fbpx
Wikipedia

Sulpiride

Sulpiride, sold under the brand name Dogmatil among others, is an atypical antipsychotic (although some texts have referred to it as a typical antipsychotic)[10] medication of the benzamide class which is used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Sulpiride is commonly used in Asia, Central America, Europe, South Africa and South America. Levosulpiride is its purified levo-isomer and is sold in India for similar purpose. It is not approved in the United States, Canada, or Australia. The drug is chemically and clinically similar to amisulpride.

Sulpiride
Clinical data
Trade namesDogmatil, others
AHFS/Drugs.comInternational Drug Names
Routes of
administration
By mouth (tablets, capsules, solution), intramuscular injection
ATC code
Legal status
Legal status
  • BR: Class C1 (Other controlled substances)[1]
  • UK: POM (Prescription only)
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability25–40%[2][3]
Protein binding<40%[2]
MetabolismNot metabolized;[5][6][7][8][9] 95% is exerted as the unchanged drug[2][5]
Elimination half-life6–8 hours[2][4]
ExcretionUrine (70–90%),[4][3]
Feces.[5]
Identifiers
  • N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide
CAS Number
  • 15676-16-1 Y
PubChem CID
  • 5355
IUPHAR/BPS
  • 5501
DrugBank
  • DB00391 Y
ChemSpider
  • 5162 Y
UNII
  • 7MNE9M8287
KEGG
  • D01226 Y
ChEMBL
  • ChEMBL26 Y
CompTox Dashboard (EPA)
  • DTXSID1042574
ECHA InfoCard100.036.124
Chemical and physical data
FormulaC15H23N3O4S
Molar mass341.43 g·mol−1
3D model (JSmol)
  • Interactive image
  • NS(=O)(=O)c1ccc(OC)c(c1)C(=O)NCC1CCCN1CC
  • InChI=1S/C15H23N3O4S/c1-3-18-8-4-5-11(18)10-17-15(19)13-9-12(23(16,20)21)6-7-14(13)22-2/h6-7,9,11H,3-5,8,10H2,1-2H3,(H,17,19)(H2,16,20,21) Y
  • Key:BGRJTUBHPOOWDU-UHFFFAOYSA-N Y
  (verify)

Medical uses Edit

Sulpiride's primary use in medicine is in the management of the symptoms of schizophrenia.[2] It has been used as both a monotherapy and adjunctive therapy (in case of treatment-resistance) in schizophrenia.[2][11][12][13][14][15] It has also been used in the treatment of dysthymia.[16] There is evidence, although low quality, that Sulpiride could accelerate antidepressant response in patients with major depressive disorder.[17] There is also evidence of its efficacy in treating panic disorder.[18][19] Sulpiride is indicated for the treatment of vertigo in some countries.[20] In Japan, Sulpiride is both approved as a treatment for schizophrenia and for major depressive disorder (low dose).[21][22]

Contraindications Edit

Contraindications[2]

  • 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[2]

Pregnancy and lactation Edit

  • 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.[2]
  • Lactation: Sulpiride is found in the milk of lactating women. Since the consequences are unclear, women should not breastfeed during treatment.[2]

Side effects Edit

Sulpiride is usually well tolerated, producing few adverse effects. Their incidences[spelling?] are as follows:[2][11][23][24][25][26][27][28][29]

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, often permanent[citation needed] movement disorder that, more often than not, 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[30]
Unknown incidence adverse effects include
  • QTc interval prolongation which can lead to potentially fatal arrhythmias.
  • Cholestatic jaundice[31]
  • Elevated liver enzymes
  • Primary biliary cirrhosis[32]
  • 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 Edit

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 Edit

Sulpiride neither inhibits nor stimulates cytochrome P450 family (CYP) of oxidizing enzymes in human, thus would not cause clinically significant interactions with other drugs,[6] 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 Edit

Pharmacodynamics Edit

Sulpiride[33]
Receptor Affinity (Ki, nM)
DAT >10,000
5-HT1A >10,000
5-HT2A 4,786
5-HT3 >10,000
5-HT6 5,011[unreliable source?]
5-HT7 5,011[unreliable source?]
α1 >10,000
α2 >10,000
D1 >10,000
D2 9.8
D3 8.05
D4 54
H1 >10,000
V3 >10,000
Affinity values are toward cloned human receptors.

Sulpiride is a selective antagonist at dopamine D2, D3 and 5-HT1A receptors. Antagonism at 5-HT1A dominates in doses exceeding 600 mg daily. In doses of 600 to 1,600 mg sulpiride shows mild sedating and antipsychotic activity. Its antipsychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200 mg daily) its prominent feature is antagonism of presynaptic inhibitory dopamine and serotonin receptors, accounting for some antidepressant activity and a stimulating effect. Additionally, it alleviates vertigo.

The benzamide neuroleptics (including sulpiride, amisulpride, and sultopride) have been shown to activate the endogenous gamma-hydroxybutyrate receptor in vivo at therapeutic concentrations.[34] Sulpiride was found in one study in rats to upregulate GHB receptors.[35] GHB has neuroleptic properties and it is believed binding to this receptor may contribute to the effects of these neuroleptics.

Sulpiride, along with clozapine, and valproate has been found to activate DNA demethylation in the brain.[36]

History Edit

Sulpiride was discovered in 1966 as a result of a research program by Justin-Besançon and C. Laville at Laboratoires Delagrange who were working to improve the anti-dysrhythmic properties of procainamide; the program led first to metoclopramide and later to sulpiride.[37][38] Laboratoires Delagrange was acquired by Synthelabo in 1991[39][40] which eventually became part of Sanofi.[41]

Society and culture Edit

Brand names Edit

Sulpiride is marketed under the brand names Dogmatil (DE, HK, SG, PH), Dolmatil (IE, UK), Eglonyl (RU, ZA, HR, SI), Espiride (ZA), Modal (IL), Prometar (UY), Equilid (BR) and Sulpor (UK), among many others.[42]

Medicinal forms Edit

These include tablet and oral solution[43]

Patient Aversions Edit

Some individuals from the Caribbean region may have an aversion to taking the medication due to the association with the brand name of Dogmatil. Dogmatil has been associated with dog medication.

Research Edit

Sulpiride has been studied for use as a hormonal contraceptive in women in whom conventional oral contraceptives are contraindicated and to potentiate progestogen-only contraceptives.[44][45] The contraceptive effects of sulpiride are due to its prolactin-releasing and antigonadotropic effects and the hyperprolactinemiaamenorrhea state that it induces.[44][45]

Since the use of psychotropic drugs is efficient in treating irritable bowel syndrome (IBS),[46] sulpiride is studied as potential sole maintenance therapy in the treatment of IBS.[47][48][46]

References Edit

  1. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). from the original on 3 August 2023. Retrieved 16 August 2023.
  2. ^ a b c d e f g h i j k . electronic Medicines Compendium (eMC). Sanofi. 21 January 2010. Archived from the original on 19 October 2013. Retrieved 19 October 2013.
  3. ^ a b Bressolle F, Brès J, Fauré-Jeantis A (January 1992). "Absolute bioavailability, rate of absorption, and dose proportionality of sulpiride in humans". Journal of Pharmaceutical Sciences. 81 (1): 26–32. doi:10.1002/jps.2600810106. PMID 1619566.
  4. ^ a b Brès J, Bressolle F (December 1991). "Pharmacokinetics of sulpiride in humans after intravenous and intramuscular administrations". J Pharm Sci. 80 (12): 1119–24. doi:10.1002/jps.2600801206. PMID 1815069.
  5. ^ a b c Imondi AR, Alam AS, Brennan JJ, Hagerman LM (March 1978). "Metabolism of sulpiride in man and rhesus monkeys". Archives Internationales de Pharmacodynamie et de Therapie. 232 (1): 79–91. PMID 96745.
  6. ^ a b Niwa T, Inoue S, Shiraga T, Takagi A (January 2005). "No inhibition of cytochrome P450 activities in human liver microsomes by sulpiride, an antipsychotic drug". Biological & Pharmaceutical Bulletin. 28 (1): 188–191. doi:10.1248/bpb.28.188. PMID 15635191.
  7. ^ Telles-Correia D, Barbosa A, Cortez-Pinto H, Campos C, Rocha NB, Machado S (February 2017). "Psychotropic drugs and liver disease: A critical review of pharmacokinetics and liver toxicity". World Journal of Gastrointestinal Pharmacology and Therapeutics. 8 (1): 26–38. doi:10.4292/wjgpt.v8.i1.26. PMC 5292604. PMID 28217372.
  8. ^ Lv Q, Yi Z (February 2018). "Antipsychotic Drugs and Liver Injury". Shanghai Archives of Psychiatry. 30 (1): 47–51. PMC 5925599. PMID 29719358.
  9. ^ Kobari T, Namekawa H, Kato Y, Yamada S (June 1985). "Biotransformation of sultopride in man and several animal species". Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 15 (6): 469–476. doi:10.3109/00498258509045020. PMID 4036171.
  10. ^ Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. ISBN 978-0-85711-084-8.
  11. ^ a b Taylor D, Paton C, Shitij K (2012). The Maudsley prescribing guidelines in psychiatry. West Sussex: Wiley-Blackwell. ISBN 978-0-470-97948-8.
  12. ^ Wang J, Omori IM, Fenton M, Soares B (January 2010). "Sulpiride augmentation for schizophrenia". The Cochrane Database of Systematic Reviews (1): CD008125. doi:10.1002/14651858.CD008125.pub2. PMID 20091661.
  13. ^ Lai EC, Chang CH, Kao Yang YH, Lin SJ, Lin CY (May 2013). "Effectiveness of sulpiride in adult patients with schizophrenia". Schizophrenia Bulletin. 39 (3): 673–83. doi:10.1093/schbul/sbs002. PMC 3627763. PMID 22315480.
  14. ^ Soares BG, Fenton M, Chue P (2000). "Sulpiride for schizophrenia". The Cochrane Database of Systematic Reviews (2): CD001162. doi:10.1002/14651858.CD001162. PMID 10796605.
  15. ^ Omori IM, Wang J, Soares B, Fenton M (October 2009). "Sulpiride versus other antipsychotics for schizophrenia (Protocol)". The Cochrane Database of Systematic Reviews (4): CD008126. doi:10.1002/14651858.CD008126.
  16. ^ Pani L, Gessa GL (2002). "The substituted benzamides and their clinical potential on dysthymia and on the negative symptoms of schizophrenia". Molecular Psychiatry. 7 (3): 247–53. doi:10.1038/sj.mp.4001040. PMID 11920152. S2CID 3153728.
  17. ^ Uchida H, Takeuchi H, Suzuki T, Nomura K, Watanabe K, Kashima H (December 2005). "Combined treatment with sulpiride and paroxetine for accelerated response in patients with major depressive disorder". Journal of Clinical Psychopharmacology. 25 (6): 545–51. doi:10.1097/01.jcp.0000185425.00644.41. PMID 16282835. S2CID 10727911.
  18. ^ Bell C, Bhikha S, Colhoun H, Carter F, Frampton C, Porter R (February 2013). "The response to sulpiride in social anxiety disorder: D2 receptor function". Journal of Psychopharmacology. 27 (2): 146–51. doi:10.1177/0269881112450778. PMID 22745189. S2CID 32951554.
  19. ^ Nunes EA, Freire RC, Dos Reis M, de Oliveira E, Silva AC, Machado S, et al. (September 2012). "Sulpiride and refractory panic disorder". Psychopharmacology. 223 (2): 247–9. doi:10.1007/s00213-012-2818-6. PMID 22864966. S2CID 14870287.
  20. ^ "Medicinanet - Equilid 50". Retrieved 5 September 2018.
  21. ^ "Search results detail| Kusurino-Shiori(Drug information Sheet)". www.rad-ar.or.jp. Retrieved 16 March 2020.
  22. ^ Towlson EK, Vértes PE, Müller-Sedgwick U, Ahnert SE (12 September 2019). "Brain Networks Reveal the Effects of Antipsychotic Drugs on Schizophrenia Patients and Controls". Frontiers in Psychiatry. 10: 611. doi:10.3389/fpsyt.2019.00611. PMC 6752631. PMID 31572229.
  23. ^ Lepola U, Koskinen T, Rimón R, Salo H, Gordin A (July 1989). "Sulpiride and perphenazine in schizophrenia. A double-blind clinical trial". Acta Psychiatrica Scandinavica. 80 (1): 92–6. doi:10.1111/j.1600-0447.1989.tb01305.x. PMID 2669445. S2CID 28719315.
  24. ^ Munk-Andersen E, Behnke K, Heltberg J, Nielsen H, Gerlach J (1984). "Sulpiride versus haloperidol, a clinical trial in schizophrenia. A preliminary report". Acta Psychiatrica Scandinavica. Supplementum. 311: 31–41. doi:10.1111/j.1600-0447.1984.tb06857.x. PMID 6367362. S2CID 31689174.
  25. ^ Gerlach J, Behnke K, Heltberg J, Munk-Anderson E, Nielsen H (September 1985). "Sulpiride and haloperidol in schizophrenia: a double-blind cross-over study of therapeutic effect, side effects and plasma concentrations". The British Journal of Psychiatry. 147 (3): 283–8. doi:10.1192/bjp.147.3.283. PMID 3904885. S2CID 24056594.
  26. ^ Standish-Barry HM, Bouras N, Bridges PK, Watson JP (1983). "A randomized double blind group comparative study of sulpiride and amitriptyline in affective disorder". Psychopharmacology. 81 (3): 258–60. doi:10.1007/bf00427274. PMID 6417717. S2CID 28134446.
  27. ^ Quinn N, Marsden CD (August 1984). "A double blind trial of sulpiride in Huntington's disease and tardive dyskinesia". Journal of Neurology, Neurosurgery, and Psychiatry. 47 (8): 844–7. doi:10.1136/jnnp.47.8.844. PMC 1027949. PMID 6236286.
  28. ^ Peselow ED, Stanley M (1982). "Clinical trials of benzamides in psychiatry". Advances in Biochemical Psychopharmacology. 35: 163–94. PMID 6756060.
  29. ^ Edwards JG, Alexander JR, Alexander MS, Gordon A, Zutchi T (December 1980). "Controlled trial of sulpiride in chronic schizophrenic patients". The British Journal of Psychiatry. 137 (6): 522–9. doi:10.1192/bjp.137.6.522. PMID 7011469. S2CID 789670.
  30. ^ Levkovitz H, Abramovitch Y, Nitzan I (June 1994). "Leukocytosis related to the therapeutic dosage of sulpiride". Biological Psychiatry. 35 (12): 963. doi:10.1016/0006-3223(94)91244-0. PMID 8080896. S2CID 43471005.
  31. ^ Melzer E, Knobel B (December 1987). "Severe cholestatic jaundice due to sulpiride". Israel Journal of Medical Sciences. 23 (12): 1259–60. PMID 3326861.
  32. ^ Ohmoto K, Yamamoto S, Hirokawa M (December 1999). "Symptomatic primary biliary cirrhosis triggered by administration of sulpiride". The American Journal of Gastroenterology. 94 (12): 3660–1. doi:10.1111/j.1572-0241.1999.01634.x. PMID 10606349. S2CID 33986018.
  33. ^ Roth BL, Driscol J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 13 November 2020.
  34. ^ Maitre M, Ratomponirina C, Gobaille S, Hodé Y, Hechler V (April 1994). "Displacement of [3H] gamma-hydroxybutyrate binding by benzamide neuroleptics and prochlorperazine but not by other antipsychotics". European Journal of Pharmacology. 256 (2): 211–4. doi:10.1016/0014-2999(94)90248-8. PMID 7914168.
  35. ^ Ratomponirina C, Gobaille S, Hodé Y, Kemmel V, Maitre M (April 1998). "Sulpiride, but not haloperidol, up-regulates gamma-hydroxybutyrate receptors in vivo and in cultured cells". European Journal of Pharmacology. 346 (2–3): 331–7. doi:10.1016/S0014-2999(98)00068-5. PMID 9652377.
  36. ^ Dong E, Nelson M, Grayson DR, Costa E, Guidotti A (September 2008). "Clozapine and sulpiride but not haloperidol or olanzapine activate brain DNA demethylation". Proceedings of the National Academy of Sciences of the United States of America. 105 (36): 13614–9. Bibcode:2008PNAS..10513614D. doi:10.1073/pnas.0805493105. PMC 2533238. PMID 18757738.
  37. ^ Sneader W (31 October 2005). Drug Discovery: A History. John Wiley & Sons. pp. 205–. ISBN 978-0-470-01552-0.
  38. ^ Sanger GJ (December 2009). "Translating 5-HT receptor pharmacology". Neurogastroenterology and Motility. 21 (12): 1235–8. doi:10.1111/j.1365-2982.2009.01425.x. PMID 19906028. S2CID 35544028.
  39. ^ Conard D (17 October 1991). "Synthélabo rachète les laboratoires Delagrange". Les Echos.
  40. ^ "Laboratoires Delagrange". Bibliothèque nationale de France. Retrieved 24 August 2016.
  41. ^ Meek T (24 May 2013). "A look back at Sanofi's merger with Synthélabo". PMLiVE.
  42. ^ "Sulpiride". Drugs.com.
  43. ^ "Sulpiride 200mg/5ml Oral Solution". EMC. Datapharm.
  44. ^ a b Buvat J, Decroix-Blacker C, Legal F, Gasnault JP (January 1976). . Revue Française de Gynécologie et d'Obstétrique (in French). 71 (1): 53–61. PMID 959705. Archived from the original on 15 April 2018. Retrieved 15 April 2018.
  45. ^ a b Payne MR, Howie PW, McNeilly AS, Cooper W, Marnie M, Kidd L (August 1985). "Sulpiride and the potentiation of progestogen only contraception". British Medical Journal. 291 (6495): 559–61. doi:10.1136/bmj.291.6495.559. PMC 1418199. PMID 2994800.
  46. ^ a b Sato M, Murakami M (August 2006). "[Treatment for irritable bowel syndrome--psychotropic drugs, antidepressants and so on]". Nihon Rinsho (in Japanese). 64 (8): 1495–500. PMID 16898620.
  47. ^ El-Reshaid K, Al-Bader S (2019). "New regimen for treatment of irritable bowel syndrome with emphasis on Sulpride as the sole maintenance therapy". Journal of Drug Delivery and Therapeutics. 9 (5): 154–157. doi:10.22270/jddt.v9i5.3424. S2CID 208163204.
  48. ^ Komarov FI, Rapoport SI, Ivanov SV, Kharaian LV, Kolesnikov DB, Kurikov AV (2000). "[Sulpiride treatment of irritable colon syndrome]". Klin Med (Mosk) (in Russian). 78 (7): 22–6. PMID 10979637.

External links Edit

  •   Media related to Sulpiride at Wikimedia Commons

sulpiride, confused, with, sulpyrine, sold, under, brand, name, dogmatil, among, others, atypical, antipsychotic, although, some, texts, have, referred, typical, antipsychotic, medication, benzamide, class, which, used, mainly, treatment, psychosis, associated. Not to be confused with sulpyrine Sulpiride sold under the brand name Dogmatil among others is an atypical antipsychotic although some texts have referred to it as a typical antipsychotic 10 medication of the benzamide class which is used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder and sometimes used in low dosage to treat anxiety and mild depression Sulpiride is commonly used in Asia Central America Europe South Africa and South America Levosulpiride is its purified levo isomer and is sold in India for similar purpose It is not approved in the United States Canada or Australia The drug is chemically and clinically similar to amisulpride SulpirideClinical dataTrade namesDogmatil othersAHFS Drugs comInternational Drug NamesRoutes ofadministrationBy mouth tablets capsules solution intramuscular injectionATC codeN05AL01 WHO Legal statusLegal statusBR Class C1 Other controlled substances 1 UK POM Prescription only In general Prescription only Pharmacokinetic dataBioavailability25 40 2 3 Protein binding lt 40 2 MetabolismNot metabolized 5 6 7 8 9 95 is exerted as the unchanged drug 2 5 Elimination half life6 8 hours 2 4 ExcretionUrine 70 90 4 3 Feces 5 IdentifiersIUPAC name N 1 ethylpyrrolidin 2 yl methyl 2 methoxy 5 sulfamoylbenzamideCAS Number15676 16 1 YPubChem CID5355IUPHAR BPS5501DrugBankDB00391 YChemSpider5162 YUNII7MNE9M8287KEGGD01226 YChEMBLChEMBL26 YCompTox Dashboard EPA DTXSID1042574ECHA InfoCard100 036 124Chemical and physical dataFormulaC 15H 23N 3O 4SMolar mass341 43 g mol 13D model JSmol Interactive imageSMILES NS O O c1ccc OC c c1 C O NCC1CCCN1CCInChI InChI 1S C15H23N3O4S c1 3 18 8 4 5 11 18 10 17 15 19 13 9 12 23 16 20 21 6 7 14 13 22 2 h6 7 9 11H 3 5 8 10H2 1 2H3 H 17 19 H2 16 20 21 YKey BGRJTUBHPOOWDU UHFFFAOYSA N Y verify Contents 1 Medical uses 2 Contraindications 2 1 Pregnancy and lactation 3 Side effects 4 Overdose 5 Interactions 6 Pharmacology 6 1 Pharmacodynamics 7 History 8 Society and culture 8 1 Brand names 8 2 Medicinal forms 8 3 Patient Aversions 9 Research 10 References 11 External linksMedical uses EditSulpiride s primary use in medicine is in the management of the symptoms of schizophrenia 2 It has been used as both a monotherapy and adjunctive therapy in case of treatment resistance in schizophrenia 2 11 12 13 14 15 It has also been used in the treatment of dysthymia 16 There is evidence although low quality that Sulpiride could accelerate antidepressant response in patients with major depressive disorder 17 There is also evidence of its efficacy in treating panic disorder 18 19 Sulpiride is indicated for the treatment of vertigo in some countries 20 In Japan Sulpiride is both approved as a treatment for schizophrenia and for major depressive disorder low dose 21 22 Contraindications EditContraindications 2 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 suppressionCautions 2 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 drugsPregnancy and lactation Edit 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 2 Lactation Sulpiride is found in the milk of lactating women Since the consequences are unclear women should not breastfeed during treatment 2 Side effects EditSulpiride is usually well tolerated producing few adverse effects Their incidences spelling are as follows 2 11 23 24 25 26 27 28 29 Common gt 1 adverse effectsDizziness Headache Extrapyramidal side effects Tremor Dystonia Akathisia a sense of inner restlessness that presents itself with the inability to stay still ParkinsonismSomnolence not a very prominent adverse effect considering its lack of a1 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 visionImpaired concentrationRare lt 1 incidence adverse effectsTardive dyskinesia a rare often permanent citation needed movement disorder that more often than not 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 30 Seizures Torsades de pointesUnknown incidence adverse effects includeQTc interval prolongation which can lead to potentially fatal arrhythmias Cholestatic jaundice 31 Elevated liver enzymes Primary biliary cirrhosis 32 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 EditSulpiride 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 EditSulpiride neither inhibits nor stimulates cytochrome P450 family CYP of oxidizing enzymes in human thus would not cause clinically significant interactions with other drugs 6 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 EditPharmacodynamics Edit Sulpiride 33 Receptor Affinity Ki nM DAT gt 10 0005 HT1A gt 10 0005 HT2A 4 7865 HT3 gt 10 0005 HT6 5 011 unreliable source 5 HT7 5 011 unreliable source a1 gt 10 000a2 gt 10 000D1 gt 10 000D2 9 8D3 8 05D4 54H1 gt 10 000V3 gt 10 000Affinity values are toward cloned human receptors Sulpiride is a selective antagonist at dopamine D2 D3 and 5 HT1A receptors Antagonism at 5 HT1A dominates in doses exceeding 600 mg daily In doses of 600 to 1 600 mg sulpiride shows mild sedating and antipsychotic activity Its antipsychotic potency compared to chlorpromazine is only 0 2 1 5 In low doses in particular 50 to 200 mg daily its prominent feature is antagonism of presynaptic inhibitory dopamine and serotonin receptors accounting for some antidepressant activity and a stimulating effect Additionally it alleviates vertigo The benzamide neuroleptics including sulpiride amisulpride and sultopride have been shown to activate the endogenous gamma hydroxybutyrate receptor in vivo at therapeutic concentrations 34 Sulpiride was found in one study in rats to upregulate GHB receptors 35 GHB has neuroleptic properties and it is believed binding to this receptor may contribute to the effects of these neuroleptics Sulpiride along with clozapine and valproate has been found to activate DNA demethylation in the brain 36 History EditSulpiride was discovered in 1966 as a result of a research program by Justin Besancon and C Laville at Laboratoires Delagrange who were working to improve the anti dysrhythmic properties of procainamide the program led first to metoclopramide and later to sulpiride 37 38 Laboratoires Delagrange was acquired by Synthelabo in 1991 39 40 which eventually became part of Sanofi 41 Society and culture EditBrand names Edit Sulpiride is marketed under the brand names Dogmatil DE HK SG PH Dolmatil IE UK Eglonyl RU ZA HR SI Espiride ZA Modal IL Prometar UY Equilid BR and Sulpor UK among many others 42 Medicinal forms Edit These include tablet and oral solution 43 Patient Aversions Edit Some individuals from the Caribbean region may have an aversion to taking the medication due to the association with the brand name of Dogmatil Dogmatil has been associated with dog medication Research EditSulpiride has been studied for use as a hormonal contraceptive in women in whom conventional oral contraceptives are contraindicated and to potentiate progestogen only contraceptives 44 45 The contraceptive effects of sulpiride are due to its prolactin releasing and antigonadotropic effects and the hyperprolactinemia amenorrhea state that it induces 44 45 Since the use of psychotropic drugs is efficient in treating irritable bowel syndrome IBS 46 sulpiride is studied as potential sole maintenance therapy in the treatment of IBS 47 48 46 References Edit Anvisa 31 March 2023 RDC Nº 784 Listas de Substancias Entorpecentes Psicotropicas Precursoras e Outras sob Controle Especial Collegiate Board Resolution No 784 Lists of Narcotic Psychotropic Precursor and Other Substances under Special Control in Brazilian Portuguese Diario Oficial da Uniao published 4 April 2023 Archived from the original on 3 August 2023 Retrieved 16 August 2023 a b c d e f g h i j k Sulpiride Tablets 200mg 400mg SPC electronic Medicines Compendium eMC Sanofi 21 January 2010 Archived from the original on 19 October 2013 Retrieved 19 October 2013 a b Bressolle F Bres J Faure Jeantis A January 1992 Absolute bioavailability rate of absorption and dose proportionality of sulpiride in humans Journal of Pharmaceutical Sciences 81 1 26 32 doi 10 1002 jps 2600810106 PMID 1619566 a b Bres J Bressolle F December 1991 Pharmacokinetics of sulpiride in humans after intravenous and intramuscular administrations J Pharm Sci 80 12 1119 24 doi 10 1002 jps 2600801206 PMID 1815069 a b c Imondi AR Alam AS Brennan JJ Hagerman LM March 1978 Metabolism of sulpiride in man and rhesus monkeys Archives Internationales de Pharmacodynamie et de Therapie 232 1 79 91 PMID 96745 a b Niwa T Inoue S Shiraga T Takagi A January 2005 No inhibition of cytochrome P450 activities in human liver microsomes by sulpiride an antipsychotic drug Biological amp Pharmaceutical Bulletin 28 1 188 191 doi 10 1248 bpb 28 188 PMID 15635191 Telles Correia D Barbosa A Cortez Pinto H Campos C Rocha NB Machado S February 2017 Psychotropic drugs and liver disease A critical review of pharmacokinetics and liver toxicity World Journal of Gastrointestinal Pharmacology and Therapeutics 8 1 26 38 doi 10 4292 wjgpt v8 i1 26 PMC 5292604 PMID 28217372 Lv Q Yi Z February 2018 Antipsychotic Drugs and Liver Injury Shanghai Archives of Psychiatry 30 1 47 51 PMC 5925599 PMID 29719358 Kobari T Namekawa H Kato Y Yamada S June 1985 Biotransformation of sultopride in man and several animal species Xenobiotica the Fate of Foreign Compounds in Biological Systems 15 6 469 476 doi 10 3109 00498258509045020 PMID 4036171 Joint Formulary Committee 2013 British National Formulary BNF 65 ed London UK Pharmaceutical Press ISBN 978 0 85711 084 8 a b Taylor D Paton C Shitij K 2012 The Maudsley prescribing guidelines in psychiatry West Sussex Wiley Blackwell ISBN 978 0 470 97948 8 Wang J Omori IM Fenton M Soares B January 2010 Sulpiride augmentation for schizophrenia The Cochrane Database of Systematic Reviews 1 CD008125 doi 10 1002 14651858 CD008125 pub2 PMID 20091661 Lai EC Chang CH Kao Yang YH Lin SJ Lin CY May 2013 Effectiveness of sulpiride in adult patients with schizophrenia Schizophrenia Bulletin 39 3 673 83 doi 10 1093 schbul sbs002 PMC 3627763 PMID 22315480 Soares BG Fenton M Chue P 2000 Sulpiride for schizophrenia The Cochrane Database of Systematic Reviews 2 CD001162 doi 10 1002 14651858 CD001162 PMID 10796605 Omori IM Wang J Soares B Fenton M October 2009 Sulpiride versus other antipsychotics for schizophrenia Protocol The Cochrane Database of Systematic Reviews 4 CD008126 doi 10 1002 14651858 CD008126 Pani L Gessa GL 2002 The substituted benzamides and their clinical potential on dysthymia and on the negative symptoms of schizophrenia Molecular Psychiatry 7 3 247 53 doi 10 1038 sj mp 4001040 PMID 11920152 S2CID 3153728 Uchida H Takeuchi H Suzuki T Nomura K Watanabe K Kashima H December 2005 Combined treatment with sulpiride and paroxetine for accelerated response in patients with major depressive disorder Journal of Clinical Psychopharmacology 25 6 545 51 doi 10 1097 01 jcp 0000185425 00644 41 PMID 16282835 S2CID 10727911 Bell C Bhikha S Colhoun H Carter F Frampton C Porter R February 2013 The response to sulpiride in social anxiety disorder D2 receptor function Journal of Psychopharmacology 27 2 146 51 doi 10 1177 0269881112450778 PMID 22745189 S2CID 32951554 Nunes EA Freire RC Dos Reis M de Oliveira E Silva AC Machado S et al September 2012 Sulpiride and refractory panic disorder Psychopharmacology 223 2 247 9 doi 10 1007 s00213 012 2818 6 PMID 22864966 S2CID 14870287 Medicinanet Equilid 50 Retrieved 5 September 2018 Search results detail Kusurino Shiori Drug information Sheet www rad ar or jp Retrieved 16 March 2020 Towlson EK Vertes PE Muller Sedgwick U Ahnert SE 12 September 2019 Brain Networks Reveal the Effects of Antipsychotic Drugs on Schizophrenia Patients and Controls Frontiers in Psychiatry 10 611 doi 10 3389 fpsyt 2019 00611 PMC 6752631 PMID 31572229 Lepola U Koskinen T Rimon R Salo H Gordin A July 1989 Sulpiride and perphenazine in schizophrenia A double blind clinical trial Acta Psychiatrica Scandinavica 80 1 92 6 doi 10 1111 j 1600 0447 1989 tb01305 x PMID 2669445 S2CID 28719315 Munk Andersen E Behnke K Heltberg J Nielsen H Gerlach J 1984 Sulpiride versus haloperidol a clinical trial in schizophrenia A preliminary report Acta Psychiatrica Scandinavica Supplementum 311 31 41 doi 10 1111 j 1600 0447 1984 tb06857 x PMID 6367362 S2CID 31689174 Gerlach J Behnke K Heltberg J Munk Anderson E Nielsen H September 1985 Sulpiride and haloperidol in schizophrenia a double blind cross over study of therapeutic effect side effects and plasma concentrations The British Journal of Psychiatry 147 3 283 8 doi 10 1192 bjp 147 3 283 PMID 3904885 S2CID 24056594 Standish Barry HM Bouras N Bridges PK Watson JP 1983 A randomized double blind group comparative study of sulpiride and amitriptyline in affective disorder Psychopharmacology 81 3 258 60 doi 10 1007 bf00427274 PMID 6417717 S2CID 28134446 Quinn N Marsden CD August 1984 A double blind trial of sulpiride in Huntington s disease and tardive dyskinesia Journal of Neurology Neurosurgery and Psychiatry 47 8 844 7 doi 10 1136 jnnp 47 8 844 PMC 1027949 PMID 6236286 Peselow ED Stanley M 1982 Clinical trials of benzamides in psychiatry Advances in Biochemical Psychopharmacology 35 163 94 PMID 6756060 Edwards JG Alexander JR Alexander MS Gordon A Zutchi T December 1980 Controlled trial of sulpiride in chronic schizophrenic patients The British Journal of Psychiatry 137 6 522 9 doi 10 1192 bjp 137 6 522 PMID 7011469 S2CID 789670 Levkovitz H Abramovitch Y Nitzan I June 1994 Leukocytosis related to the therapeutic dosage of sulpiride Biological Psychiatry 35 12 963 doi 10 1016 0006 3223 94 91244 0 PMID 8080896 S2CID 43471005 Melzer E Knobel B December 1987 Severe cholestatic jaundice due to sulpiride Israel Journal of Medical Sciences 23 12 1259 60 PMID 3326861 Ohmoto K Yamamoto S Hirokawa M December 1999 Symptomatic primary biliary cirrhosis triggered by administration of sulpiride The American Journal of Gastroenterology 94 12 3660 1 doi 10 1111 j 1572 0241 1999 01634 x PMID 10606349 S2CID 33986018 Roth BL Driscol J PDSP Ki Database Psychoactive Drug Screening Program PDSP University of North Carolina at Chapel Hill and the United States National Institute of Mental Health Retrieved 13 November 2020 Maitre M Ratomponirina C Gobaille S Hode Y Hechler V April 1994 Displacement of 3H gamma hydroxybutyrate binding by benzamide neuroleptics and prochlorperazine but not by other antipsychotics European Journal of Pharmacology 256 2 211 4 doi 10 1016 0014 2999 94 90248 8 PMID 7914168 Ratomponirina C Gobaille S Hode Y Kemmel V Maitre M April 1998 Sulpiride but not haloperidol up regulates gamma hydroxybutyrate receptors in vivo and in cultured cells European Journal of Pharmacology 346 2 3 331 7 doi 10 1016 S0014 2999 98 00068 5 PMID 9652377 Dong E Nelson M Grayson DR Costa E Guidotti A September 2008 Clozapine and sulpiride but not haloperidol or olanzapine activate brain DNA demethylation Proceedings of the National Academy of Sciences of the United States of America 105 36 13614 9 Bibcode 2008PNAS 10513614D doi 10 1073 pnas 0805493105 PMC 2533238 PMID 18757738 Sneader W 31 October 2005 Drug Discovery A History John Wiley amp Sons pp 205 ISBN 978 0 470 01552 0 Sanger GJ December 2009 Translating 5 HT receptor pharmacology Neurogastroenterology and Motility 21 12 1235 8 doi 10 1111 j 1365 2982 2009 01425 x PMID 19906028 S2CID 35544028 Conard D 17 October 1991 Synthelabo rachete les laboratoires Delagrange Les Echos Laboratoires Delagrange Bibliotheque nationale de France Retrieved 24 August 2016 Meek T 24 May 2013 A look back at Sanofi s merger with Synthelabo PMLiVE Sulpiride Drugs com Sulpiride 200mg 5ml Oral Solution EMC Datapharm a b Buvat J Decroix Blacker C Legal F Gasnault JP January 1976 One thousand months of contraception with sulpiride Revue Francaise de Gynecologie et d Obstetrique in French 71 1 53 61 PMID 959705 Archived from the original on 15 April 2018 Retrieved 15 April 2018 a b Payne MR Howie PW McNeilly AS Cooper W Marnie M Kidd L August 1985 Sulpiride and the potentiation of progestogen only contraception British Medical Journal 291 6495 559 61 doi 10 1136 bmj 291 6495 559 PMC 1418199 PMID 2994800 a b Sato M Murakami M August 2006 Treatment for irritable bowel syndrome psychotropic drugs antidepressants and so on Nihon Rinsho in Japanese 64 8 1495 500 PMID 16898620 El Reshaid K Al Bader S 2019 New regimen for treatment of irritable bowel syndrome with emphasis on Sulpride as the sole maintenance therapy Journal of Drug Delivery and Therapeutics 9 5 154 157 doi 10 22270 jddt v9i5 3424 S2CID 208163204 Komarov FI Rapoport SI Ivanov SV Kharaian LV Kolesnikov DB Kurikov AV 2000 Sulpiride treatment of irritable colon syndrome Klin Med Mosk in Russian 78 7 22 6 PMID 10979637 External links Edit nbsp Media related to Sulpiride at Wikimedia Commons Retrieved from https en wikipedia org w index php title Sulpiride amp oldid 1180143045, wikipedia, wiki, book, books, library,

article

, read, download, free, free download, mp3, video, mp4, 3gp, jpg, jpeg, gif, png, picture, music, song, movie, book, game, games.