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HMG-CoA Reductase Inhibitor

Aka: HMG-CoA Reductase Inhibitor, 3-Hydroxy-3-Methyl-Glutaryl Coenzyme A Reductase, Statin, Lovastatin, Simvastatin, Pravastatin, Atorvastatin, Fluvastatin, Rosuvastatin, Zocor, Lipitor, Crestor
  1. See Also
    1. Hyperlipidemia
    2. Statin-Induced Myopathy
  2. Indications
    1. Hyperlipidemia
      1. Most Statins are approved down to age 10 years (age 8 years for Pravastatin)
      2. If used in children and teens, LDL Cholesterol above 190 is an indication for Statins
    2. Coronary Artery Disease
  3. Mechanism: Effects
    1. Lipid-related effects
      1. LDL decreased (20-40%)
      2. HDL Increased (5-15%)
      3. Triglycerides decreased
        1. Atorvastatin (40%)
        2. Simvastatin (30%)
        3. Other Statins (10-20%)
    2. Other effects (related to decreased coronary events)
      1. Antiproliferation effect on smooth muscle cells
      2. Antioxidant and anti-inflammatory effects
    3. Outcomes: Primary Prevention
      1. NNT taken four years to prevent one coronary event: 81
      2. NNT taken four years to prevent one cerebrovascular event: 81
    4. Outcomes: Secondaary Prevention
      1. NNT taken five years to prevent one death: 50
      2. NNT taken two years to prevent one fatal MI: 77
  4. Contraindications
    1. Drug Interactions (see below): Myopathy or hepatitis
    2. Pregnancy
    3. Active or Chronic Liver Disease
      1. Now Statins thought safe despite liver disease
        1. Chalasani (2004) Gastroenterology 126(5): 1287-92
        2. Vuppalanchi (2005) Am J Med Sci 329(2):62-5
      2. May be beneficial in non-Alcoholic Steatohepatitis
        1. Rallidis (2004) Atherosclerosis 174(1): 193-6
  5. Efficacy
    1. Findings
      1. Reduces Myocardial Infarction risk (30%)
        1. Reduces need for Angioplasty (47 vs 20)
        2. Associated with regression on angiogram
      2. Reduces coronary death rate (42%)
      3. Reduces Cerebrovascular Accident risk (30%)
      4. Conflicting evidence on reducing Dementia risk
        1. Recent prospective articles do not suggest benefit
        2. Rea (2005) Arch Neurol 62:1047-51
      5. Reduces C-Reactive Protein
        1. Inflammatory factors related to ACS pathogenesis
        2. May explain benefit to normolipidemic patients
    2. References
      1. (1994) Lancet 344(8934):1383-9
      2. (1997) FDC Reports 59(46):T&G6
      3. (2004) Lancet 363:757-67
      4. Jick (2000) Lancet 356:1627-31
      5. Jukema (1995) Circulation 91:2528-40
      6. Ridker (2001) N Engl J Med 344:1959-65
      7. Sacks (1996) N Engl J Med 335:1001-9
  6. Precautions
    1. Do not stop Statins abruptly (worse CAD outcomes)
  7. Adverse Effects
    1. Statin-Induced Myopathy
    2. Mild Gastrointestinal upset
    3. Rash
    4. Insomnia (seen more with lipophilic agents)
      1. May be reduced with Pravastatin or Fluvastatin
    5. Liver Function Abnormalities (1-2% Incidence)
      1. AST and ALT increased 2-3x Normal
    6. Lupus-like syndrome
    7. Peripheral Neuropathy
    8. Concurrent use with Coumadin increases bleeding risk
  8. Adverse Effects: Possible
    1. Cognitive Impairment
      1. Subjective patient reports but not found in studies
      2. Statins may also protect cognitive function by affecting atherosclerosis
      3. Consider a water soluble Statin (e.g. Pravastatin) that does not cross blood-brain barrier
      4. Wagstaff (2003) Pharmacotherapy 23(7):871-80
  9. Compliance/Tolerance
    1. Discontinuation rate with Statins: 15%
    2. Discontinuation rate with other medications: 35%
  10. Pharmacokinetics
    1. First-pass metabolism in all Statins except Pravastatin
    2. Protein binding
      1. Most Statins are 90% protein bound
      2. Pravastatin is 50% protein bound
    3. Cytochrome P450 Metabolism
      1. CYP3A4 isoenzyme metabolizes most Statins
      2. CYP2C9 isoenzyme metabolizes Fluvastatin
      3. Pravastatin is not metabolized by P450 system
        1. Safer to use in combination with other drugs
    4. Renal elimination occurs most with Pravastatin
  11. Preparations (from least to most potent)
    1. Fluvastatin (Lescol)
      1. Dose 20 mg lowers LDL 17% (recommended starting dose)
      2. Dose 40 mg lowers LDL 23%
      3. Dose 80 mg lowers LDL 33%
    2. Pravastatin (Pravachol)
      1. Dose 10 mg lowers LDL 19%
      2. Dose 20 mg lowers LDL 24% (recommended starting dose)
      3. Dose 40 mg lowers LDL 34%
      4. Dose 80 mg lowers LDL 40%
    3. Lovastatin (Mevacor)
      1. Starting Dose: 20 mg qd
      2. Dose 20 mg lowers LDL 29% (recommended starting dose)
      3. Dose 40 mg lowers LDL 31%
      4. Dose 80 mg lowers LDL 48%
    4. Cerivastatin (Baycol, not available in US)
      1. Cerivastatin recalled in United States (August 2001)
      2. Dose 0.2 mg lowers LDL 25% (start if Renal Failure)
      3. Dose 0.3 mg lowers LDL 30% (recommended start dose)
      4. Dose 0.4 mg lowers LDL 36%
      5. Dose 0.8 mg lowers LDL 44%
    5. Simvastatin (Zocor)
      1. Dose 10 mg lowers LDL 28%
      2. Dose 20 mg lowers LDL 35% (recommended starting dose)
      3. Dose 40 mg lowers LDL 40% (maximum dose recommended in U.S. as of 2011)
      4. Dose 80 mg lowers LDL 48% (dose no longer recommended due to complications)
    6. Atorvastatin (Lipitor)
      1. Dose 10 mg lowers LDL 38% (recommended starting dose)
      2. Dose 20 mg lowers LDL 46%
      3. Dose 40 mg lowers LDL 51%
      4. Dose 80 mg lowers LDL 54%
      5. Triglycerides lowered 40%
    7. Rosuvastatin (Crestor)
      1. Dose 5 mg lowers LDL 45%
      2. Dose 10 mg lowers LDL: 52%
      3. Dose 20 mg lowers LDL 55%
      4. Dose 40 mg lowers LDL: 63%
      5. Indications to start at lower dose (5 mg)
        1. Asians
          1. Higher drug levels leads to higher toxicity risk
        2. Renal insufficiency (max 10 mg if CrCl < 30 ml/min)
        3. Hypothyroidism (uncontrolled)
        4. Age over 65 years
        5. Cyclosporine use (max dose 5 mg daily)
        6. Concurrent Gemfibrozil (max dose 10 mg daily)
  12. Management: Statin choices if special concerns
    1. Preferred agents if risk of drug interactions
      1. Pravastatin (no CYP 450 METABOLISM)
      2. Fluvastatin
    2. Preferred agents if Renal Function impaired
      1. Atorvastatin
      2. Fluvastatin
      3. Avoid Pravastatin if Creatinine Clearance <60 ml/min
        1. If used, start dosing at 10 mg and titrate slowly
  13. Monitoring: Liver transaminase testing (AST,ALT)
    1. No history of liver disease
      1. Stop Statin if >3x over baseline
      2. Liver Transaminase testing (AST, ALT) schedule
        1. Baseline
        2. Week 6
        3. Month 3
        4. Every 6 months to yearly
    2. Chronic Liver Disease history
      1. Start with lower initial Statin dose
      2. Stop Statin if transaminase >2x over baseline
      3. Liver Transaminase testing (AST, ALT) schedule
        1. Baseline
        2. Two weeks
        3. One month
        4. Two months
        5. Three months
  14. Drug Interactions (See Contraindications above)
    1. CYP3A4 Inhibitors
      1. Azole Antifungals (Intraconazole, Ketoconazole - 10-20 fold increase in Statin serum levels)
        1. Avoid with Lovastatin or Simvastatin
        2. Avoid with Atorvastatin over 20 mg daily
      2. Calcium Channel Blocker
        1. Diltiazem
          1. Avoid with Lovastatin over 20 mg daily
          2. Avoid with Simvastatin over 10 mg daily
        2. Verapamil (6-10 fold increase in Statin serum levels)
          1. Avoid with Lovastatin over 40 mg daily
          2. Avoid with Simvastatin over 20 mg daily
      3. Grapefruit juice increases some Statin levels
        1. Drugs affected: Lipitor, Zocor, Mevacor
        2. Drugs not affected: Pravachol, Crestor, Lescol
        3. Limit Grapefruit juice to 8 ounces daily (effects more likely to manifest at 32 ounces)
        4. Limit juice timing to opposite Statin dose
          1. Take juice at night, if Statin taken in morning
        5. References
          1. Reamy (2007) Am Fam Physician 76:190-1
    2. CYP3A4/oragnic anion transporting polypeptide inhibitors
      1. Cyclosporine (10-20 fold increase in Statin serum levels)
        1. Avoid with Atorvastatin over 10 mg daily
        2. Avoid with Lovastatin over 20 mg daily
        3. Avoid with Rosuvastatin over 5 mg daily
        4. Avoid with pitavastatin, Pravastatin
        5. Avoid with Fluvastatin
      2. Macrolides (Erythromycin, Azithromycin, Clarithromycin - 6-10 fold increase in Statin serum levels)
        1. Avoid while on Lovastatin and Simvastatin (or stop Statin while on Macrolide)
        2. Avoid with pitavastatin over 1 mg daily
        3. Avoid with Atorvastatin over 20 mg daily
      3. Protease inibitors (Atazanavir, Ritonavir, Lopinavir/Ritonavir)
        1. Avoid with Lovastatin, pitavastatin, and Simvastatin
        2. Avoid with Atorvastatin over 20 mg daily
        3. Avoid with Rosuvastatin over 10 mg daily
    3. CYP3A4/CYP2C9 Inhibitor
      1. Amiodarone
        1. Avoid with Lovastatin over 40 mg daily
        2. Avoid with Simvastatin over 20 mg daily
        3. Caution with Fluvastatin and Atorvastatin (consider dose adjustment)
    4. 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 Simvastatin over 10 mg daily
        2. Avoid with Rosuvastatin over 10 mg daily
        3. Avoid with Lovastatin over 20 mg daily
        4. Avoid with Pravastatin
        5. Caution with Fluvastatin or pitavastatin
    5. CYP2C9 Inhibitor
      1. Fluconazole (Diflucan)
        1. Caution with Fluvastatin
    6. Other interactions
      1. Mibefradil (Posicor)
      2. Niacin
      3. Alcohol
        1. Increases risk of liver enzyme elevations
  15. References
    1. Chong (2001) Am J Med 111:390-400
    2. Crouch (2001) Am Fam Physician 63(2):309-20
    3. Gillett (2011) Am fam Physician 83(6): 711-6
    4. Jones (1998) Am J Cardiol 81:582-7
    5. Sasaki (1998) Clin Ther 20:539-48

Hydroxymethylglutaryl-CoA Reductase Inhibitors (C0360714)

Definition (NCI) A class of agents that inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis.
Definition (CHV) cholesterol lowering drug
Definition (NCI) Any of a group of drugs that lower the amount of cholesterol and certain fats in the blood. Statins inhibit a key enzyme that helps make cholesterol. Statin drugs are being studied in the prevention and treatment of cancer.
Definition (MSH) Compounds that inhibit HMG-CoA reductases. They have been shown to directly lower cholesterol synthesis.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D019161
SnomedCT 372912004, 96302009
English HMG CoA Reductase Inhibitors, HMG-CoA Reductase Inhibitors, Inhibitors, HMG-CoA Reductase, Reductase Inhibitors, HMG-CoA, HMG-COA REDUCTASE INHIBITORS, HMG-CoA reductase inhibitor, NOS, Hydroxymethylglutaryl CoA Reductase Inhibitors, Hydroxymethylglutaryl-CoA Inhibitors, Hydroxymethylglutaryl-Coenzyme A Inhibitors, Inhibitors, HMG CoA Reductase, Inhibitors, Hydroxymethylglutaryl CoA, Inhibitors, Hydroxymethylglutaryl Coenzyme A, Inhibitors, Hydroxymethylglutaryl-CoA, Inhibitors, Hydroxymethylglutaryl-CoA Reductase, Inhibitors, Hydroxymethylglutaryl-Coenzyme A, Reductase Inhibitors, Hydroxymethylglutaryl-CoA, Statin, 3-Hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor (substance), 3-Hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, INHIB HMG COA REDUCTASE, INHIB HYDROXYMETHYLGLUTARYL COA, HMG COA REDUCTASE INHIB, HYDROXYMETHYLGLUTARYL COA REDUCTASE INHIB, HMG-CoA reductase inhibitors (medication), HMG-CoA reductase inhibitors, 808 HMG-COA REDUCTASE INHIBITORS, HMG-CoA Reductase Inhibitor, HMG-CoA Reductase Inhibitor [EPC], Hydroxymethylglutaryl-CoA Reductase Inhibitor, hydroxymethylglutaryl-coenzyme A reductase inhibitor, statin, HMG-CoA Statins, Statins, HMG CoA, Statins, HMG-CoA, HMG COA reductase inhibitor, HMG-CoA reductase inhibitor (product), HMG-CoA reductase inhibitor, Statins, HMG-CoA reductase inhibitor (substance), Hydroxymethylglutaryl CoenzymeA Reductase Inhibitors, 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) Reductase Inhibitors, Hydroxymethylglutaryl-CoA Reductase Inhibitors
Spanish inhibidor de la HMG - CoA reductasa, inhibidor de 3-hidroxi-3-metilglutaril coenzima A reductasa, inhibidor de 3-hidroxi-3-metilglutaril coenzima A reductasa (sustancia), inhibidor de la HMG - CoA reductasa (sustancia), inhibidor de la HMG-CoA reductasa (producto), inhibidor de la HMG-CoA reductasa (sustancia), inhibidor de la HMG-CoA reductasa, estatina, inhibidor de la 3-hidroxi-3-metilglutaril coenzima A reductasa, Estatinas HMG-CoA, Inhibidores de Hidroximetilglutaril-CoA Reductasas, Inhibidores de HMG CoA Reductasa
French Inhibiteurs de l'hydroxyméthylglutaryl-CoA réductase, Inhibiteurs de l'hydroxyméthylglutaryl-Coenzyme A réductase, Inhibiteurs de l'HMG-CoA réductase, Statines
Swedish Hydroximetylglutaryl-CoA-reduktashämmare
Czech HMG-CoA-reduktasa - inhibitory, hydroxymethylglutaryl-CoA-reduktasa - inhibitory, statiny
Finnish Hydroksimetyyliglutaryyli-KoA-reduktaasin estäjät
Russian GIDROKSIMETILGLUTARIL-KOA-REDUKTAZY INGIBITORY, HMG-COA REDUKTAZY INGIBITORY, GIDROKSIMETILGLUTARIL-KOA REDUKTAZY INGIBITORY, GMG-KOA REDUKTAZY INGIBITORY, STATINY GMG-KOA-REDUKTAZY, HMG-COA-РЕДУКТАЗЫ СТАТИНЫ, СТАТИНЫ ГМГ-КОA-РЕДУКТАЗЫ, HMG-COA-REDUKTAZY STATINY, HMG-COA РЕДУКТАЗЫ ИНГИБИТОРЫ, ГИДРОКСИМЕТИЛГЛУТАРИЛ-КОA-РЕДУКТАЗЫ ИНГИБИТОРЫ, ГИДРОКСИМЕТИЛГЛУТАРИЛ-КОА РЕДУКТАЗЫ ИНГИБИТОРЫ, ГМГ-КОA РЕДУКТАЗЫ ИНГИБИТОРЫ, ГМГ-КОА РЕДУКТАЗЫ ИНГИБИТОРЫ
Japanese ヒドロキシメチルグルタリルCoAレダクターゼ抑制剤, ヒドロキシメチルグルタリル-CoAレダクターゼ阻害剤, ヒドロキシメチルグルタリルCoAレダクターゼ阻害剤, HMG-CoA還元酵素阻害剤, HMG-CoAレダクターゼ抑制剤, HMG-CoAレダクターゼ阻害剤, HMG-CoAレダクターゼインヒビター, HMG-CoA還元酵素阻害薬
Polish Statyny, Inhibitory reduktazy 3-hydroksy-3-metyloglutarylokoenzymu A, HMG-CoA, Inhibitory reduktazy hydroksymetyloglutarylo CoA
German HMG-CoA-Reduktase-Inhibitoren, Hydroxymethylglutaryl-CoA-Reductase-Inhibitoren, Hydroxymethylglutaryl-CoA-Reduktase-Inhibitoren, Inhibitoren, HMG-CoA Reduktase, Inhibitoren, Hydroxymethylglutaryl-CoA, Inhibitoren, Hydroxymethylglutaryl-Coenzym A, Statine, HMG-CoA
Italian Inibitori della reduttasi del coenzima A idrossimetilglutarilico
Portuguese Estatinas de HMG-CoA, Inibidores de Hidroximetilglutaril-CoA Redutases, Inibidores de HMG-CoA Redutases
Sources
Derived from the NIH UMLS (Unified Medical Language System)


rosuvastatin (C0965129)

Definition (NCI) A statin with antilipidemic and potential antineoplastic activities. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. In addition, rosuvastatin, like other statins, exhibits pro-apoptotic, growth inhibitory, and pro-differentiation activities in a variety of tumor cell types; these antineoplastic activities may be due, in part, to inhibition of the isoprenylation of Ras and Rho GTPases and related signaling cascades.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C422923
SnomedCT 406436002
English rosuvastatin [Chemical/Ingredient], rosuvastatin, 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(ethyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-, (3R,5S,6E), Rosuvastatin, Rosuvastatin (product), ROSUVASTATIN
Spanish rosuvastatina (producto), rosuvastatina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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) 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 Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D008148
SnomedCT 74205000, 386024001, 96303004
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 (producto), lovastatina (sustancia), lovastatina-RETIRADO- (concepto no activo), lovastatina-RETIRADO-, lovastatina, mevinolina, monacolina K, Lovastatina, Mevinolina
French Lovastatine
German Lovastatin, Mevinolin
Italian Lovastatina
Portuguese Lovastatina, Mevinolina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Simvastatin (C0074554)

Definition (CHV) a kind of cholesterol- lowering drug
Definition (CHV) a kind of cholesterol- lowering drug
Definition (CSP) a derivative of lovastatin and inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG coA reductase), a rate limiting enzyme in the biosynthesis of cholesterol.
Definition (NCI) A lipid-lowering agent derived synthetically from a fermentation product of the fungus Aspergillus terreus. Hydrolyzed in vivo to an active metabolite, simvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. (NCI04)
Definition (MSH) A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.
Definition (PDQ) A lipid-lowering agent derived synthetically from a fermentation product of the fungus Aspergillus terreus. Hydrolyzed in vivo to an active metabolite, simvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=455226&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=455226&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C29454" NCI Thesaurus)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D019821
SnomedCT 387584000, 96304005
English synvinolin, Simvastatin, Synvinolin, [1S-[1alpha,3alpha,7beta,8beta(2S*,4S*),8abeta]]-1,2,3,7,8,8a-Hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl 2,2-dimethylbutanoate, simvastatin, HMG-CoA reductase inhibitors simvastatin, simvastatin (medication), SIMVASTATIN, Simvastatin [Chemical/Ingredient], simvastatin product, Velastatin, Simvastatin (product), Simvastatin (substance)
German Synvinolin, Simvastatin
Swedish Simvastatin
Czech simvastatin
Finnish Simvastatiini
Russian SIMVASTATIN, СИМВАСТАТИН
Japanese シンバスタチン
Italian Sinvinolina, Simvastatina
Polish Symwastatyna
Spanish simvastatina (producto), simvastatina (sustancia), simvastatina, simvastatin, Simvastatina
French Simvastatine
Portuguese Simvastatina, Sinvastatina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


atorvastatin (C0286651)

Definition (CHV) a kind of cholesterol lowering drug
Definition (NCI) The active ingredient in a drug used to lower the amount of cholesterol in the blood and to prevent stroke, heart attack, and angina (chest pain). It is also being studied in the prevention and treatment of some types of cancer and other conditions. Atorvastatin blocks an enzyme that helps make cholesterol in the body. It also causes an increase in the breakdown of cholesterol. It is a type of HMG-CoA reductase inhibitor and a type of statin.
Definition (CSP) a synthetic lipid-lowering agent; an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.
Definition (PDQ) A synthetic lipid-lowering agent. Atorvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. Atorvastatin also increases the number of LDL receptors on hepatic cell surfaces to enhance uptake and catabolism of LDL and reduces LDL production and the number of LDL particles. This agent lowers plasma cholesterol and lipoprotein levels and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=460239&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=460239&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C28837" NCI Thesaurus)
Definition (NCI) A synthetic lipid-lowering agent. Atorvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. Atorvastatin also increases the number of LDL receptors on hepatic cell surfaces to enhance uptake and catabolism of LDL and reduces LDL production and the number of LDL particles. This agent lowers plasma cholesterol and lipoprotein levels and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. (NCI04)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C065179
SnomedCT 391791009, 108600003, 373444002
English atorvastatin, ATORVASTATIN, (betaR,deltaR)-2-(p-Fluorophenyl)-beta,delta-dihydroxy-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-pyrrole-1-heptanoic Acid, (betaR,deltaR)-2-(4-Fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic Acid, Atorvastatin - chemical (substance), atorvastatin [Chemical/Ingredient], liptonorm, Atorvastatin, Atorvastatin (product), Atorvastatin (substance), Atorvastatin - chemical
Spanish Atorvastatin - chemical, atorvastatina (producto), atorvastatina (sustancia), atorvastatina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Lipitor (C0593906)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C065179
English Lipitor, lipitor
Sources
Derived from the NIH UMLS (Unified Medical Language System)


fluvastatin (C0082608)

Definition (NCI) A synthetic lipid-lowering agent with antilipidemic and potential antineoplastic properties. Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated antigen-presenting cells such as human vascular endothelial cells. Due to its anti-inflammatory effects mediated by alterations of lipid metabolism, fluvastatin may possess chemopreventive and therapeutic antineoplastic properties.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C065180
SnomedCT 387585004, 96307003
English 7-(3-(4-fluorophenyl)-1-(1-methylethyl)-1H-indol-2-yl)-3,5-dihydroxy-6-heptenoate, fluindostatin, fluvastatin, FLUVASTATIN, fluvastatin (medication), HMG-CoA reductase inhibitors fluvastatin, fluvastatin [Chemical/Ingredient], Fluvastatin, Fluvastatin (product), Fluvastatin (substance)
Spanish fluvastatina (producto), fluvastatina (sustancia), fluvastatina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Zocor (C0678181)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D019821
German Zocor
English zocor, Zocor
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Pravastatin (C0085542)

Definition (NCI) The active ingredient in a drug used to lower the amount of cholesterol in the blood and to prevent stroke and heart attack. It is also being studied in the treatment of cancer and other conditions. Pravastatin blocks an enzyme that helps make cholesterol in the body. It may also make tumor cells more sensitive to anticancer drugs. It is a type of HMG-CoA reductase inhibitor, a type of statin, and a type of chemosensitizer.
Definition (MSH) An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).
Definition (PDQ) A synthetic lipid-lowering agent. Pravastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. Pravastatin lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=424450&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=424450&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C29375" NCI Thesaurus)
Definition (NCI) A synthetic lipid-lowering agent. Pravastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. Pravastatin lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. (NCI04)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D017035
SnomedCT 96305006, 373566006
English Eptastatin, Pravastatin, 1-Naphthaleneheptanoic acid, 1,2,6,7,8,8a-hexahydro-beta,delta,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-, (1S-(1alpha(betaS*,deltaS*),2alpha,6alpha,8beta(R*),8aalpha))-, [1S-[1alpha(betaS*,deltaS*),2alpha,6alpha,8beta(R*),8aalpha]]-1,2,6,7,8,8a-Hexahydro-beta,!d,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-1-naphthaleneheptanoic Acid, HMG-CoA reductase inhibitors pravastatin, pravastatin (medication), pravastatin, Pravastatin [Chemical/Ingredient], Pravastatin (product), Pravastatin (substance), PRAV, PRAVASTATIN
Swedish Pravastatin
Czech eptastatin, pravastatin
Finnish Pravastatiini
Russian EPTASTATIN, PRAVASTATIN, ПРАВАСТАТИН, ЭПТАСТАТИН
Italian Eptastatina, Pravastatina
Polish Prawastatyna, Eptastatyna
Japanese エプタスタチン, プラバスタチン
Spanish pravastatina (producto), pravastatina (sustancia), pravastatina, pravastatin, Eptastatin, Pravastatina
French Eptastatine, Pravastatine
German Eptastatin, Pravastatin
Portuguese Eptastatina, Pravastatina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Rosuvastatin calcium (C1101751)

Definition (NCI) The calcium salt form of rosuvastatin, a statin with antilipidemic activity. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol.
Definition (NCI) A drug used to lower the amount of cholesterol and other harmful substances, such as triglycerides, in the blood. It is also being studied in the prevention and treatment of some types of cancer and other conditions. Crestor blocks an enzyme that helps make cholesterol in the body and it helps break down cholesterol. It also may cause cancer cells to die and may inhibit the growth of blood vessels that cancer cells need to grow. It is a type of HMG-CoA reductase inhibitor and a type of statin.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121) , Biologically Active Substance (T123)
MSH C422923
SnomedCT 406435003
English HMG-CoA reductase inhibitors rosuvastatin calcium, rosuvastatin calcium (medication), ROSUVASTATIN CALCIUM, rosuvastatin calcium, Rosuvastatin calcium (substance), Rosuvastatin calcium, Rosuvastatin Calcium
Spanish rosuvastatina cálcica (sustancia), rosuvastatina cálcica
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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