Pharmacokinetics of intranasal corticosteroids.
Topical administration of corticosteroids can reduce the total dose of corticosteroid required to treat the patient and minimize side effects. This logic has led to the development of intranasal corticosteroids (INCS) for allergic and perennial rhinitis. The second generation of these compounds includes beclomethasone dipropionate, budesonide, flunisolide, fluticasone propionate, mometasone furoate, and triamcinolone acetonide. There is evidence that the INCS are effective in rhinitis; however, there is concern about the potential for these compounds to cause growth suppression. In one study, beclomethasone dipropionate significantly reduced growth in children; however, treatment of children with mometasone furoate nasal spray for 1 year showed no signs of growth suppression. It is evident that the differences among INCS lie in their pharmacokinetics. Structural differences among the various INCS influence their metabolism. The goal of INCS therapy is to have a high ratio of topical to systemic activity. The drug delivery device, absorption of the drug, and drug distribution all contribute to effective topical activity of an INCS. In addition, individual drug metabolism and elimination (half-life and drug clearance) also contribute to the therapeutic index of a drug. Overall, the second-generation INCS cause minimal systemic effects at recommended doses.
Szefler
S J
SJ
University of Colorado Health Sciences Center and the National Jewish Center Medical and Research Center, USA.
D000042:Absorption; D000281:Administration, Intranasal; D000305:Adrenal Cortex Hormones / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000328:Adult; D000730:Androstadienes / Q000493:pharmacokinetics; D018926:Anti-Allergic Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000893:Anti-Inflammatory Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001507:Beclomethasone / Q000493:pharmacokinetics; D019819:Budesonide / Q000493:pharmacokinetics; D002648:Child; D016503:Drug Delivery Systems; D005446:Fluocinolone Acetonide / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D000068298:Fluticasone; D006801:Humans; D000068656:Mometasone Furoate; D011244:Pregnadienediols / Q000493:pharmacokinetics; D012221:Rhinitis, Allergic, Perennial / Q000097:blood / Q000188:drug therapy; D006255:Rhinitis, Allergic, Seasonal / Q000097:blood / Q000188:drug therapy; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D014222:Triamcinolone Acetonide / Q000493:pharmacokinetics
D000305:Adrenal Cortex Hormones; D000730:Androstadienes; D018926:Anti-Allergic Agents; D000893:Anti-Inflammatory Agents; D011244:Pregnadienediols; D000068656:Mometasone Furoate; D005446:Fluocinolone Acetonide; D019819:Budesonide; C007734:flunisolide; D000068298:Fluticasone; D014222:Triamcinolone Acetonide; D001507:Beclomethasone