PITAVASTATIN CALCIUM
Clinical safety rating: avoid
Contraindicated (not allowed)
Competitive inhibitor of HMG-CoA reductase, reducing cholesterol synthesis in the liver and increasing LDL receptor expression.
| Metabolism | Minimally metabolized by CYP2C9 and CYP2C8; primarily excreted unchanged in bile. |
| Excretion | Approximately 79% of the dose is excreted in feces (as parent drug and metabolites) via biliary elimination, and about 15% is excreted in urine. Less than 2% is excreted unchanged in urine. |
| Half-life | The terminal elimination half-life is approximately 12 hours (range 9–16 hours), supporting once-daily dosing. |
| Protein binding | Plasma protein binding is approximately 99% (primarily to albumin and alpha1-acid glycoprotein). |
| Volume of Distribution | Volume of distribution is approximately 0.28 L/kg, indicating limited distribution into extravascular tissues. |
| Bioavailability | Absolute oral bioavailability is approximately 60%. |
| Onset of Action | Onset of lipid-lowering effect is within 1 week, with maximal effect achieved by 4 weeks of oral administration. |
| Duration of Action | Duration of action is 24 hours with once-daily dosing, maintaining LDL-C reduction throughout the dosing interval. |
1-4 mg orally once daily
| Dosage form | TABLET |
| Renal impairment | CrCl >=60 mL/min: no adjustment; CrCl 30-59 mL/min: max 2 mg/day; CrCl <30 mL/min: contraindicated |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: caution, max 2 mg/day; Child-Pugh C: contraindicated |
| Pediatric use | Not approved for patients <18 years; safety and efficacy not established |
| Geriatric use | Start at lower end of dosing range (1 mg/day) due to increased risk of myopathy; monitor renal function |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Cyclosporine may increase levels Can cause myopathy and rhabdomyolysis.
| Breastfeeding | It is not known whether pitavastatin is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. M/P ratio is unknown. |
| Teratogenic Risk | Pitavastatin calcium is contraindicated in pregnancy. HMG-CoA reductase inhibitors decrease synthesis of cholesterol and possibly other biologically active substances derived from cholesterol, which may cause fetal harm when administered to pregnant women. First trimester: potential for teratogenicity based on animal studies and theoretical risk; second and third trimester: continued risk due to interference with fetal cholesterol synthesis essential for development. Pregnancy Category X. |
■ FDA Black Box Warning
No FDA boxed warning.
| Common Effects | Headache |
| Serious Effects |
["Active liver disease or unexplained transaminase elevations","Hypersensitivity to pitavastatin","Concomitant use with cyclosporine","Pregnancy and breastfeeding"]
| Precautions | ["Myopathy/rhabdomyolysis risk","Hepatic enzyme elevations","Increased blood glucose/hemoglobin A1c","Proteinuria, hematuria with higher doses"] |
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| Fetal Monitoring | Monitor maternal liver function tests and creatine kinase (CK) levels if symptoms of myopathy occur. Monitor for signs of myopathy/rhabdomyolysis. Fetal monitoring not typically indicated due to contraindication; if inadvertent exposure occurs, consider fetal ultrasound for structural anomalies. |
| Fertility Effects | Pitavastatin may reduce fertility based on animal studies where decreased sperm motility and concentration were observed. Effects on human fertility are unknown. |