Xynoz

Desloratadine.

Each film coated tablet contains Desloratadine 5 mg.

Pharmacology: Pharmacodynamics: Desloratadine is a non-sedating long-acting histamine antagonist with potent, selective peripheral H1-receptor antagonist activity. Desloratadine has demonstrated antiallergic, antihistaminic and anti-inflammatory activities. After oral administration, desloratadine selectively blocks peripheral histamine H1-receptors because the drug is effectively excluded from entry to the central nervous system.
Based on reported data, desloratadine inhibits the broad cascade of events that initiate and propagate allergic inflammation, including: the release of proinflammatory cytokines including IL-4, IL-6, IL-8, IL-13; the release of important proinflammatory chemokines such as RANTES (Regulated upon Activation, Normal T-cell Expressed and Secreted); superoxide anion production by activated polymorphonuclear neutrophils; eosinophil adhesion and chemotaxis; the expression of the adhesion molecules such as P-selectin; IgE-dependent release of histamine, prostaglandin (PGD2), and leukotriene (LTC4); the acute allergic bronchoconstrictor response and allergic cough in animal models.
At the recommended adult dose of 5 mg daily, there was no excess incidence of somnolence and not affect standard measures of flight performance including exacerbation of subjective sleepiness or task related to flying. Also, Xynoz tablet at a dose of 7.5 mg daily does not affect psychomotor performance. Based on reported data, at a dose 20 mg daily for 14 days resulted in no statistical or clinical cardiovascular effect. At a dose 45 mg daily for 10 days, no prolongation of the QTc interval was reported.
No clinically relevant changes in desloratadine plasma concentrations were observed when taken concomitantly with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine.
Based on literature, co-administration of alcohol did not increase the alcohol-induced impairment in performance or increase in sleepiness. No significant differences were found in the psychomotor test results, whether administered alone or with alcohol.
In adult and adolescent patients with allergic rhinitis, Xynoz tablet was effective in relieving symptoms such as sneezing, nasal discharge and itching, congestion/stuffiness, as well as ocular itching, tearing and redness, and itching of palate. Xynoz tablet effectively controlled symptoms for 24 hours.
Based on the available data, Xynoz tablet was effective in relieving pruritis and decreasing the size and number of hives as early as 1 day after initiation of treatment in adults and adolescence with chronic idiopathic urticaria (CIU). The effects were sustained over the 24-hour dosing interval. Treatment with Xynoz tablet also improved sleep and daytime function, as measured by reduced interference with sleep and routine daily activities.
Xynoz tablet was effective in alleviating the burden of seasonal allergic rhinitis as shown by the total score of the rhino-conjunctivitis quality of life questionnaires. The greatest amelioration was seen in the domains of practical problems and daily activities limited by symptoms.
Pharmacokinetics: Absorption: Desloratadine plasma concentrations can be detected within 30 minutes of administration. Desloratadine is well absorbed with maximum concentration achieved after approximately 3 hours; the terminal phase half-life is approximately 27 hours. The degree of accumulation of desloratadine was consistent with its half-life (approximately 27 hours) and a once daily dosing frequency. The bioavailability of desloratadine was dose proportional over the range of 5 mg to 20 mg.
Distribution: Desloratadine is moderately bound (83 % - 87 %) to plasma proteins. There is no reported data on desloratadine accumulation following once daily dosing (5 mg to 20 mg) for 14 days.
Biotransformation: Desloratadine does not inhibit CYP3A4 or CYP2D6 and is neither a substrate nor an inhibitor of P-glycoprotein.
Elimination: There was no effect of food (high-fat, high caloric breakfast) and grapefruit juice on the disposition of desloratadine.

Xynoz tablet 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.
Xynoz tablet is also indicated for the symptomatic relief of itching and the size and number of hives which is associated with chronic idiopathic urticaria.

Adults and Adolescents (12 years of age and older): One tablet once a day regardless of mealtime. The dose can be taken with or without food.
Route Of Administration: Oral.

No clinically relevant effects were observed for desloratadine doses up to 45 mg. The adverse event profile associated with overdosage is similar to that seen with therapeutic doses, but the magnitude of the effects can be higher.
In the event of overdose, consider standard measures to remove unabsorbed active substance. Symptomatic and supportive treatment is recommended. Desloratadine is not eliminated by haemodialysis; it is not known if it is eliminated by peritoneal dialysis.

Hypersensitivity to the active substance, to any of the excipients or to loratadine.

Efficacy and safety of Xynoz tablet in children under 12 years of age have not been established.
In the case of severe renal insufficiency, Xynoz tablet should be used with caution. Desloratadine should be administered with caution in patients with medical or family history of seizures, and mainly young children, being more susceptible to develop new seizures under desloratadine treatment. Healthcare providers may consider discontinuing desloratadine in patients who experience a seizure while on treatment.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on Ability to Drive and Use Machines: No effects on the ability to drive and use machines have been observed. Patients should be informed that most people do not experience drowsiness. Nevertheless, as there is individual variation in response to all medicinal products, it is recommended that patients are advised not to engage in activities requiring mental alertness, such as driving a car or using machines, until they have established their own response to the medicinal product.

Pregnancy: Xynoz tablet is not to be used during pregnancy unless the potential benefits outweigh the risks.
Breast-feeding: The use of Xynoz tablet is not recommended in breast-feeding women.

The most frequent of adverse reactions reported were fatigue, dry mouth and headache.
Paediatric population: Based on existing data, the most common adverse reaction was headache. Other adverse reactions reported for paediatric patients with an unknown frequency are QT prolongation, arrhythmia, bradycardia, abnormal behaviour, and aggression.
Tabulated list of adverse reactions: (See table).

Click on icon to see table/diagram/image

Based on existing data, no clinically relevant interactions were observed when desloratadine co-administered with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine.
There was no effect of food or grapefruit juice on the disposition of desloratadine. Xynoz tablet taken concomitantly with alcohol did not potentiate the performance impairing effects of alcohol. However, caution is recommended if alcohol is taken concomitantly.

Store below 30°C.
Store in the original package.

Antihistamines & Antiallergics

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

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