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  • CLASSES

    Second generation (non-sedating) Antihistamines

    DEA CLASS

    OTC

    DESCRIPTION

    Oral non-sedating antihistamine
    CNS effects are less with loratadine compared to the traditional sedating antihistamines; not associated with QT prolongation
    Used in adult and pediatric populations for allergic rhinitis and chronic idiopathic urticaria or other allergic symptoms

    COMMON BRAND NAMES

    Alavert, Allergy Relief, Claritin, Claritin Chewable, Claritin Liqui-Gel, Claritin RediTab, Claritin-D 24 Hour, Clear-Atadine, Dimetapp Children's Non-Drowsy Allergy, QlearQuil All Day & All Night Allergy Relief, Tavist ND

    HOW SUPPLIED

    Alavert Oral Tab ER: 10mg
    Alavert/Allergy Relief/Claritin/Clear-Atadine/Dimetapp Children's Non-Drowsy Allergy/Loratadine Oral Sol: 5mg, 5mL
    Alavert/Claritin RediTab/Dimetapp Children's Non-Drowsy Allergy Oral Tab Orally Dis: 5mg, 10mg
    Allergy Relief/Claritin/Claritin-D 24 Hour/Clear-Atadine/Loratadine/QlearQuil All Day & All Night Allergy Relief/Tavist ND Oral Tab: 10mg
    Claritin Chewable Oral Tab Chew: 5mg
    Claritin Liqui-Gel/Loratadine Oral Cap: 10mg

    DOSAGE & INDICATIONS

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

    10 mg PO once daily. Do not exceed 10 mg in 24 hours.

    Children and Adolescents 6 to 17 years

    10 mg PO once daily. Do not exceed 10 mg in 24 hours.

    Oral dosage (orally disintegrating tablets)
    Adults, Adolescents, and Children 6 years and older

    10 mg/day PO, given as 5 mg PO twice daily or 10 mg once daily. Tablet disintegrates with or without water. Do not exceed 10 mg in 24 hours.

    Oral dosage (chewable tablets, OTC product)
    Adults, Adolescents, and Children 6 years and older

    10 mg PO daily. Do not exceed 10 mg in 24 hours.

    Children 2 to 5 years

    5 mg PO daily. Do not exceed 5 mg in 24 hours.

    Oral dosage (oral syrup or solution)
    Adults, Adolescents, and Children 6 years and older

    10 mg PO daily. Do not to exceed 10 mg in 24 hours.

    Children 2 to 5 years

    5 mg PO once daily. Do not to exceed 5 mg in 24 hours.

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

    10 mg PO once daily. Do not exceed 10 mg in 24 hours.

    Children and Adolescents 6 to 17 years

    10 mg PO once daily. Do not exceed 10 mg in 24 hours.

    Oral dosage (orally disintegrating tablets)
    Adults, Adolescents, and Children 6 years and older

    10 mg/day PO, given as 5 mg PO twice daily or 10 mg once daily. Tablet disintegrates with or without water. Do not exceed 10 mg in 24 hours. 

    Oral dosage (chewable tablets)
    Adults, Adolescents, and Children 6 years and older

    10 mg PO daily. Do not exceed 10 mg in 24 hours.

    Children 2 to 5 years

    5 mg PO daily. Do not exceed 5 mg in 24 hours.

    Oral dosage (oral syrup or solution)
    Adults, Adolescents, and Children 6 years and older

    10 mg PO daily. Do not to exceed 10 mg in 24 hours.

    Children 2 to 5 years

    5 mg PO once daily. Do not to exceed 5 mg in 24 hours.

    For adjunctive exercise-induced bronchospasm prophylaxis† in patients with allergies.
    Oral dosage
    Adults, Adolescents, and Children 7 years of age and older

    10 mg PO once daily has been used. Because allergy control can lead to better asthma control, the American Thoracic Society recommends daily antihistamine therapy in patients with EIB and allergies who continue to have symptoms despite using an inhaled short-acting beta-2 agonist (SABA) before exercise, or in those who require daily (or more frequent) SABA use. Antihistamines should not be used in nonallergic patients with EIB. Available studies demonstrate some reduction in the symptoms of exercise-induced bronchospasm (EIB). Loratadine 10 mg/day significantly reduced the decrease from baseline in FEV-1 following exercise in a randomized, double-blind, placebo controlled trial in asthmatic patients aged 7 to 17 years with allergies.

    †Indicates off-label use

    MAXIMUM DOSAGE

    NOTE: Do not exceed recommended dosage limits for the specific product prescribed; the following are general guidelines:

    Adults

    10 mg/day PO.

    Geriatric

    10 mg/day PO.

    Adolescents

    10 mg/day PO.

    Children

    6 to 12 years: 10 mg/day PO.
    2 to 5 years: 5 mg/day PO.
    1 year: Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    For adults and children 6 years and older: Reduce initial dosage to 10 mg PO every other day.
    For children 2 to 5 years: Reduce initial dose to 5 mg PO every other day.

    Renal Impairment

    CrCl 30 mL/minute or greater: No dosage adjustment needed.
    CrCl less than 30 mL/minute: For adults and pediatric patients 6 years and older, reduce initial dosage to 10 mg PO every other day. For children 2 to 5 years, reduce initial dose to 5 mg PO every other day.
     
    Intermittent hemodialysis
    Loratadine and its active metabolite are not removed by hemodialysis. See dosage for patients with CrCl less than 30 mL/min.

    ADMINISTRATION

    Oral Administration

    Loratadine may be administered without regard to meals.

    Oral Solid Formulations

    Rapidly-disintegrating oral tablets (e.g., Alavert orally disintegrating tablets or Claritin Reditabs): Place on tongue; allow to dissolve and then swallow. May be administered with or without water. Store in a dry place at controlled room temperature. Use within 6 months of opening laminated foil pouch, and immediately upon opening an individual tablet blister.

    Oral Liquid Formulations

    Oral syrup, suspension, or solution (1 mg/ml): Measure dosage using a calibrated measuring device. Suspension formulations may not need to be shaken; check labeling.

    STORAGE

    Alavert:
    - Store between 68 to 77 degrees F
    Allergy Relief:
    - Protect from moisture
    - Store between 68 to 77 degrees F
    Claritin:
    - Protect from moisture
    - Store between 68 to 77 degrees F
    Claritin Chewable:
    - Store between 68 to 77 degrees F
    Claritin Hives Relief:
    - Store between 59 to 77 degrees F
    - Store in a dry place
    Claritin Liqui-Gel:
    - Protect from freezing
    - Store at controlled room temperature (between 68 and 77 degrees F)
    Claritin RediTab:
    - Store between 68 to 77 degrees F
    Claritin-D 24 Hour:
    - Protect from moisture
    - Store between 68 to 77 degrees F
    Clear-Atadine :
    - Protect from moisture
    - Store between 68 to 77 degrees F
    Dimetapp Children's Non-Drowsy Allergy:
    - Store between 68 to 77 degrees F
    QlearQuil All Day & All Night Allergy Relief:
    - Protect from moisture
    - Store between 68 to 77 degrees F
    Tavist ND:
    - Protect from moisture
    - Store between 68 to 77 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    Loratadine is contraindicated in any individual hypersensitive to the drug or any of the ingredients of the specific drug formulation, or in any patient hypersensitive to desloratadine, due to cross-sensitivity.

    Asthma

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

    Phenylketonuria

    Some formulations of loratadine (e.g., Alavert Orally Disintegrating tablets, Dimetapp ND Orally Disintegrating tablets) contain phenylalanine. These products should be used cautiously in patients with phenylketonuria.

    Driving or operating machinery

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

    Hepatic disease

    Loratadine is extensively metabolized in the liver. Loratadine should be used cautiously in those with hepatic disease and initial dosage adjustments should be made according to the manufacturer's guidelines.

    Renal failure, renal impairment

    Loratadine should be used cautiously in those with renal failure or renal impairment. The exposure and maximal concentrations of loratadine and its metabolite are elevated in the presence of significant renal impairment (CrCl less than 30 mL/min). Initial dosage adjustments should be made according to the manufacturer's guidelines based on patient age.

    Pregnancy

    Loratadine is available over-the-counter without a prescription. Animal studies have not demonstrated a risk to the fetus but there are no adequate studies in pregnant women. Use during pregnancy only when the benefits of therapy outweigh the risks. Self-medication with loratadine 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

    Loratadine and its metabolite, desloratadine, are excreted into breast milk; breast-feeding women are advised to consult a healthcare professional prior to using loratadine. In one study, a single loratadine dose of 40 mg (4 times the usual dose) was administered to 6 lactating women. 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. The calculated average and maximum expected exposures of loratadine and desloratadine in milk were 0.46% and 1.1% of the maternal weight-adjusted dose, respectively, after the 40 mg dose. Approximately 3 mcg would be expected to be excreted in the milk with a 10 mg dose. Because of its lack of sedation and low milk concentrations, maternal use would not be expected to cause adverse effects in breast-fed babies and loratadine is considered usually compatible with breast-feeding. The British Society for Allergy and Clinical Immunology also 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.

    Children, infants, neonates

    Safety and efficacy have not been established for loratadine use in neonates, infants, or children less than 2 years of age. Antihistamines generally should not be used in neonates due to the possibility of paradoxical CNS stimulation or seizures.

    Geriatric

    The second-generation, non-sedating antihistamines such as loratadine 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; 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

    seizures / Delayed / Incidence not known
    bronchospasm / Rapid / Incidence not known
    erythema multiforme / Delayed / Incidence not known
    angioedema / Rapid / Incidence not known
    anaphylactoid reactions / Rapid / Incidence not known
    hepatic necrosis / Delayed / Incidence not known

    Moderate

    stomatitis / Delayed / 2.0-3.0
    conjunctivitis / Delayed / 2.0-2.0
    thrombocytopenia / Delayed / 0-1.0
    hypertonia / Delayed / Incidence not known
    migraine / Early / Incidence not known
    constipation / Delayed / Incidence not known
    gastritis / Delayed / Incidence not known
    hypotension / Rapid / Incidence not known
    sinus tachycardia / Rapid / Incidence not known
    hypertension / Early / Incidence not known
    chest pain (unspecified) / Early / Incidence not known
    peripheral edema / Delayed / Incidence not known
    palpitations / Early / Incidence not known
    supraventricular tachycardia (SVT) / Early / Incidence not known
    hemoptysis / Delayed / Incidence not known
    dyspnea / Early / Incidence not known
    wheezing / Rapid / Incidence not known
    depression / Delayed / Incidence not known
    amnesia / Delayed / Incidence not known
    confusion / Early / Incidence not known
    vaginitis / Delayed / Incidence not known
    impotence (erectile dysfunction) / Delayed / Incidence not known
    urinary retention / Early / Incidence not known
    urinary incontinence / Early / Incidence not known
    jaundice / Delayed / Incidence not known
    elevated hepatic enzymes / Delayed / Incidence not known
    hepatitis / Delayed / Incidence not known
    blurred vision / Early / Incidence not known
    blepharospasm / Early / Incidence not known

    Mild

    headache / Early / 12.0-12.0
    drowsiness / Early / 8.0-8.0
    fatigue / Early / 2.0-4.0
    diarrhea / Early / 2.0-3.0
    otalgia / Early / 2.0-3.0
    pharyngitis / Delayed / 2.0-3.0
    xerostomia / Early / 3.0-3.0
    epistaxis / Delayed / 2.0-3.0
    infection / Delayed / 2.0-3.0
    rash / Early / 2.0-3.0
    abdominal pain / Early / 2.0-2.0
    hyperhidrosis / Delayed / Incidence not known
    arthralgia / Delayed / Incidence not known
    dizziness / Early / Incidence not known
    tremor / Early / Incidence not known
    hypoesthesia / Delayed / Incidence not known
    vertigo / Early / Incidence not known
    asthenia / Delayed / Incidence not known
    myalgia / Early / Incidence not known
    muscle cramps / Delayed / Incidence not known
    paresthesias / Delayed / Incidence not known
    nausea / Early / Incidence not known
    appetite stimulation / Delayed / Incidence not known
    dyspepsia / Early / Incidence not known
    flatulence / Early / Incidence not known
    polydipsia / Early / Incidence not known
    hiccups / Early / Incidence not known
    anorexia / Delayed / Incidence not known
    vomiting / Early / Incidence not known
    dysgeusia / Early / Incidence not known
    weight gain / Delayed / Incidence not known
    syncope / Early / Incidence not known
    tinnitus / Delayed / Incidence not known
    sinusitis / Delayed / Incidence not known
    nasal dryness / Early / Incidence not known
    laryngitis / Delayed / Incidence not known
    fever / Early / Incidence not known
    sneezing / Early / Incidence not known
    cough / Delayed / Incidence not known
    chills / Rapid / Incidence not known
    insomnia / Early / Incidence not known
    paranoia / Early / Incidence not known
    irritability / Delayed / Incidence not known
    libido decrease / Delayed / Incidence not known
    anxiety / Delayed / Incidence not known
    menorrhagia / Delayed / Incidence not known
    breast enlargement / Delayed / Incidence not known
    dysmenorrhea / Delayed / Incidence not known
    mastalgia / Delayed / Incidence not known
    purpura / Delayed / Incidence not known
    alopecia / Delayed / Incidence not known
    flushing / Rapid / Incidence not known
    pruritus / Rapid / Incidence not known
    photosensitivity / Delayed / Incidence not known
    xerosis / Delayed / Incidence not known
    urticaria / Rapid / Incidence not known
    urine discoloration / Early / Incidence not known
    ocular pain / Early / Incidence not known

    DRUG INTERACTIONS

    Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Dextromethorphan; Doxylamine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Dextromethorphan; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acetaminophen; Diphenhydramine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Acrivastine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Brompheniramine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Carbetapentane; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Dextromethorphan; Guaifenesin: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Guaifenesin; Hydrocodone: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Hydrocodone; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Brompheniramine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Chlorpheniramine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Chlorpheniramine; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Diphenhydramine; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Phenylephrine; Pyrilamine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbetapentane; Pyrilamine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Dextromethorphan; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Hydrocodone; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Hydrocodone; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Carbinoxamine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Cetirizine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Cetirizine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlophedianol; Dexbrompheniramine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlophedianol; Dexchlorpheniramine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorcyclizine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Codeine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dextromethorphan: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dextromethorphan; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dihydrocodeine; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Dihydrocodeine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Hydrocodone: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Hydrocodone; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Hydrocodone; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Chlorpheniramine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Clemastine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Cyclizine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Cyproheptadine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Desloratadine: (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.
    Desloratadine; 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.
    Dexchlorpheniramine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Dextromethorphan; Diphenhydramine; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Dimenhydrinate: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Hydrocodone; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Ibuprofen: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Naproxen: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Diphenhydramine; Phenylephrine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Doxylamine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Doxylamine; Pyridoxine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Fexofenadine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Fexofenadine; Pseudoephedrine: (Minor) Although loratadine 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 loratadine 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 loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Levocetirizine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Meclizine: (Minor) Although loratadine 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 loratadine with CNS depressants such as other H1-blockers.
    Sedating H1-blockers: (Minor) Although loratadine 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 loratadine 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 loratadine 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 loratadine with CNS depressants such as other H1-blockers.

    PREGNANCY AND LACTATION

    Pregnancy

    Loratadine is available over-the-counter without a prescription. Animal studies have not demonstrated a risk to the fetus but there are no adequate studies in pregnant women. Use during pregnancy only when the benefits of therapy outweigh the risks. Self-medication with loratadine 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.

    Loratadine and its metabolite, desloratadine, are excreted into breast milk; breast-feeding women are advised to consult a healthcare professional prior to using loratadine. In one study, a single loratadine dose of 40 mg (4 times the usual dose) was administered to 6 lactating women. 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. The calculated average and maximum expected exposures of loratadine and desloratadine in milk were 0.46% and 1.1% of the maternal weight-adjusted dose, respectively, after the 40 mg dose. Approximately 3 mcg would be expected to be excreted in the milk with a 10 mg dose. Because of its lack of sedation and low milk concentrations, maternal use would not be expected to cause adverse effects in breast-fed babies and loratadine is considered usually compatible with breast-feeding. The British Society for Allergy and Clinical Immunology also 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

    Loratadine 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 muscle. Loratadine 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, loratadine does not exert significant anticholinergic effects at therapeutic concentrations. In vitro studies have shown that loratadine has a weak affinity for acetylcholine and alpha-adrenergic receptors.

    PHARMACOKINETICS

    Loratadine is administered orally. It is 97% protein-bound and is excreted into breast milk. Loratadine has a high first pass effect and is almost completely metabolized in the liver to the minimally active metabolite, descarboethoxyloratadine. In vitro studies indicate that metabolism to descarboethoxyloratadine predominantly by CYP3A4 and, to a lesser extent, by cytochrome CYP2D6. In the presence of a CYP3A4 inhibitor, loratadine is metabolized to descarboethoxyloratadine predominantly by CYP2D6. The normal mean elimination half-lives of loratadine and its metabolite are 8.4 hours (range 3 to 20 hours) and 28 hours, respectively. Elimination occurs through the fecal and renal routes.
     
    Affected cytochrome P450 (CYP450) isoenzymes and drug transporters: CYP3A4, CYP2D6, P-gp
    Metabolism of loratadine occurs predominantly by CYP3A4 and, to a lesser extent, by cytochrome CYP2D6. Concurrent administration with either ketoconazole, erythromycin (both CYP3A4 inhibitors), or cimetidine (CYP2D6 and CYP3A4 inhibitor) to healthy volunteers was associated with increased plasma concentrations of loratadine. However, in drug-drug interaction studies there were no clinically relevant changes in the safety profile of loratadine associated with these increases. Loratadine is also a substrate for P-glycoprotein (P-gp) transport; however, no clinically significant drug-drug interactions have been reported with P-gp inhibitors.

    Oral Route

    After oral administration, the onset of action of loratadine occurs within 1 to 3 hours, with peak effects in 8 to 12 hours and a duration of action greater than 24 hours. Administration with food increases absorption and AUC up to 40% for the syrup or tablets and up to 48% for the rapidly-disintegrating tablets. The time to peak concentrations (Tmax) is delayed by administration with food. However, since the clinical response is unaffected, the drug can be administered without regard to meals.