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LORATADINE 10MG FILM-COATED TABLETS

Active substance(s): LORATADINE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Loratadine 10mg Film-coated Tablets

2

QUALITATIVE AND QUANTITATIVE COMPOSITION

Each film-coated tablet contains 10 mg loratadine.
Excipient with known effect: each tablet contains 84.5 mg lactose monohydrate.
For the full list of excipients, see section 6.1.

3

PHARMACEUTICAL FORM

Film-coated tablet.
White, round, biconvex film-coated tablets scored on one side and marked “LR 10” on the
other side.
The tablet can be divided into equal doses.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications

Loratadine Tablets are indicated for the symptomatic treatment of allergic rhinitis and chronic
idiopathic urticaria in adults and children over the age of 2 years with a body weight more
than 30 kg.

4.2

Posology and method of administration

Posology
Adults and children over 12 years of age:
10 mg once daily (one film-coated tablet once daily).
Paediatric population
Children 2 to 12 years of age are dosed by weight:

Body weight more than 30 kg: 10mg once daily (one film-coated tablet once daily).
Body weight 30 kg or less: The 10 mg strength film-coated tablet is not appropriate in
children with a body weight less than 30 kg.
Safety and efficacy of loratadine in children under 2 years of age has not been established. No
data are available.
Patients with hepatic impairment
Patients with severe liver impairment should be administered a lower initial dose because they
may have reduced clearance of loratadine. An initial dose of 10 mg every other day is
recommended for adults and children weighing more than 30 kg.
Patients with renal impairment
No dosage adjustments are required in patients with renal insufficiency.
Elderly
No dosage adjustments are required in the elderly.
Method of administration
For oral use. The tablet may be taken without regard to mealtime.

4.3

Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

4.4

Special warnings and precautions for use

Loratadine should be administered with caution in patients with severe liver impairment (see
section 4.2).
Loratadine contains lactose. Patients with rare hereditary problems of galactose intolerance,
the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
The administration of loratadine should be discontinued at least 48 hours before skin tests
since antihistamines may prevent or reduce otherwise positive reactions to dermal reactivity
index.

4.5

Interaction with other medicinal products and other forms of interaction

When administered concomitantly with alcohol loratadine has no potentiating effects as
measured by psychomotor performance studies.
Potential interaction may occur with all known inhibitors of CYP3A4 or CYP2D6 resulting in
elevated levels of loratadine (see section 5.2), which may cause an increase in adverse events.
Increase in plasma concentrations of loratadine has been reported after concomitant use with
ketoconazole, erythromycin, and cimetidine in controlled trials, but without clinically
significant changes (including electrocardiographic).
Paediatric population
Interaction studies have only been performed in adults.

4.6

Fertility, pregnancy and lactation

Pregnancy
A large amount of data on pregnant women (more than 1000 exposed outcomes) indicate no
malformative nor foeto/ neonatal toxicity of loratadine. Animal studies do not indicate direct
or indirect harmful effects with respect to reproductive toxicity (see section 5.3). As a
precautionary measure, it is preferable to avoid the use of loratadine during pregnancy.
Breast-feeding
Loratadine is excreted in breast milk. A risk to the newborns/infants cannot be excluded. The
use of loratadine is not recommended in breast-feeding women.
Fertility
There are no data available on male and female fertility.

4.7

Effects on ability to drive and use machines

In clinical trials that assessed driving ability, no impairment occurred in patients receiving
loratadine. However, patients should be informed that very rarely some people experience
drowsiness, which may affect their ability to drive or use machines.

4.8

Undesirable effects

Summary of the safety profile
In clinical trials involving adults and adolescents in a range of indications including allergic
rhinitis (AR) and chronic idiopathic urticaria (CIU), at the recommended dose of 10 mg daily,
adverse reactions with loratadine were reported in 2% of patients in excess of those with
placebo. The most frequent adverse reactions reported in excess of placebo were somnolence
(1.2%), headache (0.6%), increased appetite (0.5%) and insomnia (0.1%). Other adverse
reactions reported very rarely during the post-marketing period are listed in the following
table by System Organ Class.
Tabulated list of adverse reactions
Frequencies are defined as 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), very rare (< 1/10,000) and not known
(cannot be estimated from the available data).
Within each frequency grouping, adverse reactions are presented in order of decreasing
seriousness.

System Organ Classes

Common

Immune system
disorders

Nervous
system disorders
Cardiac disorders
Gastrointestinal
disorders

Hepatobiliary
disorders
Skin and
subcutaneous tissue
disorders
General disorders and
administration site
conditions

Uncommon

Rare

Very Rare
Hypersensitivity
reactions
(including
angioedema and
anaphylaxis)
Dizziness,
convulsion
Tachycardia,
palpitation
Nausea,
dry mouth,
gastritis
Abnormal hepatic
function
Rash,
alopecia
Fatigue

Paediatric population
In clinical trials in a paediatric population, children aged 2 through 12 years, common adverse
reactions reported in excess of placebo were headache (2.7%), nervousness (2.3%), and
fatigue (1%).
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 [to be
completed nationally].

4.9.

Overdose
Overdosage with loratadine increased the occurrence of anticholinergic
symptoms. Somnolence, tachycardia, and headache have been reported with
overdoses.
In the event of overdose, general symptomatic and supportive measures are to
be instituted and maintained for as long as necessary. Administration of
activated charcoal as a slurry with water may be attempted. Gastric lavage
may be considered. Loratadine is not removed by haemodialysis and it is not
known if loratadine is removed by peritoneal dialysis. Medical monitoring of
the patient is to be continued after emergency treatment.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties

Pharmacotherapeutic group: antihistamines for systemic use, ATC code: R06AX13.
Mechanism of action
Loratadine, the active ingredient in Loratadine tablets, is a tricyclic antihistamine with
selective, peripheral H1-receptor activity.
Pharmacodynamic effects
Loratadine has no clinically significant sedative or anticholinergic properties in the majority
of the population and when used at the recommended dosage.
During long-term treatment there were no clinically significant changes in vital signs,
laboratory test values, physical examinations or electrocardiograms.
Loratadine has no significant H2-receptor activity. It does not inhibit norepinephrine uptake
and has practically no influence on cardiovascular function or no intrinsic cardiac pacemaker
activity.
Human histamine skin wheal studies following a single 10 mg dose has shown that the
antihistamine effects are seen within 1-3 hours reaching a peak at 8-12 hours and lasting in
excess of 24 hours. There was no evidence of tolerance to this effect after 28 days of dosing
with loratadine.
Clinical efficacy and safety
Over 10,000 subjects (12 years and older) have been treated with loratadine 10 mg tablets in
controlled clinical trials. Loratadine 10 mg tablets once daily was superior to placebo and
similar to clemastine in improving the effects on nasal and non-nasal symptoms of AR. In
these studies somnolence occurred less frequently with loratadine than with clemastine and
about the same frequency as terfenadine and placebo.
Among these subjects (12 years and older), 1000 subjects with CIU were enrolled in placebo
controlled studies. A once daily 10 mg dose of loratadine was superior to placebo in the
management of CIU as demonstrated by the reduction of associated itching, erythema and
hives. In these studies the incidence of somnolence with loratadine was similar to placebo.
Paediatric population
Approximately 200 paediatric subjects (6 to 12 years of age) with seasonal allergic rhinitis
received doses of loratadine syrup up to 10 mg once daily in controlled clinical trials. In
another study, 60 paediatric subjects (2 to 5 years of age) received 5 mg of loratadine syrup
once daily. No unexpected adverse events were observed.
The paediatric efficacy was similar to the efficacy observed in adults.

5.2

Pharmacokinetic properties

Absorption

Loratadine is rapidly and well-absorbed. Concomitant ingestion of food can delay slightly the
absorption of loratadine but without influencing the clinical effect. The bioavailability
parameters of loratadine and of the active metabolite are dose proportional.
Distribution
Loratadine is highly bound (97% - 99 %) and its active major metabolite desloratadine (DL)
moderately bound (73% – 76%) to plasma proteins.
In healthy subjects, plasma distribution half-lives of loratadine and its active metabolite are
approximately 1 and 2 hours, respectively.
Biotransformation
After oral administration, loratadine is rapidly and well absorbed and undergoes an extensive
first pass metabolism, mainly by CYP3A4 and CYP2D6. The major metabolite desloratadine (DL) - is pharmacologically active and responsible for a large part of the
clinical effect. Loratadine and DL achieve maximum plasma concentrations (tmax) between 1 1.5 hours, and 1.5 - 3.7 hours after administration, respectively.
Elimination
Approximately 40 % of the dose is excreted in the urine and 42% in the faeces over a 10 day
period and mainly in the form of conjugated metabolites. Approximately 27% of the dose is
eliminated in the urine during the first 24 hours. Less than 1% of the active substance is
excreted unchanged in the active form, as loratadine or DL.
The mean elimination half-lives in healthy adult subjects were 8.4 hours
(range = 3 to 20 hours) for loratadine and 28 hours (range = 8.8 to 92 hours) for the major
active metabolite.
Renal impairment
In patients with chronic renal impairment, both the AUC and peak plasma levels (Cmax)
increased for loratadine and its metabolite as compared to the AUCs and peak plasma levels
(Cmax) of patients with normal renal function. The mean elimination half-lives of loratadine
and its metabolite were not significantly different from that observed in normal subjects.
Haemodialysis does not have an effect on the pharmacokinetics of loratadine or its active
metabolite in subjects with chronic renal impairment.
Hepatic impairment
In patients with chronic alcoholic liver disease, the AUC and peak plasma levels (Cmax) of
loratadine were doubled while the pharmacokinetic profile of the active metabolite was not
significantly changed from that in patients with normal liver function. The elimination halflives for loratadine and its metabolite were 24 hours and 37 hours, respectively, and increased
with increasing severity of liver disease.
Elderly
The pharmacokinetic profile of loratadine and its active metabolite is comparable in healthy
volunteers and in healthy geriatric volunteers.

5.3

Preclinical safety data

Non-clinical data reveal no special hazard based on conventional studies of safety,
pharmacology, repeated dose toxicity, genotoxicity, and carcinogenic potential.

In reproductive toxicity studies, no teratogenic effects were observed. However, prolonged
parturition and reduced viability of offspring were observed in rats at plasma levels (AUC) 10
times higher than those achieved with clinical doses.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients

Tablet core
Lactose monohydrate
Cellulose, microcrystalline
Maize starch
Starch, pregelatinised
Silica colloidal hydrated
Magnesium stearate
Film-coat
Hypromellose
Macrogol 400 and 6000
Carnauba wax
Talc

6.2.

Incompatibilities
Not applicable

6.3

Shelf life

3 years.

6.4

Special precautions for storage

Store in the original package.

6.5

Nature and contents of container

PVC/Aluminium blister packs.
Blister pack sizes of 5, 7, 10, 14, 15, 20, 21, 30, 50 and 100
Not all pack sizes will be marketed.

6.6

Special precautions for disposal

No special requirements.

7

MARKETING AUTHORISATION HOLDER

Generics [UK] Limited t/a Mylan
Station Close
Potters Bar
Hertfordshire
EN6 1TL
United Kingdom.

8

MARKETING AUTHORISATION NUMBER(S)
PL 04569/0478

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
01/08/2006

10

DATE OF REVISION OF THE TEXT
05/06/2015

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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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