Delving into the Latest Updates on Levosulpiride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

L-sulpiride, Levobren, Levosulpiride (INN)

+ [6]

Target

DRDs

Action

antagonists

Mechanism

DRDs antagonists(Dopamine receptors antagonists)

Therapeutic Areas

Nervous System DiseasesDigestive System DisordersOther Diseases

Active Indication

Chronic schizophreniaSomatosensory DisordersDyspepsia

Inactive Indication

Acute vomitingAnxiety DisordersHeadache+ [1]

Originator Organization-

Active Organization

Medochemie Ltd.

SK Chemicals Co. Ltd.

KOREA UNITED PHARM, Inc.

+ [2]

Inactive Organization

Shanghai Zhaohui Pharmaceutical Co. Ltd.

Hainan Tianya Pharmaceutical Co., Ltd.

Hainan Sihuan Pharmaceutical Co. Ltd.

+ [2]

License Organization-

Drug Highest PhaseApproved

First Approval Date

South Korea (25 Sep 1995),

Dyspepsia

Regulation-

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Structure/Sequence

Molecular FormulaC15H23N3O4S

InChIKeyBGRJTUBHPOOWDU-NSHDSACASA-N

CAS Registry23672-07-3

To study the time course of plasma drug concentration of levosulpiride tablets after a single oral administration on an empty stomach in healthy subjects, estimate the corresponding pharmacokinetic parameters, and evaluate the bioequivalence of levosulpiride (trade name Levopraid®) produced by TEOFARMA as the reference preparation.

Start Date20 Aug 2018

Sponsor / Collaborator

Jiangsu Tasly Diyi Pharmaceutical Co., Ltd.

100 Clinical Results associated with Levosulpiride

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100 Translational Medicine associated with Levosulpiride

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100 Patents (Medical) associated with Levosulpiride

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933

Literatures (Medical) associated with Levosulpiride

01 May 2025·Naunyn-Schmiedeberg's Archives of Pharmacology

Exploring the potential of a pH-sensitive hydrogel sponge: interpenetrating network of tragacanth and pectin for controlled delivery of levosulpiride

Article

Author: Salamatullah, Ahmad Mohammad ; Iqbal, Muhammad Awais ; Shazly, Gamal A ; Shazly, Gamal A. ; Aamir, Muhammad ; Ibenmoussa, Samir ; Wondmie, Gezahign Fentahun ; Ashraf, Muhammad Umer ; Barkat, Kashif ; Anjum, Irfan ; Mushtaq, Muhammad Naveed ; Gul, Rabia ; Bourhia, Mohammed

The development of drug delivery systems that allow precise control over drug release pattern has fetched significant attention in the pharmaceutical field. This research work investigates the potential of a pH-sensitive interpenetrating network (IPN) composed of tragacanth and pectin as a carrier for the controlled release of levosulpiride. To enhance the solubility of poorly soluble drug levosulpiride, inclusion complexes were formed with beta cyclodextrin (βCD). The IPN was prepared by cross-linking tragacanth with pectin by adopting a green chemistry approach. The resulting cross-linked polymeric network was subjected to repetitive freeze-drying cycles for preparation of spongy mass. The physicochemical properties of the resultant product were thoroughly characterized using a range of analytical techniques, including Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), thermal analyses (DSC/TGA), and X-ray diffraction (XRD). The physical parameters like sol-gel fraction (%), drug loading (%), swelling behavior, electrolyte responsiveness, and in vitro drug release profile of the developed sponge were systematically evaluated under varying pH conditions. Results of FTIR demonstrated the formation of cross-linked network, ruling out drug-excipient interaction. SEM analysis unveiled porous and rough geometry. Thermal analyses proved the hydrogel network thermally stable whereas, PXRD demonstrated the overall amorphous nature of the hydrogel sponge. The outcomes of physical parameters demonstrated an incremental trend in gel fraction from 63 to 85% on raising the molar concentration of cross-linker from TP1 to TP3. However, increasing tragacanth content escalation in gel fraction from 75 to 79% was noticed. While gel fraction was augmented from 79 to 83% with increasing pectin contents. The maximum drug loading formulation TP3 was computed to be 89%. Hydrogel sponges also demonstrated electrolyte responsiveness. The release profile indicated a pH-responsive behavior, with sustained release up to 10 h observed in a buffer solution of pH 6.8 and 7.4. In an acidic medium, a minor amount of drug was released during 10 h dissolution. Drug release kinetics was observed to be in zero order. The findings of this study highlight the promising potential of the tragacanth/pectin hydrogel sponge as a pH-sensitive dais for the controlled delivery of levosulpiride, emphasizing its potential application in personalized drug therapy and the treatment of gastrointestinal disorders.

01 May 2025·International Journal of Biological Macromolecules

Drug repurposing: Identification and X-ray crystallographic analyses of US-FDA approved drugs against carbonic anhydrase-II

Article

Author: Rasheed, Saima ; Huda, Noo Rul ; Tahir, Syeda Sarah ; Arif, Rida ; Falke, Sven ; Ahmad, Malik Shoaib ; Warsi, Zoha ; Gul, Sadaf

Of all isoforms, human carbonic anhydrase II (PF00194; EC 4.2.1.1), which is mostly found in red cells, kidneys, and the eyes, plays a pivotal role in numerous physiological processes, and its dysregulation has been linked to the wide range of illnesses, such as glaucoma. Finding new inhibitors that target carbonic anhydrase II, therefore has great potential in drug discovery. Using drug repurposing approach, this study focused on the investigation of different drugs as Carbonic anhydrase II inhibitors and their structural studies using X-ray crystallography. For this purpose, 100 different drugs were evaluated for bovine and human carbonic anhydrase II inhibitory activity. Among all, two drugs, i.e. acetohexamide (1) and levosulpiride (54) were found to be active, with IC₅₀ = 437.0 ± 0.2 and 1128 ± 0.75 μM, respectively. Mechanistic studies suggested that both drugs are competitive inhibitors of the human carbonic anhydrase II enzyme. The X-ray crystal structure analysis revealed that acetohexamide (1) interacts via terminal acetyl group with the active site residues of the carbonic anhydrase II enzyme, and showed strong hydrogen bonding with Zn, His94, His119, and Asn67. The sulfonamide group of levosulpiride was involved in strong hydrogen bonding with Zn, His94, His119, and Thr199. From in vivo studies, we found that carbonic anhydrase activity was significantly inhibited by the intraperitoneal administration of levosulpiride for up to 5 h. Our findings provide comprehensive insights for the optimization of the pharmacological profile of these drugs, and provide avenues for the exploration of different derivatives of these drugs with enhanced efficacy and fewer adverse effects.

11 Apr 2025·Current Drug Safety

Dopaminergic Drugs and Valproate-associated Refractory Hyponatremia Over Levosulpiride-induced Parkinsonism in an Elderly Female Patient When Deprescribing was the Only Therapy

Article

Author: Kaur, Upinder ; Chakrabarti, Sankha Shubhra ; Dehade, Amol ; Reddy, Noti Taruni Srija

Introduction:Prescribing cascade is a condition in which a drug administered to a patient causes an adverse reaction that is misinterpreted as a new condition, resulting in the addition of a new drug.Case Presentation:Here, we report the case of an elderly female patient who suffered from metabolic, neurologic, and urinary consequences of a prescribing cascade of antiemetic, antiepileptic, and dopaminergic drugs. While levosulpiride caused Parkinsonian symptoms, the dopaminergic drugs and valproate caused refractory hyponatremia followed by altered sensorium, and clidinium contributed to urinary retention.Conclusion:The case highlights the need to be vigilant for adverse consequences of the prescribing cascade, especially for antiemetic drugs, such as levosulpiride, because of its propensity to induce extrapyramidal reactions in older patients. In cases of refractory hyponatremia, a trial of de-challenge of valproate and dopaminergic drugs should be considered. The identification and removal of the culprit drugs can rescue the patient from a disabling cycle of adverse drug reactions.

100 Deals associated with Levosulpiride

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External Link

KEGG	Wiki	ATC	Drug Bank
D07312	Levosulpiride	N05AL07	DB16021

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Chronic schizophrenia	Italy	Medochemie Ltd.	04 Mar 2015
Chronic schizophrenia	Bulgaria	Medochemie Ltd.	04 Mar 2015
Chronic schizophrenia	Cyprus	Medochemie Ltd.	04 Mar 2015
Chronic schizophrenia	Romania	Medochemie Ltd.	04 Mar 2015
Somatosensory Disorders	Italy	Medochemie Ltd.	04 Mar 2015
Somatosensory Disorders	Bulgaria	Medochemie Ltd.	04 Mar 2015
Somatosensory Disorders	Cyprus	Medochemie Ltd.	04 Mar 2015
Somatosensory Disorders	Romania	Medochemie Ltd.	04 Mar 2015
Dyspepsia	South Korea	SK Chemicals Co. Ltd.	25 Sep 1995

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute vomiting	Phase 3	China	Hainan Tianya Pharmaceutical Co., Ltd.	10 Mar 2014
Acute vomiting	Phase 3	China	Shanghai Huatuo Pharmaceutical Technology Development Co. Ltd.	10 Mar 2014
Acute vomiting	Phase 3	China	Hainan Sihuan Pharmaceutical Co. Ltd.	10 Mar 2014
Anxiety Disorders	Phase 3	China	Hainan Sihuan Pharmaceutical Co. Ltd.	23 Dec 2013
Anxiety Disorders	Phase 3	China	Shanghai Huatuo Pharmaceutical Technology Development Co. Ltd.	23 Dec 2013
Anxiety Disorders	Phase 3	China	Hainan Tianya Pharmaceutical Co., Ltd.	23 Dec 2013
Headache Disorders, Primary	Phase 3	China	Hainan Sihuan Pharmaceutical Co. Ltd.	23 Dec 2013
Dyspepsia	Phase 3	China	Hainan Huatuo Nuokang Pharmaceutical Co Ltd	20 Dec 2012
Dyspepsia	Phase 3	China	Shanghai Zhaohui Pharmaceutical Co. Ltd.	20 Dec 2012
Dyspepsia	Phase 3	China	Shanghai Huatuo Pharmaceutical Technology Development Co. Ltd.	20 Dec 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SNMMI2023	Not Applicable	Diabetic Gastroparesis	-	Mastic Gum Capsules	xghpvansfd(dccgzagivt) = xyykrhvhnz ctzwhupdpn (oyupeaqeql, 2.17) View more	-	28 Aug 2023
				Levosulpiride Capsules	xghpvansfd(dccgzagivt) = sysohfkeio ctzwhupdpn (oyupeaqeql, 2.28) View more
DDW2022	Not Applicable	-	-	Levosulpiride	pvufgurqhi(eagrfkslks) = lbznvyqyum fitxqdihsx (uebepcvioh ) View more	-	21 May 2022
				Placebo	pvufgurqhi(eagrfkslks) = pqeqnjhvxa fitxqdihsx (uebepcvioh ) View more
NCT02481583 (Pubmed \| Med Lett Drugs Ther)	Phase 1	-	42	Levosulpiride tablet	(ershwvkkbm) = wnxrlvuqhc wqrcsomvkk (uppfakhopy ) View more	-	01 Nov 2015
				Levosulpiride injection (IM)	(ershwvkkbm) = sxmthkngby wqrcsomvkk (uppfakhopy ) View more