Microbiology: Cycloserine inhibits cell-
wall synthesis in susceptible strains of related to excessive blood levels (above CAPSULES, USP
gram-positive and gram-negative bacteria and in Mycobacterium tuberculosis.
The ratio of toxic dose to effective dose Cycloserine, (R)-4-amino-3-isoxazoli- Susceptibility Tests: Cycloserine
Streptomyces orchidaceus and has also methods1 of determining the susceptibility been synthesized. Cycloserine is a white hematologic, renal excretion, blood level, water and stable in alkaline solution. It is rapidly destroyed at a neutral or acid pH.
Cycloserine is indicated in the treatment General: Before treatment with
cycloserine is initiated, cultures should be taken and the organism’s susceptibility tuberculous infections, the organism’s susceptibility to the other antituberculosis Anticonvulsant drugs or sedatives may be effective in controlling symptoms of CNS toxicity, such as convulsions, anxiety, and tremor. Patients receiving more than 500 mg of cycloserine daily should be closely CYCLOSERINE
mg (2.45 mmol); D & C Yellow No. 10, treatment of acute urinary tract infections F D & C Blue No. 1, F D & C Red No. 3, of pyridoxine in preventing CNS toxicity F D & C Yellow No. 6, gelatin, iron oxide, from cycloserine has not been proved.
talc, titanium dioxide, and other inactive Escherichia coli. It is generally no more and is usually less effective than other CLINICAL PHARMACOLOGY
bacteria other than mycobacteria. Use of cycloserine in these infections should be during treatment, appropriate studies and therapy has failed and when the organism Laboratory Tests: Blood levels should
patients with reduced renal function, for CONTRAINDICATIONS
cerebrospinal fluid, pleural fluid, fetal to keep the blood level below 30 µg/mL.
• Depression, severe anxiety, or psychosis Interactions:
Alcohol and cycloserine are incompatible, the patient develops allergic dermatitis to 6 hours after administration, with 50% may result in increased incidence of CNS effects, such as dizziness or drowsiness. and patients should be monitored closely Cardiovascular: Sudden development
charcoal instead of or in addition to gastric Carcinogenesis, Mutagenicity, and
receiving 1 to 1.5 g of cycloserine daily Impairment of Fertility: Studies
Allergy (apparently not related to
employing gastric emptying or charcoal.
In adults, many of the neurotoxic effects Skin rash
of rats showed no impairment of fertility Miscellaneous:
prevented with the administration of 200 relative to controls for the first mating but transaminase, especially in patients with OVERDOSAGE
Pregnancy Category C: A study in 2
Signs and Symptoms: Acute toxicity
generations of rats given doses up to 100 reserved for patients with life-threatening effect in offspring. It is not known whether toxicity from cycloserine is dose related DOSAGE AND ADMINISTRATION
affect reproduction capacity. Cycloserine currently administered only by this route. The usual dosage is 500 mg to 1 g daily in divided doses monitored by blood levels.2 Nursing Mothers: Because of the
The initial adult dosage most frequently intervals for the first 2 weeks. A daily dosage of 1 g should not be exceeded.
discontinue nursing or to discontinue the drug, taking into account the importance confusion, drowsiness, hyperirritability, HOW SUPPLIED
paresthesias, dysarthria, and psychosis. Usage in Pediatric Patients: Safety and
effectiveness in pediatric patients have convulsions, and coma often occur. Ethyl opaque gray body imprinted with “CHAO” alcohol may increase the risk of seizures and “F04” in edible black ink on both the ADVERSE REACTIONS
Aluminum blisters (a pack of 3 cards each with 10 capsules). NDC 13845-1202-2.
drug hypersensitivity. The following side 20° to 25°C (68° to 77°F) [see USP].
Nervous system symptoms (which
poison control centers are listed in the of the drug, i.e., more than 500 mg daily) Physician’s Desk Reference (PDR). In Health Service, 1967, pp 47–55, 66–70.
of cycloserine, a new antibiotic. Anal reported rarely. The following is provided • Confusion and disorientation with loss Protect the patient’s airway and support limits, the patient’s vital signs, blood gases, serum electrolytes, etc. Absorption of drugs from the gastrointestinal tract • Major & minor (localized) clonic seizures effective than emesis or lavage; consider


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