Anti Emetic & Motility Flashcards

1
Q

Vomiting center location

A

Ill-defined

In the medulla oblongata, consists of tractus solitarius and parts of reticular formation

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2
Q

Neurotransmitters involved in NV

A

Substance P
Acetylcholine
Y-aminobutyric acid
Cannabinoids
Serotonin
Dopamine

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3
Q

Chemoreceptor trigger zone

A

Highly vascular

Lacks true blood brain barrier-direct stimulation of circulating toxins

Communicates with vomiting center via D2 and 5-HT3 receptors

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4
Q

PONV factors

A

Women/non-smokers/hx of motion sickness

Length of procedure/type of procedure

Inhaled anesthetics, nitrous, opioids, neostigmine

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5
Q

Serotonin receptor antagonists (5-HT3)

A

Competitive antagonism of 5-HT3 receptors- very specific and free of neurological effects

Not effective for Motion induced NV

CYP450 and renal elimination

Ex Ondansetron

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6
Q

Ondansetron

A

Therapeutic after 30-60 min-typically given on induction

Half-life 4 hours

Adult 4-8mg

QTc

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7
Q

Granisetron and Dolasetron

A

Similar to zofran

Double the half-life- typically used in chemo

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8
Q

Palonosetron

A

Most effective 5-HT3 antagonist
40hr half-life…
Not used in anesthesia!! But fda approved for chemo

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9
Q

Dopamine receptor antagonists

A

Dopamine receptor blocker in the CNS-blocks adenylate cyclase to reduce cAMP….

Avoid in Parkinson’s

Increase EPS

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10
Q

Serotonin cascade

A

Serotonin is released from enterochromaffin cells of small intestine

  • vagal afferents stimulated via 5-HT3 receptors

-initiates vomiting reflex.

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11
Q

Dopamine antagonist ex

A

Droperidol- QTc… eeek

Haloperidol (butyrophenone)-

Metoclopramide (benzamide)- antiemetic and prokinetic via GI cholinergic mechanisms

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12
Q

Corticosteroids MOA

A

Synthetic glucocorticoid with anti inflammatory properties

Elusive

Decreases serotonin release
Acts on glucocorticoid receptors in vomiting center

Primarily dexamethasone is given 4-8mg

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13
Q

Dexamethasone considerations

A

Perineal itching in awake patients

2 hour onset

Combine with 5-ht3

Transient hyperglycemia-careful in diabetics

And avoid in acute leukemia due to tumor lysis syndrome

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14
Q

Neurokinin-1 receptor antagonists

A

Competitive antagonism with substance P at central GPCRs (NK receptors)

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15
Q

Aprepitant

A

Only NK-1 approved by FDA

50% reduction in NV

PO only 40mg preop

Well tolerated w/out QTc

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16
Q

Anticholinergics MOA anti emetics

A

Ach acts on the CTZ, vestibular system and cerebellum

Blocking cholinergic impulses to vomiting center

Scopolamine- single most effective for motion sickness

17
Q

Scopolamine

A

Anticholinergic

PO/IV/TD

4 hour onset with peak at 8-12 hrs up to 72 hours

Can be applied night before surgery

Treatment of side effects with physostigmine…other anticholinesterases are ineffective

18
Q

Histamine receptor antagonists

A

Potentially acts on receptors in vestibular system and vomiting center

Sedation!!

Benadryl and Dramine
Promethazine- do not give IV

19
Q

GABA agonists MOA anti-emetic

A

Elusive lol

Propofol-Rescue dosing in PACU- as effective as zofran with faster onset… 20mg

Can also give benzos

20
Q

Opioid antagonists in antiemetic

A

Naloxone… can give low dose infusion in attempt to nor reverse analgesia

21
Q

Cannabionoids

A

Not recommended in prevention

Have not been shown effective in PONV but are useful in chemotherapy

22
Q

Oral antacids

A

Raise pH and increase gastric volume (30ml administration)

Quick acting 15-20 min

23
Q

Histamine receptor antagonists in GI motility

A

Reduce Gastric volume
Do not alter pH of current stomach contents but do decrease secretion of hydrogen ion

Attach the receptor and prevent response mediated by histamine…

H2!!! No H1

1-3 hour onset

Ex> famotidine-Pepcid

Cimetidine-impairs CYP system, AMS in elderly

24
Q

Proton Pump inhibitor

A

Decrease pH, no impact on volume

Inhibit secretion from gastric parietal cells

Some interfere with CYP but to a lesser extent than H2

Can take several days to have desired effect, given IV they take about an hour….

25
Q

Metoclopramide….

A

Prokinetic

Improve gastric emptying=reduce volume

Does not alter hydrogen ion

Give 15-30 min prior

Beneficial with: “full stomach”, obesity, diabetic gastroparesis, parturients

Dopamine antagonist… do not give in Parkinson’s!

26
Q

Risk factors for PONV

A

Female

Non smoker

Opioids

Previous hx

27
Q

Name first gen 5-HT3 antagonists and main complication

A

Ondansetron
Granisetron
Dolasetron

QTc prolongation

28
Q

Name first gen 5-HT3 antagonists and main complication

A

Ondansetron
Granisetron
Dolasetron

QTc prolongation

29
Q

Populations with special considerations for corticosteroid administration

A

Diabetic

Cancer- tumor lysis syndrome

30
Q

Drug with CYP inhibition and numerous drug interactions

A

Cimeditine

31
Q

Signal cascade for vomiting center diagram

A