TRICHLORMAS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRICHLORMAS (TRICHLORMAS).
TRICHLORMAS is a sedative-hypnotic agent. Its mechanism of action is not fully understood but is believed to involve potentiation of GABAergic inhibition in the central nervous system, similar to other chloral derivatives. It is metabolized to trichloroethanol, which is the active hypnotic compound.
| Metabolism | Hepatic metabolism via alcohol dehydrogenase and aldehyde dehydrogenase to trichloroethanol (active) and trichloroacetic acid. Further glucuronidation of trichloroethanol. |
| Excretion | Primarily renal via glomerular filtration and tubular secretion; about 70-80% of the dose excreted unchanged in urine within 24 hours. The remainder is metabolized to trichloroethanol (active) and trichloroacetic acid; these metabolites are also eliminated renally. |
| Half-life | Terminal elimination half-life is approximately 8-11 hours for the parent drug in adults with normal renal function. In patients with hepatic impairment, half-life may be prolonged up to 30 hours; in severe renal impairment, half-life of metabolites may increase significantly. |
| Protein binding | Approximately 35-40% bound to plasma proteins, primarily albumin. The binding is reversible and saturable at high concentrations. |
| Volume of Distribution | Vd is about 0.4-0.6 L/kg. This indicates distribution throughout total body water and rapid tissue uptake, including the brain and placenta. |
| Bioavailability | Oral: Rapidly and completely absorbed with bioavailability approaching 100%. Rectal: Not available for this drug. |
| Onset of Action | Oral: Onset of hypnosis occurs within 15-30 minutes. Intravenous: Sedative effects appear within 5-10 minutes. The onset is rapid due to high lipid solubility. |
| Duration of Action | Hypnotic/sedative effects: 5-8 hours after oral administration. Clinical duration is prolonged in patients with hepatic or renal dysfunction due to accumulation of active metabolites. |
500 mg orally once daily at bedtime, increased as needed to a maximum of 1 g per day in divided doses; for insomnia, 1-2 g orally at bedtime.
| Dosage form | TABLET |
| Renal impairment | GFR 10-50 mL/min: reduce dose by 50%; GFR <10 mL/min: not recommended. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use. |
| Pediatric use | Children 6-12 years: 250 mg orally at bedtime; may increase to 500 mg if needed. Not recommended for children under 6 years. |
| Geriatric use | Start at lowest effective dose (250 mg orally at bedtime) due to increased sensitivity; monitor for confusion and falls. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRICHLORMAS (TRICHLORMAS).
| Breastfeeding | Excreted into breast milk in low amounts. M/P ratio not reported. Thiazides may suppress lactation; avoid use in breastfeeding mothers, especially during the first month postpartum. |
| Teratogenic Risk | Trichlormas (trichlormethiazide) is a thiazide diuretic. First trimester: Limited human data; animal studies show no consistent teratogenicity. Avoid if possible. Second and third trimesters: Associated with risk of neonatal thrombocytopenia, electrolyte imbalances, and hypoglycemia. Use only if clearly needed. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to trichlormas or any component of the formulation.","Marked hepatic impairment.","Severe renal impairment.","Pregnancy (especially first trimester) and lactation.","Concurrent use with alcohol or other CNS depressants.","History of narcotic or other substance abuse."]
| Precautions | ["May cause respiratory depression, especially when used with other CNS depressants.","Avoid use in patients with severe hepatic or renal impairment.","Potential for abuse and dependence; restrict use to short-term therapy.","May cause paradoxic excitement in elderly or debilitated patients.","Caution in patients with history of drug abuse or suicidal tendencies."] |
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| Fetal Monitoring |
| Monitor maternal electrolytes (sodium, potassium, chloride), renal function, blood pressure, and blood glucose. Fetal monitoring for growth restriction and neonatal bilirubin levels. |
| Fertility Effects | No known direct effects on fertility. However, electrolyte disturbances or hypotension may indirectly affect reproductive function. |