Lovastatin

Aka: Lovastatin, Mevacor, Altoprev

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II. Indications

  1. See Hyperlipidemia Management for formal criteria
  2. See Statin
  3. Hyperlipidemia
  4. Primary of vascular disease progression (e.g. CAD, CVA, DM, CKD, PAD)

III. Contraindications

  1. See Statin
  2. Drug Interactions
    1. See Statin regarding Myopathy and hepatitis risk
  3. Pregnancy (Teratogen)
  4. Acute Liver Failure or decompensated Cirrhosis

IV. Mechanism

  1. See Statin

V. Efficacy

  1. See Statin
  2. Lovastatin 10 mg lowers LDL 21%
  3. Lovastatin 20 mg lowers LDL 24 to 29% (recommended starting dose)
  4. Lovastatin 40 mg lowers LDL 30 to 31%
  5. Lovastatin 80 mg lowers LDL 40 to 48%

VI. Adverse Effects

  1. See Statin
  2. See Statin-Induced Myopathy

VII. Safety

  1. Pregnancy Category X
  2. Contraindicated in Lactation

VIII. Pharmacokinetics

  1. See Statin
  2. Undergoes first pass metabolism as with most Statins (except Pravastatin)
  3. Protein binding
    1. As with most Statins (except Pravastatin), Lovastatin is 90% Protein bound
  4. Cytochrome P450 Metabolism
    1. CYP3A4 isoenzyme metabolizes most Statins, including Lovastatin

IX. Dosing: Adult

  1. Specific LDL and HDL targets have been replaced with high-intensity Statin if 10 year Cardiovascular Risk >20%
  2. Low intensity Statin (age >75 years, or Statin intolerant)
    1. Lovastatin 20 to 40 mg orally daily (maximum 80 mg/day)

X. Dosing: Child

  1. Approved for children over age 10 to 17 years old with heterozygous Familial Hyperlipidemia
  2. Start 10 mg orally daily
  3. Maximum: 40 mg/day

XI. Monitoring

  1. See Statin
  2. Liver transaminase testing (AST,ALT) is no longer routinely indicated as of March 2012

XII. Drug Interactions (See Contraindications above)

  1. See Statin
  2. CYP3A4 Inhibitors
    1. Azole Antifungals (Intraconazole, Ketoconazole - 10-20 fold increase in Statin serum levels)
      1. Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
      2. Avoid with Lovastatin
    2. Calcium Channel Blocker
      1. Diltiazem (limit to 240 mg daily)
        1. Avoid with Lovastatin over 20 mg daily
      2. Verapamil (6-10 fold increase in Statin serum levels)
        1. Avoid with Lovastatin over 40 mg daily
    3. Grapefruit juice increases some Statin levels
      1. Lovastatin is among the drugs most affected
        1. Avoid with any Grapefruit juice (or minimal use)
      2. References
        1. (2016) Presc Lett 23(3):18
        2. Reamy (2007) Am Fam Physician 76:190-1 [PubMed]
  3. CYP3A4/organic anion transporting polypeptide inhibitors
    1. Cyclosporine (10-20 fold increase in Statin serum levels)
      1. Avoid with Lovastatin over 20 mg daily
    2. Macrolides (Erythromycin, Clarithromycin - 6-10 fold increase in Statin serum levels)
      1. Avoid while on Lovastatin (or stop Statin while on Macrolide)
      2. Azithromycin appears to be safe with Statins
    3. Protease inibitors (Atazanavir, Ritonavir, Lopinavir/Ritonavir)
      1. Avoid with Lovastatin
  4. CYP3A4/CYP2C9 Inhibitor
    1. Amiodarone
      1. Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
      2. Avoid with Lovastatin over 40 mg daily
    2. Warfarin (Increased INR and bleeding risk)
      1. Among the highest risk with Lovastatin
  5. CYP2C9, CYP2C19/oragnic anion transporting polypeptide inhibitors
    1. Gemfibrozil (2-3 fold increase in Statin serum levels, >13 fold increase in Rhabdomyolysis risk)
      1. Avoid with Lovastatin over 20 mg daily
  6. Other interactions
    1. Mibefradil (Posicor)
    2. Niacin
    3. Alcohol
      1. Increases risk of liver enzyme elevations

XIII. Resources

  1. See Statin
  2. Lovastatin Extended Release (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=8c0db100-5df9-49c3-8af9-1bc03ae609b9
  3. Lovastatin Regular Release (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=5c707089-fb5b-4016-8ca7-11bbcfb57854

XIV. References

  1. (2017) Presc Lett 24(11): 62
  2. (2012) Presc Lett 19(5): 25
  3. (2012) Presc Lett, Characteristics of Various Statins, #280502
  4. Carpenter (2019) Am Fam Physician 99(9):558-64 [PubMed]
  5. Chong (2001) Am J Med 111:390-400 [PubMed]
  6. Crouch (2001) Am Fam Physician 63(2):309-20 [PubMed]
  7. Gillett (2011) Am Fam Physician 83(6): 711-6 [PubMed]
  8. Jones (1998) Am J Cardiol 81:582-7 [PubMed]
  9. Sasaki (1998) Clin Ther 20:539-48 [PubMed]

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Related Studies

Cost: Medications

lovastatin (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
LOVASTATIN 10 MG TABLET Generic $0.05 each
LOVASTATIN 20 MG TABLET Generic $0.05 each
LOVASTATIN 40 MG TABLET Generic $0.06 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Ontology: Lovastatin (C0024027)

Definition (NCI) A lactone metabolite isolated from the fungus Aspergillus terreus with cholesterol-lowering and potential antineoplastic activities. Lovastatin is hydrolyzed to the active beta-hydroxyacid form, which competitively inhibits 3-hydroxyl-3-methylgutarylcoenzyme A (HMG-CoA) reductase, an enzyme involved in cholesterol biosynthesis. In addition, this agent may induce tumor cell apoptosis and inhibit tumor cell invasiveness, possibly by inhibiting protein farnesylation and protein geranylgeranylation, and may arrest cells in the G1 phase of the cell cycle. The latter effect sensitizes tumor cells to the cytotoxic effects of ionizing radiation.
Definition (NCI_NCI-GLOSS) A drug used to lower the amount of cholesterol in the blood. It is also being studied in the prevention and treatment of some types of cancer. Lovastatin is a type of HMG-CoA reductase inhibitor (statin).
Definition (MSH) A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.
Definition (CSP) HMG coA reductase inhibitor which inhibits cholesterol biosynthesis and thus lowers blood cholesterol levels; also blocks isoprenylation of protein CAAX motifs.
Definition (PDQ) A lactone metabolite isolated from the fungus Aspergillus terreus with cholesterol-lowering activity and potential antineoplastic activity. Lovastatin is hydrolyszed to the active beta-hydroxyacid form, which competitively inhibits 3-hydroxyl-3-methylgutarylcoenzyme A (HMG-CoA) reductase, an enzyme involved in the cholesterol biosynthesis. In addition, this agent may inhibit tumor cell proliferation and reduce tumor cell invasiveness, thereby decreasing tumor metastatic potential; induce tumor cell apoptosis, possibly by inhibiting protein geranylgeranylation and; arrest cells in the G1 phase of the cell cycle, an effect that sensitizes tumor cells to the cytotoxic effects of ionizing radiation. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41658&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41658&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C620" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D008148
SnomedCT 74205000, 386024001, 96303004
LNC LP171620-0
English 6 Methylcompactin, 6-Methylcompactin, Mevinolin, Butanoic acid, 2-methyl-, 1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-(2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl)-1-naphthalenyl ester, (1S-(1alpha(R*),3alpha,7beta,8beta(2S*,4S*),8abeta))-, Monacolin K, (2S)-2-Methylbutanoic Acid, (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-Hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl Ester, lovastatin, Lovastatin, mevinolin, lovastatin (medication), HMG-CoA reductase inhibitors lovastatin, LOVASTATIN, Lovastatin [Chemical/Ingredient], lovastatins, monacolin k, Lovastatin (product), Lovastatin (substance), Lovastatin -RETIRED-
Swedish Lovastatin
Czech lovastatin
Finnish Lovastatiini
Russian MEVINOLIN, LOVASTATIN, ЛОВАСТАТИН, МЕВИНОЛИН
Japanese メビノリン, ロバスタチン
Polish Lovastatin, Lowastatyna
Spanish lovastatina-RETIRADO- (concepto no activo), lovastatina-RETIRADO-, lovastatina (producto), lovastatina (sustancia), lovastatina, mevinolina, monacolina K, Lovastatina, Mevinolina
French Lovastatine
German Lovastatin, Mevinolin
Italian Lovastatina
Portuguese Lovastatina, Mevinolina
Derived from the NIH UMLS (Unified Medical Language System)

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