Term
| Action of PDEs (Phosphodiesterases) |
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Definition
| break down of cAMP and cGMP |
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Term
| Tissue localization of PDE3, PDE4, PDE5 and PDE6? |
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Definition
| 3: heart, vascular smooth muscle; 4: lungs, mast cells, vascular smooth muscle; 5: corpus cavernosum, vascular smooth muscle and platelets; 6: retina |
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Term
| xanthines mode of action, examples |
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Definition
| unselective PDE inhibitors (in high doses), but mainly adenosine-1 receptor blockers; caffeine, theophylline, theobromine |
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Term
| Adenosine receptors: A1? A2A? A2B? |
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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) |
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Term
| Aminophylline, IV vs. oral? |
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Definition
xanthine (block adenosine-1 receptors), unselective PDE inhibitor
IV for relief of acute asthma symptoms, oral to control asthma over time. |
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Term
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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 |
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Term
| Xanthine PK metabolism? Inducers? Inhibitors |
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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) |
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Term
| xanthine order of kinetics? side effects? |
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Definition
| zero order above 35 microg/mL; tachyarrhythmia, nausea/vomiting, tremor, seizure, rhabdomyolysis (striated muscle damage) |
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Term
| -rinones mode of action? effect? Examples |
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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 |
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Term
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Definition
| PDE III (cardiac) selective inhibitor |
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Term
| -ilast mode of action, effect, examples |
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Definition
| PDE 4 (lung) selective inhibitors, increase cAMP which reduces mast (inflammatory) cell activation in respiratory tract (for COPD) ex: cilomilast (Ariflo) |
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Term
| -afil mode of action, effect, examples |
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Definition
| PDE 5 (corpus cavernosum) selective inhibitor, increased blood flow to the penis (for ED), examples: sildenafil (Viagra), vardenafil (Levitra), tadalafil (Cialis) |
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Term
| -afils side effects? metabolism? |
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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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