Term
|
Definition
adrenoylitc agent
alpha antagonist-alpha1 selective, reversible
-used for hypertension
-used for BPH
-used for Raynaud's disease |
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Term
|
Definition
adrenoylitc agent
alpha antagonist-alpha1 selective, reversible
-used for hypertension
-used for BPH
-used for Raynaud's disease |
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Term
|
Definition
adrenoylitc agent
alpha antagonist-alpha1 selective, reversible
-used for hypertension
-used for BPH
-used for Raynaud's disease |
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Term
|
Definition
adrenoylitc agent
alpha antagonist-alpha1 selective, reversible
-NOT used for hypertension
-used for BPH; predominant drug for BPH because the predominat alpha1 receptor subtype in prostate is alpha1A receptor and this drug has greatest affinity for it |
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Term
|
Definition
adrenoylitc agent
alpha antagonist-alpha1 selective, reversible
-NOT used for hypertension
-used for BPH |
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Term
|
Definition
adrenoylitc agent
alpha antagonist-alpha1 selective, reversible
-NOT used for hypertension
-used for BPH |
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Term
|
Definition
adrenoylitc agent
alpha antagonist-non-selective, reversible
-used for pheochromocytoma |
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Term
|
Definition
adrenoylitc agent
alpha antagonist- non-selective, irreversible
-used for pheochromocytoma |
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Term
| what's the MOA for the alpha antagonists? |
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Definition
| block the alpha receptor and prevent the binding of NE or EPI |
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Term
| describe how alpha blockers used in pheochromocytoma |
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Definition
tumor of the adrenal medulla that secretes large amounts of EPI (mostly) and NE, which causes an elevation in BP
-blocking alpha1 receptors on vascular smooth m. blocks the ability of Epi and NE to bind to that receptor, thereby cuasing vasodilation and decreasing PVR and a decrease in BP |
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Term
| what's the problem with BPH? |
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Definition
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Term
| How are alpha1 antagonists useeful for BPH? |
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Definition
blocking alpha1 reeptors relaxes smooth muscle in base of bladder and the prostate
END RESULT: improved urine flow |
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Term
| what's the predominate receptor subtype in the prostate? |
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Definition
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Term
| Which receptor subtype does tamsulosin have the greatest affinity for? |
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Definition
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Term
| What's the advantage of using tamsulosin for the treatment of BPH? |
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Definition
| less hypotension (don't get as much vasodilation as with prazosin) |
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Term
| What's happens in Raynaud's disease? |
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Definition
cold --> vasospasm in finger sand toes (painful)
--if you block alpha1 receptors then BV dilate and get rid of vasospasm |
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Term
| what are adverse effects of alpha antagonists? |
|
Definition
-orthostatic hypotension
-->1st dose effect: profound orthostatic hypotension with syncope (-> why should take at bedtime 1st time take it)
-reflex tachycardia (prazosin blocks alpha1 and BP decreases-->baroreceptor-->reflex tachycardia)
-nasal congestion (block alpha1 receptors in nasal mucosa)
-salt and water retention (drop in BP decreases kidney perfusion)
-inhibition of ejaculation (block alpha1 on smooth m. prostate, seminal vesicles, and vas deferens)
-headache (VS contributes to headache), weakness, dizziness |
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Term
| Baroreceptor reflex effect on heart and BV? |
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Definition
stand up-->decrease BP--> baroreceptor acts on CNS which effects:
heart: PS acts M receptors and is -; sym act on B1 and get increase HR and force of contraction
BV: sympathetics acts on alpha1 receptors and get vasoconstriction (especially veins) and icnrease BP |
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Term
| why is constriction of veins so important? |
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Definition
| if no vasoconstriction then blood pools in veins and blood isn't sent back to the heart |
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Term
|
Definition
Beta receptor antagonist
non-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-migraine
-essential tremor
-prophylaxis for esophaageal varice bleeding
-adverse effects:
-CNS (nightmares, lassitude, mental depression)
-bronchospasm |
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Term
|
Definition
Beta receptor antagonist
non-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-migraine
-essential tremor
-prophylaxis for esophaageal varice bleeding
-bronchospasm |
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Term
|
Definition
Beta receptor antagonist
non-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-migraine
-essential tremor
--prophylaxis for esophaageal varice bleeding
-bronchospasm |
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|
Term
|
Definition
Beta receptor antagonist
non-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-essential tremor
-prophylaxis for esophaageal varice bleeding
-bronchospasm |
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|
Term
|
Definition
Beta receptor antagonist
non-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-essential tremor
-prophylaxis for esophaageal varice bleeding
-bronchospasm |
|
|
Term
|
Definition
Beta receptor antagonist
non-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-essential tremor
-prophylaxis for esophaageal varice bleeding
-bronchospasm |
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|
Term
|
Definition
Beta receptor antagonist
Beta1-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-migraine
-adverse effects: CNS (nightmares, lassitude, mental depression)
-bronchospasm |
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Term
|
Definition
Beta receptor antagonist
Beta1-selective, competitive, reversible (high enough [] will hit Beta 2)
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-migraine
-bronchospasm |
|
|
Term
|
Definition
Beta receptor antagonist
Beta1-selective, competitive, reversible
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
-adverse effect
bronchospasm |
|
|
Term
|
Definition
Beta receptor antagonist
Beta1-selective, competitive, reversible(high enough [] will hit Beta 2)
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
adverse effect:
-bronchospasm |
|
|
Term
|
Definition
Beta receptor antagonist
Beta1-selective, competitive, reversible(high enough [] will hit Beta 2)
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
adverse effect:
-bronchospasm |
|
|
Term
|
Definition
Beta receptor antagonist
Beta1-selective, competitive, reversible(high enough [] will hit Beta 2)
therapeutic uses:
-CV diseases (hypertension, ischemia, arrhythmias, MI, heart failure)
-in conjunction with non-selective alpha blocker (i.e. phentolamine or phenoxybenzamine) for pheochromocytoma
adverse effect:
-bronchospasm |
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Term
| What class of drugs can "BEAM" be used for? |
|
Definition
beta1 selective, competitive, reversible beta receptor antagonists
--all star with the letters B, E, A, or M |
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Term
| What's the MOA for Beta receptor antagonists? |
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Definition
| bind to, but don't activate beta adrenergic receptors |
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Term
| what may happen if you administer propranolol (non-selective beta antagonist)without an alpha blocker when treating a pheochromocytoma? |
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Definition
| there will be more activation of the alpha1 receptor, BP will increase, and you'll have unopposed VC b/c have gotten rid of the Beta2 effect; get dramatic increase BP |
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Term
| What are beta receptor antagonists' effect on migraines? |
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Definition
| prophylactic treatment; reduce frequency, severity, and duration of migraine attacks; precise MOA unknown |
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Term
| what's a theory how blocking beta receptors can be helpful for migraines? |
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Definition
| prevent arterial dilation; inhibit renin secretion; decrease AA synthesis and prostaglandin production; may affect serotonin levels |
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Term
| What kind of drug do you use to treat essential tremors? why? |
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Definition
| non-selective beta blocker (i.e. propranolol) because B2 receptors on red, slow contrating skeletal m. cause tremor |
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Term
| What's the main cause of esophageal varices? |
|
Definition
| cirrhosis of the liver and portal hypertension |
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Term
| what are adverse effects with beta receptor antagonists? |
|
Definition
cardiac: bradycardia, AV block, decrease contractile force --> heart failure; hypotension
CNS: nigtmares, lassitude/fatigue, mental depression, insomnia
--->w/lipid-soluble agents (propranolol, metoprolol)
-NVD?
-sexual dysfunction
-increase TAG and decrease HDL-C (not a reason to not use these drugs)
-Bronchospasm
-unopposed VC in patients with peripheral vascular disease b/c no B2 activity
-chronic therapy upregulates beta receptors so if have abrupt withdrawal get rebound hypertension, nervousness, tachycardia, angina |
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Term
| what are some precautions with beta receptor antagonists? |
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Definition
Diabetics
--> hypoglycemia-->activate sympathetic NS; release EPI; EPI/NE act on B2 in the liver-->glycogenolysis and gluconeogenesis-->increase blood glucose and they act on B1 in the heart-->increase HR--> warning sign to eat |
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Term
| Both non-selective and B1 selective blockers are contraindicated in asthma. Why? |
|
Definition
the selectivity of Beta1 blockers may be lost at higher doses
-blocking Beta2 receptors causes bronchoconstriction and thus bronchospasm |
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