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Y2S1 - Drug Action > Drug Action 4 > Flashcards

Drug Action 4 Flashcards

1
Q

What is BRL37344 used to treat?

A

Obesity

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2
Q

What is phenylephrine used to treat?

A

Nasal decongestant

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3
Q

What is clonidine used to treat?

A

Hypertension

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4
Q

What is BRL37344 an agonist of?

A

ADR beta 3

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5
Q

Name one selective agonist for ADR beta 3.

A

BRL37344

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6
Q

What is prazocin used to treat?

A

Hypertension

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7
Q

What is yohimbine used to treat?

A

Erectile dysfunction

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8
Q

What is propanolol used to treat?

A

Angina, cardiac dysrhythmia, hypertension

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9
Q

What receptors regulate NA release?

A

Presynaptic receptors on postganglionic SS varcosities regulate the release of NA

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10
Q

What pre-synaptic neural connection negatively modulates NA synapses?

A

ACh

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11
Q

What pre-synaptic neural connection negatively modulates ACh synapses?

A

NA

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12
Q

What is released from smooth muscle that negatively modulates the NA neuron innervating it?

A

PG

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13
Q

What is released from endothelial cells that negatively modulates the ACh neuron that innervates them?

A

NO

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14
Q

What does NANC stand for?

A

Non-adrenergic, non-cholinergic NT

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15
Q

What NANC NTs are in the ANS?

A

5-HT, ATP, peptides, NO

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16
Q

Name three NANC peptides.

A

VIP, somatostatin, substance-P

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17
Q

What does VIP stand for?

A

Vasoactive intestinal polypeptide

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18
Q

Why can NANC NTs be referred to as co-transmitters?

A

They are released alongside ACh and ADR NTs to modulate the response chemically

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19
Q

What principle does NO break, and why?

A

Dale’s principle - synthesised outside the nerve terminal

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20
Q

What is NO synthesized from?

A

O2 and L-arginine

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21
Q

What synthesises NO?

A

NOS

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22
Q

What does NOS stand for?

A

Nitrogen oxide synthase

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23
Q

What does eNOS stand for?

A

Endothelia

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24
Q

What does nNOS stand for?

A

NANC

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25
Q

Where is eNOS found?

A

Endothelia

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26
Q

Where is nNOS found?

A

NANC nerves

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27
Q

What does activation of NOS result in?

A

Increased cGMP - decreased IC Ca - increased K channel - hyperpolarization - relaxation

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28
Q

What terminates the action of NO?

A

Phosphodiesterase V

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29
Q

How is the action of NO terminated?

A

Break down of cGMP by phosphodiesterase V

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30
Q

How does phosphodiesterase V terminate NO action?

A

Breaks down cGMP

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31
Q

What is the MOA of sildenafil?

A

Selective inhibitor of phosphodiesterase V

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32
Q

What is sildenafil also known as?

A

Viagra

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33
Q

What are the unwanted side effects of sildenafil?

A

Hypotension, flushing, headache, visual disturbance

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34
Q

When was the first compound for migraine treatment discovered?

A

1868

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35
Q

What did the first migraine treatment contain?

A

Ergotamine

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36
Q

What was the first compound for migraine treatment?

A

Ergot

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37
Q

When were the triptans developed?

A

20th Century

38
Q

What is the incidence of migraines?

A

1-2%

39
Q

What are the two clinical sub-types of migraine?

A

With or without aura

40
Q

What is the general treatment strategy for migraines?

A

All patients require acute treatment, frequent attacks require prophylactic pharmacology

41
Q

What is the socioeconomic cost of migraines?

A

Approx EU27 billion in Europe

42
Q

What was the ORIGINAL theory of pathophysiology of migraines?

A

Vasodilation of cranial blood vessels generates pain

43
Q

What is the neurogenic hypothesis of migraines?

A

Neural events increase noxious sensory transmission through trigeminal system, causing pain directly and through neurogenic inflammation

44
Q

What is the brain theory of migraines?

A

Linked to CSD, more likely to occur in migraine with aura, but not without

45
Q

What is CSD?

A

Cortical spreading depression

46
Q

What is CGRP?

A

Calcitonin gene related peptide

47
Q

What is neurogenic inflammation?

A

Activation of trigeminal sensory axons causes release of vasodilatory substances such as CGRP; mast cells activate and release more; blood vessels thus leak fluid; afferents are sensitised thus become hypersensitive to physiological stimuli

48
Q

Where to ergot alkaloids occur naturally?

A

In fungi that infect rye

49
Q

What is the ergot alkaloid MOA?

A

Act mainly on ADR, 5-HT or dopamine receptors

50
Q

What two ergot alkaloids are related to migraine therapy?

A

Ergotamine and methysergide

51
Q

What type of drug is ergotamine?

A

Ergot alkaloid

52
Q

What type of drug is methysergide?

A

Ergot alkaloid

53
Q

What is ergotamine used to treat?

A

Migraine

54
Q

What is methysergide used to treat?

A

Migraine

55
Q

What limits the use of methysergide?

A

Adverse effects

56
Q

What is the MOA of ergotamine?

A

Acts as antagonist and partial agonist at 5-HT-1 receptors, and partial agonist at alpha-ADR

57
Q

What does ergotamine cause?

A

Vasoconstriction and uterine contraction

58
Q

What are the side effects of ergotamine?

A

Emesis, vasospasm and adverse affects during pregnancy

59
Q

What physiological effects implicate 5-HT in the pathogenesis of migraines?

A

Elevated with vasoconstriction, decreased with vasodilation, increased excretion of 5-HT metabolites during migraine, decreased blood levels

60
Q

What pharmacological effects implicate 5-HT in the pathogenesis of migraines?

A

Many drugs that are effective against migraines target 5-HT receptor signalling pathways

61
Q

What are the three 5-HT1 receptors associated with migraines?

A

5-HT1-B/D/F

62
Q

Where are 5-HT1-B receptors found?

A

CNS, vascular smooth muscle and many others

63
Q

Where are 5-HT1-D receptors found?

A

Presynaptic location on peripheral and central trigeminal neurons

64
Q

Where are 5-HT1-F receptors found?

A

Same as 5-HT1-D - presynaptic location on peripheral and central trigeminal neurons

65
Q

What is the signalling function for all 5-HT1 receptors?

A

G-i/o protein - decreased cAMP - possible modulation of Ca channels

66
Q

Name three triptans.

A

Sumatriptan, rizatriptan, zolmitriptan

67
Q

What are the triptans used to treat?

A

Acute migraine attacks

68
Q

What is the MOA for triptans?

A

5-HT1-B/D/F agonists

69
Q

What do triptans cause?

A

Constrict large arteries - decreasing vasodilation and reducing sensory signalling; inhibit trigeminal nerve transmission - decreasing pain signalling and neurogenic inflammation

70
Q

What type of drug is sumatriptan?

A

Triptan

71
Q

What type of drug is rizatriptan?

A

Triptan

72
Q

What type of drug is zolmitriptan?

A

Triptan

73
Q

What receptor does sumatriptan bind?

A

5-HT1-B/D/F

74
Q

What receptor does rizatriptan bind?

A

5-HT1-B/D/F

75
Q

What receptor does zolmitriptan bind?

A

5-HT1-B/D/F

76
Q

What are the side effects of triptans?

A

Coronary vasoconstriction, dysrhythmias, chest pain, neck and jaw pain, muscle pain, CNS effects - functional impairment and reduced productivity

77
Q

What are triptans contra-indicated for?

A

Patients with symptoms of coronary heart disease

78
Q

What may be an alternative approach to treating migraines, other than with triptans?

A

Target neuronal release of pain sensitising neuropeptides such as CGRP - target 5-HT1-F receptors expressed on the trigeminal nerve

79
Q

What type of drug is lasmiditan?

A

Ditan

80
Q

What receptor does lasmiditan bind?

A

5-HT1-F specifically

81
Q

What are the advantages to the ditans?

A

No coronary side effects noted

82
Q

What is the new class of drugs being tested for migraine treatments?

A

Ditans

83
Q

How does lasmiditan act differently to sumatriptan?

A

Sumatriptan = vasoconstriction; lasmiditan = inhibition of neuronal activity

84
Q

What is the preferred drug for migraine related prophylaxis?

A

Propranolol

85
Q

Name four emerging migraine treatments.

A

CGRP receptor antagonists, onabotulinumtoxin, prostanoid receptor antagonism, 5-HT7 receptor antagonism

86
Q

Name two CGRP receptor antagonists.

A

Olcegepant and telcagepant

87
Q

What is the MOA of olcegepant?

A

CGRP receptor antagonist

88
Q

What is the MOA of telcagepant?

A

CGRP receptor antagonist

89
Q

What is olcegepant used to treat?

A

Migraine

90
Q

What is telcagepant used to treat?

A

Migraine

91
Q

What does 5-HT7 receptor antagonism do?

A

Prevents vasodilation in blood vessels in the trigeminal sensory areas

Y2S1 - Drug Action (4 decks)

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