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54 Cards in this Set
- Front
- Back
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What is prinzmetal's angina?
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variant angina (oxygen delivery dec. b/c of reversible coronary vasospasm)
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What drugs address demands of preload and afterload?
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nitrates and CCBs
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What drugs address the demands of HR and contractility?
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beta-blockers and some CCBs
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MOA of nitrates?
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cause vasodilation via: releasing NO which activates guanylyl cyclase which inc. cGMP which relaxes all smooth muscles! yay
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What one thing do you need to know about nitrate therapy?
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tolerance develops w/ continuous administration. need 8-12 hours nitrate free per day.
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antianginal beneficial effects of nitrates are due to what 3 things?
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1. pronounced dilation of large veins (inc. preload)
2. preferential dilation (of large epicardial arteries) 3. mild arteriolar dilation (dec. afterload) |
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Common AE of nitrates?
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throbbing headache
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One major drug interaction of nitrates?
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ED drugs (PDE5 inhibitors): sildenafil, tadalafil, vardenafil
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various uses for Nitrates?
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Big ones: all forms of angina, HF (there are other uses)
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Best drug for emergency HTN situation?
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nitroprusside (POTENT vasodilator)... but IV only
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What is nitroprusside metabolized to that could (rarely) cause AE's?
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cyanide
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3 main responses of alpha-1 stimulation?
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1. contraction of most vascular smooth muscle
2. contraction of urinary bladder 3. contraction of prostate |
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What drug irreversibly inhibits alpha-1 receptors?
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phenoxybenzamine.
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Magnitude of cardiovascular effects of alpha-1 antagonism depends largely on what?
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the activity of the sympathetic nervous system at the time
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What is yohimbine used for?
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erectile dysfunction (alpha-2 antagonist)
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Pt. has adrenal medullary tumor (or sympathetic neuron tumor). What can you give to treat?
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phenoxybenzamine; short-term: phentolamine
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70-80% of alpha-receptors in the prostate are what subtype?
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alpha-1A
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What 2 clinical settings do you want to use SELECTIVE alpha-blockers?
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HTN and benign prostatic hypertrophy
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What alpha-1 blocker must be taken w/ food?
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alfuzosin
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Biggest AE of alpha-1 selective blockers?
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marked postural hypotension and syncope (others: dizziness, sexual dysfunction)
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What alpha-1 selective blockers are useful for treating HTN?
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doxazosin, prazosin, and terazosin
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3 biggest AE's of tamsulosin?
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impaired ejaculation, orthostasis, and intraoperative floppy iris syndrome
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According to McRae... the 4 determinants of myocardial oxygen demand?
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HR, contractility, preload, afterload
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What is best to give a pt. that is having trouble meeting the supply requirements in the myocardial oxygen balance?
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vasodilators esp. CCB's... help increase coronary BF and regional myocardial BF
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Based on increasing nitrate dosage levels, which vessel types dilate first/last?
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small does- large veins dilate first
large dose- arteries dilate |
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What is the most commonly used nitrate?
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nitroglycerin (SL administration is mainstay of tx)
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Order NTG, ISDN, and mononitrate in terms of onset.... in terms of duration
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Onset, fast to slow: NTG (SL), ISDN (oral), mononitrate
Duration, shot to long: NTG (SL), ISDN (oral std.), monotitrate |
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What two drugs can be combined to create a direct acting vasodilator for CHF pts?
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isosorbid dinitrate (ISDN) and hydralazine
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What are some potential harmful reflexes seen w/ nitrate treatment?
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reflex inc, in HR and contractility and subsequent reduced diastolic perfusion
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What is an EXTREMELY potent IV-only vasodilator?
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nitroprusside... dilates arterioles and venules (very quick but short-acting)
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What are cyanide-related AE's?
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severe lactic acidosis, anorexia, nausea, fatigue, disorientation, shallow breathing, absent reflexes, hypothyroidism
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What is the main effector organ and response w/ alpha-2 stimulation?
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Effector: blood vessels of skeletal muscle
Response: vasoconstriction |
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2 Reversible (competitive) alpha-blockers?
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phentolamine and prazosin (duration of action depends on dissociation constant and half-life)
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Non-selective (at least not highly) alpha-blockers?
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phenoxybenzamine (irreversible)
phentolamine (reversible) |
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5 alpha-1 blockers? (hint: all have same ending)
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prazosin
terazosin doxazosin alfuzosin tamsulosin |
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alpha-2 selective blocker?
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yohimbine
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where are alpha-1B receptors found?
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vascular smooth muscle
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Cardiovascular effects of alpha-1 antagonism?
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inhibits vasoconstriction (induced by CATECHOLAMINES) seen both in arterioles and veins
Result: dec. BP (via dec. TPR) |
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Effects (main) of selective alpha-2 antagonism?
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potentiate the release of NE from nerve ending leading to activation of alpha-1 and beta-1 receptors in heart and peripheral vasculature
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MOA of phenoxybenzamine?
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(alpha-1 > 2)
inhibits reuptake of released NE by presynaptic adrenergic nerve terminals Blocks histamine (H1), Ach and serotonin receptors BINDS COVALENTLY |
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Clinical effects of phenoxybenzamine?
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vasodilation
dec. BP reflex tachy inc. cutaneous BF |
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What are 2 therapeutic uses for phenoxybenzamine?
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pheochromocytoma and peripheral vasospastic disorders (raynaud's)
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3 AE's of phenoxybenzamine?
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postural hypotension, reflex tachy, reversible inhibition of ejaculation .... uh i ain't EVER taking this one
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What are 4 effects of phentolamine? side note: this is given IV only!
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1. competitive inhibitor of alpha receptors
2. can block 5-HT receptors 3. cause histamine release from mast cells 4. block K+ channels |
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What are therapeutic uses for phentolamine?
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1. short-term control of HTN in pheochromocytoma
2. releive pseud-obstruction of bowel in pheo pt.s 3. local prevention of dermal necrosis (after extravasation of alpha-agonist) 4. treat HTN crisis due to clonidine w/drawal .... these largely mean nothing to me. what about you? this is so relevant |
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Imporant AE's of phentolamine?
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1. hypotension
2. reflex cardiac stim. 3. GI stim (exacerbate peptic ulcer!) |
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In what 2 pt.s should you use phentolamine w/ caution?
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patients w/ history of CAD or peptic ulcer (due to AE's)
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Which alpha blocker is uroselective?
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alfuzosin
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What receptor subtypes does tamsulosin block?
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alpha-1A and 1D
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I have a going problem. What class of drugs will help me?
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alpha-1 selective blockers (smooth muscle dilation of bladder trigone and sphincter and prostate)
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What drugs block alpha-1A, 1B, and 1D
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terazosin, doxazosin, prazosin, alfuzosin (not tamsulosin)
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Except for prazosin (2-3 x daily), what is the dosing for alpha-1 blockers?
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once daily (ideally at bedtime)
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What are two DOCs (probably) for BPH (benign prostatic hypertrophy)?
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1. tamsulosin aka flowmax
2. alfuzosin aka uroxatral (it's uroselective!) |
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As far as drug interaction, what do you want to avoid when giving a pt. alfuzosin?
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anything that inhibits CYP450 3A4.... don't give to peeps w/ moderate to severe hepatic dysf.
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