Sulpiride, sold under the brand name Dogmatil among others, is an atypical antipsychotic (although some texts have referred to it as a typical antipsychotic) medication of the benzamide class which is used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and is sometimes used in low dosage to treat anxiety and dysthymia. The drug is chemically and clinically similar to amisulpride. Levosulpiride is its purified levo-isomer and is sold in some countries for similar purposes. Sulpiride is commonly used in Asia, Central America, Europe, South Africa and South America. It is not approved in the United States, Canada, or Australia.
Medical uses
Schizophrenia Sulpiride's primary use in medicine is in the management of the symptoms of schizophrenia. It has been used as both a monotherapy and adjunctive therapy (in case of treatment-resistance) in schizophrenia.
Depression and anxiety It has also been used in the treatment of dysthymia. There is evidence, although low quality, that sulpiride could accelerate antidepressant response in patients with major depressive disorder. In Japan, sulpiride is both approved as a treatment for schizophrenia and for major depressive disorder (low dose). There is also evidence of its efficacy in treating panic disorder. It was studied at low doses in the treatment of refractory panic disorder and was reported to be effective in a small open-label study.
Other uses Sulpiride is indicated for the treatment of vertigo in some countries.
Contraindications Contraindications
Hypersensitivity to sulpiride Pre-existing breast cancer or other prolactin-dependent tumors Phaeochromocytoma Intoxication with other centrally-active drugs Concomitant use of levodopa Acute porphyria Comatose state or CNS depression Bone-marrow suppression Cautions
Pre-existing Parkinson's disease Patients under 18 years of age (insufficient clinical data) Pre-existing severe heart disease/bradycardia, or hypokalemia (predisposing to long QT syndrome and severe arrhythmias) Patients with pre-existing epilepsy. Anticonvulsant therapy should be maintained Lithium use — increased risk of neurological side effects of both drugs
Pregnancy and lactation Pregnancy: Animal studies did not reveal any embryotoxicity or fetotoxicity, nor did limited human experience. Due to insufficient human data, pregnant women should be treated with sulpiride only if strictly indicated. Additionally, the newborns of treated women should be monitored, because isolated cases of extrapyramidal side effects have been reported. Lactation: Sulpiride is found in the milk of lactating women. Since the consequences are unclear, women should not breastfeed during treatment.
Side effects Sulpiride is usually well tolerated, producing few adverse effects. Their incidences are as follows:
Common (>1%) adverse effects
Dizziness Headache Extrapyramidal side effects - Tremor - Dystonia - Akathisia — a sense of inner restlessness that presents itself with the inability to stay still - Parkinsonism Somnolence (not a very prominent adverse effect considering its lack of α1 adrenergic, histamine and muscarinic acetylcholine receptor affinity) Insomnia Weight gain or loss Hyperprolactinemia (elevated plasma levels of the hormone, prolactin which can, in turn lead to sexual dysfunction, galactorrhea, amenorrhea, gynecomastia, etc.) Nausea Vomiting Nasal congestion Anticholinergic adverse effects such as: - Dry mouth - Constipation - Blurred vision Impaired concentration Rare (<1% incidence) adverse effects
Tardive dyskinesia — a rare, potentially irreversible movement disorder that results from prolonged treatment with antidopaminergic agents such as antipsychotics. It presents with slow (hence tardive), involuntary, repetitive and purposeless movements that most often affect the facial muscles. Neuroleptic malignant syndrome — a rare, life-threatening complication that results from the use of antidopaminergic agents. Its incidence increases with concomitant use of lithium (medication) salts Blood dyscrasias — rare, sometimes life-threatening complications of the use of a number of different antipsychotics (most notably clozapine) which involves abnormalities in the composition of a person's blood (e.g. having too few white blood cells per unit volume of blood). Examples include: - Agranulocytosis — a significant drop in white blood cell count, leaving individuals wide open to life-threatening opportunistic infections - Neutropenia - Leucopenia - Leukocytosis Seizures Torsades de pointes Unknown incidence adverse effects include
QTc interval prolongation which can lead to potentially fatal arrhythmias. Cholestatic jaundice Elevated liver enzymes Primary biliary cirrhosis Allergic reactions Photosensitivity — sensitivity to light Skin rashes Depression Catatonia Palpitations Agitation Diaphoresis — sweating without a precipitating factor (e.g. increased ambient temperature) Hypotension — low blood pressure Hypertension — high blood pressure Venous thromboembolism (probably rare)
Overdose Sulpiride has a relatively low order of acute toxicity. Substantial amounts may cause severe but reversible dystonic crises with torticollis, protrusion of the tongue, and/or trismus. In some cases all the classical symptoms typical of severe Parkinson's disease may be noted; in others, over-sedation/coma may occur. The treatment is largely symptomatic. Some or all extrapyramidal reactions may respond to the application of anticholinergic drugs such as biperiden or benzatropine. All patients should be closely monitored for signs of long QT syndrome and severe arrhythmias.
Interactions Sulpiride neither inhibits nor stimulates cytochrome P450 family (CYP) of oxidizing enzymes in human, thus would not cause clinically significant interactions with other drugs, which are metabolized by CYPs. However, the risk or severity of adverse effects can be increased when sulpiride is combined with other drugs, but this is not related to substrates, inducers and inhibitors of CYPs.
Pharmacology
Pharmacodynamics
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