What is diphenoxylate and atropine, and how does it work (mechanism of action)?
Lomotil is a combination of two drugs, diphenoxylate and atropine. It is used to treat acute diarrhea (diarrhea of
limited duration). Diphenoxylate is a man-made narcotic chemically related to
meperidine (Demerol). Like other narcotics, diphenoxylate reduces diarrhea by
interfering with the propulsion of intestinal contents through the intestines.
Although diphenoxylate is chemically related to narcotics, it does not have
pain– relieving (analgesic) actions like most other narcotics. In higher doses,
however, like other narcotics, diphenoxylate can cause euphoria (elevation of
mood) and physical dependence. In order to prevent abuse of diphenoxylate for
its mood-elevating effects, atropine is combined with diphenoxylate in small
quantities. As a result, if Lomotil is taken in greater than recommended doses
unpleasant side effects from too much atropine will occur. Lomotil was approved
by the FDA in 1960.
What brand names are available for diphenoxylate and atropine?
Lomotil, Lofene, Lonox
Is diphenoxylate and atropine available as a generic drug?
GENERIC AVAILABLE: Yes
Do I need a prescription for diphenoxylate and atropine?
What are the side effects of diphenoxylate and atropine?
The most common side effects reported in persons taking diphenoxylate include:
Other important side effects include:
- numbness of extremities,
- loss of
- appetite, and
- abdominal pain.
Although the dose of atropine in Lomotil is too low to cause side effects when
taken in the recommended doses, side effects of atropine (including dryness of
the skin and mucous membranes, increased heart rate, urinary retention, and
increased body temperature) have been reported, particularly in children under
two years of age and children with
Down syndrome. Pancreatitis and toxic
megacolon also have been reported.
What is the dosage for diphenoxylate and atropine?
In adults, the usual dose is 5 mg (2 tablets) of diphenoxylate
three to four times per day initially. Thereafter, the dose may be decreased to
2.5 mg (1 tablet) two to three times a day. The dose for children (2 to 12 years
old) is 0.3 to 0.4 mg/kg/day in four divided doses. If diarrhea is not better
within 48 hours, diphenoxylate is not likely to be effective with more prolonged
Which drugs or supplements interact with diphenoxylate and atropine?
The combination of diphenoxylate and monoamine
oxidase inhibitors (MAO's), for example, isocarboxazid (Marplan), phenelzine (Nardil),
tranylcypromine (Parnate), and procarbazine (Matulane) can cause severe
blood pressure with the possibility of a cerebrovascular accident (stroke).
Drugs which increase the propulsion of intestinal contents theoretically can
reduce the effectiveness of diphenoxylate. Such drugs include bethanechol (Urecholine),
cisapride (Propulsid), metoclopramide (Reglan), and erythromycin.
decrease the propulsion of intestinal contents may exaggerate the effects of diphenoxylate and cause constipation. Such drugs include
Cystospaz), antihistamines such as hydroxyzine (Vistaril, Atarax) and
diphenhydramine (Benadryl), opiate agonists such as oxycodone (Percocet) and
hydrocodone (Vicodin, Norco,
etc.), some phenothiazine antipsychotics such as chlorpromazine
(Thorazine), thioridazine (Mellaril) and triflupromazine (Stelazine), and some
tricyclic antidepressants such as amitriptyline (Elavil,
Endep), amoxapine (Asendin),
clomipramine (Anafranil), doxepin (Sinequan), imipramine (Tofranil),
nortriptyline (Pamelor), protriptyline (Vivactil), and trimipramine (Surmontil).
Taking diphenoxylate with alcohol or other chemicals or medications that can
depress the central nervous system may cause excessive sedation. Such drugs
include barbiturates, benzodiazepines, for example, lorazepam (Ativan), diazepam
(Valium), temazepam (Restoril), oxazepam (Serax), or clonazepam (Klonopin),
zolpidem (Ambien), narcotics, and tricyclic antidepressants (listed above).
Pancreatitis is inflammation of an organ in the abdomen called the pancreas.
Is diphenoxylate and atropine safe to take if I’m pregnant or breastfeeding?
Diphenoxylic acid, a metabolite of diphenoxylate
(that is, diphenoxylate that has been changed chemically by the body) is
breast milk, as is atropine. Although there have not been problems
reported in the infants of women who breastfeed, the benefits to the mother
should be weighed against the potential risks to the nursing infant.
What else should I know about diphenoxylate and atropine?
What preparations of diphenoxylate and atropine are available?
Tablets (2.5 mg diphenoxylate and 0.025mg atropine);
liquid (2.5mg diphenoxylate and 0.025mg atropine per teaspoonsful).
How should I keep diphenoxylate and atropine stored?
Lomotil should be stored at room temperature, 15-30 C (59- 86