Loperamide hydrochloride is an opioid-receptor agonist and acts on the μ-opioid receptors. Loperamide exhibited potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently inhibited forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide hydrochloride is also a Ca2+ channel blocker. Loperamide hydrochloride blocks broad spectrum neuronal HVA Ca2+ channels at low micromolar concentrations and at higher concentrations it reduces Ca2+ flux through NMDA receptor operated channels. Loperamide is effective for the treatment of a number of types of diarrhea.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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