Adrenergic Flashcards
1
Q
Norepinephrine: Class
A
Pharm: direct acting adrenergic agonist
Ther: vasopressor/vasoconstrictor
2
Q
Norepi: PD
A
-stimulates peripheral alpha1 adrenoceptors –> venoconstriction, vasoconstriction, cardiac stimulation.
incr CO, incr SVR, incr MAP.
decr blood flow to skin/muscle/kidney
-stimulates B1 receptors in heart, incr HR and contractility.
3
Q
Norepi: PK
A
F = 100%
IV only
metabolized by COMT and MAO, mainly in liver
matabolites excreted in urine
half life 1-2 min (titrate quickly by IV)
crosses placenta but not BBB
4
Q
Norepi: tox
A
excessive vasoconstriction in mesenteric vessels and peripheral arterioles --> ischemia, infarct, gangrene. reflex bradycardia (in resp to high MAP)
5
Q
Norepi: monitor
A
BP, HR, infusion site, evidence of extravasation
6
Q
Norepi: special issues
A
correct volume depletion before giving
careful with infusion site because of extravasation
continuous monitoring of BP in ICU
caution in peds/gers
7
Q
Norepi v Epi: which has more activity on B receptors?
A
Epi
8
Q
Epi: classes
A
direct acting adrenergic agonist
vasopressor, cardiac stimulant, bronchodilator
adjunct to local anesthetics, anti-anaphylaxis
9
Q
epi: PD
A
alpha1 adrenergic receptors -> veno and vaso constriction
B1 leading to tachy and incr contractility
B2 -> bronchodilation
stabilizes mast cells!
10
Q
Epi: PK
A
IV = immediate IM = variable SC 5-15 min inh 1-5 min opthalmic topical metabolized by COMT and renally excreted
11
Q
Epi: tox
A
excessive vasoconstriction, HTN, hemorrhagic stroke, angina, arrhythmias,
risk of excessive HTN in pts taking propanolol
12
Q
Epi: special issues
A
drug of choice in anaphylaxis
useful/added to local anesthetics because of vasoconstriction: limits blood loss, increases duration of anesthetic.
13
Q
Epi: monitor
A
BP, HR, rhythm, infusion site, extravasation
14
Q
Dopamine: class
A
direct acting non-selective adrenergic and dopaminergic agonist
catecholamine
inotropic agent and vasopressor
15
Q
Dopamine: PD
A
activates Beta1 AR and Alpha1 receptors at different concentrations
Acts on D1 receptors in renal vessels (relax) and incr renal flow
16
Q
Dopamine: PK
A
IV only
acts within minutes
half life = just minutes –> continuous infusion
17
Q
Dopamine: tox
A
ectopy (disturbance of heart rhythm). tachycardia, angina
nausea
18
Q
Dopamine: special issues
A
correct hypovolemia before giving
administer thru large vein and monitor patient
19
Q
Dobutamine: class
A
adrenergic
cardiac stimulant
very sim to Dopamine
20
Q
Dobutamine: PD
A
sim to Dopamine but with less ability to cause vasoconstriction
more specific for Beta1 receptors
21
Q
Isoproterenol: class
A
non-selective B-AR agonist
Rx for bradycardia
22
Q
Isoproterenol: PD
A
vasodilator, incr HR
23
Q
Isoproterenol: tox
A
tachycardia, BP, arrhythmias
24
Q
General receptor action at molecular level: Alpha1
A
Works through PLC/PIP2 –> IP3, incr Ca2+ intracellularly, which incr contractility
25
General receptor action at molec level: Beta1
GPCR, Gs so ATP --> cAMP via increased activity of Adenylyl cyclase --> incr PKA, incr Ca in cell --> incr contractilty
26
Phenylephrine: class
relatively pure Alpha1-AR agonist
27
Phenylephrine: PD
potent constrictor, nasal decongestant, mydriatic (dilates pupil) with no affect on accomodation, BP maint during surgery.
28
Phenylephrine: PK
not inactivated by COMT
causes release of Ca2+ from SR -> incr contractility
give intranasally or topically (eye)
half life = 3h
29
Phenylephrine: tox
HTN, reflex bradycardia
30
Clonidine: class
central alpha-2 agonist
| antihypertensive, adjunct to Rx of opioid withdrawal, prophylaxis of migraine
31
Clonidine: PD
stimulates alpha-2 adrenoceptors in brainstem, thereby leading to down-regulation of sympathetic output
32
Clonidine: PD
Onset 1 h, duration 8 h, F~85%, also available as cutaneous patch
33
Clonidine: tox
withdraw gradually because of risk of rebound HTN; risk of bradycardia in sinus node disease; lethargy, fatigue, depression
34
Clonidine: interactions
additive effects with most other antihypertensives; additive sedation with other CNS drugs
35
Clonidine: special considerations
```
Pregnancy class C; avoid in patients with renal insufficiency
If pt has first or 2nd AV block, do not give. Give an EKG to most patients to make sure no block, no LVH.
```
36
Clonidine: monitor
follow BP and HR, fatigue
37
Ibuprofen: class
NSAID
| Analgesic, anti-pyretic (fever), anti-inflammatory, anti-gout, anti-dysmennorhea
38
Ibuprofen: PD
involves inhibition of prostaglandin synthetics via COX1 and COX2
39
Ibuprofen: PK
F =80%
some excreted unchanged in urine
extensive metabolism in liver
half life 2-4 h
40
Ibuprofen: tox
"allergies" to aspirin
use caution in pts with renal compromise, ulcer disease
causes fluid retention in CHF patients
41
Ibuprofen: special considerations
more side effects in geriatrics
42
Ibuprofen: interactions
with warfarin, aspirin, diuretics, anti-hypertensives
43
Albuterol: Class
pharmacologic class: selective β-2 AR agonist (SABA: short acting beta2 agonist)
Therapeutic class: bronchodilator for asthma/COPD
44
Albuterol: PD
binds to beta-2 receptors and relaxes smooth muscle of airway, causing bronchodilation
45
Albuterol: tox
tachycardia, tremor, tolerance
46
Albuterol: mechanism of delivery
nebulizer or MDI
47
Amphetamine: classes
indirectly-acting adrenergic agonist. sympathomimetic
| CNS stimulant ==> used for appetite suppression, ADHD, and narcolepsy.
48
Amphetamine: PD
```
release of biogenic amines from storage (noradrenaline)
Alpha1 -> vasoconstiction, inc BP
Beta2 -> bronchodilation
Beta1 -> inc HR
CNS stimulant
```
49
Amphetamine: PK
plasma half life approx 12h
| excreted unchanged in urine
50
Amphetamine: tox
restlessness, tremor, irritability, insomnia, dependency, tolerance, inc BP, tachycardia, psychosis if excessive dose
51
Amphetamine: special issues
tolerance, dependance, addiction can develop (unlike ephedrine)
52
Ephedrine: class
Pharmacologic class: Indirect adrenergic, stimulates NE and dopamine release
Therapeutic class: decongestant, anti-hypotension
Also potent CNS stimulants used for ADHD and appetite suppression
53
Ephedrine: PD
↑ NE and dopamine release and direct effects on α and β
54
Ephedrine: PK
Prolonged duration of action
55
Ephedrine: tox
HTN, tachyphylaxis
| insomnia
56
Ephedrine: special
ephedrine-containing herbal products have been banned in the US, Pseudoephedrine is a restricted OTC substance because it can be used to make meth
57
Pseudophedrine: class
Pharmacologic class: Indirect adrenergic, stimulates NE and dopamine release
Therapeutic class: decongestant only (not antihypotension as is Ephedrine)
Also potent CNS stimulants used for ADHD and appetite suppression
58
Pseudophedrine: PD
↑ NE and dopamine release and direct effects on α and β
59
Pseudophedrine: PK
Prolonged duration of action
60
Pseudophedrine: tox
HTN, tachyphylaxis
| insomnia
61
Pseudophedrine: special
ephedrine-containing herbal products have been banned in the US, Pseudoephedrine is a restricted OTC substance because it can be used to make meth
62
Tyramine: class
Pharmacologic class: indirectly-acting adrenergic agonist, stimulates NE and dopamine release
Therapeutic class: None.
63
Tyramine: PD
↑ Release of biogenic amines from storage, including dopamine in the CNS
64
Tyramine: PK
Byproduct of tyrosine metabolism ==> metabolized by liver MAO
65
Tyramine: tox
Can cause MAOI hypertensive crisis
66
Tyramine: special issues
use of MAO inhibitors and severe HTN, and tachypylaxis
67
Tyramine: interactions
caution with MAO inhibitors ==> can cause HTNsive crisis
68
Cocaine: class
Pharmacologic class: indirect-acting agonist via blocking Uptake 1 pathway leading to inc NA effects (vasoconstriction)
Therapeutic class: CNS stimulant, musical inspiration, song title by Eric Clapton
Local anesthetic, vasoconstrictor, drug of abuse
69
Cocaine: PD
blocks NE and dopamine reuptake via Uptake 1 pathway
| Shorter lasting than amphetamine, more intense
70
Cocaine: PK
Smoked, snorted or injected for rapid effect
71
Cocaine: tox
Hypertension, AMI, arrhythmias, seizures. if snorted can lead to nasal septal necrosis due to vasoconstriction
72
Phentolamine: class
```
alpha blocker (reversible)
Hypertensive crisis
```
73
Phentolamine: PD
blocks both Alpha1 and Alpha2.
Alpha1: block smooth muscle contraction -> vasodilation and postural hypotension
Alpha2: block leads to tachycardia and inc CO
74
Phentolamine: adverse effects
postural hypotension, tachycardia
75
Phenoxybenzamine: PD
blocks both Alpha1 and Alpha2.
Alpha1: block smooth muscle contraction -> vasodilation and postural hypotension
Alpha2: block leads to tachycardia and inc CO
76
Phenoxybenzamine: class
```
alpha blocker (IRreversible)
Hypertensive crisis
```
77
Phenoxybenzamine: adverse effects
postural hypotension, tachycardia
78
Prazosin: class
a1 blocker
79
Prazosin: indications
antihypertensive, treatment of BPH, treatment of Raynaud’s syndrome, treatment for kidney stones
80
Prazosin: PD
blocks alpha-1 receptors on arterioles and veins, thereby inhibiting NE-mediated vasoconstriction and venoconstriction
81
Prazosin: PK
available po or transdermal; variable oral bioavailability (~60%), onset 2 h, duration 12-24 h
82
Prazosin: tox
excessive hypotension with passing out, especially orthostatic, especially in patients on diuretics
83
Prazosin: excr
extensively metabolized in liver
84
Prazosin: interactions
additive effects with most other antihypertensives, especially diuretics
85
Prazosin: special
start gradually, and at bedtime, to avoid first-time passing out; male patients with BPH?
86
Prazosin: monitor
BP, weight, edema
87
Propanolol: class
b blocker (1 and 2)
88
Propanolol: indication
Antihypertensive, antianginal, antiarrhythmic, MI
89
Propanolol: PD
binds directly to beta-receptors, with a preference for beta-1 over beta-2, leading to lower blood pressure via several potential mechanisms (less cardiac output, less activation of the RAA system); recent evidence suggests less effective in preventing strokes than other drugs
90
Prolanolol: PK
available po or iv; variable oral F; onset 1-2 hours h, duration 12-24 h; can be given once per day; renally excreted (longer half-life)
91
Propanolol: tox
excessive hypotension; bradycardia; heart block can worsen severe CHF (but indicated for mild to moderate CHF); worsen bronchospasm in severe asthmatics (bc not perfectly B1 selective, will block 10% of B2s)
92
Propanolol: interactions
additive effects with most other antihypertensives, additive AV block with CEB’s
93
Propanolol: special
may be especially useful in HTN patients with exertional angina, MI, atrial fibrillation; watch out for abrupt withdrawal; may no longer be “first line” drug unless other indications exist (recent data)
94
Propanolol: monitor
BP, HR, exercise tolerance
95
Timolol: class
same class as propanolol, non-specific b blocker
96
Timolol: indication
Open angle glaucoma, antihypertensive, MI prevention
97
Pindolol: class
same as propanolol. nonspecific b blocker & partial agonist
98
Pindolol: indication
Antihypertensive, antianginal, antiarrhythmic
99
Pindolol: PD
some degree of beta-1 activation is maintained while the cardiac response to increased sympathetic activity is blunted
100
Sotalol: class
K channel blocker & b blocker
101
Sotalol: indication
Antiarrhythmic Class III, antihypertensive
102
Sotalol: PD
prolongs cardiac action potential; blocks K+ channels
103
Metoprolol: class
b1 blocker (specific)
104
Metoprolol: indication
Antihypertensive, antianginal, antiarrhythmic, CHF
105
Metoprolol: PD
binds directly to beta-receptors, with a preference for beta-1 over beta-2, leading to lower blood pressure via several potential mechanisms (less cardiac output, less activation of the RAA system); recent evidence suggests less effective in preventing strokes than other drugs
106
Metoprolol: PK
available po or iv; variable oral F; onset 1-2 hours h, duration 12-24 h; can be given once per day; renally excreted (longer half-life)
107
Metoprolol: tox
excessive hypotension; bradycardia; heart block can worsen severe CHF (but indicated for mild to moderate CHF); worsen bronchospasm in severe asthmatics (bc not perfectly B1 selective, will block 10% of B2s)
108
Metoprolol: interactions
additive effects with most other antihypertensives, additive AV block with CEB’s
109
Metoprolol: special
may be especially useful in HTN patients with exertional angina, MI, atrial fibrillation; watch out for abrupt withdrawal; may no longer be “first line” drug unless other indications exist (recent data)
110
Metoprolol: monitor
BP, HR, exercise tolerance
111
Atenolol: class
b1 blocker
112
Atenolol: indication
Antihypertensive, antianginal, antiarrhythmic, anti-MI
113
Atenolol: PD
binds directly to beta-receptors, with a preference for beta-1 over beta-2, leading to lower blood pressure via several potential mechanisms (less cardiac output, less activation of the RAA system); recent evidence suggests less effective in preventing strokes than other drugs
114
Atenolol: PK
available po or iv; variable oral F; onset 1-2 hours h, duration 12-24 h; can be given once per day; renally excreted (longer half-life)
115
Atenolol: tox
excessive hypotension; bradycardia; heart block can worsen severe CHF (but indicated for mild to moderate CHF); worsen bronchospasm in severe asthmatics (bc not perfectly B1 selective, will block 10% of B2s)
116
Atenolol: interactions
additive effects with most other antihypertensives, additive AV block with CEB’s
117
Atenolol: special
may be especially useful in HTN patients with exertional angina, MI, atrial fibrillation; watch out for abrupt withdrawal; may no longer be “first line” drug unless other indications exist (recent data)
118
Atenolol: monitor
BP, HR, exercise tolerance
119
Labetalol: class
a1 and b blocker
120
Labetaolol: indication
antihypertensive, treatment of CHF, pheochromocytoma
121
Labetalol: PD
reduces BP by blocking access of NE to beta-receptors and alpha-1 receptors, thereby lowering BP by several different mechanisms; patients differ in degree of beta-blockade vs alpha-blockade
122
Labetalol: PK
excellent absorption but high first-pass effect, leading to F~25%; onset 1-2 hours after po, 2-5 minutes when given iv; extensively metabolized in liver by IID6
123
Labetalol: tox
avoid in patient with bradycardia, heartblock, CHF, asthma, shock; use with caution in patients with cardiomyopathy, pheochromocytoma: Pregnancy Class D
124
Labetalol: interactions
additive effects with most other antihypertensives
125
Labetalol: special
use reduced doses in patients with impaired liver function; dizziness is most troubling early side effect; most often used for hypertensive crises (as with nitroprusside)
126
Labetalol: monitor
BP, HR
127
Carvedilol: class
a1 and b blocker, antioxidant
128
Carvedilol: indication
CHF
129
Carvedilol: PD
reduces BP by blocking access of NE to beta-receptors and alpha-1 receptors, thereby lowering BP by several different mechanisms; patients differ in degree of beta-blockade vs alpha-blockade
130
Carvedilol: PK
excellent absorption but high first-pass effect, leading to F~25%; onset 1-2 hours after po, 2-5 minutes when given iv; extensively metabolized in liver by IID6
131
Carvedilol: tox
avoid in patient with bradycardia, heartblock, CHF, asthma, shock; use with caution in patients with cardiomyopathy, pheochromocytoma: Pregnancy Class D
132
Carvedilol: interactions
additive effects with most other antihypertensives
133
Carvedilol: special
use reduced doses in patients with impaired liver function; dizziness is most troubling early side effect; most often used for hypertensive crises (as with nitroprusside)
134
Carvedilol: monitor
BP, HR
