1. Name Of The Medicinal Product
Imodium Classic 2 mg Capsules.
2. Qualitative And Quantitative Composition
Each capsule contains 2 mg Loperamide hydrochloride.
Excipient: lactose
For a full list of excipients, see section 6.1
3. Pharmaceutical Form
Capsule, hard.
Opaque green cap and grey body, hard gelatin capsule imprinted with 'Imodium' on cap and 'Janssen' on body containing white powder.
4. Clinical Particulars
4.1 Therapeutic Indications
For the symptomatic treatment of acute diarrhoea in adults and children aged 12 years and over.
For the symptomatic treatment of acute episodes of diarrhoea associated with Irritable Bowel Syndrome in adults aged 18 years and over following initial diagnosis by a doctor.
4.2 Posology And Method Of Administration
The capsules should be taken with liquid.
ACUTE DIARRHOEA
Adults and children over 12:
Two capsules (4 mg) initially, followed by one capsule (2 mg) after each loose stool. The usual dose is 3-4 capsules (6 mg – 8 mg) a day. The total daily dose should not exceed 8 capsules (16 mg).
SYMPTOMATIC TREATMENT OF ACUTE EPISODES OF DIARRHOEA ASSOCIATED WITH IRRITABLE BOWEL SYNDROME IN ADULTS AGED 18 YEARS AND OVER
Two capsules (4 mg) to be taken initially. The usual dose is between 2 and 4 capsules (4 mg – 8 mg) per day in divided doses, depending on severity. If required, this dose can be adjusted according to result, up to a maximum of 8 capsules (16 mg) daily.
USE IN ELDERLY
No dose adjustment is required for the elderly.
RENAL IMPAIRMENT
No dose adjustment is required for patients with renal impairment.
HEPATIC IMPAIRMENT
Although no pharmacokinetic data are available in patients with hepatic impairment, Imodium should be used with caution in such patients because of reduced first pass metabolism. (see 4.4 Special warnings and special precautions for use).
Method of administration
Oral use.
4.3 Contraindications
This medicine is contraindicated:
• in patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients.
• in children less than 12 years of age.
• in patients with acute dysentery, which is characterised by blood in stools and high fever.
• in patients with acute ulcerative colitis.
• in patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella and Campylobacter.
• in patients with pseudomembranous colitis associated with the use of broad-spectrum antibiotics.
Imodium must not be used when inhibition of peristalsis is to be avoided due to the possible risk of significant sequelae including ileus, megacolon and toxic megacolon. Imodium must be discontinued promptly when ileus, constipation or abdominal distension develop.
4.4 Special Warnings And Precautions For Use
Treatment of diarrhoea with Imodium is only symptomatic. Whenever an underlying etiology can be determined, specific treatment should be given when appropriate. The priority in acute diarrhoea is the prevention or reversal of fluid and electrolyte depletion. This is particularly important in young children and in frail and elderly patients with acute diarrhoea. Use of this medicine does not preclude the administration of appropriate fluid and electrolyte replacement therapy.
Since persistent diarrhoea can be an indicator of potentially more serious conditions, this medicine should not be used for prolonged periods until the underlying cause of the diarrhoea has been investigated.
In acute diarrhoea, if clinical improvement is not observed within 24 hours, the administration of Imodium should be discontinued and patients should be advised to consult their doctor.
Patients with AIDS treated with this medicine for diarrhoea should have therapy stopped at the earliest signs of abdominal distension. There have been isolated reports of obstipation with an increased risk for toxic megacolon in AIDS patients with infectious colitis from both viral and bacterial pathogens treated with loperamide hydrochloride.
Although no pharmacokinetic data are available in patients with hepatic impairment, this medicine should be used with caution in such patients because of reduced first pass metabolism, as it may result in a relative overdose leading to CNS toxicity.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine because it contains lactose
If you are taking this medicine to control episodes of diarrhoea associated with Irritable Bowel Syndrome previously diagnosed by your doctor, you should return to him/her if the pattern of your symptoms changes. You should also return to your doctor if your episodes of diarrhoea continue for more than two weeks or there is a need for continued treatment of more than two weeks.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Non-clinical data have shown that loperamide is a P-glycoprotein substrate. Concomitant administration of loperamide (16 mg single dose) with quinidine, or ritonavir, which are both P-glycoprotein inhibitors, resulted in a 2 to 3-fold increase in loperamide plasma levels. The clinical relevance of this pharmacokinetic interaction with P-glycoprotein inhibitors, when loperamide is given at recommended dosages, is unknown.
The concomitant administration of loperamide (4 mg single dose) and itraconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 3 to 4-fold increase in loperamide plasma concentrations. In the same study a CYP2C8 inhibitor, gemfibrozil, increased loperamide by approximately 2-fold. The combination of itraconazole and gemfibrozil resulted in a 4-fold increase in peak plasma levels of loperamide and a 13-fold increase in total plasma exposure. These increases were not associated with central nervous system (CNS) effects as measured by psychomotor tests (i.e., subjective drowsiness and the Digit Symbol Substitution Test).
The concomitant administration of loperamide (16 mg single dose) and ketoconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 5-fold increase in loperamide plasma concentrations. This increase was not associated with increased pharmacodynamic effects as measured by pupillometry.
Concomitant treatment with oral desmopressin resulted in a 3-fold increase of desmopressin plasma concentrations, presumably due to slower gastrointestinal motility.
It is expected that drugs with similar pharmacological properties may potentiate loperamide's effect and that drugs that accelerate gastrointestinal transit may decrease its effect.
4.6 Pregnancy And Lactation
Safety in human pregnancy has not been established, although from animal studies there are no indications that loperamide HCl posseses any teratogenic or embryotoxic properties. As with other drugs, it is not advisable to administer this medicine in pregnancy, especially during the first trimester.
Small amounts of loperamide may appear in human breast milk. Therefore, this medicine is not recommended during breast-feeding.
Women who are pregnant or breast feeding infants should therefore be advised to consult their doctor for appropriate treatment.
4.7 Effects On Ability To Drive And Use Machines
Loss of consciousness, depressed level of consciousness, tiredness, dizziness, or drowsiness may occur when diarrhoea is treated with this medicine. Therefore, it is advisable to use caution when driving a car or operating machinery. See Section 4.8, Undesirable Effects.
4.8 Undesirable Effects
Adults and children aged
The safety of loperamide HCl was evaluated in 2755 adults and children aged
The most commonly reported (i.e.
Table 1 displays ADRs that have been reported with the use of loperamide HCl from either clinical trial (acute diarrhoea) or post-marketing experience.
The frequency categories use the following convention: very common (
Table 1: Adverse Drug Reactions
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4.9 Overdose
Symptoms:
In case of overdose (including relative overdose due to hepatic dysfunction), CNS depression (stupor, coordination abnormality, somnolence, miosis, muscular hypertonia and respiratory depression), constipation, urinary retention and ileus may occur. Children and patients with hepatic dysfunction may be more sensitive to CNS effects.
Treatment:
If symptoms of overdose occur, naloxone can be given as an antidote. Since the duration of action of loperamide is longer than that of naloxone (1 to 3 hours), repeated treatment with naloxone might be indicated. Therefore, the patient should be monitored closely for at least 48 hours in order to detect possible CNS depression.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Pharmacotherapeutic Group: Antipropulsives; ATC code: A07DA03
Loperamide binds to the opiate receptor in the gut wall, reducing propulsive peristalsis and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter.
In a double blind randomised clinical trial in 56 patients with acute diarrhoea receiving loperamide, onset of anti-diarrhoeal action was observed within one hour following a single 4 mg dose. Clinical comparisons with other antidiarrhoeal drugs confirmed this exceptionally rapid onset of action of loperamide.
5.2 Pharmacokinetic Properties
The half-life of loperamide in man is 10.8 hours with a range of 9-14 hours. Studies on distribution in rats show high affinity for the gut wall with preference for binding to the receptors in the longitudinal muscle layer. Loperamide is well absorbed from the gut, but is almost completely extracted and metabolised by the liver where it is conjugated and excreted via the bile. Due to its high affinity for the gut wall and its high first pass metabolism, very little loperamide reaches the systemic circulation.
5.3 Preclinical Safety Data
No relevant information additional to that contained elsewhere in the Summary of Product Characteristics.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Lactose
Maize starch
Talc
Magnesium stearate (E572)
Capsule cap:
Titanium dioxide (E171)
Yellow ferric oxide (E172)
Indigo carmine (E132)
Gelatin
Capsule body:
Titanium dioxide (E171)
Black ferrous oxide (E172)
Indigo carmine (E132)
Erythrosine (E127)
Gelatin
6.2 Incompatibilities
Not applicable.
6.3 Shelf Life
60 months.
6.4 Special Precautions For Storage
None.
6.5 Nature And Contents Of Container
Blister packs consisting of aluminium foil, hermetalu and polyvinyl chloride genotherm glass clear.
The blister strips are packed in cardboard cartons to contain 2, 4, 6, 8, 12 or 18 capsules
Not all pack sizes may be marketed
6.6 Special Precautions For Disposal And Other Handling
Not applicable.
7. Marketing Authorisation Holder
McNeil Products Limited
Foundation Park
Roxborough Way
Maidenhead
Berkshire
SL6 3UG
United Kingdom
8. Marketing Authorisation Number(S)
PL 15513/0309
9. Date Of First Authorisation/Renewal Of The Authorisation
15/12/2009
10. Date Of Revision Of The Text
27/07/2011
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