CAPASTAT SULFATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CAPASTAT SULFATE (CAPASTAT SULFATE).
Capastat sulfate (capreomycin) is a cyclic polypeptide antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, interfering with initiation and elongation steps.
| Metabolism | Primarily excreted unchanged by the kidneys via glomerular filtration; minimal hepatic metabolism. |
| Excretion | Primarily renal (80-90% as unchanged drug via glomerular filtration); minor fecal (10-20%) |
| Half-life | 3-6 hours; prolonged to 12-24 hours in renal impairment; negligible hepatic metabolism |
| Protein binding | ≤10%; primarily to albumin |
| Volume of Distribution | 0.2-0.3 L/kg; low distribution confined to extracellular fluid; poor CNS penetration |
| Bioavailability | IM: ~100%; Oral: <1% (not absorbed); IV: 100% |
| Onset of Action | IM: 1-2 hours; IV: immediate; peak effect: 2-4 hours |
| Duration of Action | 8-12 hours; prolonged in renal impairment (up to 24 hours); serum levels remain bactericidal for 6-12 hours |
15 mg/kg (max 1 g) intramuscularly daily for 60-120 days.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 10-50 mL/min: administer 50% of dose every 24-48 hours; CrCl <10 mL/min: administer 25% of dose every 48-72 hours. |
| Liver impairment | No adjustment required for hepatic impairment; monitor for hepatotoxicity. |
| Pediatric use | 15 mg/kg (max 1 g) intramuscularly daily; not recommended for neonates due to risk of neuromuscular blockade. |
| Geriatric use | Reduce dose based on renal function; monitor renal function and hearing regularly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CAPASTAT SULFATE (CAPASTAT SULFATE).
| Breastfeeding | It is unknown whether capreomycin is excreted in human breast milk. Because of the potential for serious adverse reactions (e.g.,otoxicity, nephrotoxicity) in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. M/P ratio is not established. |
| Teratogenic Risk | Capreomycin sulfate is classified as pregnancy category C. Animal studies have shown teratogenic effects (skeletal anomalies) at doses 2-3 times the human dose. There are no adequate and well-controlled studies in pregnant women. Potential fetal risks include ototoxicity and nephrotoxicity, similar to observed effects in adults. Use during pregnancy only if potential benefit justifies potential risk to the fetus. |
■ FDA Black Box Warning
Capreomycin is nephrotoxic and ototoxic. Use with caution in patients with renal insufficiency or pre-existing hearing loss. Monitor renal function and audiometry regularly. Neurotoxicity may occur including neuromuscular blockade.
| Serious Effects |
Hypersensitivity to capreomycin or any component of the formulation; not recommended in pregnancy unless benefit outweighs risk.
| Precautions | Nephrotoxicity (dose-related, monitor renal function), ototoxicity (vestibular and cochlear, may be irreversible), neuromuscular blockade (risk with concurrent anesthetics or neuromuscular blocking agents), electrolyte disturbances (hypokalemia, hypomagnesemia, hypocalcemia), superinfection. |
| Food/Dietary | No significant food interactions known. Maintain adequate hydration to reduce nephrotoxicity risk. |
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| Fetal Monitoring | Monitor maternal renal function (BUN, serum creatinine, creatinine clearance) and audiometry at baseline and periodically during therapy due to risk of nephrotoxicity and ototoxicity. In pregnancy, monitor fetal growth and amniotic fluid index via ultrasound as capreomycin may cause fetal nephrotoxicity leading to oligohydramnios. Monitor maternal electrolytes (especially potassium, magnesium, calcium) as capreomycin can cause electrolyte wasting. |
| Fertility Effects | There are no adequate studies on the effect of capreomycin on human fertility. Animal studies have not reported adverse effects on fertility. However, any impact at therapeutic doses is considered unlikely. |
| Clinical Pearls | Capastat sulfate (capreomycin) is an injectable aminoglycoside-like antibiotic used as a second-line agent for multidrug-resistant tuberculosis (MDR-TB). Monitor renal function and audiometry regularly due to nephrotoxicity and ototoxicity risks. Adjust dose in renal impairment. Administer deep IM injection to avoid sterile abscesses. |
| Patient Advice | Take this medication exactly as prescribed; it is given as an injection into a muscle. · You will need regular blood tests to check kidney function and hearing tests. · Report any hearing loss, ringing in ears, dizziness, or decreased urine output immediately. · Do not stop treatment without consulting your doctor, even if you feel better. |