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McNeil Healthcare (Ireland) Ltd

Airton Road, Tallaght, Dublin 24, Ireland
Telephone: +353 1 466 5200
Fax: +353 1 466 5316


Summary of Product Characteristics last updated on medicines.ie: 24/11/2016
SPC Imodium Capsules


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1. NAME OF THE MEDICINAL PRODUCT

Imodium 2 mg Capsules.


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2. QUALITATIVE AND QUANTITATIVE COMPOSITION

Each capsule contains 2 mg of loperamide hydrochloride.

Excipients: Each capsule contains 127 mg lactose.

For a full list of excipients, see section 6.1.


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3. PHARMACEUTICAL FORM

Capsule, hard. (capsule)

Gelatin capsules with an opaque green cap and an opaque dark grey body, containing white powder.


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4. CLINICAL PARTICULARS

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4.1 Therapeutic indications

Adults

As an adjunct in the management of acute diarrhoea, together with appropriate fluid and electrolyte replacement.

In the symptomatic control of diarrhoea associated with chronic inflammatory bowel disease, e.g., Crohn's disease and ulcerative colitis, as an adjunct to specific measures such as corticosteroids and sulphasalazine. Use in these conditions should be under specialist supervision.

In the adjunctive short-term, control of post-surgical diarrhoea, including ileostomy.

Children

For the occasional use in the control of intractable diarrhoea under specialist supervision.

Since persistent diarrhoea can be an indicator of potentially serious conditions, the underlying cause must always be investigated.


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4.2 Posology and method of administration

For oral administration.The capsules should be taken with water.

i) As an adjunct in the management of acute diarrhoea

Adults and children 9-12 years

2 to 4 mg is the usual initial dose, followed by 2 mg three times daily. The maximum daily dose should not exceed 10 mg.

Children 4-8 years

A total maximum daily dose of 4 mg in divided doses.

Under 4 years

Not recommended.

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 warning and precautions for use).

ii) For the symptomatic treatment of diarrhoea associated with chronic bowel disorders

Adults only

Studies have shown that patients may need differing amounts of loperamide. The starting dosage should be between 4 to 8 mg (2 to 4 capsules) per day in divided doses depending on severity. If required, this dose can be adjusted according to response. Having established the patient's daily maintenance dose, the capsules may be administered on a twice daily regimen.


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4.3 Contraindications

• Imodium is contraindicated in patients under 4 years of age

• Imodium is contraindicated in patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients

• Imodium should not be used as the primary therapy:

- In patients with acute dysentery, which is characterised by blood in the 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 should not be used when the 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 constipation, abdominal distension or ileus develop


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4.4 Special warnings and precautions for use

Treatment of diarrhoea with loperamide HCl is only symptomatic. Whenever an underlying etiology can be determined, specific treatment should be given when appropriate.

The necessity for specific therapy, such as anti-infectives, should be borne in mind, particularly should treatment be required for a period longer than three days.

Loperamide should be used with caution when hepatic function, necessary for the drug's metabolism, is defective, as this may result in relative overdose leading to CNS toxicity.

Patients with AIDS treated with Imodium for diarrhoea should have therapy stopped at the earliest signs of abdominal distension. There have been isolated reports of toxic megacolon in AIDS patients with infectious colitis from both viral and bacterial pathogens treated with loperamide hydrochloride.

Antimotility agents such as loperamide may precipitate ileus and toxic megacolon in patients with ulcerative colitis, and should be avoided in severe acute attacks. It may be used cautiously in mild or less severe attacks as an adjunct to other measures, but should be discontinued promptly should abdominal distension or other untoward symptoms occur.

The stated dose should not be exceeded.

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.

Abuse and misuse of loperamide, as an opioid substitute, have been described in individuals with opioid addiction (see section 4.9 Overdose).


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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 Fertility, pregnancy and Lactation

Pregnancy

The safety of Imodium in human pregnancy has not been established.

Breast-Feeding

Small amounts of loperamide may appear in human breast milk. Therefore, Imodium 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.

Fertility

The effect on human fertility has not been evaluated.


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4.7 Effects on ability to drive and use machines

Tiredness, dizziness, or drowsiness may occur when diarrhoea is treated with Imodium. Therefore, it is advisable to use caution when driving a car or operating machinery. See section 4.8 Undesirable effects.


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4.8 Undesirable effects

Adults and children aged ≥ 12 years

The safety of loperamide HCl was evaluated in 2755 adults and children aged ≥ 12 years who participated in 26 controlled and uncontrolled clinical trials of loperamide HCl used for the treatment of acute diarrhoea.

The most commonly reported (i.e. ≥ 1% incidence) adverse drug reactions (ADRs) in clinical trials with loperamide HCl in acute diarrhoea were: constipation (2.7%), flatulence (1.7%), headache (1.2%) and nausea (1.1%).

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 (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); and very rare (<1/10,000).

Table 1: Adverse Drug Reactions

System Organ Class

Indication

Common

Uncommon

Rare

Immune System Disorders

Hypersensitivity reactiona

Anaphylactic reaction (including Anaphylactic shock)a

Anaphylactoid reactiona

Nervous System Disorders

Headache

Dizziness

Somnolencea

Loss of consciousnessa

Stupora

Depressed level of consciousnessa

Hypertoniaa

Coordination abnormalitya

Eye Disorders

Miosisa

Gastrointestinal Disorders

Constipation

Nausea

Flatulence

Abdominal pain

Abdominal discomfort

Dry mouth

Abdominal pain upper

Vomiting

Dyspepsiaa

Ileusa (including paralytic ileus)

Megacolona (including toxic megacolonb)

Abdominal distension

Skin and Subcutaneous Tissue Disorders

Rash

Bullous eruptiona (including Stevens-Johnson syndrome, Toxic epidermal necrolysis and Erythema multiforme)

Angioedemaa

Urticariaa

Pruritusa

Renal and Urinary Disorders

Urinary retentiona

General Disorders and Administration Site Conditions

Fatiguea

a: Inclusion of this term is based on post-marketing reports for loperamide HCl. As the process for determining post marketing ADRs did not differentiate between chronic and acute indications or adults and children, the frequency is estimated from all clinical trials with loperamide HCl (acute and chronic), including trials in children ≤ 12 years (N=3683).

b: See section 4.4 Special Warnings and Special Precautions for use.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation 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 via HPRA Pharmacovigilance, Earlsfort Terrace, IRL - Dublin 2; Tel: +353 1 6764971; Fax: +353 1 6762517. Website: www.hpra.ie; E-mail: medsafety@hpra.ie.


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4.9 Overdose

Signs and 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.

In individuals who have intentionally ingested overdoses (reported in doses from 40 mg up to 792 mg per day) of loperamide HCl, QT interval prolongation and or serious ventricular arrhythmias, have been observed (see section 4.4 Warnings and Precautions). Fatal cases have also been reported.

Treatment:

In cases of overdose, ECG monitoring for QT interval prolongation should be initiated.

If CNS symptoms of overdose occur, naloxone may be given as an antidote. Since the duration of action of loperamide is longer than that of naloxone 1 to 3 hrs), 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.


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5. PHARMACOLOGICAL PROPERTIES

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5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Antipropulsives; ATC code: A07DA03

Loperamide binds to the opiate receptor in the gut wall, reducing propulsive peristalsis, increasing intestinal transit time and enhancing resorption of water and electrolytes. Loperamide increases the tone of the anal sphincter.


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5.2 Pharmacokinetic properties

Absorption: Most ingested loperamide is absorbed from the gut, but as a result of significant first pass metabolism, systemic bioavailability is only approximately 0.3%.

Distribution: Studies on distribution in rats show a high affinity for the gut wall with a preference for binding to receptors of the longitudinal muscle layer. The plasma protein binding of loperamide is 95%, mainly to albumin. Non-clinical data have shown that loperamide is a P-glycoprotein substrate.

Metabolism: Loperamide is almost completely extracted by the liver, where it is predominantly metabolized, conjugated and excreted via the bile. Oxidative N-demethylation is the main metabolic pathway for loperamide, and is mediated mainly through CYP3A4 and CYP2C8. Due to this very high first pass effect, plasma concentrations of unchanged drug remain extremely low.

Elimination: The half-life of loperamide in man is about 11 hours with a range of 9-14 hours. Excretion of the unchanged loperamide and the metabolites mainly occurs through the faeces.


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5.3 Preclinical safety data

Within its therapeutically relevant concentration range and at significant multiples of this range (up to 47-fold), loperamide has no significant cardiac electrophysiological effects. However, at extremely high concentrations associated with intentional overdose (see section 4.4 Warnings and Precautions), loperamide has cardiac electrophysiological actions consisting of inhibition of potassium (hERG) and sodium currents, and arrhythmias in in vitro and in vivo animal models.


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6. PHARMACEUTICAL PARTICULARS

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6.1 List of excipient(s)

Capsule content

Lactose

Maize starch

Talc

Magnesium stearate

Capsule cap

Titanium dioxide (E171)

Yellow ferric oxide (E172)

Indigotindisulphonate sodium (E132)

Gelatin

Capsule body

Titanium dioxide (E171)

Black ferrous oxide (E172)

Indigotindisulphonate sodium (E132)

Erythrosin (E127)

Gelatin


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6.2 Incompatibilities

Not applicable.


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6.3 Shelf life

5 years.


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6.4 Special precautions for storage

This medicinal product does not require any special storage conditions.


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6.5 Nature and contents of container

Imodium Capsules are packaged in blister packs consisting of polyvinylchloride, glass clear 250 µm and aluminium foil (thickness 20 µm) coating on the inner side with a colourless heat seal lacquer: PVC mixed polymers with acrylates 6 g/m2, in an outer cardboard carton.

The packs contain 60 capsules.


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6.6 Special precautions for disposal and other handling

No special requirements.


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7. MARKETING AUTHORISATION HOLDER

McNeil Healthcare (Ireland) Ltd.

Airton Road

Tallaght

Dublin 24

Ireland


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8. MARKETING AUTHORISATION NUMBER(S)

PA 823/56/3


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9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION

14 April 1997 / 30 January 2009


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10. DATE OF REVISION OF THE TEXT

16 November 2016



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Active Ingredients

 
   Loperamide Hydrochloride