TRECATOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRECATOR (TRECATOR).
Inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, preventing the formation of the initiation complex and causing misreading of mRNA.
| Metabolism | Hepatic via esterases and possibly amidases; metabolites are excreted renally. |
| Excretion | Renal: 70-80% as unchanged drug; fecal: <20%; biliary: minor |
| Half-life | Terminal elimination half-life: 8-12 hours in adults with normal renal function; prolonged in hepatic impairment; clinically relevant for once-daily or thrice-weekly dosing |
| Protein binding | ~50-70% bound to serum proteins (albumin) |
| Volume of Distribution | 1.5-2.0 L/kg; suggests extensive tissue distribution including cerebrospinal fluid |
| Bioavailability | Oral: ~80-90% |
| Onset of Action | Oral: 2-4 hours for bacteriostatic effect; slow bactericidal activity after several days |
| Duration of Action | 24-48 hours after single dose; steady-state reached in 3-5 days |
15-20 mg/kg/day orally once daily; maximum 1 g/day.
| Dosage form | TABLET |
| Renal impairment | CrCl <30 mL/min: reduce dose to 500 mg/day or 15 mg/kg 3 times weekly. CrCl 30-50 mL/min: reduce dose to 750 mg/day or 15 mg/kg/day. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: avoid use or reduce dose by 75% with close monitoring. |
| Pediatric use | 15-20 mg/kg/day orally once daily; maximum 1 g/day. For children <10 kg: 15 mg/kg/day. |
| Geriatric use | Start at lower end of dosing range (15 mg/kg/day) due to potential age-related renal impairment; monitor renal function and adjust per renal guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRECATOR (TRECATOR).
| Breastfeeding | Ethionamide is excreted into human breast milk; estimated infant dose is 0.5–1% of maternal weight-adjusted dose. M/P ratio not established. Monitor infant for hepatotoxicity, gastrointestinal disturbances. Weigh benefits of breastfeeding against potential risks. |
| Teratogenic Risk | Teratogenic in animals; in humans, ethionamide crosses the placenta. First trimester exposure is associated with increased risk of congenital anomalies, particularly central nervous system defects. Second and third trimester risks include low birth weight and prematurity. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to trecator or any component of the formulation","Severe hepatic impairment"]
| Precautions | ["Hepatotoxicity: can cause severe and sometimes fatal hepatitis; monitor liver function tests.","Hypersensitivity reactions: monitor for rash, fever, and eosinophilia.","Neurologic effects: peripheral neuropathy, optic neuritis; discontinue if symptoms develop.","Drug interactions: may increase levels of drugs metabolized by CYP3A4 (e.g., cyclosporine, tacrolimus)."] |
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| Fetal Monitoring | Monitor maternal liver function tests (LFTs) monthly, thyroid function tests (TSH, T4) every 1-2 months, and neurological exam for peripheral neuropathy. Fetal surveillance with ultrasound for growth and anatomy. |
| Fertility Effects | Animal studies show impaired fertility at high doses. Human data limited; may cause menstrual irregularities in women and oligospermia in men. Reversible upon discontinuation. |