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Aerius

Aerius - General Information

Aerius is a tricyclic antihistamine, which has a selective and peripheral H1-antagonist action. It is used to treat allergies. It has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.

 

Pharmacology of Aerius

Aerius is a long-lasting antihistamine. Aerius is a second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, for example, swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergy. Aerius blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Aerius does not enter the brain from the blood and, therefore, does not cause drowsiness.

 

Aerius for patients

 

Aerius Interactions

In two controlled crossover clinical pharmacology studies in healthy male (n=12 in each study) a nd female (n=12 in each study) volunteers, desloratadine 7.5 mg (1.5 times the daily dose) once daily was coadministered with erythromycin 500 mg every 8 hours or ketoconazole 200 mg every 12 hours for 10 days. In three separate controlled, parallel group clinical pharmacology studies, desloratadine at the clinical dose of 5 mg has been coadministered with azithromycin 500 mg followed by 250 mg once daily for 4 days (n=18) or with fluoxetine 20 mg once daily for 7 days after a 23 day pretreatment period with fluoxetine (n=18) or with cimetidine 600 mg every 12 hours for 14 days (n=18) under steady state conditions to normal healthy male and female volunteers. Although increased plasma concentrations (C max and AUC 0-24 hrs) of desloratadine and 3-hydroxydesloratadine were observed, there were no clinically relevant changes in the safety profile of desloratadine, as assessed by electrocardiographic parameters (including the corrected QT interval), clinical laboratory tests, vital signs, and adverse events.

Table 1
Changes in Desloratadine and 3-Hydroxydesloratadine Pharmacokinetics in Healthy Male and Female Volunteers
Desloratadine 3-Hydroxydesloratadine
C max AUC
0-24 hrs
C max AUC
0-24 hrs
Erythromycin
(500 mg Q8h)
+24% +14% +43% +40%
Ketoconazole
(200 mg Q12h)
+45% +39% +43% +72%
Azithromycin
(500 mg day 1,
250 mg QD × 4 days)
+15% +5% +15% +4%
Fluoxetine
(20 mg QD)
+15% +0% +17% +13%
Cimetidine
(600 mg Q12h)
+12% +19% -11%  -3%

 

Aerius Contraindications

CLARINEX Tablets 5 mg are contraindicated in patients who are hypersensitive to this medication or to any of its ingredients, or to loratadine.

 

Additional information about Aerius

Aerius Indication: For the relief of symptoms of seasonal allergic rhinitis, pruritus, reduction in the number of hives in patients with chronic idiopathic urticaria.
Mechanism Of Action: Like other H1-blockers, Aerius competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Drug Interactions: Not Available
Food Interactions: Take without regard to meals.
Generic Name: Desloratadine
Synonyms: Desloratidine; Descarboethoxyoratidine; Descarboethoxyloratadine
Drug Category: Antihistamines
Drug Type: Small Molecule; Approved
Other Brand Names containing Desloratadine: Aerius; Clarinex Reditabs; NeoClarityn; Claramax; Clarinex;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: 82-87%
Biotransformation: Not Available
Half Life: 50 hours
Dosage Forms of Aerius: Tablet Oral
Syrup Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C19H19ClN2
Desloratadine on Wikipedia: http://en.wikipedia.org/wiki/Desloratadine
Organisms Affected: Humans and other mammals