DailyMed Label: Cycloserine

DailyMed Label: CYCLOSERINE

2023

DailyMed Prescription

CYCLOSERINE

CYCLOSERINE

Parsolex Gmp Center, Inc.

NDC: 13845-1201

NDC: 13845-1201

NDC: 13845-1201

Cycloserine, 3-isoxazolidinone, 4-amino –, (R)– is a broad–spectrum antibiotic that is produced by a strain of Streptomyces orchidaceus and has also been synthesized. Cycloserine is a white to off–white powder that is soluble in water and stable in alkaline solution. It is rapidly destroyed at a neutral or acid pH.   Cycloserine has a pH between 5.5 and 6.5 in a solution containing 100 mg/mL. The molecular weight of cycloserine is 102.09, and it has an empirical formula of C3H6N2O2.

Cycloserine is indicated in the treatment of active pulmonary and extrapulmonary tuberculosis (including renal disease) when the causative organisms are susceptible to this drug and when treatment with the primary medications (streptomycin, isoniazid, rifampin, and ethambutol) has proved inadequate. Like all antituberculosis drugs, cycloserine should be administered in conjunction with other effective chemotherapy and not as the sole therapeutic agent. Cycloserine may be effective in the treatment of acute urinary tract infections caused by susceptible strains of gram–positive and gram–negative bacteria, especially Enterobacter spp. and Escherichia coli. It is generally no more and is usually less effective than other antimicrobial agents in the treatment of urinary tract infections caused by bacteria other than mycobacteria. Use of cycloserine in these infections should be considered only when more conventional therapy has failed and when the organism has been demonstrated to be susceptible to the drug.

Cycloserine is effective orally and is currently administered only by this route. The usual dosage is 500 mg to 1 g daily in divided doses monitored by blood levels.2 The initial adult dosage most frequently given is 250 mg twice daily at 12–hour intervals for the first 2 weeks. A daily dosage of 1 g should not be exceeded.

Administration is contraindicated in patients with any of the following:       Hypersensitivity to cycloserine       Epilepsy       Depression, severe anxiety, or psychosis       Severe renal insufficiency       Excessive concurrent use of alcohol

Before treatment with cycloserine is initiated, cultures should be taken and the organism’s susceptibility to the drug should be established. In tuberculous infections, the organism’s susceptibility to the other antituberculosis agents in the regimen should also be demonstrated. 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 observed for such symptoms. The value of pyridoxine in preventing CNS toxicity from cycloserine has not been proved. Administration of cycloserine and other antituberculosis drugs has been associated in a few instances with vitamin B12 and/or folic–acid deficiency, megaloblastic anemia, and sideroblastic anemia. If evidence of anemia develops during treatment, appropriate studies and therapy should be instituted.

Most adverse reactions occurring during therapy with cycloserine involve the nervous system or are manifestations of drug hypersensitivity. The following side effects have been observed in patients receiving cycloserine:

Concurrent administration of ethionamide has been reported to potentiate neurotoxic side effects. Alcohol and cycloserine are incompatible, especially during a regimen calling for large doses of the latter. Alcohol increases the possibility and risk of epileptic episodes. Concurrent administration of isoniazid may result in increased incidence of CNS effects, such as dizziness or drowsiness. Dosage adjustments may be necessary and patients should be monitored closely for signs of CNS toxicity. Carcinogenesis, Mutagenicity, and Impairment of Fertility Studies have not been performed to determine potential for carcinogenicity. The Ames test and unscheduled DNA repair test were negative. A study in 2 generations of rats showed no impairment of fertility relative to controls for the first mating but somewhat lower fertility in the second mating.

Cycloserine is available as a 250 mg capsule with an opaque red cap and opaque gray body imprinted with “CHAO” and “F04” in edible black ink on both the cap and the body.  Bottles of 40  NDC 13845-1201-3 Store at controlled room temperature, 20° to 25°C (68° to 77°F) [see USP].

After oral administration, cycloserine is readily absorbed from the gastrointestinal tract, with peak blood levels occurring in 4 to 8 hours. Blood levels of 25 to 30 μg/mL can generally be maintained with the usual dosage of 250 mg twice a day, although the relationship of plasma levels to dosage is not always consistent. Concentrations in the cerebrospinal fluid, pleural fluid, fetal blood, and mother’s milk approach those found in the serum. Detectable amounts are found in ascitic fluid, bile, sputum, amniotic fluid, and lung and lymph tissues. Approximately 65 percent of a single dose of cycloserine can be recovered in the urine within 72 hours after oral administration. The remaining 35 percent is apparently metabolized to unknown substances. The maximum excretion rate occurs 2 to 6 hours after administration, with 50 percent of the drug eliminated in 12 hours.

CYCLOSERINE Capsules, USP  250mg  THE CHAO CENTER  NDC 13845-1201-3  40 capsules Rx only Usual Initial Adult Dose: One capsule (250 mg) twice a day at 12 hour intervals. See accompanying literature. Dispense in a tight container. WARNING: Potent drug. May cause serious reactions in some individuals. Use in patients under close medical supervision. Read accompanying literature before using. 13845-1201-3 LM000264.00 Keep tightly closed. Store at controlled room temperature, 20 degrees  to 25 degrees C (68 degrees to 77 degrees F). [see USP] Maunfacture  The Chao center for Industrial Pharmacy and Contract Manufacturing, West Lafayette, IN 47906, USA Expiration Date  Batch No. PURDUE GMP CYCLOSERINE LABEL