Cycloserine
Pronunciation: (sigh-kloe-SER-een)Class: Antituberculosis agent
Trade Names:
Seromycin Pulvules
- Capsules 250 mg
Pharmacology
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Inhibits cell wall synthesis in susceptible strains of certain microorganisms.
Pharmacokinetics
Absorption
Readily absorbed. T max is 4 to 8 h.
Distribution
Widely distributed in tissues (eg, CSF, pleural fluid).
Metabolism
35% metabolized to unknown metabolites.
Elimination
About 65% of a single dose is excreted in urine within 72 h. Maximum excretion rate occurs 2 to 6 h after dose, with 50% eliminated in 12 h.
Indications and Usage
Treatment of active pulmonary and extrapulmonary tuberculosis when organisms are susceptible (after failure of adequate treatment with primary medications); treatment of UTIs caused by susceptible bacteria when conventional therapy has failed; treatment of Gaucher disease.
Contraindications
Epilepsy; depression; severe anxiety or psychosis; severe renal function impairment; excessive concurrent use of alcohol.
Dosage and Administration
AdultsPO 250 to 500 mg every 12 h; start with 250 mg every 12 h for first 2 wk (max, 1 g/day).
ChildrenPO 15 to 20 mg/kg/day administered in 2 equally divided doses (max, 1 g/day).
General Advice
Administer with meals if GI upset occurs.
Storage/Stability
Store in airtight, light-resistant container at room temperature.
Drug Interactions
AlcoholIncreases possibility and risk of epileptic episodes. Do not use together.
IsoniazidMay increase cycloserine CNS adverse reactions (eg, dizziness).
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
CHF.
CNS
Convulsions; drowsiness; somnolence; headache; tremor; dysarthria; vertigo; confusion; loss of memory; psychoses with suicidal tendencies, behavior changes, hyperirritability, aggression, paresis; hyperreflexia; paresthesias; major and minor clonic seizures; coma; dizziness.
Dermatologic
Rash.
Hepatic
Elevated hepatic transaminase.
Precautions
MonitorCulturesObtain culture before treatment and verify susceptibility when results are available. Therapeutic effectivenessIn patients with tuberculosis, assess for therapeutic effectiveness by monitoring clinical signs and symptoms, sputum cultures, or smears for acid-fast bacilli and chest x-rays. UTIIn patients with UTIs, assess for therapeutic effectiveness by monitoring clinical signs and symptoms and urine cultures. |
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and dosage not well established.
Renal Function
Determine weekly blood levels of drug and adjust dosage to keep blood levels below 30 mcg/mL.
CNS toxicity
Discontinue drug or decrease dosage if symptoms of CNS toxicity develop. May be increased with excessive alcohol consumption. Pyridoxine 200 to 300 mg/day may be given to prevent neurotoxic effects.
Overdosage
Symptoms
CNS depression, drowsiness, mental confusion, headache, vertigo, hyperirritability, paresthesias, dysarthrias, psychosis, paresis, convulsions, coma.
Patient Information
- Instruct patient that if depression or suicidal thoughts occur, notify health care provider immediately.
- Stress importance of regular follow-up visits to health care provider for ongoing assessment.
- If patient does not have adequate family support system, refer patient to community health organization for monitoring and support.
- Instruct patient to report the following symptoms to health care provider: rash, anxiety, restlessness, confusion or tremor.
- Caution patient to avoid intake of alcoholic beverages because of increased risk of seizures.
- Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
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cycloserine - Includes detailed dosage instructions.
Compare Cycloserine with other medications for the treatment of:
Tuberculosis, Extrapulmonary, Tuberculosis, Active
