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. |
| Molecular Weight | 880.98 |
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 | Contraindicated due to potential teratogenicity; statins are associated with fetal malformations. Use alternative therapy. |
| 2nd trimester | Contraindicated; statins cross the placenta and may interfere with fetal cholesterol synthesis necessary for development. |
| 3rd trimester | Contraindicated; risk of toxicity to the fetus. Avoid use during pregnancy. |
Clinical note
Cyclosporine may increase levels Can cause myopathy and rhabdomyolysis.
| Placental transfer | Pitavastatin crosses the placenta; animal studies show evidence of fetal harm. Human data limited but caution is warranted. |
| Breastfeeding | Pitavastatin is excreted into human breast milk in low levels; however, due to potential for serious adverse effects in the nursing infant, it is recommended to discontinue breastfeeding or discontinue the drug. |
■ FDA Black Box Warning
No FDA boxed warning.
| Common Effects | Headache |
| Serious Effects |
Hypersensitivity to pitavastatin or any component of the formulationActive liver disease or unexplained persistent elevations of serum transaminasesPregnancy and breastfeeding
| Precautions | Myopathy/rhabdomyolysis risk, Hepatic enzyme elevations, Increased blood glucose/hemoglobin A1c, Proteinuria, hematuria with higher doses |
| Food/Dietary | Grapefruit juice should be avoided as it may increase pitavastatin plasma concentrations. No other significant food interactions reported. |
Loading safety data…
| Lactation Rating | L4 - Hazardous |
| 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. |
| 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. |
| Clinical Pearls | Pitavastatin is a potent statin with minimal CYP3A4 metabolism, reducing drug-drug interactions. It has a low propensity for muscle toxicity and is primarily excreted unchanged in feces. Monitor liver enzymes at baseline and as clinically indicated. Contraindicated in active liver disease or unexplained persistent transaminase elevations. |
| Patient Advice | Take pitavastatin once daily at the same time, with or without food. · Avoid grapefruit juice as it may increase the risk of side effects. · Report unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine. · Notify your healthcare provider if you experience symptoms of liver problems: jaundice, dark urine, or abdominal pain. · Do not take with cyclosporine, as it increases pitavastatin levels. |