Drug intelligence / Profile preview

trospium chloride + ranitidine

Development stage
Unknown
Lead developer
Universitätsklinikum Greifswald
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

trospium chloride + ranitidine is a non-fixed-dose combination used in clinical pharmacokinetic studies to evaluate interactions between trospium chloride, a muscarinic receptor antagonist used for overactive bladder, and ranitidine, a histamine H2 receptor antagonist and known inhibitor of organic cation transporters (OCTs and MATE transporters). Trospium chloride acts as a competitive antimuscarinic agent, inhibiting muscarinic acetylcholine receptors primarily in the bladder, thus reducing bladder muscle spasms. Ranitidine competitively inhibits histamine action at H2 receptors of the gastric parietal cells but is also used as a probe to study drug interactions mediated by renal and intestinal transporters. Combination administration is not indicated for therapeutic use but is studied for potential pharmacokinetic and transporter-mediated interactions. Studies show that coadministration does not significantly affect the oral absorption of trospium, but ranitidine may lower the renal clearance of trospium chloride by inhibition of MATE1 and MATE2-K, while trospium may decrease the absorption and bioavailability of ranitidine via its effects on intestinal motility[1][3][4].

02

Targets

M1 (Muscarinic acetylcholine receptor M1)CHRM3 (M3)MATE2-K (Multidrug and toxin extrusion protein 2)OCT1 (Organic cation transporter 1)CHRM2 (M2)SLC47A1 (Multidrug and toxin extrusion transporter 1)OCT2 (Organic cation transporter 2)HRH2 (Histamine H2 Receptor)

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