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Indications and Dosage
Oral
Second line drug in tuberculosis Adult: Initially, 250 mg bid for 2 wk, followed by 500-1000 mg daily in divided doses. Max: 1000 mg daily. Adjust dose by monitoring plasma concentrations.
Child: 10 mg/kg daily. Adjust doses according to blood concentrations and response. |
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Renal Impairment
Mild to moderate: Dose reduction may be needed. Severe: Contraindicated.
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Administration
May be taken with or without food. May be taken after meals if GI discomfort occurs.
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Contraindications
Hypersensitivity. Patient w/ epilepsy, depression, severe anxiety, psychosis, or in those who misuse alcohol. Severe renal impairment.
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Special Precautions
Patient w/ porphyria. Mild to moderate renal impairment. Pregnancy and lactation.
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Adverse Reactions
Drowsiness, somnolence, dizziness, headache, lethargy, depression, tremor, dysarthria, hyperreflexia, paraesthesia, nervousness, anxiety, vertigo, confusion, disorientation, loss of memory, paresis, major and minor clonic seizures, convulsions, coma; psychosis (possibly w/ suicidal tendencies), personality changes, hyperirritability, aggression; elevated serum aminotransferase levels, esp in patients w/ pre-existing liver disease. Rarely, hypersensitivity reactions including rash, and photosensitivity; cardiac arrhythmias and sudden CHF.
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Monitoring Parameters
Monitor renal, hepatic, and hematological functions; plasma cycloserine concentrations.
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Overdosage
Symptoms: Headache, vertigo, confusion, drowsiness, hyper-irritability, paraesthesias, dysarthria and psychosis; paresis, convulsions and coma often occur in larger doses. Management: Symptomatic and supportive treatment. Activated charcoal may be more effective than emesis or lavage in reducing absorption. May give 200-300 mg of pyridoxine HCl daily to treat and prevent neurotoxic events. Haemodialysis may remove the drug from the bloodstream but should only be used for life-threatening toxicity.
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Drug Interactions
Concomitant use w/ other anti-TB drugs may lead to vit B12 and/or folic acid deficiency, megaloblastic and sideroblastic anaemia. Increased incidence of CNS effects w/ ethionamide and isoniazid. May inhibit hepatic metabolism of phenytoin.
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Food Interaction
Alcohol increases risk of epileptic episodes.
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Action
Description: Cycloserine inhibits bacterial cell wall synthesis by competing w/ amino acid (D-alanine) for incorporation into the bacterial cell wall. It may be bacteriostatic or bactericidal.
Pharmacokinetics: Absorption: Readily and almost completely absorbed from the GI tract. Time to peak plasma concentration: 3-4 hr. Distribution: Widely distributed into body tissues and fluids, including the CSF, placenta, and breast milk. Metabolism: Hepatic. Excretion: Via urine by glomerular filtration (as unchanged drug). Plasma half-life: Approx 10 hr. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Cycloserine, CID=6234, https://pubchem.ncbi.nlm.nih.gov/compound/Cycloserine (accessed on Jan. 22, 2020) |
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Storage
Store between 20-25°C.
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MIMS Class
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References
Anon. Cycloserine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/08/2014. Buckingham R (ed). Cycloserine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 18/08/2014. McEvoy GK, Snow EK, Miller J et al (eds). Cycloserine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 18/08/2014. Seromycin Capsule (Purdue GMP Center LLC dba The Chao Center). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 18/08/2014.
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