AERIUS TABLETSAND SYRUP
NAME OF MEDICINE
AERIUS (desloratadine 5 mg) Tablets
AERIUS (desloratadine 0.5 mg/mL) Syrup
AERIUS tablets contain desloratadine 5 mg and the following inactive ingredients:
Core: calcium hydrogen phosphate, microcrystalline cellulose, maize starch and talc
Coating: Opadry Blue, Opadry Clear, carnauba wax and white beeswax
AERIUS Syrup contains desloratadine 0.5 mg/mL and the following inactive ingredients:
Propylene glycol, sorbitol, anhydrous citric acid, sodiumcitrate, disodium edetate, sucrose, bubble
gum flavour, colour E110, water and sodium benzoate as preservative.
Desloratadine is a non-sedating long-acting histamine antagonist with potent, selective peripheral
-receptor antagonist activity. Desloratadine has demonstrated antiallergic, antihistaminic and
After oral administration, desloratadine selectively blocks peripheral histamine H
because the drug is effectively excluded fromentry to the central nervous system.
In addition to antihistaminic activity, desloratadine has demonstrated antiallergic and anti-
inflammatory activities from numerousin vitro (mainly conducted on cells of human origin) andin
vivo studies. These studies have shown that desloratadine inhibits the broad cascade of events
that initiate and propagate allergic inflammation including:
The release of proinflammatory cytokines includingIL-4, IL-6, IL-8, IL-13,
The release of important proinflammatory chemokines such as RANTES (Regulated upon
Activation, Normal T-cell Expressed and Secreted),
Superoxide anion production by activated polymorphonuclear neutrophils,
Eosinophil adhesion and chemotaxis,
The expression of the adhesion molecules such as P-selectin,
IgE-dependent release of histamine, prostaglandin (PGD2), and leukotriene (LTC4),
The acute allergic bronchoconstrictor response and allergic cough in animal models.
In a multiple dose clinical trial, in which up to 20 mg of desloratadine was administered daily for
14 days, no statistically or clinically relevant cardiovascular effect was observed. In a clinical
pharmacological trial, in which desloratadine was administered at a dose of 45 mg daily (nine
times the clinical dose) for ten days, no prolongation of the QTc interval was seen.
Desloratadine does not readily penetrate the central nervous system. At the recommended dose
of 5mg daily, there was no excess incidence ofsomnolence as compared to placebo. AERIUS at
a dose of 7.5 mg daily did not affect psychomotor performance in clinical trials.
No clinically relevant changes in desloratadine plasma concentrations were observed in multiple-
dose azithromycin, fluoxetine, cimetidine, ketoconazole and erythromycin interaction trials.
In clinical pharmacological trials, co-administration of alcohol did not increase the alcohol-induced
impairment in performance or increase in sleepiness. No significant differences were found in the
psychomotor test results between desloratadine and placebo groups, whether administered alone
or with alcohol.
A single dose of desloratadine 5 mg did not affect standard measures of flight performance
including exacerbation of subjective sleepiness or tasks related to flying.
Assessments of quality of life in the clinical trials indicated that seasonal allergic rhinitis produced
a consistent burden of disease, and that improvements in therapeutic responses were associated
with improvements in various quality of life domains including vitality and social functioning.
In addition to the established classifications of seasonal and perennial, allergic rhinitis can
alternatively be classified as intermittent and persistent allergic rhinitis according to the duration of
symptoms. Intermittent allergic rhinitis is defined as the presence of symptoms for less than 4
days per week or for less than 4 weeks. Persistent allergic rhinitis is defined as the presence of
symptoms for 4 days or more per week and for more than 4 weeks.
Desloratadine is the primary active metabolite of loratadine. Preclinical studies conducted with
desloratadine and loratadine demonstrated that there are no qualitative or quantitative differences
in the toxicity profile of desloratadine and loratadine at comparable levels of exposure to
Desloratadine plasma concentrations can be detected within 30 minutes of desloratadine
administration. Desloratadine is well absorbed with maximum concentration achieved after
approximately 3 hours; the terminal phase half-life is approximately 27 hours. The degree of
accumulation of desloratadine was consistent with its half-life (approximately 27 hours) and a
once daily dosing frequency. The bioavailability of desloratadine was dose proportional over the
range of 5 mg to 20 mg.
The enzyme responsible for the metabolism of desloratadine has not been identified yet, and
therefore some interactions with other drugs can not be fully excluded.In-vivostudies with
specific inhibitors of CYP3A4 and CYP2D6 have shown that these enzymes are not important in
the metabolism of desloratadine. Desloratadine does not inhibit CYP3A4 or CYP2D6 and is
neither a substrate nor an inhibitor of P-glycoprotein.
Desloratadine is moderately bound (83% - 87%) to plasma proteins. There is no evidence of
clinically relevant drug accumulation following once daily dosing of desloratadine (5 mg to 20 mg)
for 14 days.
In a single dose trial using a 7.5-mg dose of desloratadine, there was no effect of food (high-fat,
high caloric breakfast) on the disposition of desloratadine.
In a single dose, crossover trial of desloratadine, the tablet and syrup formulations were
bioequivalent and not affected by the presence of food (high fat, high caloric breakfast).
In another study, grapefruit juice had no effect on the disposition of desloratadine.
In separate single dose studies, at the recommended doses, paediatric patients had comparable
AUC and C
values of desloratadine to those in adults who received a 5 mg dose of
Seasonal Allergic Rhinitis
In adult and adolescent patients with seasonal allergic rhinitis, AERIUS tabletswereeffectivein
relieving symptoms such as sneezing, nasal discharge and itching, congestion/stuffiness, aswellas
ocularitching, tearing and redness, and itching of palate. AERIUS tablets effectively controlled
symptoms for 24 hours.
AERIUS was effective in alleviating the burden of seasonal allergic rhinitis as shown by thetotal
scoreof the rhino-conjunctivitis quality of life questionnaire. The greatest amelioration was seen in
the domains of practical problems and daily activities limited by symptoms.
In two 4-week trials in adults and adolescentswithseasonalallergicrhinitisandconcurrent
asthma, desloratadine was shown to be effective in reducing the symptoms ofseasonalallergic
rhinitis(rhinorrhea, nasal congestion, nasal itching and sneezing, itching/burning eyes,
tearing/watering eyes, redness of eyes, and itching of ears or palate) andasthma(coughing,
wheezing, difficulty breathing), and decreasing beta-agonist use.FEV
was not altered in the
desloratadine or placebo treatment groups.
Chronic Idiopathic Urticaria
In trials conducted in adults and adolescents with chronicidiopathicurticaria,AERIUStabletswere
effective in relieving pruritus and decreasing the size and number of hives as early as 1 dayafter
initiationoftreatment.In each trial, the effects were sustained over the 24hour dosing interval.
Treatment with AERIUS tablets also improved sleep and daytime function, as measured by reduced
interference with sleep and routine daily activities.
Safety of AERIUS Syrup was demonstrated in three paediatric trials. Children aged 6 months-11
years who were candidates for antihistamine therapyreceivedadailydose of AERIUS 1 mg (6 to 11
monthsofage),AERIUS1.25mg(1to5 years of age) or AERIUS 2.5 mg (6to 11 years of age).
Treatment was well tolerated as documented by clinical laboratory tests, vital signsandECG
interval data, including QTc. When given at the recommended doses,theplasmaconcentrationof
desloratadine was comparable in the paediatric andadultpopulations.Althoughtheefficacyof
desloratadine has not been demonstrated in children under the age of2years.thecourseofthe
diseases(seasonalandperennialallergic rhinitis and chronic idiopathic urticaria) and the
pharmacokineticprofileofdesloratadinearesimilar in adults and paediatric patients. Therefore,
desloratadine efficacy data in adults can be extrapolated to the paediatric population.
AERIUS is indicated for the relief of symptoms associated with seasonal and perennial allergic
rhinitis, such as sneezing, nasal discharge and itching, congestion/stuffiness, as well as ocular
itching, tearing and redness, itching of palate and coughing.
AERIUS is also indicated for the relief of symptoms associated with chronicidiopathicurticaria
such as the relief of itching and the size and number of hives.
DOSAGE AND ADMINISTRATION
AERIUS can be taken regardless of mealtime for the relief of symptoms associated with allergic
rhinitis (including intermittent and persistent allergic rhinitis) and chronic idiopathic urticaria.
Intermittent allergic rhinitis (presence of symptoms for less than 4 days per week or for less than
4 weeks) should be managed in accordance with the evaluation of the patient’s disease history
and the treatment should be discontinued after symptoms are resolved and reinitiated upon their
reappearance. In persistent allergic rhinitis (presence of symptoms for 4 days or more per week
and for more than 4 weeks), continued treatment may be proposed to the patients during allergen
Adults and adolescents 12 years and over: One AERIUS 5mg film-coated tablet or 10 mL (5 mg)
AERIUS Syrup once daily.
Children 6 to 11 years of age: 5 mL (2.5 mg) AERIUS Syrup once daily.
Children 2 to 5 years of age: 2.5 mL (1.25 mg) AERIUS Syrup once daily.
Children 6 to 11 months of age: 2 mL (1 mg) of AERIUS Syrup once daily.
AERIUS tablets and syrup are contraindicatedinpatients who have shown hypersensitivity or
idiosyncrasy to desloratadine, to any of the excipients or to loratadine.
Efficacy and safety of AERIUS in childrenunder 6 months of age have not been established.
Although AERIUS is unlikely to affect the ability to drive or operate machinery, a few people may
be affected and care should be taken.
Use in Pregnancy (Category B1)
The safe use of desloratadine during pregnancy has not beenestablished.Therefore,AERIUSis
not to be used during pregnancy unless clearly indicated.
No overall effect on rat fertility was observed with desloratadine at an exposure that was 34 times
higher than the exposure in humans at the recommended clinical dose.
No teratogenic or mutagenic effects were observed in animal trials with desloratadine.
Use in Lactation
Desloratadinepassesintobreastmilk.Hence,the use of AERIUS by breastfeeding mothers is not
Carcinogenicity and Mutagenicity
Desloratadine has no carcinogenic risk in man based on the available data with loratadine.
Desloratadine showed no mutagenic effects inin vitroandin vivomutagenicity studies.
No clinically relevant interactions with AERIUS were observed in clinical trials (see
AERIUS taken concomitantly with alcohol did not potentiate the performance impairing effects of
There was no effect of food or grapefruit juice on the disposition of desloratadine.
AERIUS should be discontinued approximately 48 hours prior to skintestingproceduressince
antihistamines may prevent or diminish otherwise positive reactions to dermal reactivity indicators.
In clinical trials in a paediatric population, AERIUS Syrup was administered to a total of 246
children aged 6 months to 11 years. The overall incidence of adverse events in children 2 to 11
years of age was similar for AERIUS syrup and placebo groups. In infants and toddlers aged 6 to
23 months, the most frequent adverse events reported in excess of placebo were diarrhoea
(3.7%), fever (2.3%) and insomnia (2.3%).
In clinical trials in a range of indications including seasonal allergic rhinitis and chronic idiopathic
urticaria, at the recommended dose of 5 mg daily, undesirable effects with AERIUS Tablets were
reported in 3% of patients in excess of those treated with placebo. The most frequent adverse
events reported in excess of placebo were fatigue (1.2%), dry mouth (0.8%), and headache
No effects on the ability to drive and use machines have been observed with the use of
Very rare cases of hypersensitivity reactions (including anaphylaxis and rash), psychomotor
hyperactivity and seizures have been reported during the marketing of desloratadine.
In addition, cases of tachycardia, palpitations, elevations of liver enzymes, hepatitis, and
increased bilirubin have been reported veryrarely.
In clinical trials in a paediatric population, AERIUS syrup was administered to 115 children ages 2
through 11 years. The overall incidence of adverseevents was similar for the AERIUS Syrup and
the placebo groups.
In the event of overdose, consider standard measures to remove unabsorbed active substance.
Symptomatic and supportive treatment is recommended.
Based on a multiple dose clinical trial in adults and adolescents, in which up to 45 mg of
desloratadine was administered (9 times the clinical dose), no clinically relevant effects were
Desloratadine is not eliminated by haemodialysis; itis not known if it is eliminated by peritoneal
Tablets: The shelf-life is 24 months when stored below 25 °C. Protect from moisture.
Syrup: The shelf-life is 24 months when stored below 30 °C. Store in original container.
PRESENTATIONAND PACKAGE QUANTITIES
Tablets: 5 mg, light blue round embossed film coated- 10s, 30s
Syrup: 0.5 mg/mL, clear orange coloured solution - 100 mL and 200 mL
NAME AND ADDRESS
Schering-Plough a division of Schering-Plough Animal Health Limited
36 Kitchener Street
Telephone: 09 375 9210
DATE OF PREPARATION
8 May 2008