GI Pharmacology 2 - Slides 1-15 Flashcards

1
Q

List the indications for anti-emetic drugs

A

Severe nausea and vomiting
Motion sickness
Post-operative nausea and vomiting
Nausea and vomiting associated with chemotherapy

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2
Q

What causes vomiting reflex?

A

Mediated through the vomiting center in the medulla

Vagus nerve, spinal motor nerves to the abdominal muscles

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3
Q

What happens when the vomiting reflex is activated?

A

Reverse peristalsis of the upper GI tract
Glottis closes, breath is held, esophageal and gastric sphincters relax
Abdominal muscles contract to eject gastric contents

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4
Q

What are anti-muscarinic agents used for? What options do we have?

A

Motion sickness

Scopolamine

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5
Q

Side effects of scopolamine?

A

Dry mouth
Blurred vision
Urinary retention

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6
Q

What anti-histamines are used as anti-emetics?

A

Dimenhydrinate (Dramamine)
Promethazine
They cause sedation, anti-muscarinic side effects

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7
Q

What are ondansetron, dolasetron, granisetron?

A

5-HT3 receptor antagonists

Both CNS and peripheral

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8
Q

Indications for ondansetron, dolasetron, granisetron?

A

Effective in CINV (cisplatin)

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9
Q

Adverse effects of ondansetron, dolasetron, granisetron?

A

Headache, diarrhea, constipation

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10
Q

What are the phenothiazines?

A

Prochlorperazine
Chlorpromazine
Fluphenazine
Haloperidol

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11
Q

What is the MOA of the phenothiazines?

A

D2 receptor antagonists in the CTZ

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12
Q

Adverse effects of the phenothiazines?

A
Dizziness
Fatigue
Seizures
Sedation
Increase prolactin
Neuroleptic malignant syndrome
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13
Q

What are the cannabinoids?

A

Dronabinol
THC, oral formulation
Can be used for CINV when other agents have failed

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14
Q

MOA of Dronabinol?

A

Works via central action on the vomiting center

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15
Q

Adverse effects of Dronabinol?

A
Confusion
Euphoria
Dizziness
Mood changes
Orthostatic hypotension
Increased appetite
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16
Q

What is Aprepitant?

A

Substance P antagonists

It is an antagonist at NK1 substance P receptor

17
Q

What is Aprepitant used for?

A

Vomiting due to cisplatin in all acute (24 hr) patients and many delayed phase (36-72 hour) patients

18
Q

How does Aprepitant compare to the 5ht antagonists?

A

5ht antagonists work best against acute phase, Sub P best against delayed phase

19
Q

How is Aprepitant administered?

A

Given with chemo and on following 2 days

20
Q

What is Metoclopramide?

A

PROKINETIC DRUG
D2 antagonist, D2 receptors suppressed
Decreased CTZ sensitivity, antiemetic
Works by blocking the presynaptic D2 receptors and increasing ACH release
This increases gastric emptying/upper GI motility/Lower esophageal sphincter tone

21
Q

Indications for Metoclopramide?

A

Gastroparesis

GERD

22
Q

Adverse effects of Metoclopramide?

A

Dizziness, fatigue, seizures, sedation

Increases prolactin, can cause neuroleptic malignant syndrome

23
Q

What is Cisapride?

A

Prokinetic
5HT4 agonist
5HT3 antagonist

24
Q

Indications for Cisapride?

A

GERD

Gastroparesis not controlled by other treatments

25
Q

Adverse effects of Cisapride?

A

Cardiac arrhythmias, prolonged QT interval due to CYP3A4 interaction with other drugs (increases cisapride)

Headache, N/V, abdominal pain

26
Q

What is erithromycin?

A

Prokinetic drug

Motilin type actions in upper GI tract, LES

27
Q

Indications for erithromycin?

A

Diabetic gastroparesis

28
Q

Toxicities with erithromycin?

A

Cramps
Impairs motility
Dumping of stomach contents into small bowel (used for bezoars due to Procardia XL)

29
Q

Which agent is used for bezoars due to procardia XL?

A

Erithromycin

30
Q

What is Lubiprostone?

A

PGE1 analog used for IBS

It activates Cl channels to increase fluid secretion into the GI tract

31
Q

Indications for Lubiprostone?

A

Treatment of chronic idiopathic constipation and IBS-constipation

LUB = lube = lubes GI tract = less constipation

32
Q

What is Alosetron?

A

5HT3 antagonist, decreases gastric motility

33
Q

Indications for Alosetron?

A

Diarrhea predominant IBS in women

34
Q

Cautions with Alosetron?

A

It was introduced and withdrawn in 2000 due to acute ischemic colitis
Reintroduced in 2002 with a black box warning and lower dose/specific education and monitoring conditions
Use is very limited, a prescribing program is required, at lower doses

35
Q

Adverse effects of Alosetron?

A

Constipation, sometimes severe requiring constipation
Hypertension
Arrhythmias
Sleep disorders