Drug intelligence / Profile preview

metoclopramide + ibuprofen

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Metoclopramide + ibuprofen is a combination of two small molecule drugs formulated for the treatment of acute migraine. Metoclopramide is a dopamine D2 receptor antagonist with antiemetic and prokinetic properties, commonly used to treat nausea, vomiting, and gastroparesis by increasing gastric motility. Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that acts as a non-selective cyclooxygenase (COX-1 and COX-2) inhibitor to reduce pain, inflammation, and fever. The rationale for combining these agents in a bi-layer tablet is that metoclopramide enhances the absorption of acidic NSAIDs like ibuprofen by accelerating gastric emptying while also addressing migraine-associated nausea; meanwhile, separating their release prevents degradation of metoclopramide from prolonged contact with the acidic NSAID[1][3]. This combination aims to maximize efficacy in acute migraine management.

02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)HTR3A (5-hydroxytryptamine receptor 3A)DRD2 (Dopamine D2 Receptor)PGHS-1 (Prostaglandin G/H Synthase 1)

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