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Anti-emetics + GI disorders Flashcards

1
Q

What is NK?

A

Neurokinin

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2
Q

What is CB?

A

Cannabinoid

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3
Q

What is GR?

A

Glucocorticoid receptor

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4
Q

What are complications from N/V?

A

Dehydration

Electrolyte disturbances

Malnutrition

Aspiration pneumonia: gastric contents can get into respiratory system and cause inflammation

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5
Q

What are causes of N/V?

A

CNS: migraines, VESTIBULAR DYSFUNCTION (motion sickness)

GI: viral gastroenteritis, dysmotility, damage

Radiation = RINV

Surgery = PONV

Medications = CINV

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6
Q

What key receptors promote N/V?

A

H1, M1 = highly prevalent vestibular system

5HT3, NK1 = GI tract

D2

Opioid

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7
Q

Which receptors could be BLOCKED for potential anti-emetic effects?

A

H1
M1

5HT3
NK1

D2

Opioid

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8
Q

Which receptors inhibit N/V?

A

CB1

GR

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9
Q

Name 6 classes of antiemetics

A

5-HT3 antagonists

D2 Antagonists

M/H1 antagonists

NK1 antagonists

Corticosteroids

Cannabinoids

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10
Q

Name the 5-HT3 receptor antagonist drug

A

Ondansetron

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11
Q

What are the indications for ondansetron?

A

Acute CINV

RINV

PONV

Acute gastroenteritis

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12
Q

What drugs ENHANCE the effects of ondansetron?

A

NK1 blockers

Glucocorticoids

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13
Q

What AE’s are associated with ondansetron?

A

Headache

GI effects

Increase in LFTs

Increased QTc = inc. risk of TdP

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14
Q

Name the drug that is a D2 antagonist

A

Prochlorperazine

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15
Q

What is the MOA of prochlorperazine?

A

Blocks the following receptors:

D2
M
H1
Alpha1
Kr on heart
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16
Q

What is the indication for prochlorperazine?

A

“General purpose” antiemetics

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17
Q

What AEs are associated with prochlorperazine?

A

Drug-induced movement disorder from D2 blockade = tremor, slowness of movement, muscle rigidity

Involuntary movement of 👀, limbs => tardive dyskinesia

🍼Hyperprolactinemia from dopamine blockade

😡Anti-muscarinic side effects

💨 Orthostatic hypotension (dealing with alpha 1)

Increased QTc => increased TdP

😴 Sedation

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18
Q

What does hyperprolactinemia involve ?

A

Increased prolactin hormone

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19
Q

What are effects of having increased prolactin hormone?

A

Galactorrhea
Gynecomastia

Dec. sexual function
Dec. menses in women ⬇️🔴
ED in men ❌🍆

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20
Q

What is another D2 antagonist drug?

A

Metoclopramide

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21
Q

What is the MOA of metoclopramide?

A

Blocks:
D2
5HT3

Stimulates: 5HT4

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22
Q

What are the indications for metoclopramide?

A

PONV

GI motility induced problems = gastroparesis

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23
Q

What AEs are associated with Metoclopramide?

A

🍼🍼Hyperprolactnemia

🚷Movement disorders

◾️BLACK BOX WARNING: tardive dyskenesia

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24
Q

What are examples of D2 antagonists?

A

Prochlorperazine

Metoclopramide

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25
What are examples of M/H1 antagonists?
Scopolamine Meclizine Dimenhydrinate
26
What is the MOA of scopolamine?
M receptor antagonist
27
What is the MOA of meclizine and dimenhydrinate?
Blocks H1 + M
28
What is the therapeutic use for M/H1 antagonists?
Motion sickness ONLY
29
What AEs are associated with M/H1 antagonists?
😡Anti-muscarinic effects 😴Sedation
30
What is Aprepitant?
NK1 antagonist
31
Name an NK1 antagonist
Aprepitant
32
What is the therapeutic use for aprepitant?
CINV | in combo with -setrons and glucocorticoids to increase treatment of delayed CINV
33
What AEs are associated with aprepitant?
📈Increased LFTs
34
What is dexamethasone?
Corticosteroid
35
What are the indications for dexamethosone?
CINV (Need to combine with -setrons and NK1 antagonist) PONV
36
What AEs are associated with dexamethasone?
👹Insomnia 🍭Increase in blood glucose
37
What is dronabinol?
Cannabinoid
38
What is the MOA of dronabinol?
Stimulates CB1 receptors which can inhibit N/V
39
What is the therapeutic use of Dronabinol?
refractory CINV
40
What AEs are associated with dronabinol?
😝Increased laughing 😶Emotional changes 👾Hallucinations
41
What drugs induce N/V?
Chemotherapy drugs Opioids Drugs that increase dopamine activity SSRIs Drugs that increase ACh in the brain
42
Characterize GERD, PUD, and IBS as upper or lower GI disorders
GERD, PUD = upper GI IBS = lower GI
43
What are classical and atypical signs of GERD?
Classical = Heartburn, regurgitation, dysphagia (difficulty swallowing) Atypical = Chest pain, cough/asthma, recurrent sore throat/hoarseness, dental enamel loss
44
Describe the pathophysiology of GERD
Increased transient LES relaxations Hypotensive LES Hiatal hernia
45
What complications can arise from GERD?
Esophagitis Barrett's esophagus = increased risk of esophageal cancer Peptic strictures
46
What lifestyle changes can help with GERD?
Weight loss Elevation of head of bed approx. 6 inches Avoid lying down right after a meal Eliminate dietary triggers Chew gum to increase salivation (bicarbonate)
47
What are treatments for GERD?
Antacids H2RAs PPIs Metoclopramide
48
What is the MOA of antacids?
Neutralize acid to increase pH and eliminate pain
49
What are side effects associated with Mg-containing antacids?
💩Osmotic diarrhea Accumulation in decreased renal function
50
What AEs are associated with Al-containing antacids?
Constipation Accumulation in decreased renal function
51
What AEs are associated with Ca-containing antacids?
Hypercalcemia Belching + gastric distension Metabolic alkalosis (increase in plasma pH)
52
What AEs are associated with Na-containing antacids?
Increased sodium retention (Which can inc. BP and edema in pts with HF) Belching + gastric distension
53
What DDIs are associated with antacids?
Decreased absorption of drugs that require acidic environment Mg and Al can chelate some drugs => dec. absorption
54
What are examples of H2RAs?
Cimetidine Ranitidine
55
What is the MOA of H2RAs?
``` Block H2 receptors on parietal cells ⬇️ Decrease cAMP/PKA ⬇️ decreased activity from K/H ATPase ```
56
What AEs are associated with H2RAs?
GI discomfort 🙇🏻‍♀️😴Headache, dizziness, drowsiness Rash Inc. in plasma creatinine inc. risk of infections dec. B12 absorption => over time can lead to deficiency => neurological damage + anemia
57
Why is increase in plasma creatinine happen with H2RAs?
H2 blockers are competing with creatinine for renal secretion **not necessarily a reflection of decreased kidney function
58
What AE is associated with Cimetidine only?
Increase in prolactin in the blood = gynecomastia, galactorrhea, sexual dysfunction Anti-androgen effects = gynecomastia, sexual dysfunction (Double-whammy)
59
What DDIs are associated with H2RAs?
Decreased drug absorption requiring acidic environment Cimetidine only: inhibits multiple CYPs
60
What is the MOA of omeprazole (PPI)?
Blocks K,H ATPase on parietal cell = decrease in basal, stimulated acid maximally Needs to be absorbed into plasma
61
When should PPIs be taken?
30 min to 1 hr BEFORE meal
62
What AEs are associated with PPIs?
GI discomfort 🙇🏻‍♀️Headache, dizziness Increased LFTs Inc. risk of infections Dec. B12 absorption => eventual deficiency Dec. Ca absorption = inc. risk of osteoporosis Dec. Mg absorption = hypomagnesemia = muscle spasms, seizures, arrhythmias Increase in gastrin = ECL hyperplasia = rebound acid hypersecretion
63
What DDIs are associated with PPIs?
Inhibit absorption of drugs that require acidic environment Inhibition of CYPs
64
What is the MOA of metoclopramide?
Blocks 5HT3, D2 Stimulates 5HT4 = motility effects (prokinetic) which will increase motility of upper GIT = inc. LES pressure
65
What DDIs are associated with metoclopramide?
none!
66
What clinical findings are associated with peptic ulcer disease (PUD)?
Epigastric dyspeptic pain Relieved by food, milk, and antacids
67
What is the pathophysiology behind PUD?
Mucuosal defenses overwhelmed by HCl, pepsin Major causes: H. Pylori NSAIDs
68
What is a major complication that can result from PUD?
Perforations => bleeding => anemia
69
What lifestyle changes should be adopted for PUD?
Stop NSAIDs Dietary changes Stop smoking
70
What treatment options are available for PUD?
PPIs (or H2RAs) + antibiotics Sucralfate PG analogs Bismuth salts
71
What is the MOA of sucralfate?
Binds damaged area and increases protection PG synthesis (more mucus)
72
What AEs are associated with Sucralfate?
Not absorbed = no systemic effects
73
What is misoprostol?
Prostaglandin analog
74
What is the MOA of misoprostol?
Stimulates EP3 receptor on parietal and surface mucous cells Parietal cell = dec. cAMP/PKA = dec. HCl secretion Mucus cell = inc. mucus & HCO3 production
75
What are the indications for misoprostol?
NSAID-induced ulcers
76
What AEs are associated with Misoprostol?
Diarrhea Abdominal cramping Uterus contraction ** women of child-bearing age require negative pregnancy test before use
77
What is the MOA of bismuth salicylate?
Binds to damaged area to increase mucus, bicarbonate production Antimicrobial properties
78
Does BSS have any effect on HCl secretion?
No!
79
What AEs are associated with BSS?
Black discoloration of tongue and stool Absorption of salicylate can lead to salicylate toxicity (N/V, tinnitus, hearing loss, Reye's syndrome)
80
What clinical findings are associated with Irritable bowel syndrome (IBS)?
Recurrent abdominal pain Changes in stool frequency
81
How do you treat IBS?
Treatment varies for IBS where Constipation predominates Diarrhea predominates
82
How do you treat IBS where constipation predominates?
Lactulose Lupiprostone
83
How do you treat IBS where diarrhea predominates?
Loperamide
84
What is the MOA of Lactulose?
Osmotic agent that when metabolized will increase osmotic pressure
85
What AEs are associated with lactulose?
Flatulence Osmotic diarrhea Abdominal pain
86
What is the MOA of lupiprostone?
PGE1 analog binds to the EP4 receptor, causing increased chloride secretion
87
What AEs are associated with Lupiprostone?
Nausea Diarrhea
88
What is the MOA of loperamide?
Stimulates GI opioid receptor, resulting in: Increased non-propulsive contractions = segmentation Decreased secretions = peristalsis
89
What AEs are associated with loperamide
Abdominal pain Constipation
90
What drugs decrease pain for IBS?
Anti-spasmodic
91
What is the MOA for hyoscyamine?
Blocks GI smooth muscle M3 receptor, resulting in decreased GI SM contractions
92
What AEs are associated with hyoscyamine?
Anti-muscarinic

TBL (4 decks)

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