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VALUE HEALTH DIARRHOEA RELIEF 2MG CAPSULES

Active substance(s): LOPERAMIDE HYDROCHLORIDE / LOPERAMIDE HYDROCHLORIDE / LOPERAMIDE HYDROCHLORIDE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Value Health Diarrhoea Relief 2mg Capsules
Boots Diarrhoea Relief 2mg Capsules

2.

QUALITATIVE AND QUANTITATIVE COMPOSITION

Active ingredients
Loperamide Hydrochloride

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2 mg per capsule

PHARMACEUTICAL FORM
Capsules, hard (Capsule)
Hard, gelatine capsule (size 4) with an opaque green cap printed "0611" in
black ink, and an opaque grey body containing a white powder.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
P and GSL:
For the symptomatic treatment of acute diarrhoea, in adults and children 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. For oral administration.
Acute diarrhoea:
Adults and children of 12 years of age and over:

The initial dose is 2 capsules (4 mg) followed by 1 capsule (2 mg) after every
subsequent loose stool.
If symptoms persist for more than 24 hours consult your doctor.
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:
The initial dose is 2 capsules (4 mg). This initial dose should be adjusted until 1-2
solid stools a day are obtained, which is usually achieved with a maintenance dose of
1-6 capsules (2-12 mg) daily.
Consult your doctor if you develop new symptoms, or if your symptoms worsen, or if
your symptoms have not improved over two weeks.
The maximum dose for acute diarrhoea and acute episodes of diarrhoea associated
with irritable bowel is:
GSL – 6 capsules (12 mg) daily for adults and children of 12 years of age and over
P – 8 capsules (16 mg) daily for adults and children of 12 years of age and over
Children under 12 years
Loperamide HCl capsules should not be used in children under 12 years of age.
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,
loperamide HCl should be used with caution in such patients because of reduced first
pass metabolism (see section 4.4 special warnings and special precautions for use).

4.3

Contraindications
Loperamide HCl is contraindicated in patients with known hypersensitivity to
loperamide HCl or to any of the excipients.
The loperamide HCl capsule should not be used in children under 12 years of age.
Loperamide HCl should not be used as the primary therapy:

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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.

Loperamide HCl should 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. Loperamide HCl must be discontinued promptly when constipation,
abdominal distension or ileus develop.

4.4

Special warnings and precautions for use
Treatment of diarrhoea with loperamide HCl is only symptomatic. Whenever an
underlying aetiology can be determined, specific treatment should be given when
appropriate.
In patients with diarrhoea, especially in children, frail and elderly patients, fluid and
electrolyte depletion may occur. In such cases administration of appropriate fluid and
electrolyte replacement therapy is the most important measure.
In acute diarrhoea, if clinical improvement is not observed within 24 hours, the
administration of loperamide HCl should be discontinued and patients should be
advised to consult their physician.
This product should not be used for prolonged periods. Diarrhoea is a common
presentation of a number of significant gastrointestinal conditions. This medicine is
indicated only for the symptomatic treatment of acute episodes of diarrhoea
associated with irritable bowel syndrome. This medicine should not be used for
prolonged periods until an underlying cause for persistent diarrhoea has been
investigated and diagnosed by a doctor.
Patients with AIDS treated with loperamide HCl 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
HCl.
Although no pharmacokinetic data are available in patients with hepatic impairment,
loperamide HCl should be used with caution in such patients because of reduced first
pass metabolism. This medicine must be used with caution in patients with hepatic
impairment as it may result in a relative overdose leading to CNS toxicity.
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.
For acute diarrhoea

If symptoms persist for more than 24 hours, consult your doctor.
For acute episodes of diarrhoea associated with irritable bowel syndrome
Warnings to be included in the leaflet:
Only take loperamide HCl to treat acute episodes of diarrhoea associated with
irritable bowel syndrome (IBS) if your doctor has previously diagnosed IBS.
If any of the following now apply, do not use the product without first consulting
your doctor, even if you know you have IBS:
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If you are 40 years or over and it is some time since your last attack of IBS or
the symptoms are different this time
If you have recently passed blood from the bowel
If you suffer from severe constipation
If you are feeling sick or vomiting
If you have lost your appetite or lost weight
If you have difficulty or pain passing urine
If you have a fever
If you have recently travelled abroad

Consult your doctor if you develop new symptoms, or if your symptoms worsen, or if
your symptoms have not improved over two weeks.
Keep all medicines out of the reach of children.
Ponceau 4R (E124) can cause allergic-type reactions including asthma. Allergy is
more common in those people who are allergic to aspirin.

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
doses, 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. The increase was not associated with increased
pharmacodynamic effects as measured by pupillometry.
Concomitant treatment with oral desmopressin resulted in a 2-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
It is not advisable to administer this medicine in pregnancy. Women who are
pregnant or breast feeding should therefore be advised to consult their doctor
for appropriate treatment.
Although there is no indication that loperamide HCl possesses teratogenic or
embryotoxic properties it should not be administered in pregnancy.
Small amounts of loperamide HCl may appear in human breast-milk.
Therefore loperamide HCl is not recommended during breast-feeding.

4.7

Effects on ability to drive and use machines

Tiredness, dizziness or drowsiness may occur in the setting of diarrhoeal syndromes
treated with loperamide HCl. Therefore, it is advisable to use caution when driving a
car or operating machinery.

4.8

Undesirable effects

Adults and children aged ≥12 years
The safety of loperamide HCl was evaluated in 3076 adults and children aged
≥12 years who participated in 31 controlled and uncontrolled clinical trials of
loperamide HCl used for the treatment of diarrhoea. Of these, 26 trials were in
acute diarrhoea (N=2755) and 5 trials were in chronic diarrhoea (N=321).
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%).
In clinical trials in chronic diarrhoea, the most commonly reported (i.e. ≥1%
incidence) ADRs were: flatulence (2.8%), constipation (2.2%), nausea (1.2%)
and dizziness (1.2%).
Table 1 displays ADRs that have been reported with the use of loperamide
HCl from either clinical trial (in acute or chronic diarrhoea or both) of post-

marketing experience.
The frequency categories use the following convention: very common (≥1/10);
common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10,000
to <1/1000); and very rare (<1/10,000).

Table 1 Adverse Drug Reactions
System Organ Class
Indication
Acute
Diarrhoea
(N=2755)

Chronic
Diarrhoea
(N=321)

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
consciousness a, Hypertoniaa,
Coordination abnormalitya

Rare
Uncommon Common
Common
Common
Common
Uncommon
Uncommon
Rare

Eye Disorders
Miosisa
Gastrointestinal Disorders
Constipation, Nausea, Flatulence
Abdominal pain, Abdominal
discomfort, Dry mouth
Abdominal pain upper, Vomiting
Dyspepsia
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

Acute &
Chronic
Diarrhoea
and post
marketing
experience

Rare
Common

Common

Common

Uncommon Uncommon Uncommon
Uncommon
Uncommon
Uncommon Uncommon
Rare
Rare

Rare

Uncommon
Uncommon

Rare

Renal and urinary disorders
Rare
a
Urinary retention
General Disorders and
Administration Site Conditions
Fatiguea
Rare
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 for adults and children, the
frequency is estimated from all clinical trials with loperamide HCl combined,
including trials in children ≤12 years (N=3683).
b
: See section 4.4 Special Warnings and Special Precautions for use.
For clinical trial ADRs where no frequency is presented, the term was not
observed or considered an ADR for this indication.
Paediatric population
The safety of loperamide HCl was evaluated in 607 patients aged 10 days to
13 years who participated in 13 controlled and uncontrolled clinical trials of
loperamide HCl used for the treatment of acute diarrhoea. In general, the ADR
profile in this patient population was similar to that seen in clinical trials of
loperamide HCl in adults and children aged 12 years and over.

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 the Yellow Card Scheme at
www.mhra.gov.uk/yellowcard.

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), urinary retention,
constipation and ileus may occur. Children may be more sensitive to CNS
effects than adults.
In individuals who have ingested overdoses of loperamide HCL, cardiac
events such as QT 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
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
Loperamide hydrochloride is a synthetic opioid which inhibits gut motility by
binding to opiate receptors in the gut wall and may also reduce gastrointestinal
secretions, resulting in improvement in diarrhoeal symptoms. Loperamide also
increases the tone of the anal sphincter.
In a double blind randomised trial in 213 patients with acute diarrhoea,
loperamide (56 patients) was compared with two other common antidiarrhoeal
agents and placebo. Onset of antidiarrhoeal effect occurred as soon as one
hour after intake of a 4mg dose of loperamide.

5.2.

Pharmacokinetic properties
More than 65% of a dose of loperamide is reported to be absorbed from the
gastrointestinal tract. The drug undergoes considerable first pass metabolism
in the liver and excretion via the bile in the faeces as the inactive conjugate. As
a result of the drug’s high affinity for the gut wall and its high first pass
metabolism very little loperamide reaches the systemic circulation and
therefore there is only a small amount of urinary excretion. The elimination
half life is reported to be about 10 hours.

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), loperamide has
cardiac electrophysiological actions consisting of inhibition of potassium (hERG) and
sodium currents, and arrhythmias.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose monohydrate
Magnesium stearate
Maize starch (pregelatinised)
Hard gelatin capsule (gelatin, Ponceau 4R-E124, Indigo Carmine-E132, Titanium
dioxide-E171, Yellow and black iron oxides E172)
Ink (Black iron oxide E172, Shellac, Propylene glycol)

6.2.

Incompatibilities
Not applicable.

17.3

Shelf life
36 months

6.4.

Special precautions for storage
Do not store above 30°C. Store in the original package.

6.5.

Nature and contents of container
1. Blister of clear 250 micron PVC and 20 micron aluminium foil.
Pack size: 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 28, 30, 32, 36, 48.
2. Blister of clear 250 micron PVC coated with 40 gsm PVdC and 20 micron
aluminium foil.
Pack size: 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 28, 30, 32, 36, 48.

6.6.

Instruction for use, handling and disposal
Not applicable.

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MARKETING AUTHORISATION HOLDER
The Boots Company PLC
1 Thane Road West
Nottingham
NG2 3AA
Trading as Value Health

8.

MARKETING AUTHORISATION NUMBER
PL 00014/0611

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DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
26/10/2005

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DATE OF REVISION OF THE TEXT
19/06/2017

Expand Transcript

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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