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PHS 931 > Block 1 Lecture 6 -- Adrenergics > Flashcards

Block 1 Lecture 6 -- Adrenergics Flashcards

1
Q

Describe NT affinity for alpha receptors.

A

EPI ~ NE&raquo_space; ISO

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2
Q

Describe NT affinity for beta receptors.

A

ISO > EPI > NE

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3
Q

Where are alpha1 receptors located?

A

vascular, glandular smooth muscle

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4
Q

Where are alpha2 receptors located?

A

presynaptic nerve terminals

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5
Q

Where are beta1 receptors located?

A

cardiac muscle

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6
Q

Where are beta2 receptors located?

A
    • vascular, bronchiole smooth muscle
    • skeletal muscle
    • liver
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7
Q

Where are beta-3 receptors located?

A

adipose

bladder smooth muscle

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8
Q

What type of GPCR is alpha-1?

A

Gq

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9
Q

What type of GPCR is alpha-2?

A

Gi

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10
Q

What type of GPCR are the beta receptors?

A

Gs

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11
Q

alpha-1 agonists cause:

A

contraction of vascular and glandular smooth muscle

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12
Q

alpha-2 agonists cause:

A

decreased NE release from pre-synaptic nerve terminals

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13
Q

beta-1 agonists cause:

A

increased HR + FOC in cardiac muscle

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14
Q

beta-2 agonists cause:

A
    • relaxation of vascular and bronchiole smooth muscle
    • glycogenolysis in skeletal muscle
    • glycogenolysis + gluconeogenesis in the liver
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15
Q

beta-3 agonsits cause:

A
    • lipolysis in adipose

- - relaxation of bladder smooth muscle

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16
Q

What do G-alpha-s GPCRs do?

A

activate adenylyl cyclase

    • ++ cAMP
    • ++ Ca
    • ++ PKA, phosphorylation
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17
Q

What do G-alpha-i GPCRs do?

A

inhibits adenylyl cyclase

    • (–) cAMP
    • (++) K efflux
    • (–) Ca channels
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18
Q

What do G-alpha-q GPCRs do?

A

activates PLC-beta

    • PIP2 –> IP3 + DAG
    • IP3 causes Ca release from ER into cytosol
    • DAG activates PKC
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19
Q

What are the G protein receptor subtypes?

A

alpha-s
alpha-i
alpha-q

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20
Q

What do sympatholytics do?

A

block synthesis of catecholamines

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21
Q

What is the class and MoA of carbidopa?

A

Sympatholytic

    • inhibits DOPA-decarboxylase in the periphery (prevents L-DOPA dose wasting)
    • does not cross BBB (DA does not x either, but L-DOPA does)
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22
Q

What do sympathomimetic drugs do?

A

increase the activity of the SNS

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23
Q

How do indirect-acting sympathomimetics have effect?

A

increase [NT] in cleft

1) reuptake transporter inhibitors
2) block catabolism (MAOIs)
3) increase presynaptic NE and DA release

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24
Q

How does Atomoxetine work?

A

indirect-acting sympathomimetic (reuptake blocker)

    • NET blocker
    • nonstimulant for ADHD
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25
How does Methylphenidate work?
- - indirect-acting sympathomimetic (reuptake blocker) | - - NET, DAT blocker
26
What makes a drug a stimulant?
blocking DAT (increasing DA)
27
How does Phentermine work?
indirect-acting sympathomimetic - - increases NE/DA release - - appetite-modulatory hypothalamic effect
28
When is Phentermine used?
short-term obesity treatment (less than 1 mo.) | -- Topiramate added due to subjective evidence of weight loss in epileptics
29
What are ADRs of Phentermine?
1) HTN 2) tachycardia 3) palpitations 4) H/A 5) insomnia
30
What are C/Is of Phentermine?
1) HTN 2) CVD 3) hyperthyroidism 4) glaucoma 5) MAOIs 6) drug abusers
31
How does amphetamine work?
indirect-acting sympathomimetic - - increases presynaptic DA/NE release - - reverses DAT by acting on VMAT to increase cytoplasmic DA - - D-amphetamine also weak MAOI
32
What is amphetamine used for?
ADHD narcolepsy short-term appetite suppression
33
How does modafinil work?
same as amphetamines... indirect-acting sympathomimetic -- increases presynaptic DA/NE release -- reverses DAT by acting on VMAT to increase cytoplasmic DA -- more selective for DA neurons in HT areas
34
What is modafinil used for?
1) narcolepsy 2) shift-work sleep disorder others... MS, cognition, anti-depressant, ADHD, bipolar, meth/cocaine addiction
35
What are ADRs of modafinil?
dermatological
36
What is the MoA of pseudoephedrine?
sympathomimetic: indirect + direct agonist - - displaces NE + DA from vesicles in CNS and PNS - - direct-acting agonist for alpha/beta adrenergic receptors - - not degraded by MAO/COMT
37
What is the half-life of pseudoephedrine relative to NE?
10x longer
38
What are the effects of pseudoephedrine?
1) relax bronchiole sm 2) vasoconstriction for nasal/pulmonary 3) anorexigenic 4) thermogenesis 5) HR, FOC, TPR
39
What are ADRs of pseudoephedrine?
1) thermogenic effects worse with exercise
40
What are C/I's of pseudoephedrine?
1) CVD/HTN, obesity, MAOIs 2) overuse = HTN crisis, arrhythmias, death 3) hyperthyroidism (increased beta1 receptors...CV thyrotoxicosis)
41
What is the MoA of phenylephrine?
alpha-1 agonist - - mydriatic (dilation) and nasal decongestant - - 1% nasal, 10% ophth solns
42
What are other uses of alpha-1 agonists?
1) idiopathic orthostatic hypotension 2) alpha-1 mediated vasoconstriction for surgery (less anesthetic and blood loss) 3) allergy (decreases mediators like histamine) 4) stress incontinence
43
Describe relative potency of NE and phenylephrine?
Phenylephrine less potent but longer t1/2
44
What is the MoA of doxazosin/terazosin?
alpha-1 antagonist; 1000x more selective for a1 than a2, but non-selective among a1's -- decrease TPR by blocking a1a, a1c on vsm
45
What are uses of doxazosin/terazosin?
BPH HTN CHF pheochromocytoma
46
What is the MoA of Tamsulosin?
alpha-1 antagonist selective for a1a of trigone muscle in bladder
47
What are ADRs specific to tamsulosin?
associated with intra-operative floppy iris syndrome during surgery
48
What are ADRs of alpha-1 antagonists?
1) orthostatic hypotension 2) nocturia 3) stuffy/runny nose
49
What are C/I's of alpha-1 antagonists?
prostatic carcinoma
50
What is the MoA of clonidine?
selective alpha2 agonist | -- reduces sympathetic CNS outflow (major) and local sympathetic outflow (minor)
51
What is clonidine used for?
HTN secondary to increased CNS SNS outflow (withdrawal) | -- ADHD (sleep), migraine prophylaxis, neuropathic pain, smoking cessation, PMS, PTSD
52
What are ADRs of Clonidine?
sedation hypotension bradycardia dry mouth
53
How is clonidine supplied?
oral or TD patch
54
How does albuterol work?
beta2 agonist
55
What is albuterol used for?
acute bronchospasm - - rapid onset, short acting - - over use = status asthmaticus (PD tolerance)
56
What is the MoA for Mirabegron?
b3 agonist
57
What are the uses of Mirabegron?
OAB | -- especially if comorbid dementia when anticholinergics that cross BBB may be C/I
58
What are the ADRs of Mirabegron?
increased HR and BP also very expensive
59
How is Mirabegron metabolized?
CYP3A4 and CYP2D6 | moderate inhibitor of 2D6
60
How do beta antagonists differ?
1) subtype selectivity 2) ISA (partial agonist?) 3) lipid solubility (x BBB) 4) metabolic pathways
61
Describe ADME of propranolol
75% lost to 1st pass 90% bound in plasma t1/2 = 3 hours
62
How does propranolol work?
beta-blocker (b1/cardioselective) - - competitive antagonist - - no ISA or alpha affinity
63
How does carvedilol work?
beta-blocker - - competitive antagonist of a1 and b2 - - moderate ISA of b1
64
What are the c/i's of carvedilol?
asthma
65
Which beta blockers are nonselective?
propranolol | carvedilol
66
Which beta blockers are selective?
metoprolol | nebivolol (bystolic)
67
How does metoprolol work?
selective b1 beta blocker - - no ISA - - big 1st pack - - best for asthma pts
68
What is uptake 1?
presynaptic/primary
69
What is uptake 2?
postsynaptic/astrocytic -- secondary
70
What are Uptake 1 transporters?
- - NET, DAT, SERT (NE transporter, DA transporter, Serotonin transporter) - - MAO
71
What are uptake 2 transporters?
COMT
72
Describe NT affinity for uptake 1 vs uptake 2?
Uptake 1 = NE | Uptake 2 = Epi
73
Where is MAO expressed?
- - presynaptic terminals - - astrocytes - - gut lining
74
Where is COMT expressed?
- - pre- and post-synaptic - - astrocytes - - periphery
75
What NTs are broken down by MAO-A?
NE, Epi, 5-HT | tyramine
76
Where is NE synthesized in the CNS?
locus coeruleus
77
What is tyramine?
a toxic dietary substance if absorbed with MAOI - - found in fermented cheeses, etc. - - broken down by MAO
78
What NTs are broken down by MAO-B?
It's more selective for DA
79
In what disease might MAOB-I's be used?
PD
80
What is one counseling point for MAO-AI's?
dietary restrictions! (tyramine)
81
What are MAO-AI's used for?
depression
82
How do drugs that increase NE/DA presynaptic release work? (mechanisms)
1) alter VMAT fx (reverse direction) 2) displace NE from synaptic vesicles 3) reverse NET/DAT
83
What class of drug is yohimbine?
a2 antagonist
84
What are LABAs used for?
asthma (not acute) in conjunction with an inhaled steroid
85
What drugs has an increase in sudden death been correlated to?
LABAs | only when used for asthma; no issues for COPD
86
What are the uses of beta blockers?
1) HTN, angina, arrhythmias, MI, CHF 2) hyperthyroidism 3) migraine prophylaxis 4) acute panic attack/stage fright
87
What are ADRs of beta antagonists?
1) bradycardia 2) pulmonary airway resistance 3) cold extremities, rash (vasodilation) 4) hypoglycemia 5) weight gain 6) CNS: fatigue, insomnia, depression, nightmares, fever 7) rebound hypersensitivity
88
What are the effects of rebound hypersensitivity from b-blocker?
HTN, angina, MI, fatal arrhythmias

PHS 931 (29 decks)

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