ine inhibited that channel at a concentration 1685 times greater than the Cmax obtained after the administration of 10 mg of rupatadine. Desloratadine, the metabolite with the greatest activity, had no effect at a 10 micromolar concentration. Studies of tissue distribution in rats with radiolabelled rupatadine showed that rupatadine does not accumulate in heart tissue.
In the rat, a significant reduction of male and female fertility occurred at the high dose of 120 mg/kg/day, providing Cmax 268 times those measured in humans at the therapeutic dose (10 mg/day). Foetal toxicity (growth delay, incomplete ossification, minor skeletal findings) was reported in rats at maternotoxic dose-levels only (25 and 120 mg/kg/day). In rabbits, no evidence of developmental toxicity was noted at doses up to 100 mg/kg. The developmental No Adverse Effect Levels were determined at 5 mg/kg/day in rats and 100 mg/kg/day in rabbits, yielding Cmax 45 and 116 times higher, respectively, than those measured in humans at the therapeutic dose (10 mg/day).
6. Pharmaceutical particulars
6.1 List of excipients
Pregelatinised maize starch
Microcrystalline cellulose
Red iron oxide (E-172)
Yellow iron oxide (E-172)
Lactose monohydrate
Magnesium stearate
6.2 Incompatibilities
Not applicable
6.3 Shelf life
3 years
6.4 Special precautions for storage
Keep the blister in the outer carton in order to protect from light.
6.5 Nature and contents of container
PVC/PVDC/aluminium blister.
Packs of 3, 7, 10, 15, 20, 30, 50 and 100 tablets. Not all pack sizes may be marketed.
6.6 Special precautions for disposal and other handling
No special requirements.
Any unused product or waste material should be disposed of in accordance with local requirements.
7. Marketing authorisation holder
J. Uriach & Cía., S.A.
Av. Camí Reial, 51-57
08184 Palau-solità i Plegamans (Spain)
8. Marketing authorisation number(s)
PL 11906/0007
9. Date of first authorisation/renewal of the authorisation
24/10/2007
10. Date of revision of the text
10/02/2014
Company Contact Details
GlaxoSmithKline UK
|
