Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology - Exam 2 > Adrenergic Agonists > Flashcards

Adrenergic Agonists Flashcards

1
Q

What is the general term for NT/hormones in the sympathetic NS?

A
  • catecholemines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the major catecholamines?

A
  • dopamine (DA)
  • norepinephrine (NE)
  • epinephrine (E)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the categories of adrenergic receptors?

A
  • alpha 1 (a1)
  • alpha 2 (a2)
  • beta (1, 2, 3)
  • dopamine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What type of receptors are adrenergic receptors?

A
  • GPCRs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the factors that can alter the degree to which any adrenergic receptor responds?

A
  • selectivity
  • regulation
  • polymorphisms
  • catacholamine metabolism
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What does receptor selectivity allow for?

A
  • specific binding

- i.e. drug x only binds to a1 receptors but not a2 or b receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What effects degree of drug binding?

A
  • [drug]
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What does [low drug] allow for?

A
  • selective binding
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What does [high drug] cause?

A
  • non-selective binding

- i.e. larger [ ] flood receptors that usually do not bind the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is receptor regulation?

A
  • increasing or decreasing the number of receptors based on the long term exposure
  • i.e. up/down regulation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What does receptor regulation result in?

A
  • changes in the observed response to sympathomimetic drugs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is an example of receptor regulation?

A
  • desensitization (aka: tolerance, refractoriness, tachyphylaxis)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Describe desensitization

A
  • decrease responsiveness of that cell/tissue to additional stimulation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are the mechanisms of desensitization?

A
  • altered transcription/translation of DNA and/or RNA
  • modifications of receptors via interactions with enzymes or other proteins
  • long term exposure to an agonist
  • interactions or messages from other receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the desired therapeutic benefit of using desensitization?

A
  • results in an increased response followed by the desired decreased physiological action
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Describe receptor polymorphism

A
  • slight changes in a.a. sequences can occur in different people
  • explains why some drugs work better in some people vs. others
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What are the mechanisms of NT termination?

A
  • NE transporter (NET)
  • diffusion
  • metabolism by COMT or MAO
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is the most important mechanism of NT termination?

A
  • NET
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Describe the action of NET

A
  • pre-synaptic pump to move NE out of synapse and back into neuron (reuptake)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

How does NET act as a therapeutic target?

A
  • NET inhibition prolongs the presence of NE in the synaptic cleft leading to increased stimulation of adrenergic receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are drugs that are able to bind and inhibit NET action?

A
  • atomoxetine (used in ADHD)

- cocaine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is the action of catechol-O-methyl transferase (COMT)?

A
  • metabolizes all catecholemines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is a drug that inhibits COMT and what is its clinical use?

A
  • entacapone

- Parkinson’s

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What is the action of monoamine oxidase (MAO)?

A
  • metabolizes endogenous monoamines (i.e. linezolind)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Define sympathomimetic

A
  • drug that mimics actions of NE, E, and DA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Define direct agonist sympathomimetics

A
  • structure allows for binding to adrenergic receptors resulting in activation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Define indirect agonist sympathomimetics

A
  • cause release of stored catecholamines

- inhibits reuptake of catecholamines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

What are the locations that changes can be made on sympathomimetic drugs?

A
  • benzene ring
  • beta C
  • alpha C
  • amino group
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What is the major target of sympathomimetics?

A
  • CV system
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Where are a1 and b2 receptors in CV system?

A
  • vascular
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Where are b1 receptors in CV system?

A
  • heart
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

What is the outcome of giving a drug dependent on?

A
  • selectivity for a v. b receptors
  • pharmacologic action at the receptors (agonist/antagonist)
  • action of body’s compensatory mechanisms to maintain homeostasis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Which receptors in the CV system cause vasoconstriction?

A
  • a1
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Which receptors in the CV system cause vasodilation?

A
  • b2
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

What are the effects in the CV of a1 receptor activation?

A
  • vasoconstriction leads to increased BP which causes reflex decrease on HR
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

What is an example of a CV system a1 agonist and when is it used?

A
  • phenylephrine

- nasal decongestion and maintaining BP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What is the effect of peripheral a2 agonists in the CV system?

A
  • vasoconstriction, but only when given locally, IV push, or very high oral doses
  • rare
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

What is the effect of central a2 agonists in the CV system?

A
  • inhibits sympathetic vascular tone

- lowers BP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

What is an example of a CV system a2 agonist and when is it used?

A
  • clonidine

- HTN

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

What are the effects of a b1 receptor agonist in heart?

A
  • increase contractility
  • increase HR
  • increase CO
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

What are the effects of a b2 receptor agonist in the vasculature?

A
  • decrease resistance aka vasodilation

- decreased BP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

What is the effect of DA on d1 receptors in CV system?

A
  • vasodilation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

Where does DA bind in low doses?

A
  • b2 receptors, specifically renal
44
Q

Where does DA bind in medium doses?

A
  • b1 receptors to increase HR and contractility
45
Q

Where does DA bind in high doses?

A
  • a1 receptors to increase BP
46
Q

What receptors are activated by sympathomimetics in the lungs and what is the effect?

A
  • b2

- bronchodilation

47
Q

What receptors are activated by sympathomimetics in the eye and what is the effect?

A
  • a

- mydriasis, increase outflow of aqueous humor, decreases IOP

48
Q

What receptors are activated by sympathomimetics in the GU tract and what is the effect?

A
  • a receptors

- urine retention and mediate ejaculation

49
Q

What receptors are activated by sympathomimetics in the salivary glands and what is the effect?

A
  • b receptors

- increase salivation

50
Q

What is the effect of sympathomimetics on the apocrine sweat glands in the hands?

A
  • increased sweat production in response to stress
51
Q

What receptors are activated by sympathomimetics in metabolism and what is the effect?

A
  • b receptors

- increased glycogenolysis increases serum glucose which results in increased insulin

52
Q

What are the effects of sympathomimetics on the CNS dependent on?

A
  • ability to cross BBB
53
Q

What are the endogenous catecholamines?

A
  • NE
  • E
  • DA
54
Q

At which receptors does E act as an agonist?

A
  • a1 & 2

- b1 & 2

55
Q

What are the primary effects of E?

A
  • vasoconstrictor

- cardiac stimulant

56
Q

What are the secondary effects of E?

A
  • increased systolic BP due to a1 binding
  • increased HR and CO due to b1 binding
  • vasodilation due to b2 binding but only in skeletal m.
57
Q

At which receptors does NE act as an agonist?

A
  • a1 & 2

- b1

58
Q

What are the primary effects of NE?

A
  • vasoconstrictor

- cardiac stimulant

59
Q

What are the secondary effects of NE?

A
  • increased systolic BP due to a1 binding
  • increased HR and CO due to b1 binding

same as E

60
Q

What is a brand name for NE?

A
  • Levophed (leave them dead)
61
Q

What are the effects of DA in the CV system based on?

A
  • doses
62
Q

What is the effect of low does DA on the CV and where does it bind?

A
  • vasodilation

- b2

63
Q

What is the effect of medium dose DA on the CV and where does it bind?

A
  • increase HR and CO

- b1

64
Q

What is the effect of high dose DA on the CV and where does it bind?

A
  • vasoconstriction

- a1

65
Q

What is an action of DA on the CNS?

A
  • development of addiction based on reward stimuli
66
Q

A deficiency of ______ can contribute to ______ disease.

A
  • DA

- Parkinson’s

67
Q

What type of receptors are targets for antipsychotic drugs?

A
  • DA
68
Q

What are the main effects of direct a1 agonists?

A
  • vasoconstriction

- increase BP

69
Q

What are two examples of direct a1 agonists and what are their uses?

A
  • phenylephrine (neosynephrine): decongestant and raise BP

- midodrine (Amantine): increase BP and tx orthostatic HTN

70
Q

What is the main effect of direct a2 agonists?

A
  • decrease BP
71
Q

What is the classic example of a direct a2 agonist and what is it used for?

A
  • clonidine (Catapres): reduce BP and tx HTN (preeclampsia)
72
Q

What are the effects of direct a1 AND a2?

A
  • local vasoconstriction
73
Q

What is an example of a direct a1 AND a2 drug and what is it used for?

A
  • oxymetazoline (Afrin): decongestant
74
Q

What is an example of a nonselective b agonist and what are the effects?

A
  • isoproterenol (Isuprel): vasodilation via b2; decreased BP and MAP; increased HR and CO
75
Q

What is the primary effect of b1 selective agonists?

A
  • increase CO and HR
76
Q

How does dobutamine produce its effects without changing BP?

A
  • (+) isomer gives b1 action and a1 antagonism
  • (-) isomer gives a1 agonism
  • a1’s cancel each others effects out*
77
Q

What is the effect of b2 selective agonist?

A
  • bronchodilation

- relax uterine smooth m.

78
Q

What are examples of b2 selective agonists for each of its effects and what are they used to treat?

A
  • albuterol/salmeterol: asthma and COPD

- ritodrine/terbulatine: premature labor

79
Q

What effects are seen with mixed-acting sympathomimetics?

A
  • both a and b, combo effects

- i.e. vasoconstriction, decongestion, bronchodilation, appetite suppression, and CNS stimulation (fight or flight)

80
Q

What are examples of mixed-acting sympathomimetic?

A
  • ephedrine

- pseudoephedrine

81
Q

What are the indications and contraindications for psuedoephedrine?

A
  • indications: congestion (decongestant)

- contraindications: HTN

82
Q

What are two mechanisms for indirect-acting sympathomimetics?

A
  • displace stored catecholamines

- inhibit reuptake of released NT by interfering with NET

83
Q

What are examples of indirect-acting sympathomimetics?

A
  • amphetamine/meth/phenmetrazine/methylphenidate (Ritalin)
  • tyramine
  • catecholamine reuptake inhibitors
84
Q

What are the actions of indirect-acting sympathomimetics?

A
  • release stored NE and DA
  • increase mood and alertness
  • decrease appetite
85
Q

What is a therapeutic use for methyphenidate and how does it work?

A
  • Ritalin
  • tx: ADHD
  • reduces uptake of NE, ‘evens things out’
86
Q

What is the action and therapeutic use of modafinil or armodafinil?

A
  • indirect sympathomimetic
  • inhibits NE and DA transporters in CNS
  • increases wakefulness
  • tx: nacolepsy, obstructive sleep apnea, and shift work disorders
87
Q

What is the action of tyramine?

A
  • releases stored catecholamines
88
Q

What metabolizes tyramine?

A
  • MAO
89
Q

Who should avoid foods containing tyramine?

A
  • patients on MAOIs
90
Q

What are the therapeutic uses of catecholamine reuptake inhibitors?

A
  • ADHD
  • appetite suppressant
  • antidepressant
91
Q

What is the key feature of cocaine?

A
  • inhibition of DA reuptake in pleasure center of brain leading to rapid addiction via stimulation of b1
92
Q

What could be used to treat hypotension?

A
  • a1 agonists to raise BP

- i.e. NE, phenylephrine

93
Q

What could be used to treat HTN?

A
  • a2 agonists

- i.e. clonidine

94
Q

What could be used to treat orthostatic HTN?

A
  • a1 agonist

- i.e. midrodrine

95
Q

What is used in emergency cardiac resuscitation?

A
  • a1 and b2

- E

96
Q

What can be used to reduce blood loss at surgical site?

A
  • a1 agonist

- E or cocaine

97
Q

What can be used to slow diffusion of anesthetics away from admin site?

A
  • a1 agonist

- lido + E, NE, phenyleprine

98
Q

What can be used to treat sinus congestion?

A
  • a1 agonist

- oxymetazoline (Afrin)

99
Q

What is a concern when taking an a1 agonist to treat sinus congestion?

A
  • limit use to no more than 3 days due to risk of rebound effect
100
Q

What can be used to treat asthma and COPD?

A
  • b2 selective agonists

- albuterol/salmeterol

101
Q

How are anyphylactic reactions treated?

A
  • a1, b1, b2 agonists

- E (EpiPen) often in combo with steroid of antihistamine

102
Q

What can be used to facilitate eye examinations?

A
  • a1 agonists
103
Q

What can reduce eye redness associated with allergies?

A
  • a1 agonist
104
Q

What can reduce IOP in patients with glaucoma?

A
  • a2 agonist

- apraclonidine (Lopidine) and brimonidine (Alphagan)

105
Q

What can be used to prevent premature labor?

A
  • b2 selective agonists

- ritodrine, terbutaline

106
Q

What can be used to improve patient comfort in the ICU?

A
  • a2 agonists

Pharmacology - Exam 2 (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions