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Exam 1 Pharm II > GI drugs > Flashcards

GI drugs Flashcards

1
Q

Combination used to treat H. pylori

A

Bismuth, Metronidazole, Tetracycline, Clarithromycin, Amoxicillin, H2 blocker/PPI, Ranitidine bismuth citrate.

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2
Q

Antiacids containing NaHCO3 have a________ Neutralizing capacity

A

High

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3
Q

What are the adverse sude effects associated with NaHCO3?

A

Systemic alkalosis, fluid retension

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4
Q

CaCO3 has a _______Neutralizing capacity.

A

Moderate

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5
Q

What adverse effects are assoc. with CaCO3 antiacids?

A

Milk-alkali syndrome:

Hypercalcemia, Nephrolithiasis

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6
Q

Al(OH)3 has a ________neutralizing capacity.

A

High

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7
Q

Adverse effects assoc. with AL(OH)3 antiacids

A

Constipation, hypophosphatemia

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8
Q

Mg(OH)2 has a_________neutralizing capacity

A

High

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9
Q

Adverse effect of Mg(OH)2 antiacids

A

Diarrhea, hypermagnesemia

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10
Q

What is Alternagel?

A

Al(OH)3 antiacid

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11
Q

What is Maalox and Mylanta

A

Al(OH)3 and Mg(OH)2 antiacid. It balances the constipation from Al(OH)3 and the diarrhea from Mg(OH)2 to give you an exquisite poop.

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12
Q

We all know what Tums are…….What’s their active agent?

A

CaCO3

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13
Q

What is Gaviscon?

A

Sodium Alginate+ Antiacids. It’s a viscous weak base. It prevents reflux and effective against GERD

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14
Q

Pathology connection: Why the hell do we treat GERD besides it being annoying to deal with?

A

GERD=====>Continuous irritation of lower 1/3 pf esophagus which leads to transformation of the squamous epithilial tissue there to Columnar, mucus secreting cells (Adenocarcinoma of the esophagus)

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15
Q

What is Simethicone? (Trade name: Mylicon, Phazyme)

A

It enchances the release of gas.

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16
Q

What is Cimentidine? MOA?

A

Cimen(tidine), Rani(tidine), Famo(tidine), Niza(tidine) are H2 Histamine receptor antagonists
MOA: Competitive antagonists of H2 histamine receptor. Reduce HCL secretion from parietal cells in response to histamine, gastrin and ACh.

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17
Q

What CYP enzymes does Cimetidine inhibit? (This matters so……“bigly”

A

CYP 2C6 and 2D9 (CD-69)=====>Insert inappropriate memory aide

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18
Q

What drugs are affected by Cimetidine’s inhibition of CYP______ and CYP_______?

A
  1. CYP 2C6 & 2D9

Drugs affected: Warfarin, phenytoin, theophylline, benzodiazepines, sulfonylureas

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19
Q

Cimetidine side effects are……

A

CNS (Confusion, delirium, headaches)==Seen w/ IV admin. in elderly.
Antiandrogen (Gynecomastia, impotence)
Inhibition of estradiol metabolism (Galactorrhea- Too much milk production)

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20
Q

Name the 2nd gen H2 antagonists have?

A

Rani(tidine), Niza(tidine), Famo(tidine). “RuN Fast”

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21
Q

What advantages do 2nd gen H2 antagonists have?

A

Longer half-life
Fewer effects on CYP450 system
Greater potency
Increase ethanol bioavailability by reducing 1st pass metabolism (except Famotidine)

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22
Q

What do PPIs act on?

A

Inhibit K+/H+ antiport. Bind irreversibly (Covalently)

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23
Q

Name all PPI’s we covered

A

Ome(prazole)
Lanso(prazole)
Raber(prazole)
Panto(prazole)

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24
Q

Prior to binding to the K+/H+ antiport, omeprazole is transformed into two intermediates (in acidic environment)_______________ and finally______________

A
  1. Sulfenic acid

2. Cyclic sulfenamide

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25
Q

How are PPI’s activated?

A

They are prodrugs activated by Acid

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26
Q

PPI’s have a ___________half-life but a________duration of action.

A
  1. Short

2. Long

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27
Q

Adverse effect of PPI use?

A

Hypergastrinemia can occur and result in rebound hypersecretion of gastric acid.
Increased pH in gut can affect drug absorption and increase infection risk.

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28
Q

What is Misoprostol? How does it work?

A

Is a prostaglandin E1 derivative which reduces HCL secretion from parietal cells.
Cytoprotectant= Enchances mucus and bicarbonate secretion.

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29
Q

What drug is commonly administered with NSAIDs as pepric ulcer preventative?

A

Misoprostol

30
Q

What are the adverse effects of misoprostol?

A

Diarrhea, Abortifacient (Trump can’t stop us now!)

31
Q

How does H.Pylori cause peptic ulcers?

A

It reduces D-cell production of Somatostatin. This leads to an increased secretion of gastrin====>Stimulates parietal cells to secrete HCl====>Ulceration occurs.

32
Q

Bismuth subsalicylate (Pepto-Bismol) is converted to_______ and ______ in the GI tract

A
  1. Bismuth salts

2. Salicylic acid

33
Q

What properties does Bismuth subsalicylate have?

A

Antibacterial, antiviral and antisecretory activity

34
Q

What is bismuth used for?

A

Treatment of diarrhea and part of therapy to treat H. pylori.

35
Q

What class of drugs increase GI motility?

A

Prokinetic drugs

Laxatives

36
Q

What class of drugs reduce GI motility?

A
  1. Antidiarrheals.

2. Anti-emetics

37
Q

What does Metoclopramide(Reglan) act on?

A

It is a prokinetic drug that blocks the D2 dopamine receptor in the myenteric plexus which leads to increased ACh release.

38
Q

What is Metoclopramidine used for?

A

Facilitate small bowel intubation, post-op and diabetic gastroparesis, GERD and is an anti-emetic.

39
Q

What side effects does metoclopramide have?

A

Sedation
Parkinson’s-like syndrome
Hyperprolactinemia (Gynecomastia, galactorrhea and breat tenderness)

40
Q

How do Cisapride, Tegaserod and Prucalopride work?

A

Both are 5-HT4 agonists. They are prokinetic drugs but withdrawn freom market in US due to Cardiovascular toxicity. Prucalopride is not available in the USA.

41
Q

How does erythromycin work in relation to GI motility?

A

It’s a prokinetic…….so diarrhea is an expected side effect of using this ATB. It is a motilin agonist.

42
Q

What is Linaclotide? How does it work?

A

It is a prokinetic drug. It’s a peptide activator of guanylate cyclase 2

43
Q

What conditions does Linaclotide treat?

A

Irritable Bowel Syndrome, Constipation, Idiopathic constipation. (Take 30mins before first meal).

44
Q

What are the side effectas of linaclotide?

A

Diarrhea only It is not absorbed systemically

45
Q

What is Liaclotide’s mode of action?

A

Image is excellent. It Activates Guanylate cyclase 2 receptor=====>Increases cGMP=====>CFTR is activated increasing Cl and HCO3 release into the lumen. It also decreases activity of pain-sensing nerves as a result of elevation in extracellular cGMP concentration

46
Q

Name a secretory laxative

A

Castor oil- Hydrolyzed in small intestine into ricinoleic acid

47
Q

Bisacodyl (dulcolax), Cascara, Senna and Aloes (Anthraquinones) _How do these work?

A

Stimulate peristalsis by opening Cl- channels in intestinal mucosa to allow Cl-, Na+, and H2) into the lumen.

48
Q

Lubiprostone is used to treat what?

A

Is a specific CIC2 activator used to treat Chronic Idiopathic constipation. Also used with IBS with chronic constipation.

49
Q

How do bulk and Saline laxatives work?

A

Increase intestinal luminal osmotic force leading to distension and an increased peristalsis. Thy are non absorbable and form hydrophobic mass in presense of H2O

50
Q

Give 5 examples of a bulk laxative

A 
Psyllium
Methylcellulose
Bran
Milk of magnesia
Laculose
Iso osmotic electrolyte solutions with polyethylene glycol(GoLytely)
51
Q

What is laculose used to treat

A

Hepatic encephalopathy

52
Q

How do stool softeners work? Give 5 examples.

A 
Incorporate into stool making passage easy
Docusate sodium (Colace), mineral oil, glycerin, surfactants and lubricants.
53
Q

What is a sideefect of using stool softeners?

A

Can decrease the absorption of fat-soluble vitamins

54
Q

How do anti-diarrheals work?

A

Slow peristalsis to increase H2O and electrolyte absorption.

55
Q

Give one example of anticholinergic anti-diarrheals.

A

Dicyclomine (Bentyl)

56
Q

Give two examples of opiate anti-diarrheals.

A

Diphenoxylate (W/ atropine; Lomotil)

Loperamide

57
Q

When are the anti-diarrheal opiates_________and ________ contradindicated?

A
  1. Diphenoxylate and 2. Loperimide

Contraindicated in pts with severe ulcerative colitis and bacterial diarrhea.

58
Q

How do diphenoxylate and loperamide work?

A

They act locally (No CNS effects) to delay gastric emptying.

59
Q

How does Kaolin, Pectin and low dose fiber work?

A

Adsorb potential intestinal toxins and H2O.

60
Q

How does Crofelemer work? and when is it used?

A

Crofelemer blocks CFTR and Ca++ activated Cl- channels (CaCCs)
It is used in HIV patients on antiretroviral therapy.

61
Q

What is Alosetron? When is it used?

A

Alosetron is a 5HT3 receptor inhibitor. It is used in women with IBS+Diarrhea. It blocks visceral afferent pain sensation and decreases colon motility

62
Q

What are the side effects of Alosetron?

A

Constipation, Ischemic colitis (may be fatal)

63
Q

Name the 3 D2 dapamine receptor antagonists which are used as anti-emetics?

A

Promethazine
Prochlorperazine
Metoclopramide

64
Q

Name two anticholinergic/Antihistamines used as anti-emetics

A

Meclizine

Scopolamine

65
Q

What can scopolamine and meclizine be used for?

A

Motion sickness

66
Q

Name three 5HT3 receptor antagonists that are used as anti-emetics

A

Ondansetron
Aprepitant
Granisetron

67
Q

How do 5HT3 receptor antagonists work as anti-emetics?

A

Bock activity in chemoreceptor trigger zone (CTZ) and vagal afferents from stomach and small intestine which activate CNS emetic centers.

68
Q

5HT3 receptor antagonists are normally combined with…..?

A

Aprepatant (NK1 antagonist) and Dexamethasone

69
Q

Cannabinoids are used as…….(Besides feeling chill)

A

Anti-emetics

70
Q

Name two Cannabinoid antiemetics.

A

Dronabinol
Nabilone
Used to treat nausea and vomiting associated with chemotherapy……..As expected these will make you pretty high and are limited to pratients who wont respond to anything else (sign me up!)

Exam 1 Pharm II (8 decks)

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