Trifluoperazine

Oral
Schizophrenia
Adult: Usual dose: Initially, 2-5 mg bid, gradually increased to the usual dose range of 15-20 mg daily. Dosage is individualised and adjusted according to response and severity of the condition. In severe or resistant cases, doses of 40 mg daily may be required.
Child: 6-12 years Hospitalised or closely supervised patients: Up to 5 mg daily in divided doses. Thereafter, doses may be adjusted according to age, body, weight, and response, at intervals not less than 3 days.
Elderly: Initiate at a reduced dose, then gradually increased based on response and tolerability.
Hepatic impairment: Contraindicated.

Oral
Psychoses
Adult: Usual dose: Initially, 2-5 mg bid, gradually increased to the usual dose range of 15-20 mg daily. Dosage is individualised and adjusted according to response and severity of the condition. In severe or resistant cases, doses of 40 mg daily may be required.
Child: 6-12 years Hospitalised or closely supervised patients: Up to 5 mg daily in divided doses. Thereafter, doses may be adjusted according to age, body, weight, and response, at intervals not less than 3 days.
Elderly: Initiate at a reduced dose, then gradually increased based on response and tolerability.
Hepatic impairment: Contraindicated.

Oral
Nausea and vomiting
Adult: Usual dose: 1-2 mg bid according to response and severity of the condition. If needed, dose may be increased up to Max 6 mg daily in divided doses.
Child: As oral solution or syrup: 3-5 years Up to 1 mg daily in divided doses; 6-12 years Dose may be increased up to Max 4 mg daily in divided doses.
Elderly: Initiate at a reduced dose, then gradually increased based on response and tolerability.
Hepatic impairment: Contraindicated.

Oral
Short-term management of anxiety
Adult: Adjunct: Usual dose: 1-2 mg bid according to response and severity of the condition. If needed, dose may be increased up to Max 6 mg daily in divided doses. Max treatment duration: 12 weeks.
Child: As oral solution or syrup: 3-5 years Up to 1 mg daily in divided doses; 6-12 years Dose may be increased up to Max 4 mg daily in divided doses.
Elderly: Initiate at a reduced dose, then gradually increased based on response and tolerability.
Hepatic impairment: Contraindicated.

Special Populations: Debilitated patients: Initiate at a reduced dose, then gradually increased based on response and tolerability.

Should be taken with food.

Comatose or greatly depressed states due to CNS depressants; bone marrow suppression, blood dyscrasias, phaeochromocytoma. Hepatic impairment.

Patient with CV disease (e.g. arrhythmia, angina pectoris), hypovolaemia, diabetes, decreased gastrointestinal motility, paralytic ileus, urinary retention, benign prostatic hyperplasia, xerostomia, visual problems (e.g. narrow-angle glaucoma); predisposition to aspiration pneumonia (e.g. Alzheimer's disease), risk factors for blood dyscrasias (e.g. history of drug-induced leucopenia/neutropenia, pre-existing low WBC); myasthenia gravis, Parkinson's disease, cerebrovascular disease, history of seizures, epilepsy, previous brain damage, alcoholism. Patient subjected to dehydration, strenuous exercise, and extreme heat exposure. Discontinue at least 48 hours prior to myelography and do not resume for at least 24 hours postprocedure. Avoid use in the control of nausea and vomiting occurring before myelography or postprocedure with metrizamide. Not approved for the treatment of dementia-related psychosis. Avoid abrupt withdrawal. Debilitated patients. Children and elderly. Pregnancy and lactation. Patient Counselling This drug may cause drowsiness, dizziness and visual disturbances; if affected, do not drive or operate machinery. Monitoring Parameters Monitor vital signs, mental status, and CBC as necessary; electrolytes and LFTs annually then as clinically indicated; weight, height, BMI, and waist circumference at baseline, every visit for the 1st 6 months, then quarterly with stable dose; fasting plasma glucose level/HbA_1c and lipid panel at baseline and as clinically indicated. Monitor for abnormal involuntary movements or parkinsonian signs, tardive dyskinesia, and visual changes. Perform ocular examination.

Significant: Anticholinergic effects (e.g. constipation, xerostomia, blurred vision, urinary retention), blood dyscrasias (e.g. leucopenia, neutropenia, thrombocytopenia, anaemia, pancytopenia); oesophageal dysmotility or aspiration, CNS depression, falls; extrapyramidal symptoms (e.g. pseudoparkinsonism, acute dystonic reactions, akathisia, tardive dyskinesia); liver damage, cholestatic jaundice; hyperprolactinaemia, pigmentary retinopathy, lenticular and corneal deposits (prolonged use), orthostatic hypotension, venous thromboembolism, impaired core body temperature regulation, lowered seizure threshold; may mask toxicity of other conditions (e.g. brain tumour, Reye's syndrome, intestinal obstruction) due to its antiemetic effects. Eye disorders: Corneal changes, lens disease. Gastrointestinal disorders: Nausea, vomiting, constipation, stomach pain. General disorders and administration site conditions: Fatigue. Investigations: Increased weight. Metabolism and nutrition disorders: Anorexia, hyperglycaemia. Musculoskeletal and connective tissue disorders: Muscle weakness. Nervous system disorders: Drowsiness, dizziness, headache. Psychiatric disorders: Insomnia, agitation. Renal and urinary disorders: Difficulty in micturition, urinary retention. Reproductive system and breast disorders: Change in libido, galactorrhoea, gynaecomastia, amenorrhoea, ejactulatory disorder. Respiratory, thoracic and mediastinal disorders: Nasal congestion. Skin and subcutaneous tissue disorders: Rash, photosensitivity reactions.
Potentially Fatal: Arrhythmias, agranulocytosis, neuroleptic malignant syndrome.

Symptoms: Extrapyramidal signs, hypotension, dry mouth, ileus, CNS depression leading to somnolence or coma, agitation, restlessness, convulsion, ECG changes, and cardiac arrhythmias. Management: Supportive and symptomatic treatment. Perform gastric lavage and maintain airways. To treat extrapyramidal symptoms, administer anti-Parkinsonism drugs, barbiturates or diphenhydramine. Take caution to avoid enhancing respiratory depression. Provide fluid replacement to treat hypotension; if necessary, vasoconstrictors (e.g. norepinephrine, phenylephrine) may be considered for persistent or severe hypotension.

May potentiate the effects of antihypertensives, anticholinergics, and antidepressants. May enhance the CNS depressant effects with sedatives, hypnotics, anaesthetics, and strong analgesics. May antagonise the activity of epinephrine, clonidine, guanethidine and levodopa. May diminish the therapeutic efficacy of oral anticoagulants. Increased risk of severe extrapyramidal effects and neurotoxicity with lithium. May decrease absorption with antacids.

May enhance CNS depressant effects with alcohol.

May cause a false-positive result for phenylketonuria.

Trifluoperazine is a piperazine phenothiazine antipsychotic that blocks the dopamine D₂ receptors in the nigrostriatal and mesolimbic areas of the brain. It also possesses anxiolytic and antiemetic activities.
Absorption: Readily absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1.5-6 hours.
Distribution: Widely distributed in the body. Crosses the blood-brain barrier. Enters breast milk.
Metabolism: Metabolised in the liver to form N-desmethyltrifluoperazine, 7-hydroxy derivative, and other metabolites. Undergoes the first-pass metabolism in the gut wall.
Excretion: Via urine and faeces (as active and inactive metabolites). Terminal elimination half-life: 22 hours.

Oral: Store between 20-25°C. Protect from light and moisture.

Antiemetics / Antipsychotics / Anxiolytics

N05AB06 - trifluoperazine ; Belongs to the class of phenothiazine antipsychotics with piperazine structure.