Drugs Basic Flashcards
Bradykinin
Source, responses (3) and mech
endothelial cells
vasodilation, increased vasc permeability, pain
activation of GPCRS, B2 receptor
Etanercept
soluble TNF R antag
rheumatoid arthritis/Crohns
increased risk of infections
infliximab
TNF mab; IgG binds to neutralize TNFa inhibiting its binding to receptors
rheumatoid arthritis, AI
infxn, iv
anti-inflammatory molecule released by all cells
adenosine
zileuton
inhibits LT synthesis by inhib. 5-LOX in pathway
anti-inflamm; prophylactic tx of mild asthma
zafirlukast
competitive leukotriene receptor antagonist (of LCT4, etc)
anti-inflam, bronchoconstriction, tx of mild asthma
steroids (general mechanism and effects)
transcription activator of anti-inflammatory
inhibition of cytokines, PLA2 (mol that inhibits), COX2, adhesion molecules, leukotrienes
Use in chronic inflammation, chronic astma, gout
4 Therapeutic principles for steroids
- Ther. dose is variable and may change-reevaluate frequently
- a single dose is usually w/o harm; prolonged therapy has lethal potential
- use is not etiological or curative. symptomatic therapy
- Abrupt discontinuation may be life threatening due to adrenal insufficiency
Most potent corticosteroid
Dexamethasone
most potent mineralcorticoid
aldosterone
Metyrapone
blocks 11b hydroxylase
diagnostic test of adrenal insufficiency
Competitive antagonist of progesterone and glucocorticoid receptor
Mifepristone
What is mifepristone used for
Cushings disease
termination of pregnancy
3 Competitive antagonists of mineral corticoids (aldosterone)
Spironolactone, Eplerenone, Drospirenone
Use of Spironolactone and Eplerenone?
Diuretics, inhibit salt and water retention. Treat HTN
Drospirenone- 1 agonist, 2 antagonists
Prog R agonist- w/estrogen in HRT
MC R antag-diuretic,
androgen R antag
