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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TARACTAN (TARACTAN).
| Breastfeeding | Chlorprothixene is excreted in breast milk. M/P ratio not established. Limited data; risk of sedation, irritability, or poor feeding in infant. Use caution and monitor infant for adverse effects. Consider alternative if possible. |
| 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. |
■ FDA Black Box Warning
Increased mortality in elderly patients with dementia-related psychosis.
| Serious Effects |
["Comatose states","CNS depression (alcohol, barbiturates, narcotics)","Blood dyscrasias","Known hypersensitivity to thioxanthenes","Parkinson's disease (relative)","Severe hepatic impairment","Narrow-angle glaucoma","Prostatic hypertrophy (relative)"]
| 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"] |
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| 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. |