Clinical medicine profile
Cycloserine
Therapeutic agent (verify pharmacological class)
- Route
- See product SmPC
- Schedule
- POM
- ATC
- Not assigned
- PPB status
- registered
Safety essentials
The information most likely to change a prescribing or dispensing decision.
Contraindications
- CONTRAINDICATIONS Administration is contraindicated in patients with any of the following: • Hypersensitivity to cycloserine • Epilepsy • Depression, severe anxiety, or psychosis • Severe renal insufficiency • Excessive concurrent use of alcoho
Precautions
- WARNINGS Administration of cycloserine should be discontinued or the dosage reduced if the patient develops allergic dermatitis or symptoms of CNS toxicity, such as convulsions, psychosis, somnolence, depression, confusion, hyperreflexia, headache, tremor, vertigo paresis, or dysarthria.
- The toxicity of cycloserine is closely related to excessive blood levels (above 30 mcg/mL), as determined by high dosage or inadequate renal clearance.
- The ratio of toxic dose to effective dose in tuberculosis is small.
- The risk of convulsions is increased in chronic alcoholics.
- Patients should be monitored by hematologic, renal excretion, blood level, and liver function studies.
Dosing matrix
Population and organ-function guidance, shown together for faster comparison.
DOSAGE AND ADMINISTRATION Cycloserine is effective orally and is currently administered only by this route. The usual dosage is 500 mg to 1 g daily in divided doses monitored by blood levels. 1 The initial adult dosage most frequently given is 250 mg twice daily at 12-hour intervals for the first 2 weeks. A daily dosage of 1 g should not be exceeded.
See label paediatric section if present; otherwise use paediatric formulary — do not extrapolate adult doses.
Review renal impairment dosing; many agents need CrCl/eGFR adjustment.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.
Use, effects & interactions
Indications
- INDICATIONS AND USAGE Cycloserine is indicated in the treatment of active pulmonary and extrapulmonary tuberculosis (including renal disease) when the causative organisms are susceptible to this drug and when treatment with the primary medications (streptomycin, isoniazid, rifampin, and ethambutol) has proved inadequate.
- Like all antituberculosis drugs, cycloserine should be administered in conjunction with other effective chemotherapy and not as the sole therapeutic agent.
- Cycloserine may be effective in the treatment of acute urinary tract infections caused by susceptible strains of gram-positive and gram- negative bacteria.
- Use of cycloserine in these infections should be considered only when more conventional therapy has failed and when the organism has been demonstrated to be susceptible to the drug
Adverse effects
- ADVERSE REACTIONS Most adverse reactions occurring during therapy with cycloserine involve the nervous system or are manifestations of drug hypersensitivity.
- The following side effects have been observed in patients receiving cycloserine: Nervous system symptoms (which appear to be related to higher dosages of the drug, i.e., more than 500 mg daily) • Convulsions • Drowsiness and somnolence • Headache • Tremor • Dysarthria • Vertigo • Confusion and disorientation with loss of memory • Psychoses, possibly with suicidal tendencies • Character changes • Hyperirritability • Aggression • Paresis • Hyperreflexia • Paresthesia • Major & minor (localized) clonic seizures • Coma Cardiovascular: Sudden development of congestive heart failure in patients receiving 1 to 1.5 g of cycloserine daily has been reported.
- Allergy (apparently not related to dosage) Skin rash Miscellaneous: Elevated serum transaminase, especially in patients with preexisting liver disease To report SUSPECTED ADVERSE REACTIONS, contact Cerovene, Inc. at 1-833-304-9569 or FDA at 1‑800-FDA-1088 or www.fda.gov/medwatch.
Drug interactions
Open multi-drug checker ↗- Professional use: confirm indication, dose, duration, monitoring and patient counselling points against current Kenya STG / EML and the product SmPC.
- Document allergy status and key interactions.
Mechanism & disposition
Cycloserine, an analog of the amino acid D-alanine, interferes with bacterial cell wall synthesis by competitive inhibition of two enzymes, L alanine racemase, which forms D-alanine from L-alanine, and D-alanylalanine synthetase.
Read complete mechanism
Cycloserine, an analog of the amino acid D-alanine, interferes with bacterial cell wall synthesis by competitive inhibition of two enzymes, L alanine racemase, which forms D-alanine from L-alanine, and D-alanylalanine synthetase. These enzymes are involved in the incorporation of D-alanine into the pentapeptide necessary for peptidoglycan formation and bacterial cell wall synthesis.
Product-specific
Product-specific
See product SmPC
rate occurs 2 to 6 hours after administration, with 50% of the drug eliminated in 12 hours. Mechanism of Action: The antibacterial activity of Cycloserine results from inhibition of cell-wall synthesis in susceptible strains of gram-positive and gram-negative bacteria. Antibacter...
Pregnancy, lactation & diet
Use only if potential benefit justifies potential risk; prefer agents with better reproductive data when alternatives exist.
Assess infant risk vs benefit of maternal therapy; prefer agents with lactation data.
Brands & loaded prices
| Brand | Manufacturer | Pack | Observed price |
|---|---|---|---|
| No reviewed brand listings are linked yet. | |||
Sources & review state
Decision support only. Confirm patient-specific decisions against the current product SmPC, Kenya STG/EML, and professional judgement.