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SUMMARY OF PRODUCT CHARACTERISTICS

1 NAME OF THE MEDICINAL PRODUCT

Loratadine 5mg/5ml Syrup

2 QUALITATIVE AND QUANTITATIVE COMPOSITION

Each ml of syrup contains 1 mg of loratadine.

For excipients, see 6.1.

3 PHARMACEUTICAL FORM

Syrup

Clear colourless to pale yellow solution with a peach odour.

4    CLINICAL PARTICULARS

4.1    Therapeutic indications

Loratadine 5mg/5ml Syrup is indicated for the symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.

4.2 Posology and method of administration

Adults and children over 12 years of age:

10 ml (10mg) of the syrup once daily.

Children aged 2 to 12 years of age with:

Body weight more than 30 kg: 10 ml (10 mg) of the syrup once daily.

Body weight 30 kg or less: 5ml (5 mg) of the syrup once daily.

Efficacy and safety of Loratadine 5mg/5ml Syrup in children under 2 years of age has not been established.

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 ml (10 mg) every other day is recommended for adults and children weighing more than 30 kg, and for children weighing 30 kg or less, 5 ml (5 mg) every other day is recommended.

No dosage adjustments are required in the elderly or in patients with renal insufficiency.

The syrup may be taken without regard to mealtime.

4.3 Contraindications

Loratadine 5mg/5ml Syrup is contraindicated in patients who are hypersensitive to the active substance or to any of the excipients in the formulation.

4.4 Special warnings and precautions for use

Loratadine 5mg/5ml Syrup should be used with caution in the treatment of patients with severe liver impairment (see Section 4.2).

Loratadine 5mg/5ml Syrup contains 3.125 g of sucrose per 5 ml. This should be taken into account in patients with diabetes mellitus.

Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.

The administration of Loratadine 5mg/5ml Syrup should be discontinued at least 48 hours before skin tests, as antihistamines may prevent or reduce otherwise positive reactions to dermal reactivity index.

Interaction with other medicinal products and other forms of interaction

When administered concomitantly with alcohol, Loratadine 5mg/5ml Syrup has no potentiating effects as measured by psychomotor performance studies.

Due to the wide therapeutic index of loratadine no clinically relevant interactions are expected and none were observed in the conducted clinical trials (see Section 5.2).

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.

4.6 Pregnancy and lactation

Loratadine was not teratogenic in animal studies. The safe use of loratadine during pregnancy has not been established. The use of Loratadine 5mg/5ml Syrup during pregnancy is therefore not recommended.

Loratadine is excreted in breast milk, therefore the use of loratadine is not recommended in breastfeeding women.

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

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%).

In clinical trials involving adults and adolescents in a range of indications including AR and CIU, at the recommended dose of 10 mg daily, adverse reactions with loratadine were reported in 2 % of patients in excess of those treated 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.

Immune disorders	Anaphylaxis
Nervous system disorders	Dizziness
Cardiac disorders	Tachycardia, palpitation
Gastrointestinal disorders	Nausea, dry mouth, gastritis
Hepato-biliary disorders	Abnormal hepatic function
Skin and subcutaneous tissue disorders	Rash, alopecia
General disorders and administration site conditions	Fatigue

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 - H antagonist, ATC code: R06A X13.

Loratadine, the active ingredient in Loratadine 5mg/5ml Syrup, is a tricyclic antihistamine with selective, peripheral H₁-receptor activity.

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 on intrinsic cardiac pacemaker activity.

5.2 Pharmacokinetic properties

After oral administration, loratadine is rapidly and well absorbed, and undergoes 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 (T_max) between 1-1.5 hours and 1.5-3.7 hours after administration, respectively.

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).

Loratadine is highly bound to plasma proteins (97% to 99%), its active metabolite moderately bound (73% to 76%) to plasma proteins.

In healthy subjects, the plasma distribution half-lives of loratadine and its active metabolite are approx. 1 and 2 hours, respectively. 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.

Approximately 40% of the dose is excreted via 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 excreted in the urine during the first 24 hours. Less than 1% of the active substance is excreted unchanged in active form, as loratadine or DL.

The bioavailability parameters of loratadine and of the active metabolite are dose proportional.

The pharmacokinetic profile of loratadine and its metabolites is comparable in healthy adult volunteers and healthy geriatric volunteers.

Concomitant ingestion of food can delay slightly the absorption of loratadine but without influencing the clinical effect.

In patients with chronic renal impairment, both the AUC and peak plasma levels (C_max) increased for loratadine and its metabolite as compared to the AUCs and peak plasma levels (C_max) 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.

In patients with chronic alcoholic liver disease, the AUC and peak plasma levels (C_max) of loratadine were double while the pharmacokinetic profile of the active metabolite was not significantly changed from that in patients with normal liver function. The elimination half-lives for loratadine and its metabolite were 24 and 37 hours, respectively, and increased with increasing severity of liver disease.

Loratadine and its active metabolite are excreted in the breast milk of lactating women.

5.3 Preclinical safety data

Preclinical 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

Sucrose

Sodium benzoate Citric acid anhydrous

Peach flavour (benzyl alcohol, propylene glycol)

Glycerol

Propylene glycol

Purified water

Incompatibilities

Not applicable

6.3 Shelf life

3 years (before opening) 28 days (after opening)

6.4 Special precautions for storage

No special storage conditions

6.5 Nature and contents of container

Light weight amber, Type III glass bottle with 28mm child-resistant polypropylene screw cap:

60ml (fill volume 50 or 60 ml),

100 ml (fill volume 70 or 100ml),

150 ml (fill volume 120 or 150 ml),

200 ml (fill volume 150 or 200ml),

A 5 ml measuring spoon with a 2.5 ml graduation is provided in the carton.