Transcript Anti-inflammatory Drugs Lecture Notes Page

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, antihistamines, 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!