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Cycloserine information from DrugsUpdate  

See Available Brands of Cycloserine in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Cycloserine is an antibiotic effective against Mycobacterium tuberculosis. For the treatment of tuberculosis, it is classified as a second line drug, i.e. its use is only considered if one or more first line drugs cannot be used.
Although in principle active against other bacteria as well, cycloserine is not commonly used in the treatment of infections other than tuberculosis.

Pharmacodynamics

Pharmacokinetics

Cycloserine interferes with bacterial cell wall synthesis by competing with D-alanine for incorporation into the cell wall and competitive antagonist of the racemase enzyme. It is a second-line antituberculous drug effective against M. tuberculosis. It is also active against other mycobacteria eg,
M. fortuitum, M. kansasii and M. malmoense.
Absorption: Readily absorbed from the GI tract (oral); peak plasma concentrations after 3-4 hr.
Distribution: Body tissues and fluids (wide), CSF, breast milk, crosses the placenta (concentrations near maternal serum).
Excretion: Via urine by glomerular filtration (as unchanged); 10 hr (elimination half-life).

Cycloserine Indications / Cycloserine Uses

Information Not Available

Cycloserine Adverse Reactions / Cycloserine Side Effects

Headache, dizziness, anxiety, confusion, irritability, paraesthesia, speech difficulties, photosensitivity, vertigo, drowsiness, tremor, psychosis, depression; rashes; megaloblastic anaemia; changes in liver function tests.
Potentially Fatal: Convulsions (dose related).

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.
Overdosage: Headache, vertigo, confusion, drowsiness, hyperirritability, paresthesias, dysarthria, and psychosis, paresis, seizure and coma. Treatment is symptomatic and supportive. Emesis or gastric lavage and the use of charcoal may help to remove unabsorbed drug. Monitor patient’s vital signs, blood gases and serum electrolytes. Neurotoxic effects may be treated and/or prevented by administering 200–300 mg of pyridoxine hydrochloride daily. Haemodialysis may enhance elimination of cycloserine from the body.

Special Precautions

Discontinue or reduce dose if allergic skin reactions or CNS toxicity occurs; monitor haematological, renal and hepatic function; Blood levels should be determined wkly for renally impaired patients or if dose exceeds 500 mg/day or if there are signs of neurological toxicity. Pregnancy and lactation.

Other Drug Interactions

Concurrent usage with other antituberculosis drugs may lead to vitamin B12 and/or folic acid deficiency, megaloblastic and sideroblastic anemia.

Potentially Fatal: Inhibits phenytoin metabolism and may increase risk of epileptic seizures. Alcohol increases risk of convulsions. Increased CNS toxicity with isoniazid and ethionamide.

Other Interactions

Information Not Available

Dosage

Oral
As 2nd line drug in tuberculosis
Adult: In combination with other drugs: Initially, 250 mg bid for 2 wk, increased to 0.5-1 g daily in divided doses. Max: 1 g daily. Adjust dose by monitoring plasma concentrations. Child: 2-12 yr: 5 mg/kg bid; 12-18 yr: 250 mg bid for 2 wk then adjusted to a max dose of 1 g daily. Adjust doses according to blood concentrations and response.
Renal impairment: Mild-moderate: Dose reduction may be needed. Severe: Avoid.

Food(before/after)

May be taken with or without food. (May be taken after meals if GI discomfort occurs.)

List of Contraindications

Cycloserine and Pregnancy

Caution when used during pregnancy.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Cycloserine and Lactation

Caution when used during lactation

Cycloserine and Children

Safety and dosage not well established

Cycloserine and Geriatic

Information Not Available

Cycloserine and Other Contraindications

Severe renal impairment, porphyria, depression, epilepsy, severe anxiety, psychosis, chronic alcoholism, hypersensitivity.

Storage

Oral: Store below 25°C

Lab interference

Oral: Store below 25°C

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