Levosulpiride

Levosulpiride is a substituted benzamide antipsychotic, reported to be a selective antagonist of dopamine D2 receptor activity on both central and peripheral levels. It is an atypical neuroleptic and a prokinetic agent. Levosulpiride is also claimed to ha

A Comparative Study of Trigger Point Therapy with Local Anaesthetic (0.5 % Bupivacaine) Versus Combined Trigger Point Injection Therapy and Levosulpiride in the Management of Myofascial Pain Syndrome in the Orofacial Region.[Pubmed:27752210]

J Maxillofac Oral Surg. 2016 Sep;15(3):376-383.

AIM: To compare the efficacy of combined local anesthetic injection with 0.5 % bupivacaine and Levosulpiride versus local anesthetic injection alone on outcome measures including levels of pain intensity and depression in the management of myofascial pain syndrome in orofacial region. PATIENTS AND METHODS: This was a prospective, randomized, controlled and open-label comparative clinical study. Seventy-four patients diagnosed to have myofascial pain syndrome and fulfilling the inclusion criteria were enrolled for the study. Patients were randomly assigned into 2 groups. Group A received local anesthetic injection (0.5 % bupivacaine) on trigger points and Group B received combined trigger point injection therapy and 50 mg of tablet Levosulpiride orally B.I.D. They were assessed for pain intensity and depression at baseline and at follow-up of 1, 4, 6 and 12 week intervals. RESULTS: The mean age of patients was 44.54 + 15.977 years in group A and 39.97 + 14.107 years in group B (P value = 0.2). Group A comprised of 25 females (67.567 %) and 12 males (32.432 %) while group B had 27 females (75 %) and 9 males (25 %). 70.27 % were diagnosed with moderate depression in group A and 75 % in group B. 18.91 % in group A and 19.44 % in group B were diagnosed with severe depression. When the VAS score and BDI score was compared at the follow-up intervals with the baseline scores in both treatment groups, the mean difference was highly significant at all the follow-up intervals. However when the relative efficacies of two interventions were compared between the two groups, improvement in pain was significant at all the follow-up intervals except the 1st week follow-up whereas the improvement in depression was non-significant at 1st and 4th week interval while it was highly significant at 6th and 12th week intervals. CONCLUSION: The combined therapy with trigger point injection and Levosulpiride as antidepressant significantly reduces pain and depression in the study subjects suffering from chronic myofascial pain with moderate to severe depression in the orofacial region.

Formulation, characterization, in vitro and in vivo evaluation of castor oil based self-nano emulsifying levosulpiride delivery systems.[Pubmed:27599558]

J Microencapsul. 2016 Sep;33(6):535-543.

CONTEXT: Levosulpiride (LSP) is a hydrophobic benzamide derivative used in the treatment of schizophrenia. SNEDDS were extensively practiced for systemic delivery of poorly aqueous soluble drugs to achieve maximum bioavailability. OBJECTIVE: The present study was focussed on the formulation, optimisation and evaluation of LSP SNEDDS using castor oil, for enhancement of drug absorption and bioavailability. MATERIALS AND METHODS: Pseudo-ternary phase diagram was plotted to identify the range of SNEDDS components. Twenty formulations were designed, prepared and characterised by its particle size, zeta potential, viscosity, and stability. In vitro dissolution data modelling was performed. Microscopy, FTIR and in vivo bioavailability studies were conducted for optimum formulation. Results, discussion and conclusion: F18 containing castor oil, 0.9 mL; PEG 600, 1.36 mL and Tween 80, 2.74 mL was found to be optimum. The optimised formulation had shown uniform globule size, no interactions of LSP with SNEDDS components and higher pharmacokinetic parameters than that of commercial preparation.

Bioequivalence of a New Oral Levosulpiride Formulation Compared With a Standard One in Healthy Volunteers.[Pubmed:28196046]

Ther Drug Monit. 2017 Apr;39(2):118-123.

BACKGROUND: A monocentric, single-dose, open-label, 2-way, crossover randomized study was conducted by the San Matteo Phase I Clinical Trial Unit and Experimental Therapy (Pavia, Italy) to assess the bioequivalence and the systemic tolerability of a new oral formulation of Levosulpiride (tablet 25 mg: test) versus a commercially available formulation on the Italian market (tablet 25 mg: reference). METHODS: Thirty-five healthy adult volunteers, men (n = 19) and women (n = 16), aged between 18 and 55 years were screened and 32 of them were enrolled in the study. After having signed the written informed consent, each subject received a single oral dose of Test or Reference product with 250 mL of natural mineral water, in fasting conditions, interspersed with a 6-day washout period Blood samples were collected up to 36 hours after drug administration: the drug plasma levels were determined by high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry. The pharmacokinetic parameters included peak plasma concentration (Cmax), time corresponding to Cmax (tmax), area under the plasma concentration-time curve from zero to infinity (AUC0-infinity) or to the last sampling time assessment (AUC0-36), the elimination rate constant (ke), and the terminal half-life (t1/2). Safety was measured by pre- and post-treatment specific biochemical investigations, physical examination, electrocardiogram, occurrence of adverse events, and any information on patients' withdrawal. RESULTS: The geometric mean ratio Test/Reference (90% confidence interval) for Levosulpiride was 103.0% (95.8-110.8) for AUC0-36, 103.6% (95.9-111.9) for AUC0-infinity, and 104.3% (94.9-114.6) for Cmax. ke and t1/2 were 0.07 (SD: 0.02) and 9 hours (8-12) for both the formulations. Clearance (L/h) was 29.6 (+/-13.5) and 30.7 (+/-14.2) for the test and the reference product, respectively. CONCLUSIONS: Because the acceptance criteria required by the drug regulatory agency (European Medicines Agency, EMA) for bioequivalence prescribe limits of 80%-120% for untransformed data and 80%-125% for "ln" transformed data, we can confirm that the 2 formulations are bioequivalent, in terms of the rate and extent of absorption.

Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class.

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