AGENTS, CONTROLLING THE FUNCTIONS OF THE PERIPHERAL NERVOUS SYSTEM - Adrenoreceptor antagonist drugs Flashcards

1
Q

Which drugs is a nonselective alfa receptor antagonist?

A

Phentolamine

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2
Q

Indicate the alfa1-selective antagonist

A

Prazosin

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3
Q

Which agents is an alfa2–selective antagonist?

A

Yohimbine

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4
Q

Indicate the irreversible alfa receptor antagonist

A

Phenoxybenzamine

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5
Q

Which drugs is an nonselective beta receptor antagonist?

A

Propranolol

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6
Q

Indicate the beta1-selective antagonist

A

Metoprolol

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7
Q

Which of the following agents is a beta2–selective antagonist?

A

Butoxamine

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8
Q

Indicate the beta adrenoreceptor antagonist, which has partial beta–agonist activity

A

Pindolol

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9
Q

Which drugs is a reversible nonselective alfa, beta antagonist?

A

Labetalol

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10
Q

Indicate the indirect-acting adrenoreceptor blocking drug

A

Reserpine

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11
Q

The principal mechanism of action of adrenoreceptor antagonists is

A

Reversible or irreversible interaction with adrenoreceptors

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12
Q

Characteristics of alfa-receptor antagonists include

A
  • They cause a fall in peripheral resistance and blood pressure
  • They cause epinephrine reversal (convert a pressor response to a depressor response)
  • They may cause postural hypotension and reflex tachycardia
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13
Q

Characteristics of alfa-receptor antagonists do not include

A

Bronchospasm

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14
Q

Which drugs is an imidazoline derivative and a potent competitive antagonist at both alfa1 and alfa2 receptors?

A

Phentolamine

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15
Q

Characteristics of phentolamine include

A
  • Reduction in peripheral resistance
  • Tachycardia
  • Stimulation of muscarinic, H1 and H2 histamine receptors
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16
Q

Characteristics of phentolamine do not include

A

Stimulation of responses to serotonin

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17
Q

The principal mechanism of phentolamine-induced tachycardia is

A

Antagonism of presynaptic alfa2 receptors enhances norepinephrine release, which causes cardiac stimulation via unblocked beta receptors

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18
Q

Nonselective alfa-receptor antagonists are most useful in the treatment of

A

Pheochromocytoma

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19
Q

The main reason for using alfa-receptor antagonists in the management of pheochromocytoma is

A

Blockade of alfa2 receptors on vascular smooth muscle results in epinephrine stimulation of unblocked alfa2 receptors

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20
Q

Which drugs is useful in the treatment of pheochromocytoma?

A

Phentolamine

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21
Q

Indicate adrenoreceptor antagonist agents, which are used for the management of pheochromocytoma

A

Αlfa-receptor antagonists

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22
Q

The principal adverse effects of phentolamine include

A
  • Diarrhea
  • Arrhythmias
  • Myocardial ischemia
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23
Q

The principal adverse effects of phentolamine do not include

A

Bradycardia

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24
Q

Indicate the reversible nonselective alfa-receptor antagonist, which is an ergot derivative

A

Ergotamine

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25
Q

Indicate an alfa-receptor antagonist, which binds covalently to alfa receptors, causing irreversible blockade of long duration (14-48 hours or longer)

A

Phenoxybenzamine

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26
Q

Compared with phentolamine, prazosin has all of the following features

A
  • Highly selective for alfa1 receptors
  • The relative absence of tachycardia
  • Persistent block of alfa1 receptors
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27
Q

Compared with phentolamine, prazosin has not features

A

Irreversible blockade of alfa receptors

28
Q

True or False. ALFA1a subtype mediates both vascular and prostate smooth muscle contraction

A

FALSE

29
Q

True or False. There are at least three subtypes of alfa1 receptors, designated alfa1a, alfa1b and alfa1d

A

TRUE

30
Q

True or False. ALFA1a subtype mediates prostate smooth muscle contraction

A

TRUE

31
Q

True or False. ALFA1b subtype mediates vascular smooth muscle contraction

A

TRUE

32
Q

Indicate an alfa1 adrenoreceptor antagonist, which has great selectivity for alfa1a subtype

A

Tamsulosin

33
Q

Subtype-selective alfa1 receptor antagonists such as tamsulosin, terazosin, alfusosin are efficacious in

A

Benign prostatic hyperplasia (BPH)

34
Q

Indicate an alfa receptor antagonist, which is an efficacious drug in the treatment of mild to moderate systemic hypertension

A

Prazosin

35
Q

Which alfa receptor antagonists is useful in reversing the intense local vasoconstriction caused by inadvertent infiltration of norepinephrine into subcutaneous tissue during intravenous administration?

A

Phentolamine

36
Q

Beta-blocking drugs-induced chronically lower blood pressure may be associated with theirs effects on

A
  • The heart
  • The blood vessels
  • The renin-angiotensin system
37
Q

Characteristics of beta-blocking agents include

A
  • They occupy beta receptors and competitively reduce receptor occupancy by catecholamines or other beta agonists
  • They do not cause hypotension in individuals with normal blood pressure
  • They can cause blockade in the atrioventricular node
38
Q

Characteristics of beta-blocking agents do not include

A

They induce depression and depleted stores of catecholamines

39
Q

Beta-receptor antagonists have all of the following cardiovascular effects

A
  • The negative inotropic and chronotropic effects
  • Vasoconstriction
  • Reduction of the release of renin
40
Q

Beta-receptor antagonists have not the following cardiovascular effects

A

Acute effects of these drugs include a fall in peripheral resistance

41
Q

Beta-blocking agents have all of the following effects

A
  • Bronchoconstriction
  • Decrease of aqueous humor prodaction
  • “membrane-stabilizing” action
42
Q

Beta-blocking agents have all of the following effects except

A

Increase plasma concentrations of HDL and decrease of VLDL

43
Q

Beta-receptor antagonists cause

A

Inhibition of glycogenolysis

44
Q

Propranolol has all of the following cardiovascular effects

A
  • It decreases cardiac work and oxygen demand
  • It inhibits the renin secretion
  • It increases the atrioventricular nodal refractory period
45
Q

Propranolol has all of the following cardiovascular effects except

A

It reduces blood flow to the brain

46
Q

Propranolol-induced adverse effects include

A
  • Bronchoconstriction
  • “supersensitivity” of beta-adrenergic receptors (rapid withdrawal)
  • Sedation, sleep disturbances, depression and sexual dysfunction
47
Q

Propranolol-induced adverse effects do not include

A

Hyperglycemia

48
Q

Propranolol is used in the treatment all of the following diseases

A
  • Cardiovascular diseases
  • Hyperthyroidism
  • Migraine headache
49
Q

Propranolol is used in the treatment all of the following diseases except

A

Bronchial asthma

50
Q

Metoprolol and atenolol are members of

A

The beta1-selective group

51
Q

Which beta receptor antagonists is preferable in patients with asthma, diabetes or peripheral vascular diseases?

A

Metoprolol

52
Q

Indicate a beta receptor antagonist, which has very long duration of action

A

Nadolol

53
Q

Indicate a beta1-selective receptor antagonist, which has very long duration of action

A

Betaxolol

54
Q

Which drugs is a nonselective beta-blocker without intrinsic sympathomimetic or local anesthetic activity and used for the treatment of life-threatening ventricular arrhythmias?

A

Sotalol

55
Q

Indicate a beta receptor antagonist with intrinsic sympathomimetic activity

A

Oxprenolol

56
Q

Pindolol, oxprenolol have all of the following properties

A
  • They are nonselective beta antagonists
  • They are less likely to cause bradycardia and abnormalities in plasma lipids
  • They are effective in hypertension and angina
57
Q

Which drugs has both alfa1-selective and beta-blocking effects?

A

Labetalol

58
Q

Characteristics of carvedilol include

A
  • It has both alfa1-selective and beta-blocking effects
  • It attenuates oxygen free radical-initiated lipid peroxidation
  • It inhibits vascular smooth muscle mitogenesis
59
Q

Characteristics of carvedilol do not include

A

It is a beta1-selective antagonist

60
Q

Indicate the adrenoreceptor antagonist drug, which is a rauwolfia alkaloid

A

Reserpine

61
Q

Characteristics of reserpine include

A
  • It decreases cardiac output, peripheral resistance and inhibits pressor reflexes
  • It may cause a transient sympathomimetic effect
  • It depletes stores of catecholamines and serotonin in the brain
62
Q

Characteristics of reserpine do not include

A

It inhibits the uptake of norepinephrine into vesicles and MAO

63
Q

Indicate a beta-blocker, which is particularly efficacious in thyroid storm

A

Propranolol

64
Q

Beta-receptor blocking drugs are used in the treatment all of the following diseases

A
  • Hypertension, ischemic heart disease, cardiac arrhythmias
  • Glaucoma
  • Hyperthyroidism
65
Q

Beta-receptor blocking drugs are used in the treatment all of the following diseases except

A

Pheochromocytoma

66
Q

Beta-blocker-induced adverse effects include

A
  • Bronchoconstriction
  • Depression of myocardial contractility and excitability
  • “supersensitivity” of beta-receptors associated with rapid withdrawal of drugs
67
Q

Beta-blocker-induced adverse effects do not include

A

Hyperglycemia