Opioid-related drugs
Opioid-related drugs
Opioid-related drugs decrease peristalsis (involuntary, progressive, wavelike intestinal movement that pushes fecal matter along) in the intestines and include:
- diphenoxylate with atropine
- loperamide.
Pharmacokinetics
The combination drug diphenoxylate with atropine is readily absorbed from the GI tract. However, loperamide isn’t absorbed well after oral administration.
Distribution, metabolism, and excretion
Both drugs are distributed in serum, metabolized in the liver, and excreted primarily in stool. Diphenoxylate with atropine is metabolized to difenoxin, its biologically active major metabolite.
Pharmacodynamics
Diphenoxylate with atropine and loperamide slow GI motility by depressing peristalsis in the large and small intestines. These drugs also decrease expulsive contractions throughout the colon.
Pharmacotherapeutics
Diphenoxylate with atropine and loperamide are used to treat acute, nonspecific diarrhea. Loperamide is used to treat chronic diarrhea.
Drug interactions
Diphenoxylate with atropine and loperamide may enhance the depressant effects of barbiturates, alcohol, opioids, tranquilizers, and sedatives.
Warning!
Adverse reactions to opioid-related drugs
Adverse reactions to diphenoxylate with atropine and loperamide include:
- nausea and vomiting
- abdominal discomfort or distention
- drowsiness
- fatigue
- central nervous system depression
- tachycardia (fast heart rate)
- paralytic ileus (reduced or absent peristalsis in the intestines).
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