Approved by the U.S. Food and Drug Administration (FDA) in 1960, Lomotil is a brand name for the generic drug diphenoxylate and atropine. Each Lomotil tablet contains 2.5 mg diphenoxylate hydrochloride and .025 mg atropine sulfate. Diphenoxylate hydrochloride is an antidiarrheal drug. A small amount of the anticholinergic atropine sulfate is added to discourage deliberate abuse. Atropine sulfate causes unpleasant side effects like rapid heart rate, dry mouth and blurry vision, however, a significantly high dose is required to produce these intolerable side effects.
Why Is Lomotil a Controlled Substance?
Lomotil is federally regulated and classified as a Schedule V controlled substance because diphenoxylate hydrochloride is a manmade substance chemically related to the narcotic analgesic meperidine (Demerol). Although diphenoxylate is chemically related to Demerol, it does not impart pain-relieving (analgesic) effects like most narcotics. At higher doses, diphenoxylate causes codeine-like effects, euphoria (elevation of mood), physical dependence and addiction.
When Lomotil is digested, it is essentially converted into mild type of opioid. At regular doses, it isn’t strong enough to produce the euphoria associated with opioid painkillers. It takes excessive concentration in the bloodstream to produce a high, which is why people who abuse lomotil often take a massive number of pills.
An Indian study on 41 males found the average number of diphenoxylate tablets being consumed daily ranged from 3 to 250. The maximum number of tablets consumed a day varied from 6 to 400. The majority of individuals (38) had tried other opioids and suffered from co-occurring substance dependence (nicotine: 31, alcohol: 15, sedatives: 5 and cannabis: 1). The most common reason for taking diphenoxylate was to reduce withdrawal symptoms when other opiates were not available. Other reasons included because it was a cheap opioid substitute, curiosity and a suggestion from friends.
Lomotil vs. Imodium
Some people may be under the impression the over-the-counter medication Imodium-AD (loperamide) is harmless and far safer than Lomotil. The truth is this popular OTC antidiarrheal drug is also subject to growing abuse. In the spring of 2017, the FDA added a warning to the product label to warn consumers against ingesting high doses of loperamide. In January 2018, the FDA asked manufacturers to add additional package changes in an effort to curb the ongoing opioid epidemic. These measures included limiting the amount of loperamide per package for short-term use. For example, a retail package could contain eight 2-mg capsules for two days. “When higher than recommended doses are taken we’ve received reports of serious heart problems and deaths with loperamide, particularly among people who are intentionally misusing or abusing high doses,” said Dr. Scott Gottlieb, FDA commissioner in the news release. The maximum approved daily dose for adults is 8 mg per day for OTC use and 16 mg per day for prescription use. Prescription loperamide is used to control acute diarrhea and ongoing diarrhea associated with inflammatory bowel disease.
According to a 2016 study published in the Annals of Emergency Medicine, when taken in massive doses, loperamide imparts the same effects on the body as heroin, morphine and oxycodone. The study found loperamide abuse led to cardiac dysrhythmia (abnormal heart rhythm) and two fatalities at high doses. This is of particular concern because the drug is far cheaper than prescription opioids. In some cases, 400 tablets generic OTC tablets can be purchased for less than $10.
Lomotil is recommended as adjunctive therapy for the management of diarrhea in individuals ages 13 and older. The medication slows contraction of the intestines and decreases bowel movements. Prior to starting Lomotil, it’s important to assess the nutritional and dehydration status of individuals suffering from diarrhea. The use of Lomotil should be accompanied by appropriate fluid and electrolyte therapy if necessary. As such, if you have been prescribed Lomotil for diarrhea, you may have been given fluids or salt tablets to address dehydration.
The initial adult dosage is two Lomotil tablets four times daily, with a maximum total daily dose of 20 mg per day. The recommended dosage of liquid Lomotil is 10 ml (two regular tsp) four times daily. Most individuals require this dosage until diarrhea is under control. Often, diarrhea control is maintained with as little as two Lomotil tablets daily, although this can vary by individual. If an individual does not show clinical improvement of chronic diarrhea utilizing the maximum recommended daily dosage within 10 days, Lomotil should be discontinued.
An atropine and diphenoxylate overdose is more likely to affect children. This can cause breathing problems, permanent brain damage or death. Only the liquid form should be used in children younger than 13. Extra water should be consumed by anyone taking this medication to prevent dehydration.
Monoamine oxidase inhibitors (MAO’s) in combination with Lomotil can cause severe high blood pressure and increase the risk of stroke. Drugs that increase the propulsion of intestinal contents can theoretically reduce the effectiveness of Lomotil (e.g. bethanechol, cisapride, metoclopramide and erythromycin). Drugs that decrease the propulsion of intestinal contents may increase the effects of diphenoxylate and cause constipation. This drug list is long, including hyoscyamine, select antihistamines, prescription opioids like oxycodone and hydrocodone, a few phenothiazine antipsychotics and some tricyclic antidepressants. In addition, taking Lomotil with alcohol or any other central nervous system depressants can cause excessive and potentially fatal sedation. This includes barbiturates and benzodiazepines (e.g. lorazepam, diazepam temazepam, oxazepam, clonazepam, zolpidem and narcotics).
Lomotil Side Effects
When taken at the recommended dosage, Lomotil is relatively safe, however, like any medication, side effects are possible. Common side effects include:
- Blurred vision
- Dry mouth
- Upset stomach
- Loss of appetite
- Skin rash
Serious Side Effects
Stop using the medication and call your doctor immediately if you suffer from any of these serious side effects:
- Stomach pain or bloating
- Ongoing or worsening diarrhea
- Watery or bloody diarrhea
- Numbness in hands or feet
- Depressed mood
- Unusual thoughts or behavior
- Rapid heart rate
- Decreased or absent urination
Abusing diphenoxylate or loperamide can increase the risk and severity of side effects and lead to dependence. Only take these antidiarrheal medications as recommended and follow all precautions.