CARBASTAT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CARBASTAT (CARBASTAT).
CARBASTAT is a synthetic statin that competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, leading to reduced hepatic cholesterol synthesis and increased LDL receptor expression.
| Metabolism | Primarily hepatic via CYP3A4; metabolites are active. |
| Excretion | Renal excretion accounts for 70% (primarily unchanged drug); biliary/fecal excretion accounts for 30% (including metabolites). |
| Half-life | Terminal elimination half-life is 8–12 hours in adults with normal renal function; prolonged to 20–30 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 85–90% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.6–0.8 L/kg, indicating moderate distribution into total body water and tissues. |
| Bioavailability | Oral: 50–60% due to first-pass metabolism; Intravenous: 100%. |
| Onset of Action | Oral: 30–60 minutes; Intravenous: 5–10 minutes. |
| Duration of Action | Oral: 6–8 hours; Intravenous: 4–6 hours; clinical effect may persist longer with accumulation. |
20-40 mg orally once daily; may titrate to 80 mg once daily based on response and tolerability.
| Dosage form | SOLUTION |
| Renal impairment | GFR 30-59 mL/min: reduce dose to 20 mg once daily; maximum 40 mg once daily. GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose to 20 mg once daily; Class C: avoid use. |
| Pediatric use | Not approved for pediatric use. |
| Geriatric use | Initiate at 20 mg once daily; titrate cautiously due to increased risk of hypotension and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CARBASTAT (CARBASTAT).
| Breastfeeding | Contraindicated in breastfeeding due to potential for infant toxicity. M/P ratio not determined; extensive distribution into breast milk expected based on physicochemical properties. |
| Teratogenic Risk | First trimester: Avoid use; documented teratogenicity in animal studies with potential for cardiovascular and neural tube defects. Second and third trimesters: Increased risk of oligohydramnios and fetal renal impairment; use only if maternal benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA boxed warning exists for CARBASTAT.
| Serious Effects |
["Active liver disease","Unexplained persistent elevations in serum transaminases","Pregnancy","Lactation","Hypersensitivity to any component"]
| Precautions | ["Risk of myopathy/rhabdomyolysis","Hepatic enzyme elevations","Use with caution in patients with predisposing factors for renal failure","Avoid concurrent use with strong CYP3A4 inhibitors"] |
| Food/Dietary | No significant food interactions. Take with or without food. Avoid alcohol. |
| Clinical Pearls |
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| Baseline and serial fetal ultrasound for fetal growth and amniotic fluid volume; maternal renal function, liver enzymes, and complete blood count every 4 weeks; fetal echocardiography if exposed in first trimester. |
| Fertility Effects | Reversible impairment of spermatogenesis and ovulation observed in animal studies. No human data available; potential for reduced fertility with prolonged use. |
| Carbastat is a carbapenem antibiotic. Dose adjustment required for CrCl <50 mL/min. Infuse over 3 hours for MIC >2 mcg/mL. Monitor for seizures, especially in elderly and those with CNS disorders. Consider desensitization for IgE-mediated hypersensitivity. |
| Patient Advice | Take exactly as prescribed, do not skip doses. · Complete full course, even if feeling better. · Report severe diarrhea, rash, or seizures immediately. · May cause dizziness; avoid driving if affected. · Inform doctor of all medications, especially valproic acid. |