ODESTA

Desloratadine is a second generation, tricyclic antihistamine that which has a selective and peripheral H1-antagonist action.

It is the active descarboethoxy metabolite of loratidine (a second generation histamine).

Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.

For the relief of symptoms of seasonal allergic rhinitis, perennial (non-seasonal) allergic rhinitis.

Desloratidine is also used for the sympomatic treatment of pruritus and urticaria (hives) associated with chronic idiopathic urticaria.

Desloratadine is a long-acting second-generation

H 1 -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, such as the 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 allergies.

Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine.

Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness.

Desloratadine administered

Oral for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean T max of approximately 3 hours, a mean steady-state C max of 4 ng/ml, and a mean steady-state AUC of 56.9 ng*hr/ml.

Food was found not to affect desloratadine absorption.

Desloratadine is metabolized to the active metabolite 3-hydroxydesloratadine, which is subsequently glucuronidated.

Approximately 87% of a 14 C-desloratadine dose was equally recovered in urine and feces as metabolic products.

Desloratadine has a mean plasma elimination half-life of approximately 27 hours.

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Information regarding desloratadine overdose is limited, although somnolence has been reported.

In case of overdose, symptomatic and supportive treatment, including removing the unabsorbed drug, is recommended; note, however, that desloratadine and its active metabolite 3-hydroxydesloratadine cannot be eliminated by hemodialysis.

In animal studies, lethality was observed at or above doses of 250 mg/kg in rats and of 353 mg/kg in mice (oral LD 50 ), doses that represent and 290 times the human exposure based on the recommended daily oral dose.

In monkey, no deaths occurred at doses up to 250 mg/kg, representing an exposure roughly 810 times that of the recommended dose in humans.

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

Tablets may be taken without regard to meals.

Dosage (by age): Adults and Adolescents 12 Years of Age and Over:

• one 5 mg tablet once daily 2.1 Adults and Adolescents 12 Years of Age and Over The recommended dose of Desloratadine Tablets is one 5-mg tablet once daily. 2.5 Adults with Hepatic or Renal Impairment In adult patients with liver or renal impairment, a starting dose of one 5 mg tablet every other day is recommended based on pharmacokinetic data.

Dosing recommendation for children with liver or renal impairment cannot be made due to lack of data.

Debossed "5", light blue, round tablets that are packaged in high-density polyethylene plastic bottles of 100 (NDC 69543-107-10) and 500 (NDC 69543-107-50).

• Desloratadine Tablets: Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) .

Heat sensitive.

Avoid exposure at or above 30°C (86°F).

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

• Desloratadine Tablets: Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) .

Heat sensitive.

Avoid exposure at or above 30°C (86°F).

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Risk Summary The limited available data with Desloratadine in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage.

There are no adequate and well-controlled studies in pregnant women.

Desloratadine given during organogenesis to pregnant rats was not teratogenic at the summed area under the concentration-time curve (AUC)-based exposures of desloratadine and its metabolite approximately 320 times that at the recommended human daily oral dose (RHD) of 5 mg/day. Desloratadine given during organogenesis to pregnant rabbits was not teratogenic at the AUC-based exposures of desloratadine approximately 230 times that at the RHD.

Desloratadine given to pregnant rats during organogenesis through lactation resulted in reduced body weight and slow righting reflex of F 1 pups at the summed AUC-based exposures of desloratadine and its metabolite approximately 70 times or greater than that at the RHD.

The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown.

In the

U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Desloratadine was given orally during organogenesis to pregnant rats at doses of and 48 mg/kg/day (approximately and 320 times the summed AUC-based exposure of desloratadine and its metabolite at the RHD).

No fetal malformations were present.

Reduced fetal weights and skeletal variations noted at doses of and 48 mg/kg/day were likely secondary to the maternal toxicities of reduced body weight gain and food consumption observed at the same doses.

Desloratadine was also given orally during organogenesis to pregnant rabbits at doses of and 60 mg/kg/day (approximately and 230 times the AUC-based exposure of desloratadine at the RHD).

No adverse effects to the fetus were noted.

Reduced maternal body weight gain was noted in rabbits at 60 mg/kg/day. In a peri.

• and post-natal development study, desloratadine was given to rats orally during the perinatal (Gestation Day 6) through lactation periods (Postpartum Day 21) at doses of and 18 mg/kg/day. Reduced body weight and slow righting reflex were reported in F 1 pups at doses of 9 mg/kg/day or greater (approximately 70 times or greater than the summed AUC-based exposure of desloratadine and its metabolite at the RHD).

Desloratadine had no effect on

F 1 pup development at 3 mg/kg/day (approximately 10 times the summed AUC-based exposure of desloratadine and its metabolite at the RHD).

Maternal toxicities including reduced body weight gain and food consumption were noted at 18 mg/kg/day for F 0 dams.

F 1 offspring were subsequently mated and there was no developmental toxicity for F 2 pups observed.

The recommended dose of Desloratadine Oral

Solution in the pediatric population is based on cross-study comparison of the plasma concentration of Desloratadine in adults and pediatric subjects.

The safety of Desloratadine Oral

Solution has been established in 246 pediatric subjects aged 6 months to 11 years in three placebo-controlled clinical studies.

Since the course of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria and the effects of Desloratadine are sufficiently similar in the pediatric and adult populations, it allows extrapolation from the adult efficacy data to pediatric patients.

The effectiveness of Desloratadine Oral

Solution in these age groups is supported by evidence from adequate and well-controlled studies of Desloratadine Tablets in adults.

The safety and effectiveness of Desloratadine Tablets or Desloratadine Oral Solution have not been demonstrated in pediatric patients less than 6 months of age.

Clinical studies of desloratadine did not include sufficient numbers of subjects aged and over to determine whether they respond differently from younger subjects.

Other reported clinical experience has not identified differences between the elderly and younger patients.

In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.