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Pharmacy Y2- Exam 1 > drugs used in asthma and COPD- anti muscarinic > Flashcards

drugs used in asthma and COPD- anti muscarinic Flashcards

1
Q

which nervous system are muscarinic receptors found?

A

at target organs in the parasympathetic system

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2
Q

what type of receptors are muscarinic receptors? what neurotransmitter activates them?

A

G-protein coupled receptors activated by acetylcholine

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3
Q

how many types of muscarinic receptors are there?

A

5

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4
Q

what does the M1 muscarinic receptor do?

A
  • know as neural and mainly found in CNS
  • signal via the Gq G-protein signal via IP3/Ca2+, increases the second messenger Ca2+ in the cell and inhibition of K+ channels
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5
Q

what does the M2 muscarinic receptor do?

A

-mainly in the heart

causes decrease in cAMP and activation of K+ channels works via Gi G-protein

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6
Q

what does the M3 muscarinic receptor do?

A
  • found mainy in glands and smooth muscles

- stimulates the Gq and also increases IP3 therfore Ca2+ increases

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7
Q

what does the M4/5 muscarinic receptor do?

A

found mostly in the CNS

  • M4 stimulates Gi decrease in cAMP and activation of K+ channels
  • M5 stimulates the Gq and also increases IP3 therfore Ca2+ increases
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8
Q

what will happen if an drug agonists binds to a muscarinic receptor?

A

it will activate all the M1-5 recepetors

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9
Q

what are drugs that are agonists muscarinic receptors are termed?

A

parasympathomimetics

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10
Q

what are drugs that are antagonists muscarinic receptors are termed?

A

parasympatholtics due to their inhibition

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11
Q

what is xanomeline?

A

it is a M1 muscarnic sub-type receptor developed for alzeheimers but had bad side effects

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12
Q

what is cevimeline?

A

is selective for M3 used for sjogren sydndrome, but not license in the UK

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13
Q

what are some effects of muscarinic agonist on the cardiovascular?

A
  • decrease cardiac output
  • increase of NO causing vasodilaton
  • decrease blood pressure
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14
Q

what are some effects of muscarinic agonist on the smooth muscle?

A
  • causes contraction of smooth muscle
  • increase peristaltic activity
  • bladder contraction
  • constriction of bronchioles
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15
Q

whats the main clinical use of muscarinic agonists to treat?

A
  • treat glaucoma using the agonist pilocarpine

- treat urinary retention using the agonist bethanecol but have a lot of side effects

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16
Q

what is the main muscarinic antagonist?

A

atropine, non-selective cant distinguish between M1-5 but can between muscarinic and nicotinic receptors

17
Q

what are some other muscarinic anatagonists?

A
  • tiotropium and ipratropium
  • hyoscine
  • tropicamide
  • pirenzepine
  • darifenacin
18
Q

what are some effects of muscarinic antagonist on the cardiovascular system?

A
  • tachycardia, increase HR

- blood pressure unchanged

19
Q

what are some effects of muscarinic antagonist on the smooth muscle?

A
  • GIT mobility inhibited
  • urinary tract relaxation, prevents bladder emptying
  • bronchial relaxation
20
Q

what are some clinical uses of muscarinic antagonists?

A

used for asthma and airways disease dilation

motion sickness

21
Q

what are some side effects of muscarinc antagonists?

A 
dry mouth
dry skin
constipation
tachycardia
urinary urgency and retention
22
Q

what nervous system controls broncial smooth muscle contraction?

A

autonomic

23
Q

what sub NS controls bronchodilation?

A

sympathetic

24
Q

what sub NS controls bronchoconstriction?

A

parasympathetic

25
Q

what nerve is stimulated that mediates the effects?

A

vagus

26
Q

how does the pathway for nerve stimulation lead to contraction of smooth muscle in bronchiole?

A
  • vagus nerve is stimulates the post ganglionic neuron
  • then acytlcholine is released
  • which then acts on muscarinic receptors M1/3 on bronchial smooth muscle
  • then contraction occurs
27
Q

how does an agonist cause the constriction of smooth muscle in the bronchi?

A

an agonist like methacholine acts on receptors to cause constriction

28
Q

how does an antagonist prevent the constriction of smooth muscle in the bronchi?

A

antagonist such as ipratropium bromide would block acytlcholine from binding as it would bind its self so contracton is inhibited and bronchodilation would occur

29
Q

what does an agonist do to the control of bronchial smooth muscles?

A

causes constriction

30
Q

what does an antagonist do to control of bronchial smooth muscle?

A

causes dilation

31
Q

what are some of the uses of muscarinic antagonists in COPD and asthma?

A
  • they are non-selective (anti muscarinic)
  • tiotropium is long acting
  • they are poorely absorbed as they are charged so used as inhalation so less systemic action to cause side effects
32
Q

what commonly used muscarinic antagonists are used for COPD and asthma

A

ipratropium and tiotropium

33
Q

which anti-muscarinic is short acting?

A

iprattropium bromide

34
Q

what are some key infor about ipratropium?

A
  • brand name is Atrovent
  • used for airway obstruction, broncho spasum and acute life threatening asthma
  • maximum effect in 30mins
  • duration of 3-6hrs
  • 3/4 doses =adequate bronchodilation for the -day
35
Q

what are some key infor for tiotropium?

A

-brand name is Spiriva
-once daily
hand inhaler only for COPD and respimat inhaler for asthma and COPD
-

36
Q

why may patients experience adverse effects?

A

as they are non selective they’ll block on all muscarinic receptors. if given inhalation form they’ll reduce effects

37
Q

where are anti-muscarincic used for in guidlines?

A

barely used for asthma

38
Q

what are the key things to consider when designing a drug from a natural ligand?

A
  • identify types of interaction and structural features
  • structure activity relation
  • identify a pharmacophore
39
Q

why is acytlcholine not got a drug structure?

A

not selective works at both nicotinic and muscarinic

Pharmacy Y2- Exam 1 (13 decks)

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