Trifluoperazine: Difference between revisions

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


'''Trifluoperazine''' (中文:[[     ]]) is a typical antipsychotic or 1st Generation antipsychotic medication. It is used to treat
[[:Category: Antipsychotic Drug | '''Antipsychotic Drug''']]
*Schizophrenia
 
*Short-term adjunctive management of severe anxiety
'''Drug class: [[:Category: Typical Antipsychotic  | Typical Antipsychotic]]
*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.
'''Trifluoperazine (STELAZINE)'''（中文：[[三氟拉嗪]]）


==Pronunciation==
==Pronunciation==
Line 12: Line 11:
[[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.


==Dosage==
==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.
 
==Side Effects==
{| class="wikitable"
{| class="wikitable"
!style="text-align: left"| Indication
!style="text-align: left"| Frequency
!style="text-align: left"| Dose
!Adverse reactions
|-
| rowspan="12" | '''Common
| Drowsiness and dizziness
|-
| Dry mouth: Can be managed with sugarless gum.
|-
| Blurred vision: Can affect daily activities like reading and driving.
|-
| Constipation
|-
| Urinary retention
|-
| Insomnia
|-
| Fatigue: General tiredness and lack of energy.
|-
| Muscle weakness: May affect physical activities
|-
| Skin reactions: Includes rash, itching, and increased sensitivity to sunlight.
|-
| Loss of appetite
|-
| Menstrual irregularities: Missed periods or other changes in the menstrual cycle.
|-
|-
!style="text-align: left"| Schizophrenia
| Breast swelling or discharge: This can occur in both men and women due to increased prolactin levels.
|By ''mouth
ADULT:
*2 - 5 mg twice daily
*Usual range 15 – 20 mg daily in divided doses
*Up to 50 mg daily
|-
|-
!style="text-align: left"| Short-term adjunctive management
| rowspan="9" | '''Serious
of severe anxiety
| Extrapyramidal symptoms (movement disorders):
|By ''mouth
*Muscle stiffness or spasms
ADULT:
*Tremors
*2 – 6 mg daily in divided doses
*Restlessness (akathisia)
ELDERLY:
*Parkinson-like symptoms
*Lower initial dose to be given
*Increased gradually according to response
|-
|-
!style="text-align: left"| Severe nausea and vomiting
| Tardive dyskinesia (potentially irreversible in voluntary movements of face and tongue)
|
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:
{| 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:
| Neuroleptic malignant syndrome (fever, muscle rigidity, altered mental state)
|
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
| Low white blood cell count (agranulocytosis)
|
Not known:
*Hyponatraemia
*Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
|-
|-
!style="text-align: left"| Cardiac disorders
| Seizures
|
Rare:
*Ventricular arrhythmia
*Ventricular fibrillation, or tachycardia
Not known:
*Electrocardiogram QT prolonged
*Postural hypotension
|-
|-
!style="text-align: left"| Hepatic disorder
| QT prolongation leading to dangerous heart arrhythmias
|Jaundice (such as yellowing eyes/skin, persistent nausea, vomiting, stomach/abdominal pain)
|-
|-
!style="text-align: left"| Skin
| Orthostatic hypotension: Sudden drop in blood pressure upon standing, leading to dizziness or fainting
|
*Photosensitivity reactions
*Skin pigmentation
*Contact dermatitis
|-
|-
!style="text-align: left"|
| Jaundice: Yellowing of the skin or eyes
|Common: breast pain, galactorrhoea
|-
|-
!style="text-align: left"|
| Severe allergic reactions: Symptoms include difficulty of the face, lips, tongue, or throat.
|
Common:  
*weight gain
|}
|}


==Pharmacokinetics==
==Pharmacokinetics==
{|class="wikitable"
*Metabolism: Hepatic
!style="text-align: left"| Oral bioavailability
*Elimination half-life: 18 - 24 hours
|Sulpiride is readily absorbed after oral doses.
Onset and duration of drug action:
|-
*Onset: Within 30 to 60 minutes (oral)
!style="text-align: left"| Onset of action
*Duration: 24 hours or longer
|Peak plasma concentrations are reached 3 – 6 hours after an oral dose.
 
|-
==Drug Precautions==
!style="text-align: left"| Metabolism
'''Pregnancy
|It is metabolized in the liver
 
|-
Use only if potential benefits outweigh risks. May cause extrapyramidal symptoms in newborns if used in the third trimester.
!style="text-align: left"| Elimination half-life
 
|
'''Breastfeeding
It is excreted in the urine and faeces.
 
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
 
==FAQ==
'''How Should I Take the Tablet?
 
It can be taken with or without food.
 
'''What Should I Avoid While Taking?
 
Avoid alclhol and activities requiring mental alertness until you know how trifluoperazine affects you.
 
'''What Happens if I Miss a Dose?


The elimination half-life is approximately 8 hours.
Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double doses.
|}

Latest revision as of 22:54, 31 July 2024


Antipsychotic Drug

Drug class: Typical Antipsychotic

Trifluoperazine (STELAZINE)（中文：三氟拉嗪）

Pronunciation[edit]

Trifluoperazine 1mg[edit]

Common Strengths of Trifluoperazine Tablet[edit]

Trifluoperazine are available in the following strengths:

  • Tablets: 1 mg, 2 mg, 5 mg

Drug Trade Names of Trifluoperazine Tablet[edit]

Stelazine

Drug Usage[edit]

Managemnt of schizophrenia

Mechanism of Action[edit]

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.

Route of Administration[edit]

Oral

Dosages[edit]

  • Schizophrenia in adults: Initially 2 to 5 mg orally twice daily, increased gradually to 15 to 20 mg/day. Maximum 40 mg/day.

Side Effects[edit]

Frequency Adverse reactions
Common Drowsiness and dizziness
Dry mouth: Can be managed with sugarless gum.
Blurred vision: Can affect daily activities like reading and driving.
Constipation
Urinary retention
Insomnia
Fatigue: General tiredness and lack of energy.
Muscle weakness: May affect physical activities
Skin reactions: Includes rash, itching, and increased sensitivity to sunlight.
Loss of appetite
Menstrual irregularities: Missed periods or other changes in the menstrual cycle.
Breast swelling or discharge: This can occur in both men and women due to increased prolactin levels.
Serious Extrapyramidal symptoms (movement disorders):
  • Muscle stiffness or spasms
  • Tremors
  • Restlessness (akathisia)
  • Parkinson-like symptoms
Tardive dyskinesia (potentially irreversible in voluntary movements of face and tongue)
Neuroleptic malignant syndrome (fever, muscle rigidity, altered mental state)
Low white blood cell count (agranulocytosis)
Seizures
QT prolongation leading to dangerous heart arrhythmias
Orthostatic hypotension: Sudden drop in blood pressure upon standing, leading to dizziness or fainting
Jaundice: Yellowing of the skin or eyes
Severe allergic reactions: Symptoms include difficulty of the face, lips, tongue, or throat.

Pharmacokinetics[edit]

  • Metabolism: Hepatic
  • Elimination half-life: 18 - 24 hours

Onset and duration of drug action:

  • Onset: Within 30 to 60 minutes (oral)
  • Duration: 24 hours or longer

Drug Precautions[edit]

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

FAQ[edit]

How Should I Take the Tablet?

It can be taken with or without food.

What Should I Avoid While Taking?

Avoid alclhol and activities requiring mental alertness until you know how trifluoperazine affects you.

What Happens if I Miss a Dose?

Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double doses.

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