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59 Cards in this Set
- Front
- Back
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 to redistribute coronary blood flow from normal to ischemic areas) 3. mild arteriolar dilation (dec. afterload) |
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Common AE of nitrates?
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throbbing headache
others are: hypotension, dizziness, weakness, rash, tachycardia due to sympathetic activation, and methemoglobinemia |
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One major drug interaction of nitrates?
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ED drugs (PDE5 inhibitors): sildenafil, tadalafil, vardenafil
Profound vasodilation & hypotension is used with erectile dysfunction drugs. "Sil Taps the Vagina" -afil |
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various uses for Nitrates?
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Big ones: all forms of angina - acute and unstable angina - SL NTG take every 5 min up to 3 doses
Take for angina of effort, variant angina, and unstable angina. Take isosorbide dinitrate in combo with hydralazine as a direct vasodilator for HF |
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Best drug for emergency HTN situation?
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nitroprusside (POTENT vasodilator)... but continuous IV only
onset - 30 sec peak - 2 min disappears - 3 min |
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What is nitroprusside metabolized to that could (rarely) cause AE's?
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cyanide and then to thiocyanate, caution with pts that have renal and hepatic impairment
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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, therefore has a longer duration of effect
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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, if the pt is seated or supine, and has marked effects in hypovolemia
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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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Which classes of drugs what increase coronary and regional myocardial blood flow?
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vasodilators, especially CCBs
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Besides angina & HF, what are other uses for nitrates?
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to control hypotension in anesthesia induction, pain associated with anal fissures or hemorrhoids, uterine relaxant to expel placenta, and for impotence
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What is the main beneficial effect of nitrates?
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Decrease in Bp, ventricular volume, & ejection time, which results in reduced myocardial O2 requirement
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What are 2 harmful nitrate effects?
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reflex increase in HR & contractility, which increases myocardial O2 requirement.
reduced diastolic perfusion due to reflex tachy, which reduces myocardial perfusion |
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What is the difference between nitrates & nitroprusside regarding tolerance?
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No tolerance to nitroprusside develops
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What are vasodilator related AE of nitroprusside?
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hypotension, headache, dizziness, palpitations, and diaphoresis
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What are cyanide related AE of nitroprusside?
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sever lactic acidosis, anorexia, nausea, fatigue, disorientation, shallow breathing, hypothyroidism, happens with higher doses > 24-48 hrs
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Drug interactions with nitroprusside - with sympathomimetic drugs
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dopamine, dobutamine, epinephrine, norepinephrine
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what does alpha 2 stimulation effect?
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acts of blood vessels & skeletal muscle and results in vasoconstriction
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Name 2 non-selective alpha receptor antagonist
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Phenoxybenzamine & phentolamine
"Phenox & Phento are NOT SELECTIVE about where they Pee Pee" |
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Name 5 alpha 1 selective alpha receptor antagonist
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Prazosin, Terazosin, Doxazosin, Alfuzosin, and Tamsulosin
"PRincess TERA only DOnates alpha-1 selective ALFalfa TAMiflu" --osin |
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Where are alpha-1A receptors located?
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prostate and bladder neck
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where are alpha-1B receptors located?
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vascular smooth muscle
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Name 1 alpha receptor antagonists that is alpha-2 selective
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Yohimbine
"with alpha 2 you need 2: YOu and Him" |
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What are cardiovascular effect of alpha 1 antagonists?
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fall in BP due to decreased vascular resistance, NO reflex tachycardia, also reduces smooth muscle tone in prostate and neck of bladder
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what are pharmacologic effects of selective alpha 2 antagonism?
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increase sympathetic outflow and potentiate release of NE from nerve endiings.
alpha-2A blocks platelet aggregation in vitro, facilitate insulin release, increase penile blood inflow, decrease penile blood outflow, used to treat erectile dysfunction |
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MOA of phenoybenzamine
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irreversible binding, inhibits reuptake of released NE by presynaptic adrenergic nerve terminals, blocks histamine, acetylcholine, and serotonin receptors
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clinical effects of phenoxybenzamine
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use to reduce BP when sympathetic tone high
vasodilation, decreased BP, reflex tachy, incresed cutaneous blood flow |
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What do you know about phenoybenzamine's half life?
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t 1/2 is long = 24 hrs because of irreversible binding
oral formula |
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What can you use phenonybenzamine for?
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pheochromocytoma to decreased BP, use for BPH (not anymore), and for Raynaud's, frostbite, and acrocyanosis because of increased cutaneous blood flow
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What are 3 AE of phen
oxybenzamine? |
postural hypotension, reflex tachy, and reversible inhibition of ejeculation
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Name a nonselective, competitive inhibitor of alpha receptors and its MOA
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Phentolamine - competitively inhibits alpha 1 and 2 receptors. Also blocks serotonin (5-HT) receptors, cause release of histamine fr mast cells, and block K+ channels
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How would you administer phentolamine to your patient?
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IV only
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CV effects of phentolamine?
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vasodilation and decreased BP
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Other therepeutic uses for phentolamine?
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short term control for HTN in pheochromocytoma and to relieve pseudo-obstruction of bowel in the same disease. Treat HTN due to clonidine withdrawal
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In which patients should you be careful about using phentolamine?
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Those with a history of coronary artery disease or peptic ulcer bc AE are hypotension, reflex tachy, and GI stimulation causing abdominal pain, nausea, and exacerbation of peptic ulcer
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Which alpha 1 receptor antagonist can effect all 3 types of receptors: alpha-1A, alpha-1B, and alpha-1D?
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Prazosin, Terazosin, Doxazosin, Alfuzosin
All the -zosins |
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Which alpha 1 receptor antagonist drugs only distribute to the bladder and prostate?
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Alfuzosin and Tamsulosin
"Alfalfa Tamiflu are weird like that, and only go to the prostate and bladder." |
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Which alpha 1 receptors does Tamsulosin antagonize?
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alpha-1A and alpha-1D
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What are symptoms of Benign Prostetic Hyperplasia?
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hesitancy, weakness of urinary stream, intermittent urinary stream, feeling of incomplete bladder emptying, bladder irritability
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What are the major effect of alpha 1 receptor antagonists?
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decreased PVR and venous return to heart, which leads to decreased cardiac preload, usually no increase in HR
relaxed bladder for increased urine flow decrease size of prostate by apoptotic properties in prostate smooth muscle |
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What favorable effects does alpha 1 selective receptor antagonists have on serum lipids?
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increase HDL, and decreased in LDL and TG
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What is the dose for alpha 1 selective receptor antagonists and what is the exception?
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once daily at bedtime except for
prazosin 2-3 x day alfuzosin must be taken with food |
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Which alpha 1 selective receptor antagonists do you use for HTN? 3
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Prazosin, Terazosin, and Doxazosin
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Which 4 alpha 1 selective receptor antagonists do you use for BPH?
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all except Prazosin:
Terazosin, Doxazosin, Alfuzosin, and Tamsulosin |
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Which alpha 1 selective receptor antagonist do you not use for HTN and why?
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Alfuzosin and Tamsulosin because they have little effect on blood pressure and have uroselectivity
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When should you not give Alfuzosin to a pt?
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If the pt has moderate to sever hepatic dysfunction because it is metabolized via P450 3A4
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