Lecture 9: sympatholytics B blockers Flashcards by Brooke Thornburg

Beta blocker uses

-angina
-arrhythmia
-post-MI
-HTN
-heart failure

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Beta blocker use for angina

-reduces myocardial oxygen need
-decrease HR and contractility

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Beta blocker use for cardiac arrhythmia

-slow AV nodal conduction

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Beta blocker use for post-myocardial infraction

-reduce myocardial oxygen need
-slow AV nodal conduction

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Beta blocker use for HTN

-decrease CO
-inhibibit renin secretion

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beta blocker use for congestive heart failure

-decrease chronic overstimulation/toxicity of compensatory catecholamines

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Aryloxypropanolamines

-Beta ANTAgonists
-O side chain
-OH
-NH
-bulky alkyl group

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Aryloxypropanolamines structure

-right half (-OH, -NHR) resembles B AGONIST
-left half (aromatic ring) more lipophilic and pimary determinant of ANTAgonist activity. may also b determinant in B-1 selectivity

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Nonselective B ANTAgonists

-propranolol
-Nadolol
-Timolol
-Pindolol
-Carteolol

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Propranolol

-nonselective B ANTAgonist
-lipoPHILIC
-extensive first pass hepatic metabolism
-local anesthetic properties
-blockade is activity-DEPENDENT

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Propranolol effects

-decrease CO and HR
-reduce renin release
-increase VDL
-decrease HDL
-inhibit lipolysis
-inhibit compensetory glyconeogensis and glucose release in response to hyperglycemia
-increase bronchial airway resistance

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Therapeutic use of B ANTAgonists

-HTN
-agina
-arrhythmia
-migraine
-stage fright
-thyrotoxicosis
-glaucoma
-congestive heart failure

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Nadolol

-non selective B-ANTAgonist
-less lipophillic than propranolol
-20 hour half life
-mostly excreted unchanged in urine
-oral admin

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Nadolol uses

-HTN
-agina
-migraine

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Timolol

-non-selective B ANTAgonist
-thiadiazole nucleus with morpholine ring
-oral, ophthalmic admin

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Timolol uses

-glaucoma
-HTN
-angina
-migraine

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How will B-blockers affect pupil size?

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Timolol use in glaucoma

-decrease intraocular pressure
-target ciliary epithelium

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Pindolol

-nonselective B-ANTAgonist
-possess intrinsic sympathomimetic activity (ISA)
-PARTIAL agonist
-less likely to cause BRADYcardia and lipid abnormalities
-oral admin

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Pindolol uses

-HTN
-angina
-migraine
-good for patients with severe BRADYcardia or little cardiac reserve

What would a pindolol dose-response curve look like?

-doesnt achieve full receptor activation

Carteolol

-Non-selective
-ISA
-PARTIAL agonist
-less likely to cause BRADYcardia and lipid abnormalities
-oral or opththalmic admin

Carteolol uses

-HTN
-glaucoma

Selective B-1 ANTAGONISTs

-metaprolol and bisoprolol
-atenolol
-esmolol

Metoprolol and Bisoprolol

-selective B1 ANTAgonists -para phenyl derivatives -cardioselective -less bronchoconstriction -moderate lipophilicity -3-4hour half life -big first pass metabolism -oral or parenteral admin

Metoprolol and Bisprolol uses

-HTN -agina -antiarrythmic -congestive heart failure -oral and parenteral admin

Atenolol

-selective B-1 ANTAgonist -cardioselective -less bronchoconstriction -LOW lipophilicity ("water soluble metoprolol) -6-9 hour half life

Atenolol uses

-HTN -agina -oral and parenteral admin

Esmolol

-B1 ANTAgonist -9 min half life -rapid hydrolysis by ESTERASE in RBCs -incompatible with sodium bicarbonate

Esmolol uses

-supraventricular TACHYcardia -atrial fibrilation -perioperative HTN -parenteral admin -note compatible with sodium bicarbonate

Side effects of B-blockers

-BRADYcardia -AV block -sedation -symptoms of hypoglycemia -withdrawal syndrome

Contraindications of Beta-blockers

-asthma -COPD -congestive heart failure (type IV)

Mixed Adrenergic ANTAgonists

-Labetalol -cavedilol

Labetalol

-phenylethanolamine derivative -mixed adrenergic receptor ANTAGONIST -2 chiral carbons -racemic mix

Labetalol R isomer

-nonselective B-antagonist -activity prevents reflex TACHYcardia associated with a1 ANTAgonists

Labetalol SR isomer

-a1 ANTAgonist -vasoDILATION =prevents BRADYcardia associated with the B ANTAgonist

Carvedilol

-Both enantiomers antagonize a1 receptors -only S enantiomer B-ANTAgonist

Carvedilol S enantiomer

-non-selective B-ANTAgonist -prevents reflex TACHYcardia associated with a1 ANTAgonists

Carvedilol use

-HTN -congestive Heart failure -oral admin

Indirect-acting sympatholytics

-Metyrosine -Bretylium tosylate -reserpine

Metyrosine

-indirect sympatholytic -inhibits NE synthesis -inhibits tyrosine hydroxylase -depletes catecholamines everywhere

Metyrosine clinical use

-perioperative management of pheochromocytoma (adrenal medulla tumor that results in excessive NE and epinephrine synthesis and release)

Metyrosine problems

-depletes catecholamines everywhere

Bretylium Tosylate

-aromatic quarternary ammonium -mech unknown -displace and release NE and prevent further release -so does Guanethidine

Bretylium tosylate use

-reduce storage/release of NE -antiarrhytmic (ventricular fib) -parenteral admin

Reserpine

-indole alkaloid from root -block vesicular monoamine transporters (VMAT) -deplete vesicular pool of NE -slow onset -sustained effect (weeks)

Reserpine action

-VMAT IRREVERSIBLE inhibitor -depletes stored NE

Reserpine use

-HTN but rarely bc bad effects -may precipitate depression

Reserpine problems

-orthostatic hypotension -increased GI activity -CNS effects: sedation, depression, suicide