gemfibrozil (Lopid)
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Introduction
Tradename: Lopid.
Indications
- treatment of hypertriglyceridemia
- treatment of hypoalphalipoproteinemia
Contraindications
- severe hepatic or renal failure
- primary cirrhosis or gall bladder disease
- 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
- completely absorbed from GI tract
- 98% of plasma gemfibrozil is bound to albumin
- conjugated in the liver, mostly to glucuronide & excreted in the urine (70%)
- < 2% excreted unchanged in the urine
- some enterohepatic circulation
- elimination 1/2life is 1.5-2 hours
- maximum decrease in triglycerides should occur within 4-12 weeks
elimination via liver
elimination via kidney
1/2life = 1.5-2 hours
Monitor
- complete blood count (CBC) periodically during the 1st 12 months of therapy[8]
- liver function tests periodically[8]
Adverse effects
- common (> 10%)
- less common (1-10%)
- diarrhea, nausea/vomiting, constipation, acute appendicitis, fatigue, vertigo, headache, eczema, rash
- uncommon (< 1%)
- others[5]
- leukopenia
- thrombocytopenia
- impotence, decreased male fertility
- lupus-like syndrome
Drug interactions
- may potentiate anticoagulant effect of warfarin[9]
- may potentiate adverse effects of HMG CoA reductase inhibitors (statins)
- myopathy
- rhabdomyolysis
- acute renal failure
- pravastatin is best statin to use if combination of statin & gemfibrozil is indicated[4]
- gemfibrozil MAY BE USED with niacin[4]
- gemfibrozil may inhibit cyt P450 3A4[6]
- drug interaction(s) of statins with fibrates
- drug interaction(s) of gemfibrozil with pioglitazone
- drug interaction(s) of gemfibrozil with rosiglitazone
- drug interaction(s) of gemfibrozil with repaglinide
Mechanism of action
- fibrinic acid derivative
- decreases serum triglyceride levels
- decreases serum VLDL cholesterol
- increases serum HDL cholesterol
- effects on serum LDL cholesterol are variable
- increases in serum LDL cholesterol are observed in patient with type IV hyperlipoproteinemia
- inhibits peripheral lipolysis
- decreases hepatic extraction of free fatty acids
- reduces serum triglycerides
- inhibits synthesis & clearance of apolipoprotein B
- maximal effect
- total cholesterol: decrease of 10%
- LDL cholesterol: decrease of 10%
- HDL cholesterol: increase of 10%
- triglycerides: decrease of 50%
More general terms
Additional terms
- high density lipoprotein (HDL, alpha-lipoprotein)
- hyperlipoproteinemia (HLP)
- lipid panel (fasting lipid panel, FLP)
- low density lipoprotein (LDL, beta-lipoprotein)
- triglyceride
- very low density lipoprotein (VLDL)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ 4.0 4.1 4.2 Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ 5.0 5.1 Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
- ↑ 6.0 6.1 Prescriber's Letter 10(6):31-32 2003
- ↑ 7.0 7.1 Prescriber's Letter 16(8): 2009 Clinically Significant Statin Drug Interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250812&pb=PRL
- ↑ 8.0 8.1 8.2 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 9.0 9.1 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: https://www.ncbi.nlm.nih.gov/pubmed/19476425