Antiemetics, Decontamination Agents and IBD Tx Flashcards

1
Q

Define nausea

A

an unpleasant sensory experience of gastric discomfort with an urge to vomit

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2
Q

Nausea is associated with _____ gastric motility and ____ tone in the small intestine (manifesting as reverse peristalsis)

A

decreased; increased

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3
Q

Define retching

A

spasmodic respiratory movements conducted with a closed glottis

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4
Q

simultaneous contraction of antrum of the stomach and relaxation of fundus and cardia; repeated herniation of the abdominal esophagus and cardia into the thoracic cavity due to negative pressure

A

Retching

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5
Q

Emesis

A

Gastric and small intestinal contents are propelled up to and out of the mouth

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6
Q

Central emetic stimuli

A

Fear, anticipation, memory

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7
Q

Traditional sensory emetic stimuli

A

nociception, olfaction, vision, inner ear

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8
Q

GI sensory emetic stimuli

A

stimulate the pharyngeal and gut chemo/mechanoreceptors - Cytotoxic drugs, radiation, bacteria and viruses

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9
Q

Blood born emetics

A

stimulate the CTZ

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10
Q

The two CNS centers involved in emesis

A
  1. CTZ

2. Vomiting centre

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11
Q

First stage of emesis

A

preparatory movements to protect the airway (deep breath, close glottis, raise larynx, elevate soft palate)

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12
Q

Second stage of Emesis

A

diaphragm contracts downwards to create negative pressure thorax (open LES)
Abdominal walls contract to elevate intragastric pressure

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13
Q

Third stage of emesis

A

stomach and intestinal contents move into the esophagus

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14
Q

Is the CTZ inside or outside of the BBB?

A

Outside - makes a big difference in therapeutic targets

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15
Q

Where is the CTZ located?

A

Outside the BBB in the area postrema

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16
Q

Where is the vomiting centre located?

A

Medullary reticular formation

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17
Q

Name some 5HT3 antagonists

A

Dolasetron
Granisetron
Ondansetron
Palonosetron

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18
Q

MOA of 5HT3 antagonists?

A

Blockade of peripheral 5HT3 receptors on intestinal vagal afferents

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19
Q

Therapeutic use of 5HT3 antagonists?

A

Primary agents for prevention and treatment of chemo induced nausea and vomiting

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20
Q

What is the number one drug prescribed in the ER

A

Ondansetron

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21
Q

SE of 5HT3 antagonists?

A

Usually tolerated well - mild headache, dizziness, constipation.
Prolonged QT interval

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22
Q
Droperidol
Metoclopramide
Phenothiazine
Prochlorperazine
Promethazine
A

D2 antagonists

23
Q

MOA of D2 antagonists

A

Blockade of D2 (and muscarinic) receptors in the CTZ
May counteract reverse peristalsis
SEDATION

24
Q

Therapeutic uses of D2 antagonists

A

Vomiting due to uremia, radiation sickness, cancer chemo, infection, hyperemesis gravidarum, labour

25
Q

SE of D2 antagonists

A

Somnolence, Dystonia, Parkinsonism, tardive dyskinesia (irreversible)
Prolactin release

26
Q

Anti muscarinic agent

A

Scopalamine

27
Q

MOA of scopalamine

A

Blockade of muscarinic and dopaminergic receptors in the cerebellum

28
Q

Therapeutic use for scopalamine

A

Motion sickness

29
Q

Name some H1 antihistamines

A

dimenhydrinate, diphenhydramine, meclizine

30
Q

MOA of H1 antihistamines

A

Block H1 and muscarinic receptors in the cerebellum

31
Q

Therapeutic use of H1 antihistamines

A

motion sickness

hyperemesis gravidarum

32
Q

SE of H1 antihistamines

A

Somnolence

Anticholinergic

33
Q

Name NK1 antagonist

A

Aprepitant/Fosaprepitant

34
Q

MOA of NK1 antagonists

A

Blockade of neurokinin (tachykinin) receptor 1 (intrinsic against substance P) in CNS and GI tract

35
Q

What is the difference of aprepitant and fosaprepitant

A

Aprepitant (oral)

Fosaprepitant (IV)

36
Q

Therapeutic uses

A

Prevention of acute and delayed phases of chemo induced nausea and vomiting

37
Q

What is a NK1 antagonist combined with

A

5HT3 antagonist and dexamethasone

38
Q

Cannabinoids

A

Dronabinol
Nabilone
Medical Marijuana

39
Q

MOA of Cannabinoids

A

Activation of central cannabinoid receptors in CNS

40
Q

Therapeutic use of cannabinoids

A

Cancer chemo induced nausea nad vomiting

41
Q

Dexamethasone

A

Corticosteroid

42
Q

Whole bowel irrigation =

A

polyethelene glycol

43
Q

PEG-electrolyte MOA

A

Osmotic cathartic before endoscopic procedures - not absorbed and increases H20 retention in the lumen

44
Q

How do the anti-inflammatory agents aminosalicylates work?

A

Variants of mesalamine (5-ASA) which are poorly absorbed in the GI tract - block PG synthesis by inhibiting COX and reduce inflammation

45
Q

Balsalazide and sulfasalazine MOA

A

some moiety to 5-ASA - limit action until bacteria break down and release the 5-ASA
Topical rather than systemic
High concentration or enema/suppository

46
Q

Balsalazide nad sulfasalazine are confined to this region

A

Large intestine

47
Q

Name three anti TNFa antibodies

A

Adalimumab
Certolizumab
Infliximab

48
Q

MOA of TNFa antibodies

A

INFLIXIMABandADALMUMABareantibodies that bind to both soluble and receptor-bound TNFα, preventing binding of the cytokine to its receptors

49
Q

MOA of certolizumab

A

is a recombinant antibody consisting of an Fab component conjugated to polyethylene glycol (PEG) i.e., there is no Fc component, therefore no complement activation etc.

50
Q

SE of TNFa abs.

A

infection, reactivation of TB, delayed infusion rxns.

hepatic reactions, increased risk of T cell lymphoma?

51
Q

Anti a4 subunit of integrin

A

Natalizumab

52
Q

MOA of Natalizumab

A

inhibits diapedesis

53
Q

Therapeutics of Natalizumab

A

MS

IBD

54
Q

SE of Natalizumab

A

Reactivation of JC virus

PML