B4-005 Autonomic Drugs Flashcards
(95 cards)
1
Q
what adrenoreceptors:
* peripheral vasculature
* contraction of smooth muscle
* increase BP
A
alpha 1
2
Q
what adrenoreceptor:
* presynaptic autoregulation of neurotransmitter release
A
alpha 2
3
Q
what adrenoreceptor:
* approx equal affinity for Epi and NE
A
beta 1
4
Q
what adrenoreceptor:
* higher affinity for Epi than NE
A
beta 2
5
Q
densensitization of adrenoreceptors may limit
A
therapeutic response
6
Q
denervation supersensitivity of adrenoreceptors may
A
exacerbate side effects
7
Q
catecholamines
A
- epinephrine
- norepinephrine
- isoproternol
- dobutamine
8
Q
- very potent vasoconstrictor & cardiac stimulant
- positive inotropic and chronotropic actions on heart
- also activates beta2 receptors
A
epinephrine
9
Q
similar potency at beta 1 receptors, but relatively little effect on beta 2
A
norepinephrine
10
Q
- compensatory vagal reflexes over come direct positive chronotropy
- at high doses, may indirectly increase heart rate
A
norepinephrine
11
Q
- potent nonselective beta-receptor agonist
- positive chronotropic and inotropic actions
- decreases both diastolic and mean arterial pressure
A
isoproterenol
12
Q
- relatively beta 1 selective synthetic catecholamine
- also activates alpha 1 receptors
A
dobutamine
13
Q
- prototypic alpha1 agonist
- not a chatechol derivative
- not inactivated by COMT
- longer duration of action than catecholamines
- mydriatic and decongestant
- can raise blood pressure
A
phenylephrine
14
Q
first orally active sympathomimetic drug
A
ephedrine
15
Q
- widely available OTC decongestant
- also have indirect effects of releasing endogenous NE
A
psuedoephedrine
16
Q
- direct alpha 1 agonists
- used as topical decongestants
2
A
- oxymetazoline
- xylometazoline
17
Q
- alpha 2 selective agonists
- used (poorly) as antihypertensives
- dimish SNS outflow
2
A
- clonidine
- methyldopa
18
Q
- beta 1 selective agonist
- increases cardiac output with less reflex tachycardia
- lack of beta 2 stimulated venous dilation
A
dobutamine
19
Q
- beta 2 selective agonists
- treatment of asthma
2
A
- albuterol
- salmeterol
20
Q
- beta 2 selective agonist
- treatment of premature labor
A
ritodrine
21
Q
- indirect sympathomimetics
- marked stimulant effects on mood and alertness
- depressant effect on appetite
A
- amphetamine
- methamphetamine
22
Q
- local anesthetic
- sympathomimetic due to blockade of uptake 1
A
cocaine
23
Q
- releases stored catecholamines
- found in high concentrations in fermented foods (cheese)
- MOA inhibitors potentiate effects and can produce hypertension
A
tyramine
24
Q
- prototypic alpha antagonist
- nonselective between alpha1 and alpha2
- competitive blockade of receptors
- reduces TPR, MAP
- produces reflex tachycardia (SNA reflex)
A
phentolamine
25
* irreversible-binds covalently to alpha receptors
* postural hypotension and tachycardia limit use
phenoxybenzamine
26
* alpha receptor antagonists
* selective for alpha 1 receptors
| 3
* prazosin
* terazosin
* doxazosin
27
* alpha2 selective antagonist
* no established clinical role
yohimbine
28
* block effects of catecholamines at beta receptors
* varied affinity for beta1 vs. beta2 receptors
* selectivity has important clinical implications
* non are absolutel specific for beta1 receptors
beta receptor antagonists
29
* lower blood pressure in patients with hypertension
* negative inotropic and chronotropic effects
* reduce oxygen demand of myocardium
beta receptor antagonists
30
clinically useful for:
* hypertension
* ischemic heart disease
* cardiac arrhythmias
* glaucoma
* hyperthyroidism
beta blockers
31
* prototypical beta-blocking drug
* nonselective
propranolol
32
beta-1 selective beta blockers
| 2
metoprolol
atenolol
33
beta blockers with a very long duration of action
| 2
nadolol and timolol
34
* reversible alpha1 antagonist
* also nonselective beta antagonist
* hypotension with less tachycardia than alpha blockers
labetalol
35
* beta blocker
* selective for beta2 receptors
* no obvious clinical application
butoxamine
36
# name the adrenoreceptor:
sympathetic activity contracts the radial muscle of the iris
a1
37
# name the adrenoreceptor:
parasympathetic activity contracts the circular muscle of the iris
M3
38
# name the adrenoreceptor:
sympathetic activity relaxes ciliary muscle of eye
beta
39
# name the adrenoreceptor:
parasympathetic activity contracts the ciliary muscle of eye
M3
40
# name the adrenoreceptor:
sympathetic activity accelerates SA node
b1/b2
41
# name the adrenoreceptor:
parasympathetic activity decelerats SA node
M2
42
# name the adrenoreceptor:
sympathetic activity accelerates ectopic pacemakers
b1/b2
43
# name the adrenoreceptor:
sympathetic activity increases contractility of the heat
b1/b2
44
# name the adrenoreceptor:
parasympathetic activity decreases contractility of the heart
M2
45
# name the adrenoreceptor:
sympathetic activity contracts blood vessels of skin and splanchnic vessels
alpha
46
# name the adrenoreceptor:
sympathetic activity relaxes blood vessels in skeletal muscles
b2, M3
47
# name the adrenoreceptor:
sympathetic activity contracts blood vessels in skeletal muscles
a
48
# name the adrenoreceptor:
parasympathetic activity releases EDRF in blood vessels of endothelium
m3
49
# name the adrenoreceptor:
sympathetic activity relaxes bronchiolar smooth muscle
b2
50
# name the adrenoreceptor:
parasympathetic activity contracts bronchiolar smooth muscle
m3
51
# name the adrenoreceptor:
sympathetic activity relaxes walls of smooth muscle in GI tract
a2, b2
52
# name the adrenoreceptor:
sympathetic activity contracts sphincters of GI tract
a1
53
# name the adrenoreceptor:
parasympathetic activity contracts walls of smooth muscle in GI tract
m3
54
# name the adrenoreceptor:
parasympathetic activity relaxes spinchters in GI tract
m3
55
parasympathetic activity increases secretion in GI tract
m3
56
# name the adrenoreceptor:
parasympathetic activity activates mesenteric plexus in GI tract
m1
57
# name the adrenoreceptor:
sympathetic activity relaxes bladder wall
b2
58
# name the adrenoreceptor:
parasympathetic activity contracts badder wall
m3
59
# name the adrenoreceptor:
sympathetic activity contracts spinchters in GU tract
a1
60
# name the adrenoreceptor:
parasympathetic activity relaxes spinchters in GU tract
m3
61
# name the adrenoreceptor:
sympathetic activity relaxes uterus
b2
62
# name the adrenoreceptor:
sympathetic activity contracts uterus
a
63
# name the adrenoreceptor:
parasympathetic activity contracts uterus
m3
64
# name the adrenoreceptor:
sympathetic activity causes ejaculation
a
65
# name the adrenoreceptor:
parasympathetic activity causes erection
M
66
# name the adrenoreceptor:
sympathetic activity contracts pliomotor smooth muscle
a
67
# name the adrenoreceptor:
sympathetic activity increases thermoregulatory sweat glands
M
68
# name the adrenoreceptor:
sympathetic activity increases apocrine sweat glands
a
69
# name the adrenoreceptor:
sympathetic activity increases gluconeogenesis
b2 and a
70
# name the adrenoreceptor:
sympathetic activity increases glycogenolysis
b2 and a
71
# name the adrenoreceptor:
sympathetic activity stimultes lypolysis
b3
72
# name the adrenoreceptor:
sympathetic activity stimulates renin release
b1
73
# name the adrenoreceptor:
parasympathetic activity decreases NE release
M
74
# name the adrenoreceptor:
sympathetic activity decreases ACh release
a
75
cholinomimetic agents mimic
acetylcholine
76
cholinoceptor-activating and cholinoesterase-inhibiting drugs are classified by
**receptor action**
* muscarinic
* nicotinic
**mechanism of action**
* direct
* indirect
77
directly bind and activate muscarinic or nicotinic receptors
direct acting
78
directly bind and activate muscarinic or nicotinic receptors
direct acting
| cholinomimetic agents
79
* reduce hydrolysis of acetylcholine
* increase endogenous acetylcholine concentration at synapse
* excess acetylcholine increases responses
* drugs act primarily where acetylcholine is physiologically released
indirect acting agents
| ihibit acetylcholinesterase
80
ACh effects are terminated by
acetylcholinesterase
| indirect agents inhibit this
81
3 chemical groups that cholinesterase inhibitors fall into
1. simple alcohols
2. carbamic acid esters
3. organic derivatives of phosphoric acid (organophosphates)
82
* simple alcohol
* colinesterase inhibitor
edrophonium
83
quaternary carbamic acid ester
neostigmine
84
tertiary carbamic acid ester
physostigmine
85
organophosphates
soman
sarin
malathion
86
used as insecticide
malathion
87
direct affect is to slow heart rate
muscarinic agonists
88
* autonomic ganglia are major site of action
* simultaneous SNS and PSN discharge
* predominant tone predicts effects
nicotinic agonists
| SNS-vasculature
PNS-most other tissues
88
* autonomic ganglia are major site of action
* simultaneous SNS and PSN discharge
* predominant tone predicts effects
nicotinic agonists
| SNS-vasculature
PNS-most other tissues
89
* antimuscarinic drugs
* tertiary compounds used for their effects in **eye or CNS**
* atropine
* scopolamine
90
* antimuscarinic drugs
* quaternary amines selectively produce **peripheral effects**
ipratropium
91
* prototypic antimuscarinic drug
* causes **reversible** blockade
* not selective between subtypes
atropine
92
neuronal nicotinic receptor antagionists
| 3
* hexamethonium
* trimethapan
* mecamylamine
93
* block actions of ACh and other agonists at nicotinic receptors
* receptors located in both PNS and SNS autonomic ganglia
* non-selectivity produces limited side effects
* synthetic amines
neuronal nicotinic receptor antagonists
94
* first ANS ganglion blocking drugs
* short duration of action
* mangement of hypertension
tetraethylammonium (TEA)
