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Pharmacology > 9) Adrenoreceptor antagonists > Flashcards

9) Adrenoreceptor antagonists Flashcards

1
Q

Adrenergic agonist effect on smooth muscle (all)

A
  • Alpha-1 agonist = increase calcium, and contraction
  • Alpha-2 agonist = decrease in cAMP and contraction
  • Beta-2 agonist = increase cAMP and dilation
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2
Q

The vasomotor center in the brainstem regulates

A
  • Systemic Vascular Resistance (SVR) or Total Peripheral Resistance
  • Causes arterioles to constrict via α-1 or dilate via β-2
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3
Q

The major role of arterioles

A
  • Constrict or dilate to control the resistance to blood flow in the body
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4
Q

Alpha-2 pre-synaptic receptors

A
  • Help neurotransmitter reuptake (which prevent their release)
  • Example: Norepinephrine (NE) is reuptaken by the alpha-2 pre-synaptic receptor
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5
Q

Alpha-1 adrenergic receptors act on

A
  • Blood vessels
  • Sphincters of the GI
  • Eye
  • Genitourinary (uterus)
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6
Q

Alpha-2 adrenergic receptors act on

A
  • Pre-synaptic

- Decrease release rate of NE, insulin, and ACh

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7
Q

Beta-1 receptors act on

A
  • Heart
  • Lipolysis
  • Kidneys (release renin)
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8
Q

Beta-2 receptors act on

A
  • Blood vessels
  • Smooth muscle (lungs, uterine)
  • Muscle, liver (glycogenolysis, gluconeogenesis)
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9
Q

Alpha-1 adrenergic receptor effects

A
  • Vasoconstriction
  • Increase peripheral resistance
  • Increase blood pressure
  • Mydriasis
  • Increase closure of bladder sphincters
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10
Q

Alpha-2 adrenergic receptor effects

A
  • Inhibits norepinephrine release
  • Inhibits acetylcholine release
  • Inhibits insulin release
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11
Q

Beta-1 adrenergic receptor effects

A
  • Increase heart rate
  • Increase lipolysis
  • Increase myocardial contractility
  • Increase renin
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12
Q

Beta-1 adrenergic receptor effects

A
  • Vasodilation
  • Decrease peripheral resistance
  • Bronchodilation
  • Increase glycogenolysis (muscle, liver)
  • Increase glucagon release
  • Relaxes uterine smooth muscle
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13
Q

Subdivisions of α blockers are based on

A
  • Selective affinity for α1 versus α2

- Irreversible means they bind covalently to the α-receptors

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14
Q

Effects of non-selective blockers

A
  • Blockade of α-1 and 2 mediated responses to sympathetic nervous system
  • Reduction in vascular tone with a reduction of both arterial and venous pressures
  • Baroreceptor reflex-mediated tachycardia as a result of the drop in mean arterial pressure
  • Epinephrine reversal manifested as orthostatic hypotension
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15
Q

Orthostatic hypotension

A
  • Decrease in systolic or diastolic blood pressure upon standing from the sitting or supine position
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16
Q

Prazosin

A
  • Selective α1-inhibitor adrenergic receptor

- Lowers arterial blood pressure by blocking post-synaptic α1 receptors on arterial smooth muscle

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17
Q

Prazosin does NOT cause reflex tachycardia because

A
  • It has no effect on the presynaptic α2 receptors in sympathetic nerve endings that innervate the heart
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18
Q

Non-selective alpha blockers, such as phentolamine, are associated with

A
  • Marked reflex tachycardia due to blunting of inhibitory presynaptic α2 receptor that suppresses the uptake of norepinephrine at the synapse
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19
Q

Alpha-blocking drugs: epinephrine reversal

A
  • Manifests as orthostatic hypotension
  • Occurs when adding alpha- blockers
  • Reveals the effects of β2 vasodilation (which drops blood pressure)
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20
Q

Normally epinephrine will

A
  • Increase blood pressure through alpha-1 (vasoconstriction by decreasing the diameter of the blood vessels)
  • Increase heart contractility by acting on beta-1 receptors
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21
Q

The epinephrine (alpha and beta agonist) response exhibits

A
  • Net increase in blood pressure (the α response) to a net decrease (the β2 response) when alpha blockade is added
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22
Q

The response to phenylephrine (alpha-1 agonist)

A
  • Increases blood pressure through α response

- Suppressed but not reversed, because phenylephrine lacks β2 action

23
Q

α1 blockers reduce blood pressure with no

A
  • Reflex tachycardia (compared to nonselective)

- Useful in relaxing effects on smooth muscle in the prostate

24
Q

Clinical use of selective alpha-1 blockers

A
  • Prazosin, terazosin for hypertension
  • Tamsulosin to reduce urinary hesitancy and retention in men with benign prostatic
    hyperplasia
25
Q

Clinical use of alpha-2 blockers

A
  • Yohimbine (not a drug) used for erectile dysfunction
26
Q

Clinical use for non-selective alpha blockers

A
  • Limited use
27
Q

Selective alpha-1 blockers (generic names)

A
  • Doxazosin
  • Prazosin
  • Tamulosin
  • Terazosin
  • Alfuzosin
28
Q

Selective alpha-2 blocker

A
  • Yohimbine (natural product)
29
Q

Non-selective reversible alpha blockers

A
  • Phentolamine (Oraverse)
30
Q

Non-selective irreversible alpha blockers

A
  • Phenoxybenzamine (Dibenzyline)
31
Q

Doxazosin

A
  • Brand = Cardura
  • DOA = 24h
  • Metabolism = hepatic
32
Q

Prazosin

A
  • Brand = Minipress
  • DOA = 10-24h
  • Metabolism = hepatic
33
Q

Tamsulosin

A
  • Brand = Flomax
  • DOA = ?
  • Metabolism = hepatic
34
Q

Terazosin

A
  • Brand = ?
  • DOA = 24h
  • Metabolism = hepatic
35
Q

Alfuzosin

A
  • Brand = Uroxatral
  • DOA = 12h
  • Metabolism = hepatic
36
Q

Phentolamine

A
  • Brand = Oraverse
  • DOA = 30min (IM/IV)
  • Metabolism = hepatic
37
Q

Phenoxybenzamine

A
  • Brand = Dibenzyline
  • DOA = 24h (IV)
  • Metabolism = ?
38
Q

Side effects of alpha-adrenergic blockers

A
  • Dizziness, headaches
  • Shortness of breath
  • Swelling of arms and legs, edema
  • Erection
  • Hypotension
39
Q

Beta-blockers (subdivisions based on selective affinity for β-1 and β-2 receptors)

A
  • First generation non-selective β-blockers
  • Second generation cardio-selective β-1 blocker
  • Third generation vasodilating β-2 blocker
40
Q

Beta-blocker heart effects

A
  • Decreased HR
  • Decreased force of contraction
  • Decreased rate of atrioventricular (AV) conduction
41
Q

Beta-blocker side effects in the heart

A
  • Bradycardia
  • Lethargy
  • GI disturbance
  • Congestive heart failure (CHF)
  • Decreased BP
  • Depression
42
Q

Beta1-receptor selectivity is needed to treat patients with

A
  • Hypertension

- Asthmatic

43
Q

Since β2 receptors exist in the lungs, using a non-selective β- blocker can cause

A
  • Bronchospasm
44
Q

Partial agonists (intrinsic sympathomimetic action/ISA)

A
  • Effective in treating patients with asthma (less likely to cause bronchospasm)
  • Labetalol
  • Pindolol
  • Acebutolol
45
Q

Local anesthetic activity (“membrane-stabilizing activity”) is a disadvantage when β blockers are used topically in the eye because

A
  • Decreases protective reflexes

- Increases the risk of corneal ulceration

46
Q

Shortest acting beta-blocker

A
  • Esmolol
47
Q

Longest acting beta-blocker

A
  • Nadolol
48
Q

Beta-blockers that are less lipid-soluble and enter the central nervous system (CNS) to a lesser extent

A
  • Atenolol
  • Acebutolol
  • Esmolol
  • Labetalol
  • Nadolol
  • Nebivolol
49
Q

Clinical usage of beta-blockers

A
  • Open angle glaucoma
  • Hypertension, angina, and arrhythmias
  • Chronic heart failure
50
Q

Beta-blocker side effects

A
  • Slow SA node (which initiates heartbeat)
  • Slow heart rate (allows LV to fill completely and lowers heart workload)
  • Dilate arteries (lowering BP)
51
Q

Due to the high penetration across the blood–brain barrier, lipophilic beta blockers, such as propranolol and metoprolol, cause

A
  • Sleep disturbances (such as insomnia, vivid dreams and nightmares)
52
Q

Adverse effects associated with β2-adrenergic receptor antagonist activity

A
  • Bronchospasm
  • Peripheral
    vasoconstriction
  • Alteration of glucose and lipid metabolism
53
Q

Hypoglycemia can occur with β2-blockers because

A
  • They inhibit glycogenolysis and gluconeogenesis that form glucose
  • Blocking β2-adrenoceptors lowers plasma glucose

Pharmacology (27 decks)

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