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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
What are the receptors of the chemotherapy trigger zone?
NK1 D2 - dopamine 5HT3 - serotonin
26
Examples of dopamine D2 receptor antagonist
Metoclopramide Domperidone Haloperidol Prochlorperazine
27
What class of drug is metoclopramide?
D2 dopamine receptor antagonist 5HT3 antagonist
28
What are the uses of metoclopramide?
GORD Anti-emetic for chemotherapy patients Ileus
29
What is the mechanism of action of metoclopramide?
- Blocks D2 dopamine receptors +5HT3 serotonin receptors - acts on visceral afferent in gut > increases Ach in gut > promotes gastric emptying + peristalsis
30
What are adverse drug reactions of metoclopramide?
Depression Diarrhoea Drowsiness Hypotension Galatorrhoea Parkinsonism Dsytonia
31
What class of drug is domperidone?
D2 dopamine antagonists
32
What is a use of domperidone?
Improving lactation in breastfeeding mothers Anti-emetic
33
What is the mechanism of action of domperidone?
- blocks D2 receptors
34
What are adverse drug reactions of domperidone?
- Dry mouth - sudden cardiac death (long QT + VT) - galactorrhea - loss of libido
35
Examples of D2 receptors antagonists which work as anti-psychotics
Haloperidol Chloropromazine Prochlorperazine
36
What are the uses of haloperidol?
Post op N+V Anti-psychotic
37
What is the mechanism of action of haloperidol?
Post synaptic D2 receptors antagonism
38
What are adverse drug reactions of haloperidol?
Parkinsonism Arrhythmia Constipation Dry mouth
39
What receptors do the ‘zines’ work on?
Block H1, D2 + muscarinics receptors
40
Examples of neurokinin-1 receptor antagonists What is the suffix?
Aprepitant Fosaprepitant Netupitant -pitant
41
What are the uses of neurokinin-1 receptor antagonists
- Chemotherapy - delayed emesis - anxiolytics - antidepressants - boost 5HT3 receptor antagonists effects
42
What are adverse drug reactions of NK-1 receptor antagonists
Constipation Headache Asthenia
43
What is asthenia?
a condition in which the body lacks strength or has lost strength, either as a whole or in any of its parts
44
Examples of corticosteroids used as antiemetics
Dexamethasone Methylprednisolone
45
What are the uses of dexamethasone + methylprednisolone as antiemetics?
Perioperative N+V Chemotherapy N+V Palliation N+V
46
Where do corticosteroids act on when working as antiemetics?
Chemoreceptor trigger zone
47
What are adverse effect of corticosteroids?
- Insomnia - osteoporosis - weight gain - increased appetite - increased blood sugar - Cushing’s syndrome
48
Example of canabinoids
Nabilone
49
Where do canabinoids act when working as antiemetics?
Chemoreceptor trigger zone
50
What are adverse drug reactions of cannabinoids?
Confusion Depression Drowsiness + dizziness Movement disorders Psychosis Tremor
51
Management of pregnancy induced vomiting
- fluid replacement - antihistamines *e.g. Promethazine/cyclizine* - odanestron - Prochlorperazine - thiamine replacement
52
What class do drugs are effective for delayed nausea in chemotherapy?
Dopamine antagonists *e.g. metoclopramide*
53
What class do drug is given to cover acute emetic stimulus of chemotherapy?
5-HT3 antagonists *e.g. ondansetron*
54
Examples of 5HT3 antagonists
Ondansetron Granisetron Palonestron
55
What are the uses of 5HT3 antagonists?
Antiemetics in chemotherapy patietns Post op N+V
56
What is the mechanism of action of 5-HT3 antagonists?
- blocks serotonin receptors - Centrally: inhibit chemoreceptor trigger zone - Peripherally: reduce GI motility + secretions
57
What are adverse drug reactions of 5-HT3 antagonists?
- Uncommon - constipation - headache - elevated liver enzymes - long QT syndrome - Parkinsonism - dsytonia
58
Outline serotonin production in the GI system
Enterochromaffin cells in response to parasympathetic stimulation
59
Action of serotonin on the GI system
- regulates appetite - increases gut secretions - smooth muscle contraction increases motility
60
What drug is first line for bowel obstruction? What class is it?
Cyclizine H1 receptor antagonist
61
What are extra pyramidal side effects?
- hyperprolactinaemia side effects - dystonia - Parkinsonianism
62
What are anticholinergic side effects?
**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
What is the mechanism of action of NK-1 receptor antagonists?
- prevents action of substance P at CTZ and in peripheral nerves - boosts effect of 5HT3 receptor antagonists - anxiolytic + antidepressant properties

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