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. |
| Molecular Weight | 296.4 |
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 | Insufficient human data; animal studies show teratogenicity. Avoid in first trimester. |
| 2nd trimester | Use only if benefit outweighs risk; potential for fetal harm based on animal data. |
| 3rd trimester | Avoid near term; may cause neonatal withdrawal or respiratory depression. |
Clinical note
Comprehensive clinical and safety monograph for TRICHLORMAS (TRICHLORMAS).
| Placental transfer | Crosses placenta; detected in fetal circulation. |
| Breastfeeding | Excreted in breast milk in low amounts; monitor infant for sedation or feeding difficulties. Use caution. |
| Lactation Rating | L3 - Moderately Safe |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to chloral derivativesSevere hepatic or renal impairmentMarked cardiac disease (e.g., severe arrhythmias)History of substance abuseConcomitant use with alcohol or CNS depressants
| 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. |
| Food/Dietary | Avoid alcohol and grapefruit juice. High-fat meals may delay absorption. No specific food restrictions otherwise. |
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| 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. |
| 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. |
| Clinical Pearls | TRICHLORMAS is a sedative-hypnotic agent; avoid concurrent use with other CNS depressants. Monitor for respiratory depression, especially in elderly or debilitated patients. Tolerance and dependence may develop with prolonged use; prescribe lowest effective dose for shortest duration. Abrupt discontinuation may cause rebound insomnia or withdrawal symptoms. |
| Patient Advice | Take exactly as prescribed; do not increase dose or duration without consulting your doctor. · Avoid alcohol and other sedatives while taking this medication. · Do not drive or operate machinery until you know how this drug affects you. · Do not stop taking suddenly; dose may need gradual reduction to avoid withdrawal. · Store in a safe place away from children and pets. |