bempedoic acid/ezetimibe

Contraindicated in:

Hypersensitivity;
Moderate or severe hepatic impairment;
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;
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

Derm: rash

GI: ↑liver enzymes, abdominal pain, cholecystitis, cholelithiasis, nausea, pancreatitis

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

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Concurrent therapy with corticosteroids or fluoroquinolonesmay ↑ the risk of tendon rupture/injury associated with bempedoic acid.
Bempedoic acid may ↑ levels of and risk of myopathy with pravastatin andsimvastatin; do not exceed 40 mg/day of pravastatin or 20 mg/day of simvastatin.
Effects of ezetimibe may be ↓ by cholestyramine or other bile acid sequestrants.
Concurrent use of fibrates may ↑ levels and the risk of cholelithiasis associated with ezetimibe.
Cyclosporine may ↑ ezetimibe levels.
Ezetimibe may ↑ risk of rhabdomyolysis when used with HMG CoA-reductase inhibitors.

Availability ⬆ ⬇

Tablets: bempedoic acid 180 mg/ezetimibe 10 mg

Route/Dosage ⬆ ⬇

PO (Adults ): One tablet once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Bempedoic acid: Inhibits adenosine triphosphate-citrate lyase, which inhibits cholesterol synthesis in the liver and subsequently lowers LDL-C. Ezetimibe: Inhibits absorption of cholesterol in the small intestine.

Therapeutic effects:

Reduction in LDL-C levels.

Classifications ⬆ ⬇

Therapeutic Classification: lipid-lowering agents, none assigned

Pharmacologic Classification: adenosine triphosphate citrate lyase inhibitors, cholesterol absorption inhibitors

Pharmacokinetics ⬆ ⬇

Bempedoic acid

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.

Ezetimibe

Absorption: Following absorption, rapidly converted to ezetimibe-glucuronide, which is active. Bioavailability is variable.

Distribution: Unknown.

Metabolism/Excretion: Undergoes enterohepatic recycling, mostly eliminated in feces, minimal renal excretion.

Half-Life: 22 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
Bempedoic acid	unknown	3.5 hr	24 hr
Ezetimibe	unknown	1 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.
Advise patient to notify health care professional immediately if signs and symptoms of allergic reactions (swelling of face, lips, mouth or tongue; trouble breathing; wheezing; skin rashes, redness, or swelling; severe itching; dizziness or fainting; fast heart beat or pounding in chest) 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 breast feeding. Bempedoic acid/ezetimibe should be discontinued during pregnancy and lactation.

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Indications ⬇

Contraind./Precautions ⬆ ⬇