Lecture 5 Sympatholytics (alpha and beta blockers)

Question 1

is of now, all sympatholytics are ____Steric; that is, they bind where the normal NT binds

Answer 1

ortho

Question 2

non-selective alpha blockers:

____ is irreversible, _____ is reversible

Answer 2

phenoxybenzamine, phentolamine

Question 3

phenoxybenzamine is used in _____ and hypertensive crisis. It binds ____ to the receptor (irreversible)

Answer 3

pheochromocytoma; covalently

Question 4

phentolamine is a _____ (reversible) blocker. It is a potent vaso___ but produces pronounced reflex _____

Answer 4

competitive;

dilator, tachycardia

Question 5

suffix of alpha 1 adrenergic receptor antagonists?

Answer 5

-zosins;

ie prazosin, terazosin, doxazosin (most used)

Question 6

The zosins are used to treat _____ ____ ____ symptoms via relaxation of smooth muscle

Answer 6

benign prostatic hypertrophy

Question 7

side effect of zosins?

Answer 7

first dose orthostatic hypotension

take first dose before bed

Question 8

Besides orthostatic hypotension, what are 3 other side effects of alpha blockers? inhibition of _____; nasal _____; _____cardia

Answer 8

ejaculation, stuffiness, tachy (Reflex)

Question 9

_____ (yocon) blocks alpha 2 receptors, increasing sympathetic ___. Used as dietary supplement for _____ in men.

Answer 9

yohimbine, tone/discharge;

impotence (not very effective)

Question 10

Treatment of/effects of beta blockers:

1. Angine pectoris due to decreased ____ and _____ and ____ Oxygen consumption
2. hypertension due to decreased cardiac output and decreased ____ secretion via action on B1 receptors on the ___ cells

Answer 10

CO, HR; decreased;

renin, JGA

Question 11

Beta blockers effects:

1. Glaucoma-act on ___ receptors in the ciliary epithelium to ___ secretion of aqueous humor
2. Cardiac _____ - by acting on AV and SA node and decrease conduction velocity

Answer 11

B2, decreased;

arrhythmias

Question 12

Beta blocker effects:

1. Migraines-inhibt _____
2. Low doses may be used for ____ ____
3. ____ stage Congestive heart failure
4. Thyrotoxicosis

Answer 12

vasospams;
stage fright/nervousness;
earlly

Question 13

___ was the first beta blocker discovered. it is lipo____ and penetrates the CNS. It also blocks ____ channels acting as a local anasthetic

Answer 13

propanolol;
phillic;
Na+

Question 14

propanolol may cause transient changes in lipid levels: increased____ and decreased ____. It also ____ lipolysis and may increase _____ airway resistance

Answer 14

VLDL, HDL;
inhibits,
bronchial

Question 15

Nadolol is ___ lipophillic than propanolol and has a ____ half life.

Answer 15

less, longer

Question 16

_____ is clasically used in treatment of glaucoma by decreasing aqueous humor production. what is the effect on pupil size?

Answer 16

timolol;

none

Question 17

_____ and cartelol are partial agonists (aka intrinsic sympathomimetic activity). It is less likely to cause ____ and lipid abnormalities

Answer 17

pindolol;

bradycardia

Question 18

____ is a partial agonist that is used in treatment of glaucoma (Sometimes)

Answer 18

carteolol

Question 19

Metoprolol and bisoprolol are selective ___ adrenergic receptor antagonists. They mainly affect the ____

Answer 19

beta 1; heart (ie less bronchoconstriction)

Question 20

Metoprolol is the most commonly used beta blocker and has a ____ half life. What did they do to the drug to change this?

Answer 20

short;

created extended release tablets

Question 21

____ is a beta 1 blocker with low lipophilicity

Answer 21

atenolol

Question 22

_____ is a short acting Beta 1 blocker (half life of 9 minutes). it is used acutely to treat atrial ____ and _____ hypertension

Answer 22

esmolol;
flutter/fib;
perioperative (ie random)

Question 23

Nebivolol is a 3rd generation B1 blocker. it also causes ____ due to ____ production and is used to treat hypertension

Answer 23

vasodilation, NO

Question 24

2 mixed adrenergic receptor antagonists

Answer 24

labetalol and carvedilol

Question 25

labetalol and carvedilol’s ___ blocking activity prevents reflex ____ normally associated with ___ receptor antagonists

Answer 25

beta 1; tachycardia; alpha 1

Question 26

side effects of beta blockers:

____Cardia, ____ block, _____, mask symptoms of ____, _____ syndrome

Answer 26

brady, AV, sedation, hypoglycemia, withdrawl

Question 27

with chronic use of beta blockers, receptors are ____. if the drug is discontinued, _____ occurs

Answer 27

upregulated;

super-sensitivity

Question 28

beta blockers can exacerbate ____/_____ and type __ congestive heart failure

Answer 28

asthma, COPD; 4

Question 29

_____ works by blocking vesicular mono-amine transporters, depleting the vesicular pool of NTs. it has a ____ onset of action.

Answer 29

reserpine;

slow

Question 30

Reserpine may precipitate _____ but does not cause ____ ____

Answer 30

depression, reflex tachy (too slow)