Adult: In combination with other anti-TB agents for the treatment of pulmonary and extrapulmonary TB: Initially, 250 mg 12 hourly for the 1st 2 weeks, followed by 500-1,000 mg daily in equally divided doses. Adjust dose based on blood concentration and response. Max: 1,000 mg daily. Child: In combination with other anti-TB agents for the treatment of pulmonary and extrapulmonary TB: Initially, 10 mg/kg daily. Adjust dose based on blood concentration and therapeutic response. Max: 1,000 mg daily. Dosage and treatment recommendations may vary among countries and individual products (refer to latest local or specific product guidelines).
Oral Urinary tract infection
Adult: Usual dose: 250 mg 12 hourly for 2 weeks. Use must only be considered when the organism has been demonstrated to be susceptible and when more conventional therapy has failed. Dosage and treatment recommendations may vary among countries and individual products (refer to latest local or specific product guidelines).
Renal Impairment
Mild to moderate: Dose reduction may be needed. Severe: Contraindicated.
Administration
May be taken with or without food. May be taken after meals if GI discomfort occurs.
Contraindications
Hypersensitivity. Epilepsy, mental depression, severe anxiety, psychosis, alcohol abuse or alcoholism. Severe renal impairment.
Special Precautions
Patient with porphyria, history of chronic alcoholism; potential vitamin B12 and/or folate deficiency (e.g. malnutrition, chronic use of antiseizure medications). Patient receiving >500 mg daily dose. Mild to moderate renal impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Vitamin B12 or folate deficiency, megaloblastic anaemia, sideroblastic anaemia; exacerbations of porphyria, allergic dermatitis, CNS toxicity (e.g. psychoses possibly with suicidal tendencies; depression, somnolence, confusion, hyperreflexia, headache, tremor, vertigo, paresis, dysarthria, seizures). Rarely, heart failure (in patients receiving daily dose of 1,000-1,500 mg); hypersensitivity reactions (including rash and photosensitivity). Investigations: Increased serum aminotransferases. Nervous system disorders: Disorientation with loss of memory; paraesthesia, dizziness, coma. Psychiatric disorders: Personality changes, hyperirritability, aggression.
Monitoring Parameters
Perform culture and susceptibility tests; consult local institutional recommendations before treatment initiation due to antibiotic resistance risks. Monitor plasma cycloserine concentrations (at least weekly for patients with renal impairment, taking doses >500 mg daily, or with signs and symptoms of neurotoxicity); renal, hepatic, and haematological functions periodically. Evaluate neuropsychiatric status every month or more frequently if symptoms occur.
Overdosage
Symptoms: Headache, vertigo, confusion, drowsiness, hyperirritability, paraesthesias, dysarthria, and psychosis; in larger doses, paresis, convulsions, and coma may occur. Management: Symptomatic and supportive treatment. Airway of the patient must be protected and ventilation and perfusion supported. Monitor vital signs, serum electrolytes, and blood gases and maintain them within acceptable limits. Activated charcoal may be more effective than emesis or gastric lavage in reducing absorption. May give 200-300 mg of pyridoxine daily to treat and prevent neurotoxic events in adults. Haemodialysis may remove the drug from the bloodstream but must be reserved for life-threatening toxicity which is unresponsive to less invasive treatment.
Drug Interactions
Increased neurotoxic side effects with ethionamide. Enhanced CNS toxicity (e.g. dizziness, drowsiness) with isoniazid.
Food Interaction
Increased risk of seizures with alcohol.
Action
Description: Mechanism of Action: Cycloserine is a broad-spectrum antibiotic that inhibits cell wall synthesis in susceptible bacteria by competing with the amino acid, D-alanine, for incorporation into the bacterial cell wall. It may be bacteriostatic or bactericidal in action depending on the drug concentration at the site of infection and susceptibility of the organism. Pharmacokinetics: Absorption: Readily and almost completely absorbed from the gastrointestinal tract. Time to peak plasma concentration: 3-4 hours. Distribution: Widely distributed into body tissues and fluids, including the CSF, lungs, bile, sputum, lymph tissue, and ascitic, pleural, or synovial fluids. Crosses the placenta and enters breast milk. Metabolism: Metabolised in the liver. Excretion: Via urine (approx 65% as unchanged drug within 72 hours); faeces (small amounts). Elimination half-life: 12 hours.
Chemical Structure
Cycloserine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6234, Cycloserine. https://pubchem.ncbi.nlm.nih.gov/compound/Cycloserine. Accessed Oct. 26, 2023.
J04AB01 - cycloserine ; Belongs to the class of antibiotics. Used in the systemic treatment of tuberculosis.
References
Anon. Cycloserine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 27/07/2023.Anon. Cycloserine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/07/2023.Buckingham R (ed). Cycloserine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/07/2023.Coxerin Capsules 250 mg (Zulat Pharmacy Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 27/07/2023.Cycloserine 250 mg Hard Capsules (Neon Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 27/07/2023.Cycloserine Capsule (Dr. Reddy's Laboratories, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 27/07/2023.Cycloserine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 28/09/2023.Joint Formulary Committee. Cycloserine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/07/2023.
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