Tiova Rotacap General Medicines

TIOVA Rotacaps

Each rotacap contains:

Tiotropium (as Tiotropium Bromide Monohydrate) a a 18 mcg

Excipienta a a a a ..q.s.

Tiotropium is a long-acting, anti-muscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors, M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3-receptors at the smooth muscle, leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In pre-clinical in vitro as well as in vivo studies, prevention of methacholine induced bronchoconstriction effects was dose-dependent and lasted longer than 24 hours. The long duration is probably due to the very slow dissociation from the M3 receptor, exhibiting a significantly longer dissociation half-life than ipratropium. As an N-quaternary anticholinergic, tiotropium bromide when administered by inhalation, demonstrates acceptable therapeutic range before systemic anticholinergic effects may occur. The bronchodilation following inhalation of tiotropium is predominantly a site-specific effect. Dissociation from M2 receptors is faster than from M3, which in functional in vitro studies, elicited (kinetically controlled) receptor subtype selectivity of M3 over M2. The high potency and slow receptor dissociation found its clinical correlate in significant and long-acting bronchodilation in patients with COPD.

TIOVA Rotacaps........... Each sales pack contains 15 Rotacaps