Skip to Content

CycloSERINE

Medically reviewed by Drugs.com. Last updated on May 5, 2020.

Pronunciation

(sye kloe SER een)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Generic: 250 mg

Pharmacologic Category

  • Antibiotic, Miscellaneous
  • Antitubercular Agent

Pharmacology

Inhibits bacterial cell wall synthesis by competing with amino acid (D-alanine) for incorporation into the bacterial cell wall; bacteriostatic or bactericidal

Absorption

~70% to 90% from GI tract (WHO 2008)

Distribution

Widely to most body fluids and tissues including CSF, bile, sputum, lymph tissue, lungs, and ascitic, pleural, and synovial fluids (WHO 2008)

Metabolism

Hepatic

Excretion

Urine (~65% as unchanged drug) within 72 hours; Feces (small amounts); remainder metabolized

Time to Peak

Serum: 4 to 8 hours

Half-Life Elimination

Normal renal function: 12 hours

Protein Binding

Not plasma protein bound

Use: Labeled Indications

Tuberculosis: Treatment of active pulmonary or extrapulmonary tuberculosis, in combination with other agents, when treatment with primary tuberculosis therapy has proved inadequate

Urinary tract infections: May be effective in treatment of acute urinary tract infections caused by susceptible strains of gram-positive and gram-negative bacteria, especially Enterobacter spp. and Escherichia coli. Note: Should be considered only when more conventional therapy has failed and when the organism has been demonstrated to be susceptible to the drug.

Contraindications

Hypersensitivity to cycloserine or any component of the formulation; epilepsy; depression, severe anxiety, or psychosis; severe renal insufficiency; excessive concurrent use of alcohol

Dosing: Adult

Tuberculosis, drug-resistant: Oral: 10 to 15 mg/kg/day (maximum: 1 g/day), usually 250 to 750 mg/day in 1 or 2 divided doses as part of an appropriate combination regimen (ATS/CDC/ERS/IDSA [Nahid 2019]; ATS/CDC/IDSA [Nahid 2016]). Note: Some experts recommend the following 2-week dose titration: 250 mg once daily for 3 to 4 days, 250 mg every 12 hours for 3 to 4 days, then 250 mg in the morning and 500 mg in the evening (Curry International Tuberculosis Center 2016). Adjust based on serum concentration (ATS 2003; ATS/CDC/ERS/IDSA [Nahid 2019]; Curry International Tuberculosis Center 2016).

Note: Some neurotoxic effects may be treated or prevented by concomitant administration of 200 to 300 mg of pyridoxine daily or 50 mg of pyridoxine per 250 mg of cycloserine (Curry International Tuberculosis Center 2016; WHO 2008).

Urinary tract infections: Oral: There is no dosage provided in the prescribing information. Note: Should be considered only when more conventional therapy has failed and when the organism has been demonstrated to be susceptible to the drug.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Active tuberculosis infection (excluding meningitis); treatment (second-line therapy): Limited data available: Note: Recommendations often change due to epidemiology (resistance) and emerging information; consult CDC and WHO for current recommendations for detailed information. Always use as part of a multidrug regimen (ATS/CDC/IDSA [Nahid 2016]). Concomitant pyridoxine is recommended to prevent cycloserine-induced neuropathy (WHO 2009).

Infants, Children, and Adolescents <15 years; weighing ≤40 kg: Oral: 15 to 20 mg/kg/day divided every 12 to 24 hours (if tolerability issues, may divide into 2 doses); maximum daily dose: 1,000 mg/day (ATS/CDC/IDSA 2016; HHS [pediatric 2013]; Seddon 2012). Note: Some patients may be unable to tolerate recommended doses; experts suggest beginning with a low once daily dose and gradually increasing as tolerated; serum concentrations targeted at 25 to 30 mcg/mL have been suggested to minimize toxicity (ATS/CDC/IDSA [Nahid 2016]; HHS [pediatric 2013]).

Children and Adolescents <15 years weighing >40 kg or Adolescents ≥15 years: Oral: 10 to 15 mg/kg/day divided every 12 to 24 hours; usual dose 250 to 500 mg; maximum daily dose: 1,000 mg/day Note: Patients are often unable to tolerate the maximum dose divided twice daily (eg, in adults, 500 mg twice daily); therefore, experts suggest beginning with a low once daily dose and gradually increasing as tolerated; may consider therapeutic drug monitoring; serum concentrations targeted at 25 to 30 mcg/mL have been suggested to minimize toxicity (ATS/CDC/IDSA [Nahid 2016]; HHS [pediatric 2013]).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Administration

Administer orally in divided doses with or without food.

Dietary Considerations

May be taken with food; may increase vitamin B12 and folic acid dietary requirements.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Alcohol (Ethyl): May enhance the neurotoxic effect of CycloSERINE. Specifically, the risk for seizures may be increased. Avoid combination

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. Avoid combination

Ethionamide: May enhance the adverse/toxic effect of CycloSERINE. Monitor therapy

Isoniazid: May enhance the adverse/toxic effect of CycloSERINE. Specifically, CNS toxicity may be enhanced. Monitor therapy

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy

Prothionamide: May enhance the adverse/toxic effect of CycloSERINE. Monitor therapy

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Consider therapy modification

Terizidone: May enhance the adverse/toxic effect of CycloSERINE. Monitor therapy

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. Consider therapy modification

Adverse Reactions

Frequency not defined.

Cardiovascular: Cardiac arrhythmia, cardiac failure

Central nervous system: Coma, confusion, dizziness, drowsiness, dysarthria, headache, hyperreflexia, paresis, paresthesia, psychosis, restlessness, seizure, vertigo

Dermatologic: Skin rash

Endocrine & metabolic: Cyanocobalamin deficiency, folate deficiency

Hepatic: Increased liver enzymes

Hypersensitivity: Hypersensitivity reaction

Neuromuscular & skeletal: Tremor

Warnings/Precautions

Concerns related to adverse effects:

• CNS effects: Has been associated with dose-related CNS toxicity, including seizures, psychosis, depression, and confusion; decrease dosage or discontinue use if occurs. Pyridoxine may be coadministered to prevent/treat CNS effects.

• Skin reactions: Allergic dermatitis may occur; reduce dose or discontinue use if allergic dermatitis develops.

• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns:

• Alcoholism: Use with caution in patients with a history of chronic alcoholism; increased risk of seizures.

• Mental illness: Use with caution in patients with depression, severe anxiety, and/or psychosis.

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment may be necessary. Use is contraindicated in severe renal insufficiency.

Special populations:

• Patients with potential for vitamin deficiency: Use with caution in patients with potential vitamin B12 and/or folate deficiency (malnourished, chronic anticonvulsant therapy, or elderly).

Monitoring Parameters

Periodic renal, hepatic, hematological tests, and plasma cycloserine concentrations; assess neuropsychiatric status at monthly intervals and more frequently if symptoms occur (ATS 2003).

Reproductive Considerations

Evaluate pregnancy status prior to treatment of multidrug resistant tuberculosis in females of reproductive potential. Females of reproductive potential should use effective contraception during treatment for multidrug-resistant tuberculosis (Esmail 2018).

Pregnancy Risk Factor

C

Pregnancy Considerations

Cycloserine crosses the placenta and can be detected in the fetal blood and amniotic fluid.

Active tuberculosis infection is associated with adverse fetal outcomes, including intrauterine growth restriction, low birth weight, preterm birth, and perinatal death (Esmail 2018; Miele 2020), as well as adverse maternal outcomes, including increased risks for anemia and cesarean delivery. Placental transmission may rarely occur with active maternal disease (Miele 2020).

Data are limited for use of second-line drugs in pregnancy (ie, cycloserine). The treatment of multidrug-resistant tuberculosis in pregnant patients should be individualized; evidence to support a specific regimen is not available (ATS/CDC/ERS/IDSA [Nahid 2019]; WHO 2020).

Patient Education

What is this drug used for?

• It is used to treat TB (tuberculosis).

• It is used to treat a urinary tract infection (UTI).

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Depression like thoughts of suicide, anxiety, emotional instability, or confusion

• Behavioral changes

• Mood changes

• Fatigue

• Headache

• Confusion

• Trouble with memory

• Dizziness

• Passing out

• Seizures

• Muscle weakness

• Shortness of breath

• Excessive weight gain

• Swelling of arms or legs

• Severe loss of strength and energy

• Change in speech

• Tremors

• Burning or numbness feeling

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.