Drug information of Trifluoperazine

Trifluoperazine


Propylpiperazine-derivative phenothiazine ; conventional (prototypical, first-generation) antipsychotic agent.

Mechanism of effect

Precise mechanism(s) of antipsychotic action not determined, but may be principally related to antidopaminergic effects.

Pharmacodynamic

Exhibits weak anticholinergic and sedative effects and strong extrapyramidal effects and antiemetic activity and antidopaminergic effects.

Pharmacokinetics

Phenothiazines are generally well absorbed from the GI tract.Considerable interindividual variation in peak concentrations reported.Crosses the placenta.Distributed into breast milk.Phenothiazines are highly bound to plasma proteins.
Metabolic fate not fully elucidated. Appears to be extensively metabolized, principally in the liver. Phenothiazines and their metabolites are excreted in urine and feces.Half-life is 12–24 hours.

Drug indications

Schizophrenia

Dosage

Usual Adult Dose for Schizophrenia
 Initial dose: 2 to 5 mg orally 2 times a day
 Maintenance dose: 15 to 20 mg/day
 Maximum dose: 40 mg/day
 Comment :
-Most patients should reach therapeutic levels in 2 to 3 weeks.
Usual Adult Dose for Anxiety
 Recommended dose: 1 to 2 mg orally 2 times a day
 Maximum dose: 6 mg/day
 Duration of therapy: Up to 12 weeks
 Comment :
-The lowest effective dosage should be used for the shortest duration of time.
Usual Geriatric Dose for Schizophrenia
• Initial dose : 2 mg orally 2 times a day
• Maintenance dose : 15 to 20 mg/day
• Maximum dose : 40 mg/day
 Comment :
-Most patients should reach therapeutic levels in 2 to 3 weeks
Usual Geriatric Dose for Anxiety
 Initial dose : 1 mg orally 2 times a day
 Maximum dose : 6 mg/day
 Duration of therapy : Up to 12 weeks
 Comments :
-Due to the long half-life of this drug, this drug may be given as a once a day dose. -The lowest effective dosage should be used for the shortest duration of time.
Usual Pediatric Dose for Schizophrenia
6 to 12 years :
-Initial dose: 1 mg once a day OR 2 times a day
-Maintenance dose: 1 to 15 mg/day
12 years and older :
-Initial dose: 2 to 5 mg orally 2 times a day
-Maintenance dose: 15 to 20 mg/day
-Maximum dose: 40 mg/day

Alerts

• Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Trifluoperazine hydrochloride is not approved for the treatment of patients with dementia-related psychosis.
• Tardive dyskinesia, a syndrome consisting of potentially irreversible, involuntary, dyskinetic movements, may develop in patients treated with antipsychotic drugs. Although the prevalence of the syndrome appears to be highest among the elderly, especially elderly women, it is impossible to rely upon prevalence estimates to predict, at the inception of antipsychotic treatment, which patients are likely to develop the syndrome.
• A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with antipsychotic drugs. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mental status and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmias).
The management of NMS should include :
1) immediate discontinuation of antipsychotic drugs and other drugs not essential to concurrent therapy
2) intensive symptomatic treatment and medical monitoring
3) treatment of any concomitant serious medical problems for which specific treatments are available. There is no general agreement about specific pharmacological treatment regimens for uncomplicated NMS.
• Thrombocytopenia and anemia have been reported in patients receiving the drug. Agranulocytosis and pancytopenia have also been reported-warn patients to report the sudden appearance of sore throat or other signs of infection. If white blood cell and differential counts indicate cellular depression, stop treatment and start antibiotic and other suitable therapy.
• Jaundice of the cholestatic type of hepatitis or liver damage has been reported. If fever with grippe-like symptoms occurs, appropriate liver studies should be conducted. If tests indicate an abnormality, stop treatment.
• Because hypotension has occurred, large doses and parenteral administration should be avoided in patients with impaired cardiovascular systems.
• Since certain phenothiazines have been reported to produce retinopathy, the drug should be discontinued if ophthalmoscopic examination or visual field studies should demonstrate retinal changes.
• An antiemetic action of trifluoperazine hydrochloride may mask the signs and symptoms of toxicity or overdosage of other drugs and may obscure the diagnosis and treatment of other conditions such as intestinal obstruction, brain tumor and Reye’s syndrome.
• With prolonged administration at high dosages, the possibility of cumulative effects, with sudden onset of severe central nervous system or vasomotor symptoms, should be kept in mind.
• Antipsychotic drugs elevate prolactin levels; the elevation persists during chronic administration.
• As with all drugs which exert an anticholinergic effect, and/or cause mydriasis, trifluoperazine should be used with caution in patients with glaucoma.
Phenothiazines may diminish the effect of oral anticoagulants.
• Phenothiazines can produce alpha-adrenergic blockade.
• Concomitant administration of propranolol with phenothiazines results in increased plasma levels of both drugs.
• Drugs which lower the seizure threshold, including phenothiazine derivatives, should not be used with metrizamide.

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you :
• you have an allergy to trifluoperazine or any other part of this medicine.
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
• If you have any of these health problems: Blood problems, bone marrow disease, brain problems, liver disease, or low blood cell count.
• If you are very sleepy.
• If you have recently drunk a lot of alcohol or taken a big amount of drugs that may slow your actions like phenobarbital or some pain drugs like oxycodone.
• If you are breast-feeding or plan to breast-feed.
• Avoid driving and doing other tasks or actions that call for you to be alert until you see how this medicine affects you.
• To lower the chance of feeling dizzy or passing out, rise slowly over a few minutes when sitting or lying down. Be careful climbing stairs.
• Avoid drinking alcohol while taking trifluoperazine .
• Low white blood cell counts have happened with drugs like this one. This may lead to a higher chance of getting an infection. Deadly infections have rarely happened. Tell your doctor if you have ever had a low white blood cell count. Call your doctor right away if you have signs of infection like fever, chills, or sore throat. Talk with your doctor.
Take a missed dose as soon as you think about it. If it is close to the time for your next dose, skip the missed dose and go back to your normal time. Do not take 2 doses at the same time or extra doses.

Pregnancy level

C


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