Telazine

• Approved Indications:
• Treatment of schizophrenia and other psychotic disorders.
• Management of short-term psychomotor agitation and anxiety associated with psychotic conditions.
• Adjunct therapy for severe anxiety and agitation unresponsive to other treatments.
• Treatment of nausea and vomiting (off-label and less common use).
• Off-label Uses:
• Control of behavioral disturbances in dementia (used cautiously).
• Management of treatment-resistant anxiety disorders in select cases.

• Adults:
• Initial dose: 1–2 mg two or three times daily.
• Maintenance dose: Typically 5–15 mg daily, divided doses.
• Maximum dose: Usually not exceeding 40 mg/day in divided doses.
• Dose adjustment depends on clinical response and tolerability.
• Elderly:
• Start at lower doses (e.g., 0.5–1 mg two or three times daily) with careful titration.
• Increased sensitivity to side effects necessitates cautious dosing.
• Pediatrics:
• Use only if clearly needed; dosing individualized by weight and clinical condition, generally starting very low (e.g., 0.5 mg/day).
• Special Populations:
• Hepatic impairment: Use with caution; dose adjustment may be required.
• Renal impairment: No specific dose adjustment but monitor closely.
• Administration Route:
• Oral tablets, usually administered with or after meals to reduce gastrointestinal upset.

Trifluoperazine is a typical antipsychotic belonging to the phenothiazine class. It primarily acts by antagonizing dopamine D2 receptors in the brain’s mesolimbic and mesocortical pathways, reducing dopaminergic neurotransmission which is implicated in psychosis. It also exhibits antagonistic effects at alpha-adrenergic and serotonergic receptors, contributing to its sedative and antiemetic properties. By modulating these neurotransmitter systems, trifluoperazine alleviates positive symptoms of schizophrenia such as hallucinations and delusions and reduces anxiety and agitation.

• Absorption: Well absorbed orally with peak plasma concentrations reached in 2–4 hours.
• Bioavailability: Approximately 90%.
• Distribution: Widely distributed; crosses the blood-brain barrier and placenta; extensively binds to plasma proteins.
• Metabolism: Extensively metabolized in the liver by cytochrome P450 enzymes (primarily CYP3A4 and CYP2D6).
• Active Metabolites: Some metabolites retain pharmacological activity.
• Elimination: Primarily excreted via bile and feces; minor renal excretion.
• Half-life: Approximately 10–20 hours, allowing once or twice daily dosing.

• Pregnancy:
• FDA pregnancy category C.
• Use only if potential benefit justifies potential risk to fetus. Animal studies show adverse effects; human data are limited.
• Lactation:
• Excreted in breast milk in small amounts.
• Caution advised; breastfeeding is not generally recommended during treatment due to potential effects on the infant.

• Primary Class: Typical antipsychotic (first-generation antipsychotic)
• Subclass: Phenothiazine derivative

• Known hypersensitivity to trifluoperazine or other phenothiazines.
• Severe central nervous system depression or coma.
• Bone marrow suppression or severe hematologic disorders.
• Severe cardiovascular disease (e.g., QT prolongation, arrhythmias).
• Parkinson’s disease or severe CNS depression.
• Use with caution or avoid with drugs prolonging QT interval.

• Risk of extrapyramidal symptoms (EPS), including dystonia, akathisia, parkinsonism, and tardive dyskinesia; monitor closely.
• Neuroleptic malignant syndrome (NMS): Rare but potentially fatal; discontinue drug immediately if suspected.
• Risk of QT prolongation and cardiac arrhythmias; ECG monitoring recommended in at-risk patients.
• May cause orthostatic hypotension; monitor blood pressure especially in elderly or debilitated patients.
• Caution in patients with seizure disorders, hepatic or renal impairment.
• Use with caution in elderly patients with dementia-related psychosis due to increased mortality risk.
• Monitor for signs of hyperprolactinemia (e.g., galactorrhea, gynecomastia).

• Common Adverse Effects:
• Central Nervous System: Sedation, dizziness, headache, extrapyramidal symptoms.
• Gastrointestinal: Dry mouth, constipation, nausea.
• Cardiovascular: Orthostatic hypotension, tachycardia.
• Endocrine: Elevated prolactin levels.
• Serious and Rare Side Effects:
• Neuroleptic malignant syndrome (NMS).
• Tardive dyskinesia (may be irreversible).
• Severe allergic reactions (rash, anaphylaxis).
• Agranulocytosis or leukopenia (rare).
• QT interval prolongation leading to arrhythmias.

• CYP450 Interactions: Metabolized by CYP3A4 and CYP2D6; inhibitors (e.g., ketoconazole, fluoxetine) may increase plasma levels; inducers (e.g., rifampin) may reduce efficacy.
• Additive CNS depressant effects with alcohol, benzodiazepines, and other CNS depressants.
• Increased risk of QT prolongation with other drugs affecting cardiac conduction (e.g., antiarrhythmics, certain antibiotics).
• Anticholinergic drugs may increase risk of side effects.
• Dopaminergic agents (e.g., levodopa) may have reduced efficacy.

• No significant recent changes in approved indications.
• Ongoing emphasis on cautious use due to side effect profile, particularly EPS and cardiac risks.
• Guidelines recommend careful monitoring of metabolic, neurologic, and cardiac parameters during therapy.
• Use in elderly dementia patients continues to carry warnings due to increased mortality risk.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep container tightly closed.
• Keep out of reach of children.
• No special handling such as refrigeration or shaking is required.