Drug information of Difenoxin

Difenoxin


Difenoxin is a 4-phenylpiperidine which is closely related to the opioid analgesic meperidine. Difenoxin alone is a USA Schedule I controlled drug, as it may be habit forming. However, it is listed as a Schedule IV controlled drug if combined with atropine, which is added to decrease deliberate misuse. Motofen(R) is a brand mixture which combines atropine sulfate and difenoxin hydrochloride. It is approved by the FDA to treat acute and chronic diarrhea.

Mechanism of effect

Difenoxin acts as an antidiarrheal by activating peripheral opioid receptors in the small intestine and thereby inhibiting peristalsis. However, research has suggested that non-opioid receptor pathways exist. This would explain the potent antidiarrheal effects of difenoxin despite only limited opioid action 

Pharmacodynamic

Difenoxin acts as a potent antidiarrheal by slowing the movement of the intestines. It also crosses the blood brain barrier to a slight degree to exert weak sedative and analgesic effects.

Adverse reactions thus include dizziness, drowsiness, lightheadedness and headache, in addition to gastrointestal side effects such as nausea, vomiting, dry mouth and epigastric distress.

Pharmacokinetics

Not Available

Drug indications

This medication is used to treat diarrhea. It helps to decrease the number and frequency of bowel movements. It works by slowing the movement of the intestines. Difenoxin is similar to opioid pain relievers, but it acts mainly to slow the gut. Atropine belongs to a class of drugs known as anticholinergics, which help to dry up body fluids and also slow gut movement.

Dosage

Take this medication by mouth, usually after each loose stool, or every 3 or 4 hours as needed or as directed by your doctor. Dosage is based on your medical condition and response to therapy. For adults, do not take more than 8 milligrams of difenoxin in any 24-hour period. If you need to continue treatment once your diarrhea is controlled, your doctor may direct you to lower your dosage. Do not increase your dose, take it more often, or use it for longer than prescribed.

Side effects

Drowsiness, dizziness, headache, tiredness, blurred vision, dry mouth, and loss of appetite may occur. If any of these effects persist or worsen, tell your doctor
or pharmacist promptly.

Some products that may interact with this drug are: ambenonium, MAO inhibitors (isocarboxazid, linezolid, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine), naltrexone, potassium tablets/capsules, pramlintide.
Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).

Alerts

Before taking difenoxin with atropine, tell your doctor or pharmacist if you are allergic to either drug; or to hyoscyamine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: liver disease (e.g., obstructive jaundice, cirrhosis), diarrhea caused by certain types of infections (Clostridium difficile-associated diarrhea following recent antibiotic therapy, bacterial infection of the gut caused by E. coli, Salmonella, Shigella).
Before using this medication, tell your doctor or pharmacist your medical history, especially of: current dehydration or mineral imbalance, a certain type of bowel disease (acute ulcerative colitis), personal or family history of glaucoma (angle-closure type).
This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).
This drug is not recommended for use in children younger than 2 years. Caution is advised when using this drug in children, particularly those with Down's syndrome, because they may be more sensitive to the following side effects: high fever, fast heartbeat, decreased urination, flushing, dry skin/mouth, thirst. Very serious (possibly life-threatening) effects may occur if too much of this medication is taken by children.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

Points of recommendation

Before taking difenoxin with atropine, tell your doctor or pharmacist if you are allergic to either drug; or to hyoscyamine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: liver disease (e.g., obstructive jaundice, cirrhosis), diarrhea caused by certain types of infections (Clostridium difficile-associated diarrhea following recent antibiotic therapy, bacterial infection of the gut caused by E. coli, Salmonella, Shigella).
Before using this medication, tell your doctor or pharmacist your medical history, especially of: current dehydration or mineral imbalance, a certain type of bowel disease (acute ulcerative colitis), personal or family history of glaucoma (angle-closure type).
This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).
This drug is not recommended for use in children younger than 2 years. Caution is advised when using this drug in children, particularly those with Down's syndrome, because they may be more sensitive to the following side effects: high fever, fast heartbeat, decreased urination, flushing, dry skin/mouth, thirst. Very serious (possibly life-threatening) effects may occur if too much of this medication is taken by children.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
This medication passes into breast milk. Consult your doctor before breast-feeding.


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