Description
loperamide Hcl is an antidiarrheal used to treat diarrhea. It is also used to reduce the amount of stool in people who have an ileostomy (re-routing of the bowel through a surgical opening in the stomach). loperamide Hcl is available in generic form and over-the-counter.
Uses
Loperamide Hcl is used to treat sudden diarrhea (including traveler's diarrhea). It works by slowing down the movement of the gut. This decreases the number of bowel movements and makes the stool less watery. Loperamide is also used to reduce the amount of discharge in patients who have undergone an ileostomy. It is also used to treat on-going diarrhea in people with inflammatory bowel disease.Loperamide treats only the symptoms, not the cause of the diarrhea (such as infection).
Brand name
Imodium (Janssen); Imodium (McNeil).
Biological Activity
High affinity μ -opioid receptor agonist with peripheral selectivity (Ki values are 2, 48 and 1156 nM for μ -, δ - and κ -opioid receptors respectively). Antidiarrhoeal and antihyperalgesic agent. Also a Ca2+ channel blocker; at low micromolar concentrations it blocks broad spectrum neuronal HVA Ca2+ channels and at higher concentrations it reduces Ca2+ flux through NMDA receptor operated channels.
Pharmacology
Loperamide Hcl protects against diarrhea longer than does diphenoxylate. It reduces the daily fecal volume and decreases intestinal fluid and electrolyte loss. Loperamide Hcl produces rapid and sustained inhibition of the peristaltic reflex through depression of longitudinal and circular muscle activity.The drug also possesses antisecretory activity, presumably through an effect on intestinal opioid receptors.
Side effects
Loperamide Hcl may cause serious side effects including:
diarrhea that is watery or bloody,
stomach pain or bloating,
ongoing or worsening diarrhea,
fast or pounding heartbeats,
fluttering in your chest,
shortness of breath, and
lightheadedness
