Desloratadine

Description

Desloratadine Tablets are light blue, round tablets containing 5 mg of desloratadine, an antihistamine intended for oral administration. Each tablet comprises inactive ingredients including microcrystalline cellulose NF, pregelatinized starch NF, croscarmellose sodium NF, talc USP, zinc stearate USP, and FD&C Blue #2 HT 11-14%. Desloratadine is characterized as a white to off-white powder, exhibiting slight solubility in water and high solubility in ethanol and propylene glycol. The empirical formula of desloratadine is C19H19ClN2, with a molecular weight of 310.8. Its chemical name is 8-chloro-6,11-dihydro-11-(4-piperdinylidene)-5H-benzo5,6cyclohepta1,2-bpyridine.

Uses and Indications

This drug is indicated for the relief of nasal and non-nasal symptoms associated with seasonal allergic rhinitis in patients 12 years of age and older. It is also indicated for the relief of nasal and non-nasal symptoms associated with perennial allergic rhinitis in the same patient population. Additionally, this drug provides symptomatic relief of pruritus and reduces both the number and size of hives in patients 12 years of age and older diagnosed with chronic idiopathic urticaria.

There are no teratogenic or nonteratogenic effects associated with this drug.

Dosage and Administration

Adults and adolescents aged 12 years and over are recommended to take one 5 mg tablet of desloratadine orally once daily. It is important to ensure that the tablet is swallowed whole with a sufficient amount of water. The administration should be consistent, ideally at the same time each day, to maintain optimal therapeutic levels.

Contraindications

Use is contraindicated in patients with a known hypersensitivity to the product or any of its components.

Warnings and Precautions

Hypersensitivity reactions have been reported in patients taking Desloratadine Tablets. These reactions may manifest as rash, pruritus, urticaria, edema, dyspnea, or, in severe cases, anaphylaxis. In the event of any hypersensitivity reaction, it is imperative to discontinue the use of Desloratadine Tablets immediately and consider alternative treatment options.

Healthcare professionals are advised to monitor patients for signs of hypersensitivity, particularly during the initial stages of treatment. Prompt recognition and management of these reactions are essential to ensure patient safety and to mitigate potential complications.

Side Effects

Patients may experience a range of adverse reactions while receiving treatment. Common adverse reactions reported include pharyngitis, dry mouth, myalgia, fatigue, somnolence, and dysmenorrhea. These reactions were observed in clinical trials and are considered to be of lower severity.

In addition to the common adverse reactions, hypersensitivity reactions have been noted. These may manifest as rash, pruritus, urticaria, edema, dyspnea, and in rare cases, anaphylaxis. Such hypersensitivity reactions warrant immediate medical attention and should be closely monitored in patients.

It is important for healthcare providers to be aware of these potential adverse reactions to ensure appropriate management and support for patients during treatment.

Drug Interactions

Co-administration of desloratadine with certain medications may lead to increased plasma concentrations of desloratadine and its active metabolite, 3-hydroxydesloratadine. However, clinical studies have shown that these interactions do not result in any clinically significant changes to the safety profile of desloratadine.

Pharmacokinetic Interactions:

• Antifungals:

  • Ketoconazole: Co-administration with desloratadine has been shown to increase plasma concentrations of both desloratadine and 3-hydroxydesloratadine. No clinically relevant safety concerns were noted.

• Macrolide Antibiotics:

  • Erythromycin and Azithromycin: Similar to ketoconazole, these antibiotics also resulted in increased plasma levels of desloratadine and its metabolite, without any significant safety implications.

• Selective Serotonin Reuptake Inhibitors (SSRIs):

  • Fluoxetine: The combination with desloratadine led to elevated plasma concentrations of desloratadine and 3-hydroxydesloratadine, with no clinically relevant safety changes observed.

• Histamine H2-Receptor Antagonists:

  • Cimetidine: Co-administration resulted in increased plasma concentrations of desloratadine and its metabolite, but again, no clinically significant safety issues were reported.

Given the lack of clinically relevant changes in safety profiles, no specific dosage adjustments are required when desloratadine is used in conjunction with the aforementioned medications. However, monitoring may be considered in clinical practice to ensure patient safety.

Packaging & NDC

The table below lists all NDC Code configurations of Desloratadine, the U.S. brand-name prescription product. Columns show Packaging, Formulation Type, and Active Ingredient Strength.

Pediatric Use

The recommended dose of Desloratadine Oral Solution for pediatric patients is determined through cross-study comparisons of plasma concentrations between adults and pediatric subjects. Safety has been established in a clinical evaluation involving 246 pediatric subjects aged 6 months to 11 years across three placebo-controlled studies.

Effectiveness in these age groups is supported by data from adequate and well-controlled studies of Desloratadine Tablets conducted in adults. However, the safety and effectiveness of Desloratadine Tablets or Desloratadine Oral Solution have not been demonstrated in pediatric patients younger than 6 months of age.

Geriatric Use

Clinical studies of desloratadine did not include a sufficient number of subjects aged 65 and over to determine whether they respond differently from younger patients. However, other reported clinical experience has not identified significant differences in response between elderly patients and their younger counterparts.

In general, dose selection for geriatric patients should be approached with caution. This is particularly important due to the increased likelihood of decreased hepatic, renal, or cardiac function in this population, as well as the potential for concomitant diseases or other drug therapies. Healthcare providers are advised to consider these factors when prescribing desloratadine to elderly patients to ensure safe and effective use.

Pregnancy

There are no adequate and well-controlled studies in pregnant patients using desloratadine, which is classified as Pregnancy Category C. Animal reproduction studies have shown that desloratadine is not teratogenic in rats or rabbits at doses approximately 210 and 230 times the area under the concentration-time curve (AUC) in humans at the recommended daily oral dose. However, an increase in pre-implantation loss and a decrease in the number of implantations and fetuses were observed in a separate study involving female rats at approximately 120 times the AUC in humans at the recommended daily oral dose.

Additionally, reduced body weight and a slow righting reflex were reported in pups at doses of approximately 50 times or greater than the AUC in humans at the recommended daily oral dose. It is noteworthy that desloratadine had no effect on pup development at approximately 7 times the AUC in humans at the recommended daily oral dose. Given the potential risks observed in animal studies, desloratadine should be used during pregnancy only if clearly needed, and healthcare professionals are advised to weigh the benefits against the risks when prescribing this medication to pregnant patients.

Lactation

Desloratadine passes into breast milk. Therefore, a decision should be made regarding whether to discontinue nursing or to discontinue desloratadine, taking into account the benefit of the drug to the lactating mother and the possible risk to the breastfed infant.

Renal Impairment

Patients with renal impairment have not been specifically addressed in the available data regarding dosage adjustments, special monitoring, or safety considerations. Therefore, healthcare professionals should exercise caution when prescribing this medication to patients with reduced kidney function, as the lack of information necessitates careful clinical judgment and monitoring.

Hepatic Impairment

Patients with hepatic impairment have not been specifically studied in relation to the use of this medication. Consequently, there are no established dosage adjustments, special monitoring requirements, or precautions outlined for individuals with compromised liver function. It is recommended that healthcare providers exercise caution when prescribing this medication to patients with hepatic impairment, given the lack of data on its safety and efficacy in this population. Regular monitoring of liver function may be prudent in these cases, although specific parameters are not defined in the available information.

Overdosage

In the event of an overdose, it is essential to implement standard measures to remove any unabsorbed drug from the system. Symptomatic and supportive treatment is recommended to manage the patient's condition effectively. It is important to note that desloratadine and its metabolite, 3-hydroxydesloratadine, are not eliminated through hemodialysis.

The available information regarding acute overdosage is primarily derived from post-marketing adverse event reports and clinical trials conducted during the development of the desloratadine product. In a dose-ranging trial, somnolence was reported at doses of 10 mg and 20 mg per day. However, in another study involving normal male and female volunteers, no clinically relevant adverse events were observed when participants were administered single daily doses of 45 mg of desloratadine for a duration of 10 days.

Toxicological studies in animal models have provided additional insights into the potential effects of overdose. Lethality was observed in rats at oral doses of 250 mg/kg or greater, with estimated desloratadine and desloratadine metabolite exposures being approximately 120 times the area under the curve (AUC) observed in humans at the recommended daily oral dose. In mice, the oral median lethal dose was determined to be 353 mg/kg, with estimated desloratadine exposures approximately 290 times the human daily oral dose on a milligram per square meter (mg/m²) basis. Conversely, no fatalities were reported in monkeys at oral doses up to 250 mg/kg, where estimated desloratadine exposures were approximately 810 times the human daily oral dose on a mg/m² basis.

Healthcare professionals should remain vigilant for symptoms of overdose and provide appropriate management based on the clinical presentation of the patient.

Nonclinical Toxicology

Desloratadine was evaluated for teratogenic effects in both rats and rabbits. In rats, no teratogenicity was observed at doses up to 48 mg/kg/day, with estimated desloratadine and desloratadine metabolite exposures approximately 210 times the area under the curve (AUC) in humans at the recommended daily oral dose. Similarly, in rabbits, desloratadine did not demonstrate teratogenic effects at doses up to 60 mg/kg/day, with estimated exposures around 230 times the AUC in humans. However, an increase in pre-implantation loss and a decrease in the number of implantations and fetuses were noted in female rats at a dose of 24 mg/kg, where estimated exposures were approximately 120 times the AUC in humans. Additionally, reduced body weight and a slow righting reflex were reported in pups at doses of 9 mg/kg/day or greater, with estimated exposures being approximately 50 times or greater than the AUC in humans. At an oral dose of 3 mg/kg/day, desloratadine had no effect on pup development, with estimated exposures around 7 times the AUC in humans.

In terms of non-teratogenic effects, desloratadine did not affect female fertility in rats at doses up to 24 mg/kg/day, with estimated exposures approximately 130 times the AUC in humans. However, a male-specific decrease in fertility was observed at an oral dose of 12 mg/kg, characterized by reduced female conception rates, decreased sperm numbers and motility, and histopathologic changes in the testes, with estimated exposures around 45 times the AUC in humans. At a lower oral dose of 3 mg/kg/day, desloratadine had no effect on fertility in rats, with estimated exposures approximately 8 times the AUC in humans.

The carcinogenic potential of desloratadine was assessed through studies involving loratadine in rats and desloratadine in mice. In a 2-year study in rats, loratadine was administered in the diet at doses up to 25 mg/kg/day, with estimated desloratadine and desloratadine metabolite exposures approximately 30 times the AUC in humans. A significantly higher incidence of hepatocellular tumors (combined adenomas and carcinomas) was observed in males receiving 10 mg/kg/day and in both males and females receiving 25 mg/kg/day of loratadine. The estimated exposures in rats given 10 mg/kg of loratadine were approximately 7 times the AUC in humans. The clinical significance of these findings during long-term use of desloratadine remains unknown. In a separate 2-year dietary study in mice, males and females receiving up to 16 mg/kg/day and 32 mg/kg/day of desloratadine, respectively, did not exhibit significant increases in tumor incidence, with estimated exposures of 12 and 27 times the AUC in humans at these doses.

Genotoxicity studies with desloratadine indicated no evidence of genotoxic potential, as assessed by a reverse mutation assay (Salmonella/E. coli mammalian microsome bacterial mutagenicity assay) and two assays for chromosomal aberrations (human peripheral blood lymphocyte clastogenicity assay and mouse bone marrow micronucleus assay).

Postmarketing Experience

Postmarketing experience with Desloratadine Tablets has identified several commonly reported side effects among adults and children aged 12 years and older with allergic rhinitis. These include sore throat, dry mouth, muscle pain, tiredness, sleepiness, and menstrual pain.

Increased sleepiness or tiredness has been noted in instances where patients exceeded the prescribed dosage. Patients are encouraged to inform their healthcare provider of any side effects that are bothersome or persistent.

It is important to note that the aforementioned side effects do not encompass all possible adverse reactions associated with Desloratadine Tablets. For further information, patients should consult their healthcare provider or pharmacist.

Side effects can be reported to Belcher Pharmaceuticals LLC at 1-727-471-0850, the FDA at 1-800-FDA-1088, or through the FDA's MedWatch website at www.fda.gov/medwatch.

Patient Counseling

Patients should be instructed to use Desloratadine Tablets as directed by their healthcare provider. It is important to inform patients that there are no food effects on the bioavailability of the medication, allowing them to take Desloratadine Tablets without regard to meals.

Healthcare providers should advise patients against increasing the dose or dosing frequency, as studies have not demonstrated increased effectiveness at higher doses, and somnolence may occur. Patients should be encouraged to read the Patient Information that accompanies Desloratadine Tablets before starting the medication and each time they receive a refill, as there may be new information.

Patients should be prompted to discuss any questions or concerns regarding the use of this medication with their doctor. It is essential for patients to inform their healthcare provider if they have liver or kidney problems, any other medical conditions, are pregnant or planning to become pregnant, or are breastfeeding or planning to breastfeed.

Patients should also be advised to disclose all medications they are taking, including prescription and non-prescription medicines, vitamins, and herbal supplements. Maintaining an updated list of all medications is recommended, which should be shown to their doctor and pharmacist when obtaining a new medicine.

Patients must take Desloratadine Tablets exactly as prescribed and should not alter their dose or frequency of administration. In the event of an overdose, patients should be instructed to contact their doctor or seek medical attention immediately.

Patients should be made aware of serious side effects and instructed to stop taking Desloratadine Tablets and seek immediate medical help if they experience symptoms such as rash, itching, hives, swelling of the lips, tongue, face, or throat, or shortness of breath or difficulty breathing.

Patients should report any bothersome or persistent side effects to their doctor. They may also report side effects to Belcher Pharmaceuticals LLC at 1-727-471-0850 or the FDA at 1-800-FDA-1088 or through www.fda.gov/medwatch.

Proper storage of Desloratadine Tablets is crucial; they should be kept between 59°F to 86°F (15°C to 30°C) and protected from moisture and heat, as the tablets are sensitive to temperature. Patients should be reminded to keep Desloratadine Tablets and all medications out of the reach of children.

Finally, patients should be cautioned not to use Desloratadine Tablets for any condition for which it was not prescribed and should not share the medication with others, even if they have similar symptoms, as it may cause harm.

Storage and Handling

Desloratadine Tablets are supplied in a tight, light-resistant container as defined by the United States Pharmacopeia (USP), equipped with a child-resistant closure. The recommended storage temperature for Desloratadine Tablets is 25° C (77° F), with permissible excursions between 15° C and 30° C (59° F - 86° F). It is essential to avoid exposure to temperatures at or above 30° C (86° F) to maintain the integrity of the product.

Additional Clinical Information

No further data are available.

FDA Insert (PDF)

This document is the official FDA-approved prescribing information for Desloratadine as submitted by Belcher Pharmaceuticals, LLC. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)