Loperamide
Brand: Imodium (US/EU) / Eldoper (IN) / Loperamide (BD)
Antidiarrheal
Peripheral μ-opioid receptor agonist
Pharmacokinetics
| Half-life | 11 hours |
| Tmax | 5 h |
| Bioavailability | 40 % (approx) |
| Protein Binding | 95 % |
| Volume of Distribution | 10 L/kg (approx) |
| Clearance Route | hepatic |
| Active Metabolites | yes |
| Notes | Extensive first-pass metabolism; P-glycoprotein limits CNS entry. |
⚠️ Safety & Warnings
Severity: Severe
Adverse Effects:
Constipation, ileus; QT prolongation at overdose
Contraindications:
Acute dysentery, toxic megacolon
Precautions:
Avoid high doses; risk of cardiac arrhythmias with abuse