Generic
Pitavastatin
6 brands available in the market
At a glance
Pitavastatin is a statin used as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C) in patients with primary hyperlipidemia and mixed dyslipidemia.
Description
Pitavastatin competitively inhibits HMG-CoA reductase, a rate-determining enzyme in cholesterol biosynthesis. As a result, expression of LDL-receptors increases, and uptake of LDL from blood to liver is accelerated, decreasing plasma TC. Sustained inhibition of cholesterol synthesis in the liver also decreases VLDL levels.
Indications
- Primary hyperlipidemia
- Mixed dyslipidemia
Therapeutic class
Other Anti-anginal & Anti-ischaemic drugs, Statins
Pharmacological class
HMG-CoA Reductase Inhibitor (Statin)
Pharmacology
Pitavastatin competitively inhibits HMG-CoA reductase, preventing cholesterol synthesis in the liver. It increases LDL-receptor expression and accelerates LDL uptake from blood to liver, decreasing plasma TC. Sustained inhibition of cholesterol synthesis also decreases VLDL levels.
Mechanism of action
Prevents cholesterol synthesis by inhibiting HMG-CoA reductase.
Dosage
Adult Dose (Oral):
- Usual dose: 2 mg once daily; may increase to 4 mg/day if needed
- Maximum dose: 4 mg/day
- Renal impairment (moderate-severe, CrCl 15-60 mL/min, ESRD on hemodialysis): Initial 1 mg/day; Max 2 mg/day
- With erythromycin: Not to exceed 1 mg/day
- With rifampin: Not to exceed 2 mg/day
- Contraindicated in active liver disease
Administration
- May be taken with or without food at any time of day; take at a fixed time
- Swallow tablet whole; do not chew, crush or break
Missed dose
If you miss a dose, take it as soon as possible; if almost time for next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Myalgia
- Back pain
- Diarrhea
- Constipation
- Pain in extremity
- Elevated liver enzymes
Precautions & warnings
- Skeletal muscle effects (myopathy, rhabdomyolysis): Dose-dependent; risk increases with advanced age (>65), renal impairment, hypothyroidism, and combination with fibrates; report unexplained muscle pain, tenderness, or weakness
- Liver enzyme abnormalities; monitor before and during treatment
- Does not usually affect driving ability
- Monitor blood sugar in diabetic patients
Contraindications
- Hypersensitivity to pitavastatin calcium
- Active liver disease (including unexplained persistent transaminase elevations)
- Pregnancy or women who may become pregnant
- Co-administration with cyclosporine
Drug interactions
- Cyclosporine: Significantly increases pitavastatin exposure; contraindicated
- Erythromycin: Significantly increases exposure; not to exceed 1 mg/day
- Rifampin: Significantly increases exposure; not to exceed 2 mg/day
- Gemfibrozil, other fibrates: Increased risk of myopathy/rhabdomyolysis
- Warfarin: No significant pharmacokinetic interaction
Food interactions
Food does not affect absorption; caution is advised when consuming alcohol.
Use in pregnancy
Use in Pregnancy: Pregnancy Category X; highly unsafe; significant harmful effects to the developing baby.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unsafe during breastfeeding; data suggests drug may cause toxicity to the baby; discontinue nursing or discontinue pitavastatin.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Elderly patients (>65) have increased risk of muscle effects; caution required.
Renal / hepatic impairment
Renal Impairment: Dose adjustment required in moderate-severe renal impairment; consult your doctor.
Hepatic Impairment: Contraindicated in active liver disease; caution; dose adjustment may be needed; not recommended in severe liver disease.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Store in a cool and dry place, protected from light and moisture; keep out of reach of children.
Chemical structure
Pitavastatin