Pharmacology of the ANS Flashcards

1
Q

describe the differnt pathways of synapses for parasympathetic and sympathetic:

a) general b) adrenal gland c) kidney d) sweat gland

A

parasympathetic:

  • long preganglionic neurons -> synapse = Ach and nicotinic Ach receptor –> short postganglionic neuron: synapse is between Ach and muscarinic receptor at target organ

sympathetic:

most = a

a) short pre ganglionic neuron -> sympathetic ganglion: Ach and nicotinic Ach synapse –> long post-ganglionic neuron to target organ: synpase is between norepinephrine / noadrenaline NT and a or b adrenoreceptor

b) straight to adrenal gland: synapse = Ach N: release of noreinephrine release or epinephrine

c) sweat glands: short preganglionic neurons -> synapse = Ach and nicotinic Ach receptor –> long postganglionic neuron: synapse is between Ach and muscarinic receptor at target organ

d) kidney: short preganglionic neurons -> synapse = Ach and nicotinic Ach receptor –> long post ganglionic neuron -> synapse between dopamine and dopamine receptors

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2
Q

which out of pre ganglionic or post ganglionic targeting for drugs will be more specific?

A

post ganglionic neuron.

why? bc both parasymp and sym use Ach [N] in pre ganglionic neuron, if target this might have an effect on both instead of individual action

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3
Q

what type of receptor is Ach Nicotinic receptor?

A

ionotropic receptor

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4
Q

all preganglionic fibres - whether from sympathetic or parasympathetic NS use what as NT and as the receptor?

A

all preganglionic neurons use:

- Acetylcholine as NT

- nicotinic acetylcholine receptor as receptor

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5
Q

what are NANC neurons?

where found?

what are the NTs used ? (probs dont need to know exact)

A

- NANC = non-adrenergic non cholinergic neurons (NTs aren’t adreneric or cholinergic class)

  • location: peripheral tissues - smooth muscle in GI, airways and reproductive tracts
  • NTs: nitric oxide, ATP, 5HTP, neuropeptide Y
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6
Q

for awareness: :) (probs)

how do NANC synpases work?

A

when useing NANC neurons -> occur in sympathetic nerve varicosity:

  • vesicles are of different sizes:
  • small granular vesicles and medium granular vesicles bind to receptors and cause smooth muscle relaxation (for eg)
  • large granular vesicles can bind to receptors on BOTH sides - (pre and post ganglionic). if bind on preganglionic sides - prevent the release of NTs across synaptic cleft, if bind on post-synaptic receptor - more muscle relxation
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7
Q

what are parasympathomimetics?

A

parasympathomimetics: parasympathetic agonists
- produce similar response to Ach: can activate muscarinic receptors or prevent normal Ach break down, so can have bigger effect (more endogenous NT)

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8
Q

explain structure of nicotinic receptor

where are the different a subunits found (awareness)?

A
  • pentameric sodium ion channel
  • 2 alpha subunits:
  • alpha 3 found on autonomic ganglia
  • alpha 1 found on neuromuscular junction
  • alpha 4 & 7 found in CNS

- 3 beta subuits

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9
Q

name 4 different nicotinic agonists

A

acetylcholine

carbachol

nicotine: more selective for ganglionic and CNS (than neuromuscular junction)

suzamethonium: more selective for neuromuscular junction - muscle relaxation in anaesthesia

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10
Q

which receptors do both acetylcholine & carbachol work on? what does this mean as a consq?

what is carbachol used to treat?

A
  • work at both nicotinic and muscarinic receptors: have an effect on both para and sympathetic NS
  • carbachol: treats glaucoma
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11
Q

name and state uses for 3 nicotinic antagonists

A
  1. hexamethonium: antihypertensive treatment
  2. pancuronium: neuromuscular block: lethal injections
  3. tubocararine: skeletal muscle relaxation
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12
Q

most of autonomic NS pharmacology is targeted at which receptors? why?

^ what type of protein?

A

muscarinic receptors: bc located on target organ = precise response

muscarinic receptors: G-coupled protein receptors

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13
Q

how many types of muscarinic receptors are there? which ones are inhib/ excitatory? - what are second messengers for inhibit / excitatory/

A

5 types:

  • *- M1 = excitatory:** 2nd messenger = IP3 & DAG
  • *- M2 = inhibitory:** 2nd messenger = cAMP
  • *- M3 = excitatory:** 2nd messenger = IP3 & DAG
  • M4 and M5 in CNS (dont need to know)
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14
Q

where is M1 / 2/ 3 found? role?

A
  • *M1:**
  • location: GI system
  • function: gastric acid secretion
  • *M2:**
  • location: heart
  • function: cardiac inhibition (bradychardia)

M3:

  • location: smooth muscle, vascular endothelium
  • function: secretion of glands, vasodilation, smooth muscle contraction
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15
Q

name and say the role of 2 muscarinic agonists

A
  • *bethanechol:**
  • M3 receptor
  • increases bladder and GI contraction (gets rid of urine in bladder and aids peristalsis)
  • *pilocarpine:**
  • eye drops for glaucoma (iris circular muscle contraction, ciliary muscle contraction)
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16
Q

how do muscarinic antagonists work?
what are the two types?

A

block the action of muscarinic receptors. get:

  • non-selective for any muscarinic receptor
  • selective for specific muscarininc receprots (m1 m2 etc)
17
Q

name 4 non selective muscarinic antagonists

A
  1. atropine
  2. tropicamide
  3. scopolamine
    4 ipratropium
18
Q

name uses for all of these drugs

  1. atropine
  2. tropicamide
  3. scopolamine
    4 ipratropium
A
  1. atropine: pupil dilation, treats brachycardia, reduces bronchial secretions, used in organophosphate poisoning
  2. tropicamide: dilation of pupil
  3. scopolamine: GI antispasmodic, motion sickness

4 ipratropium: inhaled for asthma

19
Q

name a drug and role for M1, M2 and M3 muscarinic antagonists

A
  • M1: pirenzepine / telenzepine: reduces gastric acid secretions
  • M2: gallamine: causes tachycardia (increases HR)
  • M3: darifenacin / solifenacin: overactive bladder
20
Q

what is acetylcholine broken down by?

A

acetylcholinestarase

21
Q
A
22
Q

what do cholinesterase inhbitors do?

A
  • stimulate GI function
  • cognitive enhancers (given to AD patients)
  • skeletal muscle activity
23
Q

what does clostridium botulinum bacteria do?

how effect?

A

botulinium toxin (botox)

  • prevents ACh release: stops synapse signalling
  • irreversble
  • can be used for XS sweating, overactive bladder or muscle spasms
24
Q

which muscarinic receptor is found in the eye, lung and gut? what is agonist / antagonist drug for thAT has effects on them

A

M3:

  • *i) eye:
  • pilocarpine**:** pupilconstrict** (agonist)
  • tropicamide: pupil dilates (antagonist)
  • *ii)** lungs:
  • ipatroprium: lungs conflate (antagonist)
  • *iii) gut:
  • ** neostgimine: gut more moveable (antagonist)
  • scopolamine: inhibits peristalsis - antispasmodic (agonist)
25
Q

what do sympathomimetics do?

what are two important classes?

A

produces a similar response as noradrenaline and adrenaline on the sympathetic NS

classes:

  • *i) monoamines
    ii) catecholamines (**e.g. noradrenaline, adrenoline)
26
Q
A
27
Q

which is NT used in majority of the sympathetic NS?

A

noradrenaline

28
Q

need to know how adrenaline and noradrenaline are synthesised and broken down? check the MESS lectures

A
29
Q

what type of protein are adrenoreceptors? what does that mean ?

A

GCPR - can have excitatory or inhibitory response (depending on 2nd messenger system)

30
Q

what variants of adrenoreceptors are there? which are pre / post synaptic? excitatory or inhbitor?

A
  • *alpha**:
  • alpha 1: postsynaptic excitatory
  • alpha 2: presynaptic. inhbits further release of noradrenaline
  • *beta**:
  • beta 1: postsynaptic excitatory
  • beta 2: postsynaptic excitatory
  • beta 3: postsynaptic excitatory
31
Q

name 2 alpha receptor agonists - what do they do?

A
  • a1 phenylephrine: vasoconstriction, nasal decongestant
  • a2 clonidine: antihypertensive (inhbits noradren. release), sedative use when used with ketamine
32
Q

what class of drugs are alpha 1 prazosin, doxazosin, tramsulosin and alpha 1 yohimbine?

what are their functions?

A

alpha receptor antangonists

functions: smooth muscle relaxers so are anti-hypertensive, benign prostatic hyperplasia

33
Q

name 3 beta receptor agonists and their function

A

- B1 dobutamine: increases HR - used in cardiac arrest

  • B2 salbutamol: bronchodilation
  • B3 solabegron: being developed for overactive bladder and IBS
34
Q

name and state use of non selective, b1 and b2 receptor agonists

A

non-selective: timolol: used to decrease aq humour productio

b1 atenolol: decreases HR, used in angina and hypertension

b2 butoaxmine: no clinical use

35
Q
A

Beta 1:

  • heart:
    i) dobutamine (agonist). HR increase and depth
    ii) atenolol (antagonist) HR decrease (treats tachycardia)