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pharmacology 2 > anti emetics > Flashcards

anti emetics Flashcards

1
Q

how and where is emesis controlled?

A

controlled and centralised by brainstem in a nautral network on dorsal surface of medulla - referred to as the “brainstem emetic control centre” or dorsal vagal complex

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2
Q

what is the vomiting reflex regulated by?

A

CNS (medulla)

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3
Q

what is the main site of action for ant-emetic drugs?

A

chemoreceptor triggering zone (CTZ)

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4
Q

what is the CTZ physically associated with?

A

emetic centre

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5
Q

which side of the blood brain barrier is CTZ located?

A

blood side

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6
Q

what is the target for anti-emetic drugs?

A

blockade of neurotransmitters involved in triggering emesis

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7
Q

name the 6 endogenous neurotransmitters involved in triggering emesis

A 
serotonin
AcH
Dopamine
Substance P
Histamine
Enkephalin
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8
Q

name the various pathways involved in stimulating the vomiting centre

A

vestibular pathway
vagal pathway
CTZ and emetic centre

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9
Q

what stimulates the vestibular pathway?

A

disorientating movement

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10
Q

what stimulates the vagal pathway?

A

sensory input (pain, smell, sight, thought)
stimuli from pharynx
stimuli from GI tract

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11
Q

what stimulates the CTZ and emetic centre?

A

endogenous substances
toxins
drugs

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12
Q

name 7 classes of anti emetics

A 
H1 histamine antagonists
muscarinic receptor antagonists
D2 Dopamine antagonists
5HT3 serotonin antagonists
NK1R neurokinin -1 antagonists
cannabinoids
corticosteriods
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13
Q

name 3 H1 (histamine) antagonists

A

cyclizine
cinnarizine
promethazine

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14
Q

what is the mechanism of action of H1 (histamine) antagonists and in which areas to they act ?

A

blocks H1 (histamine) receptors on vestibular pathway and vomiting centre

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15
Q

what are type of emesis are H1 (histamine) antagonists used to treat?

A

cyclizine - motion sickness
cinnarizine - motion / vestibular disorders
promethazine - severe morning sickness

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16
Q

what are the side effects of H1 (histamine) antagonists?

A

drowsiness

sedation (contributes to efficacy)

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17
Q

name 2 muscarinic receptor agonists used as anti-emetics

A

hyoscine

scopolaine

18
Q

what is the mechanism of action of muscarinic receptor agonists and in which areas to they act ?

A

block muscarinic receptors in vestibular pathway and vomiting centre
block neurotransmitter Ach

19
Q

what are type of emesis are muscarinic receptor antagonists used to treat?

A 
general purpose
motion sickness (drug of choice)
20
Q

what are the side effects of muscarinic receptor antagonists?

A

dry mouth
blurred vision
less sedation (than antihistamines)

21
Q

name 5 dopamine antagonists

A 
phenothiazides
prochlorpromine
perphenazine
metaclopromide
domperidone
22
Q

what is the mechanism of action of dopamine anatagonists?

A

block dopamine receptors - strong representation in CTZ

also antagonise M and H receptors

23
Q

what type of emesis are phenothiazides, prochlorpromine and perphenazine used to treat?

A 
uremia
opiod induced emesis
CINV
GI disorders
viral gastro enteritis
24
Q

what are the side effects of phenothiazides, prochlorpromine and perphenazine?

A

sedative
hypotension
dystonia
dykinesia

25
Q

which body system does metaclopromide act on?

A

GIT, increase GI motility

26
Q

what are the side effects of metaclopromide?

A

movement disorders
fatigue
motor restlessness etc.
penetrates BBB

27
Q

what is domperidone used to treat?

A

migraine
cytotoxic induced therapy emesis
emergency contraceptive sickness
does not penetrate BBB - few SE

28
Q

name four 5HT3 serotonin antagonists

A

ondanstron
granistron
palonosetron
tropisetron

29
Q

what is the mechanism of action for 5HT3 serotonin antagonists?

A

blocks serotonin receptors in CTZ, vomiting centre and vagal pathway

30
Q

what is the drug of choice for CINV and PONV?

A

ondanstron

31
Q

what are the side effects of 5HT3 serotonin antagonists?

A

GI disterbances

headache

32
Q

name three NK1R neurokinin-1 antagonists?

A 
aprepitant
fos aprepitant (PRODRUG)
maprepitant
33
Q

what is the mechanism of action for NK1R neurokinin-1 antagonists?

A

antagonists substance P

34
Q

what is NK1R neurokinin-1 antagonists used for?

A

CINV and PONV

35
Q

what are the side effects of NK1R neurokinin-1 antagonists?

A 
fatigue
listlessness
constipation/ diahorrea
loss of appetite
hiccups
36
Q

name 2 cannabinoids

A

nabilone

marinol

37
Q

what is the mechanism of act of cannabinoids?

A

agonist cannabinoid receptors

act via opioid receptors in CTZ

38
Q

what are cannabinoids used to treat?

A

CINV

39
Q

what are the side effects of cannabinoids?

A 
drowsiness
dizziness
dry mouth
mood changes
postural hypotension
40
Q

which corticosteroid is used as an anti-emetic and which type of emesis is it used for?

A

dexamethosone

cytotoxic drugs - used in combo with D2 or 5HT3 antagonist for improved action

pharmacology 2 (11 decks)

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