Trifluoperazine
Trifluoperazine (中文:三氟拉嗪) 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:
|
| Short-term adjunctive management
of severe anxiety |
By mouth
ADULT:
ELDERLY:
|
| Severe nausea and vomiting |
By mouth ADULT:
|
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
For males it may result in
|
|---|---|
| Muscle/Nervous system disorders: |
Common:
-Tremor -Akathisia -Parkinsonism -Tardive dyskinesia
-Dry mouth -Constipation -Blurred vision Not known:
|
| Metabolism disorders |
Not known:
|
| Cardiac disorders |
Rare:
Not known:
|
| Hepatic disorder | Jaundice (such as yellowing eyes/skin, persistent nausea, vomiting, stomach/abdominal pain) |
| Skin |
|
| Common: breast pain, galactorrhoea | |
|
Common:
|
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 |
|---|---|
anxiolytics, sedative H1 antihistamines, central antihypertensives, baclofen, thalidomide and opioids. |
Potentiates the sedative effect. |
|
Increased risk of extrapyramidal side-effects when trifluoperazine given with lithium. |
|
Antipsychotics with dopamine-blocking activity and dopaminergic drugs such as those used to treat parkinsonism may be mutually antagonistic. |
|
An increased risk of ventricular arrhythmias – avoid concomitant use. |
|
|
|
Decreased GI absorption of chlorpromazine. Administer chlorpromazine and antacid more than 2 hours apart if possible. |
Caution
- In patients with impaired liver, kidney, cardiovascular and respiratory function
- In those with angle-closure glaucoma
- In patients with a history of jaundice, parkinsonism
- In those with diabetes mellitus, hypothyroidism
- In patients with myasthenia gravis, paralytic ileus
- In patients with prostatic hyperplasia or urinary retention
- Care is required in patients with epilepsy
- Debilitated patients, the elderly, especially those with dementia.
Contra-indications
Use of trifluoperazine should be avoided in individuals with:
- CNS depression
- Comatose states
- Parkinson’s disease
- Phaeochromocytoma
- In elderly patients with dementia
Hepatic impairment
- Can precipitate coma.
Renal impairment
- Start with small doses in severe renal impairment because of increased cerebral sensitivity.
Pregnancy
Should be avoided in pregnancy.
Breast-feeding
Use during breast feeding is not recommended.
Driving and skilled tasks
Drivers and machine operators should be told about the risk of drowsiness with this medication especially at the start of treatment. Affected patients should not drive or operate machinery.
FAQ
How should I take the tablet?
You will be prescribed the lowest dose needed to control your symptoms. Take with or without food. Food reduces irritation. It may take 2 to 3 weeks before you get the full benefit of this medication. Do not stop taking this medication without consulting your doctor. You may experience symptoms such as upset stomach, nausea, vomiting, dizziness and shakiness.
What should I avoid while taking?
Avoid drinking alcohol while taking trifluoperazine because it may enhance the side effects of sedation.
Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.
What happen if I overdose?
Contact your primary care doctor. If emergency situation, call 999
What happen if I miss a dose?
Take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
