LIVALO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIVALO (LIVALO).
Competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, leading to increased LDL receptor expression and reduced plasma LDL-C levels.
| Metabolism | Primarily metabolized by CYP2C9 and to a lesser extent by CYP2C8 and CYP3A4. |
| Excretion | Primarily biliary/fecal (approximately 90% of absorbed dose excreted in feces as parent drug and metabolites); renal excretion accounts for <5% of the dose. |
| Half-life | Terminal elimination half-life is approximately 12 hours (range 8-14 hours), supporting once-daily dosing; no significant accumulation with repeated administration. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd is approximately 1.2 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is approximately 60%; food does not significantly affect absorption. |
| Onset of Action | Not applicable for direct clinical effect; LDL-C reduction is measurable within 1-2 weeks, with maximum effect at 4 weeks. |
| Duration of Action | LDL-C reduction persists for 24 hours with once-daily dosing; clinical efficacy is maintained with continuous therapy. |
| Action Class | HMG CoA inhibitors (statins) |
1-4 mg orally once daily at any time of day with or without food.
| Dosage form | TABLET |
| Renal impairment | For GFR 30-59 mL/min/1.73 m²: maximum dose 2 mg once daily. For GFR 15-29 mL/min/1.73 m²: maximum dose 1 mg once daily. Not recommended for GFR <15 mL/min/1.73 m² or on dialysis. |
| Liver impairment | Contraindicated in active liver disease or persistent transaminase elevations. For Child-Pugh class A: maximum dose 2 mg once daily. Not recommended for Child-Pugh class B or C. |
| Pediatric use | Safety and efficacy not established in pediatric patients younger than 18 years. |
| Geriatric use | No specific dose adjustment required; initiate at lower end of dosing range due to increased risk of myopathy and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LIVALO (LIVALO).
| Breastfeeding | Data not available. M/P ratio unknown. Excretion in human milk is unknown; due to potential for adverse effects in nursing infants, breastfeeding is contraindicated. |
| Teratogenic Risk | Pregnancy Category X. Contraindicated in pregnancy. First trimester: Risk of fetal skeletal and cardiac anomalies based on animal studies and LDL-cholesterol reduction mechanism. Second and third trimesters: Continued risk of fetal harm due to essential role of cholesterol in fetal development; reports of congenital anomalies including vertebral, anal, cardiac, tracheoesophageal, renal, and limb defects (VACTERL association). |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
["Active liver disease or unexplained persistent elevated liver enzymes","Pregnancy and breastfeeding","Concomitant use with cyclosporine","Concomitant use with gemfibrozil","Known hypersensitivity to pitavastatin or any component"]
| Precautions | ["Myopathy/rhabdomyolysis risk increased with high doses, renal impairment, or concomitant use of certain drugs (e.g., cyclosporine, gemfibrozil, rifampin).","Hepatic effects: Elevated liver enzymes; measure before and during therapy.","Fetal toxicity: Avoid in pregnancy; can cause fetal harm."] |
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| Fetal Monitoring | Pregnancy test before initiation. Not applicable for use during pregnancy; if inadvertent exposure occurs, perform fetal ultrasound for structural anomalies and monitor for growth restriction. |
| Fertility Effects | No human data on fertility effects. Animal studies: No impairment of fertility observed at clinically relevant doses. |