No

Antibiotic, Miscellaneous; Antitubercular Agent

Adjunctive treatment in pulmonary or extrapulmonary tuberculosis; has been studied for use in Gaucher's disease

C

Known hypersensitivity to cycloserine

Epilepsy, depression, severe anxiety, psychosis, severe renal insufficiency, chronic alcoholism

Percentage unknown: Cardiac arrhythmias, drowsiness, headache, dizziness, vertigo, seizures, confusion, psychosis, paresis, coma, rash, folate deficiency, elevated liver enzymes, tremor, vitamin B₁₂ deficiency

Symptoms of overdose include confusion, agitation, CNS depression, psychosis, coma, seizures

Decontaminate with activated charcoal; can be hemodialyzed; management is supportive; administer 100-300 mg/day of pyridoxine to reduce neurotoxic effects; acute toxicity can occur with ingestions >1 g; chronic toxicity: >500 mg/day

Increased toxicity: Alcohol, isoniazid, ethionamide increase toxicity of cycloserine; cycloserine inhibits the hepatic metabolism of phenytoin

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

Absorption: Oral: ~70% to 90% from the GI tract

Distribution: Crosses the placenta; appears in breast milk; distributed widely to most body fluids and tissues including CSF, breast milk, bile, sputum, lymph tissue, lungs, and ascitic, pleural, and synovial fluids

Half-life: 10 hours in patients with normal renal function

Metabolism: Extensive in liver

Time to peak serum concentration: Oral: Within 3-4 hours

Elimination: 60% to 70% of oral dose excreted unchanged in urine by glomerular filtration within 72 hours, small amounts excreted in feces, remainder is metabolized

Some of the neurotoxic effects may be relieved or prevented by the concomitant administration of pyridoxine

Children: 10-20 mg/kg/day in 2 divided doses up to 1000 mg/day for 18-24 months

Adults: Initial: 250 mg every 12 hours for 14 days, then administer 500 mg to 1 g/day in 2 divided doses for 18-24 months (maximum daily dose: 1 g)

Dosing interval in renal impairment:

Cl_cr 10-50 mL/minute: Administer every 24 hours

Cl_cr <10 mL/minute: Administer every 36-48 hours

May be administered with food; may increase vitamin B₁₂ and folic acid dietary requirements

Periodic renal, hepatic, hematological tests, and plasma cycloserine concentrations

Toxicity is greatly increased at levels >30 mg/mL

May cause drowsiness, confusion, depression, and psychosis

Low doses (50 mg) have been used to treat negative symptoms of schizophrenia

No information available to require special precautions

No effects or complications reported

Take as prescribed; do not discontinue without consulting prescriber. Avoid alcohol. Maintain recommended diet and adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness or restlessness (use caution when driving or engaging in tasks that require alertness until response to drug is known). Report skin rash, acute headache, tremors or changes in mentation (confusion, nightmares, depression, or suicide ideation), or fluid retention (respiratory difficulty, swelling of extremities, unusual weight gain). Pregnancy precautions: Inform prescriber if you are or intend to be pregnant.

Some of the neurotoxic effects may be relieved or prevented by the concomitant administration of pyridoxine

Monitor periodic renal, hepatic, hematological tests, and plasma cycloserine concentrations

Capsule: 250 mg

Davidson PT and Le HQ, "Drug Treatment of Tuberculosis - 1992," Drugs, 1992, 43(5):651-73.

"Drugs for Tuberculosis," Med Lett Drugs Ther, 1993, 35(908):99-101.

Iseman MD, "Treatment of Multidrug-Resistant Tuberculosis," N Engl J Med, 1993, 329(11):784-91.