Histaclar 10mg film coated Tablets

Each film-coated tablet contains 10 mg loratadine.

Each tablets contains 84.5 mg Lactose monohydrate. For a full list of excipients, see section 6.1

Film-coated tablet

Film-coated white round biconvex tablets scored on one side and marked

“LR 10” on the other side.

The tablet can be divided into equal halves.

Loratadine Tablets are indicated for the symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.

Adults and children over 12 years of age:

10 mg once daily (one film-coated tablet once daily). The loratadine tablet may be taken without regard to mealtime.

Children 2 to 12 years of age with:

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.

Efficacy and safety of loratadine Tablets 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 mg every other day is recommended for adults and children weighing more than 30 kg. No dosage adjustments are required in the elderly or in patients with renal insufficiency.

Loratadine Tablets are contraindicated in patients who are hypersensitive to the active substance or to any of the excipients.

Loratadine Tablets should be administered with caution in patients with severe liver impairment (see 4.2).

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 Tablets should be discontinued at least 48 hours before skin tests since antihistamines may prevent or reduce otherwise positive reactions to dermal reactivity index.

When administered concomitantly with alcohol Loratadine Tablets 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, which may cause an increase in adverse events (see 4.8 and 5.2).

Loratadine was not teratogenic in animal studies. The safe use of loratadine during pregnancy has not been established. The use of Loratadine Tablets during pregnancy is therefore not recommended.

Loratadine is excreted in breast milk, therefore the use of loratadine is not recommended in breast-feeding women

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.

In clinical trial 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 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%).

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%).

Adverse reactions that have been reported during post-marketing surveillance are listed below by system organ class and frequency.

Frequencies are defined as: very common ( 1/10); common ( 1/100, <1/10); uncommon ( 1/1000, < 1/100); rare ( 1/10,000, <1000); very rare (< 1/10,000) according to the MedDRA frequency convention and system organ classification.

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.

Pharmacotherapeutic group: antihistamines -H₁ antagonist,

ATC code: RO6A X13. Loratadine, the active ingredient in Loratadine Tablets, 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 no intrinsic cardiac pacemaker activity.

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 (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 (97% - 99 %) and its active metabolite 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. 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 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 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 in 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 doubled 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 hours 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.

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 offsprings were observed in rats at plasma levels (AUC) 10 times higher than those achieved with clinical doses.

No evidence of mucous irritation was observed after daily administration of up to 12 tablets (120 mg) of oral lyophilisates into the hampster cheek pouch for five days.

Tablet core

Lactose monohydrate

Microcrystalline cellulose

Maize starch

Pregelatinized starch

Hydrated colloidal silica

Magnesium stearate

Film-coat

Hypromellose

Macrogol 400 and 6000

Polishing agents

Carnauba wax

Talc

Not applicable

3 years.

Store in the original package.

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.

No special requirements

McDermott Laboratories,

t/a Gerard Laboratories,

Baldoyle Industrial Estate,

Grange Road,

Dublin 13

Ireland

PA 577/46/1

Date of last authorisation: 24 January 2003

Date of last renewal: 01 August 2006

September 2008