Topical nonsteroidal anti-inflammatory drugs the importance of drug delivery and therapeutic outcome

Apply to the affected area and massage into the skin gently. Always wash your hands after you have finished rubbing the cream, gel or spray into the skin. This is to make sure that you avoid rubbing this medicine into sensitive areas of the body such as the eyes. Do not apply to skin that is broken, or near the eyes, nose, mouth, genital or bottom (anal) areas. Do not use plasters or bandages (dressings) on top of these medicines. Generally these medicines are applied to the skin 2-4 times a day. However, for specific advice for your medicine, see the leaflet that comes inside the packet.

Crisaborole topical ointment, 2% (formerly known as AN2728) is a benzoxaborole, nonsteroidal, topical, anti-inflammatory phosphodiesterase 4 (PDE4) inhibitor investigational compound that recently completed phase 3 studies for the treatment of mild to moderate atopic dermatitis (AD). The unique configuration of boron within the crisaborole molecule enables selective targeting and inhibition of PDE4, an enzyme that converts the intracellular second messenger 3'5'-cyclic adenosine monophosphate (cAMP) into the active metabolite adenosine monophosphate (AMP). By inhibiting PDE4 and thus increasing levels of cAMP, crisaborole controls inflammation. The use of boron chemistry enabled synthesis of a low-molecular-weight compound (251 daltons), thereby facilitating effective penetration of crisaborole through human skin. In vitro experiments showed that crisaborole inhibits cytokine production from peripheral blood mononuclear cells in a pattern similar to other PDE4 inhibitors and distinct from corticosteroids. Crisaborole also displayed topical anti-inflammatory activity in a skin inflammation model. Once crisaborole reaches systemic circulation after topical application, it is metabolized to inactive metabolites. This limits systemic exposure to crisaborole and systemic PDE4 inhibition. In phase 1 and 2 clinical studies, crisaborole ointment, 2% was generally well tolerated and improved AD disease severity scores, pruritus, and all other AD signs and symptoms. Two large, randomized, controlled, phase 3, pivotal clinical trials assessing the efficacy and safety of crisaborole topical ointment, 2% in children, adolescents, and adults with mild to moderate AD were recently completed with positive results.

Topical nonsteroidal anti-inflammatory drugs the importance of drug delivery and therapeutic outcome

topical nonsteroidal anti-inflammatory drugs the importance of drug delivery and therapeutic outcome

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