Exam2Lec2AdrenergicPharmacology Flashcards
(86 cards)
1
Q
Which class of receptors are adrenergic receptors?
A
G protein-coupled (GPCR)
2
Q
Which catecholamines do adrenergic receptors target?
A
1) Norepinephrine
2) Epinephrine
3
Q
Does adrenergic receptors stimulate the PNS or SNS?
A
Sympathetic NS
4
Q
How does an α1 receptor affect most vascular smooth muscle?
A
Contraction
by vasoconstriction
5
Q
What is the G protein for an α1 receptor?
A
Gq
6
Q
How does an α2 receptor affect the postsynaptic CNS?
A
Decreases SNS tone
7
Q
How does an α2 receptor affect the presynaptic ANS?
A
Decreases NT release
8
Q
What is the G protein for an α2 receptor?
A
Gi
9
Q
What are the G proteins for a β1 receptor?
A
Gs, Gi
10
Q
How does a β1 receptor affect the heart?
A
Increases force and rate
11
Q
How does a β1 receptor affect the juxtaglomerular cells?
A
Increases renin release = retains fluid
12
Q
What are the G proteins for a β2 receptor?
A
Gs, Gi
13
Q
How does a β2 receptor affect skeletal muscle blood vessels?
A
Relaxation
by vasodilation
14
Q
How does a β2 receptor affect the bronchial smooth muscle?
A
Relaxation
by bronchodilation
15
Q
How does a β2 receptor affect the liver?
A
Glycogenolysis and gluconeogenesis = increases blood glucose
16
Q
Which drug is an α1 agonist?
A
Phenylephrine = vasoconstriction
17
Q
Which drugs are α2 agonists?
A
Clonidine and Methyldopa = decrease SNS tone
18
Q
Which drugs are non-selective β agonist (β1 + β2)?
A
Isoproterenol and Dobutamine
“I would DIe to be Beta
B1: incr HR
B2: smooth m dilation
19
Q
Which drug is a β2 agonist?
A
Albuterol = dilates bronchial smooth muscle
good for asthma
20
Q
Which drug is a non-selective α antagonist (blocks α1 and α2)?
A
Phentolamine = vasodilation & increases HR
21
Q
Which drug is an α1 antagonist?
A
Prazosin
effect: vasodilate muscle instead of constrict
22
Q
Which drugs are non-selective β antagonists (β blockers)?
A
PropranOLOL
PROPs being a B antag
B1: decr HR
B2: bronchoconstriction
23
Q
Which drugs are β1 antagonists (β blockers)?
A
AtenoOLOL and MetoprOLOL = decrease HR
Oh Lol At Me then
24
Q
Which drugs are mixed α1/β antagonists?
A
CarvediLOL and LabetaLOL
LOL=funny bc it is both
CARVed a LABel to MIX up an antagonist
25
What is the oral usability of epinephrine?
completely ineffective
26
Is the duration of action of epinephrine long or short?
short
## Footnote
b/c naturally made in body
27
Does epinephrine have good or poor penetration of the CNS?
poor
28
Why is phenylephrine better than epinephrine?
More stable and is not broken down as fast
29
If given phenylephrine, is it okay to give an MAO inhibitor?
No bc you will now have a buildup of epi causing effect and phenylephrine (A1 agonists) causing effects .
## Footnote
mao breaks down epi
30
What is the primary effect of α1 agonist?
vasoconstriction of most vascular smooth muscle
## Footnote
By stim α1
31
What are the clinical uses of α1 selective agonists and mention how they are useful for each one.
● **Nasal congestion** = decreases inflammation markers
● **Hypotension** = vasoconstriction = increases BP
● **Hemorrhoids** = vasoconstriction = stops inflammation of markers to swollen/inflamed veins
● **Dilates pupils**
## Footnote
phenylephrine
32
What are the adverse effects of phenylephrine?
● Angina
● Anxiety
● Bradycardia
● HTN
● Tissue necrosis
"BHAAT" like epi but w/o the C so instead of CHAAT, its BHAAT
33
What are the contraindications of phenylephrine?
● Vfib
● Tachycardia
● HTN
34
What are the interactions of phenylephrine?
MAO inhibitors = breaks down NE
35
Phenylephrine Overview
A. Class
B. Effect
C. TX
D. SE
E. Contraindication
F. Interactions
A. class: alpha 1 agonist
B. effect: vasoconstriction
C. tx: nasal congestion, hypotension,hemorroids, dilate eye
D. se: angina, bradycardia, HTN, necrosis
E. contraindication: Vfib, tachy, HTN
F. interactions: MAOI
## Footnote
"BHAAT" for SE
dont want to give to someone with heart probs bc raises BP
36
What are the α2 selective agonist drugs?
Clonidine and Methyldopa
## Footnote
decr SNS, think PNS effects
37
Stimulation of the α2 receptors in the medulla has what type of effects?
Sympatholytic
● No reflex tachycardia
38
What are the net effects of α2 agonists?
● Decreased BP
● Decreased HR
● Decreased cardiac output
## Footnote
still an agonists, it just activates Gi thats inhibitory
39
**What is the first line of therapy for HTN during pregnancy?**
Methyldopa
## Footnote
this is a prodrug that needs to be activated so its safer
40
Why is clonidine used more often than methyldopa?
More potent
41
Why is clonidine not used for pregnancy?
Catagory C for pregnancy = risk cannot be ruled out
## Footnote
for cat C we are determing benefits vs risk
42
Why is methyldopa the first line therapy for HTN during pregnancy?
Pro drug = only effective in the brain = safer
43
Clonidine can also treat several CNS disorders such as?
* ADHD
* Mitigate drug withdrawal
* Severe pain
44
Clonidine is effective in both the ____ and the ____.
periphery, brain
## Footnote
effect everywhere with dose
45
What drug class is Clonidine and Methyldopa?
α2 agonist
46
What are the adverse effects of clonidine?
* Dry mouth
* Sedation
* Depression
* Orthostatic hypotension
47
What is the effect of Clonidine?
Decreases SNS tone
48
What are the contraindications for Clonidine?
* Depression
* Caution: Sudden withdrawal causes hypertensive crisis
49
What are the adverse effects of Methyldopa?
* Sedation
* Depression
* Tolerance
50
What are the contraindications for Methyldopa?
* Depression
* MAO inhibitory therapy = increases NE
51
Clondine/Methyldopa Overview
A. Class
B. Effect
C. TX
D. SE
E. Contraindication
F. Notes
A.α2 agonist
B. decr BP, HR, CO (sns tone)
C. HTN
D. Hypotension, depression, sedation
E. DEPRESSSION, MAO inhib, sudden withdrawl
F. Note: methyldopa is FIRST LINE for therapy . Clonidine is more potent
Clonidine=periphery, Methyldopa=prodrug
52
What drug class is Isoproterenol?
Non-selective β agonist = agonist at both β1and β2 receptors
## Footnote
potent vasodilater (B2)
bronchodilator (B2)
positive inotropic and chronotropic agent (B1)
53
What are the clinical uses for Isoproterenol?
* Cardiac arrest
* AV block
* Bradycardia
* Torsade de pointes
54
What are the adverse effects of Isoproterenol?
Arrythmias (common)
55
True or false, Isoprotenerol is NOT a first line agent for use in bronchospasm during anesthesia or shock (cardiogenic, hypovolemic, or septic)
TRUE
## Footnote
CARDIOGENIC-DOPA
SEPTIC -NOREPI
56
Isoproterenol Overview
A. Type
B. Effect
C. Use
D. SE
A. β agonist (non-selective)
B. vasodilation, bronchodilator, incr HR
C. torsade pointes
D. arrythimas
57
What drug does this graph represent?
isoproterenol
58
Dobutamine Overview
A. Type
B. Effect
A. β agonist (non selective)
B. incr HR (inotropic (force) more than chronotropic (rate)), no net change in resistance
## Footnote
racemix mixture
greater force/contractility than HR
59
Albuterol Overview
A. Type
B. Effect
C. Use
D. SE
E. Contraindications
A. β2 agonist (selective)
B. vasodilation of smooth and skel muscle
C. Asthma/bronchospasms, premature labor
D. tremors, tachy (direct and reflec), CNS stimulation
E. Hyperglycemia
## Footnote
short-action-acute bronchospasm
stimulates glucogenolysos dont give to DM
60
Can you give albuterol to a diabetic pt (hyperglycemic)?
NO
61
What is the non-selective α ANTAGONIST drug?
Phentolamine
## Footnote
causes vasodilation, incr SNS, incr NT
62
What is the α1 selective ANTAGONIST drug?
Prazosin
## Footnote
causes vasodilation
63
Phentolamine Overview
A.Type
B. Effect
C. Use
D. SE
A. Type: A Antagonist
B. Effect: Vasodilation
C. Use: Anesthesia Reversal
D. SE: Reflux Tachy, tolerance
## Footnote
vasodilation triggers incr HR (reflex tachy)
64
With phentolamine, heart rate increase is more pronounced when what occurs?
With mixed A1 and A2 antag b/c of diminished A2 feedback in heart (remember A2 in presynaptic terminal)
## Footnote
A2 antag incr SNS, NE that binds to B receptors (incr HR)
65
HR incr greater in phetolamine or prazosin?
Phentolamine
66
A1 antag causes what 3 things?
Vasodilation
Decr BP
Incr HR
67
Prazosin Overview
A. Type
B. Effect
C. Use
D. SE
E. Contraindication
A. Type: A1 Antagonist
B. Effect: Vasodilation
C. Use: BPH
D. SE: Reflux Tach
E. Contraindication: Angina, MI, BB withdrawals
## Footnote
BPH=benign prostatic hyperplasia
68
Is Prazosin use as a first line for Hypertension?
NO
69
What cardiovascular effects do you see with non selective Beta blockers (propranolol)?
Negagtive inotropic, dromotropic (conduction speed) and chronotropic effect
decr rening release
block of B2 may incr perip resistance
## Footnote
opposite of SNS, so think parasymp
70
What are some CNS and eye effects of B antagonists (non selective)
CNS: anxiolytic, maybe decr HTN
eye: decr aq humor production and eye pressure
71
What is more prominent in B1/B2 antagonists than in B1 selective antags?
Bronchoconstriction"spasm" in the lungs and inhibited lipolysis and glucogenolysis
## Footnote
not good for hyperglycemic (DM)
72
Propranolol Overview
A. Type
B. Effect
C. Use
D. SE
E. Contraindication
F. Withdrawal
Propranolol
A. Type: B Antagonist (non selective)
B. Effect: Negative inotropic and chronotropic
C. Use: HTN post MI/other cardiac uses
D. SE: Hyperglycemia, bronchoconstriction
E. Contraindication: Asthma, DM, Hyperthyroidism, preg
F. Withdrawal: Rebound HTN
## Footnote
stop taking beta blockers, incr in NE, B receptors are sensitive, Hypertension sky rockets
73
What can be used as 1st line use for hypertension and over 60?
Thiazide, ACEI, ARB, CCB
## Footnote
NOT BETA BLOCKER (not indicated as 1st line therapy for age 60 and above)
74
When are Beta blockers first line therapy for hypertension?
* Ischemic heart disease
* Recent STEMI or non-STEMI (ST-elevation myocardial infarction)
* Left ventricular systolic dysfunction
* some arrythmias
## Footnote
if there is a history of these, THEN you use Beta blockers as 1st line use
75
Since Beta 1 antags have no B2 activity, they are preferred in patients with what conditions?
Bronchospasm
Diabetes
Peripheral vascular disease
76
If you have a history of DM and astham, which antagonist can you give?
B1
77
Which b1 antag drug is used for heart failure where 1 of 3 recommend, long -acting form: succinate for success?
Metoprolol
78
Are B1 antags safe with pregnancy?
NO
79
Beta 1 antags have less effects on what?
Glucose levels
80
Atenolol and Metoprolol
A. Type
B. Effect
C. Use
D. Withdrawal
E. Notes
A. Type: B1 Antagonist
B. Effect: Negative inotropic and chronotropic
C. Use: HTN post MI/other cardiac uses
D. Withdrawal: Rebound HTN
E. Notes: Not B2 so can use for DM and Asthma. Metoprolol has a longer half-life.
81
Which mixed a1/b antag is used for heart failure where 1 of 3 recommend?
Carvedilol
82
Which mixed a1/b antag can be used ffor HTN emergency in pregnancy?
Labetalol
## Footnote
#1 is still methyl dopa
83
Do mixed A1/B antags have more or less reflec tachycardia than A1 antags?
LESS b/c of B2
84
Do mixed A1/B antags have more or less peripheral vasoconstriction than with Beta blockers?
LESS b/c of A1
85
Carvedilol and Labetalol Overview
A. Type
B. Effect
C. Use
D. Withdrawal
E. Notes
A. Type: A1/B Antagonist
B. Effect: Negative inotropic and chronotropic, Vasodilation
C. Use: HTN post MI/other cardiac uses
D. Withdrawal: Rebound HTN
E. Notes: LESS REFLEX TACHY
86
In a paitient with which of the following conditions would propranolol be contraindicated?
A.Tachy
B.Hypertension
C.Constipation
D.Asthma
E.Migraines
Asthma
## Footnote
propranolol=non selective B antag
B2 antag effect=bronchoconstriction
