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[[Category: Drugs]][[Category: Antipsychotics, typical; Antipsychotic 2nd Generation]]
[[Category: Drugs]][[Category: Atypical antipsychotic ]]
'''Aripiprazole''' (中文:[[      ]]) is an atypical antipsychotic or 2nd Generation antipsychotic medication. It is mainly used in the treatment of
*Schizophrenia: there is little difference in effectiveness between antipsychotics in prevention of relapse, the specific choice of antipsychotic be chosen based on person’s preference and side-effect profile.
*bipolar disorder: aripiprazole is effective for the treatment of acute manic episodes of bipolar disorder.It is useful for the prevention of manic episodes, but is not useful for bipolar depression.
*adjuinct treatment of major depressive disoreder


Aripiprazole rebalances dopamine and serotonin to improve thinking, mood and behaviour.
[[:Category: Antipsychotic Drug | '''Antipsychotic Drug''']]


==Pronunciation==
'''Drug class: [[:Category: Atypical antipsychotic  | Atypical Antipsychotic ]]


==Drug Names==
'''Aripiprazole (ABILIFY)'''（中文：[[阿立哌唑]]）
{| class="wikitable"
==Common Strengths of Aripiprazole Tablet==
!Generic Name 藥名
Aripiprazole tablets are available in the following strengths:
!HA Code 藥物代碼
*2 mg, 5 mg, 10 mg, 15 mg, 30 mg tablets
!Classification藥物分類
 
|-
==Drug Trade Names of Aripiprazole Tablet==
|Aripiprazole Tab 5 mg
Abilify
|ARIP03
 
|P1S1S3
==Drug Usage==
|-
Aripiprazole is used for:
|Aripiprazole Tab 10 mg
* Schizophrenia
|ARIP01
* Bipolar disorder
|P1S1S3
* Major depressive disorder (as an adjunct)
|-
* Tourette syndrome
|Aripiprazole Tab 15 mg
* Autism-related irritability
|ARIP02
|P1S1S3
|}


==Mechanism of Action==
==Mechanism of Action==
Aripiprazole is a dopamine D2 partial agonist. It is also a partial activator of serotonin 5-HT1A receptors.
Aripiprazole is a partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and an antagonist at serotonin 5-HT2A receptors.
Aripiprazole acts by modulating neurotransmission overactivity of dopamine, which is thought to mitigate schizophrenia symptoms.


==Dosage==
==Route of Administration==
* Oral (tablets and oral solution)
 
==Dosages==
* Schizophrenia (adults): Initial dose 10 - 15 mg/day, target dose 10 - 15 mg/day, maximum 30 mg/day
* Bipolar disorder (adults): Initial dose 15 mg/day, maximum 30 mg/day
 
Aripiprazole does not require dosage adjustment based on renal function, including in patients with severe renal impairment or end-stage renal disease (ESRD). This is
 
because aripiprazole is primarily metabolized in the liver and only a small fraction is excreted unchanged in the urine.
 
==Side Effects==
*Detailed percentage-based side effect information not provided in the search results.
{| class="wikitable"
{| class="wikitable"
!style="text-align: left"| Indication
!style="text-align: left"| Frequency
!style="text-align: left"| Dose
!Adverse reactions
|-
|-
!style="text-align: left"| Schizophrenia 
| rowspan="10" | '''Common
|By ''mouth
| Insomnia: Difficulty sleeping, which often improves over time.
ADULT:
*10 – 15 mg once daily,  
*Maximum 30 mg once daily
|-
|-
!style="text-align: left"| Treatment and recurrence prevention of mania
| Anxiety and Restlessness: Feelings of anxiety and restlessness that usually subside with continued use
|By ''mouth
ADULT:
*15 mg once daily
*Maximum 30 mg once daily
|-
|-
!style="text-align: left"| Adjunct treatment of major depressive disorder
| Dizziness
|By ''mouth
|-
ADULT:
| Headache: Common and can be managed with rest and hydration
*Initially 2- 5 mg once daily,
*Increased to 5 – 10 mg once daily
*Maximum 15 mg once daily
|}
 
How long does it take for Amisulpride to work?
The patient may start to feel better in a few days but it can take as long as 4 to 6 weeks before the full effects of this medication is noticed.
 
==Side Effects==
All side-effects are listed by system organ and frequency.
*Common ( ≥ 1/100 to < 1/10)
*Uncommon (≥ 1/1000 to < 1/100)
 
{| class = "wikitable"
!style="text-align: left"| Endocrine disorders
|
Uncommon: 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:
| Nausea and Vomiting: Can be mitigated by taking the medication with food
|
Common:
*Extrapyramidal symptoms (EPS)
-Tremor
-Akathisia
-Parkinsonism
*Anticholinergic side-effects such as:
-Dry mouth
-Constipation
-Blurred vision
*headache
*sedation
*somnolence
*dizziness
*salivary hypersecretion
Uncommon: tardive dyskinesia and seizures
Not known: Neuroleptic malignant syndrome
|-
|-
!style="text-align: left"| Psychiatric disorders
| Constipation: Increasing dietary fiber and water intake can help
|
Common:
*Insomnia
*Anxiety
*Restlessness
Uncommon:
*Depression
*hypersexuality
|-
|-
!style="text-align: left"| Metabolism disorders
| Dizziness: Often occurs when standing up quickly; getting up slowly can help
|
Common:
*diabetes mellitus
*weight gain
Uncommon:
*Hyponatraemia
*Anorexia
|-
|-
!style="text-align: left"| Cardiac disorders
| Weight Changes: Can cause weight gain or loss; maintaining a balanced diet is recommended
|
Uncommon:  
*tachycardia
*orthostatic hypotension
|}
 
Pathological gambling, compulsive shopping and binge eating can occur in patients treated with aripiprazole.
 
It is not recommended for older people with dementia-related psychosis due to an increased risk of death.
Discontinuation
 
It is recommended that gradual withdrawal when discontinuing antipsychotics. Symptoms of withdrawal commonly include nausea, vomiting and loss of appetite. Symptoms generally resolve after a short period of time.
 
==Pharmacokinetics==
{|class="wikitable"
!style="text-align: left"| Oral bioavailability
|It is readily absorbed after oral doses.
|-
|-
!style="text-align: left"| Onset of action
| Increased Salivation: More common in children
|Peak plasma concentrations are achieved 3 – 5 hours after an oral dose.
|-
|-
!style="text-align: left"| Metabolism
| Fatigue: Feeling tired or low in energy
|It is metabolized in the liver, principally by the enzymes CYP2D6 and CYP3A4
|-
|-
!style="text-align: left"| Elimination half-life
| rowspan="7" | '''Uncommon
|
| Neuroleptic Malignant Syndrome (NMS): Symptoms include high fever, muscle stiffness, and altered mental status
It is eliminated via urine and faeces.
 
The elimination half-life is approximately 75 hours.
 
Steady-state plasma concentrations are achieved in about 14 days.
|}
 
==Drug Management==
===Monitoring===
The following populations must be closely monitored after administration of aripiprazole:
*Elderly persons with susceptibility to drowsiness, confusion, and unsteadiness, which may increase the risk of fall
*Patients with severe liver failure because of the risk of accumulation.
*Patients on long-term treatment should receive regular eye examinations.
*Diabetic patients should get monitoring blood sugar levels during treatment.
*Changes in mood, the development or worsening depression, and/or any thoughts or behaviour of suicide.
*Be careful while taking antihistamines (chlorpheniramine), sleeping tablets while taking this medicine. Aripiprazole can increase drowsiness caused by medicines affecting the nervous system.
*Tell the doctor if notice any of the following:
-Abnormal movements of the face or tongue
-Yellowing of the skin and eyes, that is jaundice
-Muscle twitching
*Report to the doctor if absence of monthly periods for 6 months or more
 
===Drug interaction===
Aripiprazole is metabolized by multiple pathways involving the CYP2D6 and CYP3A4 enzymes but not CYP1A enzymes. Thus, no dosage adjustment is required for smokers.
 
{| class="wikitable"
!style="text-align: left"| Drugs given with aripiprazole
!style="text-align: left"| Potential Effect
|-
|-
|style="text-align: left"|
| Metabolic Changes: Increased blood sugar, cholesterol, and weight gain, which can lead to diabetes
*CNS-depressant drugs including alcohol, hypnotics, anxiolytics, sedative H1 antihistamines, central antihypertensives, baclofen, thalidomide and opioids.
|
Potentiates the sedative effect.
|-
|-
|style="text-align: left"|
| Compulsive Behaviors: Uncontrollable urges to gamble, eat, shop, or engage in sexual activities
*Strong CYP2D6 inhibitors such as qunindine, fluoxetine and paroxetine.
|
May result in higher plasma concentrations of aripiprazole, aripiprazole dose should be reduced to approximately one-half of its prescribed dose.
|-
|-
|style="text-align: left"|
| Orthostatic Hypotension: Sudden drop in blood pressure upon standing, leading to dizziness or fainting
*Strong CYP3A4 inhibitors, such as itraconazole and HIV protease inhibitors
|May result in higher plasma concentrations of aripiprazole, so aripiprazole dose should be reduced.
|-
|-
|style="text-align: left"|
| Seizures: Convulsions that require immediate medical attention
*Strong CYP3A4 inducers, such as carbamazepine, rifampicin, phenytoin, phenobarbitone and St John’s Wort.
|May lower plasma concentrations of aripiprazole, so should increase aripiprazole dose.
|-
|-
|style="text-align: left"|
| Severe Allergic Reactions: Symptoms include swelling of the face, lips, tongue, or throat, and difficulty breathing
*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.
|-
|-
|style="text-align: left"|
| Suicidal Thoughts: Increased risk in young people, particularly those under 24
*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.
|}
|}


===Caution===  
==Pharmacokinetics==
*In patients with cerebrovascular disease
*Absorption
*In patients with a history of jaundice or who have blood dyscrasias (perform blood counts if unexplained infection or fever develops)
**Aripiprazole is well absorbed after oral administration, with peak plasma concentrations occurring within 3 to 5 hours
*In patients with Parkinson’s disease
*Metabolism
*In patients with epilepsy
**Extensively metabolized in the liver, primarily by CYP3A4 and CYP2D6 enzymes
*In patients with myasthenia gravis
*Elimination
*A susceptibility to angle-closure glaucoma
** The mean elimination half-life is about 75 hours for aripiprazole
*In those with diabetes mellitus
*In patients with paralytic ileus
*In patients with prostatic hyperplasia or urinary retention
*The elderly, especially those with dementia.


===Contra-indications===
Aripiprazole has a relatively rapid initial onset of action within 1 to 2 weeks for most patients, but full therapeutic effects may take several weeks to months to develop.
Use of aripiprazole should be avoided in individuals with:
*CNS depression
*Comatose states
*Phaeochromocytoma


===Hepatic impairment===
Its long half-life results in a prolonged duration of action, allowing for once-daily dosing and steady-state levels after about 2 weeks of treatment.
Use with caution in severe impairment


===Pregnancy===
==Drug Precautions==
Should be avoided in pregnancy.
'''Increased risk in elderly patients


===Breast-feeding===
* Should not be used to treat dementia-related psychosis in older adults due to increased risk of stroke and death
Use during breast feeding should be avoided.
* May cause drowsiness, dizziness, and difficulty swallowing in elderly patients, increasing the risk of falls and choking


===Driving and skilled tasks===
'''Suicidal thoughts in young people
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.
 
* May increase the risk of suicidal thoughts in people under 24 years old, especially in the first few months of treatment or with dose changes
* Close monitoring is required for children/teens taking aripiprazole
 
''' Monitoring Requirements
 
* Monitor for suicidal thoughts and behaviors, especially in younger patients
* May cause increased blood sugar, elevated cholesterol, and weight gain
* Regular monitoring of metabolic parameters are recommended
 
'''Drug Interactions
 
* Strong CYP3A4 inhibitors and CYP2D6 inhibitors may increase aripiprazole levels
* Strong CYP3A4 inducers may decrease aripiprazole levels


==FAQ==
==FAQ==
===How should I take the tablet?===
'''How Should I Take the Tablet?
You will be prescribed the lowest dose needed to control your symptoms. The tablet should be swallowed whole with a glass of water. It may take 4 to 6 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.  
* Standard tablets: Swallow with water
===What should I avoid while taking?===
* Orodispersible tablets: Place on tongue to dissolve or dissolve in water and drink immediately
Avoid drinking alcohol while taking aripiprazole because it may enhance the side effects of sedation.  
* Take at around the same time each day, with or without food.
 
'''What should I avoid while taking?
*Avoid driving, operating machinery or doing activities that require alertness until you know how the medication affects you.
*Do not stop taking amisulpride suddenly without consulting your doctor. Abrupt withdrawal can cause unpleasant side effects or a return of symptoms.


Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.
'''What Happens if I Miss a Dose?
===What happen if I overdose?===
*Take the missed dose as soon as you remember if it is within a few hours. If it is close to the next scheduled dose, skip the missed dose and continue with the regular schedule.
A :  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.

Latest revision as of 01:17, 19 July 2024


Antipsychotic Drug

Drug class: Atypical Antipsychotic

Aripiprazole (ABILIFY)（中文：阿立哌唑）

Common Strengths of Aripiprazole Tablet[edit]

Aripiprazole tablets are available in the following strengths:

  • 2 mg, 5 mg, 10 mg, 15 mg, 30 mg tablets

Drug Trade Names of Aripiprazole Tablet[edit]

Abilify

Drug Usage[edit]

Aripiprazole is used for:

  • Schizophrenia
  • Bipolar disorder
  • Major depressive disorder (as an adjunct)
  • Tourette syndrome
  • Autism-related irritability

Mechanism of Action[edit]

Aripiprazole is a partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and an antagonist at serotonin 5-HT2A receptors.

Route of Administration[edit]

  • Oral (tablets and oral solution)

Dosages[edit]

  • Schizophrenia (adults): Initial dose 10 - 15 mg/day, target dose 10 - 15 mg/day, maximum 30 mg/day
  • Bipolar disorder (adults): Initial dose 15 mg/day, maximum 30 mg/day

Aripiprazole does not require dosage adjustment based on renal function, including in patients with severe renal impairment or end-stage renal disease (ESRD). This is

because aripiprazole is primarily metabolized in the liver and only a small fraction is excreted unchanged in the urine.

Side Effects[edit]

  • Detailed percentage-based side effect information not provided in the search results.
Frequency Adverse reactions
Common Insomnia: Difficulty sleeping, which often improves over time.
Anxiety and Restlessness: Feelings of anxiety and restlessness that usually subside with continued use
Dizziness
Headache: Common and can be managed with rest and hydration
Nausea and Vomiting: Can be mitigated by taking the medication with food
Constipation: Increasing dietary fiber and water intake can help
Dizziness: Often occurs when standing up quickly; getting up slowly can help
Weight Changes: Can cause weight gain or loss; maintaining a balanced diet is recommended
Increased Salivation: More common in children
Fatigue: Feeling tired or low in energy
Uncommon Neuroleptic Malignant Syndrome (NMS): Symptoms include high fever, muscle stiffness, and altered mental status
Metabolic Changes: Increased blood sugar, cholesterol, and weight gain, which can lead to diabetes
Compulsive Behaviors: Uncontrollable urges to gamble, eat, shop, or engage in sexual activities
Orthostatic Hypotension: Sudden drop in blood pressure upon standing, leading to dizziness or fainting
Seizures: Convulsions that require immediate medical attention
Severe Allergic Reactions: Symptoms include swelling of the face, lips, tongue, or throat, and difficulty breathing
Suicidal Thoughts: Increased risk in young people, particularly those under 24

Pharmacokinetics[edit]

  • Absorption
    • Aripiprazole is well absorbed after oral administration, with peak plasma concentrations occurring within 3 to 5 hours
  • Metabolism
    • Extensively metabolized in the liver, primarily by CYP3A4 and CYP2D6 enzymes
  • Elimination
    • The mean elimination half-life is about 75 hours for aripiprazole

Aripiprazole has a relatively rapid initial onset of action within 1 to 2 weeks for most patients, but full therapeutic effects may take several weeks to months to develop.

Its long half-life results in a prolonged duration of action, allowing for once-daily dosing and steady-state levels after about 2 weeks of treatment.

Drug Precautions[edit]

Increased risk in elderly patients

  • Should not be used to treat dementia-related psychosis in older adults due to increased risk of stroke and death
  • May cause drowsiness, dizziness, and difficulty swallowing in elderly patients, increasing the risk of falls and choking

Suicidal thoughts in young people

  • May increase the risk of suicidal thoughts in people under 24 years old, especially in the first few months of treatment or with dose changes
  • Close monitoring is required for children/teens taking aripiprazole

Monitoring Requirements

  • Monitor for suicidal thoughts and behaviors, especially in younger patients
  • May cause increased blood sugar, elevated cholesterol, and weight gain
  • Regular monitoring of metabolic parameters are recommended

Drug Interactions

  • Strong CYP3A4 inhibitors and CYP2D6 inhibitors may increase aripiprazole levels
  • Strong CYP3A4 inducers may decrease aripiprazole levels

FAQ[edit]

How Should I Take the Tablet?

  • Standard tablets: Swallow with water
  • Orodispersible tablets: Place on tongue to dissolve or dissolve in water and drink immediately
  • Take at around the same time each day, with or without food.

What should I avoid while taking?

  • Avoid driving, operating machinery or doing activities that require alertness until you know how the medication affects you.
  • Do not stop taking amisulpride suddenly without consulting your doctor. Abrupt withdrawal can cause unpleasant side effects or a return of symptoms.

What Happens if I Miss a Dose?

  • Take the missed dose as soon as you remember if it is within a few hours. If it is close to the next scheduled dose, skip the missed dose and continue with the regular schedule.
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