Desloratadine

Description

Desloratadine tablets are blue, circular, film-coated tablets containing 5 mg of desloratadine, an antihistamine intended for oral administration. Each tablet includes excipients such as corn starch, microcrystalline cellulose, meglumine, pregelatinized maize starch, sodium starch glycolate, and sodium stearyl fumarate. The coating material comprises hypromellose, titanium dioxide, polyethylene glycol, polysorbate 80, and FD&C Blue #2 Aluminum Lake.

Desloratadine is characterized as a white to off-white powder, exhibiting slight solubility in water while being very soluble in ethanol and propylene glycol. The molecular 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

Desloratadine is 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. Additionally, it is indicated for the symptomatic relief of pruritus, as well as the reduction in the number and size of hives in patients 12 years of age and older with chronic idiopathic urticaria.

There are no teratogenic or nonteratogenic effects associated with 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 and not chewed or crushed. This dosing regimen should be adhered to consistently to maintain optimal therapeutic effects.

Contraindications

Use is contraindicated in patients with a known hypersensitivity to the product or any of its components (Sections 4, 6.2).

Warnings and Precautions

Hypersensitivity reactions have been reported in patients using desloratadine. 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 desloratadine immediately and consider alternative therapeutic 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 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 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

Coadministration 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 in the safety profile of desloratadine.

Pharmacokinetic Interactions:

• Antifungals and Antibiotics: The combination of desloratadine with ketoconazole, erythromycin, or azithromycin has been studied, revealing elevated plasma levels of desloratadine and 3-hydroxydesloratadine. Despite this increase, no adverse safety implications were noted.

• Selective Serotonin Reuptake Inhibitors (SSRIs): When desloratadine is administered alongside fluoxetine, an SSRI, there is also an increase in plasma concentrations of desloratadine and 3-hydroxydesloratadine. Similar to the previous interactions, this does not lead to any clinically relevant safety concerns.

• Histamine H2-Receptor Antagonists: The use of cimetidine in conjunction with desloratadine has been associated with increased plasma levels of desloratadine and 3-hydroxydesloratadine. Again, no significant changes in the safety profile were observed.

No dosage adjustments or enhanced monitoring are required when desloratadine is coadministered with the aforementioned drugs, as the interactions do not present clinically relevant safety issues.

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 safety and effectiveness of desloratadine tablets have not been demonstrated in pediatric patients less than 6 months of age. Therefore, caution is advised when considering the use of this medication in infants within this age group.

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 experiences have 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 safety and efficacy. Monitoring for adverse effects and therapeutic response is recommended to optimize treatment outcomes in this demographic.

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 and rabbits at exposure levels significantly higher than the recommended human daily oral dose (RHD) of 5 mg/day. Specifically, in pregnant rats, doses of 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. 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) also did not show adverse fetal effects.

However, reduced fetal weights and skeletal variations were observed in rats at higher doses (24 and 48 mg/kg/day), likely due to maternal toxicities such as reduced body weight gain and food consumption. In a peri- and post-natal development study, Desloratadine was administered to pregnant rats from Gestation Day 6 through lactation, revealing reduced body weight and slow righting reflex in F1 pups at doses of 9 mg/kg/day or greater (approximately 70 times the AUC-based exposure at the RHD). Notably, no developmental toxicity was observed in F2 pups from F1 offspring that were subsequently mated.

The estimated background risk of major birth defects and miscarriage in the U.S. general population is approximately 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 passes into breast milk. There are insufficient data on the effects of desloratadine on breastfed infants or on milk production in lactating mothers.

The decision to discontinue nursing or to discontinue desloratadine should be made by considering the developmental and health benefits of breastfeeding, the clinical need of the nursing mother, and any potential adverse effects on the breastfed infant from desloratadine or from the underlying maternal condition.

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. It is important to note that desloratadine and its active metabolite, 3-hydroxydesloratadine, are not eliminated through hemodialysis.

Current knowledge regarding acute overdosage is primarily derived from postmarketing 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 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 management based on the clinical presentation of the patient.

Nonclinical Toxicology

No teratogenic effects were observed in the studies conducted.

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, there was an increase in preimplantation loss and a decrease in the number of implantations and fetuses. These effects were likely attributed to maternal toxicities, which included reduced body weight gain and food consumption.

A male fertility study involved the oral administration of desloratadine to male rats for 70 days prior to mating and throughout the mating period, totaling 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 observed 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 noted at 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 males receiving 10 mg/kg/day and in both males and females receiving 25 mg/kg/day. The clinical significance of these findings during long-term use of desloratadine remains unknown. 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.

Genotoxicity studies indicated no evidence of genotoxic potential for desloratadine, as assessed by a reverse mutation assay and two assays for chromosomal aberrations, including a human peripheral blood lymphocyte clastogenicity assay and a mouse bone marrow micronucleus assay.

The findings from these studies provide important insights into the nonclinical toxicology of desloratadine, particularly regarding its effects on fertility and potential carcinogenicity.

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.

Additionally, instances of increased sleepiness or tiredness have been noted, particularly in cases where dosages exceeded those prescribed by a healthcare professional.

Patients are advised to consult their healthcare provider for medical advice regarding side effects. Reports of adverse events can also be made to the FDA at 1-800-FDA-1088.

Patient Counseling

Healthcare providers should advise patients to read the FDA-approved patient labeling (Patient Information) prior to starting 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.

Before initiating treatment with desloratadine tablets, patients should inform their healthcare provider if they have liver or kidney problems, any other medical conditions, or if they are pregnant, planning to become pregnant, or breastfeeding. It is essential to communicate that desloratadine can pass into breast milk, and patients should consult their doctor regarding the best feeding options for their baby while taking this medication.

Patients should be reminded to disclose all medications they are currently taking, including prescription and non-prescription drugs, vitamins, and herbal supplements. Maintaining an updated list of all medications is advisable, and patients should present this list to their healthcare provider or pharmacist when obtaining new medications.

Desloratadine tablets should be taken exactly as prescribed, and patients should not alter their dosage or frequency without consulting their healthcare provider. In the event of an overdose, patients must seek medical attention immediately.

Patients should 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. They should also report any bothersome side effects or those that do not resolve to their healthcare provider. Side effects can be reported to the FDA at 1-800-FDA-1088.

Storage instructions should be communicated to patients, emphasizing that desloratadine tablets should be stored at 25°C (77°F), with permissible excursions between 15° and 30°C (59° and 86°F). Patients should be informed that desloratadine tablets are sensitive to heat and should not be stored above 86°F (30°C) or exposed to moisture. It is crucial to keep desloratadine tablets and all medications out of the reach of children.

Finally, patients should be cautioned against using desloratadine tablets for any condition other than that for which it was prescribed and should not share this medication with others, even if they have similar symptoms, as it may be harmful to them.

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° and 30°C (59° and 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) due to the product's heat sensitivity.

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 Sun Pharmaceutical Industries, Inc.. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)