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.png | CAS_number = 15676-16-1 | ATC_prefix = N05 | ATC_suffix = AL01 | ATC_supplemental = | PubChem = 5355 | DrugBank = APRD00032 | chemical_formula = C15H23N3O4S | molecular_weight = 341.427 g/mol | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | pregnancy_category = | legal_status = | routes_of_administration = }} Sulpiride (sold as Meresa®, Sulpirid Ratiopharm®, Sulpirid Neuraxpharm®, Bosnyl, Dogmatil®) is an anti-psychotic drug used mainly in the treatment of psychosis (e.g. schizophrenia) and depression. It is a substituted benzamide. Sulpiride is more commonly used in Europe and Japan. So far it has not been approved in the US and Canada. The drug has strong chemical and clinical similarities to the novel anti-psychotic amisulpride.
Pharmacology
Pharmacokinetics
Sulpiride is slowly absorbed from the GI-Tract. Its oral bioavailability is only 25 to 35% with marked interindividual differences. The peak plasma concentration is reached 4.5 hours after oral dosing. The usual halflife is 6 to 8 hours. Ninety-two percent are found in urine as the unchanged drug. Sulpiride is usually given in 2 or 3 divided doses.Pharmacodynamic Properties
Sulpiride is a selective antagonist at postsynaptic D2-Receptors. This action dominates in doses exceeding 600mg daily. In doses of 600 to 1,600mg Sulpiride shows mild sedating and anti-psychotic activity. Its anti-psychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200mg daily) its prominente feature is a reuptake inhibition of Dopamine accounting for some antidepressant activity and a stimulating effect. Therefore, it is in these doses used as a second line antidepressant. Additionally, it alleviates vertigo.Uses and Dosage
- Productive psychosis - treatment with rather high doses in exceed of 600mg daily.
- Longterm Treatment of negative (unproductive) psychosis in moderate doses (approx. 600mg daily)
- Treatment of depression and vertigo in low to moderate doses (50 to 200mg daily)
Contraindications and Cautíons
- Hypersensitivity to Sulpiride
- Preexisting Breast Cancer or other prolactin-dependent tumors
- Phaeochromocytoma
- Intoxication with other central active drugs
- Concomitant use of Levodopa
- Caution : Preexisting Morbus Parkinson
- Caution : Patients below 18 yrs. of age (no sufficient clinical data)
- Caution : Preexisting severe heart disease/bradycardia, or hypokalemia (predisposing to long QT syndrome and severe arrhythmias)
- Caution : Patients with preexisting epilepsy. The anticonvulsive therapy should be maintained.
Pregnancy and Lactation
- Pregnancy : Animal studies did not reveal any embryo- or fetotoxic properties nor did limited human experience. Because the human data is not sufficient, pregnant women should only be treated with Sulpiride 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 has fewer extrapyramidal side-effects (dystonia, parkinsonism, tardive dyskinesia and akathisia) than many of the older anti-psychotic medications. Most of these do not seem to occur in a dose related manner. Other side effects occur infrequently (hypotension, rarely long-QT-syndrome, dry mouth, sweating, nausea, activation or sedation, insomnia, allergic rash or pruritus). Isolated cases of the potentially life-threatening NMS (neuroleptic malignant syndrome) have been reported. Sulpiride should not be taken after 4 p.m. in order to avoid insomnia. The foremost problem with Sulpiride is a strong stimulation of prolactin-secretion. It is currently not known, if this may contribute to the development of breast-cancer in women.
Interactions
- Levodopa : Sulpiride and Levodopa have antagonistic effects.
- Alcohol : Sedation and hypotension may be potentiated.
- Antihypertensive Agents : Hypotension may be potentiated (risk of postural collapse).
- Other central Depressants : Increased sedation with negative impact on the capacity to drive or operate machinery.
Overdose
Sulpiride has a relative low order of acute toxicity. Substantial amounts may cause severe but reversible dystonic crises with torticollis, protrusion of the tongue, and/or trism. In some cases all symptoms of severe Morbus Parkinson or oversedation/coma can be noticed. The treatment is largely symptomatic. Some or all extrapyramidal reactions may react to application of anticholinergic drugs such as Biperiden or Benztropine. All patients should be closely monitored for signs of long-QT-syndrome and severe arrhythmias.
References
- British National Formulary, 2005
"Sulpiride"