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.
'''Trifluoperazine (STELAZINE)'''（中文：[[三氟拉嗪]]）
==Pronunciation==
==Pronunciation==
Line 12:
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[[File:Trifluoperazine 1mg.mp3]]
[[File:Trifluoperazine 1mg.mp3]]
==Drug Names==
==Common Strengths of Trifluoperazine Tablet==
{| class="wikitable"
Trifluoperazine are available in the following strengths:
!Generic Name 藥名
*Tablets: 1 mg, 2 mg, 5 mg
!HA Code 藥物代碼
!Classification藥物分類
==Drug Trade Names of Trifluoperazine Tablet==
|-
Stelazine
|Trifluoperazine Tab 1 mg
|TRIF01
==Drug Usage==
|P1S1S3
Managemnt of schizophrenia
|-
|Trifluoperazine Tab 5 mg
|TRIF02
|P1S1S3
|}
==Mechanism of Action==
==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.
It works primarily by blocking dompamine D<sub>1</sub> and D<sub>2</sub> receptors in the brain, particularly in the mesocortical and mesolimbic pathways. It also has antiadrenergic, antihistaminic, and minimal anticholinergic effects.
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.
==Route of Administration==
Oral
==Dosages==
*Schizophrenia in adults: Initially 2 to 5 mg orally twice daily, increased gradually to 15 to 20 mg/day. Maximum 40 mg/day.
!style="text-align: left"| Severe nausea and vomiting
| Blurred vision: Can affect daily activities like reading and driving.
|
|-
By ''mouth
| Constipation
|-
ADULT:
| Urinary retention
*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:
{| class = "wikitable"
!style="text-align: left"| 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)
|-
|-
!style="text-align: left"| Muscle/Nervous system disorders:
| Insomnia
|
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
|-
|-
!style="text-align: left"| Metabolism disorders
| Fatigue: General tiredness and lack of energy.
|
Not known:
*Hyponatraemia
*Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
|-
|-
!style="text-align: left"| Cardiac disorders
| Muscle weakness: May affect physical activities
|
Rare:
*Ventricular arrhythmia
*Ventricular fibrillation, or tachycardia
Not known:
*Electrocardiogram QT prolonged
*Postural hypotension
|-
|-
!style="text-align: left"| Hepatic disorder
| Skin reactions: Includes rash, itching, and increased sensitivity to sunlight.
|Jaundice (such as yellowing eyes/skin, persistent nausea, vomiting, stomach/abdominal pain)
|-
|-
!style="text-align: left"| Skin
| Loss of appetite
|
*Photosensitivity reactions
*Skin pigmentation
*Contact dermatitis
|-
|-
!style="text-align: left"|
| Menstrual irregularities: Missed periods or other changes in the menstrual cycle.
|Common: breast pain, galactorrhoea
|-
|-
!style="text-align: left"|
| Breast swelling or discharge: This can occur in both men and women due to increased prolactin levels.
|
Common:
*weight gain
|}
==Pharmacokinetics==
{|class="wikitable"
!style="text-align: left"| Oral bioavailability
|Sulpiride is readily absorbed after oral doses.
|-
|-
!style="text-align: left"| Onset of action
| rowspan="9" | '''Serious
|Peak plasma concentrations are reached 1.5 – 6 hours after an oral dose.
| Extrapyramidal symptoms (movement disorders):
*Muscle stiffness or spasms
*Tremors
*Restlessness (akathisia)
*Parkinson-like symptoms
|-
|-
!style="text-align: left"| Metabolism
| Tardive dyskinesia (potentially irreversible in voluntary movements of face and tongue)
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.
{| class="wikitable"
!style="text-align: left"| Drugs given with trifluoperazine
!style="text-align: left"| Potential Effect
|-
|-
|
| Low white blood cell count (agranulocytosis)
*CNS-depressant drugs including alcohol, hypnotics,
anxiolytics, sedative H1 antihistamines, central
antihypertensives, baclofen, thalidomide and opioids.
|
Potentiates the sedative effect.
|-
|-
|style="text-align: left"|
| Seizures
*Lithium
|Increased risk of extrapyramidal side-effects when trifluoperazine given with lithium.
|-
|-
|style="text-align: left"|
| QT prolongation leading to dangerous heart arrhythmias
|Antipsychotics with dopamine-blocking activity and dopaminergic drugs such as those used to treat parkinsonism may be mutually antagonistic.
|-
|-
|style="text-align: left"|
| Orthostatic hypotension: Sudden drop in blood pressure upon standing, leading to dizziness or fainting
*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.
|-
|-
|style="text-align: left"|
| Jaundice: Yellowing of the skin or eyes
*Oral anticoagulants
|
|-
|-
|style="text-align: left"|
| Severe allergic reactions: Symptoms include difficulty of the face, lips, tongue, or throat.
*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.
|}
|}
===Caution===
==Pharmacokinetics==
*In patients with impaired liver, kidney, cardiovascular and respiratory function
*Metabolism: Hepatic
*In those with angle-closure glaucoma
*Elimination half-life: 18 - 24 hours
*In patients with a history of jaundice, parkinsonism
Onset and duration of drug action:
*In those with diabetes mellitus, hypothyroidism
*Onset: Within 30 to 60 minutes (oral)
*In patients with myasthenia gravis, paralytic ileus
*Duration: 24 hours or longer
*In patients with prostatic hyperplasia or urinary retention
*Care is required in patients with epilepsy
==Drug Precautions==
*Debilitated patients, the elderly, especially those with dementia.
'''Pregnancy
Use only if potential benefits outweigh risks. May cause extrapyramidal symptoms in newborns if used in the third trimester.
'''Breastfeeding
Use caution. Trifluoperazine is excreted in breast milk.
'''Children and Elderly
*Children: Use caution. Safety and efficacy not established in children under 6 years.
*Elderly: Start with lower doses and titrate slowly. Increased risk of adverse effects.
'''Monitoring Requirements
*Extrapyramidal symptoms
*ECG in patients at risk of QT prolongation
*Complete blood count
*Liver function tests
*Blood pressure
*Eye examinations (long-term use)
'''Drug Interactions
*Increased sedation with CNS depressants
*Increased risk of QT prolongation with other QT-prolonging drugs
*Reduced effectiveness of levodopa
*Increased plasma levels with CYP3A4 inhibitors
===Contra-indications===
==FAQ==
Use of trifluoperazine should be avoided in individuals with:
'''How Should I Take the Tablet?
*CNS depression
*Comatose states
*Parkinson’s disease
*Phaeochromocytoma
*In elderly patients with dementia
===Hepatic impairment===
It can be taken with or without food.
*Can precipitate coma.
===Renal impairment===
'''What Should I Avoid While Taking?
*Start with small doses in severe renal impairment because of increased cerebral sensitivity.
===Pregnancy===
Avoid alclhol and activities requiring mental alertness until you know how trifluoperazine affects you.
Should be avoided in pregnancy.
===Breast-feeding===
'''What Happens if I Miss a Dose?
Use during breast feeding is not recommended.
===Driving and skilled tasks===
Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double doses.
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.
It works primarily by blocking dompamine D1 and D2 receptors in the brain, particularly in the mesocortical and mesolimbic pathways. It also has antiadrenergic, antihistaminic, and minimal anticholinergic effects.
