Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1 Pharmacodynamic properties
Pharmacotherapeutic group: DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE, Corticosteroids, ATC code: R 01 AD11
Mechanism of action
Triamcinolone acetonide is a more potent derivative of triamcinolone and is approximately 8 times more potent than prednisone. Although the precise mechanism of corticosteroid antiallergic action is unknown, corticosteroids are very effective in the treatment of allergic diseases in man.
Pharmacodynamic effects
STERONASE AQ NASAL SPRAY does not have an immediate effect on allergic signs and symptoms.
An improvement in some patient symptoms may be seen within the first day of treatment with STERONASE AQ NASAL SPRAY and relief may be expected in 3 to 4 days. When STERONASE AQ NASAL SPRAY is prematurely discontinued symptoms may not recur for several days.

In clinical studies performed in adults and children 6 years of age and above at doses up to 440 mcg/day intranasally, and in children 2 to 5 years of age at 110 μg/day intranasally, no suppression of the Hypothalamic-Pituitary-Adrenal (HPA) axis has been observed.

A one-year double-blind, placebo-controlled parallel group study in 298 treated pediatric patients (3 to 9 years of age) was conducted to assess the effect of STERONASE AQ NASAL SPRAY (once-daily dose of 110 micrograms) on growth velocity using stadiometry. From the primary analysis of evaluable patients (134 STERONASE AQ NASAL SPRAY and 133 placebo), the estimated growth velocity in the STERONASE AQ NASAL SPRAY group was 0.45 cm/year lower than that in the placebo group with 95% CI ranging between 0.11 to 0.78 cm/year lower than placebo. Difference between treatment groups started within 2 months of drug initiation. After stopping treatment during the 2-month follow- up period it was observed that the mean growth velocity in the treatment group returned to baseline (pre-treatment) values.

Pharmacokinetic Properties

5.2 Pharmacokinetic properties
Single dose intranasal administration of 220 micrograms of STERONASE AQ NASAL SPRAY in normal adult subjects and in adult patients with allergic rhinitis demonstrated low absorption of triamcinolone acetonide. The mean peak plasma concentration was approximately 0.5 ng/mL (range 0.1 to 1 ng/mL) and occurred at 1.5 hours post dose. The mean plasma drug concentration was less than 0.06 ng/mL at 12 hours and below the assay detection limit at 24 hours. The average terminal half life was 3.1 hours. Dose proportionality was demonstrated in normal subjects and in patients following a single intranasal dose of 110 micrograms or 220 micrograms STERONASE AQ Nasal Spray.

Paediatric population
Following multiple doses intranasal administration of STERONASE AQ, systemic exposures observed in paediatric patients 6 to 12 years of age were similar to those observed in adult patients. Intranasal administration of STERONASE AQ 110 μg once daily in pediatric patients 2 to 5 years of age exhibited similar systemic exposure to that achieved in adult patients at a dose of 220 μg once daily.
The apparent clearance and volume of distribution in pediatric patients 2 to 5 years of age were found to be approximately half of that in adults.