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Monday, November 28, 2011

CYCLOSERINE

Antibacterial activity

Used in combination with other antituberculosis medications in the treatment of pulmonary tuberculosis caused by Mycobacterium tuberculosis after failure with the primary medications (isoniazid, aminosalicylic acid, streptomycin, ethambutol, and rifampin) or when these cannot be used because of toxicity or development of resistant tubercle bacilli
Also used in the treatment of atypical mycobacterial infections, such as Mycobacterium avium complex

Pregnancy Risk Factor

Class C

Contraindication/Precaution

Do not use in the presence of:
hypersensitivity to cycloserine or any component
epilepsy
depression
severe anxiety, or psychosis
sever renal insufficiency
excessive concurrent use of alcohol
Do not use if nursing
Safety of the use of cycloserine in infants and children has not been established.

Mechanism of Action

Inhibits bacterial cell wall synthesis by competing with amino acid (D-alanine) for incorporation into the bacterial cell wall; bacteriostatic or bactericidal

Pharmacodynamics

Metabolism: liver
Half-life: 10 hours, changes with renal function
Elimination: excreted in urine and some in feces

Dosage

Children: (max 1000 mg/day)

Safety of the use of capreomycin sulfate in infants and children has not been established.
But 10-20 mg/kg/day PO div bid  for 18-24 months have been used

Adults: (max 1000 mg/day)

250 mg PO q12h for 14 days then 
0.5-1 g/day div bid for 18-24 months
always administered in combination with at least 1 other antituberculosis agent

Dose VS renal function

Cr. clearance (ml/min):
<10: give q36-48h 10-50: give q24h >50: unchanged

Dialysis
Hemo: N/A
CAPD:  N/A

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