Cycloserine

Indications
 Oral
Tuberculosis
Adult: As 2nd line drug: In combination with other drugs: Initially, 250 mg bid for 2 wk, increased to 0.5-1 g daily in divided doses. Max: 1 g daily. Adjust dose by monitoring plasma concentrations.
Child: As 2nd line drug: 2-12 yr: 5 mg/kg bid; 12-18 yr: 250 mg bid for 2 wk then adjusted to a max dose of 1 g daily. Adjust doses according to blood concentrations and response.
Renal impairment: Mild-moderate: Dose reduction may be needed. Severe: Avoid.

Special Populations: Reduce dose in patients with renal impairment.
Contraindications
 Severe renal impairment, porphyria, depression, epilepsy, severe anxiety, psychosis, chronic alcoholism, hypersensitivity.
Warnings / Precautions
 Discontinue or reduce dose if allergic skin reactions or CNS toxicity occurs; monitor haematological, renal and hepatic function; Blood levels should be determined wkly for renally impaired patients or if dose exceeds 500 mg/day or if there are signs of neurological toxicity. Pregnancy and lactation.
Adverse Reactions
 Headache, dizziness, anxiety, confusion, irritability, paraesthesia, speech difficulties, photosensitivity, vertigo, drowsiness, tremor, psychosis, depression; rashes; megaloblastic anaemia; changes in liver function tests.
Potentially Fatal: Convulsions (dose related).
Overdose Reactions
 Headache, vertigo, confusion, drowsiness, hyperirritability, paresthesias, dysarthria, and psychosis, paresis, seizure and coma. Treatment is symptomatic and supportive. Emesis or gastric lavage and the use of charcoal may help to remove unabsorbed drug. Monitor patient's vital signs, blood gases and serum electrolytes. Neurotoxic effects may be treated and/or prevented by administering 200-300 mg of pyridoxine hydrochloride daily. Haemodialysis may enhance elimination of cycloserine from the body.
Drug Interactions
 Concurrent usage with other antituberculosis drugs may lead to vitamin B12 and/or folic acid deficiency, megaloblastic and sideroblastic anemia.
Potentially Fatal: Inhibits phenytoin metabolism and may increase risk of epileptic seizures. Alcohol increases risk of convulsions. Increased CNS toxicity with isoniazid and ethionamide.
See Below for More cycloserine Drug Interactions
Mechanism of Actions
 Cycloserine interferes with bacterial cell wall synthesis by competing with D-alanine for incorporation into the cell wall and competitive antagonist of the racemase enzyme. It is a second-line antituberculous drug effective against M. tuberculosis. It is also active against other mycobacteria eg, M. fortuitum, M. kansasii and M. malmoense.
Absorption: Readily absorbed from the GI tract (oral); peak plasma concentrations after 3-4 hr.
Distribution: Body tissues and fluids (wide), CSF, breast milk, crosses the placenta (concentrations near maternal serum).
Excretion: Via urine by glomerular filtration (as unchanged); 10 hr (elimination half-life).
Administration
 May be taken with or without food. (May be taken after meals if GI discomfort occurs.)
Storage Conditions
 Oral: Store below 25°C.
ATC Classification
 J04AB01 - cycloserine ; Belongs to the class of antibiotics. Used in the systemic treatment of tuberculosis.
Storage
 Oral: Store below 25°C.
Available As
  • Cycloserine 250 mg

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