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gemfibrozil (Lopid)

Tradename: Lopid. Indication: 1) treatment of hypertriglyceridemia 2) treatment of hypoalphalipoproteinemia Contraindications: 1) severe hepatic or renal failure 2) primary cirrhosis or gall bladder disease 3) concurrent administration of cerivastatin (Baycol) & perhaps other HMG CoA reductase inhibitors; use fenofibrate instead [7] Dosage: 600 mg PO BID. Tabs 300, 600 mg. Pharmacokinetics: 1) completely absorbed from GI tract 2) 98% of plasma gemfibrozil is bound to albumin 3) conjugated in the liver, mostly to glucuronide & excreted in the urine (70%) 4) < 2% excreted unchanged in the urine 5) some enterohepatic circulation 6) elimination 1/2life is 1.5-2 hours 7) maximum decrease in triglycerides should occur within 4-12 weeks Monitor: - complete blood count (CBC) periodically during the 1st 12 months of therapy [8] - liver function tests periodically [8] Adverse effects: 1) common (> 10%) - dyspepsia - abdominal pain - cholelithiasis 2) less common (1-10%) - diarrhea, nausea/vomiting, constipation, acute appendicitis, fatigue, vertigo, headache, eczema, rash 3) uncommon (< 1%) - paresthesia, hypoesthesia, atrial fibrillation, dizziness, drowsiness, somnolence, mental depression, flatulence, blurred vision 4) others [5] - leukopenia - thrombocytopenia - impotence, decreased male fertility - lupus-like syndrome Drug interactions: 1) may potentiate anticoagulant effect of warfarin [9] 2) may potentiate adverse effects of HMG CoA reductase inhibitors (statins) a) myopathy b) rhabdomyolysis c) acute renal failure d) pravastatin is best statin to use if combination of statin & gemfibrozil is indicated [4] 3) gemfibrozil MAY BE USED with niacin [4] 4) gemfibrozil may inhibit cyt P450 3A4 [6] Mechanism of action: 1) fibrinic acid derivative 2) decreases serum triglyceride levels 3) decreases serum VLDL cholesterol 4) increases serum HDL cholesterol 5) effects on serum LDL cholesterol are variable 6) increases in serum LDL cholesterol are observed in patient with type IV hyperlipoproteinemia 7) inhibits peripheral lipolysis 8) decreases hepatic extraction of free fatty acids 9) reduces serum triglycerides 10) inhibits synthesis & clearance of apolipoprotein B 11) maximal effect a) total cholesterol: decrease of 10% b) LDL cholesterol: decrease of 10% c) HDL cholesterol: increase of 10% d) triglycerides: decrease of 50%

Interactions

drug interactions drug adverse effects (more general classes) monitor with fibrates

Related

high density lipoprotein (HDL) hyperlipoproteinemia (HLP) lipid panel (fasting lipid panel, FLP) low density lipoprotein (LDL, beta-lipoprotein) triglyceride very low density lipoprotein (VLDL)

General

fibrate

Properties

MISC-INFO: elimination route LIVER KIDNEY 1/2life 1.5-2 HOURS pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
  5. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  6. Prescriber's Letter 10(6):31-32 2003
  7. Prescriber's Letter 16(8): 2009 Clinically Significant Statin Drug Interactions Detail-Document#: 250812
  8. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com
  9. Dixon DL, Williams VG. Interaction between gemfibrozil and warfarin: case report and review of the literature. Pharmacotherapy. 2009 Jun;29(6):744-8. Review. PMID: 19476425