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CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, PLAIN › HMG CoA reductase inhibitors
pitavastatin
C10AA08
Forms & Strengths
- Tablet: 1 mg
- Tablet: 2 mg
- Tablet: 4 mg
Adult Dosing
- Hyperlipidemia and mixed dyslipidemia: 1 mg to 4 mg orally once daily
- Initial dose: 2 mg orally once daily; adjust based on response
- Maximum dose: 4 mg orally once daily
- Renal impairment (moderate to severe, eGFR <60 mL/min/1.73m2) or end-stage renal disease on hemodialysis: Initial 1 mg once daily, maximum 2 mg once daily
- Hepatic impairment: Contraindicated in active liver disease
Pediatric Dosing
- Heterozygous familial hypercholesterolemia (Pediatric patients aged 8 to 17 years): 1 mg to 4 mg orally once daily
- Initial dose: 2 mg orally once daily
- Maximum dose: 4 mg orally once daily
Indications
- Adjunct to diet for the treatment of primary hyperlipidemia and mixed dyslipidemia to reduce LDL-C, total cholesterol, ApoB, triglycerides, and to increase HDL-C
- Adjunct to diet for the treatment of heterozygous familial hypercholesterolemia in pediatric patients aged 8 to 17 years
Mechanism of Action
- Competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase
- Rate-limiting enzyme that converts HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis
- Increases hepatic LDL receptors on the cell surface, enhancing uptake and catabolism of LDL-C
Contraindications
- Hypersensitivity to pitavastatin or any component of the product
- Active liver disease, including unexplained persistent elevations of serum transaminases
- Pregnancy and lactation
- Co-administration with cyclosporine
Adverse Reactions
- Myalgia
- Back pain
- Arthralgia
- Diarrhea
- Constipation
- Nasopharyngitis
- Rare: Immune-mediated necrotizing myopathy, rhabdomyolysis, autoimmune hepatitis, cognitive impairment, new-onset diabetes mellitus
Drug Interactions
- Cyclosporine: Significantly increases pitavastatin exposure; co-administration is contraindicated
- Erythromycin: May increase pitavastatin exposure and adverse effects
- Rifampin: May affect pitavastatin plasma concentrations
- Gemfibrozil: Increases risk of myopathy and rhabdomyolysis; avoid concurrent use
- Coumarin anticoagulants: May increase INR and prothrombin time; monitor closely when initiated
Curated Content: Needs Vetting Before Put to Clinical Use