L1 and 2 - Autonomic drugs Flashcards
1
Q
What are the 2 main fibres of neurone?
A
pre and post ganglionic
2
Q
what are the 2 main NT?
A
cholinergic and adrenergic
3
Q
what 2 systems is the nervous system split into?
A
- central
2. peripheral
4
Q
2 branches of peripheral NS
A
somatic and autonomic
5
Q
which NS is the sympathetic and parasympathetic a part of ?
A
autonomic
6
Q
4 conditions where autonomic drugs are used?
A
- angina
- asthma
- anaphylactic shock
- hypertension
7
Q
what does the parasympathetic system do?
A
rest and digest
8
Q
what does the sympathetic system do?
A
fight or flight
9
Q
where do parasympathetic neurones synapse?
A
cranial and sacral
10
Q
where do sympathetic neurones synapse?
A
thoracic, lumbar, sacral
11
Q
what type of synapse are ALL pre-ganglionic synapses in the ANS?
A
Cholinergic
12
Q
what is the difference between the post-ganglionic synapses in the parasympathetic and sympathetic NS?
A
para - Ach
symp - ACh and NE
13
Q
describe the difference in synapses in the symp NS
A
sweat glands - Ach
Cardiac +smooth muscle, gland cells, nerve terminals - NE
14
Q
what synapses are the in somatic nervous system?
A
ACh
15
Q
2 main types of autonomic receptors?
A
cholinoceptors
adrenoceptors
16
Q
2 types of adrenoceptors
A
alpha and beta
17
Q
2 types of cholinoceptors
A
nicotinic and muscarinic
18
Q
what are the adrenoceptor alpha and beta subtypes?
A
a-1, a-2
b1 to b3
19
Q
what are the cholinoceptor nicotinic subtypes?
A
muscle, ganglion and CNS
20
Q
what are the cholinoceptor muscarinic subtypes?
A
M1 to M5
21
Q
what type of receptors are in the heart for sympathetic stimulation?
A
B1
22
Q
what type of receptors are in the heart for parasympathetic stimulation?
A
M2
23
Q
which 2 tissues arterioles can both constrict and dialate (para and symp systems)?
A
erectile tissue and salivary glands
24
Q
what type of transduction method is there in nicotinic receptors?
A
type 1 ionitropic
25
what type of transduction method is there in muscaranic receptors?
type 2 metabotropic
26
what does ionotropic mean?
ligand gated
27
what does metabotropic mean?
second messenger model
28
which is the only process which has an M1 parasympathetic receptr?
gastric acid secretion
29
which types of receptrs are present in the sympathetic system?
adrenonergic
30
which types of receptrs are present in the parasympathetic system?
cholinergic
31
what are the remaining organs parasympathetic receptors?
M3
32
what are all muscles sympathetic receptors?
b2
33
sympathetic receptor for BV arterioles; coronary, viscera, skin, brain, erectile tissue, salivary gland ?
a
34
sympathetic receptor for muscle arterioles and vein dilation?
b2
35
is there sympathetic stimulation for smooth muscle ? explain why
no - it is dilated by cirulating adrenaline
36
sympathetic receptor for smooth muscle which adrenaline acts on
b2
37
3 sympathetic receptor for smooth muscle GI tract
b2, a1, a2
38
2 sympathetic receptor for sphincters GI tract
b2, a2
39
what sympathetic receptor for uterine contraction for pregnant women?
a
40
what sympathetic receptor for uterine contraction for non-pregnant women?
b2
41
sympathetic receptor for bladder relaxation?
b2
42
sympathetic receptor for bladder sphincter contraction?
a1
43
which is the only process which uses b3 receptor - is this para or symapthetic?
adipose lipolysis - symp
44
sympathetic receptor for pupil dilation?
a
45
sympathetic receptor for ciliary eye muscle?
b
46
sympathetic receptor for sweat glands? why?
M3 - is it cholinergic
47
sympathetic receptor for piloerection in skin?
a
48
2 sympathetic receptor for salivary gland secretion?
a, b
49
sympathetic receptor for kidney renin secretion?
b1
50
sympathetic receptor for liver gluconeogeneis and glycogenolysis?
a, b2
51
6 types of cholinergic drugs
1. muscarinic agonists
2. muscarinic antagonists
3. ganglion stimulating
4. ganglion blocking
5. neuro-muscular blockers
6. anticholinesterases
52
what is another name for anticholinergic drugs?
muscarininc antagonsits
53
another name for muscarininc agonsits?
direct acting parasympatomimetic
54
4 naturally occuring muscarinic agonists
ACh
muscarine
arecoline
pilocarpine
55
2 clinically used muscarinic agonists
pilocarpine
| betanechol
56
5 peripheral effects of muscarinic agonists
1. exocrine secretion
2. contraction of SM
3. relaxation of sphincters
4. eye; miosis (pupil constricion) + contraction of ciliary mucsle
5. fall in arterial BP
57
what are pilocarpine drops useful in treating? explain how
glaucoma - allows fluid to drain out
58
equation for BP
BP = cardiac output x peripheral resistance
59
2 CV effects of muscarinic agonists
1. reduction in cardiac output
| 2. vasodilation
60
how do muscarinic antagonists work?
inhibiting responses of ACh
61
3 types of muscarinic antagonists
1. non-selective receptor
2. M1 selective
3. M3 selective
62
example of non-selective muscarinic antagonists
atropine
63
example of M1 receptor muscarinic antagonists and use
pirenezipine - peptic ulcer
64
example of M3 receptor muscarinic antagonists and use
darifenacin - urinary incontinence
65
effects of muscarinic antagonists on the eye
mydriasis
| paralysis of cilary muscle
66
pathological effects of atropine when trreating eye conditons
1. blurred vision
2. photophobia
3. poor night vision
67
can alternative drug can be used instead of atropine to reduce side effects
tropicamide
68
when are cycloplegic drugs used?
treat squints
69
effect of muscarinic antagonists on CV
increases HR
70
clinical use of muscarinic antagonists on CV
treat bradycardia following MI
71
3 effects of muscarinic antagonists on resp system
1. bronchodilation
2. increased vital capacity
3. decreased mucus secretion
72
example of 2 muscarinic antagonists drugs which are used to treat asthma/COPD
ipratropium
| tiortropium
73
effects of muscarinic antagonists on urinary tract
contracts internal sphincter muscle
74
clinical use of muscarinic antagonists on urinary tract
treat urinary incontinence
75
5 clinical uses of muscarinic antagonists on CNS
1. anti-emetic
2. pre-med for anaethesia
3. treat ridigitity parkinsons
4. block cholingeric effects of antipsychotics
5. antidote to parasympathomimetic drugs
76
1 muscarinic antagonists drug which is used to treat ridigitity in parkinsons
1. Orphenadrine
2. procyclidine
3. trihexyphenidyl
77
naturally occuring ganglion stimulating drug
nicotine
78
clinical use of ganglion stimulating drug
smoking cessation
79
2 ways ganglion-blockign drugs work
1. competitve inhibition of ACh at NICOTINIC receptors
| 2. block cation channels which are normally activated by ACh binding
80
what is hexomethonium used for ? what type of drug is it?
hypertension - ganglion blockign drug
81
clinical use of neuromuscular blocking drug
relaxation for surgery
82
2 sites where neuromuscular blocking drugs work
1. pre synaptic
| 2. post synaptic
83
how do pre-synaptic neuromuscular blocking drug works
1. block ACh release
| 2. block ACh synthesis
84
example of neuromuscular blocking drug which blocks Ach synthesis?
hemicholinium
85
how does botulinum work?
neuromuscular blocking - preventing exocytosis of ACh from pre-neurone
86
2 types of neuromuscular blocking drug post synatptic
1. non-depolarising
| 2. depolarising
87
how do post-synaptic non-depolarising neuromuscular blocking drug work?
competitive ACh antagonist at receptor
88
how do post-synaptic depolarising neuromuscular blocking drug work?
decrease electrical excitability of end plate - cannot produce AP when ACh attaches
89
2 examples of post-synaptic non-depolarising neuromuscular blocking drug
tubocurarine
| pancuronium
90
2 examples of post-synaptic depolarising neuromuscular blocking drug
decamethonium
| suxamethonium
91
function of cholinesterases
hydrolyse and inactivate ACh
92
2 types of cholinesterases
1. acetylcholinesterase (AChE)
| 2. Butyrylcholinesterase (BuChE)
93
which synapses are AChE found at?
cholinergic
94
which is more specific ; 1. acetylcholinesterase (AChE)
| 2. Butyrylcholinesterase (BuChE)
acetylcholinesterase (AChE)
95
AChE has 2 binding sites for its substrates. what are they - what do they do?
```
anionic = correct orientation
esteric = hydrolysis reaction
```
96
function of anticholinesterases
inhibit ACh hydrolysis
97
what effect do anticholinesterases have on the synapse?
- build up of ACh
| - prolonged + intensified effects
98
how are anticholinesterases classified?
nature of complex they form with ACh
99
3 types of anticholinesterases
1. rapidly reversible
2. slowly reversible
3. irreversible
100
describe nature of rapidly reversible anticholinesterases
bind to anionic site
short duration
ionic bond
101
describe nature of slowly reversible anticholinesterases
- strongly bind to anionic site
| - esteric site = slowly hydrolysed
102
describe nature of irreversible anticholinesterases
- binds to active/esteric site
| - bond initially reversible but then irreversible
103
example of rapidly reversible anticholinesterase drug and clinical use
edrophonium - diagnosis of Myasthenia Gravis
104
2 examples of slowly reversible anticholinesterase drug and clinical use
physostigmine
neostigmine
miotic, alzheimers
105
which patients expeience milder SE when given anticholinesterases
dementia
106
2 side effects of anticholinesterases
1. excessive peripheral muscarinic stimulation
| 2. CNS effects due to build up of excess ACh
107
Antagonistic drug to reduce SE of anticholinestarases
atropine
108
how to treat resp paralysis arising from progressive nicotinic peripheral excitation - how does the drug work?
pralidoxime - reactivates cholinesterase
109
what is the oxidative NE pathway metabolised by?
aldehyde dehydrogenase
110
what is the reductive NE pathway metabolised by?
aldehyde rectucase
111
which catecholamine is most potent in alpha receptors?
NA
112
which catecholamine is most potent in beta receptors?
isoprenaline
113
peripheral location of a1 receptor and function
BV, smooth muscle; contract
114
peripheral location of a2 receptor and function
nerve endings - inhibit release
115
peripheral location of b1 receptor and function
heart; increase rate and force
116
peripheral location of b2 receptor and function
smooth muscles ; relax
117
peripheral location of b3 receptor and function
fat cells; lipolysis
| detrusor muscle; relax
118
transduction method of all alpha and beta receptors
type 2 - metabotropic
119
2 main drug categories of adrenergic transmission
sympathomimetic
| sympatholytic
120
2 types of sympathomimetic drugs
1. direct acting - adrenoceptor agonists
| 2. indirect acting
121
2 types of sympatholytic drugs
1. direct acting - adrenoceptor antagonists
| 2. indirect acting
122
2 ways in which sympathomimetic indirect acting drugs work?
1) Ca2+ independent release of NA from vesicles into synapse
2) block reuptake of NA at nerve terminals
123
how do sympatholytic indirect acting drugs work?
inhibit NE release
124
3 examples of direct acting sympathomimetic drugs
1. Epinephrine
2. salbutamol
3. terbutaline
125
3 examples of indirect acting sympathomimetic drugs
1. tyramine
2. TCA
3. amphetamine
126
2 types of direct acting symaptholytic drugs
alpha and beta blockers
127
3 examples of direct acting symaptholytic drugs
1. doxazosin
2. propanolol
3. atenolol
128
2 examples of indirect acting symaptholytic drugs
1. methyldopa
| 2. resperine
129
side effect of tyramine
cheese effect
130
effects of isoprenaline and adrenaline on
i) HR
ii) peripheral resistance
iii) BP
i) increase
ii) decrease
iii) increase systolic, decreases diastolic
131
effects of NA
i) HR
ii) peripheral resistance
iii) BP
i) dec
ii) incre
iii) increase
132
how do catecholamines regulate energy metabolism
mobilise glygogen and fat stores to meet energy req
133
2 effect of sympathomimetics on the eye
1. mydriasis
| 2. dec intraocular pressure in glaucoma
134
effect of sympathomimetic drugs on vasculature
vasoconstriction
135
in terms of the CVD effects, what can sympathomimetic drugs be used to treat?
1. hypertension
2. cardiac arrest
3. circ shock
4. anaphylactic shock
136
effect of sympathomimetic drugs on smooth muscle
relaxation
137
what is mirabegron used for
treatment of overactive bladder
138
3 examples of alpha blockers
1. phentolamine
2. prazosin
3. yahimbine
139
3 clinical uses of alpha blockers
1. raynauds syndrome
2. hypertension
4. benign hypertrophy prostate
140
what type of drug is doxazocin and what is it used for?
alpha blocker - hypertension
141
main beta blocker
propanaolol
142
what condition are beta blockers contraindiacted in?
asthma
143
5 use of beta blockers in CV
1. MI
2. angina
3. hypertension
4. heart failure
5. cardiac arrythmias
144
4 uses (not CV) of beta blockers
1. reduce formation of aq fluid in glaucoma
2. migraine headaches
3. overactive thyroud
4. anxiety
145
2 functions of indirect acting sympatholytic drugs
1. blocks NA stores
| 2. inhibits NA release
146
indirect acting sympatholytic drug which blocks NA stores
reserpine
147
indirect acting sympatholytic drug which inhibits NA release
Guanethidine
148
clinical use of indirect acting sympatholytic drugs
treat hypertension during pregnancy
149
nerve terminal of nerves supplying sympathetic innveration to adrenal medulla
cholinergic
150
nerve terminal of somatic nerves to voluntary/skeletal muscles
cholingerfic
151
all organs supplied by this division can be stimulated simultaenously
sympathetic
152
which nerve supplies the parasymp autonomic innervations to most organs in abdo and thorax
vagus nerve
153
receptor subtype of neuro-effector junction of all parasymp nerves
muscarinic
154
receptor subtype of neuro-effector junction of all symp nerves (except sweat glands)
adrenergic - alpha or beta
155
receptor subtype of neuro-effector junction of all symp nerves supplyin sweat glands
M3
156
location of M1 receptors
stomach
157
location of M2 receptors
heart
158
location of M3 receptors
glands + smooth muscle
159
what is organophosphase poisoning ?
organophosphates irreversibly inhibit cholinesterases - build up of ACh
160
2 drug used to treat organophosphase poisoning ?
atropine (antimuscarinic) - inhibits effects of ACh
pralaxidome - reactivates cholinesterase enzymes
