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Desloratadine Orally Disintegrating Tablets | Desloratadine

05:56 EDT 27th August 2014 | BioPortfolio
Note: While we endeavour to keep our records up-to-date one should not rely on these details being accurate without first consulting a professional. Click here to read our full medical disclaimer.

Desloratadine orally disintegrating tablets contain either 2.5 mg or 5 mg of desloratadine, an antihistamine, to be administered orally. Each tablet also contains the following inactive ingredients: anhydrous citric acid, aspartame, colloidal silicon dioxide, crospovidone, ferric oxide, mannitol, lactose anhydrous, microcrystalline cellulose, polacrilex resin, sodium stearyl fumarate, talc, tutti frutti flavor. 

Desloratadine is a white to off-white powder that is soluble in dichloromethane. It has an molecular formula: CHClN and a molecular weight of 310.8. The chemical name is 8-chloro-6,11-dihydro-11-(4-piperdinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine and has the following structure :

Desloratadine is a long-acting tricyclic histamine antagonist with selective H-receptor histamine antagonist activity. Receptor binding data indicates that at a concentration of 2 to 3 ng/mL (7 nanomolar), desloratadine shows significant interaction with the human histamine H-receptor. Desloratadine inhibited histamine release from human mast cells in vitro.

Results of a radiolabeled tissue distribution study in rats and a radioligand H-receptor binding study in guinea pigs showed that desloratadine did not readily cross the blood brain barrier.

Absorption: Following oral administration of desloratadine 5 mg once daily for 10 days to normal healthy volunteers, the mean time to maximum plasma concentrations (T) occurred at approximately 3 hours post dose and mean steady state peak plasma concentrations (C) and area under the concentration-time curve (AUC) of 4 ng/mL and 56.9 ng·hr/mL were observed, respectively. Neither food nor grapefruit juice had an effect on the bioavailability (C and AUC) of desloratadine.

Water had no effect on the bioavailability (AUC and C) of desloratadine orally disintegrating tablets.

Distribution:Desloratadine and 3-hydroxydesloratadine are approximately 82% to 87% and 85% to 89%, bound to plasma proteins, respectively. Protein binding of desloratadine and 3-hydroxydesloratadine was unaltered in subjects with impaired renal function.

Metabolism:Desloratadine (a major metabolite of loratadine) is extensively metabolized to 3-hydroxydesloratadine, an active metabolite, which is subsequently glucuronidated. The enzyme(s) responsible for the formation of 3- hydroxydesloratadine have not been identified. Data from clinical trials indicate that a subset of the general population has a decreased ability to form 3-hydroxydesloratadine, and are poor metabolizers of desloratadine. In pharmacokinetic studies (n= 3,748), approximately 6% of subjects were poor metabolizers of desloratadine (defined as a subject with an AUC ratio of 3-hydroxydesloratadine to desloratadine less than 0.1, or a subject with a desloratadine half-life exceeding 50 hours). These pharmacokinetic studies included subjects between the ages of 2 and 70 years, including 977 subjects aged 2 to 5 years, 1,575 subjects aged 6 to 11 years, and 1,196 subjects aged 12 to 70 years. There was no difference in the prevalence of poor metabolizers across age groups. The frequency of poor metabolizers was higher in Blacks (17%, n=988) as compared to Caucasians (2%, n=1,462) and Hispanics (2%, n=1,063). The median exposure (AUC) to desloratadine in the poor metabolizers was approximately 6-fold greater than in the subjects who are not poor metabolizers. Subjects who are poor metabolizers of desloratadine cannot be prospectively identified and will be exposed to higher levels of desloratadine following dosing with the recommended dose of desloratadine. Although not seen in these studies, an increased risk of exposure-related adverse events in patients who are poor metabolizers cannot be ruled out.

Elimination:The mean elimination half-life of desloratadine was 27 hours. Cand AUC values increased in a dose proportional manner following single oral doses between 5 and 20 mg. The degree of accumulation after 14 days of dosing was consistent with the half-life and dosing frequency. A human mass balance study documented a recovery of approximately 87% of the C-desloratadine dose, which was equally distributed in urine and feces as metabolic products. Analysis of plasma 3-hydroxydesloratadine showed similar Tand half-life values compared to desloratadine.

Geriatric: In older subjects (≥ 65 years old; n=17) following multiple-dose administration of desloratadine tablets, the mean Cmax and AUC values for desloratadine were 20% greater than in younger subjects (<65 years old). The oral total body clearance (CL/F) when normalized for body weight was similar between the two age groups.The mean plasma elimination half-life of desloratadine was 33.7 hr in subjects ≥ 65 years old. The pharmacokinetics for 3-hydroxydesloratadine appeared unchanged in older versus younger subjects. These age-related differences are unlikely to be clinically relevant and no dosage adjustment is recommended in elderly subjects.

Pediatric Subjects: In subjects 6 to 11 years old, a single dose of 5 mL of desloratadine syrup containing 2.5 mg of desloratadine, resulted in desloratadine plasma concentrations similar to those achieved in adults administered a single 5 mg desloratadine tablet. In subjects 2 to 5 years old, a single dose of 2.5 mL of desloratadine syrup containing 1.25 mg of desloratadine, resulted in desloratadine plasma concentrations similar to those achieved in adults administered a single  5 mg desloratadine tablet. However, the C and AUCof the metabolite (3-OH desloratadine) were 1.27 and 1.61 times higher for the 5 mg dose of syrup administered in adults compared to the C and AUC obtained in children 2 to 11 years of age receiving 1.25 to 2.5 mg of desloratidine syrup.

A single dose of either 2.5 mL or 1.25 mL of desloratadine syrup containing 1.25 mg or 0.625 mg, respectively, of desloratadine was administered to subjects 6 to 11 months of age and 12 to 23 months of age. The results of a population pharmacokinetic analysis indicated that a dose of 1 mg for subjects aged 6 to 11 months and 1.25 mg for subjects 12 to 23 months of age is required to obtain desloratadine plasma concentrations similar to those achieved in adults administered a single 5 mg dose of desloratadine syrup.

The 2.5 mg desloratadine orally disintegrating tablet has not been evaluated in pediatric patients. In conjunction with the dose finding studies in pediatrics described, the pharmacokinetic data for desloratadine orally disintegrating tablets supports the use of the 2.5 mg dose strength in pediatric patients 6 to 11 years of age.

Renally Impaired: DESLORATADINE pharmacokinetics following a single dose of 7.5 mg were characterized in patients with mild (n=7; creatinine clearance 51 to 69 mL/min/1.73 m), moderate (n=6; creatinine clearance 34 to 43 mL/min/1.73 m), and severe (n=6; creatinine clearance 5 to 29 mL/min/1.73 m) renal impairment or hemodialysis dependent (n=6) patients. In patients with mild and moderate renal impairment, median C and AUC values increased by approximately 1.2- and 1.9-fold, respectively, relative to subjects with normal renal function. In patients with severe renal impairment or who were hemodialysis dependent, C and AUC values increased by approximately 1.7- and 2.5-fold, respectively. Minimal changes in 3-hydroxydesloratadine concentrations were observed. Desloratadine and 3-hydroxydesloratadine were poorly removed by hemodialysis. Plasma protein binding of desloratadine and 3-hydroxydesloratadine was unaltered by renal impairment. Dosage adjustment for patients with renal impairment is recommended (see DOSAGE AND ADMINISTRATION).

Hepatically Impaired:Desloratadine pharmacokinetics were characterized following a single oral dose in patients with mild (n=4), moderate (n=4), and severe (n=4) hepatic impairment as defined by the Child-Pugh classification of hepatic function and eight subjects with normal hepatic function. Patients with hepatic impairment, regardless of severity, had approximately a 2.4-fold increase in AUC as compared with normal subjects. The apparent oral clearance of desloratadine in patients with mild, moderate, and severe hepatic impairment was 37%, 36%, and 28% of that in normal subjects, respectively. An increase in the mean elimination half-life of desloratadine in patients with hepatic impairment was observed. For 3-hydroxydesloratadine, the mean C and AUC values for patients with hepatic impairment were not statistically significantly different from subjects with normal hepatic function. Dosage adjustment for patients with hepatic impairment is recommended (see DOSAGE AND ADMINISTRATION).

Female subjects treated for 14 days with desloratadine tablets had 10% and 3% higher desloratadine C and AUC values, respectively, compared with male subjects. The 3-hydroxydesloratadine Cand AUC values were also increased by 45% and 48%, respectively, in females compared with males. However, these apparent differences are not likely to be clinically relevant and therefore no dosage adjustment is recommended.

Following 14 days of treatment with desloratadine tablets, the C and AUC values for desloratadine were 18% and 32% higher, respectively, in Blacks compared with Caucasians. For 3-hydroxydesloratadine there was a corresponding 10% reduction in Cmax and AUC values in Blacks compared to Caucasians. These differences are not likely to be clinically relevant and therefore no dose adjustment is recommended.

In two controlled crossover clinical pharmacology studies in healthy male (n=12 in each study) and 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 (Cand AUC) of desloratadine and 3-hydroxydesloratadine were observed (see Table 1), 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

                                                  Desloratadine    3-Hydroxydesloratadine
                                                    Cmax                 AUC 0-24 hrs    Cmax               AUC 0-24 hrs
                                                                                                      
Erythromycin + 24% +14% + 43% + 40%
  (500 mg Q8h)        
Ketoconazole + 45% + 39% + 43% + 72%
  (200 mg Q12h)        
Azithromycin + 15% + 5% + 15% + 4%
  (500 mg day        
  1, 250 mg QD x 4 days)        
Fluoxetine + 15% + 0% + 17% + 13%
  (20 mg QD)        
Cimetidine + 12% + 19% - 11% - 3%
  (600 mg Q12h)        

Wheal and Flare:Human histamine skin wheal studies following single and repeated 5 mg doses of desloratadine have shown that the drug exhibits an antihistaminic effect by one hour; this activity may persist for as long as 24 hours. There was no evidence of histamine-induced skin wheal tachyphylaxis within the desloratadine 5 mg group over the 28 day treatment period. The clinical relevance of histamine wheal skin testing is unknown.

Effects on QT:Single dose administration of desloratadine did not alter the corrected QT interval (QT) in rats (up to 12 mg/kg, oral), or guinea pigs (25 mg/kg, intravenous). Repeated oral administration at doses up to 24 mg/kg for durations up to 3 months in monkeys did not alter the QT at an estimated desloratadine exposure (AUC) that was approximately 955 times the mean AUC in humans at the recommended daily oral dose. See OVERDOSAGE section for information on human QT experience.

Seasonal Allergic Rhinitis:The clinical efficacy and safety of desloratadine tablets were evaluated in over 2,300 patients 12 to 75 years of age with seasonal allergic rhinitis. A total of 1,838 patients received 2.5 to 20 mg/day of desloratadine in four double-blind, randomized, placebo-controlled clinical trials of 2 to 4 weeks duration conducted in the United States. The results of these studies demonstrated the efficacy and safety of desloratadine 5 mg in the treatment of adult and adolescent patients with seasonal allergic rhinitis. In a dose ranging trial, desloratadine 2.5 to 20 mg/day was studied. Doses of 5, 7.5, 10, and 20 mg/day were superior to placebo; and no additional benefit was seen at doses above 5 mg. In the same study, an increase in the incidence of somnolence was observed at doses of 10 mg/day and 20 mg/day (5.2% and 7.6%, respectively), compared to placebo (2.3 %).

In two 4 week studies of 924 patients (aged 15 to 75 years) with seasonal allergic rhinitis and concomitant asthma, desloratadine tablets 5 mg once daily improved rhinitis symptoms, with no decrease in pulmonary function. This supports the safety of administering desloratadine tablets to adult patients with seasonal allergic rhinitis with mild to moderate asthma.

Desloratadine tablets 5 mg once daily significantly reduced the Total Symptom Scores (the sum of individual scores of nasal and non-nasal symptoms) in patients with seasonal allergic rhinitis. See Table 2.

Table 2

TOTAL SYMPTOM SCORE (TSS)

Changes in a 2 Week Clinical

Trial in Patients with Seasonal Allergic Rhinitis

There were no significant differences in the effectiveness of desloratadine tablets 5 mg across subgroups of patients defined by gender, age, or race.

Perennial Allergic Rhinitis:The clinical efficacy and safety of desloratadine tablets 5 mg were evaluated in over 1,300 patients 12 to 80 years of age with perennial allergic rhinitis. A total of 685 patients received 5 mg/day of desloratadine in two double blind, randomized, placebo controlled clinical trials of 4 weeks duration conducted in the United States and internationally. In one of these studies desloratadine tablets 5 mg once daily was shown to significantly reduce symptoms of perennial allergic rhinitis (Table 3).

Table 3

TOTAL SYMPTOM SCORE (TSS)

Changes in a 4 Week Clinical

Trial in Patients with Perennial Allergic Rhinitis

Treatment Group (n) Mean Baseline* (sem) Change from Baseline** (sem) Placebo Comparison (P- value)
Desloratadine 14.2 (0.3) -4.3 (0.3) P<0.01
5 mg (171)        
Placebo (173) 13.7 (0.3) -2.5 (0.3)  
*At baseline, a total nasal symptom score (sum of 4 individual symptoms) of at least 6 and a total non-nasal symptom score (sum of 4 individual symptoms) of at least 5 (each symptom scored 0 to 3 where 0=no symptom and 3=severe symptoms) was required for trial eligibility. TSS ranges from 0=no symptoms to 24=maximal symptoms.  
**Mean reduction in TSS averaged over the 2 week treatment period.
   
Treatment Group(n) Mean Baseline*  (sem) Change from Baseline**(sem) Placebo Comparison (P- value)
Desloratadine 12.37 (0.18) -4.06 (0.21) P=0.01
5 mg (337)        
Placebo (337) 12.30 (0.18) -3.27 (0.21)  
*At baseline, average of total symptom score (sum of 5 individual nasal symptoms and 3 non-nasal symptoms, each symptom scored 0 to 3 where 0=no symptom and 3=severe symptoms) of at least 10 was required for trial eligibility. TSS ranges from 0=no symptoms to 24=maximal symptoms.  
**Mean reduction in TSS averaged over the 4-week treatment period.

Seasonal Allergic Rhinitis: Desloratadine orally disintegrating tablets are indicated for the relief of the nasal and non-nasal symptoms of seasonal allergic rhinitis in patients 6 years of age and older. 

Perennial Allergic Rhinitis: Desloratadine orally disintegrating tablets are indicated for the relief of the nasal and non-nasal symptoms of perennial allergic rhinitis in patients 6 years of age and older.

Desloratadine orally disintegrating tablets are contraindicated in patients who are hypersensitive to this medication or to any of its ingredients, or to loratadine.

The carcinogenic potential of desloratadine was assessed using a loratadine study in rats and a desloratadine study in mice. In a 2 year study in rats, loratadine was  administered in the diet at doses up to 25 mg/kg/day (estimated desloratadine and desloratadine metabolite exposures were approximately 30 times the AUC in humans at the recommended daily oral dose). A significantly higher incidence of hepatocellular tumors (combined adenomas and carcinomas) was observed in males given 10 mg/kg/day of loratadine and in males and females given 25 mg/kg/day of loratadine. The estimated desloratadine and desloratadine metabolite exposures in rats given 10 mg/kg of loratadine were approximately 7 times the AUC in humans at the recommended daily oral dose. The clinical significance of these findings during long-term use of desloratadine is not known.

In a 2 year dietary study in mice, males and females given up to 16 mg/kg/day and 32 mg/kg/day desloratadine, respectively, did not show significant increases in the incidence of any tumors. The estimated desloratadine and metabolite exposures in mice at these doses were 12 and 27 times, respectively, the AUC in humans at the recommended daily oral dose.

In genotoxicity studies with desloratadine, there was no evidence of genotoxic potential in a reverse mutation assay (Salmonella/E. coli mammalian microsome bacterial mutagenicity assay) or in two assays for chromosomal aberrations (human peripheral blood lymphocyte clastogenicity assay and mouse bone marrow micronucleus assay).

There was no effect on female fertility in rats at desloratadine doses up to 24 mg/kg/day (estimated desloratadine and desloratadine metabolite exposures were approximately 130 times the AUC in humans at the recommended daily oral dose). A male specific decrease in fertility, demonstrated by reduced female conception rates, decreased sperm numbers and motility, and histopathologic testicular changes, occurred at an oral desloratadine dose of 12 mg/kg in rats (estimated desloratadine exposures were approximately 45 times the AUC in humans at the recommended daily oral dose).Desloratadine had no effect on fertility in rats at an oral dose of 3 mg/kg/day (estimated desloratadine and desloratadine metabolite exposures were approximately 8 times the AUC in humans at the recommended daily oral dose).

Desloratadine was not teratogenic in rats at doses up to 48 mg/kg/day (estimated desloratadine and desloratadine metabolite exposures were approximately 210 times the AUC in humans at the recommended daily oral dose) or in rabbits at doses up to 60 mg/kg/day (estimated desloratadine exposures were approximately 230 times the AUC in humans at the recommended daily oral dose). In a separate study, an increase in pre-implantation loss and a decreased number of implantations and fetuses were noted in female rats at 24 mg/kg (estimated desloratadine and desloratadine metabolite exposures were approximately 120 times the AUC in humans at the recommended daily oral dose). Reduced body weight and slow righting reflex were reported in pups at doses of 9 mg/kg/day or greater (estimated desloratadine and desloratadine metabolite exposures were approximately 50 times or greater than the AUC in humans at the recommended daily oral dose). Desloratadine had no effect on pup development at an oral dose of 3 mg/kg/day (estimated desloratadine and desloratadine metabolite exposures were approximately 7 times the AUC in humans at the recommended daily oral dose). There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, desloratadine should be used during pregnancy only if clearly needed.

Desloratadine passes into breast milk, therefore a decision should be made whether to discontinue nursing or to discontinue desloratadine, taking into account the importance of the drug to the mother.

The 2.5 mg desloratadine orally disintegrating tablet has not been evaluated in pediatric patients. In conjunction with the dose finding studies in pediatrics described, the pharmacokinetic data for desloratadine orally disintegrating tablets supports the use of the 2.5 mg dose strength in pediatric patients 6 to 11 years of age.

Clinical studies of desloratadine did not include sufficient numbers of subjects aged 65 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. (see CLINICAL PHARMACOLOGY- Special Populations).

Patients should be instructed to use desloratadine tablets as directed. As there are no food effects on bioavailability, patients can be instructed that desloratadine orally disintegrating tablets may be taken without regard to meals. Patients should be advised not to increase the dose or dosing frequency as studies have not demonstrated increased effectiveness at higher doses and somnolence may occur.

Phenylketonurics: Desloratadine orally disintegrating tablets contain phenylalanine 2.55 mg per 5 mg desloratadine orally disintegrating tablet or 1.28 mg per 2.5 mg desloratadine orally disintegrating tablet.

Allergic Rhinitis:In multiple-dose placebo-controlled trials, 2,834 patients ages 12 years or older received desloratadine tablets at doses of 2.5 mg to 20 mg daily, of whom 1,655 patients received the recommended daily dose of 5 mg. In patients receiving 5 mg daily, the rate of adverse events was similar between desloratadine and placebo-treated patients. The percent of patients who withdrew prematurely due to adverse events was 2.4% in the desloratadine group and 2.6% in the placebo group. There were no serious adverse events in these trials in patients receiving desloratadine. All adverse events that were reported by greater than or equal to 2% of patients who received the recommended daily dose of desloratadine tablets (5 mg once-daily), and that were more common with desloratadine tablets than placebo, are listed in Table 4.

Table 4

Incidence of Adverse Events Reported by 2% or More of Adult and Adolescent  Allergic Rhinitis Patients in Placebo-Controlled, Multiple-Dose Clinical Trials with the Tablet Formulation of Desloratadine

The frequency and magnitude of laboratory and electrocardiographic abnormalities were similar in desloratadine and placebo-treated patients.

There were no differences in adverse events for subgroups of patients as defined by gender, age, or race.

Adverse Experience Desloratadine Tablets
5 mg(n=1,655)
Placebo
 (n=1,652)
Pharyngitis 4.1% 2.0%
Dry Mouth 3.0% 1.9%
Myalgia 2.1% 1.8%
Fatigue 2.1% 1.2%
Somnolence 2.1% 1.8%
Dysmenorrhea 2.1% 1.6%

Two hundred and forty-six pediatric subjects 6 months to 11 years of age received desloratadine for 15 days in three placebo-controlled clinical trials. Pediatric subjects aged 6 to 11 years received 2.5 mg once a day, subjects aged 1 to 5 years received 1.25 mg once a day, and subjects 6 to 11 months of age received 1 mg once a day. In subjects 6 to 11 years of age, no individual adverse event was reported by 2 percent or more of the subjects. In subjects 2 to 5 years of age, adverse events reported for desloratadine and placebo in at least 2 percent of subjects receiving desloratadine and at a frequency greater than placebo were fever (5.5%, 5.4%), urinary tract infection (3.6%, 0%) and varicella (3.6%, 0%). In subjects 12 months to 23 months of age, adverse events reported for the desloratadine product and placebo in at least 2 percent of subjects receiving desloratadine and at a frequency greater than placebo were fever (16.9%, 12.9%), diarrhea (15.4% 11.3%), upper respiratory tract infections (10.8%, 9.7%), coughing (10.8%, 6.5%), appetite increased ( 3.1%, 1.6%), emotional lability (3.1%, 0%), epistaxis (3.1%, 0%), parasitic infection, (3.1%, 0%) pharyngitis (3.1%, 0%), rash maculopapular (3.1%, 0%). In subjects 6 months to 11 months of age, adverse events reported for desloratadine and placebo in at least 2 percent of subjects receiving desloratadine and at a frequency greater than placebo were upper respiratory tract infections (21.2%, 12.9%), diarrhea (19.7.% 8.1%), fever (12.1%, 1.6%), irritability (12.1%, 11.3%) coughing (10.6%, 9.7%), somnolence (9.1%, 8.1%), bronchitis (6.1%, 0%), otitis media (6.1%, 1.6%), vomiting (6.1%, 3.2%), anorexia (4.5%, 1.6%), pharyngitis (4.5%, 1.6%), insomnia (4.5%, 0%), rhinorrhea (4.5%, 3.2%), erythema (3%, 1.6%), and nausea (3%, 0%). There were no clinically meaningful changes in any electrocardiographic parameter, including the QTc interval. Only one of the 246 pediatric subjects receiving desloratadine in the clinical trials discontinued treatment because of an adverse event.

The following spontaneous adverse events have been reported during the marketing of desloratadine: tachycardia, palpitations, rare cases of hypersensitivity reactions (such as rash, pruritus, urticaria, edema, dyspnea, and anaphylaxis), psychomotor hyperactivity, seizures, and elevated liver enzymes including bilirubin, and very rarely, hepatitis.

There is no information to indicate that abuse or dependency occurs with desloratadine tablets.

Information regarding acute overdosage is limited to experience from clinical trials conducted during the development of the desloratadine product. In a dose ranging trial, at doses of 10 mg and 20 mg/day somnolence was reported.

Single daily doses of 45 mg were given to normal male and female volunteers for 10 days. All ECGs obtained in this study were manually read in a blinded fashion by a cardiologist. In desloratadine-treated subjects, there was an increase in mean heart rate of 9.2 bpm relative to placebo. The QT interval was corrected for heart rate (QT) by both the Bazett and Fridericia methods. Using the QT (Bazett) there was a mean increase of 8.1 msec in desloratadine-treated subjects relative to placebo. Using QT (Fridericia) there was a mean increase of 0.4 msec in desloratadine-treated subjects relative to placebo. No clinically relevant adverse events were reported.

In the event of overdose, consider standard measures to remove any unabsorbed drug. Symptomatic and supportive treatment is recommended. Desloratadine and 3-hydroxydesloratadine are not eliminated by hemodialysis.

Lethality occurred in rats at oral doses of 250 mg/kg or greater (estimated desloratadine and desloratadine metabolite exposures were approximately 120 times the AUC in humans at the recommended daily oral dose). The oral median lethal dose in mice was 353 mg/kg (estimated desloratadine exposures were approximately 290 times the human daily oral dose on a mg/m basis). No deaths occurred at oral doses up to 250 mg/kg in monkeys (estimated desloratadine exposures were approximately 810 times the human daily oral dose on a mg/m basis).

Adults and Children 12 years of Age and Over: The recommended dose of desloratadine orally disintegrating tablets is one 5 mg tablet once daily.

Children 6 to 11 Years of Age: The recommended dose of desloratadine orally disintegrating tablets is one 2.5 mg tablet once daily.

NOTE: Desloratadine orally disintegrating tablets are not recommended for use in pediatric patients under 6 years of age as desloratadine syrup is better suited for these patients.

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.

Administration of Desloratadine Orally Disintegrating Tablets: Place desloratadine  orally disintegrating tablet on the tongue and allow to disintegrate before swallowing. Tablet disintegration occurs rapidly. Administer with or without water. Take tablet immediately after opening the blister.

Desloratadine Orally Disintegrating Tablets 2.5 mg : Desloratadine tablets 2.5 mg are light red colored, speckled, round, flat, uncoated, beveled edged debossed with “R” on one side and “551” on the other side and are supplied in unit dose packages of 30 (5 x 6). 

Unit dose packages of 30 (5 x 6)                                               NDC 55111-551-31

Desloratadine Orally Disintegrating Tablets 5 mg : Desloratadine tablets 5 mg are light red colored, speckled, round, flat, uncoated, beveled edged debossed with “RDY” on one side and “360” on the other side and are supplied unit dose packages of 30 (5 x 6). 

Unit dose packages of 30 (5 x 6)                                               NDC 55111-360-31

Store orally disintegrating tablets at 20°-25°C (68°-77°F) excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature].

Rx Only

Manufactured by:

Dr. Reddy’s Laboratories Limited

Bachepalli – 502 325 INDIA

Issued: 1207

2.5 mg : Unit dose package 30 (5x6)

5 mg : Unit dose package 30 (5x6)

Manufacturer

Dr. Reddy's Laboratories Limited

Active Ingredients

Source

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Desloratadine [Sun Pharmaceutical Industries Limited ]

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PubMed Articles [2 Associated PubMed Articles listed on BioPortfolio]

Effects of Rupatadine on Platelet- Activating Factor-Induced Human Mast Cell Degranulation Compared With Desloratadine and Levocetirizine (The MASPAF Study).

Platelet-activating factor (PAF) is a lipid mediator involved in the pathophysiology of several allergic diseases, for example, in the amplification of mast cell (MC) activation in anaphylaxis. Rupat...

Drug interaction at hERG channel: In vitro assessment of the electrophysiological consequences of drug combinations and comparison against theoretical models.

Drugs carry a proarrhythmic risk, which gets even greater when they are used in combination. In vitro assessment of the proarrhythmic potential of drugs is limited to one compound and thus neglects th...

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