CAPREOMYCIN SULFATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CAPREOMYCIN SULFATE (CAPREOMYCIN SULFATE).
Inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, causing misreading of mRNA and inhibiting translation initiation. Also alters membrane permeability.
| Metabolism | Not significantly metabolized; primarily excreted unchanged in urine via glomerular filtration. |
| Excretion | Primarily renal (80-90% as unchanged drug via glomerular filtration). Biliary/fecal elimination: <1%. |
| Half-life | Terminal elimination half-life: 24-40 hours (prolonged in renal impairment; anuria may extend to 96-120 hours). |
| Protein binding | Approximately 30% bound to serum proteins (albumin). |
| Volume of Distribution | 0.4-0.6 L/kg (suggests distribution primarily into extracellular fluid; poor CNS penetration unless meninges inflamed). |
| Bioavailability | IM: 100% (only IM route available; no oral formulation). |
| Onset of Action | IM: Bacteriostatic effects within 24-48 hours; peak serum concentrations at 1-2 hours. |
| Duration of Action | IM: Antimicrobial activity persists for 12-24 hours post-dose; drug accumulation occurs with daily dosing in renal impairment. |
15 mg/kg (up to 1 g) intramuscularly or intravenously once daily for 60 days, then 15 mg/kg (up to 1 g) 2-3 times weekly for 12-18 months in combination with other antituberculosis agents.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 50-80 mL/min: 15 mg/kg every 24-36 hours; CrCl 30-50 mL/min: 15 mg/kg every 48 hours; CrCl 10-30 mL/min: 15 mg/kg every 72 hours; CrCl <10 mL/min: 15 mg/kg every 96-120 hours. |
| Liver impairment | No dose adjustment required for hepatic impairment; monitor for hepatotoxicity. |
| Pediatric use | 15-30 mg/kg intramuscularly or intravenously once daily (maximum 1 g) for 60 days, then 15-30 mg/kg 2-3 times weekly (maximum 1 g). |
| Geriatric use | Initiate at lower end of dosing range; adjust based on renal function due to age-related decline in glomerular filtration rate. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CAPREOMYCIN SULFATE (CAPREOMYCIN SULFATE).
| Breastfeeding | Small amounts excreted in breast milk; not expected to cause adverse effects in infants due to poor oral absorption. M/P ratio unknown. |
| Teratogenic Risk | Animal studies suggest embryotoxicity and teratogenicity; human data limited. Avoid in first trimester; use in second and third trimesters only if clearly needed. Risk of ototoxicity and nephrotoxicity to fetus. |
| Fetal Monitoring |
■ FDA Black Box Warning
None officially listed by FDA; however, use with caution due to potential nephrotoxicity and ototoxicity.
| Serious Effects |
["Hypersensitivity to capreomycin or any component","Pre-existing severe renal impairment (CrCl < 30 mL/min) unless benefit outweighs risk","Pre-existing hearing loss"]
| Precautions | ["Nephrotoxicity: Monitor renal function; risk increases with cumulative dose and concomitant nephrotoxic drugs.","Ototoxicity: Can cause vestibular and cochlear damage, especially in patients with renal impairment.","Neuromuscular blockade: May exacerbate weakness in patients with myasthenia gravis or other neuromuscular disorders.","Electrolyte disturbances: Hypokalemia, hypocalcemia, and hypomagnesemia due to renal tubular effects."] |
| Food/Dietary | No specific food interactions. However, maintain adequate hydration and electrolyte-rich diet (bananas, potatoes) to mitigate hypokalemia. |
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| Monitor maternal renal function (serum creatinine, BUN), audiometry, and vestibular function. Assess fetal growth and development via ultrasound; check for signs of nephrotoxicity and ototoxicity in neonate. |
| Fertility Effects | No known significant impact on fertility in humans; animal studies show no adverse reproductive effects. |
| Clinical Pearls | Capreomycin is a second-line injectable agent for multidrug-resistant tuberculosis (MDR-TB). Monitor for nephrotoxicity (creatinine, BUN) and ototoxicity (audiometry, vestibular testing). Electrolyte disturbances (hypokalemia, hypomagnesemia) are common; replace aggressively. Administer deep IM injection; rotate sites. Contraindicated in pregnancy (teratogenic). Synergistic with other antituberculars; never use as monotherapy. |
| Patient Advice | Take exactly as prescribed; do not skip doses to prevent resistance. · Report hearing loss, ringing in ears, or dizziness immediately. · Report decreased urine output, swelling, or unusual fatigue. · You will need regular blood tests (kidney function, electrolyte levels). · Avoid alcohol and excessive salt intake. · Contact your doctor if you develop severe injection site pain or fever. |