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Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Trecator: 250 mg [contains fd&c yellow #6 (sunset yellow)]
Brand Names: U.S.
- Antitubercular Agent
Inhibits peptide synthesis; bacteriostatic
Essentially complete absorption
Vd: 93.5 L; widely distributed into body tissues and fluids including CSF
Prodrug; extensively hepatic to active and inactive metabolites
Urine (<1% as unchanged drug; as active and inactive metabolites)
Time to Peak
Serum: ~1 hour
Use: Labeled Indications
Tuberculosis: Treatment of active tuberculosis, in combination with other antituberculosis agents, in patients with Mycobacterium tuberculosis resistant to isoniazid or rifampin, or when there is intolerance to other drugs.
Hypersensitivity to ethionamide or any component of the formulation; severe hepatic impairment
Manufacturer’s labeling: 15 to 20 mg/kg/day; initiate dose at 250 mg/day for 1 to 2 days, then increase to 250 mg twice daily for 1 to 2 days, with gradual increases to highest tolerated dose; average adult dose: 750 mg/day (maximum daily dose: 1 g/day in 3 to 4 divided doses)
Alternate dosing: 15 to 20 mg/kg/day in 1 or 2 divided doses (usually 500 to 750 mg/day; maximum daily dose: 1 g/day) (Blumberg 2003).
Refer to adult dosing.
Tuberculosis: Children and Adolescents: Oral:
Manufacturer’s labeling: 10 to 20 mg/kg/day in 2 to 3 divided doses or 15 mg/kg/day as a single daily dose.
Alternate recommendations: 15 to 20 mg/kg/day in 1 to 2 divided doses (maximum daily dose: 1,000 mg/day) (HHS OI [pediatric] 2013; WHO 2008)
Dosing: Renal Impairment
There are no dosage adjustments provided in manufacturer's labeling; however, the following adjustments for adults have been reported in the literature (Blumberg 2003; WHO 2008):
CrCl ≥30 mL/minute: No dosage adjustment necessary.
CrCl <30 mL/minute: 250 to 500 mg/day
End-stage renal disease (ESRD) on hemodialysis: 250 to 500 mg/day
Dosing: Hepatic Impairment
Mild or moderate impairment: There are no dosage adjustments provided in the manufacturer’s labeling; use with caution (Blumberg 2003)
Severe impairment: Use is contraindicated.
Directly observed therapy (DOT) is recommended. Neurotoxic effects may be prevented or relieved by the coadministration of pyridoxine (see Pyridoxine monograph for dosing). Administer with or without meals. Gastrointestinal adverse effects may be decreased by administration at meals or bedtime, decreased dose, or giving with antiemetics.
Healthcare provider may recommend an increase in dietary intake of pyridoxine to prevent neurotoxic effects of ethionamide. Avoid alcohol.
Store at 20°C to 25°C (68°F to 77°F). Keep containers tightly closed.
Alcohol (Ethyl): May enhance the adverse/toxic effect of Ethionamide. Specifically, there may be a risk for a psychotic episode/reaction. Monitor therapy
CycloSERINE: Ethionamide may enhance the adverse/toxic effect of CycloSERINE. Monitor therapy
Isoniazid: Ethionamide may increase the serum concentration of Isoniazid. Monitor therapy
Frequency not defined.
Cardiovascular: Orthostatic hypotension
Central nervous system: Altered sense of smell, depression, dizziness, drowsiness, headache, metallic taste, peripheral neuritis, psychiatric disturbance, restlessness, seizure
Dermatologic: Acne vulgaris, alopecia, purpura, skin photosensitivity, skin rash
Endocrine & metabolic: Goiter, gynecomastia, hypoglycemia, hypothyroidism, menstrual disease, pellagra (pellagra-like syndrome), weight loss
Gastrointestinal: Abdominal pain, anorexia, diarrhea, sialorrhea, nausea, stomatitis, vomiting
Hematologic & oncologic: Leukopenia, thrombocytopenia
Hepatic: Hepatitis, increased liver enzymes, increased serum bilirubin, jaundice
Hypersensitivity: Hypersensitivity reaction
Neuromuscular & skeletal: Arthralgia
Ophthalmic: Blurred vision, diplopia, optic neuritis
• Diabetes: Use with caution in patients with diabetes mellitus; may cause hypoglycemia.
• Hepatotoxicity: May cause hepatotoxicity; monitor liver function tests at baseline and monthly.
• Porphyria: Use not recommended; porphyria-inducing in animal and in vitro studies (WHO, 2008).
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction; hypothyroidism (reversible; with and without goiter) has been reported.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Appropriate use: Drug-resistant tuberculosis develops rapidly if ethionamide is used alone; must administer with other antituberculosis agents. Directly observed therapy (DOT) is recommended.
• Ethanol use: Instruct patients to avoid excessive ethanol intake; psychotic reaction may occur.
• Eye exams: Eye exams are recommended at baseline and periodically during therapy.
Baseline and monthly serum ALT and AST; baseline and periodic ophthalmic exams; periodic blood glucose and TSH
Pregnancy Risk Factor
Ethionamide crosses the placenta; teratogenic effects were observed in animal studies. Use during pregnancy is not recommended.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience abdominal pain, nausea, vomiting, diarrhea, bad taste, drooling, lack of appetite, or weight loss. Have patient report immediately to prescriber signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), burning or numbness feeling, depression, vision changes, or signs of low blood sugar (dizziness, headache, fatigue, feeling weak, shaking, a fast heartbeat, confusion, hunger, or sweating) (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about ethionamide
- Other brands: Trecator