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Pharmacology > Exam II: Adrenergic Agonists > Flashcards

Exam II: Adrenergic Agonists Flashcards

1
Q

The general term for neurotransmitters/hormones in the sympathetic nervous system is:

A

Catecholamines

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2
Q

What are the 3 major catecholamines?

A

Dopamine
Norepinephrine
Epinephrine

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3
Q

What are the 4 basic adrenergic receptors?

A

alpha 1
alpha 2
beta
dopamine

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4
Q

Alpha 1 receptors are coupled with ____ proteins and produce ____ effects

A

Gq proteins

Activate other enzymes, resulting in positive effects

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5
Q

Alpha 2 receptors are coupled with ____ proteins and produce ____ effects

A

Gi proteins

Decrease cAMP causing negative action

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6
Q

Beta receptors are coupled with ____ proteins and produce ____ effects

A

Gs proteins

Inc. conversion of ATP to cAMP (inc. cAMP)

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7
Q

Dopamine receptors are coupled with ____ proteins and produce ____ effects

A

Gi and Gs

D1: increase cAMP
D2: decrease cAMP

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8
Q

What are the 4 factors that can alter the degree to which adrenergic receptors respond to a stimulus

A
  1. Selectivity
  2. Regulation
  3. Polymorphism
  4. Catecholamine metabolism
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9
Q

What are the 4 examples of mechanisms of desensitizations?

A
  1. Altered transcription or translation of DNA and/or RNA
  2. Modifications of receptors
  3. Long term exposure to an agonist
  4. Interactions or messages from other receptors
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10
Q

How is NE terminated in the cell? (4 ways)

A
  1. NET acts as pre-synaptic pump to move NE out of synapse and back into neuron
  2. Movement of NE out of synaptic cleft and into bloodstream
  3. Metabolism b COMT
  4. Metabolism by MAO
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11
Q

What are 2 drugs that inhibit NET?

A

Atomoxetine (for ADHD)

Cocaine

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12
Q

What does COMT stand for?

A

catecholamine-O-methyltransferase

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13
Q

What does COMT metabolize?

A

All catecholamines (NE, Epi, DA)

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14
Q

What is a drug that inhibits COMT and what disease is it used to treat?

A

Entacapone

Treats Parkinson’s dz to inhibit metabolism of levodopa

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15
Q

What does MAO stand for?

A

Monoamine Oxidase

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16
Q

What does MAO metabolize?

A

Endogenous monoamines (NE, epi, serotonin, DA)

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17
Q

Define sympathomimetic

A

Drugs that mimic actions of NE, epi, DA

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18
Q

Where on the chemical structure can changes be made to sympathomimetics to alter affinity?

A
  1. Benzene Ring Substitutions
  2. Amino group substitutions
  3. Alpha carbon substitutions
  4. Beta carbon substitutions
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19
Q

Describe possible benzene ring substitutions

A
  1. Adding hydroxyl groups to C3 and C4
  2. Adding a hydroxyl group to either C3 or C4
  3. Absence of hydroxyl group on benzene ring
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20
Q

If a sympathomimetic has -OH groups added to C3 and C4 position of the benzene ring then what characteristics would you expect?

A

Maximized alpha and beta activity

Susceptible to COMT breakdown so they will have a shorter half-life

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21
Q

If a sympathomimetic has an -OH group added to either C3 or C4 position of the benzene ring then what characteristics would you expect?

A

Reduced adrenergic potency

COMT can NOT break down so inc. drug duration

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22
Q

If a sympathomimetic has no -OH groups on its benzene ring then what characteristics would you expect?

A

Lipophilic –> can enter CNS

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23
Q

Describe the possible amino group substitutions

A

Increasing the size of alkyl substitutions

Isopropyl groups on the amino nitrogen

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24
Q

What does increasing the size of an alkyl substitution do to the sympathomimetic drug?

A

Increases beta activity

The larger the group, the lower the alpha activity

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25
Q

What does adding an isopropyl group to the amino nitrogen do to the sympathomimetic drug?

A

Increases beta activity

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26
Q

What do substitutions to the alpha carbon of a sympathomimetic cause?

A

They block oxidation by MAO and therefore have a prolonged duration of action

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27
Q

What can adding a methyl group to the alpha carbon do?

A

Increases drugs ability to act as an indirect sympathomimetic and a direct sympathomimetic

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28
Q

What is an example of a drug with a methyl group added to the alpha carbon?

A

Amphetamine

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29
Q

The outcome of giving a drug is dependent upon 3 things:

A
  1. Selectivity for alpha and beta receptors
  2. Pharmacologic action at the receptors (at/antag)
  3. Action of body’s compensatory mechanisms to maintain homeostasis (ie: desensitization)
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30
Q

Where are alpha 1 receptors located in the cardiovascular system?

A

Vascular beds

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31
Q

When an alpha 1 receptor is activated in the CV system what occurs?

A

Arterial and venous vasoconstriction –> inc. BP, a reflexive slowing of HR, but venous return also increases which increases stroke volume and maintains CO

(CO= HR x SV)

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32
Q

Name a drug that activates alpha 1 receptors in CV system. What does it treat?

A

Phenylephrine

Maintain BP in pt w/ poor organ perfusion
Treat stuffy nose (neosenephrine)

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33
Q

Where are alpha 2 receptors located in the CV system?

A

Vascular beds and CNS

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34
Q

When the peripheral alpha2 receptors are activated what occurs?

A

Vasoconstriction – but only when given locally, IV push, or very high oral doses

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35
Q

When the central alpha 2 receptors are activated what occurs?

A

A decrease in sym. activity –> dec. BP

*Needs to be given systemically

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36
Q

What is a therapeutic use involving alpha 2 receptors….what drug is commonly used?

A

Hypertension

Clonidine

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37
Q

If a beta 1 receptor is activated then what CV effects will be seen:

A

Inc. HR –> inc. CO

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38
Q

If a beta 2 receptor is activated then what CV effects will be seen?

A

Dec. BP

39
Q

What does stimulation of dopamine 1 receptors do in terms of the CV system?

A

Vasodilation

40
Q

Dopamine also binds to ____ and ____ receptors.

A

Alpha and beta

41
Q

A low dose of dopamine….

A

activates beta 2 receptors

42
Q

A medium dose of dopamine….

A

activates beta 1 receptors

43
Q

A high dose of dopamine…

A

activates alpha 1 receptors

44
Q

What receptors are present in the lungs and what does stimulation of these receptors cause?

A

Beta 2 receptors –> bronchodilation

45
Q

What receptors are present in the eyes and what does stimulation of these receptors cause?

A

Alpha receptors (in radial muscle) –> mydriasis

46
Q

What receptors are present in the GU system and what does stimulation of these receptors cause?

A

Alpha receptors (in bladder, sphincter, prostate, etc) –> promotes urine retention and ejaculation

47
Q

What receptors are present in salivary glands and what does stimulation of these receptors cause?

A

Beta receptors –> inc. salivation

48
Q

Sympathomimetics ______ glycogenolysis in liver via ______ _________.

A

Increase

Beta Receptors

49
Q

____ receptors increase lipolysis while ____ receptors decrease lipolysis.

A

Beta

Alpha 2

50
Q

____ receptors increase release of renin while ___ receptors decrease release of renin

A

Beta 1

Alpha 2

51
Q

Besides insulin and renin, what are 4 other hormones mediated by adrenergic receptors:

A
  1. Parathyroid hormone
  2. Calcitonin
  3. Thyroxine
  4. Gastrin
52
Q

Epinephrine is an agonist at ____ and ____ receptors

A

alpha and beta

53
Q

Epi causes a ____ in systolic BP due to _____. And it also ____ HR and CO due to _____.

A

Increase
Alpha 1
Increases
Beta 2

54
Q

NE causes an ____ in systolic BP due to ____. It also ____ HR and CO via _____.

A

increased
Alpha 1
Increased
Beta 1

55
Q

Phenylephrine

A

Direct alpha 1 agonist

Not inactivated by COMT…longer duration

Used as a decongestant and to raise BP

56
Q

Midodrine

A

Direct alpha 1 agonist (a prodrug…its hydrolyzed form is actually the alpha 1 agonist)

Inc. BP and treats orthostatic hypotension

57
Q

Name the 4 drugs that act as alpha 2 agonists and reduce blood pressure, treating HTN

A

“Gross Men Chew Gum”

Guanfacine
Methyldopa
Clonidine
Guanabenz

58
Q

What is dexmedetomidine used for? What type of sympathomimetic drug is it?

A

Acts in the CNS and used for sedation of patients in the ICU setting

Direct Alpha 2 Agonist

59
Q

What is an example of a direct alpha (1 and 2) agonist?

A

Oxymetazoline

60
Q

What does oxymetazoline do?

A

Alpha 1 action causes vasoconstriction and used as a decongestant

Alpha 2 reduces BP

61
Q

Name a non-selective beta agonist

A

Isoproterenol

62
Q

Isoproterenol: effects and what it is used for

A

Vasodilation (beta 2) –> dec. BP and mean arterial pressre

Positive chronotropic and inotropic effects (beta 1) –> inc. HR and CO

Variety of effects so not really used

63
Q

_____ is a beta 1 selective agonist.

A

Dobutamine

64
Q

Describe the actions of the two dobutamine isomers

A

(+) isomer: Beta 1 agonist, alpha 1 antagonist
–> Inc. CO w/o increase BP

(-) isomer: Alpha 1 agonist
–> Inc. BP

*When given together = positive inotropic effect w/ little change in BP

65
Q

What type of sympthomimetics are used to treat asthma and COPD?

A

Beta 2 selective agonists

66
Q

What type of sympathomimetics are used to relax uterine smooth muscle during labor?

A

Beta 2 selective agonists

67
Q

List the drugs used to treat asthma and COPD

A

“Albert Met Soloman Teaching Pilates Form”

Albuterol
Metaproterenol
Salmeterol
Terbutaline
Pirbuterol
Formoterol
68
Q

What is the drug (beta 2 selective agonist) used to relax uterine smooth muscle during early labor?

A

Ritodrine

69
Q

How would one classify ephedrine (pseudoephedrine)

A

Mixed-acting sympathomimetic

AKA: provides effects of alpha and beta receptors

70
Q

What are the two mechanisms in which indirect-acting sympathomimetics act?

A
  1. They displace stored catecholamines

2. Inhibit reuptake of released neurotransmitter by interferring w/ NET

71
Q

What do amphetamines release and what is their action within in the CNS system?

A

Cause release of NE and DA

They are a CNS stimulant meaning they inc. mood and alertness while dec. appetite

72
Q

What are the 3 amphetamine derivatives?

A
  1. Methamphetamine (crystal meth)
  2. Phenmetrazine
  3. Methyphenidate (Ritalin)
73
Q

How does methyphenidate work? (aka what does it treat)

A

(Ritalin) reduces reuptake of NE, improving its function in the brain in order to treat ADHD

74
Q

What two drugs can be used to treat patients w/ narcolepsy, obstructive sleep apnea, and shift work disorder?

What class are these drugs?

A

Modafinil and Armodafinil

Indirect acting sympathomimetics

75
Q

Patients taking an MAO inhibitor need to be warned not to consume ______ because of _______.

A

tyramine containing foods (aged foods)

Potentially dangerous HTN

76
Q

Describe tyramine actions

A

Causes release of stored catecholamines…similar actions to NE (alpha 1, alpha 2, beta 1)

77
Q

4 examples of catecholamine reuptake inhibitors:

A
  1. Atomoxetine
  2. Subutramine
  3. Doluxetine
    4 Cocaine
78
Q

Atomoxetine

A

Selective inhibitor of NE reuptake w/ mostly CNS effects (maybe inc. in BP)

Used to treat ADHD

79
Q

Subutramine

A

Serotonin and NE reuptake inhibitor

Appetite suppressant, but taken off the market recently b/c of negative CV effects

80
Q

Doluxetine

A

Serotonin and NE reuptake inhibitor

Antidepressant

81
Q

Cocaine

A

Inhibits peripheral reuptake of NE

In CNS, has amphetamine-like actions, more intense.

Inhibition of DA reuptake in pleasure center of brain –> leads to rapid addiction

82
Q

What would be used to treat a patient w/ hypotension?

A

Goal: Raise BP

Use alpha 1 agonists such as NE, phenylephrine

83
Q

What would you use to treat a patient in shock?

A

Positive inotropic agents such as dopamine and dobutamine

84
Q

What would you use to treat a patient w/ hypertension?

A

an alpha 2 agonist such as clonidine

85
Q

What would you use to treat orthostatic hypotension?

A

Alpha 1 agonist like midodrine

86
Q

What would you use in emergency cardiac measures?

A

Epinephrine

Isoproterenol

87
Q

What are the two goals of surgical use of sympathomimetics?

A
  1. Reduce blood loss at site of surgical manipulations

2. Slow diffusion of anesthetics away from site of administration

88
Q

What drugs are used to reduce blood loss at site of surgical manipulations?

A

Epi or cocaine

89
Q

What drugs slow diffusion of anesthetics away from site of administration?

A

Epi, NE, phenylephrine

90
Q

What drugs are used as a sinus decongestant?

A

Alpha 1 agonist –> cause vasoconstriction

Phenylephrine and Oxymetazoline (Afrin)
**No more than 3 days of use due to rebound effect!!!

91
Q

How are sympathomimetics used to treat anaphylaxis?

A

Epi activates alpha 1, beta1, and beta2 receptors to reverse symptoms of anaphylaxis

*Often use steroid or antihistamine in combination

92
Q

What are the 3 ways drugs can treat ophthalmic problems?

A
  1. Alpha 1 agonists cause mydriasis –> useful for eye exam
  2. Alpha 1 agonists used as decongestants to reduce red eye
  3. Alpha 2 agonists reduce intraocular pressure of glaucoma
93
Q

Three drugs used in the treatment of ADHD

A
  1. Methylphenidate (ritalin)
  2. Dextroamphetamine (Adderall)
  3. Lisdexamfetamine (Vynase)

Pharmacology (17 decks)

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