bezafibrate

REMS

Use in conjunction with diet and other modalities in the treatment of hypercholesterolemia (type IIa and IIb mixed hyperlipidemia, to ↓ serum TG, LDL-C, and apolipoprotein B and ↑ HDL-C and apolipoprotein A).
Hypertriglyceridemia (type IV and V hyperlipidemias) in patients at risk of pancreatitis and other sequelae.

Action ⬆ ⬇

Inhibits TG synthesis.

Therapeutic effects:

Lowered cholesterol and TGs, ↑ HDL-C, with ↓ risk of pancreatitis and other sequelae.

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed (100%) following oral administration.

Distribution: Unknown.

Metabolism/Excretion: 50% metabolized. 50% excreted unchanged in urine; 3% excreted in feces.

Half-Life: 1–2 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3–4 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity/photosensitivity to bezafibrate or other fibric acid or fibrate derivatives;
Severe hepatic or renal impairment (CCr <60 mL/min), primary biliary cirrhosis, gallstone or gallbladder disease, or hypoalbuminemia;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

History of liver disease;
Geri: Consider age-related ↓ in renal function; avoid in patients >70 yr;
Pedi: Limited experience in children at a dose of 10–20 mg/kg/day.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia, photosensitivity, pruritus, rash, urticaria

GI: dyspepsia, flatulence, gastritis, ↓appetite, abdominal distension, abdominal pain, cholestasis, constipation, diarrhea, nausea

GU: erectile dysfunction, renal failure

MS: muscle cramps, muscle weakness, myalgia, RHABDOMYOLYSIS

Neuro: dizziness, headache

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

↑risk of bleeding with oral anticoagulants; ↓ anticoagulant dose by 50% with frequent monitoring.
Cyclosporine may ↑ risk of severe myositis/rhabdomyolysis.
Immunosuppressants may ↑ risk of reversible renal impairment.
↑risk of myopathy with HMG CoA reductase inhibitors (statins); combination therapy should be undertaken with extreme caution; must be discontinued at the 1st signs of myopathy and should not be undertaken in the presence of predisposing factors including impaired renal function, severe infection, trauma, surgery, hormonal/electrolyte imbalance or ↑ alcohol intake.
↑risk of serious hypoglycemia with insulin or sulfonylureas.
MAO inhibitors may ↑ risk of hepatotoxicity.
Cholestyramine and other bile-acid sequestrants may ↓ absorption and effectiveness; separate administration by ≥2 hr.
Effectiveness may be ↓ by estrogen.

Route/Dosage ⬆ ⬇

PO (Adults ): 400 mg once daily.

Availability ⬆ ⬇

Sustained-release tablet: 400 mg

Assessment ⬆ ⬇

Obtain a diet history with regard to fat consumption. Before starting bezafibrate, every attempt should be made to obtain a normal TG concentration with diet, exercise, and weight loss.
Assess for cholelithiasis (epigastric pain after meals, pain that radiates to right shoulder or back). If gallbladder studies are indicated and gallstones confirmed, discontinue therapy.
Assess for hypersensitivity reactions (anaphylaxis). If hypersensitivity reaction occurs, discontinue bezafibrate immediately and implement supportive measures (epinephrine) as indicated.

Lab Test Considerations:

Monitor serum lipids before and periodically during therapy.
May ↑ AST and ALT. Monitor liver enzymes periodically during therapy. Baseline tests are recommended after 3–6 mo and at least yearly thereafter. Discontinue bezafibrate if AST or ALT levels ↑ >3 times upper limit of normal.
If muscle tenderness develops during therapy, monitor CK. If CK is >10 times the upper limit of normal or if myopathy occurs, discontinue bezafibrate.

Implementation ⬆ ⬇

PO: Administer without regard to meals. DNC: Swallow sustained-release tablets whole; do not crush, break, or chew.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Advise patient to take the medication as directed. Missed doses should be taken as soon as remembered; do not double dose. Advise patient that medication helps control but does not cure ↑ serum TG concentrations.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Advise patient that medication should be taken in conjunction with diet restrictions of fat, cholesterol, carbohydrates, and alcohol, as well as an exercise regimen and smoking cessation.
Advise patient to notify health care provider of unexplained muscle pain or weakness, tiredness, fever, nausea, vomiting, or abdominal pain. If hypersensitivity reactions (anaphylaxis) occurs, advise patient to seek immediate medical attention.
Rep: Advise women of reproductive potential to immediately notify health care provider if pregnancy is planned or suspected, and advise to use strict birth control measures. If pregnancy occurs despite birth control, discontinue bezafibrate. If planning a pregnancy, bezafibrate should discontinued several months before conception.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇