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Pharmacology > Adrenergic Antagonists > Flashcards

Adrenergic Antagonists Flashcards

1
Q

nonselective antagonism of ALPHA receptors is useful in treating ?

A

phaeochromocytoma

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2
Q

alpha 1 selective antagonists treat ? and ?

A

Htn

BPH

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3
Q

most common adrenergic antagonists used?

A

beta antagonists

*Htn, ischemic heart disease, arrhythmias, endocrinologic, neurologic disorders

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4
Q

phentolamine

phenoxybenzamine

A

non selective alpha 1 antagonists

phenoxybenzamine is slightly alpha 1

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5
Q

only alpha 2 selective?

A

yohimbine

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6
Q

alpha 1 selective?

A

prazosin
doxazosin
terazosin
tamsulosin

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7
Q

reversible nonselective alpha? irreversible?

A

phentolamine

phenoxybenzamine

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8
Q

irreversible will shift the curve to higher concentrations (also reversible) AND it will ?

A

reduce the maximum effect

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9
Q

blockade of alpha receptors in smooth m reduces ? and ?

A

peripheral resistance

blood pressure

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10
Q

giving an alpha antagonist to a mixed a&b agonist i.e. epi would result in?
known as??

A

fall in peripheral resistance (NO EFFECT ON B)
fall in BP (antagonizes alpha)
EPINEPHRINE REVERSAL

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11
Q

giving an alpha antagonist to NE?

A

just blocks the increase in BP

practically no B receptor activity w/ NE

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12
Q

on the heart, alpha antagonists do two things:

A
  1. decreased blood pressure leads to reflex tachycardia via B1 receptors
  2. presynaptic a2 receptors that decrease NE release are blocked, increasing NE release on heart & increasing HR and force of contraction
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13
Q

blockade of a1 receptors in VEINS can results in ?

A

orthostatic hypotension

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14
Q

phentolamine used in treatment of ? and ?

|&raquo_space;causes a drop in ? thru inhibiting a1 and reflex stim of ? to the heart (tachycardia)

A

hypertension
pheochromocytoma
peripheral resistance
SNS nerve terminals

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15
Q

presynaptic inhibition of a2 causes an increased release of ? from sympathetic nerve terminals and an ? of reflex tachycardia

A

exacerbation

  • net result is vasodilatation, increased CO&rate
  • little effect on BP of patients with essential hypertension
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16
Q

phentolamine ALSO inhibits ? receptors and activates ? and ? receptors

A

dopamine
muscarinic, histaminergic
*adverse effects include severe tachycardia, arrhythmias, myocardial ischemia, nasal congestion, and headache

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17
Q

phenoxybenzamine inhibits ?, histamine, Ach, and serotonin receptors
-can cause ? from the presynaptic a2 blockade

A

NE reuptake
reflex tachycardia
*treatments same as phentolamine- Htn, phaeochromocytoma

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18
Q

A/E of phentolamine and phenoxybenzamine include tachycardia, postural ?, nasal stuffiness, sexual ?, fatigue, sedation, and nausea

A

hypotension, dysfunction

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19
Q

Tx for raynaud’s syndrome?

*also relieve Sx in ? and useful in ?

A

prazosin*, terazosin, doxazosin

BPH, BPH w/ comorbid Htn

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20
Q

alpha 1 selective adr ant have less ? due to its lack of ?

A

reflex tachycardia, a2

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21
Q

alpha one selective
3 hours?
9-12 hours?
22 hours?

A

praZOSIN
teraZOSIN
doxaZOSIN

22
Q

4th a1 selective but structurally diff?
-met in the ?
higher potency for inhibiting ? contraction but less potency at vascular smooth m compared to other three
-used for relieving ? while producing less ?

A

tamsuLOSIN
liver
urinary retention in BPH
BPH, hypotension (use other in hypertensive pts)

23
Q

a2 selective adrenoceptor antagonist?

-? effect that produces increases in HR, BP, anxiety and agitation

A

yohimbine
antidiuretic
**more serious a/e have been reported including renal failure, seizures, death

24
Q

partial agonists that are also beta blockers? (2)

  • inhibit activation of B receptors in presence of ? but moderately activate receptors in presence of ?
  • said to have?
A

pindolol, acebutolol
high catecholamine concentrations
endogenous agonists

25
Q

block alpha and beta receptors?

A

carvedilol, labetalol

26
Q

in normotensive patients, taking beta antagonists does not usually cause ?

A

hypotension

27
Q

at rest the PNS innervation of heart dominates» therefore blockade of B receptors would ?

A

have little effect

28
Q

Propanolol

  • decreased CO results in a transient reduction in ? activating a baroreflex increase in SNS outflow
  • ? will increase due to ? (normally vasodilatory)
  • the reflex increase in SNS outflow and less B2 receptor mediated vasodilation combine to increase the ? on vascular resistance causing an increase in ?
A

blood pressure
peripheral resistance, blockade of B2 receptors
SNS, arterial pressure

29
Q

B1 selective agents will not block B2 vasodilation so there will be less of a decrease in ?

A

diastolic pressure

30
Q

CHRONIC USE of B blockers:

  • in presence of ? total peripheral resistance returns to ? or is ?
  • delayed fall in ? and persistent reduction of ? accounts for its ? actions
  • beta blockers also reduce the release of ? from the kidney
A

hypertension, initial value, decreased
peripheral resistance, CO, antihypertensive
renin

31
Q

drugs used to treat supraventricular arrhythmias and ventricular arrhythmias?

A

beta blockers

**also useful in angina, MI, and HF (the HF is counterintuitive because the heart is failing/decreased CO)

32
Q

due NOT give an asthma patient a B2 blocker ie?

A

propanolol

*EVEN B1 selective agents at a high enough concentration can antagonize B2 receptors

33
Q

mixed acting agents like ? hold promise in patients w/ asthma

A

celiprolol

34
Q

nonselective B ant and B2 ant are CI in ? due to its blockage of glycogenolysis and gluconeogenesis
-B blockers also mask the ? associated with ?, which is a warning sign in diabetics

A

insulin independent diabetes
tachycardia
hypoglycemia

35
Q

chronic use of B blockers is associated with an increase in ? and decreased ? which is undesirable in CVD; also increases risk of CAD

A

VDL, HDL

36
Q

b blocker used to decrease IOP in GLC? used in conjunction with muscarinic agonist?

A

timolol

pilocarpine

37
Q

labetolol
penbutolol
pindolol
acebutolol

A

partial agonists

38
Q

longest acting beta blocker?

A

nadolol

39
Q

alpha 1, beta 1 and partial agonist B2; can cause orthostatic hypotension

A

labetalol

40
Q

ultra short B-1 selective?

A

esmolol

41
Q

b1 selective widely used, htn, angina, MI

A

metoprolol

42
Q

most b1 selectivity, NO mediated vasodilation, hypertension

A

nebivolol

43
Q

to reduce effects like fatigue, sedation, sleep disturbances, depression, etc. use agents with lower ? like ? or ?

A

lower lipid solubility

nadolol, atenolol

44
Q

B1 selective agents should only be used when completely necessary because they still ?

A

acting on the b2 receptor (asthma- bronchoconstriction)

45
Q

life threatening a/e from b-blockers - being used in CHF or MI- reverse with ? or ?

A

isoproterenol

glucagon

46
Q

b-blockers can interact with the ca2+ channel antagonist ? and cause bradycardia, HF, severe hypotension

A

verapamil

47
Q

insulin dependent diabetes- give a ?

A

b1 selective blocker (as little activity on b2 as possible bc that deals with liver glycogenolysis&gluconeogenesis)

48
Q

men complain of ? from b-blockers

A

impaired sexual activity

49
Q

guanethidine
metyrosine
reserpine

A

indirect adrenergic; nonselective!

blocks the synthesis or release of catecholamines

50
Q

blocks release of NE & can displace NE from storage vesicles?

A

guanethidine

51
Q

inhibits tyrosine hydroxylase and prevents catecholamine synthesis?

A

metyrosine; rarely used to reduce pheochromocytoma

52
Q

blocks uptake of catecholamines from cytoplasm to vesicles? results in accumulation of NE in cytoplasm degraded by MAO, decreasing BP and HR

A

reserpine

*long-acting and effects persist for days

Pharmacology (21 decks)

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