TRIFLUOPERAZINE 5

Indications

• Schizophrenia
• Other psychotic disorders

Dosage

Children: Refer to the BNF for Children for specific pediatric dosing recommendations.

Adults: Refer to the BNF for specific dosing guidelines. For initial treatment, lower doses are recommended, especially in the elderly or those with hepatic or renal impairment. Doses should be titrated according to patient response.

Mechanism of action

Trifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain, which is believed to reduce the release of hypothalamic and hypophyseal hormones. This action affects basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. The drug also increases the turnover rate of dopamine in the corpus striatum due to a neuronal feedback mechanism.

Pharmacodynamics

Trifluoperazine is effective in managing symptoms of schizophrenia and other psychotic disorders, highlighting its role in modulating dopaminergic neurotransmission. The drug's efficacy is linked to its ability to affect the dopaminergic pathways involved in mood and behavior regulation.

Pharmacokinetics

Trifluoperazine is absorbed following oral administration, with its pharmacokinetics characterized by extensive liver metabolism and variable half-life. It is primarily excreted through urine as metabolites. The drug's effects can be influenced by renal and hepatic function, necessitating dosage adjustments in patients with impairments.

Contra-indications

• CNS depression
• Comatose states
• Phaeochromocytoma

Adverse effects

• Breast abnormalities
• Hypersalivation
• Increased muscle tone
• Decreased alertness
• Anxiety
• Appetite changes
• Confusion
• Dyspnoea
• Hyponatraemia
• SIADH
• Trismus
• Urticaria
• Photosensitivity reactions
• Postural hypotension (dose-related)
• Skin reactions
• Thrombocytopenia
• Urinary hesitation
• Blurred vision
• Withdrawal syndrome
• Extrapyramidal symptoms (more frequent at doses exceeding 6mg daily)
• Acute dystonias (more common with potent first-generation antipsychotics)

Interactions

• Sulpiride
• Phenothiazines

Precautions

• Start with small doses in severe renal impairment due to increased cerebral sensitivity
• Lower initial dose in the elderly, increase gradually according to response
• Monitor for acute dystonias, especially in men and young adults

Pregnancy

Trifluoperazine should be used with caution during pregnancy. The risks and benefits must be weighed carefully.

Breast-feeding

Trifluoperazine is excreted in breast milk. Caution is advised when administered to nursing mothers.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Tablets
• Oral solution
• Injectable solution

Mechanism of action

Trifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. ...PHENOTHIAZINES, BLOCK DOPAMINE RECEPTORS & INCR TURNOVER RATE OF DOPAMINE IN CORPUS STRIATUM. INCR TURNOVER RATE IS BELIEVED TO BE RESULT OF NEURONAL FEEDBACK MECHANISM. ...OF IDENTIFIED DOPAMINERGIC NEURONS IN SUBSTANTIA NIGRA & VENTRAL TEGMENTAL AREAS. SPONTANEOUS FIRING OF THESE CELLS IS INCR... /PHENOTHIAZINES/

Pharmacodynamics

Trifluoperazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Trifluoperazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.