Diphenoxylate Hydrochloride and Atropine Sulfate

Uses

Doctors recommend diphenoxylate hydrochloride and atropine sulfate to patients suffering from diarrhea.

General Drug Information

Drug makers offer diphenoxylate hydrochloride and atropine sulfate as a tablet or solution for oral use. Many pharmaceutical companies offer generic preparations of diphenoxylate hydrochloride and atropine sulfate; a division of Pfizer Inc. offers diphenoxylate hydrochloride and atropine sulfate as the brand name preparation, Lomotil.

These preparations typically contain 2.5 mg of diphenoxylate hydrochloride and 0.025 mg of atropine sulfate.

Diphenoxylate hydrochloride is an opioid drug, sometimes referred to as a narcotic. Recreational drug users target opioids because of the euphoria these drugs produce. Drug makers add atropine sulfate to discourage abuse.

Administration/Dosage

Consumers should not exceed recommended doses.

Patients may require higher initial doses to gain control over diarrhea before lowering dosages to meet individual need. Most consumers see improvement within the first 48 hours of treatment. The usual initial dosage for adults is two tablets four times each day. Initial adult dosage for liquid preparations is two 5 mL teaspoons four times daily. An adult patient may maintain control with dosages as low as two tablets or 10 mL of diphenoxylate hydrochloride and atropine sulfate daily. If the patient does experience improvement within 10 days, the prescribing physician should consider another form of treatment as continuing diphenoxylate hydrochloride and atropine sulfate is not likely to work.

Diphenoxylate hydrochloride and atropine sulfate is not appropriate for children younger than two years. Caregivers should exercise special caution when administering to young children. Physicians should consider the child’s nutritional status and degree of dehydration when prescribing diphenoxylate hydrochloride and atropine sulfate. Children under the age of 13 years should use diphenoxylate hydrochloride and atropine sulfate solution rather than tablets.

Pediatricians base dosages for children on the child’s weight. Doctors and pharmacists discuss pediatric diphenoxylate hydrochloride and atropine sulfate doses in terms of milligrams of medicine per kilogram of body weight, or mg/kg. The total daily-recommended dose for children is 0.3 to 0.4 mg/kg divided into four equal doses throughout the day. This means the average 2-year old weighing 25 lbs will receive 1.5 to 3 mL of diphenoxylate hydrochloride and atropine sulfate four times a day while a 12-year old who weighs 120 lbs might take 3.5 to 5 mL four times daily.

Pediatricians should reduce dosages for children as soon as possible. Maintenance doses for children may be as low as one-fourth the initial dosages. If a child does not respond to diphenoxylate hydrochloride and atropine sulfate within 48 hours, pediatricians should consider alternate therapies.

Administrators should always use an approved measuring device when dispensing diphenoxylate hydrochloride and atropine sulfate solutions, especially for administration to children. A household spoon may yield inaccurate doses, causing ineffective doses or toxic overdoses.

Action

Diphenoxylate hydrochloride slows peristalsis, the action that pushes stool through the intestines. This gives the intestines more time to absorb excess liquid from the stool.

Drug makers add small amounts of atropine sulfate as a deterrent to drug abuse. Large amounts of atropine make the consumer feel very weak and nauseated.

Warnings

Diphenoxylate hydrochloride and atropine sulfate preparations are not harmless. Consumers should adhere to recommendations, especially when used by children. Diphenoxylate hydrochloride and atropine sulfate is not appropriate for use in children younger than 2 years. An overdose of diphenoxylate hydrochloride and atropine sulfate may cause severe breathing problems and coma, possibly leading to permanent brain damage or death.

Respiratory Depression

Opioids work with the central nervous system to relieve pain, cause sedation and slow breathing. Depression of the respiratory centers of the brain may result in the dangerous breathing condition, respiratory depression. Signs of respiratory depression include slow, shallow and irregular breathing patterns along with a bluish tint around the victim’s eyes, mouth and fingertips.

Dehydration and Electrolyte Imbalances

Severe and prolonged diarrhea may cause dehydration and imbalances in electrolytes such as potassium and sodium. Patients should participate in fluid and electrolyte replacement therapy while taking diphenoxylate hydrochloride and atropine sulfate as necessary. Patients suffering from severe dehydration or electrolyte imbalance should tend to these conditions before beginning diphenoxylate hydrochloride and atropine sulfate therapy, as taking drugs that inhibit peristalsis may cause fluid retention in the intestine that can further aggravate dehydration and electrolyte imbalances.

Special Risk Consumers

Caregivers should exercise special caution when giving diphenoxylate hydrochloride and atropine sulfate to young children because young patients may be more vulnerable to a delayed onset of accidental pediatric overdose in which the signs of toxic overdose do not appear immediately. Additionally, young patients experience a wider variety of responses to diphenoxylate hydrochloride and atropine sulfate than do older ones, producing inconsistent and sometimes dangerous results.

Physicians should not prescribe diphenoxylate hydrochloride and atropine sulfate for patients suffering diarrhea resulting from certain types of bacterial infections, including E. coli, salmonella and shigella. Diphenoxylate hydrochloride and atropine sulfate is not appropriate for treating diarrhea caused by some types of antibiotics.

Physicians should closely monitor the condition of diphenoxylate hydrochloride and atropine sulfate consumers suffering from the intestinal condition, acute ulcerative colitis. This drug may slow peristalsis to the point of causing dangerous widening of the intestine, known as toxic megacolon. These consumers should discontinue diphenoxylate hydrochloride and atropine sulfate promptly if they experience swelling of the stomach or other symptoms suggesting toxic megacolon.

Patients with advanced liver or kidney disease should exercise extreme caution when using diphenoxylate hydrochloride and atropine sulfate, as liver failure may cause the patient to become comatose.

Precautions

Diphenoxylate hydrochloride and atropine sulfate can cause drowsiness or dizziness and can interfere with activities that require mental alertness. Alcohol, barbiturates and other opioids can enhance these effects. Consumers should exercise caution while operating motor vehicles or heavy machinery.

Contraindications

Diphenoxylate hydrochloride and atropine sulfate may not be appropriate for all patients. Those with a known hypersensitivity to diphenoxylate hydrochloride, atropine sulfate or any inactive ingredient in these preparations should not use these products.

Patients with yellowing of the skin and eyes due to an obstruction in the flow of bile from the liver should not use diphenoxylate hydrochloride and atropine sulfate.

Diphenoxylate hydrochloride and atropine sulfate is not appropriate for the treatment of diarrhea caused by certain types of bacterial infections or antibiotic use.

Pregnancy, Labor and Delivery, Breastfeeding

The FDA rates diphenoxylate hydrochloride and atropine sulfate as a , meaning there are no adequately controlled studies in humans to determine how this drug affects a pregnant woman or fetus, or if it affects male or female reproductive capabilities. A pregnant woman should use diphenoxylate hydrochloride and atropine sulfate only when the benefits to her health clearly outweigh the possible risks.

Diphenoxylate hydrochloride may pass into human milk. Atropine sulfate does pass from the mother to the baby through breast milk. Since scientists do not know the possible effects on a nursing baby, mothers should not breastfeed while using diphenoxylate hydrochloride and atropine sulfate.

Drug Interactions

Diphenoxylate hydrochloride and atropine sulfate can interact with other medications in dangerous or undesirable ways.

Diphenoxylate hydrochloride and atropine sulfate may interact with MAOIs, commonly prescribed to treat depression or high blood pressure, to cause dangerously high blood pressure.

Diphenoxylate hydrochloride and atropine sulfate can enhance the effects of alcohol, tranquilizers and barbiturates. When the patient needs both diphenoxylate hydrochloride and atropine sulfate and these substances, physicians should monitor the patient closely.

Side effects

All drugs, including therapeutic doses of diphenoxylate hydrochloride and atropine sulfate, can cause adverse reactions in some consumers.

Diphenoxylate hydrochloride can cause headache, restlessness, dizziness, drowsiness, itching, stomachache, nausea and vomiting, and loss of appetite. The consumer may also experience confusion, itching, lack of energy, mood changes, and rash. Serious diphenoxylate hydrochloride side effects include numbness in the extremities, swelling, the serious form of an allergic reaction known as anaphylaxis, toxic megacolon, pancreatitis and the dangerous intestinal problem, paralytic ileus.

Atropine sulfate can cause adverse reactions such as high body temperature, rapid heartbeat, urinary retention, dryness of the skin and mucus membranes, including those in the nose and mouth. Consumers may experience flushing, which is an uncomfortable warmth and redness that spread across the face and throat. Children are at special risk for suffering these effects.

Overdose

Diphenoxylate hydrochloride and atropine sulfate overdose is a dangerous and sometimes fatal condition. An overdose in a child may cause severe, even fatal respiratory depression. Early signs of diphenoxylate hydrochloride and atropine sulfate overdose include dry skin and mucus membranes, wide pupils, restlessness, flushing, high body temperature and rapid pulse. Later, the patient may fall into a coma or have unresponsive reflexes, erratic eye movements, pinpoint pupils and respiratory depression.

Diphenoxylate hydrochloride and atropine sulfate overdose requires immediate medical care. Emergency department workers will ask the patient to drink ipecac to induce vomiting then pump the patient’s stomach to remove excess diphenoxylate hydrochloride and atropine sulfate. Nurses will introduce a slurry of 100 grams of activated charcoal into the alert patient’s stomach to absorb any residual medication.
Nurses will help the patient breathe by sliding a flexible tube into the patient’s throat to hold his airway open; nurses may connect this tube to a mechanical ventilator to take over breathing responsibilities.

Physicians will order naloxone to reverse the effects of respiratory depression if the patient shows signs of breathing problems. The typical adult dose is 0.4 mg to 2 mg administered intravenously, while the usual pediatric dose is 0.01 mg/kg intravenously. Naloxone usually takes effect within two minutes; intravenous administration provides faster relief than other routes but this relief is shorter lived than when injected into a muscle or just under the skin. Caregivers can repeat doses of naloxone every two minutes, as the respiratory depressant effects of diphenoxylate hydrochloride often outlast the therapeutic effects of naloxone. If the adult patient does not experience relief from respiratory depression after a total of 10 mg naloxone, the attending physician should consider a different course of action as further administration of naloxone is unlikely to produce positive results.

The signs of respiratory depression may appear as late as 30 hours after the toxic overdose and may resist treatment, recurring many hours later. Emergency department physicians should admit the patient for close observation for at least 48 hours.

Abuse

The ranks diphenoxylate hydrochloride and atropine sulfate as a class V drug, meaning it poses a relatively low risk for abuse. Despite this low risk, diphenoxylate hydrochloride and atropine sulfate is available only by prescription.

Withdrawal

At high doses, diphenoxylate hydrochloride produces a pleasant feeling of euphoria similar to that associated with morphine. At therapeutic doses, diphenoxylate hydrochloride and atropine sulfate does not cause euphoria. There is a wide gap between dosage prescribed to treat diarrhea and dosages strong enough to produce euphoria.

Anyone who takes large doses of opioids regularly for more than a few weeks can become opioid-dependent and suffer uncomfortable withdrawal symptoms when he stops using opioids suddenly. Someone would have to take 40 to 120 diphenoxylate hydrochloride and atropine sulfate tablets for 40 to 70 days to become opioid-dependent.

Withdrawal causes uncomfortable flu-like symptoms, such as body aches, stomachache, sweating, chills, insomnia, and irritability. Without intervention, these symptoms last for five or more days before disappearing. These symptoms will not return unless the patient again becomes opioid-dependent. The patient may stop the withdrawal symptoms by taking more diphenoxylate hydrochloride but relapsing to opioid use returns the patient to an opioid-dependent state.

To avoid withdrawal symptoms, doctors suggest patient wean themselves from opioids by taking successively smaller doses increasingly further apart. While this tapering method works well for most consumers, persistent and severe withdrawal symptoms prevent many from stopping diphenoxylate hydrochloride and atropine sulfate when they no longer need it to control diarrhea.

Detox

The estimates there are almost 2 million opioid-dependent people across the United States. Many hospitals and local healthcare institutions are addressing this need by offering detoxification services. Detoxification typically includes drugs that interfere with the action of diphenoxylate hydrochloride along with medications to relieve the resulting withdrawal symptoms. Detoxification eases the severity of withdrawal symptoms but does not shorten the duration of withdrawal symptoms.

Many informed consumers now choose rapid detox to help them overcome withdrawal symptoms associated with opioids such as diphenoxylate hydrochloride. Rapid detox patients receive sedation and anesthesia prior to the standard detoxification and anti-withdrawal drugs so the rapid detox patient rests in a comfortable “twilight sleep” during the difficult detoxification process. The rapid detox patient awakens a few hours later, rested and renewed.

Storage

Consumers and caregivers should store diphenoxylate hydrochloride and atropine sulfate preparations at temperatures between 68 and 77 degrees Fahrenheit, in a tightly sealed container and out of the reach of children.

Consumers should throw away opened bottles of diphenoxylate hydrochloride and atropine sulfate solution after 90 days.

Miscellaneous information

Liquid formulas of diphenoxylate hydrochloride and atropine sulfate may be cherry flavored.