gem-FYE-broe-zil

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: fibric acid derivatives

• Management of type II-b hyperlipidemia (decreased high-density lipoprotein cholesterol [HDL-C], increased low-density lipoprotein cholesterol [LDL-C], increased triglycerides) in patients who do not yet have clinical coronary artery disease and have failed therapy with diet, exercise, weight loss, or other agents (niacin, bile acid sequestrants).

• Inhibits peripheral lipolysis.
• Decreases triglyceride production by the liver.
• Decreases production of the triglyceride carrier protein.
• Increases HDL-C.

• Decreased plasma triglycerides and increased HDL-C.

Absorption: Well absorbed after oral administration.

Distribution: Unknown.

Metabolism/Excretion: Some metabolism by the liver, 70% excreted by the kidneys (mostly unchanged), 6% excreted in feces.

Half-life: 1.3–1.5 hr.

(triglyceride-lowering effect)

Contraindicated in:

• Hypersensitivity
• Severe renal impairment
• Hepatic impairment
• Primary biliary cirrhosis
• Gallbladder disease
• Concurrent use of simvastatin, repaglinide, dasabuvir, or selexipag
• OB: Avoid use during 1st trimester of pregnancy
• Lactation: Lactation.

Use Cautiously in:

• OB: May be used starting in 2nd trimester of pregnancy, if needed
• Pedi: Safety and effectiveness not established in children.

Derm: alopecia, rash, urticaria.

EENT: blurred vision.

GI: abdominal pain, diarrhea, epigastric pain, flatulence, gallstones, heartburn, nausea, vomiting.

Hemat: anemia, leukopenia.

MS: myositis.

Neuro: dizziness, headache.

Drug-Drug:

• May ↑ levels of CYP2C8 substrates, including dabrafenib, dasabuvir, enzalutamide, loperamide, montelukast, paclitaxel, pioglitazone, or selexipag; concurrent use with dasabuvir or selexipag contraindicated.
• May ↑ levels of OATP1B1 substrates, including atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, olmesartan, pitavastatin, pravastatin, repaglinide, rifampin, rosuvastatin, simvastatin, and valsartan; concurrent use with simvastatin or repaglinide is contraindicated; avoid concurrent use with other HMG-CoA reductase inhibitors.
• May ↑ levels and the risk of bleeding with warfarin.
• Concurrent use with colchicine may ↑ risk of rhabdomyolysis, especially in patients with renal dysfunction or older adults.
• May ↓ the effect of cyclosporine.
• Cholestyramine and colestipol may ↓ absorption; separate administration by 2 hr.

• PO (Adults): 600 mg twice daily 30 min before breakfast and dinner.

(Generic available)

• Capsules: 300 mg;
• Tablets: 600 mg;

• Obtain patient’s diet history, especially regarding fat and alcohol consumption.

• Monitor serum triglyceride and cholesterol levels before and periodically during therapy. Assess LDL and triglyceride levels before and periodically during therapy. Discontinue gemfibrozil if paradoxical ↑ in lipid levels occurs.
  • Assess liver function tests before and periodically during therapy. May cause ↑ serum bilirubin, alkaline phosphatase, CK, LDH, AST, and ALT. If hepatic function tests rise significantly, discontinue therapy and do not resume.
  • Evaluate CBC and electrolytes every 3–6 mo and then yearly during therapy. May cause mild ↓ in hemoglobin, hematocrit, and leukocyte counts. May cause ↓ serum potassium concentrations.
  • May cause slight ↑ in serum glucose.

• Do not confuse gemfibrozil with gabapentin.
• PO: Administer 30 min before breakfast or dinner.

• Instruct patient to take medication as directed, not to skip doses or double up on missed doses. Take missed doses as soon as remembered unless almost time for next dose.
• Advise patient that gemfibrozil should be used in conjunction with dietary restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
• Instruct patient to notify health care professional promptly if severe stomach pains with nausea and vomiting, fever, chills, sore throat, rash, diarrhea, muscle cramping, general abdominal discomfort, or persistent flatulence occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

• Decrease in serum triglyceride and cholesterol levels and improved HDL-C to total cholesterol ratios. If response is not seen within 3 mo, medication is usually discontinued.

Lopid