Drug Detail

Capreomycin

Last Updated June 10, 2016

Trade Names

Capastat

Drug Classification

Polypeptide antibiotic, aminoglycoside

Formulations

Capreomycin sulphate 1,000,000 units/vial (equivalent to 1 g capreomycin activity), to be reconstituted for intramuscular or intravenous injection

Indications and Pharmacology

Indication: treatment of active tuberculosis resistant to first-line agents, when administered in combination with at least 1 or 2 other drugs to which the organism is known to be susceptible.

Mechanism of action: inhibits protein synthesis, likely through interaction with ribosomal subunits.

Pharmacokinetics: not well absorbed from gastrointestinal tract; after intramuscular administration: Cmax 20-47 μg/mL, Tmax 1-2 hrs, half-life 12 hrs; Cmax 30 ± 47% higher after intravenous administration; AUC similar. Minimal metabolism.

Dosage

Adult Dose:

  • 750-1000 mg/day intramuscularly, maximum 20 mg/kg/day, for 2-4 months, then dose reduce to maximum 1000 mg 2-3 times weekly.
  • Older than 50 years of age: 10 mg/kg/day, maximum 750 mg/day.

Use in Renal or Hepatic Insufficiency: 

  • For renal impairment, reduce dose and extend dose interval: glomerular filtration rate < 30 mL/min or on haemodialysis, 12-15 mg/kg 2-3 times weekly; glomerular filtration rate < 10 mL/min, dosing interval should be extended to 48 hours.
  • No adjustments needed for hepatic insufficiency.

Use in Pregnancy and Breastfeeding: Pregnancy Category C. Teratogenicity in animals has been reported. Excretion into breast milk unknown. Risk of congenital deafness if used in pregnancy.*

Use in Children: 15-20 mg/kg/day, maximum 1 g/day

Warnings

Contraindicated in patients with hypersensitivity to capreomycin.

Caution should be used in those with renal insufficiency or preexisting auditory impairment; risk of cranial nerve VIII impairment or renal injury should be weighed against potential benefit of treatment.

Use limited by renal toxicity; monthly creatinine and electrolyte monitoring recommended.

Concomitant administration of other parental antituberculosis agents or non-antituberculosis drugs with potential ototoxic or nephrotoxic effects not recommended.

Perform audiometry at baseline, monthly during the injectable phase, and 3 months after cessation of the injectable.*

Use alone or failure to complete full treatment regimen may result in rapid development of resistance.

Drug–Drug Interactions

Contraindicated: other aminoglycosides (streptomycin, kanamycin, amikacin) due to cumulative toxicity; other antituberculosis agents or non-antituberculosis drugs with potential ototoxic or nephrotoxic effects.

Cross-resistance: occurs with viomycin; may occur with kanamycin and neomycin; not observed with isoniazid, para-aminosalicylic acid, cycloserine, streptomycin, ethionamide, or ethambutol.

Considerations for Special Populations

Frequent monitoring of renal function recommended in high-risk patients such as HIV-infected patients with extremely drug-resistant tuberculosis and documented acute renal failure.

Adverse Effects

Nephrotoxicity; electrolyte disturbances including hypokalaemia, hypomagnesaemia, hypocalcaemia; ototoxicity; hypersensitivity reactions including urticaria, maculopapular rash, fever; neuromuscular blockade with high doses or rapid infusions; haematological: leucopenia, leucocytosis, eosinophilia; liver function abnormalities when used with other tuberculosis drugs; local pain when given intramuscularly.

*Information from Aurum Institute Drugs on the Go.
Information from US Prescribing Information.