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  • CLASSES

    Second generation (non-sedating) Antihistamines

    DEA CLASS

    Rx

    DESCRIPTION

    Oral non-sedating, long acting second-generation antihistamine; the active metabolite of loratadine
    Used to relieve symptoms associated with seasonal and perennial allergic rhinitis and used for chronic idiopathic urticaria
    Does not cause QT prolongation

    COMMON BRAND NAMES

    Clarinex, Clarinex RediTab

    HOW SUPPLIED

    Clarinex RediTab/Desloratadine Oral Tab Orally Dis: 2.5mg, 5mg
    Clarinex/Desloratadine Oral Tab: 5mg
    Desloratadine Oral Sol: 0.5mg, 1mL

    DOSAGE & INDICATIONS

    For the management of symptoms of seasonal allergies or perennial allergies, including allergic rhinitis.
    Oral dosage (tablet)
    Adults

    5 mg PO once daily.

    Children and Adolescents 12 years and older

    5 mg PO once daily.

    Oral dosage (orally disintegrating tablet)
    Adults

    5 mg PO once daily.

    Children and Adolescents 12 years and older

    5 mg PO once daily.

    Children 6 to 11 years

    2.5 mg PO once daily.

    Oral dosage (oral solution)
    Adults

    5 mg PO once daily.

    Children and Adolescents 12 years and older

    5 mg PO once daily.

    Children 6 to 11 years

    2.5 mg PO once daily.

    Children 1 to 5 years

    1.25 mg PO once daily. NOTE: Desloratadine is not FDA-approved for the treatment of seasonal allergic rhinitis in children less than 2 years.

    Infants 6 months and older

    1 mg PO once daily. NOTE: Desloratadine is not FDA-approved for the treatment of seasonal allergic rhinitis in infants.

    For the management of symptoms of chronic idiopathic urticaria (e.g., relief of pruritus, reduction in the size and number of hives).
    Oral dosage (tablet)
    Adults

    5 mg PO once daily.

    Children and Adolescents 12 years and older

    5 mg PO once daily.

    Oral dosage (orally disintegrating tablet)
    Adults

    5 mg PO once daily.

    Children and Adolescents 12 years and older

    5 mg PO once daily.

    Children 6 to 11 years

    2.5 mg PO once daily.

    Oral dosage (oral solution)
    Adults

    5 mg PO once daily.

    Children 6 to 11 years

    2.5 mg PO once daily.

    Children and Adolescents 12 years and older

    5 mg PO once daily.

    Children 1 to 5 years

    1.25 mg PO once daily.

    Infants 6 months and older

    1 mg PO once daily.

    MAXIMUM DOSAGE

    Adults

    5 mg/day PO.

    Geriatric

    5 mg/day PO.

    Adolescents

    5 mg/day PO.

    Children

    12 years: 5 mg/day PO.
    6 to 11 years: 2.5 mg/day PO.
    1 to 5 years: 1.25 mg/day PO.

    Infants

    6 to 11 months: 1 mg/day PO.
    Less than 6 months: Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    In adults with hepatic impairment, a starting dose of 5 mg PO every other day is recommended. Recommendations for dosage adjustments in pediatric patients with hepatic impairment are not available, but dosage interval adjustment may be necessary.

    Renal Impairment

    CrCl 50 mL/minute or less: In adults, 5 mg PO every other day is recommended. Recommendations for dosage adjustments in pediatric patients with renal impairment are not available, but dosage interval adjustment may be necessary.
     
    Intermittent hemodialysis
    Desloratadine and its metabolite are not removed by hemodialysis. See dosage for CrCl 50 mL/minute or less.

    ADMINISTRATION

    Oral Administration
    Oral Solid Formulations

    Tablets: Swallow tablets whole, do not chew.
    Disintegrating Tablets: Administer by placing on the tongue. The tablet will dissolve rapidly until it can be swallowed in the saliva. Food or water do not affect bioavailability.

    Oral Liquid Formulations

    Oral syrup (0.5 mg/mL): Measure dose using a calibrated oral syringe, cup, or dropper.

    STORAGE

    Clarinex:
    - Protect from light
    - Store at 77 degrees F; excursions permitted to 59-86 degrees F
    Clarinex RediTab:
    - Product should always be stored in the blister and only removed immediately before use
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    - Store in carton until time of use

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    Desloratadine products are contraindicated in patients who are hypersensitive to desloratadine or to any of the product ingredients or to loratadine.

    Asthma

    The anticholinergic activity of H1-antagonists may result in thickened bronchial secretions in the respiratory tract thereby aggravating asthma or an asthmatic attack. However, these anticholinergic effects do not preclude the use of H1-antagonists in all asthmatic patients, particularly if the upper respiratory symptom is not a primary component of the illness. Because desloratadine possesses only weak anticholinergic properties, it would not be expected to adversely affect the respiratory status of most asthmatic patients.

    Hepatic disease, renal failure, renal impairment

    Use desloratadine with caution in pediatric patients with hepatic disease or renal impairment; dosage adjustments may be necessary, Desloratadine dosage adjustments are recommended for adults with hepatic disease, renal impairment, or renal failure due to increased serum concentrations of desloratadine in these patients.

    Infants, neonates

    The safety and effectiveness of desloratadine in infants less than 6 months have not been established. Antihistamines generally should not be used in neonates due to the possibility of paradoxical CNS stimulation or other adverse reactions. In January 2007, the CDC warned caregivers and healthcare providers of the risk for serious injury or fatal overdose from the administration of cough and cold products to children and infants less than 2 years of age. The report estimated that 1,519 children less than 2 years of age were treated in emergency departments during 2004 to 2005 for adverse events related to cough and cold medications; some cases were due to inadvertent inappropriate use. In January 2008, the FDA issued a Public Health Advisory recommending that non-prescription cough and cold products not be used in infants and children less than 2 years. If prescription or non-prescription ncough and cold products are used in children, labels should be read carefully, caution should be used when administering multiple products, and only measuring devices specifically designed for use with medications should be used. While some combination cough/cold products containing these ingredients are available by prescription only and are not necessarily under scrutiny by the FDA, clinicians should thoroughly assess each patient's use of similar products, both prescription and nonprescription, to avoid duplication of therapy and the potential for inadvertent overdose.

    Pregnancy

    No adequate, well controlled studies exist for desloratadine use during human pregnancy; caution is recommended. No teratogenic or mutagenic effects were observed in animal trials. A long-term study of desloratadine and its metabolite in mice with exposures that were 12 and 27 times, respectively, the AUC in humans at recommended daily doses showed no significant increase in the incidence of tumors. Self-medication with antihistamines during pregnancy is not recommended. Pregnant patients should see their health care professional for a proper diagnosis and for treatment recommendations. The American College of Obstetricians and Gynecologists (ACOG) and the American College of Allergy, Asthma, and Immunology consider loratadine an acceptable alternative in pregnancy, preferably after the first trimester, when first generation antihistamines are not tolerated.

    Breast-feeding

    Desloratadine is distributed into breast milk. According to the manufacturer, the decision should be made to either discontinue breast feeding or discontinue the drug, taking into account the importance of the drug to the mother. However, literature with loratadine, the parent drug, suggests that because of its expected low milk levels and lack of sedation and anticholinergic effects, maternal use of desloratadine is unlikely to affect a breast-fed infant or milk production. In one study, a single loratadine dose of 40 mg was administered to 6 lactating women (note that the suggested daily dose of desloratadine is 5 mg). Average loratadine peak milk concentrations, 2 hours after administration, were 29.2 mcg/L (range 20.4 to 39 mcg/L); average desloratadine peak milk concentrations, 5.3 hours after loratadine administration, were 16 mcg/L (range 9 to 29.6 mcg/L). The total amount excreted in milk over 48 hours was 11.7 mcg of loratadine and desloratadine. However, as noted above, the dose administered was 4 times greater than the usual adult dose of the drug; a total dose of about 3 mcg would be expected with a 10 mg dose. The calculated average and maximum expected doses of loratadine and desloratadine in milk were 0.46% and 1.1% of the maternal weight-adjusted dose, respectively, after the 40 mg dose. Loratadine is considered to be compatible with breast-feeding. The British Society for Allergy and Clinical Immunology recommends loratadine at the lowest dose as a preferred antihistamine in breast-feeding women. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    Driving or operating machinery

    Desloratadine is generally non-sedating. However, the drug may cause drowsiness or somnolence in individual patients; therefore, patients receiving desloratadine should be advised to avoid activities requiring concentration and coordination, such as driving or operating machinery, until the effects of the drug are known.

    Phenylketonuria

    Desloratadine oral disintegrating tablets contain aspartame, a source of phenylalanine. Caution should be used and the source of phenylalanine taken into account in patients with phenylketonuria.

    Geriatric

    While clinical trials with desloratadine did not contain sufficient numbers of older adult patients to determine if they respond differently than younger adult patients, the second-generation, non-sedating antihistamines are generally preferred for the management of allergic rhinitis or other conditions in the geriatric patient. Doses should be adjusted if renal impairment is present. The federal Omnibus Budget Reconciliation Act (OBRA) regulates medication use in residents (e.g., geriatric adults) of long-term care facilities. According to the OBRA guidelines, cough, cold, and allergy medications should be used only for a limited duration (less than 14 days) unless there is documented evidence of enduring symptoms that cannot otherwise be alleviated and for which a cause cannot be identified and corrected.

    ADVERSE REACTIONS

    Severe

    anaphylactoid reactions / Rapid / 0-1.0
    seizures / Delayed / Incidence not known

    Moderate

    erythema / Early / 0-3.0
    hepatitis / Delayed / 0-1.0
    edema / Delayed / 0-1.0
    dyspnea / Early / 0-1.0
    sinus tachycardia / Rapid / Incidence not known
    hyperbilirubinemia / Delayed / Incidence not known
    elevated hepatic enzymes / Delayed / Incidence not known
    palpitations / Early / Incidence not known
    dystonic reaction / Delayed / Incidence not known
    involuntary movements / Delayed / Incidence not known

    Mild

    infection / Delayed / 3.1-21.2
    diarrhea / Early / 0-19.7
    fever / Early / 5.5-16.9
    headache / Early / 14.0-14.0
    irritability / Delayed / 0-12.1
    cough / Delayed / 0-10.8
    drowsiness / Early / 2.1-9.1
    vomiting / Early / 0-6.1
    fatigue / Early / 2.1-5.0
    nausea / Early / 3.0-5.0
    pharyngitis / Delayed / 3.0-4.5
    rhinorrhea / Early / 0-4.5
    anorexia / Delayed / 0-4.5
    insomnia / Early / 0-4.5
    dizziness / Early / 4.0-4.0
    epistaxis / Delayed / 0-3.1
    appetite stimulation / Delayed / 0-3.1
    emotional lability / Early / 0-3.1
    maculopapular rash / Early / 0-3.1
    xerostomia / Early / 3.0-3.0
    myalgia / Early / 2.1-3.0
    dyspepsia / Early / 3.0-3.0
    dysmenorrhea / Delayed / 2.1-2.1
    pruritus / Rapid / 0-1.0
    urticaria / Rapid / 0-1.0
    rash / Early / 0-1.0
    hyperactivity / Early / Incidence not known
    restlessness / Early / Incidence not known

    DRUG INTERACTIONS

    Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Dextromethorphan: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Phenylephrine : (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Dextromethorphan; Doxylamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Diphenhydramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Pamabrom; Pyrilamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Acrivastine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Carbetapentane; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Dextromethorphan; Guaifenesin: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Dextromethorphan; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Guaifenesin; Hydrocodone: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Hydrocodone; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Pseudoephedrine; Dextromethorphan: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Chlorpheniramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Chlorpheniramine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Diphenhydramine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Phenylephrine; Pyrilamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Pyrilamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Dextromethorphan; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Hydrocodone; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Hydrocodone; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Cetirizine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Cetirizine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlophedianol; Dexbrompheniramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlophedianol; Dexchlorpheniramine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorcyclizine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Codeine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dextromethorphan: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dextromethorphan; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dextromethorphan; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dihydrocodeine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dihydrocodeine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Hydrocodone: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Hydrocodone; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Hydrocodone; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Ibuprofen; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Clemastine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Cyclizine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Cyproheptadine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Dexbrompheniramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Dexbrompheniramine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Dexchlorpheniramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Dextromethorphan; Diphenhydramine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Dimenhydrinate: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Hydrocodone; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Ibuprofen: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Naproxen: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Phenylephrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Doxylamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Doxylamine; Pyridoxine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Fexofenadine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Fexofenadine; Pseudoephedrine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Heparin: (Minor) Antihistamines may partially counteract the anticoagulant actions of heparin, according to the product labels. However, this interaction is not likely of clinical significance since heparin therapy is adjusted to the partial thromboplastin time (aPTT) and other clinical parameters of the patient.
    Hydroxyzine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Levocetirizine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Loratadine: (Major) Desloratadine is the active metabolite of Loratadine. These 2 drugs should not be given at the same time due to the duplication of therapy and the resultant increase in desloratadine concentrations, which may lead to increased CNS or anticholinergic effects.
    Loratadine; Pseudoephedrine: (Major) Desloratadine is the active metabolite of Loratadine. These 2 drugs should not be given at the same time due to the duplication of therapy and the resultant increase in desloratadine concentrations, which may lead to increased CNS or anticholinergic effects.
    Meclizine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Pseudoephedrine; Triprolidine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Pyrilamine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Sedating H1-blockers: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.
    Sincalide: (Moderate) Sincalide-induced gallbladder ejection fraction may be affected by concurrent medications, including H1-blockers. False study results are possible; thorough patient history is important in the interpretation of procedure results.
    Triprolidine: (Minor) Although desloratadine is considered a 'non-sedating' antihistamine, dose-related sedation has been noted. For this reason, it would be prudent to monitor for drowsiness during concurrent use of desloratadine with CNS depressants such as other H1-blockers.

    PREGNANCY AND LACTATION

    Pregnancy

    No adequate, well controlled studies exist for desloratadine use during human pregnancy; caution is recommended. No teratogenic or mutagenic effects were observed in animal trials. A long-term study of desloratadine and its metabolite in mice with exposures that were 12 and 27 times, respectively, the AUC in humans at recommended daily doses showed no significant increase in the incidence of tumors. Self-medication with antihistamines during pregnancy is not recommended. Pregnant patients should see their health care professional for a proper diagnosis and for treatment recommendations. The American College of Obstetricians and Gynecologists (ACOG) and the American College of Allergy, Asthma, and Immunology consider loratadine an acceptable alternative in pregnancy, preferably after the first trimester, when first generation antihistamines are not tolerated.

    Desloratadine is distributed into breast milk. According to the manufacturer, the decision should be made to either discontinue breast feeding or discontinue the drug, taking into account the importance of the drug to the mother. However, literature with loratadine, the parent drug, suggests that because of its expected low milk levels and lack of sedation and anticholinergic effects, maternal use of desloratadine is unlikely to affect a breast-fed infant or milk production. In one study, a single loratadine dose of 40 mg was administered to 6 lactating women (note that the suggested daily dose of desloratadine is 5 mg). Average loratadine peak milk concentrations, 2 hours after administration, were 29.2 mcg/L (range 20.4 to 39 mcg/L); average desloratadine peak milk concentrations, 5.3 hours after loratadine administration, were 16 mcg/L (range 9 to 29.6 mcg/L). The total amount excreted in milk over 48 hours was 11.7 mcg of loratadine and desloratadine. However, as noted above, the dose administered was 4 times greater than the usual adult dose of the drug; a total dose of about 3 mcg would be expected with a 10 mg dose. The calculated average and maximum expected doses of loratadine and desloratadine in milk were 0.46% and 1.1% of the maternal weight-adjusted dose, respectively, after the 40 mg dose. Loratadine is considered to be compatible with breast-feeding. The British Society for Allergy and Clinical Immunology recommends loratadine at the lowest dose as a preferred antihistamine in breast-feeding women. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Desloratadine is highly selective for histamine H1-receptors. Unlike cromolyn and nedocromil which block histamine release, H1-antagonists compete with free histamine for binding at H1-receptor sites. This competitive antagonism blocks the effects of histamine on H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. Blockade of H1-receptors also suppresses the formation of edema, flare, and pruritus that result from histaminic activity. At higher concentrations, H1-receptor antagonism becomes relatively irreversible. In vitro studies have demonstrated that desloratadine has a 15-fold higher affinity for the H1-receptor than does the parent compound, loratadine.
     
    Desloratadine does not readily cross the blood-brain barrier, and it preferentially binds at H1-receptors in the periphery rather than within the brain, which probably accounts for some of its nonsedating character. H1-blockers are similar in structure to anticholinergics, local anesthetics, antispasmodics, and ganglionic- and adrenergic-blocking agents, sharing some of their properties. H1-blockers possess anticholinergic properties in varying degrees; however, desloratadine does not exert significant anticholinergic effects at therapeutic concentrations.
     
    In patients with allergic rhinitis, the inflammatory response plays a prominent role in the development of nasal obstruction and involves a number of mediators. Initial release of histamine from mast cells is followed by late-phase reactions involving a number of other cells, such as fibroblasts, epithelial cells, neutrophils, eosinophils (especially in conditions with raised IgE levels), macrophages, platelets, and lymphocytes. Cell adhesion can also be part of the inflammatory process. Desloratadine has demonstrated anti-inflammatory effects in both in vitro and in vivo studies. The anti-inflammatory action appears to be related to a reduction in eosinophils, neutrophils, interleukin-4 and interleukin-8.

    PHARMACOKINETICS

    Desloratadine is administered orally. It is extensively metabolized and only minimal amounts of the orally administered dose are recovered in the urine (less than 2%) and feces (less than 7%). The major metabolic pathway is hydroxylation to form 3-OH-desloratadine that is glucoronidated and the glucuronide conjugate is excreted in the urine and bile. The elimination plasma half-life is approximately 20 to 30 hours. Steady state plasma concentrations are attained in 4 to 6 days.
     
    Affected cytochrome P450 (CYP450) isoenzymes and drug transporters: None
    Clinically relevant drug interactions related to inhibition of CYP450 system enzymes, such as CYP3A4, or drug transporters (such as P-glycoprotein) with desloratadine have not been noted in drug-drug interaction studies. Desloratadine is a CYP3A4 and P-gp substrate. Increased plasma concentrations (Cmax and AUC) of desloratadine and 3-hydroxydesloratadine were observed with some potent CYP3A4 inhibitors in studies. However, 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.

    Oral Route

    Peak plasma concentrations are obtained 3 hours after a 5 mg oral dose of the conventional tablets. Food has no effect on the extent of desloratadine absorption. The conventional tablet, disintegrating tablet, and oral solution are bioequivalent.