What is Lomotil

Lomotil is a prescription medicine (2.5 mg diphenoxylate and 0.025 mg atropine combination ) used to treat acute or chronic diarrhea. Lomotil contains diphenoxylate hydrochloride and atropine sulfate along with other ingredients. The diphenoxylate primarily affects the opiate receptors in the intestine thus reduces diarrhea by slowing down the movements of the intestines – causing constipation and preventing diarrhea. Because diphenoxylate may be abused by taking it in doses that are larger than prescribed, a small amount of atropine sulfate is included in Lomotil. This causes unpleasant effects if larger than normal doses of Lomotil are taken and discourages abuse.

Lomotil (2.5 mg diphenoxylate and 0.025 mg atropine combination) has been used as an antidiarrheal since a long time and had been approved by the Food and Drug Administration (FDA) in 1960s.

Lomotil, in pack sizes of 20 and 100 tablets, is only available with a doctor’s prescription. Lomotil in a pack size of 8 tablets is available as a pharmacist only medicine.

Lomotil is available as tablets 2.5 mg of diphenoxylate with 0.025 mg of atropine and as a solution of similar concentration in 5 mL generically and under the brand name Lomotil. The usual dose in adults is 5 mg four times a day for until diarrhea is controlled, followed by 2.5 mg up to four times daily as needed.

Why is lomotil a controlled substance?

Lomotil is a controlled substance because of the presence of diphenoxylate which is a synthetic opioid that may be abused ¹. Diphenoxylate has been hence kept in schedule V of controlled substances of the FDA ². There have been however, only case reports of diphenoxylate being abused by patients with medical illnesses and substance users ³. It has also been tried during detoxification from opioids and has been shown to decrease withdrawals ⁴.

Diphenoxylate is similar to loperamide and is not structurally related to morphine or codeine, and has minimal euphoric or analgesic effects, largely because it is given in low doses and in fixed combination with atropine. Diphenoxylate hydrochloride is devoid of morphine-like subjective effects at therapeutic doses ¹. At high doses, it exhibits codeine-like subjective effects. To limit the extent to which Lomotil can be abused, a small amount of atropine is added to prevent abuse and excessive intake, which can also augment the anti-diarrheal effect of diphenoxylate, however, at high doses causes unpleasant side effects like tachycardia, dry mouth and blurring of vision. However, a considerably high dose of atropine is required to produce these intolerable side-effects ⁵. Thus abuse of diphenoxylate for opiate like effects becomes a valid possibility.

Lomotil safety precautions

When you must not use Lomotil

DO NOT take Lomotil if you are allergic to:

• Diphenoxylate or atropine or any of the tablet ingredients listed at the end of this leaflet
• If you have an allergic reaction you may get a skin rash, difficulty in breathing, hayfever or faintness.
• You have jaundice
• You have diarrhea caused by pseudomembranous enterocolitis (a potentially serious infection of the gut) which may occur during or up to several weeks following antibiotic treatment
• You have an inflammatory bowel disease such as ulcerative colitis or Crohn’s disease
• You have bacterial colitis or amoebic colitis.
• You are breastfeeding. You should use an alternative form of infant feeding while you are taking Lomotil. Lomotil passes into breast milk, so if you take Lomotil while breastfeeding, your baby may have some effects from it.

Do not use Lomotil if you have diarrhea that is caused by bacteria or by taking an antibiotic.

You should not use Lomotil if you have a bile duct disorder causing jaundice (yellowing of your skin or eyes).

Keep this medicine where a child cannot reach it. An overdose can be fatal to a child.

Lomotil is NOT recommended for children less than 13 years old.

Children, especially very young children and those with Down’s syndrome, are very sensitive to the effects of Lomotil.

Lomotil must be kept out of the reach of children, since accidental overdose in children may result in serious breathing difficulties, or even death.

• Do not use tablets after the use by date, which appears on the label after the letters “EXP”.
• They may have no effects at all, or an entirely unexpected effect if you use them after the expiry date.
• Do not use Lomotil if the packaging is torn or shows signs of tampering.
• Do not use Lomotil to treat any other complaints unless your doctor says to.
• Do not give this medicine to anyone else, even if their symptoms seem similar to yours.

Before you start to use Lomotil

You must tell your doctor if:

• You are allergic to any other medicines, or foods, dyes or preservatives
• You have any other medical conditions, especially:
  • Liver disease, jaundice
  • Kidney disease
  • Colitis
  • History of drug abuse
• You are taking any other medicines, including medicines that you buy without a prescription from a pharmacy, supermarket or health food shop.

Some of the medicines in common use that may interfere with Lomotil include:

• Tranquillizers – medicines used to produce calmness, treat anxiety or help you sleep
• Antidepressants – medicines used to treat depression, such as monoamine oxidase inhibitors (MAOI)
• Barbiturates – medicines used to treat epilepsy and to help you sleep.

These medicines may be affected by Lomotil, or may affect how well it works. You may need to take different amounts of your medicine or you may need to take different medicines. Your doctor or pharmacist has a more complete list of medicines to avoid while taking Lomotil.

Do not drink alcohol while taking Lomotil.

Tell your doctor if you become pregnant while you are taking Lomotil.

• You should not take Lomotil near or at the time of giving birth, because diphenoxylate is chemically related to medicines which can slow down the breathing of newborn infants.

What should I avoid while taking Lomotil?

Avoid driving or hazardous activity until you know how Lomotil will affect you. Your reactions could be impaired.

Avoid becoming overheated or dehydrated during exercise, in hot weather, or by not drinking enough fluids. Follow your doctor’s instructions about the type and amount of liquids you should drink.

Drinking alcohol with Lomotil can cause side effects.

What other drugs will affect Lomotil?

Using Lomotil with other drugs that make you drowsy can worsen this effect. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, cold or allergy medicine, or medicine for anxiety, depression, or seizures.

Tell your doctor about all your other medicines. Some may affect Lomotil, especially:

• medicine to treat Parkinson’s disease;
• medicine to treat excess stomach acid, stomach ulcer, motion sickness, or irritable bowel syndrome;
• bladder or urinary medicines;
• a bronchodilator; or
• an MAO inhibitor–isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others.

This list is not complete. Other drugs may affect Lomotil, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

What is lomotil used for?

Lomotil is a combination medicine (2.5 mg diphenoxylate and 0.025 mg atropine combination) used to treat diarrhea in adults and children who are at least 13 years old.

Lomotil dosage

Follow you doctor’s or pharmacist’s instructions exactly on how much Lomotil (2.5 mg diphenoxylate and 0.025 mg atropine combination) to take and for how long to take it.

The usual starting dose of Lomotil is 2 tablets, three or four times a day, until the diarrhea is under control.

The dose is then usually cut down, so that you are taking just enough tablets to control the diarrhea. This may be as few as 2 tablets a day. Please check with your doctor as to how you should take Lomotil.

The usual maximum dose is 8 tablets in a day (24 hours).

Your doctor may want you to stop taking Lomotil when your bowel movements return to normal.

If your diarrhea contains blood or lasts for more than 2 days, tell your doctor.

Management of Diarrhea in Patients 13 Years of Age and Older

Lomotil is recommended as adjunctive therapy for the management of diarrhea in patients 13 years of age and older. Consider the nutritional status and degree of dehydration in patients prior to initiating therapy with Lomotil. The use of Lomotil should be accompanied by appropriate fluid and electrolyte therapy, when indicated. If severe dehydration or electrolyte imbalance is present, do not administer Lomotil until appropriate corrective therapy has been indicated

Initial and Maximum Recommended Dosage in Patients 13 Years of Age and Older

The initial adult dosage is 2 Lomotil tablets four times daily (maximum total daily dose of 20 mg per day of diphenoxylate hydrochloride). Most patients will require this dosage until initial control of diarrhea has been achieved. Clinical improvement of acute diarrhea is usually observed within 48 hours.

Dosage after Initial Control of Diarrhea

After initial control has been achieved, the Lomotil dosage may be reduced to meet individual requirements. Control may often be maintained with as little as two Lomotil tablets daily.

Duration of Treatment

If clinical improvement of chronic diarrhea after treatment with the maximum recommended daily dosage is not observed within 10 days, discontinue Lomotil as symptoms are unlikely to be controlled by further administration.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Lomotil side effects

As well as benefits, medicines may have some effects you do not want (side effects). Knowledge of this medicine is continually increasing. Side effects may possibly occur, which were previously unknown, and so this list of possible side effects cannot be complete. It is therefore important to tell your doctor if you experience any unusual side effects or any changes in your health, while you are taking Lomotil.

Side effects which have been reported in patients taking Lomotil are:

• Lack of energy
• Confusion
• Drowsiness
• Dizziness
• Restlessness
• Depression
• Euphoria
• Numbness in hands and feet
• Headache
• Allergic wheals and swelling
• Rash
• Swelling of gums
• Itching
• Vomiting
• Nausea
• Loss of appetite
• Abdominal discomfort
• Severe allergic reaction (anaphylaxis)
• Obstruction or paralysis of the intestine (paralytic ileus)

Reported side effects of atropine sulfate are:

• Unusually high fever
• Rapid heart beat
• Being unable to urinate
• Flushing
• Dry skin and
• Dry mouth

If any side effects do not settle down during treatment and are a problem for you, or if you develop any new medical problem while you are taking Lomotil, tell your doctor.

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are using Lomotil.

Lomotil helps most people with diarrhoea, but it may have unwanted effects in a few people.

All medicines have side effects.

Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Ask your doctor or pharmacist about any questions you may have.

Lomotil overdose

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222 from anywhere in the United States. An overdose of Lomotil can cause breathing problems and may result in death or permanent brain damage.

Early overdose symptoms include weakness, blurred vision, slurred speech, feeling hot, fast heartbeats, slowed breathing, fainting, seizure, or coma. Report any early overdose symptoms to your doctor as soon as possible.

Symptoms of a Lomotil overdose include:

• Slowdown or stoppage of the bowels
• Coma (decreased level of consciousness, lack of responsiveness)
• Constipation
• Convulsions
• Drowsiness
• Dry mucous membranes in the mouth
• Eyes: pupils are tiny or enlarged
• Eyes move quickly from side to side
• Flushed skin
• Hallucinations (seeing or hearing things that aren’t there)
• Pounding heartbeat (palpitations)
• Rapid heartbeat
• Restlessness
• Slow breathing, or breathing stops
• Urination difficulty
• Vomiting

Note: Symptoms may take up to 12 hours to appear.

What to expect at the emergency room

Take the container to the hospital with you, if possible.

Your doctor will measure and monitor the person’s vital signs, including temperature, pulse, breathing rate, and blood pressure. Symptoms will be treated.

Tests that may done include:

• Chest x-ray
• ECG (electrocardiogram or heart tracing)

Treatment may include:

• Fluids through a vein (by IV)
• Laxative
• Activated charcoal
• Medicine to reverse the effect of atropine
• Medicine to reverse the effect of the diphenoxylate
• Breathing support, including tube through the mouth and connected to a breathing machine (ventilator)

Some people may need to stay in the hospital to be monitored.

Lomotil overdose prognosis

How well someone does depends on how much medicine was swallowed and how quickly treatment is received. The faster medical help is given, the better the chance for recovery.

A hospital stay may be needed for more doses of the medicines that reverse the effects of the drug. Complications, such as pneumonia, muscle damage from lying on a hard surface for a prolonged period of time, or brain damage from lack of oxygen may result in permanent disability. However, unless there are complications, long-term effects and death are rare.

People who quickly receive medicine to reverse the effect of the opioid usually get better within 24 to 48 hours. However, children do not do as well.

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