BARSTATIN 100
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BARSTATIN 100 (BARSTATIN 100).
HMG-CoA reductase inhibitor; decreases cholesterol synthesis in the liver by competitively inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, leading to upregulated LDL receptor expression and enhanced clearance of LDL from the bloodstream.
| Metabolism | Primarily metabolized by CYP3A4 isoenzyme; undergoes extensive first-pass metabolism in the liver. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 30% as metabolites |
| Half-life | Terminal elimination half-life: 3-4 hours; in renal impairment (CrCl <30 mL/min) extended to 8-12 hours; clinical context: supports twice-daily dosing in normal renal function |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 0.15 L/kg; indicates limited extravascular distribution, primarily confined to plasma volume |
| Bioavailability | Oral: 85%; intravenous: 100% |
| Onset of Action | Oral: 1-2 hours; intravenous: 15-30 minutes |
| Duration of Action | Oral: 8-12 hours; intravenous: 6-8 hours; clinical notes: lipid-lowering effect persists with sustained dosing |
100 mg orally once daily.
| Dosage form | POWDER |
| Renal impairment | GFR 30-59 mL/min: 50 mg once daily; GFR <30 mL/min: 25 mg once daily. |
| Liver impairment | Child-Pugh Class A: no dose adjustment; Child-Pugh Class B: 50 mg once daily; Child-Pugh Class C: contraindicated. |
| Pediatric use | Children 10-17 years: 2 mg/kg/day (max 100 mg/day) orally once daily; Children <10 years: not established. |
| Geriatric use | Start at 50 mg once daily; titrate cautiously based on renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BARSTATIN 100 (BARSTATIN 100).
| Breastfeeding | Contraindicated during breastfeeding. HMG-CoA reductase inhibitors are excreted in human milk; M/P ratio not available for this specific agent. Potential for serious adverse effects in nursing infants. |
| Teratogenic Risk | Pregnancy Category X. First trimester: High risk of congenital anomalies, particularly CNS and cardiovascular defects. Second and third trimesters: Risk of fetal growth restriction, preterm birth, and neonatal hypolipidemia. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA boxed warning reported.
| Serious Effects |
["Active liver disease or unexplained persistent elevations of serum transaminases","Hypersensitivity to any component of the drug","Pregnancy and lactation","Concomitant use with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, erythromycin, clarithromycin, telithromycin, HIV protease inhibitors, nefazodone, cobicistat-containing products)"]
| Precautions | ["Risk of myopathy/rhabdomyolysis, especially with concomitant use of strong CYP3A4 inhibitors, cyclosporine, or gemfibrozil","Hepatic enzyme elevations; monitor liver function tests before and during therapy","Avoid in active liver disease or unexplained persistent transaminase elevations","Caution in patients with predisposing factors for renal impairment"] |
| Food/Dietary | Avoid grapefruit and grapefruit juice during therapy, as they inhibit CYP3A4 and increase statin levels. Limit alcohol intake to reduce risk of liver damage. |
Loading safety data…
| Baseline and periodic liver function tests; renal function tests; creatine kinase levels if neuromuscular symptoms; fetal ultrasound for growth assessment if inadvertent exposure; lipid panels to assess efficacy. |
| Fertility Effects | No significant effects on fertility in animal studies. In humans, reduced sperm motility and count reported in males; effects reversible upon discontinuation. |
| Clinical Pearls | BARSTATIN 100 is a high-intensity statin; monitor for muscle pain, tenderness, or weakness, especially in patients on concurrent CYP3A4 inhibitors. Check baseline liver function and CPK; avoid in active liver disease or unexplained transaminase elevations. Consider dose reduction if used with potent CYP3A4 inhibitors (e.g., clarithromycin, itraconazole). |
| Patient Advice | Take BARSTATIN 100 exactly as prescribed, at the same time each day, preferably in the evening. · Do not take with grapefruit or grapefruit juice; avoid large amounts of alcohol. · Report any unexplained muscle pain, tenderness, or weakness to your doctor immediately. · Inform your doctor of all other medications, including over-the-counter drugs and supplements. · Maintain a heart-healthy diet and exercise regimen as advised by your healthcare provider. |