Adrenergic Pharm Flashcards

1
Q

T/F: The interstitial fluid has a similar composition to seawater.

A

True

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2
Q

T/F: The interstitial fluid has high concentration of Na+, and the cells have high concentration of K+.

A

True

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3
Q

Which component (cell of IF) has a higher Ca++ and Cl- concentration?

A

Interstitial fluid

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4
Q

What is the major and minor components involved in establishing a resting membrane potential?

A

Major: K+ channels in the cell membrane

Minor: ion flux from Na+/K+ ATPase pump

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5
Q

T/F: K+ is 100x more permeable than Na+.

A

True

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6
Q

Describe how the permeability of K+ leads to a resting potential.

A

K+ concentrations stay high in the cell from ATPase -> due to permeability they constantly flow out of the cell from high concentration to low

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7
Q

Is the efflux of K+ constant?

A

It continues until the chemical force leading K+ out of cell (gradient) is balanced by the electrical force bringing it back in

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8
Q

What happens when a cell receives an action potential?

A

Becomes permeable to Na+ which counteracts the flow of K+ and depolarizes the cell

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9
Q

T/F: K+ conductance is slower than Na+ conductance in an action potential.

A

True

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10
Q

What two systems are primarily responsible for maintaining homeostasis?

A

Autonomic nervous system and endocrine system

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11
Q

What three body systems are under control of the autonomic nervous system?

A

Smooth muscle, heart, secretory glands

*secretory glands can self regulate

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12
Q

The somatic nervous system uses __________ to stimulate ________ receptors.

A

acetylcholine; nicotinic

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13
Q

T/F: All parts of the autonomic system use acetylcholine to stimulate nicotinic receptors in the ganglia.

A

True

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14
Q

The sympathetic nervous system uses _________ as a post-ganglionic nt to stimulate ________ receptors.

A

norepinephrine; adrenergic

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15
Q

The parasympathetic nervous system uses ___________ as a post-ganglionic nt to stimulate _________ receptors.

A

acetylcholine; muscarinic

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16
Q

How is the signal conducted in the adrenal medulla?

A

Symp: acetylcholine -> nicotinic receptor in medulla -> stimulates release of epinephrine into blood stream to stimulate adrenergic receptors

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17
Q

Altering which system can have the most widespread effects?

A

The adrenal system (EPI and NE)

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18
Q

What are the precursors to adrenergic amines?

A

tyrosine -> DOPA -> dopamine -> norepinephrine -> epinephrine

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19
Q

What happens to the NT after the signal is transduced in adrenergic transmission?

A

Transmitter is transported back into the presynaptic terminus

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20
Q

What happens to the NT after signal transduction in cholinergic transmission?

A

NT hydrolyzed in the synapse

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21
Q

Once the NT reaches the target organ, how is the signaling likely to continue?

A

Some type of chemical signaling pathway; not an action potential

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22
Q

What is the rate limiting step in the synthesis of adrenergic amines?

A

Tyrosine hydroxylase - turns tyrosine into L-DOPA

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23
Q

Where does the synthesis of catecholamines happen?

A

Sympathetic nerve terminals and adrenal medulla

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24
Q

Where are dopamine receptors found?

A

In the CNS, kidneys, and some smooth muscles

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25
Q

What are the important adrenergic receptors in the PNS?

A

alpha1, alpha2, beta1, and beta2

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26
Q

What is the major function of alpha1 receptors on smooth muscle cells?

A

Increase Ca++ via Galpha(q) and IP3 -> increase myosin light chain kinase activity -> phosphorylation of myosin light chain and therefore increase muscle activity

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27
Q

Agents increasing Ca++ in the __________ cell will act as smooth muscle _________.

A

smooth muscle; constrictors

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28
Q

What is the role of alpha2 receptors?

A

Inhibit epinephrine and norepinephrine release

Important at presynaptic termini

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29
Q

What is the difference between the adrenergic and cholinergic systems?

A

Adrenergic = sympathetic - uses norepinephrine and epinephrine (adrenaline)

Cholinergic = parasympathetic - uses ACh

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30
Q

T/F: The alpha2 receptor is more important in the CNS than the PNS.

A

True

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31
Q

What will be the effect of an alpha2 agonist?

A

Reduce CNS response

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32
Q

What will be the effect of an alpha2 antagonist?

A

Enhance CNS response

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33
Q

An alpha1 agonist is a ________, and will ________ BP.

A

vasoconstrictor; raise

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34
Q

An alpha1 antagonist is a _________, and will _______ BP.

A

vasodilator; lower

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35
Q

Describe how an alpha2 agonist will act on the brain and vessels.

A

Will reduce brains signal to the vessel smooth muscles and will allow vessels to dilate

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36
Q

Describe how an alpha2 antagonist will act on the brain and vessels.

A

Antagonist will block receptor from reducing signal -> signal will get to the vessel smooth muscles telling them to contract -> vasoconstriction

37
Q

Where and how do alpha1 agonists act?

A

Activate alpha1 receptor in vessel smooth muscles -> muscle contraction -> vasoconstriction

38
Q

Where and how do alpha1 antagonists act?

A

Deactivate alpha1 receptors in vessel smooth muscles -> no muscle contraction -> vasodilation

39
Q

What is the effect of alpha2 agonists and antagonists on heart rate?

A

When alpha2 is activated (agonist) heart rate will be decreased

40
Q

What type of GPCR is activated via beta2 receptors in the smooth muscle?

A

Gaplha(s)

41
Q

What happens after a beta2 receptor activates a Galpha(s) in the smooth muscle?

A

adenylate cyclase converts ATP to cAMP -> PKA is activated -> myosin light chain kinase inhibited and Ca++ levels lowered -> less muscle contraction

42
Q

On smooth muscle cells, the activation of alpha1 receptors will cause _______, while activation of beta2 receptors will cause ________.

A

contraction; relaxation

43
Q

How do beta2 receptors diminish Ca++ levels in the cell?

A

PKA activates K+ channels leading to hyperpolarization

44
Q

Where are beta1 receptors found?

A

Cardiac muscle

45
Q

What is the effect of beta1 receptor activation?

A

Activates PKA -> activate L type Ca++ channels -> increase Ca++ levels lead to increased contraction -> increased HR and contraction strength

46
Q

What are three major outcomes of beta2 receptor activation?

A
  1. Reduce blood pressure
  2. Broncho dilation
  3. Reduce uterine contraction
47
Q

T/F: There are more alpha1 receptors than beta2 receptors on vascular smooth muscle.

A

True

48
Q

Epinephrine comes into contact with a vascular smooth muscle cell. What will be the outcome and why?

A

Both alpha1 and beta2 receptors will be activated. Blood pressure will increase because alpha1 response dominates the beta2 response.

49
Q

T/F: Norepinephrine activates all alpha and beta receptors.

A

False

Epinephrine activates them all

Norepinephrine does not activate beta2

50
Q

Why is there epinephrine in local anesthetic?

A
  1. Prolong duration and increase success of nerve block
  2. Diminish systemic toxicity
  3. Minimize blood loss during surgury
51
Q

What happens when epinephrine is given in a small dose?

A

The activation of beta2 receptors can dominate leading to a decrease in BP

52
Q

What is the typical response to E and NE in non vascular smooth muscle?

A

Relaxation mediated by beta2 receptors

53
Q

Which receptors mediate sphincter contraction?

A

Alpha

54
Q

What is the net effect of E and NE on salivary glands?

A

Modest secretion with high protein content (alpha1 and beta1)

55
Q

T/F: Peripherally administered E and NE cause feelings of anxiety and jitteriness via the CNS.

A

False

Peripherally administered E and NE do not cross the BBB

56
Q

T/F: Norepinephrine is used to treat anaphylaxis.

A

False

Need epinephrine because b2 receptors must be stimulated for bronchodilation

57
Q

_________ is an alpha1 receptor agonist sometimes used instead of epinephrine as a vasoconstrictor in conjunction with a local anesthetic.

A

Levonordefrin

58
Q

________ is an alpha1 receptor agonist often used to treat hypotension during surgery.

A

Metaraminol

59
Q

List some common alpha1 agonists used in oral decongestants.

A

Methoxamine, Phenylephrine, midodrine, oxymetazoline

60
Q

What are some alpha2 agonists that are used to treat hypertension via autonomic regulation of the cardiovascular system?

A

Clonidine, guanfacine, guanoxabenz, methyldopa

61
Q

_________ is an alpha2 agonist used primarily to treat ADHD.

A

Clonidine

62
Q

________ is an alpha2 agonist used as a sedative.

A

Dexmedetomidine

63
Q

________ is ab alpha2 agonist used as a muscle relaxant.

A

Tizanidine

64
Q

What is the primary purpose of beta1 agonists?

A

Treatment of heart failure and cardiogenic shock

65
Q

What are some examples of beta1 agonists?

A

Denopamine, dobutamine, xamoterol, isoprenaline

66
Q

What is the most common application of drugs like albuterol, pirbuterol, formoterol, and clenbuterol?

A

Beta2 agonists

Used to treat respiratory disease (e.g. asthma)

67
Q

What are the most serious complications involved with alpha and beta agonists?

A
  1. Myocardial ischemia
  2. Heart attack
  3. Arrhythmias
68
Q

What can be a common side effect to alpha2 agonists?

A

CNS disturbances

69
Q

What is the general purpose of alpha1 adrenergic receptor antagonists?

A

Relaxing smooth muscle

70
Q

What are some problems that can be treated by relaxing vascular smooth muscle?

A
  1. Hypertension
  2. Pulmonary hypertension
  3. Hemodynamic shock
  4. Raynaud’s disease
71
Q

Conditions associated with increased sympathetic activity can be treated with alpha1 _________.

A

antagonists

72
Q

What two alpha1 antagonists are used to treat BPH?

A

Alfuzosin and tamulosin

73
Q

__________ is a non-selective alpha adrenergic receptor agonist that is sometimes used to reverse soft tissue numbness after dental procedures.

A

Phentolamine

74
Q

T/F: Beta3 blockers are common in practice.

A

False

There are none

75
Q

T/F: Beta blockers are typically either non-selective or selective for B2 receptors.

A

False

Either non-selective or selective to block B1.

Typically do not want to block B2

76
Q

What are the general effects of beta blockers?

A
  1. Decrease heart rate

2. Decrease blood pressure

77
Q

How do beta blockers lower blood pressure?

A

Decreased renin release in the kidneys

78
Q

What is the effect of ISA in beta blockers?

A

Beta blockers without ISA will have a stronger effect than those with ISA

79
Q

Why would you use beta blockers to treat CHF?

A

Reduce catecholamine production that is increased during CHF

80
Q

How do beta blockers help treat ischemic heart disease and post-myocardial infarction?

A

Reduce O2 consumption -> less ROS

81
Q

T/F: Patients taking beta blockers are most likely just dealing with a minor disease.

A

False

Can be anything from minor to major

82
Q

What are some adverse effects of beta blockers?

A

Heart: bradycardia, AV block

Smooth muscle: reduced vasodilatory response, increase bronchospasms

Metabolic: hypoglycemia

Negative CNS effects

83
Q

Which types of drugs can cause orthostatic hypotension (trouble when they stand up)?

A

Alpha antagonists

84
Q

A patient taking which type of drugs is more at risk for a hypertensive episode after receiving local anesthetic with vasoconstrictor?

A

non-selective beta blockers

*beta2 mediated vasodilation blocked

85
Q

________ causes xerostomia.

A

Clonidine

86
Q

Many drugs belonging to which group end in -zosin?

A

alpha1 antagonists

87
Q

Many drugs belonging to which group end in -olol?

A

beta antagonist

88
Q

Many drugs belonging to which group end in -ilol or -alol?

A

Beta antagonist with alpha1 activity