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59 Cards in this Set

  • Front
  • Back
What is prinzmetal's angina?
variant angina (oxygen delivery dec. b/c of reversible coronary vasospasm)
What drugs address demands of preload and afterload?
nitrates and CCBs
What drugs address the demands of HR and contractility?
beta-blockers and some CCBs
MOA of nitrates?
cause vasodilation via: releasing NO which activates guanylyl cyclase which inc. cGMP which relaxes all smooth muscles! yay
What one thing do you need to know about nitrate therapy?
tolerance develops w/ continuous administration. need 8-12 hours nitrate free per day
antianginal beneficial effects of nitrates are due to what 3 things?
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)
Common AE of nitrates?
throbbing headache

others are: hypotension, dizziness, weakness, rash, tachycardia due to sympathetic activation, and methemoglobinemia
One major drug interaction of nitrates?
ED drugs (PDE5 inhibitors): sildenafil, tadalafil, vardenafil

Profound vasodilation & hypotension is used with erectile dysfunction drugs.

"Sil Taps the Vagina" -afil
various uses for Nitrates?
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
Best drug for emergency HTN situation?
nitroprusside (POTENT vasodilator)... but continuous IV only

onset - 30 sec
peak - 2 min
disappears - 3 min
What is nitroprusside metabolized to that could (rarely) cause AE's?
cyanide and then to thiocyanate, caution with pts that have renal and hepatic impairment
3 main responses of alpha-1 stimulation?
1. contraction of most vascular smooth muscle
2. contraction of urinary bladder
3. contraction of prostate
What drug irreversibly inhibits alpha-1 receptors?
phenoxybenzamine, therefore has a longer duration of effect
Magnitude of cardiovascular effects of alpha-1 antagonism depends largely on what?
the activity of the sympathetic nervous system at the time, if the pt is seated or supine, and has marked effects in hypovolemia
What is yohimbine used for?
erectile dysfunction (alpha-2 antagonist)
Pt. has adrenal medullary tumor (or sympathetic neuron tumor). What can you give to treat?
phenoxybenzamine; short-term: phentolamine
70-80% of alpha-receptors in the prostate are what subtype?
alpha-1A
What 2 clinical settings do you want to use SELECTIVE alpha-blockers?
HTN and benign prostatic hypertrophy
What alpha-1 blocker must be taken w/ food?
alfuzosin
Biggest AE of alpha-1 selective blockers?
marked postural hypotension and syncope (others: dizziness, sexual dysfunction)
What alpha-1 selective blockers are useful for treating HTN?
doxazosin, prazosin, and terazosin
3 biggest AE's of tamsulosin?
impaired ejaculation, orthostasis, and intraoperative floppy iris syndrome
Which classes of drugs what increase coronary and regional myocardial blood flow?
vasodilators, especially CCBs
Besides angina & HF, what are other uses for nitrates?
to control hypotension in anesthesia induction, pain associated with anal fissures or hemorrhoids, uterine relaxant to expel placenta, and for impotence
What is the main beneficial effect of nitrates?
Decrease in Bp, ventricular volume, & ejection time, which results in reduced myocardial O2 requirement
What are 2 harmful nitrate effects?
reflex increase in HR & contractility, which increases myocardial O2 requirement.

reduced diastolic perfusion due to reflex tachy, which reduces myocardial perfusion
What is the difference between nitrates & nitroprusside regarding tolerance?
No tolerance to nitroprusside develops
What are vasodilator related AE of nitroprusside?
hypotension, headache, dizziness, palpitations, and diaphoresis
What are cyanide related AE of nitroprusside?
sever lactic acidosis, anorexia, nausea, fatigue, disorientation, shallow breathing, hypothyroidism, happens with higher doses > 24-48 hrs
Drug interactions with nitroprusside - with sympathomimetic drugs
dopamine, dobutamine, epinephrine, norepinephrine
what does alpha 2 stimulation effect?
acts of blood vessels & skeletal muscle and results in vasoconstriction
Name 2 non-selective alpha receptor antagonist
Phenoxybenzamine & phentolamine

"Phenox & Phento are NOT SELECTIVE about where they Pee Pee"
Name 5 alpha 1 selective alpha receptor antagonist
Prazosin, Terazosin, Doxazosin, Alfuzosin, and Tamsulosin

"PRincess TERA only DOnates alpha-1 selective ALFalfa TAMiflu"

--osin
Where are alpha-1A receptors located?
prostate and bladder neck
where are alpha-1B receptors located?
vascular smooth muscle
Name 1 alpha receptor antagonists that is alpha-2 selective
Yohimbine

"with alpha 2 you need 2: YOu and Him"
What are cardiovascular effect of alpha 1 antagonists?
fall in BP due to decreased vascular resistance, NO reflex tachycardia, also reduces smooth muscle tone in prostate and neck of bladder
what are pharmacologic effects of selective alpha 2 antagonism?
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
MOA of phenoybenzamine
irreversible binding, inhibits reuptake of released NE by presynaptic adrenergic nerve terminals, blocks histamine, acetylcholine, and serotonin receptors
clinical effects of phenoxybenzamine
use to reduce BP when sympathetic tone high

vasodilation, decreased BP, reflex tachy, incresed cutaneous blood flow
What do you know about phenoybenzamine's half life?
t 1/2 is long = 24 hrs because of irreversible binding

oral formula
What can you use phenonybenzamine for?
pheochromocytoma to decreased BP, use for BPH (not anymore), and for Raynaud's, frostbite, and acrocyanosis because of increased cutaneous blood flow
What are 3 AE of phen
oxybenzamine?
postural hypotension, reflex tachy, and reversible inhibition of ejeculation
Name a nonselective, competitive inhibitor of alpha receptors and its MOA
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
How would you administer phentolamine to your patient?
IV only
CV effects of phentolamine?
vasodilation and decreased BP
Other therepeutic uses for phentolamine?
short term control for HTN in pheochromocytoma and to relieve pseudo-obstruction of bowel in the same disease. Treat HTN due to clonidine withdrawal
In which patients should you be careful about using phentolamine?
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
Which alpha 1 receptor antagonist can effect all 3 types of receptors: alpha-1A, alpha-1B, and alpha-1D?
Prazosin, Terazosin, Doxazosin, Alfuzosin

All the -zosins
Which alpha 1 receptor antagonist drugs only distribute to the bladder and prostate?
Alfuzosin and Tamsulosin

"Alfalfa Tamiflu are weird like that, and only go to the prostate and bladder."
Which alpha 1 receptors does Tamsulosin antagonize?
alpha-1A and alpha-1D
What are symptoms of Benign Prostetic Hyperplasia?
hesitancy, weakness of urinary stream, intermittent urinary stream, feeling of incomplete bladder emptying, bladder irritability
What are the major effect of alpha 1 receptor antagonists?
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
What favorable effects does alpha 1 selective receptor antagonists have on serum lipids?
increase HDL, and decreased in LDL and TG
What is the dose for alpha 1 selective receptor antagonists and what is the exception?
once daily at bedtime except for

prazosin 2-3 x day
alfuzosin must be taken with food
Which alpha 1 selective receptor antagonists do you use for HTN? 3
Prazosin, Terazosin, and Doxazosin
Which 4 alpha 1 selective receptor antagonists do you use for BPH?
all except Prazosin:

Terazosin, Doxazosin, Alfuzosin, and Tamsulosin
Which alpha 1 selective receptor antagonist do you not use for HTN and why?
Alfuzosin and Tamsulosin because they have little effect on blood pressure and have uroselectivity
When should you not give Alfuzosin to a pt?
If the pt has moderate to sever hepatic dysfunction because it is metabolized via P450 3A4