Sulpiride

Drug Class: Antipsychotics, typical ; Antipsychotics, 1st Generation

Sulpiride (中文:[[ ]]) is a typical antipsychotic or 1st Generation antipsychotic medication. It is used in the treatment of psychosis associated with schizophrenia and major depressive disorder. In low dosage, it is used for anxiety and mild depression.

Pronunciation

Sulpiride 200mg

Sulpiride 50mg

Drug Names

Generic Name 藥名	HA Code 藥物代碼	Classification藥物分類
Sulpiride Cap 50 mg	SULP19	P1S1S3
Sulpiride Tab 200 mg	SULP20	P1S1S3

Mechanism of Action

Sulpiride is a selective antagonist at dopamine D2, D3 and 5-HT1A receptors. The presumed effectiveness of antipsychotic drugs relied on their ability to block dopamine receptors. This assumption arose from the dopamine hypothesis that maintains that both schizophrenia and bipolar disorder are a result of excessive dopamine activity.

Dosage

Indication	Dose
Schizophrenia with predominantly negative symptoms(flattening of affect, poverty of speech, apathy, as well as depression)	By mouth ADULT: 200 – 400 mg twice daily. Maximum 800 mg per day ELDERLY or debilitated patients: Lower initial dose to be given Increased gradually according to response
Schizophrenia with mainly positive symptoms(hallucinations, delusions, incongruity of speech) Respond to higher doses	By mouth ADULT: 200 – 400 mg twice daily Maximum 2.4 g per day ELDERLY or debilitated patients: Lower initial dose to be given Increased gradually according to response

Side Effects

Most serious and/or frequently occurring adverse effects of sulpiride include the following:

Endocrine disorders	Common: hyperprolactinaemia (elevated plasma levels of the hormone prolactin, which in turn lead to galactonrrhea, amornorrhea, gynecomastia etc)
Nervous system	Common: Sedation or drowsiness Extrapyramidal side effects -Tremor -Akathisia – a sense of inner restlessness that cannot stay still -Parkinsonism Anticholinergic side-effects such as: -Dry mouth -Constipation -Blurred vision Uncommon: Hypertonia Dyskinesia Rare: Oculogyric crisis Not known: Neuroleptic malignant syndrome Convulsion Tardive dyskinesia
Metabolism disorders	Not known: Hyponatraemia Syndrome of inappropriate antidiuretic hormone secretion (SIADH)
Cardiac disorders	Rare: Ventricular arrhythmia Ventricular fibrillation, or tachycardia Not known: Electrocardiogram QT prolonged
Vascular disorder	Uncommon: orthostatic hypotension
Gastrointestinal disorder	Common: constipation Uncommon: saliva hypersecretion
Breast disorder	Common: breast pain, galactorrhoea
	Common: weight gain

Pharmacokinetics

Oral bioavailability	Sulpiride is readily absorbed after oral doses.
Onset of action	Peak plasma concentrations are reached 3 – 6 hours after an oral dose.
Metabolism	It is metabolized in the liver
Elimination half-life	It is excreted in the urine and faeces. The elimination half-life is approximately 8 hours.

Drug Management

Monitoring

• Sulpiride does not affect blood pressure to the same extent as other antipsychotic drugs and so blood pressure monitoring is not mandatory for this drug.
• Careful monitoring is required in the elderly who are particularly susceptible to sedation, and extrapyramidal effects, chronic constipation, and possible prostatic hypertrophy.

Drug interaction

Sulpiride does not inhibits or stimulates cytochrome P450 enzymes, so would not cause clinically significant interactions with other drugs which are metabolized by CYPs.

Drugs given with sulpiride	Potential Effect
CNS-depressant drugs including alcohol, hypnotics, anxiolytics, sedative H1 antihistamines, central antihypertensives, baclofen, thalidomide and opioids.	Potentiates the sedative effect.
Lithium	Increased risk of extrapyramidal effects.
Tricyclic antidepressants such as amitriptyline, a CYP2D6 substrate, and pericyazine is potent inhibitor of CYP2D6.	Metabolism and elimination of tricyclics significantly decreased, increased toxicity such as anticholinergic and cardiovascular side effects.
Levodopa, Antiparkinsonian drugs (including ropinirole)	Antipsychotics with dopamine-blocking activity and dopaminergic drugs such as those used to treat parkinsonism may be mutually antagonistic.
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

• Sulpiride may increase prolactin levels. Therefore, caution should be exercised in patients with a history or a family history of breast cancer.
• In patients with impaired liver
• In patients with cardiovascular disorders, bradycardia, hypokalaemia or prolongation of QT, because of a risk of worsening of long QT-syndrome, which may also elevate the risk of tachycardia and sudden death.
• Concomitant use with QT prolonging drugs should be avoided
• In epileptics due to a possible lowering of the seizure threshold. The occurrence of convulsive seizures necessitates the discontinuation of treatment.
• In patients with a history of glaucoma, urine retention or hyperplasia of the prostate.

Contra-indications

Use of sulpiride should be avoided in individuals with:

• CNS depression
• Comatose states
• Parkinson’s disease
• Phaeochromocytoma
• Concomitant prolactin-dependent tumours e.g. pituitary gland prolactinomas and breast cancer

Hepatic impairment

• Can precipitate coma.

Renal impairment

• Start with small doses in severe renal impairment because of increased cerebral sensitivity.

Pregnancy

• Should be avoided in pregnancy.

Breast-feeding

• Use during breast feeding is not recommended.

Driving and skilled tasks

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.

FAQ

How should I take the tablet?

You will be prescribed the lowest dose needed to control your symptoms. Take with food. Food reduces irritation.

What should I avoid while taking?

Avoid drinking alcohol while taking sulpiride because it may enhance the side effects of sedation.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

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.