Sulpiride belongs to the group of atypical neuroleptics. In addition to its official use listed in the safety data sheet, it also has off-lebel applications, i.e. it is used to treat diseases other than those listed in the leaflet.

Sulpiryd - action

Sulpiride is used to treat schizophrenia . In this disease, the patient has two types of symptoms:

  • so-called positive (productive) symptoms:
    • hallucinations,
    • hallucinations,
    • delusions,
    • thinking disorder
  • and the so-called negative symptoms, that is:
    • apathy,
    • reticence,
    • no contact with the environment,
    • anhedonia.

It is assumed that disorders of dopaminergic transmission in the brain lie at the root of schizophrenia. In some parts of it, dopaminergic transmission is increased and leads to positive symptoms, while in some parts the dopamine receptors are underactive, which results in negative symptoms.

Sulpiride is a D2 receptor antagonist . It is rather weak compared to other antipsychotics. The safety profile of sulpiride is comparable to that of other neuroleptics.

Sulpiride was assumed to be selective for the D2 receptor in early laboratory studies, while later it was found to be active on D3 and D4 receptors.

Most sources, however, describe sulpiride as selective for the D2 receptor. However, it has no effect on the receptors:

  • D1,
  • cholinergic,
  • adrenergic,
  • gabaergiczne,
  • histamine
  • or serotonin.

The oral bioavailability of sulpiride is low and ranges between 33-35%. Sulpiride poorly crosses the blood-brain barrier, which is related to its lipophilicity. You might be tempted to say that thanks to this, it causes fewer side effects on the part of the central nervous system.

Unfortunately, among the second-generation atypical neuroleptics, sulpiride most often causes extrapyramidal side effects in the form of drug-induced parkinsonism and tremors.

Sulpiride works in two ways anddependent on the dose.

In small doses, sulpiride has an antidepressant effect , which can be noticed after a few days of therapy. However, this is not its most common use, as it loses ground to SSRIs in treating depression.

In high doses, sulpiride inhibits the acute symptoms of schizophrenia. Despite the fact that it causes extrapyramidal side effects, they are not as strongly marked as in the case of classic neuroleptics, e.g. phenothiazines. Therefore, it is one of the most commonly used atypical medications to treat acute symptoms of schizophrenia.

Sulpiride has another effect that is particularly appreciated by gastroenterologists. Namelythis drug improves the secretion of mucus by the gastric and duodenal mucosa and has an anti-emetic effect . It is for this reason that this drug has been used in the treatment of gastro-oesophageal reflux disease and peptic ulcer disease.

Doctors prescribe sulpiride along with other medications treating these diseases as an adjunctive therapy. In this case, sulpiride is prescribed in small doses, much lower than during antipsychotic therapy. This use of sulpiride is not officially registered.

Sulpiride is also used to treat migraines and Tourett's syndromeoutside of official treatment regimens.

Sulpiryd - indications

According to the safety data sheet, sulpiride is recommended in the treatment of acute and chronic psychoses occurring in schizophrenia, especially if they are associated with symptoms of impaired activity.

This drug is also used to treat depression when other antidepressants do not have a therapeutic effect or cannot be used to treat the patient for some reason.

Sulpiryd - dosage

The treatment of schizophrenia is long-lasting and constitutes a challenge for both the patient and the attending physician.

According to the official treatment regimen, the treatment of schizophrenia is divided into 3 stages:

  • acute phase therapy,
  • stabilization therapy phase,
  • maintenance phase.

The main goals of treatment are:

  • relapse prevention,
  • reducing the severity of schizophrenia symptoms
  • and improvement of the patient's quality of life.

Each of these phases has a different duration. However, the patient should be made aware of the fact that the treatment of schizophrenia is continuous, and the attempts to use intermittent therapy have not brought positive results. Unfortunately, pharmacological treatment of schizophrenia is the therapy of first choice and so farthe only effective one.

It has been assumed that the risk of side effects of antipsychotic drugs is greater in patients who have experienced an episode of schizophrenia only once than in those who have had multiple psychotic episodes. Therefore, the dose of neuroleptics in patients with the first symptoms should be lower than in patients with an acute relapse of schizophrenia.

From theresult above, the starting dose for the treatment of schizophrenia is 400 to 800 mg / day . The dose is divided into morning and evening (depending on symptoms).

It is not recommended to take sulpiride just before going to bed as it may be difficult for the patient to fall asleep (the drug may have a stimulating effect).

In patients with more positive symptoms, higher doses are recommended, but if most of the patient's symptoms are negative, the amount may be smaller. The maximum dose of sulpiride is 1,200 mg.

When treating depression, the recommended dose of sulpiride is 150 to 300 mg . Treatment is started with 50 mg and then the supply of the drug is gradually increased depending on the effect of the drug on the patient.

In patients with impaired renal function, the amount of the administered drug should be reduced. The percentage by which the dose should be reduced depends on the condition of the patient's kidneys and is directly determined by the physician. Such patients should have their kidneys checked regularly by means of laboratory tests.

In people with liver failure or liver dysfunction, theoretically, no dose adjustment is required. However, the treatment of such a patient requires caution, because one of the side effects of sulpiride is an increase in liver enzymes. Laboratory tests should be carried out systematically during the treatment of this group of patients.

Dosage for treating Tourett's syndrome starts at 50 mg . Thereafter, the amount of the drug is gradually increased up to the recommended therapeutic dose of 200-400 mg. Treatment of tics is only symptomatic and no current medication is effective in all patients. Antipsychotic drugs only reduce tics to around 50%. Additionally, sulpiride in patients with Tourett's syndrome causes:

  • calming down,
  • reduction of obsessive-compulsive symptoms
  • and acts as an antidepressant.

In gastroenterological treatment, the doses of the drug are approx. 50-100 mg . So they are much smaller than those used in the treatment of mental diseases and disorders. As a result, the risk of side effects from the central systemnervous system is slight.

There are studies that show high effectiveness of ulcer therapy with sulpiride in combination with antacids. Sulpiride should be taken at least 2 hours apart after taking antacids.

Sulpiride should be taken orally, one hour before or two hours after a meal.

Sulpiryd - contraindications

Do not take sulpiride if you are hypersensitive to the active ingredient.

Do not take the drug:

  • in case of diagnosis or suspicion of a phaeochromocytoma,
  • if the patient suffers from severe porphyria,
  • if a patient has tumors that cause excessive secretion of prolactin (pituitary adenoma or breast cancer), it should be emphasized here that in animal studies an increased risk of breast cancer in female rats was noted. Such an action has not been documented in humans.
  • with the simultaneous use of levodopa, it is associated with the antagonizing effect of both drugs. The therapy in this case will not be effective.
  • while breastfeeding or during pregnancy,
  • in children under the age of 14.

If a patient suffers from Parkinson's disease, consider the use of sulpiride. The physician should estimate the risk-to-benefit ratio of the therapy.

Since sulpiride may cause drug-induced parkinsonism, increase tremors in a patient and reduce the effectiveness of drugs used in the treatment of Parkinson's, its use in this group of patients is not recommended.

Sulpiride - precautions and drug interactions

One of the most serious complications of taking sulpiride is the neuroleptic malignant syndrome. It is an individual reaction and affects approximately 0.1% of patients treated with this substance. However, it is a serious condition that cannot be ignored and requires immediate diagnosis and hospitalization.

Full-blown neuroleptic malignant syndrome (NMS) develops within 24-72 hours of the first signs of an abnormal response . NMS belongs to the hyperthermia syndrome whose major symptoms are:

  • fever above 38.5 degrees Celsius,
  • muscle stiffness described as a symptom of a lead tube,
  • increased activity of phosphocreatine kinase.

Minor symptoms are:

  • tachycardia,
  • abnormal blood pressure,
  • increased sweating,
  • disturbance of consciousness.

It should be emphasized, however, that the risk of death in patientstaking atypical neuroleptics such as sulpiride is lower than in patients taking classic antipsychotics. If this adverse reaction occurs, the drug should be discontinued immediately and the patient hospitalized.

If a high temperature occurs in a patient treated with sulpiride, the drug should be discontinued and the cause of the fever should be determined.

It has been noted in clinical trials thatelderly people treated with sulpiride are more likely to experience side effects such as drug-induced parkinsonism . This situation is explained by the fact that with age dopamine nerve cells of the nigrostrial system degenerate, which is an additional factor predisposing to extrapyramidal symptoms such as Parkinson's or tremors.

In addition, older people are more likely to experience kidney problems, which makes it necessary to reduce the dose in this group of patients.

Another study investigating the treatment of gastroenterological disorders involving sulpiride found that possible extrapyramidal side effects were more common in women than in men.

It has been theorized that the cause of this phenomenon is estrogen, which reduces the expression of dopamine receptors. Of course, this hormone is present in greater amounts in women than in men. No official research confirming the validity of this theory has been published.

Sulpiride should be discontinued with caution aswithdrawal symptoms have been documented after long-term treatment . These include:

  • nausea,
  • vomiting,
  • sweating,
  • insomnia.

If you stop taking it, you may also experience a relapse of the disease originally treated with sulpiride. The patient should not make the decision alone to discontinue the preparation. The drug should be discontinued by the physician after a case analysis in a gradual manner, providing the patient with an alternative treatment.

Neuroleptics, including sulpiride, can lower the seizure threshold . These drugs should be used with caution together with other drugs that work in a similar manner. If a patient has a history of seizures or a medical history has diagnosed a predisposition to seizures, sulpiride should be used with caution in this patient.

If a doctor decides to include sulpiride in the therapy of a patient suffering from epilepsy, he should not reduce the doses of antiepileptic drugs in favor of sulpiride.

Sulpiride may lengthen the QT interval on the EKG trace. Caution should be exercised when using sulpiride in cariological patients and patients taking the following drugs:

  • beta blockers,
  • calcium channel blockers,
  • medications containing digitalis,
  • diuretics,
  • laxatives,
  • glucocorticoids,
  • amphotericin B,
  • Class I and III antiarrhythmics.

It is not recommended to use sulpiride with other neuroleptics due to the increased risk of side effects.

Alcohol should not be consumed while taking sulpiride as it increases the sedative effect of this drug.

Take sulpiride with caution with CNS depressants:

  • opioids, including codeine-containing cough medications, analgesics for moderate to severe pain,
  • painkillers,
  • barbiturates,
  • benzodiazepines,
  • anxiolytics and hypnotics other than benzodiazepines,
  • antidepressants that have a sedative effect,
  • first-generation antihistamines with a sedative effect (found in preparations such as aviomarin, hydroxyzine, ketotifen, clemastine)
  • centrally acting antihypertensive drugs, e.g. baclofen, thalidomide, pizotifen,
  • clonidine and its derivatives.

Sulpiryd - side effects

Side effects include:

  • hyperprolactemia,
  • amenorrhea,
  • impotence,
  • increase in liver enzymes,
  • calming down,
  • sleepiness,
  • extrapyramidal symptoms,
  • dyskinesia,
  • Neuroleptic Malignant Syndrome,
  • galactorrhea,
  • gynecomastia,
  • rotating eye movements,
  • orthostatic hypotension,
  • venous clots,
  • excessive drooling,
  • spastic torticollis,
  • szczękościsk,
  • rash.

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