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Source: https://en.wikipedia.org/wiki/Loperamide#Mechanism_of_action


Lomotil (diphenoxylate and atropine) contains diphenoxylate hydrochloride 2.5 mg, and atropine sulfate 0.025 mg to discourage deliberate overdosage and injection.

The atropine additive strategy is designed to discourage use of the drug in a manner inconsistent with its labelling and physician and manufacturer instructions; in theory, the anticholinergic effect of atropine will produce severe weakness and nausea if standard dosage is exceeded, and at the time diphenoxylate was introduced in the United States a number of manufacturers used this strategy with oral forms of morphinemethadone(also using scopolamine), oxycodone and others. Currently, the only other narcotic produced in the United States to use this strategy is Motofen (difenoxin 1 mg with 25 µg atropine sulfate). Difenoxin is a DEA schedule C-I without atropine, but a schedule C-IV or C-V with varying doses of concurrent atropine.[4]

The 25 µg of atropine present in each 2½ mg Lomotil tablet is 1/40 of the standard therapeutic dose of atropine via the oral route for normal anticholinergic uses.
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