Sulpiride

Registered South African indications:

• Schizophrenia

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Known or suspected phaeochromocytoma
• Pregnancy (200mg tab)
• Lactation
• Patients with bone marrow depression (200mg tab)
• Concurrent use with other medicines that may induce leucopenia and blood dyscrasias (200mg tab)
• Porphyria
• Concomitant prolactin-dependent tumours, e.g., pituitary gland prolactinomas and breast cancer
• Congenital QT prolongation
• Concomitant use with anti-Parkinson dopaminergic medicines
• Not recommended in hypomanic patients, in the manic or pre-manic phase of manic depressive psychosis or in patients with acute mania, as sulpiride may precipitate manic states, which can last up to 2 days in certain patients prone to these conditions. If this should occur, sulpiride may either be discontinued or, if the therapeutic effect is required not withstanding, sulpiride must be combined with sedative neuroleptics or other psychotropic medicines (50mg cap)

Contraindications registered in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients
• Phaeochromocytoma
• Acute porphyria
• Concomitant prolactin-dependent tumours e.g. pituitary gland prolactinomas and breast cancer
• Coadministration with  levodopa or antiparkinsonian drugs (including ropinirole)

South African recommendations

• Pregnancy (50mg tab) (South African recommendations)
• Pregnancy (Recommendations in other jurisdictions)
• Breastfeeding (Recommendations in other jurisdictions)
• Renal impairment
• Hepatic impairment
• Elderly
• Children 
• Hypomania 
• Abrupt withdrawal 
• Dementia 
• Risk factors for venous thromboembolism
• Breast cancer or family history thereof 
• Parkinson's disease
• History of epilepsy
• Unstable epilepsy
• Glaucoma
• Ileus
• Congenital digestive stenosis
• Urinary retention
• Prostate hyperplasia
• Risk factors for QT prolongation 
• Hypertension
• Risk factors for stroke 
• Galactose intolerance
• Lapp lactose deficiency
• Glucose-galactose malabsorption

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

South African registered indications and dosages

Schizophrenia
- For the management of acute episodes and the prevention of acute relapses in chronic cases

• Oral (cap, tab): Initial: 200-800mg, in divided doses 8-12hrly over a 24hr period; Treatment duration: 1-6 weeks; Maintenance: 600-800mg/day, in divided doses; Treatment duration: As long as necessary

Not established for use in children below 18 years

Pregnancy

South African recommendations

50mg capsule

• Caution; not recommended
• The safety of sulpiride in pregnancy has not been established

200mg tablet

• Contraindicated
• The safety and/or efficacy of sulpiride during pregnancy has not been established

Recommendations in other jurisdictions

• Caution; not recommended
• There are only very limited data available from the use of sulpiride in pregnant women. The safety of sulpiride during human pregnancy has not been established
• Sulpiride crosses the placenta. Studies in animals are insufficient with respect to reproductive toxicity
• The use of sulpiride is not recommended during pregnancy and in women of childbearing potential not using effective contraception, unless the benefits justify the potential risks
• Neonates exposed to antipsychotics (including sulpiride) 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

South African recommendations

• Contraindicated
• The safety and/or efficacy of sulpiride during lactation has not been established
• Sulpiride is excreted in breastmilk. Mothers on sulpiride should not breastfeed their infants

Recommendations in other jurisdictions

• Caution; not recommended
• Sulpiride is excreted into breastmilk in rather large amounts, far above the accepted value of 10% of the maternal weight-adjusted dosage in some cases, but blood concentrations in breastfed infants have not been evaluated
• There is insufficient information on the effects of sulpiride in newborns/ infants
• A decision must be made whether to discontinue breastfeeding or to abstain from sulpiride therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman

Fertility

South African recommendations

• No information available

Recommendations in other jurisdictions

• A decrease in fertility linked to the pharmacological effects of the drug (prolactin-mediated effect) was observed in treated animals

South African recommendations

• CrCl>60ml/min: Caution; no dose adjustment recommended
  As sulpiride is eliminated mainly unchanged in the urine, the pharmacokinetic parameters are altered in patients with impaired renal function
  There is a progressive diminution in the rate of elimination and an increase in half-life with decreasing renal function
• CrCl≤60ml/min: Caution; dose adjustment recommended
  There is a progressive reduction in the rate of elimination and an increase in half-life with decreasing renal function
  Recommended adjustments:
  CrCl 30-60ml/min: 70% of normal dose OR increase dosage interval between doses by a factor of 1.5
  CrCl 10-30ml/min: 50% of normal dose OR increase dosage interval between doses by a factor of 2
  CrCl≤10ml/min: 35% of normal dose OR increase dosage interval between doses by a factor of 3

Recommendations in other jurisdictions

• Mild to moderate: Caution; no dose adjustment recommended
• Severe: Caution; dose adjustment recommended
  GFR<30ml/min: Consider low doses; Titrate dose gradually; Monitor closely

South African recommendations

50mg capsule

• Caution; no information available

200mg tablet

• Caution; no dose adjustment recommended

Recommendations in other jurisdictions

• Caution; no information available

South African recommendations

• Caution; no dose adjustment recommended (CrCl>60ml/min)
• Caution; dose adjustment recommended (CrCl≤60ml/min)
  Plasma concentrations may be increased in elderly patients due to renal insufficiency
  Dose adjustment is based on renal function see renal impairment recommendations
  Elderly patients are more susceptible to postural hypotension, sedation and extrapyramidal effects. There is an increased mortality in elderly people with dementia who are treated with sulpiride
  Sulpiride is not indicated for the treatment of dementia-related behavioural disturbances

Recommendations in other jurisdictions

• Caution; no dose adjustment recommended
  The same dose ranges are applicable in the elderly, but the dose should be reduced if there is evidence of renal impairment

Central Nervous System Depressants

• Insomnia
• Confusion
• Sedation
• Drowsiness
• Parkinsonism
• Tremor
• Akathisia
• Hypertonia
• Dyskinesia
• Dystonia
• Neuroleptic malignant syndrome
• Hypokinesia
• Tardive dyskinesia
• Neonatal drug withdrawal syndrome 

Cardiovascular Disorders

• Ventricular arrhythmia
• Ventricular fibrillation
• Ventricular tachycardia
• Prolonged QT 
• Cardiac arrest
• Torsade de pointes
• Sudden death
• Orthostatic hypotension
• Venous embolism
• Pulmonary embolism
• Deep vein thrombosis

Respiratory Disorders

• Dyspnoea 

Gastrointestinal Disorders

• Salivary hypersecretion

Hepatobiliary Disorders

• Increased hepatic enzymes

Genitourinary Disorders

• Breast pain
• Galactorrhoea
• Breast enlargement
• Amenorrhoea
• Abnormal orgasm 
• Erectile dysfunction
• Gynaecomastia

Endocrine and Metabolic Disorders

• Hyponatraemia
• Syndrome of inappropriate antidiuretic hormone secretion
• Weight gain
• Hyperprolactinaemia 

Musculoskeletal Disorders

• Trismus
• Torticollis

Skin and Subcutaneous Tissue Disorders

• Maculopapula rash 
• Urticaria  

Immune, Blood and Lymphatic System Disorders

• Leukopaenia 
• Neutropaenia 
• Agranulocytosis 
• Anaphylaxis 

Sensory Disorders

• Oculogyric crisis

• Levodopa
• Antiparkinsonian agents 
• Ropinirole
• Central nervous system depressants 
• Beta blockers
• Calcium channel blockers 
• Clonidine 
• Digoxin
• Stimulant laxatives
• Potassium depleting diuretics
• IV amphotericin B
• Glucocorticoids 
• Tetracosactides
• Antiarrhythmic agents 
• Pimozide
• Haloperidol
• Methadone
• Imipramine antidepressants
• Lithium
• Cisapride
• Thioridazine
• IV erythromycin
• Halofantrine
• Pentamidine
• Antihypertensives 
• Antacids 
• Sucralfate

None routine. Specific cases may require

• Prolactin levels
• ECG
• Blood pressure

Sulpiride is a selective dopamine D2 antagonist. It does not exert effects on norepinephrine, acetylcholine, serotonin, histamine, or gamma-aminobutyric acid receptors.

Capsule 50mg 

• Eglonyl (Sanofi)
• Espiride (Pharmacare)
• Sandoz Sulpiride (Sandoz)
• Sulpiride 50 Oethmaan (Oethmaan Biosims)

Tablet 200mg 

• Bio-Sulpiride (Biotech)