Diphenoxylate hydrochloride

Drug Class: Diphenoxylate Hydrochloride > Diphenoxylate > Fully Synthetic Opioid > Opioids > Opioid Agonist > Analgesic.

Uses

Physicians prescribe diphenoxylate hydrochloride to treat a patient’s diarrhea.

General Drug Information

Physicians Total Care, Inc. offers diphenoxylate hydrochloride as the brand name anti-diarrheal, Lomotil, in tablet or liquid forms for oral use.

Diphenoxylate hydrochloride is an opioid drug. Recreational drug users abuse because of the pleasant euphoric feeling they produce. Drug makers add atropine sulfate to diphenoxylate hydrochloride products to deter abuse, as large doses of atropine makes the consumer severely nauseated and weak.

Administration/Dosage

The recommended dosage for adults is two diphenoxylate hydrochloride tablets four times each day or two 5 mL teaspoonfuls of diphenoxylate hydrochloride liquid four times daily. Most patients stay on this high dosage until they gain control over diarrhea, after which they may reduce dosages to 5 mg, or 2 tablets or 10 mL of liquid each day.

Pediatricians base a child’s dosage on the patient’s body weight in kilograms. Doctors and pharmacists discuss pediatric doses in terms of milligrams of diphenoxylate hydrochloride per kilogram of body weight, or mg/kg. The recommended initial total daily dosage for children is 0.3 to 0.4 mg/kg, divided into four equal doses throughout the day. Pediatricians should prescribe the lowest effective dose to reduce side effects.

Patients usually see improvement within 48 hours of starting treatment. If an adult patient taking the maximum daily dosage of 20 mg diphenoxylate hydrochloride does not see improvement within 10 days, physicians should consider another course of treatment as continuing diphenoxylate hydrochloride treatment is not likely to work.

Children younger than 2 years old should not use diphenoxylate hydrochloride. Caregivers should exercise caution when giving diphenoxylate hydrochloride to young children. Caregivers should give diphenoxylate hydrochloride liquid rather than diphenoxylate hydrochloride tablets to children under the age of 13 years old.

Administrators should use the plastic dropper provided when dispensing diphenoxylate hydrochloride, especially to children. Caregivers or consumers should not use a household spoon as doing so may result in inadequate doses or dangerous overdoses.

Action

Diphenoxylate hydrochloride slows the rate at which stool moves through the intestines, a motion known as peristalsis. Diphenoxylate hydrochloride increases the tone of the intestinal muscles that propel stool through the digestive tract to stiffen them and make them less functional, slowing peristalsis. This gives the intestines more time to absorb excess water from the stool. Diphenoxylate hydrochloride is an anti-peristaltic drug because it slows down peristalsis.

Opioids like diphenoxylate hydrochloride depress the central nervous system, or CNS, to cause pain relief, sedation and a pleasant sense of euphoria. Opioids also depress respiratory centers in the brain to slow breathing.

Warnings

Respiratory Depression

Large doses of opioids, including diphenoxylate hydrochloride, depress respiratory centers in the brain enough to cause respiratory depression, a serious and sometimes fatal breathing problem. During respiratory depression, the lungs do a poor job of exchanging spent carbon dioxide for fresh oxygen.

Pediatric Use

Diphenoxylate hydrochloride is not a harmless drug - patients should adhere to recommendations, especially when administering diphenoxylate hydrochloride to a child. Diphenoxylate hydrochloride is not appropriate for children younger than two years. Overdose in a child may result in respiratory depression and coma, possibly leading to permanent brain damage or death.

Caregivers should exercise special caution when administering diphenoxylate hydrochloride to young children, as these patients may be vulnerable to delayed diphenoxylate toxicity and because these young consumers have a wide variety of responses to diphenoxylate hydrochloride.

Consumers and caregivers should keep diphenoxylate hydrochloride out of the reach of children.

Severe Diarrhea and Electrolyte Imbalances

Severe diarrhea can cause dehydration and imbalances in electrolytes, such potassium and sodium. Patients should drink extra fluids or receive intravenous fluids and participate in electrolyte replacement therapy as necessary. In cases of extreme dehydration or electrolyte imbalances, the patient should not take diphenoxylate hydrochloride until he has begun therapy to correct these fluid problems. Taking diphenoxylate hydrochloride during periods of extreme dehydration or electrolyte imbalance may cause fluid retention in the intestines, worsening dehydration and electrolyte imbalance.

Diarrhea Caused by Bacterial Infections and Antibiotic Use

Physicians should not prescribe diphenoxylate hydrochloride to treat diarrhea caused by certain organisms, such as E. coli, salmonella and shigella, or antibiotics. Diphenoxylate hydrochloride may prolong or worsen diarrhea in these conditions.

Use in Special Risk Patients

Physicians should exercise care when prescribing diphenoxylate hydrochloride for patients with an acute case of intestinal inflammation known as ulcerative colitis. In some cases of acute ulcerative colitis, anti- peristaltic drugs like diphenoxylate hydrochloride can cause the extremely serious condition known as toxic megacolon, which is a sudden widening of the intestine. Physicians and caregivers should monitor the condition of these consumers closely and discontinue diphenoxylate hydrochloride treatment immediately if the patient’s stomach begins to swell.

Physicians should exercise extreme caution when prescribing diphenoxylate hydrochloride to patients with advanced liver or kidney disease. Diphenoxylate hydrochloride may cause coma in patients with abnormal liver function.

Diphenoxylate hydrochloride can enhance the effects of alcohol, barbiturates and tranquilizers. Caretakers should closely monitor patients who use both diphenoxylate hydrochloride and these other substances together.

Precautions

Diphenoxylate hydrochloride can make the consumer feel drowsy or dizzy. Like other opioids, diphenoxylate hydrochloride can impair the user’s physical and mental capabilities. Using alcohol, barbiturates or other opioids enhance these effects. Consumers should not operate a motor vehicle or other heavy equipment until they know how diphenoxylate hydrochloride affects them.

Drug manufacturers often add atropine to diphenoxylate hydrochloride as a deterrent to abuse. Like diphenoxylate hydrochloride, atropine is not a harmless drug. Physicians and consumers should consider any effect atropine has before using diphenoxylate hydrochloride. Atropine can cause unsafe or unpleasant effects, especially for pediatric consumers with Down’s syndrome.

Contraindications

Diphenoxylate hydrochloride is not appropriate for everyone.

Individuals with a known hypersensitivity to diphenoxylate hydrochloride should not use products containing this opioid. Since drug makers frequently add atropine to diphenoxylate hydrochloride products, those with atropine hypersensitivity should avoid this product.

Patients with the serious liver problem known as obstructive jaundice should avoid diphenoxylate hydrochloride products. Obstructive jaundice is yellowing of the skin and eyes caused by an obstruction to the flow of bile, sometimes brought about by hepatitis or liver cancer.

Patients suffering from diarrhea caused by certain bacterial infections should not use diphenoxylate hydrochloride. Diphenoxylate hydrochloride is not for treating diarrhea caused by some antibiotics.

Pregnancy, Labor and Delivery, Breastfeeding

Diphenoxylate hydrochloride is an FDA , as researchers have not yet established its potential to cause harm to a pregnant woman or unborn baby or if it affects male or female reproductive capabilities. Pregnant women should use diphenoxylate hydrochloride only if the benefits clearly outweigh the possible risks.

Diphenoxylate hydrochloride may pass from the mother to her nursing baby. Scientists do not yet know how this might affect the infant. Women should discontinue breastfeeding while taking diphenoxylate hydrochloride to avoid possible risk to her child.

Drug Interactions

Diphenoxylate hydrochloride can interact with other medications to produce unsafe or unintended results. Patients should supply a list of all their medications, including prescription and over-the-counter remedies, to their physicians to avoid possible drug interactions.

Alcohol, tranquilizers and barbiturates enhance the effects of diphenoxylate hydrochloride.

Diphenoxylate hydrochloride may interact with the class of drugs known as MAOIs, commonly prescribed to treat depression and high blood pressure, to cause high blood pressure.

Side effects

All medications, including diphenoxylate hydrochloride, can cause side effects in some patients. Consumers have commonly reported non-serious side effects, such as headache, restlessness, dizziness, and drowsiness. Diphenoxylate hydrochloride may cause lack of energy, confusion, mood changes, stomachache, itching, nausea and vomiting, and loss of appetite.

Serious side effects include numbness in the patient’s extremities, swelling, allergic reactions, pancreatitis and the serious digestive disorders, toxic megacolon and paralytic ileus. Paralytic ileus is a condition where part of the intestine stops working.

Overdose

Diphenoxylate hydrochloride overdose is a serious medical emergency that could result in severe respiratory depression, coma, permanent brain damage or death. Nearly die each year following an overdose of prescription painkillers, many of them from opioids such as diphenoxylate hydrochloride.

Consumers and healthcare providers should keep diphenoxylate hydrochloride in a child-resistant container and out of the reach of children to prevent accidental overdose.

Early symptoms of a diphenoxylate hydrochloride overdose include dry skin and mucus membranes, like those in the nose and mouth. The victim may seem restless and have wide pupils, warmth and redness that spread across the face and neck, high body temperature and rapid heartbeat. Later, the patient may be lethargic or fall into a coma, poor reflexes, involuntary eye movements, pinpoint pupils and respiratory depression. Respiratory depression may occur as late as 30 hours after ingestion of the diphenoxylate hydrochloride overdose. Respiratory depression may recur, despite treatment.

All diphenoxylate hydrochloride are serious conditions requiring immediate medical attention and observation. Emergency department workers will ask the patient to drink ipecac to induce vomiting or pump excess medication from the patient’s stomach immediately followed by 100 grams of activated charcoal to absorb any remaining diphenoxylate hydrochloride. Healthcare providers will help the patient breathing by introducing a flexible tube into the patient’s throat to hold his airway open; workers may attach this tube to a mechanical ventilator that takes over breathing responsibilities.

Doctors may order an initial dose of 0.4 mg to 2 mg of naloxone to reverse respiratory depression if the patient shows signs of breathing trouble. Pediatric doses are 0.1 mg/kg given intravenously. Intravenous administration of naloxone brings relief within two minutes but its effects wear off quickly; administration into a muscle or just under the skin provides a slower onset of relief but a more prolonged effect. The respiratory effects of diphenoxylate hydrochloride frequently outlast the therapeutic effects of naloxone, so doctors may order repeat doses every two to three minutes. If the patient’s respiratory depression does not improve after a total of 10 mg naloxone, physicians should consider another form of treatment as subsequent doses are not likely to help.

Emergency department physicians should admit the patient for observation for at least 48 hours.

Abuse

Diphenoxylate hydrochloride is a class V drug, meaning it poses a relatively low risk for abuse. To reduce even this low risk, diphenoxylate hydrochloride products are available only by prescription.

Therapeutic doses of diphenoxylate hydrochloride do not produce morphine-like euphoria or pose a risk for addiction. High doses of diphenoxylate hydrochloride do pose these risks. There is a wide gap between therapeutic doses and doses causing euphoria and addiction.

Withdrawal

Regular use of very high doses of diphenoxylate hydrochloride can cause the consumer to become opioid-dependent and suffer withdrawal symptoms when he stops using diphenoxylate hydrochloride. Someone would have to take 100 mg to 300 mg, the equivalent of 40 to 120 tablets, for 40 - 70 days to become dependent on diphenoxylate hydrochloride.

Physicians suggest opioid-dependent people wean themselves from diphenoxylate hydrochloride by taking smaller doses further apart. This tapering method works for the majority of people but, according to statistics cited by the , almost 2 million Americans are opioid-dependent at any given time.

Detox

Local healthcare institutions are addressing the widespread need of opioid-dependent people by offering detoxification services. Detoxification usually entails drugs to counteract the effects of diphenoxylate hydrochloride plus medications to soothe the ensuing withdrawal symptoms. Detoxification reduces the severity of withdrawal symptoms to tolerable levels and provides professional monitoring against complications, such as dehydration or relapse.

Many informed patients now choose rapid detox, a more humane and efficient approach to detoxification. Rapid detox doctors sedate and anesthetize patients before giving them the usual detoxification and anti-withdrawal drugs. These patients rest in a comfortable “twilight sleep,” blissfully unaware of the grueling detoxification process. Rapid detox patients awaken a few hours later, refreshed and renewed.

Storage

Consumers and administrators should store diphenoxylate hydrochloride out of the reach of children. Consumers should never share prescription opioid drugs with other individuals, even if the individuals share similar symptoms.

Miscellaneous information

Janssen Laboratories discovered diphenoxylate hydrochloride in 1956.

Astronauts used the brand name diphenoxylate hydrochloride preparation, Lomotil, during the Apollo space program.