Action and Spectrum

Action

The drug’s mechanism of action involves inhibiting the brain’s dopamine and serotonin neurotransmitters, which are thought to be involved in the emergence of psychotic symptoms.

Spectrum

trifluoperazine treats both the positive and negative symptoms of schizophrenia, including delusions, hallucinations, disordered thinking, and emotional blunting. It has a broad range of activity.

Drug Interaction

Adverse Reaction

Frequency not defined 

Anticholinergic effects

Weight gain

Oligomenorrhea/amenorrhea

Erectile dysfunction

Insomnia

Restlessness

Anxiety

Euphoria

EPS (60%; muscle stiffness, dystonia, parkinsonism, tardive dyskinesia, akathisia)

NMS

Sedation

Cerebral edema

Poikilothermia

Orthostatic hypotension

Tachycardia

Dizziness

Agitation

Depression

Weakness

Headache

Pruritis

Diarrhea

Galactorrhea

Ejaculatory

Seizure

Priapism

Cholestatic jaundice

Lens opacities Anorexia

Dyspepsia

Constipation

Ileus

Blood dyscrasia

ECG changes

Photosensitivity

Black Box Warning

Black Box Warning:

There is a black box warning on trifluoperazine about the elevated mortality risk in older adults with dementia-related psychosis. Trifluoperazine, among other antipsychotic medications, increases the risk of death in elderly individuals with dementia-related psychosis compared to placebo.

The use of trifluoperazine to treat psychosis brought on by dementia is not authorised. The prescription also carries a black box warning about the elevated risk of suicide ideas and actions in kids, teenagers, and young adults who are taking antidepressants or antipsychotic drugs, including trifluoperazine.

Contraindication / Caution

Contraindication

A history of phenothiazine or trifluoperazine hypersensitivity

Central nervous system

Hypertension or severe hypotension

Serious renal or liver illness

Blood dyscrasias like agranulocytosis, neutropenia, or leukopenia

Pheochromocytoma

Caution

Cardiovascular illness, including a history of congestive heart failure, arrhythmias, and QT prolongation

seizures or epilepsy disorders

Glaucoma

urinary retention or enlarged prostate

Hyperthyroidism

extrapyramidal illnesses such as Parkinson’s disease

Breast cancer or breast cancer in the family

Those over the age of 65 may be more prone to negative side effects such drowsiness, disorientation, and orthostatic hypotension

Pregnancy / Lactation

Pregnancy consideration:

Pregnancy category: NA

Lactation: Excreted into human milk.

Pregnancy Categories:     

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category.

Pharmacology

Pharmacology:

A common antipsychotic drug is trifluoperazine, which works pharmacologically by inhibiting dopamine and serotonin receptors in the brain. It specifically inhibits dopamine receptors in the brain’s mesolimbic and mesocortical regions, which control emotion, motivation, and reward. Dopamine activity in these regions is decreased by this blockage, which helps lessen psychotic symptoms like hallucinations and delusions

Pharmacodynamics:

Dopamine antagonists like trifluoperazine attach to and block dopamine receptors in the brain. In particular, the mesolimbic and mesocortical pathways, which are involved in the regulation of emotion, motivation, and reward, are affected by this action, which lowers the activity of dopamine there. Trifluoperazine can reduce psychotic symptoms like delusions and hallucinations by inhibiting dopamine receptors in these regions.

Pharmacokinetics:

Absorption

trifluoperazine is quickly and virtually entirely absorbed after being taken orally. After a single dose, the peak plasma concentration is obtained in 2 to 4 hours. Unfortunately, the medication’s bioavailability is only about 20% after substantial first-pass hepatic processing.

Distribution

trifluoperazine can easily breach the blood-brain barrier and disperse throughout the body’s tissues since it is highly lipophilic and has a large volume of distribution. Most of the plasma proteins it is 99% linked to are albumin.

Metabolism

trifluoperazine undergoes significant cytochrome P450 system metabolization in the liver, principally via the CYP2D6 and CYP3A4 pathways. Sulfoxide, the primary metabolite, is pharmacologically active and has a potency comparable to that of the parent medication. Trifluoperazine in its N-demethylated and hydroxylated forms are two further minor metabolites. Because of the medication’s 6 to 8 hour half-life, once-daily dosing is possible.

Elimination and Excretion

trifluoperazine is mostly excreted in the urine, with 10% of the dose being excreted unaltered and around 60% of the dose being excreted as metabolites. In the feces, the remaining 30% is excreted. In healthy people, the medication has a half-life of 6 to 8 hours, however patients with liver or renal disease may experience a longer half-life.

Adminstartion

Administration:

trifluoperazine is typically used once day, with or without food, in the form of oral pills or capsules. The recommended starting dose is 1 to 2 mg per day, and the dose can be gradually raised as needed up to a maximum of 20 mg per day. Two to four smaller doses spread out throughout the day typically make up the entire daily dose.

trifluoperazine may be administered intramuscularly in urgent or emergency situations where oral administration is impractical. Injections of 1 to 2 mg of the typical dosage are administered to big muscles like the gluteus maximus. As required, the injection may be repeated every two to four hours, with a daily dose cap of 6 to 8 mg.

Patient Information Leaflet

Patient information leaflet

Generic Name:  trifluoperazine

Pronounced: [TRYE-floo-oh-PER-a-zeen]

Why do we use trifluoperazine?

A drug called trifluoperazine is primarily used to treat schizophrenia and other psychotic diseases. It is occasionally used to treat extreme agitation and anxiety.

trifluoperazine is used to treat symptoms like delusions, hallucinations, disorganized thinking, and social disengagement in schizophrenia and other psychotic diseases.

It functions by obstructing serotonin and dopamine receptors in the brain, which can assist to lessen their activity and ease symptoms.