Esloray

Desloratadine.

Film-coated tablet: Each tablet contains 5 mg of desloratadine.
Syrup: Each mL contains 0.5 mg of desloratadine.

Pharmacology: Pharmacodynamics: Mechanism of Action: Desloratadine, the active descarboethoxy metabolite of loratadine, is a second generation antihistamine and long-acting tricyclic histamine antagonist with selective H1-receptor histamine antagonist activity. Desloratadine shows significant interaction with the human histamine H1-receptor. Desloratadine inhibited histamine release from human mast cells in vitro.
Pharmacokinetics: Absorption: Onset: Following single- and multiple-dose administration, antihistaminic effects occur within 1 hour.
Symptomatic (nasal and non-nasal) improvement observed as early as 1 day after initiation of therapy.
Duration: Following single- and multiple-dose administration, antihistaminic effects persist for up to 24 hours. No evidence of histamine-induced skin wheal tachyphylaxis over 28-day treatment period.
Food: Food or grapefruit juice does not appear to affect bioavailability following administration as conventional tablets, oral solution, or fixed-combination tablets.
Special Populations: In patients with renal impairment and those who require hemodialysis, peak plasma desloratadine concentrations and AUC are increased.
Distribution: Plasma Protein Binding: Approximately 82-87% (for desloratadine) and 85-89% (for 3-hydroxydesloratadine).
Special Populations: Protein binding not altered in patients with renal impairment.
Metabolism: Extensively metabolized to 3-hydroxydesloratadine (active metabolite), which subsequently undergoes glucuronidation; enzyme(s) responsible for metabolism of desloratadine not identified.
Excretion: Approximately 87% excreted as metabolic products in urine and feces in equal proportions. Desloratadine and 3-hydroxydesloratadine are poorly removed by hemodialysis.
Half-life: 27 hours for desloratadine and 3-hydroxydesloratadine.
Special Populations: In patients ≥65 years of age, plasma desloratadine concentrations are increased and elimination half-life is prolonged. In patients with hepatic impairment, AUC and elimination half-life are increased and clearance is decreased.

Esloray tablet/syrup is indicated for the rapid relief of symptoms associated with allergic rhinitis, such as sneezing, nasal discharge and itching, congestion/stuffiness, as well as ocular itching, tearing and redness, itching of palate and coughing.
Esloray tablet/syrup is also indicated for the relief of symptoms associated with urticaria such as the relief of itching and the size and number of hives.

Recommended Dose: Film-coated tablet: Adults and adolescents (≥12 years of age): One Esloray tablet 5 mg once a day regardless of mealtime. For the relief of symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria. For oral use.
Syrup: Children 6 through 11 years of age: 5 mL (2.5 mg) Esloray syrup once a day, with or without a meal for the relief of symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria.
Children 1 through 5 years of age: 2.5 mL (1.25 mg) Esloray syrup once a day, with or without a meal for the relief of symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria.
Children 6 months through 11 months of age: 2 mL (1 mg) Esloray syrup once a day, with or without a meal for the relief of symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria.
In adults and adolescents (12 years of age and over): 10 mL (5 mg) Esloray syrup once a day, with or without a meal for the relief of symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria.
Intermittent allergic rhinitis (presence of symptoms for less than 4 days per week or for less than 4 weeks) should be managed in accordance with the evaluation of patient's disease history and the treatment could be discontinued after symptoms are resolved and reinitiated upon their reappearance. In persistent allergic rhinitis (presence of symptoms for 4 days or more per week and for more than 4 weeks), continued treatment may be proposed to the patients during allergen exposure periods.
Mode of Administration: Esloray tablet/syrup is administered orally once daily with or without regards to meals.

Overdosage and toxicity (including death) have been reported in children younger than 2 years of age receiving nonprescription (over-the-counter, OTC) preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. Clinicians should ask caregivers about use of nonprescription cough and cold preparations to avoid overdosage.
In the event of overdose, consider standard measures to remove nonabsorped active substance. Symptomatic and supportive treatment is recommended. Based on a multiple dose clinical trial in adults and adolescents, in which up to 45 mg of desloratadine was administered (9 times the clinical dose), no clinically relevant effects were observed. Desloratadine is not eliminated by hemodialysis; it is not known if it is eliminated by peritoneal dialysis.

Known hypersensitivity to desloratadine, loratadine, or any ingredient in the formulation.

Film-coated tablet: 1. This medication may cause drowsiness in some patients. Individual response should be determined that it does not cause drowsiness before driving, operating machines or working in areas with risk of falling.
2. Should not use in breast-feeding women and children under 6 months. Should not use during pregnancy especially in first trimester unless the potential benefits outweigh the risk.
3. Use with caution in renal disease patients.
4. Serum levels of this medication may be increased when using with macrolides antimicrobials such as erythromycin or imidazole antifungal such as ketoconazole.

Efficacy and safety in children younger than 12 months of age have not been established.
The medication may cause drowsiness in some patients. Individual response should be determined that it does not cause drowsiness before driving, operating machines or working in areas with risk of falling. In clinical trials, this medication was no more likely than placebo to cause drowsiness (for film-coated tablet only).
Be careful in patients with renal disease. In the case of severe renal insufficiency (GFR < 30 mL/min), it should be used as alternate day dosage until the physicians can determine the individual patient's response.
Serum levels of this medication may be increased when using with macrolides antimicrobials such as erythromycin or imidazole antifungal such as ketoconazole. No clinical relevant changes in desloratadine plasma concentrations were observed in multiple-dose ketoconazole and erythromycin interaction trials.
Desloratadine should be administered with caution in patients with a medical or family history of seizures. In particular, young children may be more susceptible to developing new seizures under desloratadine treatment. Healthcare providers may consider discontinuing desloratadine in patients who experience a seizure while on treatment.
Effects on ability to drive and use machines: No effects on the ability to drive and use machines have been observed.

Pregnancy: The safe use of this drug during pregnancy has not been established. It is not to be used during pregnancy unless the potential benefits outweigh the risks.
Lactation: Desloratadine is excreted into milk, therefore the use is not recommended in breast-feeding women.
Film-coated tablet: Discontinue nursing or the drug, taking into account the importance of the drug to the woman.

Adverse effects reported in 2% or more of patients 12 years of age and older receiving desloratadine for management of allergic rhinitis and occurring more frequently than placebo include pharyngitis, dry mouth, myalgia, fatigue, somnolence, and dysmenorrhea.
Adverse effects reported in at least 2% of patients 12 years of age and older receiving desloratadine for management of chronic idiopathic urticaria and more frequently than placebo include headache, nausea, fatigue, dizziness, pharyngitis, dyspepsia, and myalgia.
Adverse effects reported in 2% or more of pediatric patients (2-5 years of age) receiving desloratadine and occurring more frequently than placebo include fever, urinary tract infection, and varicella (chicken pox).
Adverse effects reported in 2% or more of patients 12-23 months of age and occurring more frequently than placebo include fever, diarrhea, upper respiratory tract infection, coughing, increased appetite, emotional lability, epistaxis, parasitic infection, pharyngitis, and maculopapular rash.
Adverse effects reported in 2% or more of patients 6-11 months of age and occurring more frequently than placebo include upper respiratory tract infection, diarrhea, fever, irritability, coughing, somnolence, bronchitis, otitis media, vomiting, anorexia, pharyngitis, insomnia, rhinorrhea, erythema, and nausea.
Syrup: Adverse effects reported in 2% or more of patients 12 years of age and older receiving the fixed combination of desloratadine and pseudoephedrine sulfate include dry mouth, headache, insomnia, fatigue, pharyngitis, somnolence, nausea, dizziness, nervousness, hyperactivity, and anorexia.

Potential pharmacokinetic interaction (increased plasma concentrations of desloratadine and active metabolite) when desloratadine is used with drugs affecting hepatic microsomal enzymes (e.g., azithromycin, cimetidine, erythromycin, fluoxetine, ketoconazole). No clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects were reported. Grapefruit juice, Pharmacokinetic interaction unlikely (for syrup only).

Store below 30°C.
Syrup: Shelf-life after opening is 9 months.

Antihistamines & Antiallergics

R06AX27 - desloratadine ; Belongs to the class of other antihistamines for systemic use.

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