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Cycloserine: Drug information

Cycloserine: Drug information
(For additional information see "Cycloserine: Patient drug information" and see "Cycloserine: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Antibiotic, Miscellaneous;
  • Antitubercular Agent
Dosing: Adult
Tuberculosis, drug resistant

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).

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

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; use is contraindicated in severe impairment. However, the following adjustments have been used by some clinicians:

ATS/CDC/IDSA guidelines: CrCl <30 mL/minute or hemodialysis: 250 mg once daily or 500 mg 3 times per week. Note: The appropriateness of 250 mg daily doses has not been established, and careful monitoring is necessary for evidence of neurotoxicity. Monitor serum concentrations to minimize toxicity (ATS/CDC/IDSA [Nahid 2016]).

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Older Adult

Refer to adult dosing; start at lower end of dosage range and use with caution.

Dosing: Pediatric

(For additional information see "Cycloserine: Pediatric drug information")

Active tuberculosis infection, treatment

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.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; use is contraindicated in severe impairment; based on experience in adult patients, dosage adjustment suggested in moderate impairment.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Adverse Reactions

The following adverse drug reactions are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.

Frequency not defined:

Cardiovascular: Heart failure

Endocrine & metabolic: Vitamin B12 deficiency

Hepatic: Increased serum transaminases

Nervous system: Amnesia, behavioral changes, coma, confusion, disorientation, drowsiness, dysarthria, hyperreflexia, paresis, paresthesia, seizure, tremor, vertigo

Postmarketing:

Dermatologic: Lichenoid eruption (Kim 2017), Stevens-Johnson syndrome (Akula 1997)

Endocrine & metabolic: Folate deficiency (Klipstein 1967)

Hematologic & oncologic: Megaloblastic anemia (Klipstein 1967), sideroblastic anemia (Klipstein 1967)

Nervous system: Encephalopathy (Kwon 2008), headache (Singanamala 2019), psychiatric disturbance (including aggressive behavior, depression, hallucination, hyperirritability, mania, psychosis, and suicidal tendencies) (Bakhla 2013; Intini 2019; Singanamala 2019)

Contraindications

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

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

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 antiseizure medication therapy, or elderly).

Dosage Forms: US

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

Capsule, Oral:

Generic: 250 mg

Generic Equivalent Available: US

Yes

Pricing: US

Capsules (cycloSERINE Oral)

250 mg (per each): $91.88

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral: Administer in divided doses with or without food.

Administration: Pediatric

Oral: May administer without regard to meals; administer with meals to decrease GI distress

Use: Labeled Indications

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

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

Medication Safety Issues
Sound-alike/look-alike issues:

CycloSERINE may be confused with cyclobenzaprine, cycloPHOSphamide, cycloSPORINE

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

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

Bacillus clausii: Antibiotics may diminish the therapeutic effect of Bacillus clausii. Management: Bacillus clausii should be taken in between antibiotic doses during concomitant therapy. Risk D: Consider therapy modification

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

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Risk C: 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. Risk X: Avoid combination

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

Fecal Microbiota (Live) (Oral): May diminish the therapeutic effect of Antibiotics. Risk X: Avoid combination

Fecal Microbiota (Live) (Rectal): Antibiotics may diminish the therapeutic effect of Fecal Microbiota (Live) (Rectal). Risk X: Avoid combination

Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies): Antibiotics may diminish the therapeutic effect of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Risk C: Monitor therapy

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

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

Prothionamide: May enhance the adverse/toxic effect of CycloSERINE. Risk C: 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. Risk D: Consider therapy modification

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

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Avoid use of live attenuated typhoid vaccine (Ty21a) in patients being treated with systemic antibacterial agents. Postpone vaccination until 3 days after cessation of antibiotics and avoid starting antibiotics within 3 days of last vaccine dose. Risk D: Consider therapy modification

Food Interactions

May increase vitamin B12 and folic acid dietary requirements. Management: Vitamin B12 and folic acid supplementation may be needed.

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 Considerations

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

Tuberculosis (TB) disease (active TB) 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).

Breastfeeding Considerations

Cycloserine is present in breast milk.

Cycloserine levels in breast milk are similar to those found in the maternal serum. Due to the potential for serious adverse reactions in the nursing infant, the manufacturer recommends a decision be made whether to discontinue nursing or to discontinue the drug, considering the importance of treatment to the mother. Patients with multidrug-resistant tuberculosis and a sputum smear-positive test should avoid breastfeeding when possible (Esmail 2018).

Dietary Considerations

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

Monitoring Parameters

Periodic renal and hematological tests, and plasma cycloserine concentrations; assess neuropsychiatric status at monthly intervals and more frequently if symptoms occur (ATS/CDC/ERS/IDSA [Nahid 2019]; Curry International Tuberculosis Center 2016).

Reference Range

Therapeutic peak (2 hours post-dose) levels: Tuberculosis: 20 to 35 mcg/mL (ATS/CDC/ERS/IDSA [Nahid 2019]; Curry International Tuberculosis Center 2016; ATS 2003).

Toxicity is greatly increased at levels >35 mcg/mL (Curry International Tuberculosis Center 2016).

Mechanism of Action

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

Pharmacokinetics (Adult Data Unless Noted)

Absorption: ~70% to 90% from GI tract (WHO 2008). Absorption is delayed and Cmax lowered when administered with high-fat meal compared to fasting, but AUC not impacted (Zhu 2001).

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

Protein binding: Not plasma protein bound

Metabolism: Hepatic

Half-life elimination: Normal renal function: 12 hours

Time to peak, serum: 4 to 8 hours

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

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Cyclocat;
  • (CN) China: Sai lai xing;
  • (CO) Colombia: Cicloserina;
  • (EE) Estonia: Cicloserina antibiotice | Seromycin;
  • (FI) Finland: Cycloserin;
  • (FR) France: Seromycine;
  • (GR) Greece: Cicloserina | D Cycloserine;
  • (HK) Hong Kong: Seromycin;
  • (IE) Ireland: Seromycin;
  • (IN) India: Coxerin | Cyclorine | Cyclotec | Cyserine | Myser;
  • (JP) Japan: Cyclomycin | Cycloserine aventis | Cycloserine kyowa | Cycloserine meiji | Cycloserine pfizer | Cycloserine sankyo | Cycloserine sumitomo | Cycloserine takeda | Orientmycin;
  • (KE) Kenya: Aspen cycloserine | Coxerin;
  • (KR) Korea, Republic of: Closerin | Curos | Cyrine;
  • (LT) Lithuania: Cicloserina antibiotice | Seromycin;
  • (LV) Latvia: Cycloserin | Seromycin;
  • (MY) Malaysia: Coxerin;
  • (NO) Norway: Cicloserina specific;
  • (PE) Peru: Cicloserina | Neoseryn;
  • (PK) Pakistan: Cyclocin | Cyclosen | Xerine;
  • (PL) Poland: Cicloserina | Coxerin | Cyclorine | Seromycin;
  • (PR) Puerto Rico: Seromycin;
  • (RO) Romania: Cicloserina antibiotice | Helpocerin;
  • (RU) Russian Federation: Coxerin | Cyclorine | Cycloserin | Cycloserin ferein | Cycloserine ferein | Kansamin | Myser | Myzer;
  • (SG) Singapore: Seromycin;
  • (SI) Slovenia: Seromycin;
  • (TH) Thailand: Hawon Cycloserine | Proserine;
  • (TR) Turkey: Seromycin | Siklocap;
  • (TW) Taiwan: Cyclocin;
  • (UA) Ukraine: Coxerin | Helposerin;
  • (UG) Uganda: Coxerin
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