1
Q
M1
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
A
- cholinergic
- nerve endings
- Gq
- increased IP2 and DAG
- activate myenteric plexus
2
Q
M2 cholinergic/adrenergic - location -mechanism -2nd messenger -Action
A
-cholinergic
-heart, some nerve endings
-Gi
-decreases cAMP, activates K+ channels
Slows SA node
3
Q
M3
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
A
- cholinergic
- smooth muscle, glands, endothelium
- Gq
- increased IP3, DAG cascade
- contract detrusor, increase salivation
4
Q
Nn
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
A
- cholinergic
- ANS ganglia
- Na-K ion channel
- Na
- Depolarizes postgang fiber, evokes AP
5
Q
Nm
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
A
- cholinergic
- neuromuscular plate
- Na-K ion channel
- Na
- depolarizes muscle cell and evokes AP and contraction
6
Q
A1
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
A
- adrenergic
- smooth muscle (especially vasculature) , glands
- Gq
- increase IPR, DAG
- increase Ca and causes contraction of vascular SM and/or secretion from glands
7
Q
A2
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
A
- adrenergic
- nerve endings and some smooth muscle
- Gi
- decrease cAMP
- decrease transmitter release in the nerve and decrease contraction in smooth muscle
8
Q
B1
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
A
- adrenergic
- cardiac muscle and JGA
- Gs
- increase cAmP
- increase HR and contractility and renin release
9
Q
B2
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
A
- adrenergic
- smooth muscle, liver,heart
- Gs
- increase cAMP
- relax bronchiolar smooth muscle; increase glycogenolysis; increase HR and contractility
10
Q
B3
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
A
- adrenergic
- adipose cells
- Gs
- Increase cAMP
- increase lipolysis
11
Q
Dopamine
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
A
- adrenergic
- smooth mucle
- Gs
- increased cAMP
- relax vasculature in renal arterioles
12
Q
Phenylephrine Description
A
synthetic alpha receptor agonist that is most selective for a1
13
Q
Phenylephrine Action
A
vaso and venoconstriction by stimulating contraction of vascular smooth muscle
14
Q
Phenylephrine Indications (3)
A
Nasal decongestant
Mydriatic (pupil dilator)
increased BP in vasodilator state
15
Q
Other facts about phenylephrine (3) -potency compared to Norepi -deactivation -routes
A
less potent than norepi
not deactivated by COMT
can be given topically and IV
16
Q
Clonidine short card info
Description
A
-selective A2 agonist
17
Q
Clonidine short card Action
A
stimulate a2 in brianstem, causes down regulation of sympathetic nervous system
18
Q
Clonidine indications (short card) (2)
A
treat hypertension
treat migraine
19
Q
Clonidine other facts
- route
- side effects
- overdose effect
A
- orally or patch
- sedation/ dry mouth
- if given IV or OD can cause high BP
20
Q
Phenylephrine brand name
A
Neosynephrine
21
Q
Clonidine brand name
A
Catapres
22
Q
Isoproterenol brand name
A
Isuprel
23
Q
Isoproterenol description
A
B1/B2 receptor agonist
24
Q
isoproterenol actions
A
potent b1/b1 agonist
25
isoproterenol indications
| 3
increase cardiac contractility
increase HR
increase cardiac conduction
26
isoproterenol other facts
- route
- why isn't it used so much
- what else does it cause
- iv
- no longer used in CCu b/c can cause tachyarrhythmias like V-tach
- also causes vasodilation
27
Dobutamine trade name
Dobutrex
28
Dobutamine description
synthetic B1 receptor agonist
29
dobutamine action
potent b1 agonist in heart (increases contractility more than HR) and blood vessels (dilates renal and mesenteric vessels)
30
```
dobutamine indications
(2)
```
- increase cardiac contractility more than HR
| - Use for in CCU for patients in cardiogenic shock where you do not want tachycardia (i.e. most MI)
31
dobuatmine other facts
- route
- side effects (3)
-IV
| tachy, hypertension, ectopy
32
albuterol trade name
ventolin
33
albuterol description
synthetic b2 selective receptor agonist
34
albuterol actions
b2 agonist: receptors on smooth muscle cells in airways and uterus and relaxes above tissues
35
albuterol indications (2)
prompt acting rescue inhaler for asthma, COPD
| and inhibits premature labor
36
albuterol other facts
- most often given as..
- other route
- what's the deal w/ IV
- side effects (3)
- metered dose inhaler
- nebulizer
- rarely given as iv infusion
- anxiety, tachy, tremor
37
Mirabegron trade name
Myrbetriq
38
Mirabegron Description
selective B3 agonist
39
Mirabgeron action
stimulates b3 receptors in smooth muscle of bladder, reduces detrusor muscle tone
40
Mirabegron indications
- treatment of patients w/ overactive bladder with features of urinary urgency/frequency
- inreases bladder capacity
- does not produce bothersome anticholinergic symptoms like tolteridine
41
other facts about mirabegron
| 2
approved in June 2012
| administered orally as extended release tablets
42
Methoxamine description
alpha 1 and 2 agonist
43
Epinephrine tradename/ and one other name
EpiPen
| Adrenaline
44
Epinephrine Drug class
- pharmacologic
- therapeutic
- pharm: direct acting adrenergic agonist
| - Therapeutic: vasopressor, cardiac stimulant, bronchodilator, adjunct to local anesthetics, treatment for anaphylaxis
45
Epinephrine Pharmacodynamics
major action is to stimulate a1 adrenoreceptors to cause vasoconstriction and venoconstriction; stimulate b1 receptors for tachycardia and increased contractility ; b2 for bronchodilation--these actions are helpful in severe allergic runs by stabilizing mast cells (b1/b2)
46
Epi Pharmacokinetics
- route(4)
- metabolism
can be given IV (immediate), IM variable , SC (5-15 min), via inhalation (1-5 min onset) , opthalmic topical
- metabolized by COMT and then renally excreted
47
Epi Toxicity (5)
```
excessive vasoconstriction
HTN
hemorrhagic stroke
angina
arrhythmias
```
48
Epi Interactions
risk of excessive hypertension in patents taking propranolol
49
Epi special considerations (2)
utility w/ local anesthetics
| drug of choice in severe anaphylactic runs (along w/ others)
50
Epi indications and dose/route
| 3
for anaphylaxis: 0.1-0.5 mg SC or IM
for cardiac arrest: 1-5 mg IV push
for infusion 1-4 mcg/min
51
Epi : things to monitor (5)
```
BP
HR
rhythm
infusion site
evidence of extravasation
```
52
Norepinephrine trade name/ one other name
Levophed
| noradrenaline
53
norepi drug class
- pharm
- therapeutic
pharm- direct acting adrenergic agonist
| therapeutic- vasopressor, vasoconstrictor
54
Norepi pharmacodynamic
major action is to stimulate a1 adrenorecpetors to increase vasoconstriction and venoconstriction. This increases CO, SVR, and MAP, but decrease blood flow to vulnerable tissues like skin, muscle, and kidney
also stimulates b1 in heart, increasing HR and contractility. Main effects are vasoconstriction and cardiac stimulation
55
Norepi Toxicity
| 2
excessive vasoconstriction in mesenteric vessels, peripheral arterioles causing ischemia, infraction, gangrene, reflex brady
56
Norepi interactions
use cautiously in peeps takin MAO inhibitors like phenlzine;
risk of excessive hypertension in peeps taking propranolol
57
Norepi special considerations
| 3
correct volume depletion before giving NE
select infusion site carefully-extravasation is a major problem; monitor patent and BP continuously in ICu; use cautiously in ped and geriatric patients
58
Norepi Indications and dose/route
for adults with acute hypotension and shock related to low SVR
infuse 2-12 mcg/min
59
norepi things to monitor (4)
BP
HR
infusion site
extravasation
60
Dopamine trade name
intropin
61
dopamine descrption
agonist at DA, B1, and a1 receptors
62
dopamine actions
relative potency depends on dose being delivered; DA agonist at low dose, B1 agonist at medium dose; a1 agonist at high dose
63
Dopamine indications (2)
shock of various etiologies in ICu
can produce increased contractility (B1)
vasoconstriction (a1) and improve mesenteric and renal perfusion (DA)
64
Dopamine Other facts
| -route
given IV , preferably for a short period of time
65
Norepi pharmacokinetics
```
F~ 100%
Given IV only
metabolized by comt and mao in liver
metabolites excreted in urine
half life is 1-2 minutes
can cross placenta, but not BBB
```
66
Ephedrine description
Alkaloid obtained from plants
67
Ephedrine action
acts inertly to release NE from adrenergic nerve endings, also some direct agonism at receptors
68
Ephedrine Indications (2)
Mild to moderate hypotension during surgery (very fast acting)
Nasal decongestion
69
other facts about ephedrine
- duration of action
- potent stimulant of what
- side effects (2)
- FDA status
- somewhat prolonged action
- potent CNS stimulant
- side effects = hypertension and insomnia
- OtC banned by FDA
70
Pseudoephedrine description
synthetic derivative of ephedrine
71
actions of pseudoephedrine
acts indirectly to release NE from adrenergic nerve endings, and some direct agonism at alpha and beta adrenergic receptors
72
pseudoephedrine indications
- nasal and sinus decongestant
| - less ability to dilate bronchioles than ephedrine
73
other fact about pseudo ephedrine
- when approved
- what year were bulk sales reported
- what year increased security
- what year labeled as risk of injury/death or no cold products for kids
- 1959
- 1996
- 2005
- 2008
74
Amphetamine description
synthetic compound similar to ephedrine
75
amphetamine actions
acts indirectly to release NE from adrenergic nerve endings
76
amphetamine indications
- none are FDA approved
- obesity
- narcolepsy
- ADHD
77
amphetamine other facts
- approval
- risk of dependence
- side effects
- 1939
- high risk of dependence
- insomnia, restlessness, tremor
78
Tyramine description
naturally occurring byproduct of tyrosine metabolism; present in fermented food
79
tyramine actions
indirectly releases NE from adrenergic nerve endigns
80
tyramine indications
none are FDA approved
- obesity
- narcolepsy
- ADHD
81
tyramine other facts
- metabolized by what enzyme
- what kind of patients should be watched out for
- what is a common interations
- MAO
- patients on MAOIs
- food/drug
- MAOI+ food= hypertensive crisis
82
Cocaine description
purifed alkaloid extract from coca plant
83
cocaine actions
indirectly blocks reuptake of NE, Epi, and DA, and can stimulate release of Ne, Epi, and DA
can also sat as local anesthetic and CNS stimulant
84
indications (2)
- nose bleeds (anesthesia plus vasoconstriction)
| - anesthesia for corneal surgery
85
other facts about cocaine
- effects compared to amphetamine
- routes
- side effects (5)
more intense, longer lasting
smoked, snorted, injected
HTN, tachy, arrhythmias, seizures, MI
86
Prazosin Trade name
Minipress
87
Prazosin Drug class
- pharmacologic
- therapeutic
- selective alpha 1 adrenoreceptor blocker
| - antihypertensive, treatment of BPH
88
Prazosin pharmacodynamics
blocks alpha 1 receptors on arterioles and veins, thereby inhibiting NE-mediated faso and venoconstriction
89
Prazosin pharmacokinetics
- route
- bioavailability
- onset
- duration
- where is it metabolized
available po or transdermal
| variable oral bioavailability (~60%) , onset 2h, duration 12-24h; extensively metabolized in liver
90
Prazosin Toxicity
excessive hypotension with syncope, especially orthostatic, especially in patients on diuretics
91
Prazosin Interactions
additive effects w/ most other antihypertensives, especially diuretics
92
Prazosin special considerations
| 2
start gradually, and at bedtime, to avoid first time passing out; male patients w/ BPH?
93
Prazosin indications and dose/route
as mono therapy begin with 1 mg tid, advance to 20mg per day divided tie
94
Prazosin monitor
BP, weight, edema
95
Tamsulosin tradename
Flomax
96
Tamsulosin cost
5-70 $ per month
97
Tamsulosin drug class
- phram
- therapeutic
selective a1blocker
| treatment of obstructive symptoms of BPH
98
Tamsulosin pharmacodynamics
selectively blocks a1 receptors, but preferentially in the prostate, leading to relaxation of smooth muscles in the bladder neck and prostate, improving urine flow, and reducing obstructive symptoms of BPH venoconstricton
99
Tamsulosin Pharmacokinetics
- how much is absorbed
- what % metabolized by CYP 450 enzymes
- half life
- duration of action
completely absorbed after oral ingestion; >90% metabolized by CYP 450 enzymes
half life about 6 hrs, but duration of action up to 15 hours due to slow absorption
100
Tamsulosin Toxicity (3)
excessive hypotension with syncope, especially orthostatic, especially in patients on diuretics,allergic rxns, decreased libido
101
Tamsulosin Interactions
additive effects w/ most antihypertensives, especially diuretics
102
Tamsulosin special considerations (3)
- rule out carcinoma of prostate before beginning treatment
- do not crush or chew tablets, as that wills speed up absorption;
- can ask be used to treat spasm of ureter in patients with kidney stones
103
Tamsulosin Indications and dose/route
for symptoms of BPH, 0.4 mg po qd or bid; similar doses for renal colic
104
Tamsulosin monitor
BP
105
Prazosin cost
4-20 $ per month
106
Phentolamine trade name
Regitine
107
Phentolsamine Drug class
- pharm
- therapeutic
- non-selective competitive alpha adrenergic receptor blocker
- antihypertensive drug for patents w/ pheochromocytoma
108
phentolamine pharmacodynamics
blocks a1/a2 adrenergic receptors and presynaptic and post synaptic alpha receptors , decreasing preload and after load
109
```
phentolamine/regitine
pharmacokinetics
- route
-F
- plasma half-life
```
only comes in IV formulations, so F=100%; plasma half-life about 20 min after IV dose
110
phentolamine/regitine toxicity (3)
- excessive hypotension w/ syncope especially orthostatic, especially in patients on diuretics;
- allergic rxns;
- decrease libido
111
phentolamine interactions
additive effects w/ most other antihypertensives, especially diuretics
112
phentolamine special considerations
| 3
- rule out carcinoma of prostate before beginning treatment
- do not crush or chew tablets, as that wills speed up absorption;
- can ask be used to treat spasm of ureter in patients with kidney stones
113
phentolamine indications and dose/route
| -indications (4
- Aid Dx of pheo
- treatment of intraop HTN during pheo removal surgery
- prevention of dermal slugging after extravasation of NE infusion
- hypertensive crisis from sympathomimetic amines
- Dose 5 mg IV, then titrate
114
phentolamine/regitine monitor
BP
115
Atenolol brand name
Tenormin
116
Atenolol similar drugs (2)
metroprolol
| Toprol XL
117
atenolol class price range
4/52 to $100 for Toprol XL
118
Atenolol/Tenormin
- pharm
- therapeutic (4)
- specific b1 blocker
| - antihypertensive, anti arrhythmic, primary and secondary prevention of MI, anti anginal
119
Atenolol/Tenormin pharmacodynamics
binds directly to B1 receptors w/ preference for beta-1 --leads to lower bP via several potential mechanisms; recent evidence suggests less effective in preventing strokes than other drugs
120
Atenolol/ Tenormin pharmacokinetics
- route
- F
- onset
- duration
- how many times/ day
- how excreted
- metroprolol metabolism
- po/iv
- variable
- onset 1-2 hrs
- durations 12-24h
- can be given once per day
- renally excreted (so has longer half life)
- metoprolol has hepatic metabolism so has shorter half life
121
Atenolol/ Tenormin Toxicity
| 5
- excessive hypotension
- bradycardia
- heart block
- can worsen severe cHF (but indicated for mild/moderate/stable CHF)
- worsen bronchospasm in severe asthmatics
122
Atenolol/Tenormin Interactions
- additive effects w/ most other anti-hypertensives
| - additive AV block with CEBs (calcium entry blockers)
123
Atenolol/Tenormin Special Considerations
may be especially useful in HTN patients w/ exertional angina, MI, A fib
watch out for abrupt withdrawal
metoprolol has more data for use in patents s/p MI
124
Atenolol/Tenormin Inidcations and dose/route
for HTN patients
| 25-100 mg per day in one or two doses
125
Atenolol/Tenormin monitor (3)
BP HR exercise
126
Propranolol trade name
Inderal
127
Propranolol/Inderal drug class
- pharm
- therapeutic (4)
-non specific B blocker
-antihypertensive, antiarrhythmic, primary and secondary prevention of MI
; anti-anginal
128
Propranolol/Inderal cost
4$ up to $180
129
Propronalol/Inderal pharmacodynamics
binds to B1/B2 receptors leading to lower BP via several potential mechanisms; recent evidence suggests less effective in preventing strokes than other drugs
130
Propranolol/Inderal Pharmacokinetcs
- route
- F
- onset
- duration
- how often given / day
- how cleared/metabolized
```
availabel po or iv
variable F
onset 1-2 hrs
duration: 12-24h
can be given once per day
cleared by hepatic metabolism
```
131
Propranolol/Inderal Toxicity
| -4
excessive hypotension; brady; heart block can worse severe CHF (but indicated for mild/moderate/stable CHF; worsen bronchospasm in severe asthmatics
132
Propranolol/Inderal Interactions
- additive effects w/ most other anti-hypertensives
| - additive AV block with CEBs (calcium entry blockers)
133
Propranolol/Inderal Special considerations
may be especially useful in HTN patients w/ exertional angina, MI, A fib
watch out for abrupt withdrawal
metoprolol has more data for use in patents s/p MI
134
Propranolol/Inderal indications and dose/route
for HTN patients
| 25-100 mg per day in one or two doses
135
Propranolol/Inderal
| Monitoring
BP, HR, exercise tolerance
136
Labetalol brand name
Trandate
137
Labetalol/Trandate similar drugs
carvedilol/Coreg (brand name)
138
Labetalol class cost
$4 (carvedilol) to $24 per month
139
Labetalol/Trandate drug class
- pharm
- therapeutic
mixed a/b blocker
| therapeutic- antihypertensive, treatment of stable CHF (corey)
140
Labetalol/Trandate Pharmacodynamics
reduce BP by blocking b/a receptors and thereby lowering BP by several different mechanisms; patents differ in degree of beta and alpha blockade
141
Labetalol/Trandate Pharmacokinetics
- absorption
- F
- onset
- metabolism: where/which enzyme
-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 by liver 2D6
142
Labetalol/Trandate Toxicity
- avoid in ( 5)
- cautious use (3)
```
avoid in patients with brady, heart block, cHF, asthma, shock
-use cautiously in patients with cardiomyopathy, pheochromocytoma, or pregnancy class D
```
143
Labetalol/Trandate Interactions
additive effect with most antihypertensives
144
Labetalol/Trandate Special considerations
- liver fxn
- most troubling side effect
- most often used in which situation
- use reduced doses w/ reduced liver fxn
- dizziness is most troubling side effect
- most often used for HTN crisis
145
Labetalol/Trandate Indications and dose/route
- most common
- chronic treatment
most commonly given IV with small initial boluses of 20 mg, followed by continuous infusion at 2 mg/min
not usually given po for chronic treatment
80 mg thrice daily, or 240 mg SR (sustained release) once daily
146
Labetalol/Trandate Monitor (2)
BP, HR
Pharmacology
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