Last Updated June 10, 2016
Broad spectrum antibiotic targeting cell envelope; derivative of cycloserine
Indication: treatment of tuberculosis resistant to first-line agents, when administered in combination with at least 1 or 2 other second-line drugs to which the organism is known to be susceptible.
Mechanism of action: inhibits cell wall synthesis through enzymatic inhibition.
Pharmacokinetics: readily absorbed and widely distributed to tissues and fluids; Tmax 2-6 hours.
Adult Dose: 10-20 mg/kg/day in divided doses, usually 250-500 mg twice daily.
Take on empty stomach; give with meals if gastrointestinal intolerance occurs.*
Give with pyridoxine 150 mg/day.*
Use in Renal or Hepatic Insufficiency:
Use in Pregnancy and Breastfeeding: Limited information available in pregnancy and lactation.
Use in Children: Off-label use: 15-20 mg/kg/day as single dose; used for multidrug-resistant tuberculosis and drug-resistant tuberculosis meningitis.
Should be given with pyridoxine 25 mg per terizidone 250 mg.*
Contraindicated in patients with hypersensitivity to cycloserine, neurological conditions (epilepsy, depression, severe anxiety, psychosis), severe renal insufficiency, porphyria, or excessive concurrent alcohol use.*
Pyridoxine 150-300 mg/day may prevent or reduce neurotoxicity and should be coadministered.*
Greatest neurological risk in patients with renal insufficiency or those receiving higher doses; reduce dose or discontinue if central nervous system toxicity occurs.
Use as monotherapy or failure to complete full treatment regimen may result in rapid development of resistance.
Stop drug or reduce dose if allergic dermatitis develops.
Increased risk of convulsions in chronic alcoholics.*
Monitor closely if used in psychiatric patients.*
Avoid in patients with uncontrolled seizures. However, if no other option, it may be given and the treatment for seizures adjusted to ensure control.*
Potentiation of adverse effects of concomitant medication: ethionamide (neurotoxicity), isoniazid (central nervous system effects).*
Incompatible with alcohol (increased risk of epilepsy).*
Greatest neurological risk in patients with renal insufficiency or receiving higher doses; reduce dose or discontinue if central nervous system toxicity occurs.
Central nervous system effects (dose related): dizziness, slurred speech, convulsions, headache, vertigo, drowsiness, tremor, paraesthesia, coma, insomnia, confusion, depression, anxiety suicidality, psychosis, confusion, aggression, irritability, paranoia, peripheral neuropathy; changes in liver function tests, hepatitis; hypersensitivity, allergic dermatitis; photosensitivity; megaloblastic anaemia; heart failure at high doses.*
*Information from Aurum Institute Drugs on the Go.