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Therapeutics > Lecture 9: sympatholytics B blockers > Flashcards

Lecture 9: sympatholytics B blockers Flashcards

1
Q

Beta blocker uses

A

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

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2
Q

Beta blocker use for angina

A

-reduces myocardial oxygen need
-decrease HR and contractility

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3
Q

Beta blocker use for cardiac arrhythmia

A

-slow AV nodal conduction

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4
Q

Beta blocker use for post-myocardial infraction

A

-reduce myocardial oxygen need
-slow AV nodal conduction

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5
Q

Beta blocker use for HTN

A

-decrease CO
-inhibibit renin secretion

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6
Q

beta blocker use for congestive heart failure

A

-decrease chronic overstimulation/toxicity of compensatory catecholamines

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7
Q

Aryloxypropanolamines

A

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

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8
Q

Aryloxypropanolamines structure

A

-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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9
Q

Nonselective B ANTAgonists

A

-propranolol
-Nadolol
-Timolol
-Pindolol
-Carteolol

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10
Q

Propranolol

A

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

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11
Q

Propranolol effects

A

-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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12
Q

Therapeutic use of B ANTAgonists

A

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

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13
Q

Nadolol

A

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

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14
Q

Nadolol uses

A

-HTN
-agina
-migraine

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15
Q

Timolol

A

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

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16
Q

Timolol uses

A

-glaucoma
-HTN
-angina
-migraine

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17
Q

How will B-blockers affect pupil size?

A
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18
Q

Timolol use in glaucoma

A

-decrease intraocular pressure
-target ciliary epithelium

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19
Q

Pindolol

A

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

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20
Q

Pindolol uses

A

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

21
Q

What would a pindolol dose-response curve look like?

A

-doesnt achieve full receptor activation

22
Q

Carteolol

A

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

23
Q

Carteolol uses

A

-HTN
-glaucoma

24
Q

Selective B-1 ANTAGONISTs

A

-metaprolol and bisoprolol
-atenolol
-esmolol

25
Q

Metoprolol and Bisoprolol

A

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

26
Q

Metoprolol and Bisprolol uses

A

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

27
Q

Atenolol

A

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

28
Q

Atenolol uses

A

-HTN
-agina
-oral and parenteral admin

29
Q

Esmolol

A

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

30
Q

Esmolol uses

A

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

31
Q

Side effects of B-blockers

A

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

32
Q

Contraindications of Beta-blockers

A

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

33
Q

Mixed Adrenergic ANTAgonists

A

-Labetalol
-cavedilol

34
Q

Labetalol

A

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

35
Q

Labetalol R isomer

A

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

36
Q

Labetalol SR isomer

A

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

37
Q

Carvedilol

A

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

38
Q

Carvedilol S enantiomer

A

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

39
Q

Carvedilol use

A

-HTN
-congestive Heart failure
-oral admin

40
Q

Indirect-acting sympatholytics

A

-Metyrosine
-Bretylium tosylate
-reserpine

41
Q

Metyrosine

A

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

42
Q

Metyrosine clinical use

A

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

43
Q

Metyrosine problems

A

-depletes catecholamines everywhere

44
Q

Bretylium Tosylate

A

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

45
Q

Bretylium tosylate use

A

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

46
Q

Reserpine

A

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

47
Q

Reserpine action

A

-VMAT IRREVERSIBLE inhibitor
-depletes stored NE

48
Q

Reserpine use

A

-HTN but rarely bc bad effects
-may precipitate depression

49
Q

Reserpine problems

A

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

Therapeutics (78 decks)

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