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Drugs reference index «Cycloserine»

Cycloserine


Cycloserine

Pronunciation: (sigh-kloe-SER-een)Class: Antituberculosis agent

Trade Names:Seromycin Pulvules- Capsules 250 mg

Pharmacology

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

Adults

PO 250 to 500 mg every 12 h; start with 250 mg every 12 h for first 2 wk (max, 1 g/day).

Children

PO 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

Alcohol

Increases possibility and risk of epileptic episodes. Do not use together.

Isoniazid

May 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

Monitor

Cultures

Obtain culture before treatment and verify susceptibility when results are available.

Therapeutic effectiveness

In 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.

UTI

In 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.

Copyright © 2009 Wolters Kluwer Health.

  • Cycloserine MedFacts Consumer Leaflet (Wolters Kluwer)
  • Seromycin Prescribing Information (FDA)
  • cycloserine Advanced Consumer (Micromedex) - Includes Dosage Information
  • cycloserine Concise Consumer Information (Cerner Multum)

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