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Pharmacology > Drugs of the ANS + NMJ > Flashcards

Drugs of the ANS + NMJ Flashcards

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1
Q

what are ganglion blocking drugs?

A

nAchR receptor antagonists

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2
Q

types of nAchR receptor antagonists

A
  • Hexamethonium

- Trimethaphan

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3
Q

what does trimethaphan do?

A

nAchR short acting antagonist; used for resolving hypertension during surgery

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4
Q

what does a-bungarotoxin do?

A

irreversible antagonist of nAchR, toxin produced causes respiratory and brain paralysis

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5
Q

what is Atropine?

A

competitive mAchR antagonist

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6
Q

what is Hyoscine?

A

competitive mAchR antagonist

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7
Q

what is tropicamide?

A

topical mAchR antagonist causing miosis, useful when examining the retina

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8
Q

why are mAchR antagonists used as anaesthetic pre-medication?

A
  • reduced tracheal secretions
  • bronchodilation
  • hypotension

allows easier inhalation of anaesthetic

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9
Q

clinical uses of hyoscine?

A

hyoscine patch is used to treat motion sickness, inhibits cholinergic nerve transmission to the vomiting centre

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10
Q

how are anticholinergic drugs used for treatment of Parkinson’s?

A

M4R usually reduces D1 dopaminergic transmission in the nigrostriatal pathway. inhibiting the muscarinic receptor means enhanced dopaminergic receptor transmission

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11
Q

what anticholinergics are used in Obstructive Airway Disease like asthma?

A
  • Ipratropium Bromide
  • Atropine

inhibits bronchoconstriction

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12
Q

how are anticholinergics used for IBS?

A

reduces M3R stimulation, hence decreasing GI motility and secretion

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13
Q

how would you treat an atropine overdose?

A

anti-cholinesterase or cholinomemetic

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14
Q

what does botulinum toxin do?

A

prevents Ach exocytosis

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15
Q

types of directly acting cholinomemetics?

A

Agonists of Muscarinic Receptor:

  • Choline Esters: Bethanechol
  • Alkaloids: Pilocarpine
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16
Q

what is Pilocarpine?

A

non selective mAchR agonist, treatment for closed angle glaucoma

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17
Q

What is Bethanechol?

A

M3 receptor agonist; assists in bladder emptying and improving GI motility

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18
Q

types of indirectly acting cholinomemetics

A

Increase endogenous levels of Ach by inhibition of AchEsterase

  • reversible
  • irreversible
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19
Q

types of reversible anticholinesterases

A
  • physostigmine
  • neostigmine
  • donepezil

work by donating a carbide group blocking the active site which is slowly hydrolysed back.

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20
Q

types of irreversible anticholinesterases

A
  • ecothipate
  • dyflos
  • sarin

these are all organophosphates and covalently bind a large blocking group

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21
Q

clinical uses of physostigmine

A
  • Treating atropine poisoning

- glaucoma (aiding drainage of IOF)

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22
Q

uses of ecothipate

A

for glaucoma, this is the only organophosphate used in clinical use. this is more long acting than other cholinomemetics

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23
Q

what does pralidoxime do?

A

reverses the block in organophosphate poisoning

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24
Q

SNS agonists

A
  • adrenaline
  • phenylephrine
  • clonidine
  • dobutamine
  • salbutamol
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25
how is adrenaline used clinically?
Non selective SNS agonist: - used for anaphylaxis - acute bronchoconstrictive emergencies - cariogenic shock - maintains BP in Spinal Anaesthesias - vasoconstriction in local anaesthetics prolonged actions
26
phenylephrine clinical uses
a1 receptor agonist resistant to COMT degreadation: - decongestant - mydriatic vasoconstriction causes reduced white cell infiltration and reduced oedema and fluid leakage
27
clinical uses of clonidine
a2 receptor agonist treats: - hypertension - migraine - reduces CNS sympathetic outflow
28
uses of isoprenaline
non selective beta agonist treats: - Cariogenic shock - acute heart failure - MI resistant to MAO and uptake 1
29
what is b2 mediated reflex tachycardia?
stimulating b2 receptors in skeletal muscles causes vasodilation hence there is a reflex tachycardia
30
which drug overcomes b2 mediated reflex tachycardia?
Dobutamine; selective b1 agonism
31
clinical uses of dobutamine
short acting emergency treatment for cariogenic shock | short half life as rapidly degraded by COMT
32
clinical uses of Salbutamol
selective B2 agonist: - asthma - treating threatened premature labour (relaxes uterine smooth muscle)
33
target for carvedilol
non selective a1 and b1 + b2 adrenoceptor antagonist Dual action means also alpha 1 mediated vasoconstriction decreased
34
target for Phentolamine
a1 + a2 adrenoceptor antagonist
35
target for prazosin
a1 selective adrenoceptor antagonist
36
propranolol target
non selective b1 +b2 adrenoceptor antagonist
37
atenolol target
b1 selective adrenoceptor antagonist
38
how to beta blockers work as an antihypertensive?
- propranolol - atenolol - carvedilol - Nebivolol - Sotalol they decrease b1 mediated cardiac output and angiotensin ii release.
39
how does Nebivolol work?
b1 antagonism and potentiates the release of NO hence vasodilation and reduced Q
40
how does Sotalol work?
causes vasodilation and reduced Q by inhibiting K+ channels and blocking b1 + b2
41
what is phentolamine used for?
phaeochromocytoma induced hypertension (non selective alpha blocker)
42
what is prazosin used for?
adjunctive hypertension treatment (mild hypotensive effects)
43
how does methyldopa work as false transmitter?
converted into a methyl noradrenaline which doesn't stimulate adrenoceptors
44
used for methyldopa
Antihypertensive in: - renal disease - cerebrovascular disease
45
what are beta (b1 selective) blockers used for apart from hypertension
- arrhythmias - angina - glaucoma (reduced beta mediated AH production)
46
types of neuromuscular blocking drugs
- non depolarising blockers (competitive antagonists) | - depolarising blockers (agonists)
47
types of depolarising blockers
- suxamethonium | - decamethonium
48
types on non depolarising blockers
- tubercurarine | - atracurium
49
uses for suxamethonium
depolarising blocker: - Tracheal Intubations - Muscle relaxant for ECT
50
what are tubocurarine based drugs used for
competitive skeletal nAchR antagonist inducing: - flaccid paralysis in surgery - paralyses respiratory muscles hence easy to ventilate under anaesthesia
51
why is atracurium preferred for renal disease patients
chemically unstable at physiological pH hence breaks down into non toxic substances in blood stream naturally in 15 mins.
52
Side effects of adrenaline
``` Palpitations Hypertension Cold extremities Thicker/reduced secretions Arrhythmias Tremor ```
53
What happens when you overdose on adrenaline
Cerebral haemorrhage | Pulmonary oedema
54
a1 agonism
``` Vasoconstriction Relaxation of GIT Dilator pupilae activation Piloerection Constricts internal bladder sphincter ```
55
a2 agonism
Decrease CNS Sympathetic outflow | Decreases SNS actions
56
b1 agonism
Renin secretion Chronotropy Inotropy Relaxation of GIT
57
b2 agonism
Hepatic glucose output Vasodilation Bronchodilation AH formation
58
Side effects for beta blockers
``` Bad dreams Fatigue Cold extremities Heart failure Hypoglycaemia Bronchoconstriction ```
59
Why is atenolol better?
Cardio selective (b1) hence fewer side effects (bronchoconstriction and hypoglycaemia)
60
M1 agonism
Parietal cell secretion Salivary glands CNS
61
M2 agonism
Decreases heart contractility and rate
62
M3 agonism
``` Salivary glands Constrictor pupilae Visceral Smooth muscle contraction Sweat glands Vasodilation Ciliary muscle contraction ```
63
Antimuscarinics side effects
- heat intolerance due to decreased sweating - decreased secretions - cyclopegia (cannot focus) - CNS disturbance
64
Side effects for suxamethonium
Muscle pain from fasciculations Hyperkalaemia Increases IOP Bradycardia
65
Side effects of tubocurarine based drugs
Hypotension Tachycardia Bronchospasm Secretions

Pharmacology (8 decks)

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