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Exam 4: Adrenergic Agents Flashcards

1
Q

Where would adrenergic drug act on?

A
  1. Effector cells through adrenoceptors (activated by NE/E)
  2. Neurons that release norepinephrine
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2
Q

What does adrenergic mean?

A

Admin of adrenaline (E) producing similar effects of stimulation the Sympathetic NS (adrenergic system)

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3
Q

Describe the adrenergic transmission/NE biosynthesis in a neuron?

A
  1. Tyrosine and Na+ enter the neuron through an aromatic L-amino acid transporter
  2. Tyrosine is converted into L-DOPA by Tyrosine hydroxylase
  3. L-DOPA -> Dopamine by DOPA-decarboxylase
  4. Dopamine is transported into a synaptic vesicle by VMAT while H+ leaves
  5. Dopamine is synthesized into NE by Dopamine B-hydroxylate
  6. Ca2+ mediates depolarization of neuron and vesicle exits to synaptic cleft and binds to a and b receptors
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4
Q

What are the post synaptic adrenergic the receptors?

A

a1, b1, b2

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5
Q

What is the adrenergic auto receptor?

A

a2

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6
Q

What is an autoreceptor?

A

Inhibitory receptor that prevents presynaptic neurons from releasing NE

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7
Q

What are the fates of NE after presynaptic neuron release?

A

Brownian motion push NE to different places
1. Bind to postsynaptic adrenergic receptors
2. Binds to autoreceptor
3. Goes back to presynaptic neuron through NE transporter and convert to DOPGAL by MAO

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8
Q

Draw the structure of NE

A
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9
Q

Draw the structure of VMA

A
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10
Q

Describe the major metabolism processes of NE for excretion

A
  1. NE under goes non-specific NON-CYP oxidative deamination by MAO to DOPGAL
  2. DOPGAL is metabolized by non-cyp aldehyde dehydrogenase into DOMA
  3. DOMA is synthesized to VMA (Vanillylmandelic acid) by non-cyp phase 2 COMT
  4. VMA is excreted into urine
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11
Q

What is the optimal structure for NE b2-receptor binding according to Easson- Stedman
Hypothesis?

A
  1. Catechol
  2. Beta OH
  3. Protonated amine
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12
Q

What bonds are associated with NE receptor binding?

A
  1. Optimal H-bond with 2 OH on catechol and 2 serines
  2. Pi-pistacking with catechol ring and Phe
  3. Ionic binding with protonated amine and Asp
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13
Q

Draw the structure of Epinephrine

A
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14
Q

Describe the difference between +E and -E configurations

A

+E does not fully occupy the Receptor site from the secondary OH (less active)
-E fully binds to receptor by secondary OH (more active)

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15
Q

What are the a1 signaling molecules?

A

Gq, Gi, Go

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16
Q

What are the tissue effects of a1 receptors?

A
  1. Vascular smooth muscle contraction
  2. Genitourinary smooth contraction
  3. Intestinal smooth muscle relaxation
  4. Increased isotropy and excitability in heart
  5. Glycogenolysis and gluconeogensis in liver
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17
Q

What are the signaling molecules of a2?

A

Gi and Go

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18
Q

What are the tissue effects of a2?

A
  1. Decreased insulin secretion by pancreatic b-cells
  2. Platelet aggregation
  3. Decreased nerve NE release
  4. Vascular smooth muscle contraction
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19
Q

What are the tissue effects of B1?

A
  1. Increased chronotropy and inotropy in heart
  2. Increased AV node conduction velocity in heart
  3. Increased renin secretion in Renal juxtaglomerular cells
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20
Q

What are the signaling mediators of B2?

A

Gs

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21
Q

What are the tissue effects for B2?

A
  1. Smooth muscle relaxation
  2. Glycogenolysis and gluconeogensis in liver
  3. Glycogenolysis and K+ uptake in skeletal muscle
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22
Q

What are the signaling mediators for B1?

A

Gs

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23
Q

What are the B3 signaling mediators?

A

Gs

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24
Q

What are the tissue effects of B3?

A

Lipolysis in adipose tissue

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25
Q

What receptor types are associated with arteriole constriction?

A

a1, a2

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26
Q

What receptor types are associated with skeletal muscle dialtion?

A

B2

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27
Q

What receptor types are associated with radial eye muscle contraction (miosis)?

A

a1

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28
Q

What receptor types are associated with lung relaxation (bronchodilation)?

A

B2

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29
Q

What receptor types are associated with gluconeogenesis and glycogenolysis?

A

a1, b2

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30
Q

What receptor types are associated with lipolysis in fat cells?

A

a1, b3

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31
Q

What receptor types are associated with uterine contraction (pregnant)?

A

a1

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32
Q

What receptor types are associated with decrease in intestine motility?

A

a1, b2

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33
Q

What is the therapeutic use for a1 agonists?

A
  1. Shock, hypotension (raise BP)
  2. Nasal decongestants
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34
Q

What is the therapeutic use for a1 antagonists?

A

Antihypertensives

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35
Q

What is the therapeutic use for a2 agonists?

A
  1. Antihypertensives
  2. Glaucoma
  3. Analgesia
  4. Sedatives
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36
Q

What is the therapeutic use for b1 antagonists?

A
  1. Antihypertensives
  2. Antiarrhythmics
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37
Q

What is the therapeutic use for b2 agonists?

A

Bronchodilators (asthma and COPD)

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38
Q

What is the therapeutic use for b3 agonists?

A

Weight loss

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39
Q

What is myriad effect of a1?

A
  1. Vasoconstriction
  2. Increased peripheral resistance
  3. Increased BP
  4. Mydriasis
  5. Increased closure of sphincter of bladder
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40
Q

What is myriad effect of a2?

A
  1. Inhibition of NE release
  2. Inhibition of ACh release
  3. Inhibition of insulin release
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41
Q

What is myriad effect of b1?

A
  1. Tachycardia
  2. Increased lipolysis
  3. Increased myocardial contractility
  4. Increased renin release
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42
Q

What is myriad effect of b2?

A
  1. Vasodilation
  2. Decreased peripheral resistance
  3. Bronchodilation
  4. Increased muscle and liver glycogenolysis
  5. Increased release of glucagon
  6. Relaxed uterine smooth muscle
43
Q

Why is catechol unstable?

A
  1. Catechol oxides when exposed to air (solutions darken)
  2. Rapid metabolism by COMT
44
Q

How does a1 agonist cause vascular constriction?

A

Induces the phosphorilization of myosin causing smooth muscle contraction

45
Q

How does a1 antagonists cause vascular constriction?

A

It doesn’t not cause relaxation but lessens contraction frequency by dephophorilizing Myosin

46
Q

Why do nonselectiv a1 agonists have limited clinical significance?

A

Selectivity issues and poor oral bioavailability

47
Q

In what ways is Epi more clinically relevant as an a1 agonists compared to NE?

A
  1. Assists with trauma (b-stimulation of cardiac muscle
  2. Trauma based-hypotension from bleeding incidents
48
Q

What are examples of phenylethanolamine selective a1 agonists?

A
  1. Phenylephrine
  2. Metaraminol
  3. Methoxamine
49
Q

What are examples of 2-arylimidazoline selective a1 agonists?

A
  1. Xylometazoline
  2. Oxymetazoline (Afrarin)
  3. Tetrahydrozoline (Visin)
  4. Naphazoline
50
Q

What is the therapeutic use of tetrahydrozoline?

A

Reduces redness in eye by vasoconstriction

51
Q

What is the therapeutic use of oxymetazoline?

A

Vasoconstrictor in nasal cavity

52
Q

What is the cardiac activity of a1 agonists?

A

Minimum cardiac stimulation (little b activity)

53
Q

How does a1 agonist serve as vasoconstrictors?

A
  1. Nasal decongestants
  2. Red eye
54
Q

What is the therapeutic use for phenylephrine?

A

Decongestant and Vasoconstrictor

55
Q

What would you expect about a1-agonist DOA as compared to NE/Epi?

A

Longer due to Carbon ratio

56
Q

How does a2 agonist structure differ from a1 agonist?

A

Structurally related but have opposite effects
1. Initial a1 effect, then overpowered by a2
2. Used as sedatives and epidural enhancers
3. N-C spacer

57
Q

Describe the clonidine (catapres) therapeutic use

A

Flagship compound used as a nasal decongestant with hypotensive properties

58
Q

What are examples of selective a2- agonist (2-aminoimidazolines)?

A
  1. Clonidine (Catapres)
  2. Apraclonidine (Iopidine)
  3. Brimonidine (Alphagan)
  4. Tizanidine
59
Q

What is the therapeutic use for Apraclonidine (Iopidine) and Brimonidine (Alphagan)?

60
Q

How does Brimonidine compare to clonidine and apraclonidine?

A
  1. 1000x more selective a2 agonist
  2. First line treatment for glaucoma
  3. Topical formulation with little systemic effect
61
Q

What are the selective guanidine a2 agonists?

A

Guanfacine (Tenex®) and Guanabenz (Wytensin®)
- Imidazle ring is not necessary
- Similar to clonidine

62
Q

How does Methyldopa (Aldomet®) differ from other a2-agonists?

A

1, Not a phenylethanolamine
2. Metabolized to active compound
3. Antihypertensive during pregnancy

63
Q

What are the characteristics of B1 agonism?

A
  1. Cardiac stimulation increasing contractile force
  2. Not strictly adrenergic drugs, but catecholamine
  3. Cardiac stimulate for post-surgical
64
Q

Examples of B1 agonists?

A

Dopamine and Dobutamine

65
Q

What are the b2 adrenergic effect?

A
  1. Bronchodilation
  2. Short and long acting
  3. Asthma and chronic pulmonary diseases
66
Q

What is the difference between Salmetero and Albuterol?

A

Albuterol is emergency use not for chronic
Salmetero is a daily medication

67
Q

Describe the SAR of b2-phenylethanolamine adrenergic?

A

AR-C-C-N > AR-C-N > AR-C-C-C-N
b-OH important for b2 selectivity
1o or 2o amine (ionizable)
R > CH3 decreases B-activity
R = t-butyl selective for B2

68
Q

What are examples of short-acting adrenergic agonists?

A
  1. Isoproterenol
  2. Albuterol
  3. Pirbuterol
  4. Levalbuterol
69
Q

Describe the characteristics of Isoproterenol

A
  1. Little selectivity
  2. B1 side effects
  3. Not clinically relevant
  4. Instability due to catechol
70
Q

What makes a drug B2 selective?

A

t-butyl group

71
Q

What’s an example of long-acting b2 agonists?

A
  1. Salmeterol (Serevent) w/ Fluticasone = Advair Diskus
  2. Formoterol (Formadil) w/ Budesonide = Symbicort
72
Q

What makes Salmeterol long acting?

A

Lipophilic side chain interacts with b-exocite and log P is greater than albuterol

73
Q

How does Salmeterol bing to B2-receptors?

A

Lipophilic side chain continues to bind to exocite
After amine dissociates from receptor -
thus, long-acting

74
Q

How does Formoterol compare to Salmeterol?

A

4xs more potent and has faster onset

75
Q

What is the relationship between onset and DOA of B1-agonists?

A

Faster onset does not mean longer duration

76
Q

What is indirect action?

A

Drug enhances release of NE from vesicles

77
Q

What is direct action?

A

Directly activates receptors

78
Q

What is mixed action?

A

Drug acts both directly and indirectly

79
Q

What is the therapeutic use of ephedrine and pseudoephedrine?

A

Nasal decongestant and raise BP

80
Q

What is the clinical use for mixed acting sympathomimetic?

A
  1. Nasal decongestant
  2. Oral vs local route of admin
  3. Increase BP
  4. Most effects come from indirect action, direct but over taken by indirect
  5. a and b binding
  6. Increase NE and E released
81
Q

What the main catecholamine drugs?

A
  1. E
  2. NE
  3. Isoproterenol
  4. Dopamine
  5. Dobutamine
82
Q

What are characteristics of catecholamines?

A
  1. Rapid onset of action
  2. Brief duration of action
  3. Not administered orally
  4. Doesn’t penetrate the BBB
83
Q

What is the receptor specificity for epinephrine?

A

a1, a2, b1, b2

84
Q

What is the therapeutic uses of epinephrine?

A
  1. Acute asthma
  2. Anaphylactic shock
  3. In local anesthetic to increase duration of action
85
Q

What is the receptor specificity for norepinephrine?

A

a1, a2, b1

86
Q

What is the therapeutic uses of norepinephrine?

A

Treatment of shock

87
Q

What is the therapeutic uses of isoproterenol?

A

cardiac stimulant

88
Q

What is the receptor specificity of isoproterenol?

89
Q

What is the therapeutic uses of dopamine?

A
  1. Shock
  2. Congestive heart failure
  3. Raise BP
90
Q

What is the receptor specificity dopamine?

A
  1. Dopaminergic
  2. a1, b1
91
Q

What is the receptor specificity dobutamine?

92
Q

What is the therapeutic use of dobutamine?

A

Acute heart failure

93
Q

What is the receptor specificity of oxymetazoliene?

94
Q

What is the therapeutic use of oxymetazoline?

A

Nasal decongestant

95
Q

What is the receptor specificity of Phenylephrine?

96
Q

What is the therapeutic uses of methoxamine?

97
Q

What is the therapeutic use of methoxamine?

A

Superventricular tachycardia

98
Q

What is the receptor specificity of clonidine?

99
Q

What is the receptor specificity of albuterol and terbutaline?

100
Q

What is the receptor specificity of salmeterol and formoterol?

101
Q

What is the receptor specificity of amphetamine?

102
Q

What is the therapeutic uses of amphetamine?

A

CNS fo narcolepsy and appetite control

103
Q

What is the receptor specificity of ephedrine and pseudoephedrine?

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