L4 Therapeutics for Nausea and Vomiting Flashcards

1
Q

Vomiting is stimulated by the vomiting center of the _______________!

  • ____________________ (motion sickness)
  • ____________________(anticipatory/psychogenic)
A

Vomitting is stimulated by the vomiting center of medulla oblongata!!

  • Vestibular apparatus (motion sickness)
  • Cerebral cortex (anticipatory/psychogenic)
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2
Q

________________: suited for anticipatory Emesis (relaxes patient relieving psychological causes)

________________: Suited for Delayed emesis

A

Benzodiazepine: suited for anticipatory Emesis (relaxes patient relieving psychological causes)

Dexamethasone: Suited for Delayed emesis

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3
Q

Central vs. Peripheral inducers of emesis in Chemotherapy?

A

Central: Chemoreceptor Trigger Zone (CTZ) sits outside blood Brain barrier => activates Vomiting Center (Medulla Oblingata)

Peripheral: Serotonin (5HT) released from enterochromaffin cells in the gut

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4
Q

Receptors Regulating Nausea and Vomiting?

A

ACh (Hystocine Targets)

H1 - histamine (Cyclyzine/Promethazine Target)

5HT2 - serotonin (Ondansetron)

Dopamine (Metoclopramide, Domperidone, Haloperidol)

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5
Q

Anticholinergic Antiemetics

Drug(s)?

MOA?

Indication?

Side Effects?

A

Hyocine: Inhibits muscarinic neurotransmission to the vomiting center from Vestibular centers and Gut

Used For:

  • Motion Sickness
  • Post Operative Nausea and vomiting (PONV)
  • Inhibition of saliva pre-operatively

Side Effects: Drowsiness, Dry mouth, Urinary retention, Blurred vison/Dilated pupils

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6
Q

Anti-Histamine Antiemetics

Drug(s)?

MOA?

Indication?

Side Effects?

A

Cyclizine: FIRST LINE for Drug-induced Vomiting and PONV

Promethazine: FIRST LINE IN PREGNANCY

MOA: Block H1 Receptor (Promethazine also Muscarinic + 5HT)

Side Effects:

  • Sedation (esp Promethazine as it can pass BBB)
  • Antimuscarinic => dry mouth, urinary retention
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7
Q

Dopamine Antiemetics

Drug(s)?

MOA?

Indication?

Side Effects?

A

Phenothiazines_ : Prochlorperazine, Perphenazine
Butyrophenone: Haloperidol
Benzamides: Metoclopramide, Domperidone

MOA: Non-Selective dopamine antagonists block Receptors abundant throughout the Chemoreceptor trigger zone (CTZ) and Vomiting Center

Indication: Most effective against Sevre N/V caused by direct stimulation of CTZ

Side Effects

  • Prokinetic: gets GI tract moving => less bloating/stagnation can alleviate a lot of nausea/emesis
  • Dopamine blockers => Parkinson like symptoms + Can lactate
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8
Q

5-HT Antagonists

Drug(s)?

MOA?

Indication?

Side Effects?

A

(-setron): Ondansetron; Granisetron; Palonosetron

MOA: Blocks 5-HT3 receptors in gut, CTZ and vomiting center: Free radicals cause the release of large amounts of 5-HT from gastric enterochromaffin cells

Indication: FIRST LINE FOR CHEMOTHERAPY. Also Prophylactically when vomiting is dangerous

Side Effects Ondansetron prolongs Q-T interval (risky if underlying arrhythmia)

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9
Q

Neurokokini-1 Antagonists

Drug(s)?

MOA?

Indication?

Side Effects?

A

(-itant): Aprepitant, Fosaprepitant, Rolapitant

MOA: Inhibit action of neurokinin at NK1 receptor

Indication: Used in conjunction w/ 5HT antagonists and steroids to augments effects of 5-HT3 antagonists and steroid in preventing (NOT TREATNG) Cisplatin (chemo-drug) induced emesis

_Side Effects: Hiccups, Anorexia, Extensive drug interactions

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10
Q

Corticosteroids for Nassau/Vomitting

Drug(s)?

MOA?

Indication?

A

(-asone): Dexamethasone and Prednisolone

MOA: Exert weak anti-emetics but produce synergistic effects with 5HT3 antagonists (Ondansetron) or Dopamine Antagnonist (Metoclopramide)

Indication: Suited for Delayed N/V. Dexamethasone given iv prior to chemo

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11
Q

Benzodiazepines

Drug(s)?

MOA?

Indication?

A

(-epam): Lorazepam, Diazepam

Suited for ANTICIPATORY N/V

  • produces amnesia & sedation
  • relaxes patient relieving psychological causes
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12
Q

ALL antiemetics have a more pronounced effect on ________ than ________

A

ALL DRUGS have a more pronounced effect on vomiting than nausea

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13
Q

Drug choice for motion sickness?

A

Hyoscine (Anti ACh)

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14
Q

Drug choice for Post-Operative Nausea and Vomiting (PONV)?

A

Cyclizine (Anti Histamine)

Hyocine (Anti-ACh)

Metoclopramide/Domperidone/Prochlorophernazine (Dopamine Antagonists)

Ondansetron (5HT3 Antagonist)

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15
Q

Drug choice for Drug-Induced Vomiting?

A

Cyclizine (esp. for opioid-induced vomiting)

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16
Q

Drug choice for Chemotherapy?

A

Ondansetron (5HT3 Antagonist)

Neurokokini-1 Antagonists (-itant)

Also: Prochlorperazine (Dopamine Antagonist), Nabilone ± Dexamethatome/Benzodiazepines

17
Q

Drug choice for pregnancy-induced vomiting?

A

Promethazine: Antihistamine that blocks H1 Receptors (also muscarinic and 5HT)