Term
| adrenoceptor antagonists block what type(s) of receptors |
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Definition
| can block alpha-adrenoceptors, beta-adrenoceptors, or both |
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Term
| therapeutic effects of adrenoceptor antagonists |
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Definition
| blockade of alpha1 or beta1 adrenoceptors |
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Term
| adverse effects of adrenoceptor antagonists |
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Definition
| blockade of alpha2 or beta 2 adrenoceptors |
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Term
| outcome of blockade of alpha1 andrenoceptors |
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Definition
| relaxes vascular and other smooth muscles in tissues innervated by the sympathetic nervous system |
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Term
| outcome of blockade of beta1 adrenoceptors |
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Definition
| reduces sympathetic stimulation of the heart |
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Term
phenoxybenzamine:
type of drug
competitive/noncompetitive
mechanism of action
duration of action |
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Definition
nonselective alpha blocker
noncompetitive
undergoes transformation in the body into an active metabolite that covalently binds to the alpha adrenoceptor
3-4 days because of it stable covalent bonding with the alpha adrenoceptor |
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Term
phenoxybenzamine:
effects
indications |
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Definition
decreases vascular resistance and lowers both the supine and the standing BP
used to treat hypertensive in pts with pheochromocytoma (tumor of the adrenal medulla is secreting huge amounts of catecholamines, pts have VERY high BP) |
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Term
phenotolamine
type of drug
competitive/noncompetitive
duration of action |
|
Definition
nonselective alpha blocker
competitive
has a rapid onset of action and when given IV, a duration of action of 10-15 minutes, and when given IM or Subq, a duration of action of 3-4 hours
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Term
phentolamine:
effects
indications
side effects |
|
Definition
produces vasodilation, decreases peripheral vascular resistance, and decreases BP
used in hypertensive episodes caused by alpha adrenoceptors agonists;treats dermal necrosis and ischemia caused by extravasation/accidental injection of epi or other vasopressor amines
side effects: reflex tachycardia, hypotension, and nasal congestion |
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Term
selective alpha1 antagonists
names
general information |
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Definition
alfuzosin, daxazosin, prazosin, tamsulosin, and terazosin
adminstered orally and undergo varying amounts of first-pass and system matabolism
highly bound to plasma proteins and are excreted in the bile, urine and feces |
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Term
selective alpha1 antagonists
effects
indications
side effects |
|
Definition
effects: relax vascular and other smooth muscles producing vasodilation and decreased BP
indications: used to treat essential (primary) HTN; useful in treating lower urinary tract symptoms associated with benign prostatic hyperplasia
side effects: hypotension, dizziness, |
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Term
| which selective alpha1 antagonist(s) has/have the shortest half life |
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Definition
prazosin has a shorter half-life than the half lives of other alpha1 antagonists
(duration of action = about 6 hours) |
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Term
| which selective alpha1 antagonists have a longer half life |
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Definition
doxazosin and terazosin are longer acting alpha1 blockers that are usually administered once a day
(duration of action = about 20 (terazosin) - 30 hours (doxazosin)) |
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Term
| which selective alpha1 antagonists are more uroselective |
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Definition
| alfuzosin and tamsulosin are more uroselective alpha1 blockers that relieve lower urinary tract symptoms w/o causing much hypotension, dizziness; these are typically not used to treat HTN, they are indicated for treating symptoms of urinary outflow obstruction in men with prostatic hyperplasia |
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Term
nonselective beta adrenoceptor antagonists
names
mechanism of action |
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Definition
nadolol, pindolol, propranolol, and timolol
(nonselective because they block the beta1 adrenceptors in heart tissues as well as the beta2 adrenoceptors in smooth muscle, liver, and other tissues)
competitively block the effects of NE and other adrenoceptor agonists at beta1 and beta2 adrenceptors |
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Term
| blockade of beta1 adrenoceptors |
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Definition
| reduces sympathetic stimulation of the heart -> producing a neg chronotropic (rate), inotropic (force of contractility), and dromotropic effect (conduction speen in AV node) -> reducing CO and BP |
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Term
| blockade of beta2 adrenoceptors |
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Definition
lungs -> bronchoconstriction
liver -> inhibition of epinephrine-stimulated glycogenolysis (and can thereby slow the recovery of blood glucose after a hypoglycemic episode in pt with DM) |
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Term
| the only nonselective beta adrenoceptor to have intrinsic sympathomimetic activity |
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Definition
pindolo
partial agonist activity -> enables it to exert a weak agonist effect on beta adrenoceptors. when sympathetic tone is high, pindolol acts as a competitive receptor antagonist to inhibit sympathetic stimulation of the heart in the same manner as other beta blockers |
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Term
| which nonselevtive beta adrenoceptors exhibit membrane stabilizing activity (local anesthetic activity) |
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Definition
pindolol and propanalol
they can block Na+ channels in nerves and heart tissue and thereby slow conduction velocity |
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Term
| which drug is used to ONLY treat HTN (has no other clinical applications) |
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Definition
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Term
propanolol
indications
side effects |
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Definition
indications -> adjunctive treatment of HTN
alternative treatment of HTN
angina pectoris
dysrhythmias
MI
side effects -> bradcardia
heart failure
bronchoconstriction
inhibition of glycogenolysis
depression |
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Term
selective beta1 adrendoceptors antagonists
names |
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Definition
acebutolol, atenolol, esmolol, metoprolol
cardioselective beta blockers -> produce less bronchoconstriction than nonselective |
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Term
| best beta blocker to treat glaucoma |
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Definition
| timolol (a nonselective beta andreoceptor antagonist) |
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Term
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Definition
cardioselective beta blocker
lower degree of intrinsic sympathomimetic activity
have a long duraction of action (bc metabolite is more active than parent drug) |
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Term
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Definition
show less variability in its oral absorption than do other beta blockers
lower lipid solubility and has lower indicident of central nervous system side effects
adjunctive treatment for HTN
alternative treatment of HTN
angina
Acute MI
side effects -> bradycardia and depression |
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Term
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Definition
has a much shorter half life than other beta blockers and is given IV
used to treat emergency tachycardia
side effects -> bradycardia and hypotension |
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Term
|
Definition
adjunctive treatment of HTN
alternative treatment of HTN
angina
acute MI
side effect -> bradycardia and depression |
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Term
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Definition
blocks beta1, beta2, and alpha1 adrenoceptors
possess antioxidant activity
both of the above = cardioprotective effects in pts with MI
antiapoptotic -> prevent myocyte death and reduce infarct size in pt suffering from myocardial ischemia
third generation beta blocker
adjunctive treatment of HTN, alternative treatment of HTN
chronic heart failure
acute MI |
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Term
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Definition
nonselective beta block and selective alpha1 blocker (much more potent as a beta blocker than as an alpha blocker)
decreases HR and CO (from beta blocker) and decreases peripheral vascular resistance (from alpha blocker)
adjunctive treatment of HTN; alternative treatment of HTN
chronic heart failure
acute MI |
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