Clarius Syrup 0.5 mg/mL

Desloratadine.

Clarius Syrup 0.5 mg/ml: Clear, orange colored aqueous solution with orange flavor.
Each 1 mL of Clarius Syrup 0.5 mg/ml contains Desloratadine 0.5 mg.

Pharmacology: Pharmacodynamics: Desloratadine is the major active metabolite of loratadine. Similar to loratadine, desloratadine is a non-sedating antihistamine. Desloratadine is a long-acting tricyclic antihistamine with selective peripheral histamine H₁ receptor antagonistic activity.
Pharmacokinetics: Absorption: Peak plasma concentrations in children occur in about 2 hours after a single oral 1.25 mg and 5 mg of desloratadine syrup. These values are similar to what was measure in adults who receives 5 mg oral desloratadine. Food has no effect on the extent of absorption.
Distribution: Desloratadine is 82% to 87% bound to plasma proteins. An active metabolite (3-Hydroxydesloratadine) is 85% to 89% bound to plasma proteins. Total protein binding of desloratadine is 73% to 76%. Volume of distribution of desloratadine in children is 686 L to 1565 L.
Metabolism: Desloratadine is metabolized via liver. Metabolism of desloratadine to major active metabolite 3-Hydroxydesloratadine and its associated O-glucuronide was mediated by CYP2C8 in conjunction with UGT2B10. Desloratadine is rapidly metabolized via hydroxylation. Metabolism decrease in slow metabolizers of desloratadine.
Excretion: Desloratadine is excreted in the urine 40.6% and 46.5% was excreted in feces. Total body clearance in adults, approximately 150 L/hr and 31.4 to 64.5 L/hr in children. The mean half-life elimination of desloratadine in children 2-5 years is 16.4 hours, 6-11 years is 19.4 hours and about 27 hours in adults.

CLARIUS 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.
The relief of symptoms associated with urticaria such as the relief of itching and the size and number of hives.

CLARIUS SYRUP should be orally once a day with or without meal. The solution must not be poured into the mouth directly from the bottle, but should use the oral syringe provided to measure the dose as follows: Children 6-11 months: 2 mL (1 mg) once daily.
Children 1-5 years: 2.5 mL (1.25 mg) once daily.
Children 6-11 years: 5 mL (2.5 mg) once daily.
Children 12-17 years: 10 mL (5 mg) once daily.
Adult: 10 mL (5 mg) once daily.
Elderly: No dosage adjustment in Desloratadine is necessary for the elderly.
Hepatic impairment: No dosage adjustment necessary; use with caution in severe impairment.
Renal impairment: Moderate to severe impairment.
No dosage adjustment necessary; use with caution in severe impairment.

Overdose and Treatment: In the event of overdose, consider standard measures to remove unabsorbed active substance. Symptomatic and supportive treatment is recommended. Desloratadine is not eliminated by hemodialysis.
Based on 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 effect were observed.

CLARIUS SYRUP is contraindicated in patients with hypersensitivity to Desloratadine, Loratadine or any ingredient in the formulation.

Liver dysfunction (Desloratadine is metabolized in the liver; potential for enhance toxicity and need for dose adjustment).
Renal impairment: Using with caution in patients with severe renal impairment.
Hepatic impairment: Using with caution in patients with severe hepatic impairment.
Sedative: Effects may be potentiated when used with other sedative drugs or ethanol.
Slow metabolizers: Use with caution in patients knows to be slow metabolizers of desloratadine (incidence of side effect may be increase).
Desloratadine may increase susceptibility to seizures in pediatrics patients, particularly in patients with a history of seizure disorders.

Pregnancy: Desloratadine categorized as pregnancy category C. There is no evidence of teratogenicity or mutagenicity. Second generation antihistamine may be used for treatment allergic rhinitis and urticaria during pregnancy; however, information related to the used of desloratadine in pregnancy is limited and other medication may be preferred.
Lactation: Desloratadine is present in breast milk. The decision to continue or discontinue breastfeeding during therapy should consider the risk of exposure to the infant and the benefits of treatment to the mother.

Cardiovascular Effects: Palpitations, tachycardia.
Dermatologic Effects: Erythema, maculopapular eruption, pruritus, rash.
Gastrointestinal Effects: Diarrhea, increase appetite, loss of appetite, indigestion, nausea, vomiting, xerostomia.
Hepatic Effects: Hepatitis, increase liver enzymes.
Immunologic Effects: Hypersensitivity reaction, Varicella zoster infection, parasitic infection.
Musculoskeletal Effects: Myalgia.
Neurologic Effects: Dizziness, drowsiness, headache, hyperactive behavior, insomnia, movement disorder, seizure, somnolence.
Otic Effects: Otitis media.
Psychiatric Effects: Irritability, mood swings.
Renal Effects: Urinary tract infectious disease.
Reproductive Effects: Dysmenorrhea.
Respiratory Effects: Bleeding from nose, bronchitis, cough, dyspnea, nasal discharge, pharyngitis, upper respiratory infection, epistaxis.
Other: Fatigue, fever.

No clinically relevant interactions with Desloratadine were observed in clinical trials. There was no effect of food or grapefruit juice on the disposition of Desloratadine.
Inhibitors of CYP3A4: In controlled clinical studies co-administration of desloratadine with ketoconazole, erythromycin or azithromycin resulted in increase plasma concentrations of desloratadine and 3-Hydroxydesloratadine, but there were no clinically relevant changes in the safety profile of desloratadine.
Fluoxetine: In controlled clinical studies co-administration of desloratadine with fluoxetine resulted in increase plasma concentrations of desloratadine and 3-Hydroxydesloratadine, but there were no clinically relevant changes in the safety profile of desloratadine.
Cimetidine: In controlled clinical studies co-administration of desloratadine with cimetidine resulted in increase plasma concentrations of desloratadine and 3-Hydroxydesloratadine, but there were no clinically relevant changes in the safety profile of desloratadine.

Do not store above 30°C.

Antihistamines & Antiallergics

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

D