Consumer medicine information

Lomotil

Diphenoxylate hydrochloride; Atropine sulfate monohydrate

BRAND INFORMATION

Brand name

Lomotil

Active ingredient

Diphenoxylate hydrochloride; Atropine sulfate monohydrate

Schedule

S4 | S3

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Lomotil.

SUMMARY CMI

Lomotil®

Consumer Medicine Information (CMI) summary

The full CMI on the next page has more details. If you are worried about using this medicine, speak to your doctor or pharmacist.

1. Why am I using Lomotil?

Lomotil contains the active ingredients diphenoxylate hydrochloride and atropine sulfate monohydrate. Lomotil is used to for the treatment of acute or chronic diarrhoea.

For more information, see Section 1. Why am I using Lomotil? in the full CMI.

2. What should I know before I use Lomotil?

Do not use if you have ever had an allergic reaction to diphenoxylate or atropine or any of the ingredients listed at the end of the CMI.

Talk to your doctor if you have any other medical conditions, take any other medicines, are pregnant or are breastfeeding.

For more information, see Section 2. What should I know before I use Lomotil? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with Lomotil and affect how it works.

A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use Lomotil?

  • The usual starting dose is 2 tablets, three to four times daily, until the diarrhoea is under control.
  • The usual maximum dose is 8 tablets in a day (24 hours).

More instructions can be found in Section 4. How do I use Lomotil? in the full CMI.

5. What should I know while using Lomotil?

Things you should do
  • Remind any doctor, dentist or pharmacist you visit that you are using Lomotil.
  • Drink plenty of liquids, such as an oral rehydration solution.
  • Eat as little as possible for the first few days.
Things you should not do
  • Do not give Lomotil to children under 12 years of age.
Driving or using machines
  • Make sure you know how you react to Lomotil before driving or operating machinery. Lomotil can make some people drowsy or dizzy.
Drinking alcohol
  • Do not drink alcohol while using the medicine.
Looking after your medicine
  • Store below 30°C.
  • Store away from heat, direct light and steamy or damp places.
  • Keep out of reach of children. Accidental overdosage can lead to severe breathing problems or death.

For more information, see Section 5. What should I know while using Lomotil? in the full CMI.

6. Are there any side effects?

Common side effects include nausea and vomiting, stomach upset, drowsiness and dizziness. Serious side effects include severe allergic reactions, severe stomach or bowel problems, fast shallow breathing, fast heartbeat, and a very high temperature.

For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.



FULL CMI

Lomotil®

Active ingredients: diphenoxylate hydrochloride and atropine sulfate monohydrate


Consumer Medicine Information (CMI)

This leaflet provides important information about using Lomotil. You should also speak to your doctor or pharmacist if you would like further information or if you have any concerns or questions about using Lomotil.

Where to find information in this leaflet:

1. Why am I using Lomotil?
2. What should I know before I use Lomotil?
3. What if I am taking other medicines?
4. How do I use Lomotil?
5. What should I know while using Lomotil?
6. Are there any side effects?
7. Product details

1. Why am I using Lomotil?

Lomotil contains the active ingredients diphenoxylate hydrochloride and atropine sulfate monohydrate. Lomotil is an anti-diarrhoeal agent. Diphenoxylate reduces diarrhoea by slowing down the movements of the intestines. 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 are taken and discourages abuse.

Lomotil is used to treat short- or long-lasting episodes of diarrhoea when used with other measures such as oral rehydration.

2. What should I know before I use Lomotil?

Warnings

Do not use Lomotil if:

  • You are allergic to diphenoxylate or atropine, or any of the ingredients listed at the end of this leaflet. Always check the ingredients to make sure you can use this medicine.
  • You have jaundice.
  • You have diarrhoea caused by pseudomembranous enterocolitis. This is 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.
  • It is past the expiry date printed on the pack or if the packaging is torn or shows signs of tampering.

Check with your doctor if you:

  • Have any other medical conditions, especially
  • Liver disease
  • Kidney disease
  • Down's Syndrome
  • A history of drug abuse
  • Take any medicines for any other condition.

During treatment, you may be at risk of developing certain side effects. It is important you understand these risks and how to monitor for them. See additional information under Section 6. Are there any side effects?

Pregnancy and breastfeeding

Check with your doctor if you are pregnant. Lomotil should not be taken near or at the time of giving birth, because diphenoxylate is chemically related to medicines, which can slow down the breathing of newborn infants.

Talk to your doctor if you are breastfeeding or intend to breastfeed. The active ingredients in Lomotil may pass into breast milk. Infants of nursing mothers taking Lomotil may show some effects of the medicine.

Use in children

  • Do not give Lomotil to children under 12 years of age.
  • Keep Lomotil out of reach of children since accidental overdosage may result in severe, even fatal breathing problems.

3. What if I am taking other medicines?

Tell your doctor or pharmacist if you are taking any other medicines, including any medicines, vitamins or supplements that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines may interfere with Lomotil and affect how it works.

Medicines that Lomotil may increase the effect of include:

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

Check with your doctor or pharmacist if you are not sure about what medicines, vitamins or supplements you are taking and if these affect Lomotil.

4. How do I use Lomotil?

How much to take

  • The usual starting dose is 2 tablets three or four times daily until the diarrhoea is under control.
  • Do not take more than 8 tablets in 24 hours.
  • After the diarrhoea is under control the dosage may be reduced, so that you are taking just enough tablets to control the diarrhoea. This may be as few as 2 tablets a day. Your doctor will advise you how much to take.
  • Your doctor may want you to stop taking Lomotil when your bowel movements return to normal.

If you forget to use Lomotil

Lomotil should be used regularly at the same time each day.

If you miss your dose at the usual time and it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Do not take a double dose to make up for the dose you missed.

If you use too much Lomotil

If you think that you have used too much Lomotil, or if a child has accidentally taken Lomotil, you should get urgent medical attention.

You should immediately:

  • phone the Poisons Information Centre
    (by calling 13 11 26), or
  • contact your doctor, or
  • go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

5. What should I know while using Lomotil?

Things you should do

See your doctor straight away if:

  • the diarrhoea contains blood or continues for more than 2 days.

Drink plenty of liquids, such as an oral rehydration solution

Drinking plenty of liquids makes sure you do not become dehydrated (lose too much liquid from your body). If you have become very dehydrated, see your doctor to make sure this is corrected, before taking Lomotil.

Eat as little as possible for the first few days

Eat only plain, bland foods, such as unbuttered toast, plain biscuits, boiled potatoes, rice, or pasta. Gradually return to your normal diet when the diarrhoea has stopped.

Remind any doctor, dentist, or pharmacist you visit that you are using Lomotil.

Things you should not do

  • Do not drink alcohol while taking Lomotil.
  • Do not exceed the recommended dose. Addiction to Lomotil is possible at high doses.

Driving or using machines

Be careful before you drive or use any machines or tools until you know how Lomotil affects you.

Lomotil may cause dizziness or drowsiness in some people

Drinking alcohol

Tell your doctor if you drink alcohol.

Lomotil may increase the effects of alcohol.

Looking after your medicine

  • Store below 30°C.

Store it in a cool dry place away from moisture, heat or sunlight; for example, do not store it:

  • in the bathroom or near a sink, or
  • in the car or on window sills.

Keep it where young children cannot reach it.

Getting rid of any unwanted medicine

If you no longer need to use this medicine or it is out of date, take it to any pharmacy for safe disposal.

Do not use this medicine after the expiry date.

6. Are there any side effects?

All medicines can have side effects. If you do experience any side effects, most of them are minor and temporary. However, some side effects may need medical attention.

See the information below and, if you need to, ask your doctor or pharmacist if you have any further questions about side effects.

Less serious side effects

Less serious side effectsWhat to do
Stomach related:
  • Nausea or vomiting
  • Loss of appetite
  • Abdominal discomfort
Nervous system related:
  • Drowsiness
  • Dizziness
  • Confusion
  • Lacking energy
  • Depression or euphoria
  • Headache
  • Numbness of extremities
Speak to your doctor if you have any of these less serious side effects and they worry you.

Serious side effects

Serious side effectsWhat to do
Signs of an allergic reaction:
  • Rash
  • Allergic wheals and swelling
  • Swelling of the gums
Signs of atropine poisoning:
  • Unusually high fever
  • Rapid heartbeat
  • Unable to urinate
  • Dry skin and mucous membranes
  • Flushing of the skin
Signs of an overdose:
  • Slow, shallow breathing or abnormally rapid breathing
  • Pinpoint pupils or other visual changes
  • Lethargy or coma.
Call your doctor straight away, or go straight to the Emergency Department at your nearest hospital if you notice any of these serious side effects.

Tell your doctor or pharmacist if you notice anything else that may be making you feel unwell.

Other side effects not listed here may occur in some people.

Reporting side effects

After you have received medical advice for any side effects you experience, you can report side effects to the Therapeutic Goods Administration online at www.tga.gov.au/reporting-problems. By reporting side effects, you can help provide more information on the safety of this medicine.

Always make sure you speak to your doctor or pharmacist before you decide to stop taking any of your medicines.

7. Product details

This medicine is only available with a doctor's prescription for packs sizes of 20 and 100 tablets.

The 8 tablet pack size is available without prescription at a pharmacy on the advice of a pharmacist.

What Lomotil contains

Active ingredients
(main ingredients)
Diphenoxylate hydrochloride
Atropine sulfate monohydrate
Other ingredients
(inactive ingredients)
sucrose
acacia
sorbitol
talc
magnesium stearate
liquid paraffin.

Do not take this medicine if you are allergic to any of these ingredients.

What Lomotil looks like

Lomotil is a white to off-white, uncoated biconvex tablets marked LT on one side.

Registration number: AUST R 74475

Who distributes Lomotil

iNova Pharmaceuticals (Australia) Pty Limited
Level 10, 12 Help Street
Chatswood NSW 2067
Tel (Australia): 1800 630 056

This leaflet was prepared in November 2021

Published by MIMS February 2022

BRAND INFORMATION

Brand name

Lomotil

Active ingredient

Diphenoxylate hydrochloride; Atropine sulfate monohydrate

Schedule

S4 | S3

 

1 Name of Medicine

Diphenoxylate hydrochloride and atropine sulfate.

2 Qualitative and Quantitative Composition

Each Lomotil tablet contains diphenoxylate HCl 2.5 mg and atropine sulfate 25 micrograms.

Excipients with known effect.

Sorbitol, sucrose.
For the full list of excipients, see Section 6.1 List of Excipients.
Lomotil is a white to off white, uncoated, round, biconvex tablet embossed "LT" on one side and plain on the other.

3 Pharmaceutical Form

Tablet.

4 Clinical Particulars

4.1 Therapeutic Indications

Lomotil is indicated as an adjunctive therapy for acute and chronic diarrhoea.

4.2 Dose and Method of Administration

The recommended adult starting dose is 5 mg (two tablets) three or four times daily. After initial control is achieved, the dosage should be reduced to meet the requirements of the individual patient. Control may often be maintained with as little as 5 mg (two tablets) daily.

4.3 Contraindications

1. Known hypersensitivity to diphenoxylate HCl or atropine.
2. Jaundice.
3. Diarrhoea associated with pseudomembranous enterocolitis, which may occur during or up to several weeks following treatment with certain antibiotics.
4. Diarrhoea associated with inflammatory bowel disease (e.g. ulcerative colitis, Crohn's disease) and bacterial and amoebic colitis, as diphenoxylate may exacerbate the underlying condition (see Section 4.4 Special Warnings and Precautions for Use).
5. Lomotil is not recommended for children under 12 years of age. The medication should be kept out of reach of children since accidental overdosage may result in severe, even fatal, respiratory depression.

4.4 Special Warnings and Precautions for Use

Interaction with CNS depressants.

Diphenoxylate may have an additive effect on certain central nervous system depressants, e.g. barbiturates, tranquillizers and alcohol (see Section 4.5 Interactions with Other Medicines and Other Forms of Interactions).

MAO inhibitors.

Concurrent use with MAO inhibitors may, in theory, precipitate hypertensive crisis. Therefore, close observation is required when these medications are given concomitantly with diphenoxylate hydrochloride.

Antibiotic use.

Bacterially induced diarrhoea should be treated with appropriate antimicrobial therapy.
The possibility of serious underlying aetiology should be considered before anti-diarrhoeal treatment of any type is instituted as other therapeutic measures may occasionally be necessary. Special caution should be exercised in treating diarrhoea which may be attributable to antibiotics known to cause colitis or pseudomembranous colitis.

Toxic megacolon in patients with acute ulcerative colitis.

In some patients with acute ulcerative colitis, agents which inhibit intestinal motility or prolong intestinal transit time have been reported to induce toxic megacolon.

Dehydration and electrolyte imbalance.

Appropriate fluid and electrolyte therapy should be given to protect against dehydration. If severe dehydration or electrolyte imbalance is present, Lomotil should be withheld until appropriate corrective therapy has been initiated, in order to prevent diphenoxylate intoxication due to variability of response.
Caution patients to adhere strictly to recommended dosage schedules.

Dependence potential.

Addiction (dependency) to diphenoxylate hydrochloride is theoretically possible at high dosage. Therefore, the recommended dosage should not be exceeded. Because of the structural and pharmacologic similarity of diphenoxylate hydrochloride to drugs with definite addiction potential, Lomotil should be administered with considerable caution to patients who are receiving addicting drugs, to individuals known to be addiction prone, or to those whose histories suggest they may increase the dosage on their own initiative.
A subtherapeutic dose of atropine has been added to the diphenoxylate hydrochloride. Therefore, consideration should be given to the precautions relating to the use of atropine in children.

Atropinism.

Lomotil should be used with caution since signs of atropinism may occur particularly in Down's Syndrome.

Use in hepatic impairment.

Lomotil should be used with extreme caution in patients with advanced hepatorenal disease and in all patients with abnormal liver function, since hepatic coma may be precipitated.

Use in the elderly.

No data available.

Paediatric use.

Lomotil is not recommended for children under 12 years of age. The medication should be kept out of reach of children since accidental overdosage may result in severe, even fatal respiratory depression (see Section 4.3 Contraindications).

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Diphenoxylate may have an additive effect on certain central nervous system depressants, e.g. barbiturates, tranquillizers and alcohol (see Section 4.4 Special Warnings and Precautions for Use).

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category C)
Diphenoxylate is chemically related to the narcotic pethidine. Narcotic analgesics may cause respiratory depression in the newborn infant. This drug should not be given at, or near, term.
Diphenoxylate hydrochloride may be and atropine sulfate is excreted in human breast milk. Therefore, infants of nursing mothers taking Lomotil may exhibit some effects of the drug.

4.7 Effects on Ability to Drive and Use Machines

Lomotil may produce drowsiness or dizziness. The effects of this medicine on a person's ability to drive and use machines were not assessed as part of its registration. However, patients should refrain from driving or using machines until they know that Lomotil does not negatively affect these abilities as confusion, lethargy, sedation, drowsiness and dizziness may occur (see Section 4.8 Adverse Effects (Undesirable Effects)).

4.8 Adverse Effects (Undesirable Effects)

At therapeutic doses the following have been reported.

Nervous system.

Malaise/lethargy, confusion, sedation/drowsiness, dizziness, restlessness, depression, euphoria, numbness of extremities, headache.

Allergic.

Anaphylaxis, angioneurotic oedema, urticaria, swelling of gums, pruritus.

Gastrointestinal system.

Toxic megacolon, paralytic ileus, vomiting, nausea, anorexia, abdominal discomfort.
Atropine sulfate effects are hyperthermia, tachycardia, urinary retention, flushing, dryness of the skin and mucous membranes.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at www.tga.gov.au/reporting-problems.

4.9 Overdose

Symptoms.

Initial signs of overdosage may include dryness of the skin and mucous membranes, mydriasis, restlessness, flushing, hyperthermia and tachycardia followed by lethargy or coma, hypotonic reflexes, nystagmus, pinpoint pupils and respiratory depression. Respiratory depression may be evidenced as late as 30 hours after ingestion and may recur in spite of an initial response to narcotic antagonists.

Management.

Treat all possible Lomotil overdosages as serious and maintain medical observation for at least 48 hours.
Establishment of a patent airway, and if necessary, artificial ventilation should be instituted. If the patient is not comatose, gastric lavage and administration of a slurry of activated charcoal may be indicated.
Naloxone hydrochloride should be administered if respiratory depression develops. If naloxone hydrochloride is not available, nalorphine hydrochloride should be used.
When naloxone hydrochloride is administered intravenously the onset of action in generally apparent within two minutes. Naloxone hydrochloride may also be administered subcutaneously or intramuscularly providing a slightly less rapid onset of action but a more prolonged effect.
To counteract the respiratory depression caused by Lomotil overdosage, the following dosage schedule for naloxone hydrochloride should be followed:
The usual initial adult dose of naloxone hydrochloride is 0.4 mg (1 mL) administered intravenously. The action of naloxone hydrochloride is of shorter duration than that of diphenoxylate hydrochloride, so repeated injections of the antidote may be required. If respiratory function does not adequately improve after the initial dose the same I.V. dose may be repeated at two to three minute intervals.
Since the duration of action of diphenoxylate hydrochloride is longer than that of naloxone hydrochloride improvement of respiration following administration may be followed by recurrent respiratory depression. Consequently, continuous observation is necessary until the effect of diphenoxylate hydrochloride on respiration (which may persist for many hours) has passed. The period of observation should extend over at least 48 hours, preferably under continuous hospital care.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Diphenoxylate is chemically related to the narcotic pethidine and acts by slowing intestinal motility. The formulation contains a small amount of atropine sulfate which has little therapeutic significance and is added to discourage excessive self-medication.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

Diphenoxylate is rapidly absorbed reaching peak blood levels in about two hours.

Metabolism.

Its relatively short plasma half-life (about 2.5 hours) and large plasma clearance suggest its rapid biotransformation. The major metabolic pathway of diphenoxylate in man is the hydrolysis of the ester group to give diphenoxylic acid - a pharmacologically active metabolite. Diphenoxylate metabolites probably undergo enterohepatic circulation.

Excretion.

The drug is excreted principally as its metabolites in both urine and, to a larger extent, in the faeces.

5.3 Preclinical Safety Data

Genotoxicity.

No data available.

Carcinogenicity.

No data available.

6 Pharmaceutical Particulars

6.1 List of Excipients

Lomotil contains the following excipients: acacia, magnesium stearate, liquid paraffin, sorbitol solution, sucrose and purified talc.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG).

6.4 Special Precautions for Storage

Store below 30°C.

6.5 Nature and Contents of Container

Blister packs of 2's, 8's, 20's and 100's.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Diphenoxylate hydrochloride is a white or almost white, crystalline powder, very slightly soluble in water, freely soluble in methylene chloride, sparingly soluble in alcohol, practically insoluble in ether.
Atropine sulfate is a white, crystalline powder or colourless crystals, very soluble in water, freely soluble from alcohol, practically insoluble in ether.

Chemical structure.


C30H32N2O2, HCl. M.W. = 489.1.
Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylate hydrochloride.
C34H48N2O10S, H2O. M.W. = 695.
Bis (1R, 3r, 5S)-3-[(RS)-(3-hydroxy-2-phenylpropionyl)oxy]-8-methyl-8-azabicyclo[3.2.1] octane sulphate.

CAS number.

Diphenhydramine hydrochloride: 3810-80-8.
Atropine sulfate: 5908-99-6.

7 Medicine Schedule (Poisons Standard)

2 tablets. (S3) Pharmacist Only Medicine.
8 tablets. (S3) Pharmacist Only Medicine.
20 tablets. (S4) Prescription Only Medicine.
100 tablets. (S4) Prescription Only Medicine.

Summary Table of Changes