Anti-Emetics Flashcards

1
Q

What stimulates Nausea and vomiting?

A
  • Toxins: Bacterial poisons, alcohol (15%)
  • Smells
  • Motion sickness
  • Migraine
  • Pregnancy
  • Drugs
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2
Q

What is the physiological response of Vomiting and Nausea?

A
  1. Discomfort, dry mouh, salivary inhibition
  2. Yawning-sympathetic distress
  3. Reappearence of saliva
  4. Pylorus closes
  5. Tone of stomach increase
  6. Deep breath
  7. Contraction of abdominal muscle to force out food
  8. Forced expiration to prev inhalation
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3
Q

What NT are involved in Nausea and vomiting?

A
  • Histamine
  • Acetylcholine
  • Dopamine
  • 5-HT
  • Neurokinin
  • Blocking these receptors in the brain prevents nausea and vomiting
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4
Q

What is the vomit centre of the brain?

A
  • Located within medulla
  • Recieves afferent signals from vagus nerve and CTZ
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5
Q

What receptors are important for vomiting?

A
  • 3 receptors abundant in the chemoreceptor trigger zone (CTZ)
  • BLocking these is important for prev vomiting
  1. D2
  2. 5-HT3
  3. NK-1
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6
Q

What are the 4 main pathways?

A
  1. Chemoreceptor trigger zone (CTZ)
  2. Vagal afferent nerve fibres from GIT
  3. Central vestibular nuclei
  4. Higher centres of brain
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7
Q

What is the chemoreceptor zone(CTZ)?

A
  • Outside BBB
  • REceptors 5-HT3, D2 and NK1 (substance P)
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8
Q

What is motion sickness?

A
  • Afferents from inner ear (vestibulo-cochlear system) feed into vomiting centre
  • Mediated by acetlycholine and histamine
  • Inner ear infections can also cause motion sickness
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9
Q

How does chemotherapy induce nausea?

A
  • Some chemotherapy agents stimulate release of 5-HT from enterochromaffin cells in GIT
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10
Q

What are Histamine H1 receptor antagonists work?

A
  • Motion sickness
  • Morning sickness of pregnancy
  • Space motion sickness
  • Anti-muscarininc actions
  • Produce drowsiness and sedation

(Block receptor in Vestibular nuclei see PP)

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11
Q

What are Muscarinic M1 receptor antagonists?

A
  • Prophylaxis and treatment of motion sickness
  • Also reduce gastic motility
  • Anti-muscarinic side effects
  • Produce drowsiness
  • Naturally occuring foundin Atropa belladona
  • Block receptor in Vestibular nuclei (See pp)
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12
Q

What is the Reflex mechanism of vomiting?

A
  1. Central regulation of vomiting occurs in the vomiting cntre and the CTZ
    (CTZ sensitive to chemical stimuli–main site of anti-emetics)
  2. Output from CTZ stimulates the vomiting centre, leading to initiation of vomitin
  3. Neuronal signals from GI tract feed into CTZ and vomiting centre
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13
Q

What is the Vomiting protective reflex?

A
  1. Chemoreceptors in GIT activated by toxins–
  2. effect vagal nerves–
  3. feed into nucleus tractus solitarius and in turn, vomiting centre
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14
Q

What are Dopamine D2 receptor antagonists?

A
  • Act in CTZ but has unwanted CNS effects
  • D2 receptor inv in movt
  • Antagonism leads to parkinson’s like symptoms
  • Effective against chemotherapy-induced emesis
  • Also stimulates gastric emptying and reduce nausea
  • Works in CTZ on D2 receptor
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15
Q

What are 5-HT receptor antagonists?

A
  • Blocks 5-HT at 5-HT3 receptors in gut and CNS
  • Particularly effective against chemotherapy-induced emesis
  • Not effective for motion sickness
  • Work in GIT and CTZ (See pp)
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16
Q

What are Neurokinin (NK1) receptor antagonists?

A
  • NK1 receptor activated by substance P
  • NK1 receptor antagonists suppress nausea and vomiting
  • Used in chemotherapy-inuced N&V in combo with 5-HT receptor antagonist
  • Work on NK1 receptors in CTZ an GIT
17
Q

What are seroids used for in N&V?

A
  • Used in chemotherapy-induced N&V
  • Mechanism unknown
18
Q

What is Apomprohine?

A
  • Metabolite of morphine
  • No effect on opiod receptors
  • Non-selective dopamine receptor agonist
  • Used as emetic in veterinary medicine
  • Also used to treat Parkinson’s disease
19
Q

Summarise N&V.

A
  • N&V regulated by CNS
  • Response to signals from periphery
  • Number of NTs involved
  • Chemotherapy-induced N&V controlled using 5-HT3 and NK1 receptor antagonist along with a steroid