraindications including: Hypersensitivity to any component of this medication. Active liver disease or unexplained persistent elevations of serum transaminases (see WARNINGS ).. Always consult the full prescribing information and a clinician.
Note. Data for lovastatin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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