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58 Cards in this Set
- Front
- Back
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vasodilation→ ↓TPR→ ↓BP
relax bladder sphinchter ↓sexual fxn |
alpha 1 receptor inhibition
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↑BP ↑HR generalized symp response
↑sympathetic outflow from CNS ↑release of NE from adrenergic neurons peripherally |
Alpha 2 receptor inhibition
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What is the MOA of Phenoxybenzamine?
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inhibition of a1 and a2 receptors
alkylates a receptors which is a non-competitive block |
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What is the mechanism behind phenoxybezamines reversal of high dose Epi vaso constriction?
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block a ---> unmask B2
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WHat are 2 main effects of Phenoxybenzamine?
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vaso dilation which leads to TPR
Reflex tachycardia |
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WHat are the kinetics of Phenoxybenzamine?
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slow onset
Long Lasting orrally effective |
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What can phenoxybenzamine be used to treat?
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Tx for:
Pheochromo reversible spastic disease |
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WHat are contraindications to phenoxybenzamine?
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tachy-arrhyth-angina
ortho hypo boner problems |
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What does phenoxybenamine inhibit more, a1 or a2?
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a1
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What is the MOA of phentolamine?
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competitive inhibition of a1 = a2
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What are the main differences b/w phenoxybenzamine and phentolamine?
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t1/2 is shorter
IV only more prominent rflex tachycardia |
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What are 3 main uses for phentolamine?
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hypertensive crises
surgical intervation of pheochromo reversible vasospastic disease |
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Prazosin
Tamulosin |
Relatively specific a1 - receptor antagonists
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What are the effects of Prazosin?
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arteriolar dilation, which leads to decreased TPR and decreased BP
relaxation of bladder sphincter |
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WHy would prazosin be used for BPH?
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will decrease urinary retention
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What can often happen upon the first dose of prazosin?
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precipitous drop in BP causing syncope
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What is a selective a1A inhibitor that relaxes bladder sphincter and is often used for BPH?
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Tamulosin (flomax)
(watch out for syncope with this drug) |
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What happens if you use Yohimbine to block a2 receptors?
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increased sympathetic outflow with ↑BP ↑HR
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What is a possible, but not FDA approved use for Yohimbine?
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Sex dysfunction
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What B receptor inhibition will cause the following:
↓heart automaticity ↓contractility ↓conduction velocity ↓renin secretion ↓lipolysis |
B1 receptor blockade
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Bronchoconstriction
↑TPR ↓glycogenolysis |
B2 receptor inhibition
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What does propranolol do to the heart?
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↓automaticity
↓contractility ↓MVO2 ↓conduction velocity |
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What is the long term effect of propanonlol?
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equivocal effect of TPR
↓CO ↓renin release |
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What will propranolol do to coronary blood flow?
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↓coronary blood flow
↓MVO2 ↓B-mediated coronary vasodilation |
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What will propranolol do to the glycogenolic response induced by Epi?
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it will decrease it
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What will propranolol do to lipolysis?
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↑Triglycerides
↓FFA ↓Lipolysis |
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What will propranolol do to HDL?
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↓HDL
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Where is propranolol metabolized?
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liver
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What is bioavaialbitlty of propranolol?
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poor
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When propranolol is used to treat pheochromo, what is used in conjuction?
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alpha receptor agonist
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besides treating the tachy in hyperthroidism, what else will propranolo do?
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↓T4 metabolism to T3
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Why is propranolol given for IHSS?
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increase in outflow
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Why is propranolol given for Htn?
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↓CO
↓renin release |
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Why is propranolol given for hronic stable angina?
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↓MVO2
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What else is propranolol used for ?
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migraines
stage fright essential tremors |
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What conduction problem can propranolol cause?
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AV block
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Why should propranolol be avoided in diabetics?
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-augmentation of insulin induced hypoglycemia
-inhibition of tachycardia in response to hypoglycemia |
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What are two respiratory contraindications of propranolol?
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asthma
COPD |
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What kind of angina will be made worse by propranolol?
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variant
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Why would Timolol and Nadolol have lower CNS side effects?
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lower lipid solubility
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Besides timolol, what else can be given for glaucoma?
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levobunolol, metipranol
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What are two cardioselective B1 - receptor antagonists?
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Metoprolol (atenolol)
Esmolol |
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What happens at high doses of metoprolol?
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lose B1 o2 selectivity
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Which cardioselective B blockers are used for CHF and Htn?
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Meteoprolol, Bisoprolol
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Which cardioselective B blocker is used for Htn and glaucoma?
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betaxolol
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Which conditions are less affected by Metoprolol than propranolol?
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COPD
Raynauds Diabetes |
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-short acting cardioselective B Blocker
-metabolized by red cell esterase --> t1/2 = mins IV antiarrhythmic |
Esmolol
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What is a possible advantage in B Blockers that have Intrinsic SympathoMIMETIC activity?
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a general reduction in typical side effects and less effect on conditions in which B Blockers may be contraindicated
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Pindolol
Acebutolol |
B Blockers with ISA
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Which has more ISA of pindolol or acebutolol?
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pindolol
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This drug has Non-specific B Blocker activity as well as antioxidant and alpha 1 blocking activity?
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Carvedilol, Labetalol
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Generally, carvedilol/labetalol have the typical side effects of B Blockers, what is a particular risk with these drugs?
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severe hypotension
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This drug is cardioselective for B1 blockade and alos works via NO mediated vasodilation?
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Nebivolol
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What does carvedilol do to TPR, HR, CO, HDL?
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↓TPR
↑HDL +/- HR and CO |
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Will nebivolol affect HDL
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probably not
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What will Nebivolol do to TPR, HR, and CO?
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↓TPR
+/- HR and CO |
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What is the therapeutic use for Carvedilol?
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Htn
mild/severe CHF |
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What is the therapeutic use for Nebivolol?
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Htn
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