Anti-Inflammatory Drugs Steroids and NSAIDs RC 195

Corticosteroids, “Steroids” Naturally-occurring hormones produced by the adrenal glands Glucocorticoids: Hydrocortisone Mineralcorticoids: Aldosterone Sex Hormones: Testosterone

Actions of Glucocorticoids Anti-inflammatory Supresses actions of kinins, cytokines, and other mediators of inflammation Maintains microcirculation and minimizes edema Maintains cell membrane integrity Inhibits macrophage movement Inhibition of immune response Stabilizes mast cells Reduces histamine levels Bronchodilation Potentiates catecholamine activity by inhibiting COMT and increasing adenyl cyclase production Decreased cholinergic and alpha stimulation Decreased phosphodiesterase production

Steroid Uses Acute Inflammation Organ Transplant Allergic Inflammation

Steroid Side Effects: “Cushing’s Syndrome” Gluconeogenesis Osteoporosis Physical changes Increased fat production and redistribution Acne Hirsutism Fragile skin Sodium retention Fluid retention Potassium loss and metabolic alkalosis Increased gastric acidity Decreased resistance to infection MDI may cause candida albicans, “thrush” Patients need to rinse mouth after MDI Dependency Both physical and psychological Patients may need to be weaned from steroid therapy

Interaction with other drugs Increased breakdown in the presence of: Dilantin, barbiturates, certain tranquilizers, anti-histamines, ephedrine Decreased breakdown (and greater chance of severe side effects) in the presence of some antibiotics, eg erythromycin

Steroids in Respiratory Care For prevention of inflammation – aerosol For relief of inflammation: systemic

Hydrocortisone Brand name(s): Solu-Cortef, Cortef Given orally or IV Not usually aerosolized because of side effects

Prednisone (Prednisolone) Brand: Deltasone, Delta-Cortef 4X as potent as hydrocortisone Given orally Side effects minimized if given every other day Patient’s usually need to be weaned from it

Methylprednisolone Brand: Solu-Medrol Oral or IV Often used to help relieve airway inflammation

Triamcinolone Brands: Azmacort, Kenalog MDI- to prevent airway inflammation

Dexamethasone Brand: Decadron Often nebulized for acute upper airway inflammation What else is used with it?

Beclomethasone Brands: Vanceril, Beclovent, Becotide MDI– to prevent airway inflammation

Mometasone Furoate Brand: Asmanex DPI “Twisthaler” 220mcg per pff Started as one puff per day in then evening and may go as high two puffs BID

Flunisolide Brand: AeroBid MDI – to prevent airway inflammation Usually effective when given only BID

Fluticasone Brand: Flovent MDI (similar to Flunisolide) Fluticasone is also sold as a combo drug, Advair, which contains fluticasone and salmeterol Taken as a dry powder inhaler (DPI)

Budesonide Brand: Pulmicort MDI – to prevent airway inflammation Seems to get best effects with minimal side effects

NSAIDs Drugs that prevent airway inflammation but usually have less side effects than steroids

Cromolyn Sodium Brands: Intal, Aarane Is a mast cell stabilizer so used to prevent airway inflammation Does not relieve airway inflammation! Often used as an alternative to aerosol steroids in children Administered via Spinhaler (DPI), MDI, nebulizer Usually needs to be administered Q.I.D. May take at least two weeks before any effects are seen

Nedocromil Sodium Brand: Tilade Similar to cromolyn sodium (used to prevent airway inflammation) MDI – usually only needed B.I.D.

NSAIDs: Leukotriene Inhibitors (used to prevent airway inflammation) Zafirlukast (Accolate) Taken as a pill B.I.D. Zileuton (Zyflo) Taken as a pill Q.I.D. Montelukast (Singulair) Taken as a pill just once a day

NSAIDs: Omalizumab (Xolair) Genetically engineered recombinant humanized monoclonal antibody Binds to IgE and prevents it from attaching to mast cells Given sub-Q 1-2 times per month

Case Study Time!