BEM-pe-DOE-ik AS-id

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification:

• 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).

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

• Reduction in LDL-C levels.

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.

(plasma concentrations)

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.

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.

Drug-Drug:

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

• PO (Adults): 180 mg once daily.

• Tablets: 180 mg;

• 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 tendon rupture (joint pain, swelling, inflammation) periodically during therapy. May occur within days to months of starting therapy and more frequently in patients >60 years of age, taking corticosteroid or fluoroquinolones, with renal failure, and with previous tendon disorders. Consider discontinuing therapy if symptoms occur and discontinue therapy if tendon rupture occurs.

• 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 cause ↑ BUN and serum creatinine.
  • May cause ↓ hemoglobin and leukocytes and ↑ platelet count.
  • May cause ↑ AST, ALT, and creatine kinase.

• PO: Administer once daily without regard to food.

• 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 breast feeding. Bempedoic acid should be discontinued during pregnancy and lactation.

• Reduction in LDL-C levels. Evaluate in 8–12 wk.

Nexletol