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Diphenoxylate


The drug Diphenoxylate is called an opioid agonist that is mainly used for the treatment of diarrhea which acts by slowing down the intestinal contractions and stomach movement (peristalsis) which in turn allows the body to let intestinal contents group together and prolong movement outside, giving way for the intestines to draw moisture at a relatively normal or higher rate, preventing liquid or loose stools. Diphenoxylate is the main ingredient in the medicine Lomotil which contains atropine as well.

Diphenoxylate Hydrochloride and Atropine Sulfate tablets, commonly known as Lomotil and/or Co-phenotrope are drugs used effectively to manage patients suffering from diarrhea or loose bowel movement.

Diphenoxylate comes in either a tablet or liquid formulation. The tablet is made up of 2.5 mg diphenoxylate and 0.025mg of atropine. The liquid formulation contains 2.5mg of diphenoxylate and 0.025mg of atropine per teaspoonful. Initially, the usual recommended dose for adults is 5mg or 2 tablets three to four times per day. Afterwards, dosage may be decreased to a tablet two to three times a day. For children, dosage is based on weight.

The most commonly reported side effects of taking diphenoxylate include drowsiness, dizziness, headache, nausea or vomiting, and dry mouth. Less common side effects reported include a sense of euphoria, lethargy, feelings of restlessness, numbness, appetite loss, and abdominal pain.

It is highly advised to report a patient’s medical history prior to taking the drug, especially if there is a documented drug allergy, liver disease, lung disease or alcohol use. When taking the drug, caution must be exercised when performing activities requiring mental alertness as diphenoxylate affects mental focus. Alcohol use is to be limited as well as it may increase the dizzying effects of the drug.

Diphenoxylate is an opioid agonist, hence it should not be taken by patients concurrently taking Monoamine oxidase inhibitors (MOI) such as L-Deprenyl. Antihistamines and tranquilizers should also be avoided as they may enhance the sedative properties of the drug.

General precaution is given to patients who wish to take, or currently taking other drugs which may affect the potency and medicinal action of the drug. Combining diphenoxylate and MOIs may cause severe high blood pressure and even cerebrovascular accidents, or a stroke.

Constipation may result if diphenoxylate is taken with other drugs that increase the movement of intestines and the stomach, and reduce the action of diphenoxylate. Drugs that depress the action of the central nervous system may react with diphenoxylate, causing excessive sedation. Such drugs may include barbiturates, narcotics and antidepressants.

No clear reports have been made to prove that diphenoxylate brings general harm to the fetus, however, it should be only used when clearly needed. However, a by-product of diphenoxylate – diphenoxylic acid, is found to be excreted in breast milk. There have been no known problems reported in infants who are breastfed with the byproduct. Still, the benefits of using the drug should always be weighed to the potential risks it may bring to the nursing infant.

Diphenoxylate has the following structural formula:

Chemical structure of diphenoxylate


• Molecular formula of diphenoxylate is C30H32N2O2
• Chemical IUPAC Name is ethyl 1-(3-cyano-3,3-diphenyl-propyl)-4-phenyl-piperidine-4-carboxylate
• Molecular weight is 452.587 g/mol
Diphenoxylate available : 5ml injection and 2,5mg tablets




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