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CPT > Antiemetics > Flashcards

Antiemetics Flashcards

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1
Q

What is emesis?

A

Involuntary,forceful expulsion of gastric contents through the mouth

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2
Q

Process of vomiting

A
  • coordinated by vomiting centre in medulla
  • take a deep breath
  • glottis closes
  • abdominal muscles contract
  • lower oesophageal sphincter relaxes
  • retrograde peristalsis of small bowels
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3
Q

What is vomiting coordinated by?

A

Vomiting centre in medulla

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4
Q

Neurological pathway of vomiting

A
  • When the vomiting centre in the medulla is stimulated the vomiting reflex occurs
  • motion + morning sickness trigger the vestibular centre > CTZ > vomiting centre
  • cytotoxic agents trigger the CTZ > vomiting centre
  • high cortical centre in brain can be triggered by pain, emotion or repulsive sights/smells > vomiting centre
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5
Q

What receptors are found in the vomiting centre

A
  • NK1
  • Muscarinic Ach
  • H1 - histamine
  • 5HT2 - serotonin receptor
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6
Q

Stimuli for the higher cortical centre of nausea

A
  • Pain
  • Repulsive sights + smells
  • Emotional factors e.g. stress
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7
Q

Management of nausea due to stimuli from higher cortical centre

A

Conservative management - avoid stimulus

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8
Q

What portion of the brain is involved in motion sickness?

A

Vestibular nuclei
Due to inputs from the labyrinth centre
Act on NK1, Muscarinic Ach, H1 + 5HT2

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9
Q

What receptors are in the vestibular nuceli?

A

Muscarinic Ach
H1

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10
Q

What receptor is in the higher cortical centres?

A

GABA

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11
Q

Example of Muscarinic antagonists

A

Hyoscine hydrobromide

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12
Q

What is the mechanism of action of Muscarinic antagonists?

A

Competitive blockage of Muscarinic acetylcholine receptors - act on vestibular nuclei

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13
Q

What are adverse drug reactions of muscarinic antagonists?

A

Sedation
Consiptiaon
Dizziness
Dry mouth
Visual problems
Confusion

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14
Q

What are contraindications of muscarinic antagonists?

A

Elderly patients
Glaucoma

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15
Q

What are important drug drug interactions of Muscarinic antagonists?

A

Anti-psychotic meds

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16
Q

Examples of H1 antagonists

A

Cycilzine
Levomepromazine
Prochlorperazine
Promethazine

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17
Q

What are uses of H1 antagonist?

A

Motion sickness
Promethazine - morning sickness in pregnancy

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18
Q

What is the mechanism of action of H1 antagonists in treatment of vomiting?

A
  • Works centrally
  • Acts on vomiting centre + vestibular nuclei
  • inhibits histaminergic signals from vestibular system to CTZ in medulla
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19
Q

What are adverse drug reactions of H1 antagonists?

A

Sedation
Dry mouth
Constipation
Urinary retention
Blurred vision

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20
Q

What are contraindications of H1 antagonists?

A

Epilepsy
Urinary retention
Children + elderly
Glaucoma

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21
Q

Who is motion sickness more common?

A

Women
Children
People who have migraines

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22
Q

Prevention of motion sickness

A

Hydration
Position in vehicle
Distraction

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23
Q

What 2 classes of drugs are used in the treatment of motion sickness?/
Examples of each

A
  • Anti muscarinics e.g. hyoscine hydrobromide
  • anti histamines e.g. cyclizine, propchlorperazine
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24
Q

What affects the chemotherapy trigger zone?

A
  • inputs from vestibular centre
  • cytotoxic agents e.g. chemotherapy
  • vagal afferents
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25
Q

What are the receptors of the chemotherapy trigger zone?

A

NK1
D2 - dopamine
5HT3 - serotonin

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26
Q

Examples of dopamine D2 receptor antagonist

A

Metoclopramide
Domperidone
Haloperidol
Prochlorperazine

27
Q

What class of drug is metoclopramide?

A

D2 dopamine receptor antagonist
5HT3 antagonist

28
Q

What are the uses of metoclopramide?

A

GORD
Anti-emetic for chemotherapy patients
Ileus

29
Q

What is the mechanism of action of metoclopramide?

A
  • Blocks D2 dopamine receptors +5HT3 serotonin receptors
  • acts on visceral afferent in gut > increases Ach in gut > promotes gastric emptying + peristalsis
30
Q

What are adverse drug reactions of metoclopramide?

A

Depression
Diarrhoea
Drowsiness
Hypotension
Galatorrhoea
Parkinsonism
Dsytonia

31
Q

What class of drug is domperidone?

A

D2 dopamine antagonists

32
Q

What is a use of domperidone?

A

Improving lactation in breastfeeding mothers
Anti-emetic

33
Q

What is the mechanism of action of domperidone?

A
  • blocks D2 receptors
34
Q

What are adverse drug reactions of domperidone?

A
  • Dry mouth
  • sudden cardiac death (long QT + VT)
  • galactorrhea
  • loss of libido
35
Q

Examples of D2 receptors antagonists which work as anti-psychotics

A

Haloperidol
Chloropromazine
Prochlorperazine

36
Q

What are the uses of haloperidol?

A

Post op N+V
Anti-psychotic

37
Q

What is the mechanism of action of haloperidol?

A

Post synaptic D2 receptors antagonism

38
Q

What are adverse drug reactions of haloperidol?

A

Parkinsonism
Arrhythmia
Constipation
Dry mouth

39
Q

What receptors do the ‘zines’ work on?

A

Block H1, D2 + muscarinics receptors

40
Q

Examples of neurokinin-1 receptor antagonists
What is the suffix?

A

Aprepitant
Fosaprepitant
Netupitant
-pitant

41
Q

What are the uses of neurokinin-1 receptor antagonists

A
  • Chemotherapy - delayed emesis
  • anxiolytics
  • antidepressants - boost 5HT3 receptor antagonists effects
42
Q

What are adverse drug reactions of NK-1 receptor antagonists

A

Constipation
Headache
Asthenia

43
Q

What is asthenia?

A

a condition in which the body lacks strength or has lost strength, either as a whole or in any of its parts

44
Q

Examples of corticosteroids used as antiemetics

A

Dexamethasone
Methylprednisolone

45
Q

What are the uses of dexamethasone + methylprednisolone as antiemetics?

A

Perioperative N+V
Chemotherapy N+V
Palliation N+V

46
Q

Where do corticosteroids act on when working as antiemetics?

A

Chemoreceptor trigger zone

47
Q

What are adverse effect of corticosteroids?

A
  • Insomnia
  • osteoporosis
  • weight gain
  • increased appetite
  • increased blood sugar
  • Cushing’s syndrome
48
Q

Example of canabinoids

A

Nabilone

49
Q

Where do canabinoids act when working as antiemetics?

A

Chemoreceptor trigger zone

50
Q

What are adverse drug reactions of cannabinoids?

A

Confusion
Depression
Drowsiness + dizziness
Movement disorders
Psychosis
Tremor

51
Q

Management of pregnancy induced vomiting

A
  • fluid replacement
  • antihistamines e.g. Promethazine/cyclizine
  • odanestron
  • Prochlorperazine
  • thiamine replacement
52
Q

What class do drugs are effective for delayed nausea in chemotherapy?

A

Dopamine antagonists e.g. metoclopramide

53
Q

What class do drug is given to cover acute emetic stimulus of chemotherapy?

A

5-HT3 antagonists e.g. ondansetron

54
Q

Examples of 5HT3 antagonists

A

Ondansetron
Granisetron
Palonestron

55
Q

What are the uses of 5HT3 antagonists?

A

Antiemetics in chemotherapy patietns
Post op N+V

56
Q

What is the mechanism of action of 5-HT3 antagonists?

A
  • blocks serotonin receptors
  • Centrally: inhibit chemoreceptor trigger zone
  • Peripherally: reduce GI motility + secretions
57
Q

What are adverse drug reactions of 5-HT3 antagonists?

A
  • Uncommon
  • constipation
  • headache
  • elevated liver enzymes
  • long QT syndrome
  • Parkinsonism
  • dsytonia
58
Q

Outline serotonin production in the GI system

A

Enterochromaffin cells in response to parasympathetic stimulation

59
Q

Action of serotonin on the GI system

A
  • regulates appetite
  • increases gut secretions
  • smooth muscle contraction increases motility
60
Q

What drug is first line for bowel obstruction?
What class is it?

A

Cyclizine
H1 receptor antagonist

61
Q

What are extra pyramidal side effects?

A
  • hyperprolactinaemia side effects
  • dystonia
  • Parkinsonianism
62
Q

What are anticholinergic side effects?

A

Alice in Wonderland:
- bind as a bat: mydriasis
- mad as a hater: confusion
- red as a beet: flushed skin
- hot as a desert: hyperthermia
- dry as a bone: urinary retention + dry mouth
- tachycardia
- absent bowel sounds

63
Q

What is the mechanism of action of NK-1 receptor antagonists?

A
  • prevents action of substance P at CTZ and in peripheral nerves
  • boosts effect of 5HT3 receptor antagonists
  • anxiolytic + antidepressant properties

CPT (29 decks)

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