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FIU - PDE inhibitors
PDE inhibitors
13
Pharmacology
Professional
12/21/2011

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Cards

Term
Action of PDEs (Phosphodiesterases)
Definition
break down of cAMP and cGMP
Term
Tissue localization of PDE3, PDE4, PDE5 and PDE6?
Definition
3: heart, vascular smooth muscle; 4: lungs, mast cells, vascular smooth muscle; 5: corpus cavernosum, vascular smooth muscle and platelets; 6: retina
Term
xanthines mode of action, examples
Definition
unselective PDE inhibitors (in high doses), but mainly adenosine-1 receptor blockers; caffeine, theophylline, theobromine
Term
Adenosine receptors: A1? A2A? A2B?
Definition
Are are purinergic (activated by purines), activated A1 in heart lowers heart rate (xanthines block and raise HR), A2A: coronary artery vasodilation, A2B bronchiconstriction (not numerous enough to be affected by xanthines, unless asthmatic)
Term
Aminophylline, IV vs. oral?
Definition
xanthine (block adenosine-1 receptors), unselective PDE inhibitor
IV for relief of acute asthma symptoms, oral to control asthma over time.
Term
Xanthine PD effects?
Definition
Non-selective PDE-inhibition (cAMP and cGMP up causing smooth muscle relaxation and striated muscle contraction); adenosine receptor antagonist (HR up), increases catecholamine levels
Term
Xanthine PK metabolism? Inducers? Inhibitors
Definition
1A2, inducers (clear faster): Smoke, high protein/low carbs, omeprazole (GERD, ulcer), barbiturates (sedative/seizure), carbamazepine (seizure), phenytoin (seizure), rifampin (orange color); Inhibitors (clear slower): high carbs/low protein, cimetidine (H2 blocker, stomach acid), Fluvoxamine (SSRI, anti-depressant), Quinolones, Macrolids (erythromycin)
Term
xanthine order of kinetics? side effects?
Definition
zero order above 35 microg/mL; tachyarrhythmia, nausea/vomiting, tremor, seizure, rhabdomyolysis (striated muscle damage)
Term
-rinones mode of action? effect? Examples
Definition
PDE III (cardiac) selective inhibitors. Increase cAMP and thus cardiac muscle contraction (increase HR/positive inotropes), also vasodilation (net O2 consumption/bp the same); ex: amrinone, milrinone, vesnarinone
Term
Enoximome
Definition
PDE III (cardiac) selective inhibitor
Term
-ilast mode of action, effect, examples
Definition
PDE 4 (lung) selective inhibitors, increase cAMP which reduces mast (inflammatory) cell activation in respiratory tract (for COPD) ex: cilomilast (Ariflo)
Term
-afil mode of action, effect, examples
Definition
PDE 5 (corpus cavernosum) selective inhibitor, increased blood flow to the penis (for ED), examples: sildenafil (Viagra), vardenafil (Levitra), tadalafil (Cialis)
Term
-afils side effects? metabolism?
Definition
sildenafil and vardenafil inhibit PDE 6 (retina, night blindness), tadalafil inhibits PDE 11 (skeletal muscle = back pain); mostly 3A4 (some 2C9) and excreted in feces
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