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[[Category: Drugs]][[Category: Antipsychotics, typical; Antipsychotic 2nd Generation]]
[[Category: Drugs]][[Category: Atypical antipsychotic ]]
'''Amisulpride'''(中文:[[     ]]) is an atypical antipsychotic or 2nd Generation antipsychotic medication. It is used to treat acute and chronic schizophrenia, in which
 
*positive symptoms (such as delusions, hallucinations, thought disorders) and/or
[[:Category: Antipsychotic Drug | '''Antipsychotic Drug''']]
*negative symptoms (such as blunted affect, emotional and social withdrawal) are prominent.
 
'''Drug class: [[:Category: Atypical antipsychotic  | Atypical Antipsychotic ]]
 
'''Amisulpride (SOLIAN)'''（中文：[[氨磺必利]]）


==Pronunciation==
==Pronunciation==
Line 11: Line 14:
[[File:Amisulpride 400mg.mp3]]
[[File:Amisulpride 400mg.mp3]]


==Drug Names==
==Common Strengths of Amisulpride Tablet==
{| class="wikitable"
Amisulpride tablets are available in the following strengths:
!Generic Name 藥名
*100 mg, 200 mg, 400 mg tablets
!HA Code 藥物代碼
 
!Classification藥物分類
==Drug Trade Names of Amisulpride Tablet==
|-
Solian
|Amisulpride Tab 100 mg
 
|AMIS01
==Drug Usage==
|P1S1S3
Amisulpride is used for:
|-
* Treatment of schizophrenia
|Amisulpride Tab 200 mg
|AMIS02
|P1S1S3
|-
|Amisulpride Tab 400 mg
|AMIS04
|P1S1S3
|}


==Mechanism of Action==
==Mechanism of Action==
Amisulpride selectively blocks dopamine D2 receptors in the brain.  
Amisulpride is a selective dopamine D2 and D3 receptor antagonist. At low doses, it selectively binds to presynaptic dopamine autoreceptors, while at high doses, it preferentially binds to post-synaptic dopamine receptors. This explains its effectiveness in treating both negative and positive symptoms of schizophrenia.
It has no affinity for serotonic, α-adrenergic, histamine H1 and cholinergic receptors.
The effectiveness of amisulpride in treating the negative symptoms of schizophrenia is due to its blockade of the presynaptic dompamine D2 receptors. By blocking them amisulpride increases dopamine concentrations in the synapse. This increased dopamine is theorized to act on dopamine D1 receptors to relieve the negative symptoms of schizophrenia.


==Dosage==
==Route of Administration==
{| class="wikitable"
* Oral (tablets and oral solution)
!style="text-align: left"| Indication
!style="text-align: left"| Dose
|-
!style="text-align: left"| Acute psychotic episode in Schizophrenia 
|By ''mouth
ADULT:
*400 - 800 mg daily in 2 divided doses, adjusted according to response;
*Maximum 1.2 g per day
|-
!style="text-align: left"| Schizophrenia with predominantly negative symptoms
|By ''mouth
ADULT:
*50 – 300 mg daily
|}


How long does it take for Amisulpride to work?
==Dosages==
* Schizophrenia: 400 - 800 mg/day orally, divided into two doses.


The patient may start to feel better in a short time but it can take as long as 6 to 8 weeks before the benefits of this medicine is noticed.
Renal dose based on eGFR:
For  severe renal impairment (eGFR <30 mL/min/1.73 m2): Use is not recommended


==Side Effects==
==Side Effects==
It produces a moderate degree of extrapyramidal symptoms (EPS. These symptoms include:
{| class="wikitable"
*Drooling/trouble swallowing
!style="text-align: left"| Frequency
*Restlessness/constant need to move
!Adverse reactions
*Shaking (tremor)
|-
*Shuffling walk
| rowspan="12" | '''Common
*Stiff muscles
| Drowsiness/sleepiness
*Severe muscle spasms/cramping (such as twisting neck, arching back, eyes rolling up)
|-
*Mask-like expression of the face
| Weight gain
*Tardive dyskinesia (any uncontrollable movements such as lip smacking, mouth puckering, tongue thrusting, chewing, or unusual arm/leg movements
|-
 
| Dizziness
Other adverse effects include the following:
|-
{| class = "wikitable"
| Increased appetite
!style="text-align: left"| Endocrine disorders
|-
|  
| Nausea and vomiting
Common: hyperprolactinaemia (elevated levels of the hormone prolactin, which for females may result in
|-
*Galactorrhea (unwanted breast milk)
| Constipation
*amornorrhea (missed/stopped periods),
|-
For males it may result in
| Dry mouth
*decreased sexual ability, or
|-
*gynecomastia (enlarged breast)
| Blurred vision
Rare: benign pituitary tumour such as prolactinoma
|-
|-
!style="text-align: left"| Muscle/Nervous system disorders:
| Insomnia  
|
Common:
*Extrapyramidal symptoms (EPS)
-Tremor
-Akathisia
-Parkinsonism
-hypersalivation
*Anticholinergic side-effects such as:
-Dry mouth
-Constipation
-Blurred vision
*Insomnia
*Anxiety
*Agitation
*Nausea and vomiting
Uncommon: tardive dyskinesia and seizures
Rare:
*Neuroleptic malignant syndrome
|-
|-
!style="text-align: left"| Metabolism disorders
| Anxiety and agitation
|
Uncommon: hyperglycemia
Rare:
*Hyponatraemia
*Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
|-
|-
!style="text-align: left"| Cardiac disorders
| Sexual problems (e.g. difficulty with orgasm)
|
Common: hypotension
Rare:
*Ventricular arrhythmia
*Ventricular fibrillation, or tachycardia
*QT interval prolongation
|-
|-
!style="text-align: left"| Hypersensitivity reactions
| Excess saliva production
|Increased sensitivity to the sun or notice symptoms of sunburn (such as redness, swelling, blistering) which may occur more quickly than normal
|-
|-
!style="text-align: left"| Investigations
| rowspan="9" | '''Uncommon
|
| Unexplained infections
Common:
*weight gain
|}
 
==Pharmacokinetics==
{|class="wikitable"
!style="text-align: left"| Oral bioavailability
|It is readily absorbed after oral doses.
|-
|-
!style="text-align: left"| Onset of action
| Fast breathing
|It shows two absorption peaks: one is attained rapidly, one hour post-dose and a second between 3 and 4 hours after administration.
Peak plasma concentrations are reached 1.5 – 6 hours after an oral dose.
|-
|-
!style="text-align: left"| Metabolism
| Sweating
|It is metabolized in the liver
|-
|-
!style="text-align: left"| Elimination half-life
| High blood sugar (increased thirst, hunger, urination)
|
It is predominantly eliminated in the urine.
 
The elimination half-life is approximately 12 hours.
|}
 
==Drug Management==
===Monitoring===
The following populations must be closely monitored after administration of amisulpride:
*Elderly persons with susceptibility to drowsiness, confusion, and unsteadiness, which may increase the risk of fall
*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 should get monitoring blood sugar levels during treatment.
*May cause increased susceptibility to sunburn and individuals should avoid undue exposure to direct sunlight.
*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. Ampisulpride 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
-An absence of monthly periods for 6 months or more
 
===Drug interaction===
The most common interactions encountered with amisulpride result from use with drugs that have similar pharmacological actions, for example:
 
Amisulpride may aggravate Parkinsonism and antagonize the action of levodopa.
{| class="wikitable"
!style="text-align: left"| Drugs given with amisulpride
!style="text-align: left"| Potential Effect
|-
|-
|style="text-align: left"|
| Breast pain or milk production (in women)
*CNS-depressant drugs including alcohol, hypnotics, anxiolytics, sedative H1 antihistamines, central antihypertensives, baclofen, thalidomide and opioids.
|
Potentiates the sedative effect.
|-
|-
|style="text-align: left"|
| Menstrual changes
*Antipsychotics such as clozapine
|
Imprudent to combine antipsychotics due to additive risk for tardive dyskinesia and neuroleptic malignant syndrome.
|-
|-
|style="text-align: left"|
| Heart rhythm changes (QT prolongation)
*Lithium
|Increased risk of extrapyramidal side-effects when antipsychotics given with lithium.
|-
|-
|style="text-align: left"|
| Low potassium levels
*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"|
| Neuroleptic malignant syndrome (high fever, muscle rigidity, altered mental state)
*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 impaired liver, kidney, and cardiovascular function
*Onset Time
*In patients with a history of jaundice, parkinsonism
**1 to 4 hours after oral administration; immediate after IV administration.
*In those with diabetes mellitus
*Metabolism
*In patients with paralytic ileus
**Amisulpride undergoes minimal metabolism
*In patients with prostatic hyperplasia or urinary retention
*Elimination
*The elderly, especially those with dementia.
** Amisulpride is primarily eliminated unchanged in the urine
** The elimination half-life is approximately 12 hours
** Duration of Action: Approximately 12 hours based on the elimination half-life, with sustained therapeutic effects for long-term treatment in chronic conditions like schizophrenia.
 
A person should begin to feel better within six weeks of starting antipsychotic medication.
 
However, it may take several months before they feel the full benefits.
 
==Drug Precautions==
''' Pregnancy
 
Insufficient data on use during pregnancy to establish risk
 
''' Breastfeeding
 
Contraindicated during breastfeeding
 
'''Children and Elderly
*Not recommended for use in children under 18 years old
*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
 
'''Renal Imapirment
 
Dose adjustments are necessary for patients with renal insufficiency.
 
'''QT Prolongation


===Contra-indications===
Amisulpride can cause dose- and concentration-dependent prolongation of the QT interval, which can lead to serious ventricular arrhythmias like torsades de pointes. It should be avoided in patients with congenital long QT syndrome and those taking other drugs that prolong the QT interval (e.g., droperidol, ondansetron).
Use of amisulpride should be avoided in individuals with:
*CNS depression
*Comatose states
*Phaeochromocytoma
*Prolactin-dependent tumours e.g. prolactinoma, breast cancer


===Hepatic impairment===
'''Abrupt Withdrawal
Since the drug is weakly metabolized a dosage reduction should not be necessary


===Renal impairment===
Should not be stopped abruptly to avoid withdrawal symptoms such as nausea, vomiting, insomnia, and the recurrence of psychotic symptoms
*Halve dose with creatinine clearance between 30 – 60 ml/minute
*Use one-third dose with creatinine clearance between 10 – 30 ml/minute


===Pregnancy===
'''Monitoring Requirements
Should be avoided in pregnancy.
*Blood glucose monitoring as it may cause elevated blood glucose levels.
*ECG Monitoring: Recommended for patients with preexisting arrhythmias, cardiac conduction disorders, electrolyte imbalances (e.g., hypokalemia, hypomagnesemia), and congestive heart failure.


===Breast-feeding===
'''Drug Interaction
Use during breast feeding should be avoided.
*Dopamine Agonists: Reciprocal antagonism with dopamine agonists (e.g., levodopa); concurrent use should be avoided.
*Other QT-Prolonging Drugs: Avoid coadministration with other drugs known to prolong the QT interval.


===Driving and skilled tasks===
==Contraindications==
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.
* Pheochromocytoma
* Prolactin-dependent tumors (e.g., prolactinoma, breast cancer)
* Movement disorders (e.g., Parkinson's disease, dementia with Lewy bodies)


==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 6 to 8 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?===
Swallow the tablets whole with a full glass of water. Do not chew, crush or break the tablets
Avoid drinking alcohol while taking trifluoperazine because it may enhance the side effects of sedation.
 
'''What should I avoid while taking?
* Amisulpride may cause drowsiness, dizziness or blurred vision, especially when you first start taking it. 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.
 
* Be cautious about getting overheated or dehydrated, as amisulpride can affect your body's ability to regulate temperature.
 
'''What Happens if I Miss a Dose?


Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.
Answer not provided in the given information. If you miss a dose, take it as soon as you remember. However, if it's almost time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one.
===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.

Latest revision as of 21:08, 14 July 2024


Antipsychotic Drug

Drug class: Atypical Antipsychotic

Amisulpride (SOLIAN)（中文：氨磺必利）

Pronunciation[edit]

Amisulpride 100mg[edit]

Amisulpride 400mg[edit]

Common Strengths of Amisulpride Tablet[edit]

Amisulpride tablets are available in the following strengths:

  • 100 mg, 200 mg, 400 mg tablets

Drug Trade Names of Amisulpride Tablet[edit]

Solian

Drug Usage[edit]

Amisulpride is used for:

  • Treatment of schizophrenia

Mechanism of Action[edit]

Amisulpride is a selective dopamine D2 and D3 receptor antagonist. At low doses, it selectively binds to presynaptic dopamine autoreceptors, while at high doses, it preferentially binds to post-synaptic dopamine receptors. This explains its effectiveness in treating both negative and positive symptoms of schizophrenia.

Route of Administration[edit]

  • Oral (tablets and oral solution)

Dosages[edit]

  • Schizophrenia: 400 - 800 mg/day orally, divided into two doses.

Renal dose based on eGFR:

For severe renal impairment (eGFR <30 mL/min/1.73 m2): Use is not recommended

Side Effects[edit]

Frequency Adverse reactions
Common Drowsiness/sleepiness
Weight gain
Dizziness
Increased appetite
Nausea and vomiting
Constipation
Dry mouth
Blurred vision
Insomnia
Anxiety and agitation
Sexual problems (e.g. difficulty with orgasm)
Excess saliva production
Uncommon Unexplained infections
Fast breathing
Sweating
High blood sugar (increased thirst, hunger, urination)
Breast pain or milk production (in women)
Menstrual changes
Heart rhythm changes (QT prolongation)
Low potassium levels
Neuroleptic malignant syndrome (high fever, muscle rigidity, altered mental state)

Pharmacokinetics[edit]

  • Onset Time
    • 1 to 4 hours after oral administration; immediate after IV administration.
  • Metabolism
    • Amisulpride undergoes minimal metabolism
  • Elimination
    • Amisulpride is primarily eliminated unchanged in the urine
    • The elimination half-life is approximately 12 hours
    • Duration of Action: Approximately 12 hours based on the elimination half-life, with sustained therapeutic effects for long-term treatment in chronic conditions like schizophrenia.

A person should begin to feel better within six weeks of starting antipsychotic medication.

However, it may take several months before they feel the full benefits.

Drug Precautions[edit]

Pregnancy

Insufficient data on use during pregnancy to establish risk

Breastfeeding

Contraindicated during breastfeeding

Children and Elderly

  • Not recommended for use in children under 18 years old
  • 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

Renal Imapirment

Dose adjustments are necessary for patients with renal insufficiency.

QT Prolongation

Amisulpride can cause dose- and concentration-dependent prolongation of the QT interval, which can lead to serious ventricular arrhythmias like torsades de pointes. It should be avoided in patients with congenital long QT syndrome and those taking other drugs that prolong the QT interval (e.g., droperidol, ondansetron).

Abrupt Withdrawal

Should not be stopped abruptly to avoid withdrawal symptoms such as nausea, vomiting, insomnia, and the recurrence of psychotic symptoms

Monitoring Requirements

  • Blood glucose monitoring as it may cause elevated blood glucose levels.
  • ECG Monitoring: Recommended for patients with preexisting arrhythmias, cardiac conduction disorders, electrolyte imbalances (e.g., hypokalemia, hypomagnesemia), and congestive heart failure.

Drug Interaction

  • Dopamine Agonists: Reciprocal antagonism with dopamine agonists (e.g., levodopa); concurrent use should be avoided.
  • Other QT-Prolonging Drugs: Avoid coadministration with other drugs known to prolong the QT interval.

Contraindications[edit]

  • Pheochromocytoma
  • Prolactin-dependent tumors (e.g., prolactinoma, breast cancer)
  • Movement disorders (e.g., Parkinson's disease, dementia with Lewy bodies)

FAQ[edit]

How Should I Take the Tablet?

Swallow the tablets whole with a full glass of water. Do not chew, crush or break the tablets

What should I avoid while taking?

  • Amisulpride may cause drowsiness, dizziness or blurred vision, especially when you first start taking it. 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.
  • Be cautious about getting overheated or dehydrated, as amisulpride can affect your body's ability to regulate temperature.

What Happens if I Miss a Dose?

Answer not provided in the given information. If you miss a dose, take it as soon as you remember. However, if it's almost time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one.

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