Corticosteroids

Corticosteroids

The anti-inflammatory corticosteroids act as glucocorticoid receptor agonists and modulate expression of genes containing the glucocorticoid response element (GRE). Although complex, the response appears to include inhibition of the biosynthesis of pro-inflammatory prostaglandins including prostaglandin E2 (PGE2) and PGI2 (prostacyclin), and leukotrienes (especially leukotriene LTB4).

Note: corticosteroid absorption can occur following topical and local use, so be aware of systemic effects if high doses are used or if treatment is prolonged. Potent or very potent topical corticosteroids should be used under specialist supervision in psoriasis.

Examples in clinical use include:

Beclometasone (prodrug beclometasone dipropionate) is prescribed for prophylaxis of asthma (inhalation), allergic and vasomotor rhinitis and severe inflammatory skin disorders such as eczemas unresponsive to less potent corticosteroids (topical), psoriasis (topical) and as an adjunct to aminosalicylates in acute mild to moderate ulcerative colitis (oral).

Betamethasone provides local treatment of inflammation (short term use in eye drops and ointments, intranasal for inflammatory conditions of the nose, ear drops for eczematous inflammation in otitis externa) and for severe inflammatory skin disorders such as eczemas unresponsive to less potent corticosteroids (topical), psoriasis (topical), suppression of inflammatory and allergic disorders (oral).            

Budesonide is delivered by inhalation as prophylaxis and management for mild to moderate asthma. Intranasal delivery is used to manage allergic and vasomotor rhinitis and nasal polyps.

Deflazacort is an oral therapy for suppression of inflammatory and allergic disorders.     

Dexamethasone is administered orally for suppression of inflammatory and allergic disorders, topically for short-term treatment of ocular inflammation, and as intra-articular injection for local inflammation of joints.

Flumetasone contained in ear drops with clioquinol (antifungal/antiprotozoal drug) is used to manage eczematous inflammation in otitis externa and mild bacterial or fungal infections in otitis externa.

Fluorometholone ophthalmic solutions are prescribed for short term local treatment of ocular inflammation.

Fluticasone is applied topically for severe inflammatory skin conditions (dermatitis, eczema, psoriasis), or by inhalation/intranasal administration for prophylaxis of asthma. 

Hydrocortisone (cortisol). In addition to being used as hormone replacement in adrenocortical insufficiency, hydrocortisone is also used to treat mild eczema (topical), severe/life-threatening acute asthma (i.v.) and acute hypersensitivity reactions and anaphylaxis (given i.v. as an adjunct to adrenaline).

Methylprednisolone is prescribed for suppression of inflammatory and allergic disorders (oral), local inflammation in joints and soft tissues (intra-articular injection) and treatment of graft rejection reactions (i.v.).

Loteprednol is prescribed to manage post-operative ocular inflammation.

Mometasone is prescribed as prophylaxis of (severe) asthma (inhalation), treatment of severe inflammatory skin disorders such as eczemas unresponsive to less potent corticosteroids and psoriasis (topical), as well as prophylaxis and treatment of allergic rhinitis (intranasal).

Triamcinolone by intra- or peri-articular administration is used as treatment of local inflammation of joints and soft-tissues (triamcinolone hexacetonide), deep intramuscular injection for suppression of inflammatory and allergic disorders and intranasal administration for prophylaxis and treatment of allergic rhinitis.

Prednisolone is administered orally for mild to moderate acute asthma or severe or life-threatening acute asthma, severe croup, acute exacerbation of chronic obstructive pulmonary disease and for suppression of inflammatory and allergic disorders (including ulcerative colitis, Crohn’s disease and eczematous inflammation in otitis externa (applied locally to the ear)). Can be used short-term to alleviate ocular inflammation.      

Rimexolone is administered for postoperative ocular inflammation and uveitis.

Corticosteroids- an introduction

This 9-slide slide set created with PowerPoint is a short introduction to corticosteroids, in particular, the glucocorticoids, describing their receptor-mediated effects as well as why they exert both wanted and unwanted effects when used as anti-inflammatory and immunosuppressant drugs. This introduction to the topic of corticosteroids would be appropriate for beginners. Contributed by Christopher Fowler, Umeå University, Sweden.

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