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MODA drugs > 1 - Drug interactions with receptors and ion channels > Flashcards

1 - Drug interactions with receptors and ion channels Flashcards

1
Q

Benzilylcholine mustard

A

Irreversibly alkylates muscarinic receptor

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2
Q

Cholera toxin

A

ADP ribosylation of a(s)
Inhibits GTPase activity
Sustained activation of adenylyl cyclase

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3
Q

Pertussis toxin

A

ADP ribosylation of a(i)

Prevents activation of Gi in response to receptor stimulation

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4
Q

AIF4-

A

Mimics gamma-phosphate of GTP

Causes persistent activation of G proteins

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5
Q

Lithium

A

Uncompetitively inhibits phosphatases converting IP1 to inositol
Blocks inositol recycling

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6
Q

Tyrphostins

A

Inhibitors of tyrosine kinase

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7
Q

Prednisolone

A

Agonist for glucocorticoid receptors

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8
Q

Mifepristone

A

Antagonist for glucocorticoid receptors

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9
Q

Fludrocortisone

A

Agonist for mineralocorticoid receptors

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10
Q

Spironolactone

A

Antagonist for mineralocorticoid receptors

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11
Q

Ethinylestradiol

A

Agonist for estrogen receptor

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12
Q

Tamoxifen

A

Antagonist for estrogen reveptor

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13
Q

Norethisterone

A

Agonist for progestagen receptor

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14
Q

Danazol

A

Antagonist for progestagen receptor

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15
Q

Lidocaine

  • 2 main uses
  • what fibres does it affect?
  • what does it bind to?
  • acid or base?
  • how does it act in different pHs?
A

-Local anaesthetic
Antidysrhythmic agent
-Affects c and Adelta fibres
-Binds preferentially to and stabilises inactivated state (Na channels)
-Weak base
-High ph-greater inhibition, lower potency

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16
Q

Procaine

  • main uses
  • what fibres does it affect?
  • what does it bind to?
A

-Local anaesthetic
Antidysrhythmic agent
-Affects c and Adelta fibres
-Binds preferentially to and stabilises inactivated state (Na channels)

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17
Q

QX314

A

Quaternary local anaesthetic
Ineffective outside axon
Potent LA when perfused inside

18
Q

Benzocaine

A

Local anaesthetic
Uncharged
Extent of block is independent of pH
Faster block - hydrophobic pathway within membrane for uncharged LAs

19
Q

Quinidine

A

Local anaesthetic
Slow in slow out
Use dependence at low rates of stimulation

20
Q

Tetrodotoxin

TTX

A

Guanidinium groups
Block Na channels from outside
Do not show use dependence

21
Q

Bay K 8644

A

Dihydropyridine (DHP)
Calcium agonist
Lipid soluble

22
Q

Nifedipine

A

Dihydropyridine (DHP)
Lipid soluble
Calcium antagonist

23
Q

Verapamil

A 
Ca channel blocker
Bind to site away from DHP binding site 
Site interact, so reduces DHP binding
Use dependence
Prolonged block
Preferentially cardiac muscle
Antidysrhythmics
24
Q

Diltiazem

A 
Ca channel blocker
Bind to site away from DHP binding site 
Site interact, so enhances DHP binding
Use dependence
Prolonged block
Preferentially cardiac muscle
Antidysrhythmics
25
Q

Diazoxide

A

K channel opener
Hyper polarise cell membrane
Relax smooth muscle

26
Q

Minoxidil

A

K channel opener
Hyper polarise cell membrane
Relax smooth muscle

27
Q

Nicorandil

A

K channel opener
Hyper polarise cell membrane
Relax smooth muscle

28
Q

Tolbutamide

How does it work?

A 
Close Katp acting on sulphonylurea receptor
Depolarise pancreatic B cell memb
Fires VGCa channel
Ca influx
Insulin release
29
Q

Glibenclamide

How does it work?

A 
Close Katp acting on sulphonylurea receptor
Depolarise pancreatic B cell memb
Fires VGCa channel
Ca influx
Insulin release
30
Q

Muscarine

A

Agonist for muscarinic receptor on smooth muscle

31
Q

Nicotine

A

Agonist for nicotinic receptor on skeletal muscle

32
Q

Atropine

A

Antagonist for muscarinic receptor on smooth muscle

33
Q

D-tubocurarine

A

Antagonist for nicotinic receptors on skeletal muscle

34
Q

Acetyl-B-methylcholine

A

Cholinergic agonist

Inactive isomer has no affinity

35
Q

Isoprenaline

A

B-adrenoreceptor agonist

Inactive isomer has affinity

36
Q

Adenosine

A

?

37
Q

a bungarotoxin

A

?

38
Q

Lidocaine

  • how does it cross the membrane and block the channel?
  • dependence?
  • what in what out?
A 
-Cross membrane in uncharged form
Blocks channel best in charged form
-Use dependence at high rates of stimulation
Voltage dependence 
-Fast in fast out
39
Q

Procaine

  • acid or base?
  • how does it act in different pHs?
  • how does it cross the membrane and block the receptor?
A

-Weak base
-High ph-greater inhibition, lower potency
-Cross membrane in uncharged form
Blocks channel best in charges form

40
Q

Tolbutamide

What is it and what does it do/treat?

A

Orally acting hypoglycaemic agent
Treat type 2 diabetes
Sulphonylurea

41
Q

Glibenclamide

What is it, what does it do/treat?

A

Orally acting hypoglycaemic agent
Treat type 2 diabetes
Sulphonylurea

MODA drugs (5 decks)

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