Nasonex (Mometasone)
Asmanex® Twisthaler®, Elocon®, Nasonex®
Classification:
Dermatological Agents
- Topical Antiinflammatory Agents
Hormones and Hormone Modifiers
Respiratory Agents
- Respiratory Antiinflammatory Agents
Description: Mometasone is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. It is used topically to relieve the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses and psoriasis and intranasally for symptoms of perennial or seasonal allergic rhinitis. Since mometasone is resistant to metabolism in the skin, repeated applications may lead to a depot effect and prolonged actions, increased side effects, and an increased risk of systemic absorption. Medium potency topical corticosteroids, such as mometasone, may be used on the face or intertriginous areas for limited periods. Topical mometasone was first approved by the FDA in 1987 and is now off-patent. Intranasal mometasone (Nasonex®) was approved by the FDA in 1997, with a scent-free formulation approved by the FDA in 2004. In December 2004 intranasal mometasone (Nasonex®) was approved for the treatment of nasal polyps in adults. A once-daily dry-powder respiratory inhalational form of mometasone (Asmanex® Twisthaler®) was FDA appproved March 30, 2005 for the preventative treatment of asthma in patients 12 years of age and older.
Mechanism of Action: Topical corticosteroids exhibit anti-inflammatory, antipruritic, and vasoconstrictive properties. At the cellular level, corticosteroids induce peptides called lipocortins. Lipocortins antagonize phospholipase A2, an enzyme which causes the breakdown of leukocyte lysosomal membranes to release arachidonic acid. This action decreases the subsequent formation and release of endogenous inflammatory mediators including prostaglandins, kinins, histamine, liposomal enzymes and the complement system. Early anti-inflammatory effects of topical corticosteroids include the inhibition of macrophage and leukocyte movement and activity in the inflamed area by reversing vascular dilation and permeability. Later inflammatory processes such as capillary production, collagen deposition, keloid (scar) formation also are inhibited by corticosteroids. Clinically, these actions correspond to decreased edema, erythema, pruritus, plaque formation and scaling of the affected skin.
In the treatment of allergies, intranasal mometasone reduces allergic responses of several cell types (e.g., mast cells and eosinophils) involved in the allergic response by the same cellular mechanism as the topical corticosteroids. Clinically, symptoms such as rhinorrhea and postnasal drip, nasal congestion, sneezing, and pharyngeal itching are reduced.
Asmanex Twisthaler Powder for Inhalation(Inhalant 220 mcg/actuation)
Pharmacokinetics: Mometasone is administered topically to the skin as a cream, lotion or ointment, and intranasally as a spray. Absorption after topical administration to the skin is determined by several factors including the vehicle, and the integrity of the epidermal barrier. Occlusive dressings for up to 24 hours have not been shown to increase penetration; however, occlusion for 96 hours markedly enhances topical corticosteroid penetration. In healthy volunteers with normal skin, approximately 0.7% of the applied mometasone 0.1% ointment was absorbed systemically over an 8-hour period after a single application; absorption from the cream and lotion formulations occurs to a similar extent. Inflammation and/or other diseases of the skin may increase percutaneous absorption. The amount of mometasone absorbed after intranasal administration has not been determined; plasma concentrations are undetectable. Once in the systemic circulation, mometasone undergoes extensive metabolism to multiple metabolites. Excretion is primarily in the bile, and to a limited extent, in the urine.
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[ Revised 1/11/2006 10:03:00 PM ]
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