DESCRIPTION: Each AERIUS Tablet contains 5.0 mg
of desloratadine. AERIUS Tablet is a light blue round
tablet, embossed with elongated letters 'S' and 'P' on
one side and plain on the other.
Inactive Ingredients: dibasic calcium phosphate
dihydrate, microcrystalline cellulose, corn starch, talc,
Dye Opadry II Blue, Dye Opadry Clear, carnauba wax,
white wax and purified water.
ACTIONS: Desloratadine is a non-sedating long-acting
histamine antagonist with potent, selective peripheral
H1-receptor antagonist activity. Desloratadine has
demonstrated antiallergic, antihistaminic,
and anti-inflammatory activity.
PRECLINICAL TOXICOLOGY: 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.
Preclinical data with desloratadine reveal no special
hazard for humans based on conventional studies
of safety pharmacology, repeated dose toxicity,
genotoxicity, and toxicity to reproduction. The lack of
carcinogenic potential was demonstrated in studies
conducted with loratadine.
Pharmacodynamic Properties: After oral administration,
desloratadine selectively blocks peripheral
histamine H1-receptors because the drug is effectively
excluded from entry to the central nervous
In addition to antihistaminic activity, desloratadine
has demonstrated antiallergic and anti-inflammatory
activity from numerous in vitro (mainly conducted
on cells of human origin) and in 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 including
IL-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
• eosinophil adhesion and chemotaxis,
• the expression of the adhesion molecules such as
• 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 pharmacologic 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 5 mg daily,
there was no excess incidence of somnolence as
compared to placebo. AERIUS even at a dose of
7.5 mg daily did not affect psychomotor performance
in clinical trials. 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.
No clinically relevant changes in desloratadine plasma
concentrations were observed in multiple-dose
ketoconazole, erythromycin, azithromycin, fluoxetine
and cimetidine interaction trials.
In clinical pharmacologic 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.
In adult and adolescent patients with allergic rhinitis
(AR), AERIUS tablets were effective in relieving
symptoms such as sneezing, nasal discharge and
itching, congestion/stuffiness, as well as ocular itching,
tearing and redness, and itching of palate. AERIUS
tablets effectively controlled symptoms for
In two 4-week trials in patients with seasonal allergic
rhinitis (SAR) and concurrent asthma, desloratadine
was shown to be effective in reducing the symptoms of
SAR (rhinorrhea, nasal congestion, nasal itching and
sneezing, itching/burning eyes, tearing/watering eyes,
redness of eyes, and itching of ears or palate) and
asthma (coughing, wheezing, difficulty breathing), and
decreasing beta-agonist use. FEV1 was not altered in
the desloratadine or placebo treatment groups.
In trials conducted in adults and adolescents with
chronic idiopathic urticaria (CIU), AERIUS tablets were
effective in relieving pruritus and decreasing the size
and number of hives as early as 1 day after initiation of
treatment. In each trial, the effects were sustained over
the 24 hour dosing interval. Treatment with AERIUS
tablets also improved sleep and daytime function, as
measured by reduced interference with sleep and
routine daily activities.
AERIUS was effective in alleviating the burden of
seasonal allergic rhinitis as shown by the total score
of the rhino-conjunctivitis quality of life questionnaire.
The greatest amelioration was seen in the domains
of practical problems and daily activities limited by
Pharmacokinetic Properties: 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. In adults and
adolescents, the bioavailability of desloratadine was dose proportional over
the range of 5 mg to 20 mg.
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.
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 vivo studies 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.
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 another study, grapefruit juice had no effect on the
disposition of desloratadine.
INDICATIONS AND USAGE: AERIUS Tablets are indicated for the rapid
relief of symptoms associated with allergic rhinitis, such as sneezing,
nasal discharge and itching, congestion/stuffiness, as well as ocular
itching, tearing and redness.
AERIUS Tablets are also indicated for the relief of symptoms associated with
chronic idiopathic urticaria such as the relief of itching and the size and
number of hives.
DOSAGE AND ADMINISTRATION: Adults and Adolescents (12 years of age
and older): One AERIUS 5 mg film-coated tablet once a day regardless of
mealtime. For oral use.
DRUG INTERACTIONS: No clinically relevant interactions with AERIUS
were observed in clinical trials (see section on Pharmacodynamic
properties). There was no effect of food or grapefruit juice on the
disposition of desloratadine. AERIUS taken concomitantly with alcohol did
not potentiate the performance impairing effects of alcohol (see section on
ADVERSE EFFECTS: In clinical trials in a range of indications
including AR and CIU, 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
Very rare cases of hypersensitivity reactions, including anaphylaxis and
rash, have been reported during the marketing of desloratadine. In addition,
cases of tachycardia, palpitations, psychomotor hyperactivity, somnolence,
seizures, elevations of liver enzymes, hepatitis, and increased bilirubin
have been reported very rarely.
CONTRAINDICATIONS: Hypersensitivity to the active substance or to any
of the excipients.
PRECAUTIONS: Efficacy and safety of AERIUS Tablets in children under
12 years of age have not been established.
Effects on ability to drive and use machines: No effects on the
ability to drive and use machines have been observed (see Pharmacodynamic
USAGE DURING PREGNANCY AND LACTATION: 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 (see PRECLINICAL TOXICOLOGY). Since no clinical data on
exposed pregnancies are available with desloratadine, the safe use of AERIUS
during pregnancy has not been established. AERIUS is not to be used during
pregnancy unless the potential benefits outweigh the risks.
Desloratadine is excreted into breast milk; therefore the use of AERIUS is
not recommended in breast-feeding women.
OVERDOSAGE INFORMATION: In the event of overdose, consider standard
measures to remove nonadsorped 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 observed.
Desloratadine is not eliminated by hemodialysis; it is not known if it is
eliminated by peritoneal dialysis.
HOW SUPPLIED: AERIUS Tablets: In blister packs of 10's, 10 X 10's and
50 X 10's.
STORAGE: Store below 30 °C. Store in the original container.
Protect AERIUS Tablets from excessive moisture.
Keep out of reach of children.