Trifluoperazine

[[Category: ]] Drug Class: Antipsychotics, typical; Antipsychotic 1st Generation

Trifluoperazine (中文:[[ ]]) is a typical antipsychotic or 1st Generation antipsychotic medication. It is used to treat

• Schizophrenia
• Short-term adjunctive management of severe anxiety
• Severe nausea and vomiting

It helps patient to think more cleaerly, feel less nervous, and take part in everyday life. It can reduce aggressive behavior and the desire to hurt oneself/others. It helps to decrease hallucinations.

Pronunciation

Trifluoperazine 1mg

Drug Names

Generic Name 藥名	HA Code 藥物代碼	Classification藥物分類
Trifluoperazine Tab 1 mg	TRIF01	P1S1S3
Trifluoperazine Tab 5 mg	TRIF02	P1S1S3

Mechanism of Action

Trifluoperazine has central antiadrenergic, antidopaminergic, and minimal anticholinergic effects. It works by blocking postsynaptic mesolimbic dopamine D1 and D2 receptors in the brain, minimizing such symptoms of schizophrenia as hallucinations, delusions and disorganized thought and speech. Antiemetic effects are attributed to dopamine receptor blockade in the medullary chemoreceptor trigger zone. The presumed effectiveness of antipsychotic drugs relied on their ability to block dopamine receptors. This assumption arose from the dopamine hypothesis that maintains that both schizophrenia and bipolar disorder are a result of excessive dopamine activity.

Dosage

Indication	Dose
Schizophrenia	By mouth ADULT: 2 - 5 mg twice daily Usual range 15 – 20 mg daily in divided doses Up to 50 mg daily
Short-term adjunctive management of severe anxiety	By mouth ADULT: 2 – 6 mg daily in divided doses ELDERLY: Lower initial dose to be given Increased gradually according to response
Severe nausea and vomiting	By mouth ADULT: 2 – 4 mg daily in divided doses Maximum 6 mg daily

Trifluoperazine is not approved for the treatment of dementia-related behavior problems. Typical (First-generation) antipsychotic agents may increase mortality in such patients. Most fatalities appeared to result from cardiovascular-related events (e.g. heart failure, sudden death) or infectious (mostly pneumonia).

Side Effects

Extrapyramidal symptoms (EPS) are frequent, especially at doses exceeding 6 mg daily. These symptoms include:

• Drooling/trouble swallowing
• Restlessness/constant need to move
• Shaking (tremor)
• Shuffling walk
• Stiff muscles
• Severe muscle spasms/cramping (such as twisting neck, arching back, eyes rolling up)
• Mask-like expression of the face
• Tardive dyskinesia (any uncontrollable movements such as lip smacking, mouth puckering, tongue thrusting, chewing, or unusual arm/leg movements

Other adverse effects of trifluoperazine include the following:

Endocrine disorders	Common: hyperprolactinaemia (elevated levels of the hormone prolactin, which for females may result in Galactorrhea (unwanted breast milk) amornorrhea (missed/stopped periods), For males it may result in decreased sexual ability, or gynecomastia (enlarged breast)
Muscle/Nervous system disorders:	Common: Sedation or drowsiness Extrapyramidal symptoms (EPS) -Tremor -Akathisia -Parkinsonism -Tardive dyskinesia Anticholinergic side-effects such as: -Dry mouth -Constipation -Blurred vision Not known: Neuroleptic malignant syndrome Convulsion
Metabolism disorders	Not known: Hyponatraemia Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
Cardiac disorders	Rare: Ventricular arrhythmia Ventricular fibrillation, or tachycardia Not known: Electrocardiogram QT prolonged Postural hypotension
Hepatic disorder	Jaundice (such as yellowing eyes/skin, persistent nausea, vomiting, stomach/abdominal pain)
Skin	Photosensitivity reactions Skin pigmentation Contact dermatitis
	Common: breast pain, galactorrhoea
	Common: weight gain

Pharmacokinetics

Oral bioavailability	Sulpiride is readily absorbed after oral doses.
Onset of action	Peak plasma concentrations are reached 1.5 – 6 hours after an oral dose.
Metabolism	It is metabolized in the liver
Elimination half-life	It is excreted in the urine and faeces. The elimination half-life is approximately 24 hours.

Drug Management

Monitoring

The following populations must be closely monitored after administration of trifluoperazine:

• Epileptics, since chlorpromazine may lower the seizure threshold. Treatment must be stopped if seizures occur.
• Elderly persons with susceptibility to orthostatic hypotension, sedation, and extrapyramidal effects, chronic constipation, and prostatic hypertrophy.
• Patients with cardiovascular disease since chlorpromazine can induce tachycardia and hypotension. Regular BP and pulse monitoring are recommended.
• Patients with severe liver and/or renal failure because of the risk of accumulation.
• Patients on long-term treatment should receive regular eye examinations.
• Diabetic patients who are started on chlorpromazine should get glycemic monitoring during treatment.
• Trifluoperazine may cause increased susceptibility to sunburn and individuals should avoid undue exposure to direct sunlight.
• Trifluoperazine impairs body temperature regulation. The elderly or hypothyroid patient may be particularly susceptible to hypothermia. The hazard of hyperthermia may be increased by hot weather.

Drug interaction

The most common interactions encountered with trifluoperazine result from use with drugs that have similar pharmacological actions, for example:

Trifluoperazine may aggravate Parkinsonism and antagonize the action of levodopa.

Drugs given with trifluoperazine	Potential Effect
CNS-depressant drugs including alcohol, hypnotics, anxiolytics, sedative H1 antihistamines, central antihypertensives, baclofen, thalidomide and opioids.	Potentiates the sedative effect.
Lithium	Increased risk of extrapyramidal side-effects when trifluoperazine given with lithium.
Antiparkinsonian drugs (amantadine, bromocriptine, levodopa, ropinirole)	Antipsychotics with dopamine-blocking activity and dopaminergic drugs such as those used to treat parkinsonism may be mutually antagonistic.
Drugs that prolong the QT interval e.g. amiodarone, sotalol, quinidine Drugs which induce bradycardia e.g. diltiazem, verapamil Drugs which can cause hypokalaemia such as diuretics e.g. frusemide	An increased risk of ventricular arrhythmias – avoid concomitant use.
Oral anticoagulants
Antacids (magnesium, aluminum and calcium salts, oxides and hydroxides)	Decreased GI absorption of chlorpromazine. Administer chlorpromazine and antacid more than 2 hours apart if possible.