Amisulpride: Difference between revisions

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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
|-
| Insomnia
|-
| Anxiety and agitation
|-
| Sexual problems (e.g. difficulty with orgasm)
|-
| Excess saliva production
|-
| rowspan="9" | '''Uncommon
| Unexplained infections
|-
| Fast breathing
|-
| Sweating
|-
| High blood sugar (increased thirst, hunger, urination)
|-
|-
!style="text-align: left"| Muscle/Nervous system disorders:
| Breast pain or milk production (in women)
|
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
| Menstrual changes
|
Uncommon: hyperglycemia
Rare:
*Hyponatraemia
*Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
|-
|-
!style="text-align: left"| Cardiac disorders
| Heart rhythm changes (QT prolongation)
|
Common: hypotension
Rare:
*Ventricular arrhythmia
*Ventricular fibrillation, or tachycardia
*QT interval prolongation
|-
|-
!style="text-align: left"| Hypersensitivity reactions
| Low potassium levels
|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
| Neuroleptic malignant syndrome (high fever, muscle rigidity, altered mental state)
|
Common:
*weight gain
|}
|}
==Pharmacokinetics==
*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==
''' 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==
* Pheochromocytoma
* Prolactin-dependent tumors (e.g., prolactinoma, breast cancer)
* Movement disorders (e.g., Parkinson's disease, dementia with Lewy bodies)
==FAQ==
'''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.

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.