gemfibrozil (gem-fye-broe-zil) Lopid

 Indications

Management of type II-b hyperlipidemia (decreased

HDL, increased LDL, 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).

Action

Inhibits peripheral lipolysis. Decreases triglyceride

production by the liver. Decreases production of the

triglyceride carrier protein. Increases HDL. Therapeutic

Effects: Decreased plasma triglycerides and

increased HDL.

Pharmacokinetics

Absorption: Well absorbed after oral administration.

Distribution: Unknown.

Metabolism and Excretion: Some metabolism by

the liver, 70% excreted by the kidneys (mostly unchanged),

6% excreted in feces.

Half-life: 1.3–1.5 hr.

TIME/ACTION PROFILE (triglyceride-VLDL–

lowering effect)

ROUTE ONSET PEAK DURATION

PO 2–5 days 4 wk several mo

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Hepatic impairment;

Severe renal impairment; Primary biliary cirrhosis;

Gallbladder disease; Concurrent use of simvastatin,

repaglinide, or dasabuvir.

Use Cautiously in: OB, Lactation, Pedi: Safety not

established.

Adverse Reactions/Side Effects

CNS: dizziness, headache. EENT: blurred vision. GI:

abdominal pain, diarrhea, epigastric pain, flatulence,

gallstones, heartburn, nausea, vomiting. Derm: alopecia,

rash, urticaria. Hemat: anemia, leukopenia. MS:

myositis.

Interactions

Drug-Drug: Mayqlevels of CYP2C8 substrates, including

dabrafenib, dasabuvir, enzalutamide, loperamide,

montelukast, paclitaxel, pioglitazone, or rosiglitazone; concurrent use with dasabuvir

contraindicated. Mayqlevels 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. Mayqlevels and the risk of

bleeding with warfarin. Concurrent use with colchicine

mayqrisk of rhabdomyolysis, especially in patients

with renal dysfunction or elderly. Maypthe effect

of cyclosporine. Cholestyramine and colestipol

maypabsorption; separate administration by 2 hr.

Route/Dosage

PO (Adults): 600 mg twice daily 30 min before breakfast

and dinner.

Availability (generic available)

Tablets: 600 mg. Cost: Generic—$24.07/100. Capsules:

300 mg.