Trifluoperazine

Indications

Anxiety states: It controls excessive anxiety, tension, and agitation seen in neuroses or associated with somatic conditions. The treatment or prevention of nausea and vomiting of various causes. The management of psychotic disorders, such as acute or chronic catatonic, hebephrenic and paranoid schizophrenia; psychosis due to organic brain damage, toxic psychosis, and the manic phase of manic-depressive illness.

Pharmacology

Trifluoperazine is one of the phenothiazine class of compounds and as such has many pharmacodynamic effects which relate to its therapeutic actions and side effects. The most notable action of phenothiazines is antagonism at dopamine receptors in the CNS. It is hypothesised that this action in the limbic system and associated areas of cerebral cortex is the basis of the antipsychotic action of phenothiazines, whilst in the medullary chemoreceptor trigger zone it appears to be responsible for the antiemetic effect of these agents.

Dosage And Administration

Schizophrenia and other psychoses:

  • Adults and child over 12 years: Recommended starting dose is 2-5 mg b.i.d, increased by 5 mg daily after 1 week then at interval of 3 days, according to response. 
  • Children (6-12 years): Dosage should be adjusted to the weight of the child and severity of the symptoms. The starting dosage is 1 mg b.i.d. Dosage may be increased gradually until symptoms are controlled or until side effects become troublesome. While it is usually not necessary to exceed dosages of 15 mg daily.
  • Elderly: Reduce initial dose by at least half

Short-term management of severe anxiety:

  • Adult and child over 12 years: 1-2 mg b.i.d, increased if necessary to 6 mg daily.
  • Child (3-5 years): 1 mg daily
  • Child (6-12 years): Up to 4 mg daily in divided dose.
  • Elderly: Reduce initial dose by at least half

Antiemetic:

  • Adult: 2-4 mg daily in divided doses; max. 6 mg daily;
  • Child 3-5 years: up to 1 mg daily, 6-12 years up to 4 mg daily.

Interaction

Trifluoperazine may diminish the effect of oral anticoagulants. Concomitant administration of propranolol with trifluoperazine results in increased plasma levels of both drugs. Antihypertensive effects of guanethidine and related compounds may be counteracted when phenothiazines are used concurrently. Potentiation may occur if antipsychotic drugs are combined with CNS depressants such as alcohol. hypnotics and anticonvulsant.

Contraindications

Do not use Trifluoperazine in comatose patients, or in those with existing blood dyscrasias or known liver damage, or in those hypersensitive to the active ingredient or related compounds.

Side Effects

Common side effects are transient restlessness, dystonias or may resemble parkinsonism. Other CNS Reactions are drowsiness, dizziness, fatigue, blurred vision, seizures. Without these Peripheral oedema, blood dyscrasias, jaundice may occasionally occur. Tachycardia, constipation, urinary hesitancy and retention and hyperpyrexia have been reported very rarely.

Pregnancy And Lactation

Pregnancy: Safety for the use of trifluoperazine during pregnancy has not been established. Therefore, it is not recommended that the drug be given to pregnant patients except when, in the judgement of the physician, it is essential. The potential benefits should clearly outweigh possible hazards. There are reported instances of prolonged jaundices, extrapyramidal signs, hyperreflexia or hypoflexia in newborn infants whose mother received phenothiazines.

Lactation: Adequate human data are not available in case of lactation.

Precautions And Warnings

Care should be taken when treating elderly patients, and initial dosage should be reduced. Such patients can be specially sensitive, particularly to extra pyramidal and hypotensive effects. Patients with cardiovascular disease including arrhythmias should also be treated with caution. Care should be taken in patients with angina pectoris.

Overdose Effects

Signs and symptoms will be predominantly extrapyramidal; hypotension may occur. Treatment consists of gastric lavage together with supportive and symptomatic measures. Do not induce vomiting. Extra pyramidal symptoms may be treated with an anticholinergic, antiparkinsonism drug. Treat hypotension with fluid replacement; if severe or persistent. nor adrenaline may be considered. Adrenaline is contraindicated.

Therapeutic Class

Phenothiazine drugs.

Storage Conditions

It should be store at room temperature between 15-30° C away from light and moisture.