Loratadine .................................................... 10 mg
Excipients: q.s ………………………………………… 1 tablet
Tablet.
Product description: An oval, white to off-white tablet, plain on one side, imprinted on the other side, undamaged edges.
Box of 2 blisters x 10 tablets.
Pharmacotherapeutic group: Antihistamines - H1 antagonist, ATC code: R06A X13.
Mechanism of action
Loratadine 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 on 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.
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% to 99%) and its active major metabolite desloratadine (DL) moderately bound (73% to 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 active 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 active 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 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 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 adult volunteers and in healthy geriatric volunteers.
In clinical trials that assessed driving ability, no impairment occurred in patients receiving loratadine. Loratadine tablets has no or negligible influence on the ability to drive and use machines. However, patients should be informed that very rarely some people experienced drowsiness, which may affect their ability to drive or use machines.
Loratadine tablets should be administered with caution in patients with severe liver impairment.
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.
Excipients
Wheat starch: This medicine contains only very low levels of gluten. It is very unlikely to cause problems if you have coeliac disease. If you have wheat allergy, you should not take this medicine.
Lactose monohydrate: Patients with problems of galactose intolerance, lactase deficiency, glucose-galactose malabsorption should not take this medicine.
Pregnancy
A large amount of data on pregnant women (more than 1000 exposed outcomes) indicates no malformative nor foeto/neonatal toxicity of loratadine. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of loratadine during pregnancy.
Breast-feeding
Loratadine is excreted in breast milk, therefore the use of loratadine is not recommended in breast-feeding women.
Fertility
There is no data available on male and female fertility.
When administered concomitantly with alcohol, Loratadine tablets have 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.
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.
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%).
The following adverse reactions reported during the post-marketing period are listed in the following table by system organ class. 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
Immune system disorders
Very rare: Hypersensitivity reactions (including angioedema and anaphylaxis).
Nervous system disorders
Very rare: Dizziness, convulsion.
Cardiac disorders
Very rare: Tachycardia, palpitation.
Gastrointestinal disorders
Very rare: Nausea, dry mouth, gastritis.
Hepato-biliary disorders
Very rare: Abnormal hepatic function.
Skin and subcutaneous tissue disorders
Very rare: Rash, alopecia.
General disorders and administration site conditions
Very rare: Fatigue.
Investigations
Not known: Weight increased.
Please inform your doctor of all undesirable effects upon drug administration.
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.
Store in dry places, not exceeding 30oC, protect from light.
Loratadine tablets are indicated for the symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria
Hypersensitivity to the active substance or to any of the excipients listed in the medicinal product.
METHOD OF ADMINISTRATION
For oral administration.
POSOLOGY
Adults and children over 12 years of age: 10 mg (1 tablet) once daily. The tablet may be taken without regard to mealtime.
Children 2 to 12 years of age with:
- Body weight more than 30 kg: 10 mg (1 tablet) once daily.
- Body weight 30 kg or less: These tablets are not suitable in children with a body weight less than 30 kg.
Efficacy and safety of loratadine 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, 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.
Or as directed by the physician.
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