Cycloserine

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Cycloserine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gloria Picoy [2]

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Overview

Cycloserine is an antitubercular that is FDA approved for the treatment of active pulmonary and extrapulmonary tuberculosis and in the treatment of acute urinary tract infections caused by susceptible strains of gram positive and gram negative bacteria. Common adverse reactions include confusion, dizziness, headache and somnolence.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

  • 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.
  • Dosage: initial, 250 mg, oral, every 12 h for 2 weeks, then as tolerated to 250 mg every 6 to 8 h; MAX 1 g daily


  • Dosage: 15 to 20 mg/kg; MAX 1 gram daily

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Cycloserine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Cycloserine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

  • 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.
  • Dosage: 10 to 20 mg/kg/day ORALLY (divide every 12 h)

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Cycloserine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Cycloserine in pediatric patients.

Contraindications

Administration is contraindicated in patients with any of the following:

Warnings

Adverse Reactions

Clinical Trials Experience

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:

  • Nervous system symptoms (which appear to be related to higher dosages of the drug, i.e., more than 500 mg daily)


  • Cardiovascular


  • Allergy (apparently not related to dosage)


  • Miscellaneous

Postmarketing Experience

There is limited information regarding Cycloserine Postmarketing Experience in the drug label.

Drug Interactions

  • 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.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C A study in 2 generations of rats given doses up to 100 mg/kg/day demonstrated no teratogenic effect in offspring. It is not known whether cycloserine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Cycloserine should be given to a pregnant woman only if clearly needed.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Cycloserine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Cycloserine during labor and delivery.

Nursing Mothers

A study in 2 generations of rats given doses up to 100 mg/kg/day demonstrated no teratogenic effect in offspring. It is not known whether cycloserine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Cycloserine should be given to a pregnant woman only if clearly needed.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatic Use

There is no FDA guidance on the use of Cycloserine in geriatric settings.

Gender

There is no FDA guidance on the use of Cycloserine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Cycloserine with respect to specific racial populations.

Renal Impairment

Blood levels should be determined at least weekly for patients with reduced renal function, for individuals receiving a daily dosage of more than 500 mg, and for those showing signs and symptoms suggestive of toxicity. The dosage should be adjusted to keep the blood level below 30 μg/mL.

Hepatic Impairment

There is no FDA guidance on the use of Cycloserine in patients with hepatic impairment.

Females of Reproductive Potential and Males

  • 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.

Immunocompromised Patients

There is no FDA guidance one the use of Cycloserine in patients who are immunocompromised.

Administration and Monitoring

Administration

Oral

Monitoring

  • Doses monitored by blood levels.
  • Blood levels should be determined at least weekly for patients with reduced renal function, for individuals receiving a daily dosage of more than 500 mg, and for those showing signs and symptoms suggestive of toxicity.

IV Compatibility

There is limited information regarding the compatibility of Cycloserine and IV administrations.

Overdosage

  • Acute toxicity from cycloserine can occur if more than 1 g is ingested by an adult. Chronic toxicity from cycloserine is dose related and can occur if more than 500 mg is administered daily.
  • Patients with renal impairment will accumulate cycloserine and may develop toxicity if the dosing regimen is not modified. Patients with severe renal impairment should not receive the drug.
  • The central nervous system is the most common organ system involved with toxicity. Toxic effects may include headache, vertigo, confusion, drowsiness, hyperirritability, paresthesias, dysarthria and psychosis.
  • Following larger ingestions, paresis, convulsions, and coma often occur.
  • Ethyl alcohol may increase the risk of seizures in patients receiving cycloserine.
  • The oral median lethal dose in mice is 5290 mg/kg.


Treatment
  • To obtain up–to–date information about the treatment of overdose, a good resource is your certified Regional Poison Control Center. Telephone numbers of certified poison control centers are listed in the Physicians’ Desk Reference (PDR).
  • In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in your patient.
  • In adults, many of the neurotoxic effects of cycloserine can be both treated and prevented with the administration of 200 to 300 mg of pyridoxine daily.
  • The use of hemodialysis has been shown to remove cycloserine from the bloodstream. This procedure should be reserved for patients with life-threatening toxicity that is unresponsive to less invasive therapy.

Pharmacology

Template:Px
Cycloserine
Systematic (IUPAC) name
(R)-4-Amino-1,2-oxazolidin-3-one
Identifiers
CAS number 68-41-7
ATC code J04AB01
PubChem 6234
DrugBank DB00260
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 102.092 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability ~70% to 90%
Metabolism Hepatic
Half life 10 hrs (normal renal function)
Excretion Renal
Therapeutic considerations
Licence data

US

Pregnancy cat.

C

Legal status

[[Prescription drug|Template:Unicode-only]](US)

Routes ?

Mechanism of Action

Cycloserine inhibits cell–wall synthesis in susceptible strains of gram–positive and gram–negative bacteria and in Mycobacterium tuberculosis.

Structure

The molecular weight of cycloserine is 102.09, and it has an empirical formula of C3H6N2O2.

Pharmacodynamics

There is limited information regarding Cycloserine Pharmacodynamics in the drug label.

Pharmacokinetics

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.

Nonclinical Toxicology

Carcinogenesis and Mutagenicity

  • Studies have not been performed to determine potential for carcinogenicity.
  • The Ames test and unscheduled DNA repair test were negative.

Clinical Studies

There is limited information regarding Cycloserine Clinical Studies in the drug label.

How Supplied

Cycloserine is available as a 250 mg capsule

  • Bottles of 40 capsules
  • NDC 13845-1201-3

Storage

Store at 20° to 25°C (68° to 77°F)

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Cycloserine Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Cycloserine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

There is limited information regarding Cycloserine Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. "FDA LABEL: CYCLOSERINE - cycloserine capsule".

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