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Summer pharm 4 > Antiemetics > Flashcards

Antiemetics Flashcards

1
Q

What causes nausea

A

Physiologic, Metabolic, Treatment related, and Emotional.spiritual/psych all transmit signals to the Vomiting center of the brain AKA the lower medulla

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2
Q

What receptors are associated with nausea and vomiting

A

Cytotoxics, opiates: D2, 5HT3, NK1
Pain, anxiety, depression: H1, GABA in cortex and thalamus
Vertigo, motion: AChM, H1 in vestibular system
Cytotoxics, gastric irritants, ipecac: 5HT3 in GI
ALL those report to Emesis center receptors: AChM, H1, 5HT3, mu, and NK1

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3
Q

What is the “vomiting center”

A

Neuronal region in lateral medullary reticular formation
Coordinates vomiting thru CN VIII and X (control respiratory, salivatory, and vasomotor centers)
High concentrations in M1, H1, NK1, D2, GABA, and 5-HT receptors in the vomiting center

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4
Q

What are 4 important sources of afferent input to vomiting center

A
  1. Chemoreceptor trigger zone: emetogenic stimuli
  2. Vestibular system: motion sickness
  3. Vagal and spinal afferent nerves (from GI): chemo, radiation, distention, gastroenteritis
  4. CNS: psych d/p, stress, anticipatory vomiting before chemo
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5
Q

How does N/V present

A

Simple: self limiting, resolves spontaneously, requires Sx therapy. complain of “queasy” or discomfort
Complex: no relief after anti-emetic. Noxious agents or psych events. can cause weight loss, fever, abdominal pain

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6
Q

What lab tests can you get for n/v

A

simple: none
complex: Electrolytes, upper and lower GI eval
Both: fluid input/output, Med history, recent behavior or visual change, HA, pain, stress, or FHx of psychogenic vomiting

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7
Q

Treatment of choice for n/v involves

A

ID of neurotransmitters involved with emesis!

Can use combo meds that have different MOA, esp if vomiting 2/2 chemo

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8
Q

MC drugs used are

A 
Antacids 
Antihistamine/anticholinergic 
Benzodiasepines 
Corticosteroids 
5-HT receptor antagonists 
Phenothiazine 
Substance P/NK1 receptor antagonist
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9
Q

When should Antacids be used

A

Simple N/VUse sodium bicarbonate, calcium carbonate, magnesium hydroxide, or aluminum hydroxide
OTC liquid or oral

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10
Q

Slide 14 says ADE

A

Listen to recording

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11
Q

What are the serotonin antagonists (5HT3)

A

Ondansetron
Granisetron
Dolasetron
Palonosteron

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12
Q

What is the PK of 5-HT3 antagonists

A

Centrally block the 5HT3 receptors, which are in the vomiting center on extrinsic intestinal vagal and spinal afferent nerves

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13
Q

Antiemetic action of 5-HT3 antagonists is restricted to emesis attributable to

A

Vagal stimulation (post-op)
Chemotherapy
-NOT good for motion sickness

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14
Q

What is palonosetron

A

New IV agent with greater affinity for 5HT3 receptors
Has longer half life (40 hours)
-All others have a half life 4-9 hrs and PO or IV

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15
Q

What happens to 5HT3 antagonists in the body

A

Extensive hepatic metabolism
Renal and hepatic excretion
Do not inhibit dopamine or muscarinic receptors
No effect on esophageal or gastric motility
May slow colonic transit**

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16
Q

Do you need to adjust 5HT3 antagonists

A

NO dose reduction in elderly with renal excretion

Only reduce Zofran dose if w/ hepatic insufficiency

17
Q

When should you take 5HT3 antagonists for chemo

A

IV, 30 minutes prior to getting chemo
PO 1 hr before chemo (but higher doses)
They are preventive, but have little efficacy in curing delayed n/v
Efficacy enhanced if combined w/ corticosteroid (DXM) or NK antagonist

18
Q

5HT3 antagonists are also used for

A

post-op and post-radiation n/v, esp whole body radiation

19
Q

What are ADE of 5HT3 antagonists

A

Headache*
Constipation*
Dizziness
QT prolongation (esp. dolasetron)

20
Q

5HT3 antagonists interact with

A

Nothing significant!
Some CYP450 hepatic metabolism
But do not affect metabolism of other drugs
Slide 22, listen (red question marks)

21
Q

What are NK1 antagonists

A

Aprepitant (emend), Fosaprepitant, Rolapitant (varubi); Netupitant + Palonosetron (Akynzeo) for acute and delayed prevention
They provide relief from delayed emesis associated with emetogenic meds

22
Q

What are the ADE of NK1 antagonists

A

Constipation
diarrhea
HA
hiccups

23
Q

What do you monitor when on NK1 antagonists

A

assess for efficacy as prophylaxis

episodes of n/v and hydration status

24
Q

What antihistamines are used for nausea

A 
Dimenhydrinate (Dramamine) OTC
Diphenhydramine (Benadryl) Rx/OTC
Hydroxizine (vistaril, atarax) Rx
Meclizine (bonine, antivert) RX/OTC 
Scopolamine (transderm scop) Rx
Trimethobenzamide (tigan) Rx
25
Q

What is Dramamine used for/ADE

A

Can cause drowsiness, confusion, blurred vision, dry mouth, and urinary retention
Used for: Episodic relief of motion sickness or n/v

26
Q

What is Meclizine especially good for

A

Vertigo

27
Q

What phenothiazines are used for nausea

A

Prochlorperazine (compazine): simple n/v and breakthrough chemo
Promethazine (phenergan)
Chlorpromazine (thorazine): simple n/v

28
Q

What are ADE of phenothiazines

A

Compazine: *prolonged QT interval, sedation, tardive dyskinesia
Phenergan: drowsy, sedation
Thorazine: constipation, dizziness, tachycardia, tardive dyskinesia

29
Q

What are the Butyphenones good for nausea

A

Haloperidol (haldol): great for palliative care

Droperidol (inapsine): limited use outside of clinical trial

30
Q

What are the ADE of butyphenones

A

Haldol: sedation, constipation, hypotension- obs for sedation if used w/ narcotics
Inapsine: QT prolongation, Torsades- ECG prior to admin and 2-3 hours after

31
Q

What benzos are used for nausea

A

Alprazolam (xanax) Rx: anticipatory n/v, take prior to chemo
Lorazepam (ativan) Rx: give the night before chemo

32
Q

What are ADE of benzos

A

xanax: dizziness, sedation, appetite changes, memory impairment

33
Q

What corticosteroids can be used for nausea

A

Dexamethasone, Rx: antiemetic by enhancing efficacy of 5HT3 antagonists
Monitor for nausea, vomiting, and hydration status
Useful as single agent or combo for prophylaxis of CINV and PONV

34
Q

ADE of dexamethasone are

A

Insomnia
GI Sx
Agitation
appetite stimulation

35
Q

What can cannabinoids be used for nausea

A

Dronabinol (marinol): Sx relief and refractory CINV. May cause euphoria, somnolence, xerostomia
Nabilone (cesamet): may cause somnolence, vertigo, xerostomia

36
Q

What miscellaneous agents can be used for nausea and vomiting

A

Metoclopramide (reglan): prokinetics are useful in diabetics with gastroparesis! Watch for asthenia, HA, or somnolence
Olanzapine (zyprexa): breakthrough CINV. watch for sedation

37
Q

What antiemetics can be used in pregnancy

A

Before meds: dietary changes or lifestyle mod
1. Pyridoxine w/ or w/o doxylamine
Persistence: IV fluids w/ Thiamine
Ondansetron: NVP
Methylprednisolone: refractory NVP or hyperemesis gravidarum

Summer pharm 4 (14 decks)

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