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sulpiride

Sulpiride is an atypical antipsychotic drug, belonging to the class of benzamidic derivatives. It is a neuroleptic drug, that is, a drug that can strongly depress the central nervous system.

Sulpiride - Chemical Structure

Its chemical structure is analogous to that of metoclopramide, an antiemetic drug (that is, antivomito).

Indications

For what it uses

The use of sulpiride is indicated for the treatment of:

  • Chronic and acute psychoses, such as schizophrenia and bipolar disorder;
  • Anxious-depressive psycho-neurosis with cenestopathy and somatization.

Warnings

Sulpiride should be used with caution in manic states and in the manic phases of anxiety-depressive psychoneurosis. In these cases, association with a sedative may be helpful.

Since sulpiride is excreted renally, attention should be paid to the administration of the drug in patients with renal insufficiency.

Particular caution should be used in the administration of sulpiride in patients suffering from Parkinson's disease; furthermore, these patients must be constantly monitored.

Because sulpiride can cause convulsive seizures, patients with epilepsy - or a history of seizure disorders - must be carefully monitored.

Much attention must be paid to the administration of sulpiride in patients suffering from arterial hypertension, heart failure, in patients suffering from cardiovascular diseases or who have a family history of prolongation of the QT interval (the interval of time necessary for the ventricular myocardium to depolarize and repolarize).

An increased risk of cerebrovascular events has been observed in patients with dementia and treated with sulpiride.

Much caution should be used in the administration of sulpiride in patients who have a high risk of stroke.

Since sulpiride can promote thrombus formation, the drug should be administered with caution in patients with a clinical history - including family history - of thrombosis.

Sulpiride can cause neuroleptic malignant syndrome (SNM), in which case it is necessary to immediately stop treatment with the drug.

In patients with aggressive behavior or agitation with impulsivity, sulpiride should be administered in combination with a sedative.

Sulpiride can cause an increase in the glycemic rate, so diabetic patients - or those at risk of diabetes - must be monitored.

Since sulpiride can cause a decrease in white blood cell levels in the bloodstream, these levels must be regularly monitored.

Sulpiride could cause adverse effects that could affect the ability to drive and use machines.

Interactions

Simultaneous intake of sulpiride and other neuroleptics should be avoided.

Sulpiride is able to enhance the action of drugs, such as, hypotensive, antihypertensive, hypnotic, tranquilizers, anesthetics and analgesics .

Concurrent administration of sulpiride and drugs that prolong the QT interval increases the risk of developing cardiac arrhythmias. Among these drugs, we recall:

  • β-blockers ;
  • Calcium channel blockers, such as verapamil and diltiazem ;
  • Clonidine, an antihypertensive drug;
  • Digitalici ;
  • Antiarrhythmics, such as - for example - quinidine and amiodarone ;
  • Other antipsychotics, such as pimozide, haloperidol and thioridazine ;
  • Antidepressants, such as - for example - imipramine ;
  • Erythromycin, an antibiotic;
  • Alofantrine, an antimalarial drug.

Sulpiride should not be administered concomitantly with drugs that cause alterations in the concentration of electrolytes, such as:

  • Diuretics that induce hypokalemia (ie that reduce blood levels of potassium);
  • Laxatives ;
  • Amphotericin B, an antifungal;
  • Glucocorticoids ;
  • Tetracosactide, a synthetic analogue of the adrenocorticotropic hormone.

Alcohol potentiates the sedative effect of sulpiride, so this association must be avoided.

The absorption of sulpiride decreases in case of concomitant administration of antacid drugs or sucralfate (a cytoprotective agent used in the treatment of duodenal and gastric ulcers).

Co-administration of sulpiride and lithium increases the risk of extrapyramidal side effects (Parkinson's-like symptoms).

Side effects

Sulpiride can induce many side effects, but not all patients manifest them. This is due to the different sensitivity that each individual has towards the drug.

The following are the main side effects that may occur following sulpiride therapy.

Cardiac disorders

Treatment with sulpiride can cause arrhythmias, ventricular tachycardia, atrial fibrillation, prolongation of the QT interval and cardiac arrest. Cases of sudden death have also occurred.

Vascular pathologies

Sulpiride therapy can cause orthostatic hypotension, which is the sudden drop in blood pressure when moving from a lying or sitting position to an upright position.

In addition, the drug can cause even fatal venous thromboembolism (including pulmonary embolism), deep vein thrombosis and hypertension.

Endocrine disorders

Treatment with sulpiride may induce hyperprolactinemia, ie an increase in the blood concentration of the hormone prolactin.

Gastrointestinal disorders

Sulpiride can cause nausea, dry mouth and hypersalivation.

Hepatobiliary disorders

Treatment with sulpiride can cause increased levels of liver enzymes in the bloodstream.

Nervous system disorders

Sulpiride therapy may favor the onset of:

  • Sedation;
  • Drowsiness;
  • Sleep disorders;
  • Extrapyramidal symptoms;
  • Tremors;
  • Akathisia (psychomotor syndrome characterized by the inability to remain still);
  • Hypertonia;
  • Dyskinesia;
  • Dystonia;
  • hypokinesia;
  • Tardive dyskinesia, observed after about three months of treatment;
  • Convulsions.

Malignant Neuroleptic Syndrome

Neuroleptic Malignant Syndrome is a neurological disorder characterized by:

  • Temperature;
  • Dehydration;
  • Muscle stiffness;
  • akinesia;
  • Sweating;
  • Tachycardia;
  • Arrhythmia;
  • Changes in the state of consciousness that can progress to stupor and coma.

In the event of such symptoms appearing, it is necessary to immediately stop therapy with sulpiride and immediately contact the doctor who will start a symptomatic supportive therapy.

Reproductive system and breast disorders

Treatment with sulpiride can cause pain and / or breast augmentation, galactorrhea (abnormal milk secretion) both in women and men, amenorrhea (absence of the menstrual cycle), abnormal orgasm and erectile dysfunction. Cases of gynecomastia, ie breast development in men, have also been reported.

Allergic reactions

The intake of sulpiride in sensitive subjects can trigger allergic reactions. These reactions can occur in the form of hives, dyspnea, hypotension and anaphylactic shock.

Blood and lymphatic system disorders

Sulpiride therapy can cause disorders of the hemolymphopoietic system, the system responsible for the production of blood cells. These disorders can lead to a decrease in blood levels of white blood cells, with a consequent increased susceptibility to the contraction of infections.

Other side effects

Other adverse effects that may arise from taking sulpiride are:

  • Insomnia;
  • Confusion;
  • Maculopapular rash;
  • Spasmodic torticollis;
  • Trismus (spastic contracture of the jaw muscles).

Overdose

There is no specific antidote in case of overdose with sulpiride, therefore the therapy is only symptomatic and supportive. Hemodialysis may be useful, thanks to which the sulpiride can be partially removed from the body.

Symptoms that may appear following an overdose of medication consist of dyskinetic manifestations with spasmodic torticollis, tongue protrusion, trismus. In some cases, severe parkinsonian syndrome and coma may occur.

If you suspect a overdose of sulpiride, you must contact a doctor immediately and contact the nearest hospital.

Action mechanism

The pathogenesis of schizophrenia is still not entirely clear today. However, it appears that the mesolimbic and mesocortic dopaminergic pathways (ie the neuronal pathways that exploit the dopamine neurotransmitter) are implicated in the etiology of this psychiatric disease.

Sulpiride is a dopamine D2 receptor antagonist, both centrally and peripherally, and it is this action of its own that gives it antipsychotic properties.

Mode of Use - Posology

Sulpiride can be administered orally in the form of tablets or capsules. Different dosages are available. The drug is also available in vials for intramuscular administration.

The dosage of sulpiride must be established by the doctor on an individual basis.

The dosages of the drug normally used are given below.

In any case, it is advisable never to exceed the maximum dose of 1 g of sulpiride per day.

In elderly patients a decrease in the amount of drug administered may be necessary and the maximum daily dose is decreased to 300 mg.

Oral administration

The dose of sulpiride usually used varies from 150 mg to 600 mg of drug per day, to be administered in divided doses. The doctor may decide to change the dosage according to the patient's response to therapy.

Intramuscular administration

This type of administration is used in the therapy of attack of acute and chronic psychoses. The usual dose is 200-300 mg of sulpiride per day, to be administered in divided doses.

Pregnancy and breastfeeding

In newborns whose mothers took sulpiride in the last trimester of gestation symptoms such as tremor, muscle stiffness, muscle weakness, drowsiness, agitation, respiratory problems and difficulty in food intake may occur.

Furthermore, sulpiride is excreted in breast milk and can cause serious harm to the infant.

For the reasons mentioned above, the use of sulpiride by pregnant women - established or presumed - and by mothers who are breast-feeding, should be avoided.

Contraindications

The use of sulpiride is contraindicated in the following cases:

  • Known hypersensitivity to sulpiride;
  • In patients with pheochromocytoma, a type of tumor that affects the adrenal gland;
  • In patients suffering from prolactinomas (tumors of the pituitary gland that induce an increase in prolactin secretion) and mammary tumors;
  • In patients taking levodopa and other anti-Parkinson drugs;
  • In patients suffering from acute porphyria (a rare disease due to the alteration of the activity of an enzyme involved in the synthesis of the haem group present in hemoglobin);
  • In pediatric patients;
  • In pregnancy, ascertained or presumed;
  • During breastfeeding.

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