bempedoic acid

REMS

Primary hyperlipidemia, including heterozygous familial hypercholesterolemia (as adjunct to diet, in combination with other LDL-C-lowering therapies, or as monotherapy when concurrent LDL-C-lowering therapy is not possible).
To reduce the risk of MI and coronary revascularization in patients who are unable to take recommended statin therapy (including those not taking a statin) and have established cardiovascular disease (CVD) or are at high risk for a CVD event but without established CVD.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
OB: Pregnancy.

Use Cautiously in:

History of gout;
Concurrent use of corticosteroids or fluoroquinolones, renal failure, or previous tendon disorders (↑ risk of tendon rupture/injury);
Severe hepatic impairment;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
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: ↑CK, back pain, muscle spasm, tendon rupture/injury

Resp: upper respiratory tract infection

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

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 ⬆ ⬇

Tablets: 180 mg
In combination with:
ezetimibe (Nexlizet); see Combination Drugs.

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.
Reduction in risk of MI and coronary revascularization.

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; 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 ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and smoking cessation.
Advise patient to notify health care provider if signs/symptoms of hyperuricemia (severe foot pain, especially in the toe; tender, warm, red, or swollen joint) occur.
Advise patient to stop therapy, rest and notify health care provider at the first sign of tendinitis (pain; swelling; tears; inflammation of tendons, including arm, shoulder, or back of 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).
Advise patient to notify health care provider immediately if signs/symptoms of allergic reactions (swelling of face, lips, mouth or tongue; trouble breathing; wheezing; skin rash, redness, or swelling; severe itching; dizziness or fainting; fast heartbeat) occur.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇