General

Pronunciation:
bem-pe-doe-ik as-id

Trade Name(s)

• Nexletol

Ther. Class.

lipid-lowering agents

Pharm. Class.

adenosine triphosphate citrate lyase inhibitors

Indications

• 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.

Action

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

Therapeutic Effect(s):

• Reduction in LDL-C levels.
• Reduction in risk of MI and coronary revascularization.

Pharmacokinetics

Absorption: Unknown.

Distribution: Some distribution to extravascular tissues.

Metabolism and 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)

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;
• OB:   Pregnancy;
• 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.

Adverse Reactions/Side Effects

CV: atrial fibrillation

GI: ↑ liver enzymes, abdominal pain

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

Hemat: anemia

Metabolic: hyperuricemia, gout

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

Resp: upper respiratory tract infection

Misc: HYPERSENSITIVITY REACTIONS (including angioedema)

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

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.

Route/Dosage

PO (Adults): 180 mg once daily.

Availability

Tablets: 180 mg

In Combination with: ezetimibe (Nexlizet); see combination drugs.

Assessment

• Obtain a diet history, especially with regard to fat consumption.
• Monitor for signs and symptoms of hyperuricemia (gout) periodically during therapy. May occur within 4 wk of therapy. Initiate treatment with urate-lowering drugs as appropriate.
• Monitor for signs and symptoms of allergic reactions (anaphylaxis, angioedema, rash, urticaria) during therapy.
• Monitor for signs and symptoms of tendon rupture (joint pain, swelling, inflammation) periodically during therapy. May occur within days to months of starting therapy and more frequently in patients >60 yr, taking corticosteroids or fluoroquinolones, with renal failure, or with previous tendon disorders.  If joint pain, swelling, or inflammation occur,  consider discontinuing.  If tendon rupture occurs,  immediately discontinue bempedoic acid.

Lab Test Considerations:

Evaluate serum cholesterol levels before initiating, after 8–12 wk of therapy, and periodically thereafter.

• Monitor serum uric acid levels periodically if symptoms of hyperuricemia occur.
• May ↑ BUN and serum creatinine.
• May ↓ hemoglobin and leukocytes and ↑ platelet count.
• May ↑ AST, ALT, and CK.

Implementation

• PO Administer once daily without regard to food.

Patient/Family Teaching

• Explain purpose and side effects of medication. Advise patient to read  Patient Information  before starting therapy.
• 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; tender, warm, red, or swollen joint) occur.
• Advise patient to rest 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), 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 rash, redness, or swelling; severe itching; dizziness or fainting; fast heartbeat 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:  May cause fetal harm. Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid use during breastfeeding.

Evaluation/Desired Outcomes

• Reduction in LDL-C levels. Evaluate in 8–12 wk.
• Reduction in risk of MI and coronary revascularization.