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Pharmacology
PDE Inhibitors
7
Medical
Graduate
03/03/2010

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Cards

Term
phosphodiesterase inhibitors (PDE-Is)
Definition
inhibits PDE and breakdown of cAMP and cGMP, PDE-Is are location-specific, unselective, eg xanthine
Term
xanthines
Definition

unselective PDE-I and adenosine-1 receptor blocker (low dose, increase kidney perfusion)

 

theophylline and aminophylline are asthma drugs, reliever (iv) or controller (po) drugs

Term
xanthine clearance
Definition

1A2 induction

(smoke induces 1A2 [cigs and bbq])

easy to move into toxic range (small therapeutic index)

Term
xanthine side effects
Definition

easily saturable, shifts to zero order kinetics

 

CNS activation and catecholamine release: tachyarrhythmia, N&V, etc

Term
PDE-III inhibitor
Definition

selective

-rinone

inotropic agents in severe cardiac failure

Term
PDE 4 inhibitors
Definition

selective

-milast

used for COPD, reduce inflammation

Term
PDE 5
Definition

block the degradative action of PDE type 5 on cGMP; vasodilation

-afil

side effects due to vasodilation; Sildenafil also inhibits PDE6 in the retina, which is thought to be responsible for the vision changes

mostly 3A4 metabolized

 

sildenafil and vardenafil = short

tadalafil (cave in CAD)= long

 

cave nitrates

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