Desloratadine

Description

Desloratadine tablets USP, 5 mg are light blue, circular, biconvex, film-coated tablets debossed "LU" on one side and "S71" on the other side. Desloratadine is a white to off-white crystalline powder that is freely soluble in dichloromethane and in methanol. The empirical formula of desloratadine is C19H19ClN2, and its molecular weight is 310.8 g/mol. The chemical name of desloratadine is 8-chloro-6,11-dihydro-11-(4-piperdinylidene)-5H-benzo5,6cyclohepta1,2-bpyridine. Desloratadine tablets USP contain the following excipients: anhydrous lactose, colloidal silicon dioxide, FD&C Blue#2/Indigo Carmine Aluminium Lake, hydrogenated vegetable oil, hypromellose, microcrystalline cellulose, polyethylene glycol, pregelatinised starch, and titanium dioxide.

Uses and Indications

Desloratadine tablets are indicated for the relief of nasal and non-nasal symptoms associated with seasonal allergic rhinitis and perennial allergic rhinitis in patients 12 years of age and older.

There are no teratogenic or nonteratogenic effects associated with the use of desloratadine.

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 water and not chewed or crushed. Consistent daily administration at the same time is advised 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 crucial to ensure patient safety and to mitigate potential complications.

Side Effects

Patients may experience a range of adverse reactions while using the medication. Common adverse reactions reported include pharyngitis, dry mouth, myalgia, fatigue, somnolence, and dysmenorrhea. Notably, somnolence was specifically observed in a dose-ranging trial at doses of 10 mg and 20 mg per day, indicating a potential dose-dependent effect.

In addition to these common reactions, hypersensitivity reactions have been documented. These may manifest as rash, pruritus, urticaria, edema, dyspnea, and, in rare cases, anaphylaxis. Healthcare providers should monitor patients for these serious reactions and take appropriate action if they occur.

Drug Interactions

Co-administration of desloratadine with certain medications may lead to increased plasma concentrations of desloratadine and its active metabolite, 3-hydroxydesloratadine. The following interactions have been identified:

Antifungals and Macrolides

• Ketoconazole, Erythromycin, Azithromycin: The combination with desloratadine results in elevated plasma levels of desloratadine and 3-hydroxydesloratadine. However, no clinically significant changes in the safety profile have been observed.

Antidepressants

• Fluoxetine: Co-administration with desloratadine also leads to increased plasma concentrations of desloratadine and 3-hydroxydesloratadine, with no clinically relevant safety concerns noted.

H2 Antagonists

• Cimetidine: Similar to the aforementioned interactions, cimetidine increases the plasma concentrations of desloratadine and 3-hydroxydesloratadine without any clinically significant changes in safety.

In all cases, while increased plasma concentrations have been documented, no dosage adjustments or enhanced monitoring are specifically recommended due to the absence of clinically relevant safety profile changes.

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 in both 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 oral solution have not been demonstrated in pediatric patients younger than 6 months of age. Caution is advised when considering treatment in this population.

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 subjects. However, other reported clinical experience has not identified significant differences in response between elderly patients and younger patients.

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

The available data regarding the use of desloratadine in pregnant patients is limited and does not provide sufficient evidence to establish a drug-associated risk for major birth defects or miscarriage. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown that desloratadine, when administered during organogenesis, did not result in teratogenic effects in pregnant rats or rabbits at exposure levels significantly higher than the recommended human daily dose (RHD) of 5 mg/day. Specifically, in pregnant rats, doses of desloratadine at 6, 24, and 48 mg/kg/day (approximately 50, 200, and 320 times the AUC-based exposure at the RHD) did not produce fetal malformations, although reduced fetal weights and skeletal variations were observed at the higher doses, likely due to maternal toxicities such as reduced body weight gain and food consumption.

Similarly, in pregnant rabbits, doses of 15, 30, and 60 mg/kg/day (approximately 30, 70, and 230 times the AUC-based exposure at the RHD) did not show adverse effects on fetal development, although reduced maternal body weight gain was noted at the highest dose. In a peri- and post-natal development study, desloratadine was administered to pregnant rats from Gestation Day 6 through lactation at doses of 3, 9, and 18 mg/kg/day. At doses of 9 mg/kg/day or greater, reduced body weight and slow righting reflex were observed in F1 pups, while no developmental effects were noted at 3 mg/kg/day (approximately 10 times the AUC-based exposure at the RHD). Maternal toxicities were also reported at 18 mg/kg/day for F0 dams.

The estimated background risk of major birth defects and miscarriage in the U.S. general population is 2 to 4% and 15 to 20%, respectively. Given the limited data, healthcare professionals should weigh the potential benefits against the risks when considering the use of desloratadine in pregnant patients.

Lactation

Desloratadine is not known to be excreted in human breast milk, and there are no data available regarding its effects on breastfed infants. In animal studies, desloratadine did not show clinically relevant effects on female fertility in rats. However, a male-specific decrease in fertility was observed at an oral dose of 12 mg/kg or greater in rats, which corresponds to approximately 65 times the summed AUC-based exposure of desloratadine and its metabolite at the recommended human dose (RHD). Male fertility remained unaffected at a dose of 3 mg/kg, approximately 10 times the summed AUC-based exposure at the RHD. Given the lack of data on human lactation and the findings in animal studies, caution is advised when considering the use of desloratadine in lactating mothers.

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 gastrointestinal tract. Symptomatic and supportive treatment should be initiated as necessary to manage the patient's condition effectively.

Desloratadine and its active metabolite, 3-hydroxydesloratadine, are not eliminated through hemodialysis, which should be taken into consideration when planning management strategies for overdose cases.

Current knowledge 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, it is noteworthy that in another study involving normal male and female volunteers, no clinically relevant adverse events were observed when participants received single daily doses of desloratadine at 45 mg for a duration of 10 days.

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

Nonclinical Toxicology

In a female fertility study, desloratadine was administered orally to female rats at doses of 6, 12, and 24 mg/kg/day for 14 days prior to mating and throughout the mating period until Gestation Day 7. At the highest dose of 24 mg/kg, an increase in preimplantation loss and a decrease in the number of implantations and fetuses were observed. These effects were likely attributed to maternal toxicities, including reduced body weight gain and food consumption.

In a male fertility study, desloratadine was given orally to male rats for a total dosing period of 106 to 108 days at doses of 3, 12, and 40 mg/kg/day. At the highest dose of 40 mg/kg/day, reduced body weight gain, decreased food consumption, and lower absolute organ weights of the testes, epididymis, and cauda epididymis were noted. A male-specific decrease in fertility was demonstrated at doses of 12 mg/kg/day or greater, characterized by reduced female conception rates, decreased sperm numbers and motility, and histopathologic changes in the testes and epididymis. No effects on male fertility were observed at a dose of 3 mg/kg/day.

The carcinogenic potential of desloratadine was evaluated 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. A significantly higher incidence of hepatocellular tumors (combined adenomas and carcinomas) was observed in male rats receiving 10 mg/kg/day and in both male and female rats receiving 25 mg/kg/day. The clinical significance of these findings during long-term use of desloratadine remains uncertain. In a separate 2-year dietary study in mice, administration of desloratadine at doses of up to 16 mg/kg/day for males and 32 mg/kg/day for females did not result in significant increases in tumor incidence.

Postmarketing Experience

Reports of adverse events have been received through voluntary reporting and surveillance programs. Healthcare professionals and patients are encouraged to report side effects to Lupin Pharmaceuticals, Inc. at 1-800-399-2561 or to the FDA at 1-800-FDA-1088 or via the website www.fda.gov/medwatch. This information contributes to the ongoing assessment of the safety profile of the product.

Patient Counseling

Healthcare providers should advise patients to read the FDA-approved patient labeling (Patient Information) prior to initiating treatment with desloratadine tablets and each time they receive a refill, as there may be new information available. Patients should be instructed to use desloratadine tablets strictly as directed by their healthcare provider. It is important to inform patients that desloratadine tablets can be taken without regard to meals, as there are no food effects on bioavailability.

Patients must be cautioned against increasing the dose or frequency of desloratadine tablets, as studies have not shown increased effectiveness at higher doses and may lead to somnolence. They should be encouraged to discuss any questions regarding the use of this medication with their healthcare provider.

Patients should inform their healthcare provider if they have liver or kidney problems, are pregnant or planning to become pregnant, or are breastfeeding or planning to breastfeed, as desloratadine can pass into breast milk and its effects on an unborn baby are not fully known.

It is essential for patients to maintain an updated list of all medications they are taking and to share this list with their healthcare provider and pharmacist when receiving new prescriptions. Patients should take desloratadine tablets exactly as prescribed and should not alter their dosage or frequency without consulting their healthcare provider.

In the event of an overdose, patients should seek medical attention immediately. They should also be instructed to stop taking desloratadine tablets and contact their healthcare provider or seek emergency help if they experience symptoms such as rash, itching, hives, swelling of the lips, tongue, face, or throat, or difficulty breathing.

Patients should report any bothersome or persistent side effects to their healthcare provider. They may also report side effects to Lupin Pharmaceuticals, Inc. at 1-800-399-2561 or to the FDA at 1-800-FDA-1088 or via www.fda.gov/medwatch.

Desloratadine tablets should be stored at a temperature of 25° C (77° F), with permissible excursions between 15° to 30° C (59° to 86° F). Patients should be informed that desloratadine tablets are sensitive to heat and should not be stored above 30°C (86°F) or exposed to moisture. It is crucial to keep desloratadine tablets and all medications out of the reach of children and to avoid using desloratadine tablets for any condition other than that for which it was prescribed. Patients should not share their medication with others, even if they have similar symptoms, as it may cause harm.

Storage and Handling

The product is supplied in a tight, light-resistant container that complies with USP standards and features a child-resistant closure. It is essential to store the product at a temperature of 25°C (77°F), with permissible excursions between 15°C to 30°C (59°F to 86°F) as outlined by USP Controlled Room Temperature guidelines. Care should be taken to avoid exposure to temperatures at or above 30°C (86°F), as the product is heat sensitive.

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 Lupin Pharmaceuticals, Inc.. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)