Amisulpride

Registered South African indications:

• Schizophrenia

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients 
• Breastfeeding
• Concomitant prolactin-dependent tumours
• Phaeochromocytoma 
• Children before the onset of puberty 
• Coadministration with levodopa  

Cautions

• Pregnancy 
• Renal impairment 
• Elderly 
• Abrupt withdrawal 
• Diabetes mellitus
• Epilepsy
• Parkinson's disease
• Withdrawal symptoms
• Cardiovascular disease
• QT prolongation 
• Risk factors for stroke 
• Dementia-related behavioural disturbances
• Risk factors for venous thromboembolism
• History or a family history of breast cancer
• Benign pituitary tumour
• Galactose intolerance
• Lapp lactase deficiency 
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: tab

Schizophrenia - acute 

• Oral (tab): 200-600mg, 12hrly; Max: 1200mg/24hrs

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For patients with mixed positive and negative symptoms, doses should be adjusted to obtain optimal control of positive symptoms

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Schizophrenia - predominantly negative symptoms

• Oral (tab): 50-100mg, dly

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Amisulpride can be administered once daily at oral doses up to 300mg, higher doses should be administered as 2 divided doses

Not established for use in children younger than 18 years

Pregnancy

• Caution
• In animals, amisulpride did not show direct reproductive toxicity. A decrease in fertility linked to the pharmacological effects of the agent (prolactin-mediated effect) was observed. No teratogenic effects of amisulpride were noted
• Very limited clinical data on exposed pregnancies are available. Therefore, the safety of amisulpride during human pregnancy has not been established. Use of the drug is not recommended during pregnancy unless the benefits justify the potential risks. For women of childbearing potential, effective contraception should be fully discussed with the physician prior to treatment
• Neonates exposed to antipsychotics (including amisulpride) during the third trimester of pregnancy are at risk of adverse reactions including extrapyramidal and/or withdrawal symptoms that may vary in severity and duration following delivery. There have been reports of agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, or feeding disorder. Consequently, newborns should be monitored carefully

Breastfeeding

• Contraindicated
• It is not known whether amisulpride is excreted in breast milk, breastfeeding is therefore contraindicated

Renal Impairment

• Caution; dose adjustment recommended
  eGFR ≥10-60ml/min: Reduce dose by 50%
  eGFR <10ml/min: Use is not recommended

Hepatic Impairment

• No dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Tremor
• Rigidity
• Akathisia
• Dyskinesia
• Acute dystonia
• Somnolence
• Tardive dyskinesia 
• Seizures
• Insomnia
• Anxiety
• Confusion
• Neuroleptic malignant syndrome 
• Neonatal drug withdrawal syndrome 

Cardiovascular Disorders

• Hypotension
• Bradycardia
• QT prolongation 
• Ventricular arrhythmias
• Cardiac arrest
• Venous thromboembolism

Respiratory Disorders

• Nasal congestion

Gastrointestinal Disorders

• Constipation
• Nausea and vomiting
• Dry mouth
• Hypersalivation 

Hepatobiliary Disorders

• Elevations of hepatic enzymes

Genitourinary Disorders

• Breast pain
• Erectile dysfunction
• Orgasmic dysfunction

Endocrine and Metabolic Disorders

• Increased plasma prolactin levels
• Hyperglycemia 
• Benign pituitary tumour 
• Dyslipidaemia
• Hyponatraemia
• Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
• Weight gain
• Galactorrhoea
• Amenorrhoea
• Gynaecomastia

Musculoskeletal  Disorders

• Osteopenia
• Osteoporosis

Skin and Subcutaneous Tissue Disorders

• Angioedema
• Urticaria

Immune, Blood and Lymphatic System Disorders

• Allergic reaction
• Leukopenia
• Neutropenia 
• Agranulocytosis 

Sensory Disorders

• Blurred vision

• Levodopa
• Alcohol
• Central nervous system depressants 
• Antihypertensive agents
• QT prolonging agents

None routine. Specific cases may require

• Blood glucose levels
• ECG
• Weight

Amisulpride binds selectively to dopaminergic D2 and D3 receptors in the limbic system. At low doses it preferentially blocks presynaptic D2 and D3 receptors, producing dopamine release responsible for its disinhibitory effects. At high doses, it blocks postsynaptic dopamine receptors thus inhibiting dopaminergic hyperactivity.

Tablet 200mg

• Solian (Sanofi) originator

Tablet 50mg 

• Solian (Sanofi) originator