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COLOFAC TABLETS 135MG

Active substance(s): MEBEVERINE HYDROCHLORIDE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Colofac Tablets 135 mg

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Mebeverine hydrochloride 135mg
Excipients with known effect: Lactose and Sucrose
For a full list of excipients, see section 6.1

3

PHARMACEUTICAL FORM
Coated tablets (Tablets)
Round white sugar coated tablets, with no superficial markings

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
For the symptomatic treatment of irritable bowel syndrome and other conditions
usually included in this grouping, such as: chronic irritable colon, spastic
constipation, mucous colitis, spastic colitis. Colofac is effectively used to treat the
symptoms of these conditions, such as: colicky abdominal pain and cramps,
persistent, non-specific diarrhoea (with or without alternating constipation) and
flatulence.

4.2

Posology and method of administration
For oral use.
The coated tablets should be swallowed with a sufficient amount of water (at least
100 ml water). They should not be chewed because of the unpleasant taste.
Duration of use is not limited.

If one or more doses are missed, the patient should continue with the next dose as
prescribed; the missed dose(s) should not be taken in addition to the regular dose.
Adults (including the elderly):
One tablet three times a day, preferably 20 minutes before meals. After a period of
several weeks, when the desired effect has been obtained, the dosage may be
gradually reduced.
Paediatric Population
Mebeverine 135 mg tablets are not recommended for use in children and adolescents
below 18, due to insufficient data on safety and efficacy.
Special Population
No posology studies in elderly, renal and/or hepatic impaired patients have been
performed. No specific risk for elderly, renal and/or hepatic impaired patients could
be identified from available post-marketing data. No dosage adjustment is deemed
necessary in elderly, renal and/or hepatic impaired patients.

4.3

Contraindications
Hypersensitivity to the active substance or to any of the excipients.

4.4

Special warnings and precautions for use
Since Mebeverine coated tablets contain lactose, patients with rare hereditary
problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose
malabsorption should not take this medicine.
The coated tablets contain sucrose and should not be used by patients with rare
hereditary problems of fructose intolerance, glucose-galactose malabsorption or
sucrase-isomaltase insufficiency.

4.5

Interaction with other medicinal products and other forms of interaction
No interaction studies have been performed, except with alcohol. In vitro and
in vivo studies in animals have demonstrated the absence of any interaction
between mebeverine hydrochloride and ethanol.

4.6

Fertility, Pregnancy and lactation
Pregnancy

There are no or limited amounts of data from the use of mebeverine in
pregnant women. Animal studies are insufficient with respect to reproductive
toxicity (see section 5.3) mebeverine is not recommended during pregnancy.
Lactation
It is unknown whether mebeverine or its metabolites are excreted in human
milk. The excretion of mebeverine in milk has not been studied in animals.
Mebeverine should not be used during breast-feeding.
Fertility
There are no clinical data on male or female fertility; however, animal studies
do not indicate harmful effects of mebeverine (see section 5.3).

4.7

Effects on ability to drive and use machines
No studies on the effects on the ability to drive and use machines have been
performed. The pharmacodynamic and pharmacokinetic profile as well as
postmarketing experience do not indicate any harmful effect of mebeverine on
the ability to drive or to use machines.

4.8

Undesirable effects
The following adverse reactions have been reported spontaneously during
postmarketing use. A precise frequency cannot be estimated from available
data.
Allergic reactions mainly but not exclusively limited to the skin have been
observed.
Immune system disorders:
Hypersensitivity (anaphylactic reactions)
Skin and subcutaneous tissue disorders:
Urticaria, angioedema, face oedema, exanthema
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

Theoretically CNS excitability may occur in cases of overdose. In cases where
mebeverine was taken in overdose, symptoms were either absent or mild and
usually rapidly reversible. Observed symptoms of overdose were of a
neurological and cardiovascular nature.
No specific antidote is known and symptomatic treatment is recommended.
Gastric lavage should only be considered in case of multiple intoxication or if
discovered within about one hour. Absorption reducing measures are not
necessary.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Pharmacotherapeutic group: Synthetic anticholinergics, esters with tertiary
amino group, ATC-Code: A03AA04
Mebeverine is a musculotropic antispasmodic with a direct action on the smooth
muscle of the gastrointestinal tract, without affecting normal gut motility. The
exact mechanism of action is not known, but multiple mechanisms, such as a
decrease in ion channel permeabilities, blockade of noradrenaline reuptake, a
local anesthetic effect, changes in water absorption as well as weak antimuscarinergic and phosphodiesterase inhibitory effect might contribute to the
local effect of mebeverine on the gastrointestinal tract. Systemic side-effects
as seen with typical anti-cholinergics are absent.
Clinical efficacy and safety
All formulations of mebeverine were generally safe and well tolerated in the
recommended dose regimen.
Paediatric population
The safety and efficacy of the product has only been evaluated in adults.

5.2

Pharmacokinetic properties
Absorption:
Mebeverine is rapidly and completely absorbed after oral administration of
tablets.
Distribution:
No significant accumulation occurs after multiple doses.
Biotransformation:
Mebeverine hydrochloride is mainly metabolised by esterases, which split the
ester bonds into veratric acid and mebeverine alcohol firstly.

The main metabolite in plasma is DMAC (demethylated carboxylic acid).
The steady state elimination half-life of DMAC is 2.45 h. During multiple
dosing Cmax of DMAC for the coated tablets with 135mg is 1670ng/ml and
tmax is 1 h.
Elimination:
Mebeverine is not excreted as such, but metabolised completely; the
metabolites are excreted nearly completely. Veratric acid is excreted into the
urine, mebeverine alcohol is also excreted into the urine, partly as the
corresponding carboxylic acid (MAC) and partly as the demethylated
carboxylic acid (DMAC).
Paediatric population
The safety and efficacy of the product has only been evaluated in adults.

5.3

Preclinical safety data
Effects in repeat-dose toxicity studies, after oral and parenteral doses, were
indicative of central nervous involvement with behavioural excitation, mainly
tremor and convulsions. In the dog, the most sensitive species, these effects
were seen at oral doses equivalent to 3 times the maximum recommended
clinical dose of 400mg/day based on body surface area (mg/m2) comparisons.
The reproductive toxicity of mebeverine was not sufficiently investigated in
animal studies.
There was no indication of teratogenic potential in rats and rabbits. However,
embryotoxic effects (reduction in litter size, increased incidence of resorption)
were noticed in rats at doses equivalent to twice the maximum daily clinical
dose. This effect was not observed in rabbits. No effects on male or female
fertility were noted in rats at doses equivalent to the maximum clinical dose.
In conventional in vitro and in vivo genotoxicity tests mebeverine was devoid
of genotoxic effects. No carcinogenicity studies have been performed.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose, starch (potato), povidone, talc, magnesium stearate, sucrose, gelatin,
acacia, carnauba wax

6.2

Incompatibilities
Not applicable

6.3

Shelf life
5 years

6.4

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

6.5

Nature and contents of container
Boxes containing 10, 15, 84 or 100 tablets in blister strips

6.6

Special precautions for disposal
None

7

MARKETING AUTHORISATION HOLDER
BGP Products Ltd.
Abbott House,
Vanwall Business Park,
Vanwall Road, Maidenhead,
SL6 4XE,
UK

8

MARKETING AUTHORISATION NUMBER(S)

PL 43900/0028

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
14/03/1978 / 20/04/2005

10

DATE OF REVISION OF THE TEXT
05/04/2015

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Source: Medicines and Healthcare Products Regulatory Agency

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