TARACTAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TARACTAN (TARACTAN).
Thioxanthene antipsychotic; blocks postsynaptic dopamine D1 and D2 receptors in the mesolimbic system; also has anticholinergic, antihistaminergic, and alpha-adrenergic blocking effects.
| Metabolism | Hepatic metabolism primarily via CYP450 enzymes (CYP2D6, CYP3A4); major metabolite is chlorprothixene sulfoxide. |
| Excretion | Primarily hepatic metabolism; <1% excreted unchanged in urine. Metabolites eliminated renally (30%) and fecally (70%). |
| Half-life | Terminal elimination half-life is approximately 20-40 hours (mean 30 hours). Steady-state reached in 5-7 days. |
| Protein binding | Approximately 90-98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 7-20 L/kg; extensive tissue distribution with high CNS penetration. |
| Bioavailability | Oral: approximately 10-30% due to extensive first-pass metabolism; IM: 100%. |
| Onset of Action | Oral: 1-3 hours; IM: 30-60 minutes. |
| Duration of Action | Antipsychotic effect persists 6-12 hours after single oral dose; sedative effects may last 24 hours. With chronic dosing, therapeutic effects are continuous. |
| Molecular Weight | 315.86 |
Oral: 25-50 mg three times daily, increased as needed to 400-600 mg/day. IM: 12.5-25 mg every 6-8 hours.
| Dosage form | CONCENTRATE |
| Renal impairment | CrCl 10-50 mL/min: Administer 50-75% of normal dose. CrCl <10 mL/min: Administer 25-50% of normal dose. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 25-50%. Child-Pugh C: Avoid use or reduce by 75%. |
| Pediatric use | Not recommended for children under 6 years. For children 6-12 years: 10-25 mg orally 2-4 times daily. Dosage based on weight: 0.5-2 mg/kg/day in divided doses. |
| Geriatric use | Initial dose: 10-25 mg orally 2-3 times daily; increase gradually. Use lower end of dosing range due to increased sensitivity and risk of anticholinergic effects. |
| 1st trimester | Avoid due to teratogenic effects (e.g., cardiovascular malformations) in animal studies and limited human data. |
| 2nd trimester | Avoid unless essential; may cause extrapyramidal symptoms or jaundice in neonate. |
| 3rd trimester | Avoid; risk of neonatal extrapyramidal symptoms, jaundice, and prolonged QT syndrome in neonate. |
Clinical note
Comprehensive clinical and safety monograph for TARACTAN (TARACTAN).
| Placental transfer | Chlorprothixene crosses the placenta; detectable in fetal plasma at concentrations similar to maternal plasma. Animal studies show placental transfer and potential fetal effects. |
| Breastfeeding | Chlorprothixene is excreted in breast milk in low concentrations (milk-to-plasma ratio ~0.5-1.0). Monitor infant for drowsiness, poor feeding, or extrapyramidal symptoms. Generally compatible with breastfeeding if benefits outweigh risks; use lowest effective dose. |
■ FDA Black Box Warning
Increased mortality in elderly patients with dementia-related psychosis.
| Serious Effects |
Known hypersensitivity to chlorprothixene or other thioxanthenesComatose states or severe CNS depressionHistory of agranulocytosis due to phenothiazine-like drugsConcurrent use of high-dose CNS depressants (e.g., barbiturates, alcohol)
| Precautions | Neuroleptic malignant syndrome (NMS), Tardive dyskinesia, QT prolongation and risk of arrhythmias, Seizure threshold lowering, Orthostatic hypotension, Sedation and impaired cognitive function, Anticholinergic effects (urinary retention, constipation, blurred vision), Hyperprolactinemia, Leukopenia/neutropenia, Photosensitivity, Concomitant use with other CNS depressants, Avoid abrupt withdrawal |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase blood levels of chlorprothixene. Limit caffeine intake as it can worsen agitation or insomnia. Avoid alcohol and marijuana due to additive sedation. |
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| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Taractan (chlorprothixene) is an antipsychotic. Data on fetal risks are limited. First trimester: potential for malformations based on animal studies; human data insufficient. Second/third trimester: risk of extrapyramidal symptoms and/or withdrawal in neonates after third trimester exposure. Avoid unless clearly needed. |
| Fetal Monitoring | Monitor maternal blood pressure, liver function, and CBC. For fetus: serial ultrasound for growth and anatomy if used in first trimester; neonatal assessment for extrapyramidal symptoms, sedation, and withdrawal signs. |
| Fertility Effects | Chlorprothixene may cause hyperprolactinemia, leading to menstrual irregularities, anovulation, and reduced fertility. Reversible upon discontinuation. |
| Clinical Pearls | TARACTAN (chlorprothixene) is a low-potency first-generation antipsychotic with strong sedative and anticholinergic effects. Monitor for orthostatic hypotension, especially during dose titration. Due to high sedation, it is often used for agitation in acute psychosis but avoid in elderly with dementia-related psychosis due to increased mortality risk. Can prolong QTc interval; obtain baseline ECG and monitor electrolytes. Taper slowly to avoid withdrawal dyskinesia. |
| Patient Advice | This medication may cause drowsiness; avoid driving or operating heavy machinery until you know how it affects you. · Rise slowly from sitting or lying down to prevent dizziness from low blood pressure. · Avoid alcohol and other central nervous system depressants. · Report any unusual movements of the face, tongue, or jaw, or a fast or irregular heartbeat. · May cause dry mouth; use sugarless candy or ice chips for relief. |