aside from [15:<30 mL/minute or undergoing hemodialysis. 106 Cautions for Ethionamide Contraindications Known hypersensitivity to ethionamide or any ingredient in the formulation. 127 Severe hepatic impairment. 127 Warnings/Precautions General Precautions Hepatic Effects Hepatitis (with or without jaundice) reported. 127 Transient increases in serum bilirubin, AST, and ALT have occurred. 127 Determine serum AST and ALT concentrations at baseline and at monthly intervals. 106 127 If AST or ALT concentrations become elevated, temporarily discontinue ethionamide and concomitant antituberculosis drugs until laboratory abnormalities resolve. 127 Reintroduce ethionamide and concomitant antituberculosis drugs sequentially to determine which drug(s) are responsible for hepatotoxicity. 127 Diabetes Mellitus Measure blood glucose at baseline and periodically during therapy. 127 Use caution in diabetic patients; 127 must be particularly alert for episodes of hypoglycemia. 127 Nervous System and Ophthalmic Effects Psychotic disturbances (including mental depression), drowsiness, dizziness, restlessness, headache, and postural hypotension reported. 127 Peripheral neuritis, diplopia, optic neuritis, blurred vision, and a pellagra-like syndrome reported rarely. 127 Perform ophthalmic evaluations (including ophthalmoscopy) at baseline and periodically during therapy. 127 Manufacturer recommends concomitant use of pyridoxine (vitamin B 6 ) to prevent or relieve neurotoxic effects. 127 Hypothyroidism Hypothyroidism (with or without goiter) reported. 127 Monitor thyroid function. 127 Some experts recommend determining thyroid-stimulating hormone (TSH) concentrations at baseline and at monthly intervals. 106 Precautions Related to Treatment of Tuberculosis Should not be used alone for treatment of TB; must be given in conjunction with other antituberculosis agents. 106 107 127 Clinical specimens for microscopic examination and mycobacterial cultures and in vitro susceptibility testing should be obtained prior to initiation of antituberculosis therapy and periodically during treatment to monitor therapeutic response. 106 127 The antituberculosis regimen should be modified as needed. 106 Patients with positive cultures after 4 months of treatment should be considered to have failed treatment (usually as the result of noncompliance or drug-resistant TB). 106 If ethionamide is added as a new drug to a regimen in patients experiencing treatment failure who have proven or suspected drug-resistant TB, at least 2 (preferably 3) new drugs known or expected to be active against the resistant strain should be added at the same time. 106 Compliance with the full course of antituberculosis therapy and all drugs included in the multiple-drug regimen is critical. 106 Missed doses increase the risk of treatment failure and increase the risk that M. tuberculosis will develop resistance to the antituberculosis regimen. 106 To ensure compliance, ATS, CDC, IDSA, and AAP recommend that directly observed (supervised) therapy (DOT) be used for treatment of active (clinical) TB whenever possible, especially when intermittent regimens are used, when the patient is immunocompromised or infected with HIV, or when drug-resistant M. tuberculosis is involved. 106 107 Specific Populations Pregnancy Category C. 127 ATS, CDC, and IDSA state that ethionamide should not be used in pregnant women. 106 Lactation Not known whether ethionamide is distributed into milk. 127 Use with caution and only when benefits outweigh risks; carefully observe breast-fed infants for adverse effects. 127 Pediatric Use Limited data are available. 127 Manufacturer states the drug should not be used in children> <12 years of age except when TB is known to be resistant to first-line therapy and systemic dissemination of the disease or other life-threatening complications of TB are judged to be imminent. 127 Hepatic Impairment Use caution in patients with hepatic disease; 106 contraindicated in those with severe hepatic impairment. 127 Renal Impairment Dosage reduction advised. 106 (See Renal Impairment under Dosage and Administration.) Common Adverse Effects Nausea, vomiting, diarrhea, abdominal pain, excessive salivation, metallic taste, stomatitis, anorexia, weight loss. 127 Interactions for Ethionamide Specific Drugs Drug Interaction Comments Alcohol Psychotic reaction reported 127 Avoid excessive alcohol ingestion 127 Cycloserine Possible increased risk of adverse effects; seizures reported 127 Use concomitantly with caution 127 Isoniazid Increased isoniazid concentrations 127 Use concomitantly with caution 127 Ethionamide Pharmacokinetics Absorption Bioavailability Essentially completely absorbed following oral administration; does not undergo any appreciable first-pass metabolism. 127 Peak plasma concentrations attained within about 1 hour. 127 Peak plasma concentrations are higher and attained more quickly with ethionamide film-coated tablets (Trecator ) than with the previously available sugar-coated tablets (Trecator -SC); AUC is similar for both preparations. 128 Distribution Extent Studies using sugar-coated tablets (Trecator -SC; no longer commercially available in the US) indicate ethionamide is rapidly and widely distributed into body tissues and fluids and concentrations in plasma and various organs are approximately equal. 127 Although studies have not been performed to date with ethionamide film-coated tablets (Trecator ), distribution of the drug is expected to be the same as that reported with the sugar-coated tablets. 127 CSF concentrations may be equal to concurrent plasma concentrations. 106 Crosses placenta. 106 Not known whether ethionamide is distributed into milk. 127 Plasma Protein Binding 30%. 127 Elimination Metabolism Metabolized to active and inactive metabolites in the liver. 127 Elimination Route Less than 1% of an oral dose is excreted in urine 127 as active drug and metabolites; a the remainder is excreted in urine as inactive metabolites. a Only low concentrations removed by hemodialysis. 106 129 Half-life 1.9 3 hours. 127 129 a Stability Storage Oral Tablets 20 25 C in a tight container. 127 Actions and Spectrum Bactericidal or bacteriostatic in action. 127 b d Appears to inhibit peptide synthesis in susceptible organisms. 127 Like isoniazid, ethionamide inhibits mycolic acid synthesis in susceptible organisms. d May form covalent adducts with nicotinamide adenine dinucleotide (NAD). d A highly specific agent; active only against Mycobacterium . a Active against M. tuberculosis , a b d M. bovis , a M. kansasii , 113 a and M. malmoense . 113 Some strains of M. avium complex (MAC) may be susceptible, a b c but high concentrations may be required. c Also active against M. leprae . a d Natural and acquired resistance to ethionamide demonstrated in vitro and in vivo in strains of M. tuberculosis. a Cross-resistance may occur between ethionamide and isoniazid or thiosemicarbazones such as thiacetazone (drugs not commercially available in the US). 127 No evidence of cross-resistance between ethionamide and aminosalicylic acid, cycloserine, or streptomycin. 127 Advice to Patients Advise patients that poor compliance with antituberculosis regimens can result in treatment failure and development of drug-resistant TB, which can be life-threatening and lead to other serious health risks. 106 127 Importance of completing full course of therapy; importance of not missing any doses. 127 Importance of informing clinicians of any change in visual acuity (with or without eye pain). 127 Importance of avoiding excessive alcohol consumption. 127 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses. 127 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 127 Importance of informing patients of other important precautionary information. 127 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Ethionamide Routes Dosage Forms Strengths Brand Names Manufacturer Oral Tablets, film-coated 250 mg Trecator (with povidone) Wyeth AHFS DI Essentials. Copyright 2017, Selected Revisions February 1, 2008. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. Use is not currently included in the labeling approved by the US Food and Drug Administration. References 100. Drucker D, Eggo MC, Salit IE et al. Ethionamide-induced goitrous hypothyroidism. Ann Intern Med . 1984; 100:837-9. [PubMed 6721300] 101. Gupta DK. Acceptability of thioamides. I. Ethionamide. J Postgrad Med . 1977; 23:175-80. [PubMed 615264] 102. Moulding T, Fraser R. Hypothyroidism related to ethionamide. Am Rev Respir Dis . 1970; 101:90-4. [PubMed 5410078] 103. Schless JM, Allison RF, Inglis RM et al. The use of ethionamide in combined drug regimens in the re-treatment of isoniazid resistant pulmonary tuberculosis. Am Rev Respir Dis . 1965; 91:728-37. [PubMed 14280946] 104. Report of a WHO Study Group. Chemotherapy of leprosy for control programmes. Technical Report Series No. 675. Geneva: World Health Organization; 1982:3-33. 105. Jacobson RR. Treatment. In: Hastings RC, ed. Leprosy. New York: Churchill Livingstone; 1985:193-222. 106. Centers for Disease Control and Prevention. Treatment of tuberculosis, American Thoracic Society, CDC, and Infectious Diseases Society of America. MMWR Recomm Rep . 2003; 52(RR-11):1-77. 107. American Academy of Pediatrics. 2006 Red Book: Report of the Committee on Infectious Diseases. 27th ed. Elk Grove Village, IL: American Academy of Pediatrics; 2006. 110. Donald PR, Seifart HI. Cerebrospinal fluid concentrations of ethionamide in children with tuberculous meningitis. J Pediatr . 1989; 115:483-6. [PubMed 2769511] 113. Griffith DE, Aksamit T, Brown-Elliott BA et al. An official ATS/IDSA statement: diagnosis, treatment, and prevention of nontuberculous mycobacterial diseases. Am J Respir Crit Care Med . 2007; 175:367-416. [PubMed 17277290] 114. Reviewers comments (personal observations) on the Antituberculosis Agents General Statement 8:16.04. 115. Wyeth. Trecator -SC (ethionamide) sugar-coated tablets prescribing information. Philadelphia, PA; 2002 Mar 14. 116. WHO Expert Committee on Leprosy. Seventh Report. WHO Technical Report Series No. 874. Geneva: World Health Organization; 1998:1-43. 117. Whitty CJ, Lockwood DN. Leprosy new perspectives on an old disease. J Infect . 1999; 38:2-5. [PubMed 10090496] 118. Jacobson RR, Krahenbuhl JL. Leprosy. Lancet . 1999; 353:655-60. [PubMed 10030346] 119. MacDougall AC, Ulrich MI. Mycobacterial Disease: Leprosy. In: Fitzpatrick TB, Eisen AZ, Wolff K et al, eds. Dermatology in General Medicine, 4th ed. New York, NY: McGraw -Hill Inc; 1993:2395-2410. 120. Panda S. Let s learn some clinical facts on leprosy - before it is eradicated. Bull on Drug Health Information (India) . 1998; 5:5-12. 121. Anon. Choice of antibacterial drugs. Med Lett Treat Guid . 2004; 2:18-26. 122. Anon. Essential drugs. WHO Model Formulary. Antibacterials. Antileprosy Drugs. WHO Drug Information . 1997; 11:253. 123. WHO Study Group on Chemotherapy of Leprosy. Seventh Report. WHO Technical Report Series No. 847. Geneva: World Health Organization; 1994:1-24. 124. WHO. Action Programme for the elimination of leprosy (LEP). From WHO Website () 1999 Sept 23. 125. WHO. Reports on individual drugs. Simplified treatment for leprosy. WHO Drug Information . 1997; 11:131. 126. Single-lesion multicentre trial group. Efficacy of single-dose multidrug therapy for the treatment of single-lesion paucibacillary leprosy. Indian J Leprosy . 1997; 69:121-9. 127. Wyeth. Trecator (ethionamide) tablets prescribing information. Philadelphia, PA; 2006 Sept. 128. Tucker HR. Dear healthcare provider letter regarding reformulation of Trecator -SC (ethionamide sugar-coated tablets). Philadelphia, PA: Wyeth Pharmaceuticals; 2005 Mar 10. 129. Malone RS, Fish DN, Spiegel DM et al. The effect of hemodialysis on cycloserine, ethionamide, para-aminosalicylate, and clofazimine. Chest . 1999; 116:984-90. [PubMed 10531163] a. AHFS Drug Information 2007. McEvoy GK, ed. Ethionamide. American Society of Health-System Pharmacists; 2007:552-4. b. Heifets LB, Lindholm-Levy JP, Flory M. Comparison of bacteristatic and bactericidal activity of isoniazid and ethionamide against Mycobacterium avium and Mycobacterium tuberculosis . Am Rev Respir Dis . 1991; 143:268-70. [PubMed 1899326] c. Rastogi N, Bauriaud RM, Bourgoin A et al. French multicenter study involving eight test sites for radiometric determination of activities of 10 antimicrobial agents against Mycobacterium avium complex. Antimicrob Agents Chemother . 1995; 39:638-44. [PubMed 7793865] d. Wang F, Langley R, Gulten G et al. Mechanism of thioamide drug action against tuberculosis and leprosy. J Exp Med . 2007; 204:73-8. [PubMed 17227913] e. Centers for Disease Control and Prevention. Treating opportunistic infections among HIV-infected adults and adolescents: recommendations from CDC, the National Institutes of Health, and the HIV Medicine Association/Infectious Diseases Society of America. MMWR Recomm Rep . 2004; 53(RR-15):1-112. f. Centers for Disease Control and Prevention. Treating opportunistic infections among HIV-exposed and infected children: recommendations from CDC, the National Institutes of Health, and the Infectious Diseases Society of America. MMWR Recomm Rep . 2004; 53(RR-14):1-92. Next Interactions Print this page Add to My Med List More about ethionamide Side Effects During Pregnancy or Breastfeeding Dosage Information Drug Interactions Support Group En Español 0 Reviews Add your own review/rating Drug class: nicotinic acid derivatives Consumer resources Ethionamide Ethionamide (Advanced Reading) Professional resources Ethionamide (Wolters Kluwer) Other brands: Trecator Related treatment guides Tuberculosis, Active> ]} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Nicotinic acid derivatives Related Drugs Tuberculosis, Active ciprofloxacin , Levaquin , levofloxacin , rifampin , moxifloxacin , Avelox , isoniazid , ethambutol , amikacin , gatifloxacin , streptomycin , pyrazinamide , Floxin , Rifadin , Amikin , Myambutol , cycloserine , Tequin , isoniazid / pyrazinamide / rifampin , rifapentine , kanamycin , Rifamate , More... 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