Trifluoperazine


Generic Medicine Info
Indications and Dosage
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.

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.

Oral
Psychoses, 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.
Special Patient Group
Debilitated patients: Initiate at a reduced dose, then gradually increased based on response and tolerability.
Hepatic Impairment
Contraindicated.
Administration
Should be taken with food. May be taken w/ food to decrease GI upset; do not take w/in 2 hr of antacids.
Contraindications
Comatose or greatly depressed states due to CNS depressants; bone marrow suppression, blood dyscrasias, phaeochromocytoma. Hepatic impairment.
Special Precautions
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.
Adverse Reactions
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, ejaculatory disorder.
Respiratory, thoracic and mediastinal disorders: Nasal congestion.
Skin and subcutaneous tissue disorders: Rash, photosensitivity reactions.
Potentially Fatal: Arrhythmias, agranulocytosis, neuroleptic malignant syndrome.
Patient Counseling Information
This drug may cause drowsiness, dizziness and visual disturbances; if affected, do not drive or operate machinery.
MonitoringParameters
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/HbA1c 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.
Overdosage
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.
Drug Interactions
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.
Food Interaction
May enhance CNS depressant effects with alcohol.
Lab Interference
May cause a false-positive result for phenylketonuria.
Action
Description: 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.
Pharmacokinetics:
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.
Chemical Structure

Chemical Structure Image
Trifluoperazine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5566, Trifluoperazine. https://pubchem.ncbi.nlm.nih.gov/compound/Trifluoperazine. Accessed Jan. 26, 2021.

Storage
Store between 20-25°C. Protect from light and moisture.
ATC Classification
N05AB06 - trifluoperazine ; Belongs to the class of phenothiazine antipsychotics with piperazine structure.
References
Anon. Trifluoperazine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/12/2020.

Apo-Trifluoperazine 1 mg & 5 mg Tablets (Pharmaforte [M] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 21/01/2021.

Buckingham R (ed). Trifluoperazine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/12/2020.

Joint Formulary Committee. Trifluoperazine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/12/2020.

Stelazine 1 mg/5 mL Syrup (Mercury Pharmaceuticals Ltd,). MHRA. https://products.mhra.gov.uk/. Accessed 21/01/2021.

Trifluoperazine 5 mg Tablets (Genetics Europe Limited). MHRA. https://products.mhra.gov.uk/. Accessed 23/12/2020.

Trifluoperazine 5 mg/5 mL Oral Solution (Focus Pharmaceuticals Limited). MHRA. https://products.mhra.gov.uk/. Accessed 21/01/2021.

Trifluoperazine Hydrochloride Tablet, Film Coated (Sandoz Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/12/2020.

Trifluoperazine Tablets 1 mg (Advanz Pharma Generics [UK] Limited). MHRA. https://products.mhra.gov.uk/. Accessed 23/12/2020.

Disclaimer: This information is independently developed by MIMS based on Trifluoperazine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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