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Johnson & Johnson (Ireland) Ltd

Airton Road, Tallaght, Dublin 24, Ireland
Telephone: +353 1 466 5200
Fax: +353 1 466 53160
Medical Information Direct Line: 1 800 22 00 44
Medical Information e-mail: crc@its.jnj.com
Customer Care direct line: 1 800 22 00 44


Summary of Product Characteristics last updated on medicines.ie: 10/11/2017
SPC Imodium Instants 2mg Orodispersible Tablets


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1. NAME OF THE MEDICINAL PRODUCT

Imodium Instants 2 mg Orodispersible Tablets


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2. QUALITATIVE AND QUANTITATIVE COMPOSITION

Loperamide hydrochloride 2 mg per tablet.

Excipients: Each tablet contains 750 micrograms of Aspartame (E951) and the Mint flavouring contains traces of Sulphites.

For a full list of excipients see section 6.1.


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3. PHARMACEUTICAL FORM

Orodispersible tablet

White to off-white, circular, freeze-dried tablets.


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4. CLINICAL PARTICULARS

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4.1 Therapeutic indications

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


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4.2 Posology and method of administration

The orodispersible tablet should be placed on the tongue. The tablet will dissolve and is to be swallowed with saliva. No liquid intake is needed for the orodispersible tablet.

Adults and children over 12 years only

The usual dose is 2 tablets initially, followed by 1 tablet after each further episode of diarrhoea up to a maximum of 5 in 24 hours.

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 Instants should be used with caution in such patients because of reduced first pass metabolism (see 4.4 Special warnings and precautions for use).

Method of administration

Oral.


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4.3 Contraindications

• Imodium use is contraindicated in patients under 12 years of age.

• Imodium Instants are 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.

Imodium is not a substitute for rehydration therapy. In addition to taking Imodium, the patient should be advised to drink plenty of fluids such as water, clear soup and squash.

Patients should be advised to consult their doctor if diarrhoea persists for more than 24 hours.

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 Instants 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.

Cardiac events including QT prolongation and Torsades de Pointes have been reported in association with overdose. Some cases had a fatal outcome (see section 4.9). Patients should not exceed the recommended dose and/or the recommended duration of treatment.

The package leaflet contains the following information:

• Aspartame (E951) contains a source of phenylalanine which may be harmful for people with phenylketonuria.

• Mint flavour contains traces of sulphites. This may rarely cause severe hypersensitivity reactions and bronchospasm.


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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 loperamide in human pregnancy has not been established.

Breast feeding

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

Glossodynia

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 ingested overdoses of loperamide HCl, cardiac events such as QT interval prolongation, Torsades de Pointes, other serious ventricular arrhythmias, cardiac arrest and syncope have been observed (see section 4.4). 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 hours), the patient should be kept under constant observation for at least 48 hours in order to detect any possible depression of the central nervous system.


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5. PHARMACOLOGICAL PROPERTIES

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5.1 Pharmacodynamic properties

Loperamide binds to the opiate receptors 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 antidiarrhoeal 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.


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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

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


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6. PHARMACEUTICAL PARTICULARS

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6.1 List of excipient(s)

Gelatin

Mannitol (E421)

Aspartame (E951)

Sodium hydrogen carbonate

Mint flavour


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6.2 Incompatibilities

Not applicable.


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6.3 Shelf life

4 years.


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6.4 Special precautions for storage

This medicine does not require any special storage conditions.


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6.5 Nature and contents of container

All-aluminium blister packs of 6, 12, 18, and 24 tablets in printed cardboard cartons. The all-aluminium blisters are made from paper, PET, aluminium, PVC and polyamide. Not all pack sizes may be marketed.


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6.6 Special precautions for disposal and other handling

No special requirements.


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7. MARKETING AUTHORISATION HOLDER

Johnson & Johnson (Ireland) Ltd.

Airton Road

Tallaght

Dublin 14

Ireland


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8. MARKETING AUTHORISATION NUMBER(S)

PA 330/45/1


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9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION

3 October 2003 / 3 October 2008


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10. DATE OF REVISION OF THE TEXT

20 October 2017



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Active Ingredients

 
   Loperamide Hydrochloride