bempedoic acid

REMS

Heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease in patients who require additional lowering of low-density lipoprotein cholesterol (LDL-C) levels (as adjunct to diet and maximally tolerated statin therapy).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

OB: Pregnancy (may cause fetal harm);
Lactation: Lactation.

Use Cautiously in:

History of gout;
Concurrent use of corticosteroids or fluoroquinolones, renal failure, or previous tendon disorders (↑ risk of tendon rupture/injury);
Severe renal impairment or end-stage renal disease;
Severe hepatic impairment;
Pedi: Safety and effectiveness in children not established;
Geri: ↑risk of tendon rupture/injury in patients >60 yr.

Adv. Reactions/Side Effects ⬆ ⬇

CV: atrial fibrillation

GI: ↑liver enzymes, abdominal pain

GU: ↑blood urea nitrogen, ↑serum creatinine, benign prostatic hyperplasia

Hemat: anemia

Metab: hyperuricemia, gout

MS: ↑creatine kinase, back pain, muscle spasm, tendon rupture/injury

Resp: upper respiratory tract infection

Interactions ⬆ ⬇

Drug-drug:

Concurrent therapy with corticosteroids or fluoroquinolones may ↑ the risk of tendon rupture/injury.
May ↑ levels of and risk of myopathy with pravastatin and simvastatin; do not exceed 40 mg/day of pravastatin or 20 mg/day of simvastatin.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults ): 180 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits adenosine triphosphate-citrate lyase, which inhibits cholesterol synthesis in the liver and subsequently lowers LDL-C.

Therapeutic effects:

Reduction in LDL-C levels.

Classifications ⬆ ⬇

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: adenosine triphosphate citrate lyase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Unknown.

Distribution: Some distribution to extravascular tissues.

Metabolism/Excretion: Metabolized in liver to active metabolite (ESP15228); both parent drug and ESP15228 are also metabolized via glucuronidation to inactive metabolites. 70% excreted in urine and 30% excreted in feces primarily as metabolites (<5% excreted as unchanged drug in urine and feces).

Half-Life: 21 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3.5 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
Advise patient to notify health care professional if signs and symptoms of hyperuricemia (severe foot pain especially in the toe joint, tender joints, warm joints, joint redness, swelling) occur.
Advise patient to rest at the first sign of tendinitis (pain, swelling, tears, inflammation of tendons including arm, shoulder, back of the ankle) or tendon rupture (hear or feel a snap or pop in a tendon area, bruising right after an injury in a tendon area, unable to move affected area or put weight on affected area) and stop medication and contact health care professional if tendinitis or tendon rupture symptoms occur.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Bempedoic acid should be discontinued during pregnancy and lactation.

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Indications ⬇