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VPharma 101 > Chapter 6: Adrenergic Receptor Agonists and Antagonists > Flashcards

Chapter 6: Adrenergic Receptor Agonists and Antagonists Flashcards

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1
Q

What are the 3 classifications of sympathomimetic drugs?

A

1st Group (Direct Agonists), 2nd Group (Indirect Agonists), 3rd Group (Mixed-Acting Adrenergic Agonists)

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2
Q

Drugs that mimic the physiological and pharmacological actions of the endogrnous catecholamines

A

Sympathomimetic Drugs

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3
Q

Classification of sympathomimetic drugs that directly binds to and activate adrenergic receptors

A

1st Group or Direct Agonists

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4
Q

Examples of 1st group or direct agonists

A

Phenylephrine, Dobutamine

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5
Q

This group enhances the availability of endogenous catecholamines to bind adrenergic receptors

A

2nd Group (indirect Acting Agonists

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6
Q

Group of drugs that directly activate adrenergic receptors as well as increase the release of NE from adrenergic nerve terminals

A

3rd Group (Mixed-Acting Adrenergic Agonists)

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7
Q

Main neurotransmitters utilized by the SNS

A

Epinephrine, Norepinephrine

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8
Q

Parent comound of sympathomimetic amines, consists of benzene ring and ethylamine side

A

B-phenylethylamine

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9
Q

Sympathomimetic drugs

A

Epinephrine, Norepinephrine, Dopamine, Isoproterenol

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10
Q

Required for maximum alpha and beta receptor potencies

A

Catechol nucleus

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11
Q

Any chemical containing catechol

A

Catecholamines

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12
Q

Modification in phenylethylthalamine that results in reduced B-adrenergic receptor activity

A

removal of hydroxyl group

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13
Q

Modification in phenylethylthalamine that produces a compound with reduced CNS effects

A

Substitution of B-carbon atoms

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14
Q

Modification in phenylethylthalamine that produces a drug that is generally more resistant to oxidation by monoamine oxidase

A

Substitution of a-carbon atom

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15
Q

Modification in phenylethylthalamine that affects a nd B agonistic properties of various drugs

A

Alkyl substitutions on the amino acid

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16
Q

A type of G-coupled receptor

A

Adrenergic Receptors

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17
Q

Members of the B-adrenergic receptor family

A

B1, B2, B3

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18
Q

Activation of this receptor results in stimulation of adenylyl cyclase and increase cAMP

A

B-adrenergic receptor family

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19
Q

B-adrenergic receptor that increase heart rate and enhance cardiac contractility

A

B1

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20
Q

B-adrenergic receptor found in the pulmonary airways

A

B2 receptors

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21
Q

B-adrenergic receptors found in the detrusor muscle of the bladder

A

B2 and B3 receptors

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22
Q

Members of the a1 receptor family

A

A1A, A1B, A1D

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23
Q

This receptor family activates phospholipase C

A

a1 receptor family

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24
Q

Where are a1 receptors located?

A

vascular smooth muscles

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25
Q

Function of the a1 receptor

A

smooth muscle contraction

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26
Q

Members of the a2 receptor family

A

A2A, A2B, and A2C

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27
Q

Activation of these receptor inhibits adenyl cyclase activity, hence, a reduced cAMP levels

A

a2 receptors

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28
Q

Location of a2 receptors

A

terminals of postganglionic sympathetic nerve fibers

29
Q

Activation of this receptor will reduce norepinephrine release from nerve terminals

A

a2 receptors

30
Q

This receptor is expressed at the thrombocytes, endothelial cells, and CNS

A

a2 receptors

31
Q

Members of the dopamine receptors

A

D1, D2

32
Q

Activation of this dopamine receptor is associated with increased cAMP

A

D1 receptor activation

33
Q

Activation of this dopamine receptor inhibits adenyl cyclase activity

A

D2 receptor activation

34
Q

Provides an important framework for understanding target organ effects of endogenous catecholamines and sympathomimetic drugs

A

Receptor Selectivity

35
Q

A potent and selective agonist at A1 adrenergic receptors

A

Phenylephrine

36
Q

Drug that can cause an increase in peripheral vascular resistance, hence, an increase in blood pressure

A

Phenylephrine

37
Q

An agonist at a1, a2, and b1 adrenergic receptors

A

Norepinephrine

38
Q

A potent agonist at a-adrenergic and b-adrenergic receptors

A

Epinephrine

39
Q

Produces vasodilation when bound to B2 receptors

A

Epinephrine

40
Q

Used for downer patients

A

Epinephrine

41
Q

Has competing vasoconstriction and vasodilation effects

A

Epinephrine

42
Q

A potent nonselective B1 and B2 receptor agonists that exerts little effect on A-adrenergic receptors

A

Isoproterenol

43
Q

Used for hypertensive patients

A

Isoproterenol

44
Q

Blocks adrenergic receptors

A

Adrenergic-Receptor Antagonists

45
Q

Used in veterinary medicine to reverse sedation caused by a2-adrenergic receptor agonist

A

A2-Adrenergic receptor Antagonist

46
Q

Non-selective antagonist that bind covalently to a-adrenergic receptors to produce an irreversible bond

A

Phenoxybenzamine

47
Q

Inhibition of reuptake of Norepinephrine at presynaptic nerve terminals is an effect of?

A

Phenoxybenzamine

48
Q

What are some exampls of non-seslective a1, a2-adrenergic receptor antagonists?

A
  1. Phenoxybenzamine
  2. Phentolamine
  3. Phenothiazine tranquilizers
49
Q

Potent nonselective a-adrenergic receptor antagonists, have profound CNS effect

A

Phenothiazine tranquilizers

50
Q

Used in dogs, can antagonize a1 drenergic receptors

A

Trazodone

51
Q

A competitive antagonist marked selectivity for a1-adrenergic receptor

A

Prasozin

52
Q

Reversible a1-adrenergic receptor antagonists with similar effects to prazosin

A

Terazosin, Doxazosin, Alfuzosin

53
Q

A second generation A1 adrenergic receptor antagonist, used for orthostatic hypotension

A

Tamsulosin

54
Q

A1 adrenergic receptor antagonist that has higher affinity for A1A and A1D receptors

A

Tamsulosin

55
Q

Third generation, highly selective A1 adrenergic receptro antagonist

A

Silodosin

56
Q

The prototype for selective A2 adrenergic receptor antagonists

A

Yohimbine

57
Q

Yohimbe can be found in the bark of ______ and root of _______

A

Pausinystalia yohimbe, Rauwolfia root

58
Q

Demonstrates a degree of antagonistic activity at serotonin receptors

A

Yohimbine

59
Q

Belongs to the synthetic group of competitive A2 adrenergic receptor antagonist

A

Tolazoline

60
Q

Licensed for reversing xylazine in horses

A

Tolazoline

61
Q

A mixed A1 and A2 adrenergic receptor antagonist

A

Tolazoline

62
Q

An A2 adrenergic receptor antagonist with an imidazole structure

A

Atipamezole

63
Q

Has binding affinity and A2/A1 selectivity ratio higher than those of yohimbine or tolazoline

A

Atipamezole

64
Q

Group of beta blockers that can stimulate beta-adrenergic receptors (agonist effect) and oppose catecholamines (antagonistic effect) in a competitive way

A

Intrinsic Sympathomimetic Activity (ISA)

65
Q

Drugs considered as partial antagonists

A

Pindolol, Acebutolol

66
Q

Cause incomplete activation of B receptors

A

Partial Antagonists

67
Q

Inhibit the activation of B-adrenergic receptors in the presence of high levels of Epinephrine and Norepinephrine

A

Partial Antagonists

68
Q

Beta blockers used in veterinary medicine

A

Propranolol, Atenolol, Esmolol, Metoprolol, Carvedilol

69
Q

Classifications of beta blockers

A
  1. Nonselective B-adrenergic receptor antagonists (1st Generation)
  2. Selective B1-ddrenergic receptor antagonists (2nd Generation)
  3. Third Generation Nonselective Antagonists

VPharma 101 (7 decks)

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