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GI- Week 2 > Fitzakerly: Anti-ulcer Drugs > Flashcards

Fitzakerly: Anti-ulcer Drugs Flashcards

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1
Q

What diseases are treated w/ anti-ulcer drugs?

A
  1. Peptic acid disease (H. Pylori, NSAIDS)
  2. GERD and NER
  3. Hypersecretory States (hyperacidity, dyspepsia, stress ulcers, gastrinoma, systemic mastocytoses)
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2
Q

What are the objectives for treating PUD, hypersecretory diseases and GERD?

A
  1. Heal the lesion
  2. Stop the pain
  3. remove possibility of recurrence
  4. avoid complications
  5. eliminate maintenance doses
  6. prevent development of resistance
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3
Q

What are the treatment strategies?

A
  1. eliminate the cause (h. pyolori)
  2. Reduce pain by decreasing H secretion
  3. Eliminate NSAIDs
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4
Q

What are hte most effective drugs for preventing and treating peptic ulcer disease? Why?

A

Antimicrobials because they ERADICATE H. pylori

Amoxicillin
clarithromycin
metronidazole
rifabutin
tetracycline
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5
Q

What is the penicillin of choice for h. pylori? Why?

A

Amoxicillin

More acid stable

More than twice the blood levels are achieved w/ the same oral dose

Affective against gram -

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6
Q

What is the MOA and toxicity of Amoxicillin?

A

CIDAL
cell wall inhibitors

hypersensitivity

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7
Q

What is the macrolide antibiotic of choice for h. pylori treatment?

A

Clarithromycin

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8
Q

Why is clarithromycin better than azithro or erythro?

A

lowest MIC50 and is more acid stable

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9
Q

How do you compare azithro, clarithro and erythro?

A

Azithro and clarithro are better than erythro b/c they can be given at lower doses and have less GI effects.

Clarithro is better than azithro b/c the MIC90 is .06 vs. .25

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10
Q

What is the MOA of macrolides? Toxicity?

A

Static
Protein synthesis inhibitor (50S RNA)

GI irritation
drug interactions

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11
Q

What else can be used to treat h. pylori infections? Co administration with what can significantly decrease the antibiotic efficacy d/t chelation.

A

Tetracyclines

Antacids

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12
Q

You should always give tetracycline w/ ______NOT ________.

A

Food

NOT antacids

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13
Q

What is the MOA and toxicity of tetracyclines?

A

Static
protein synthesis inhibitors (30S)

Gi irritation
photosensitivity
discoloration of teeth (not good for pregnant women or children)

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14
Q

What drug is a bacterialcidal and inhibits hte DNA dep RNA pol?

A

Rifabutin= rifamycin

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15
Q

What are the SE of rifamycin?

A

Hypersensitivity/fever
hepatotoxicity
cyp 450 inhibition
orange/red body fluids

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16
Q

Why don’t we often use metronidazole/tinidazole to treat h. pylori?

A

up to 65% of infections are resistant

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17
Q

What is the MOA and SE of metronidazole/tinidazole?

A

DNA damage?

SE: GI, CNS toxicity, disulfiram rxn, teratogenic

Inhibits cyp2C9 (can potentiate warfarin and reduce clearance of H2 blockers)

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18
Q

What is the MOA of Bismuth?

A
  1. Antimicrobial- disrupts the cell wal and prevents adhesion or inhibits urease
  2. protects surface (coats surface and stimulates secretion of mucus, PG and bicarb)
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19
Q

Bismuth is only active in ______not_______.

A

stomach not the lower GI

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20
Q

Whare are the SE of bismuth subsalicylate?

A

Subsalicylate causes most SE: vomiting, tinnitus, confusion, hyperthermia, resp. alkalosis> met. acidosis

Bismuth: black tongue/stool

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21
Q

What are the causes of antimicrobial treatment failure?

A
  1. resistance (metronidazole and clarithromyacin)

2. compliance (too many pills for too long)

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22
Q

What drugs are used to eradicate H. Pylori?

A
  1. Amoxicillin
  2. Clarithromycin
  3. Tetracycline
  4. Rifabutin
  5. Metronidazole/tinidazole
  6. Bismuth subsalicylate
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23
Q

What drugs promote mucosal defence?

A
  1. bismuth subsalicylate
  2. misoprostol
  3. simethicone
  4. sucralfate
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24
Q

What antacids reduce intragastric acidity?

A
  1. aluminum hydroxid
  2. Ca carbonate
  3. magnesium hydroxide
  4. sodium bicarbonate
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25
What antimuscarinics reduce intragastric acidity?
1. atropine | 2. pirenzipine
26
What H1 blockers reduce intragastric acidity?
1. Cimetidine 2. famotidine 3. Nizatidine 4. Ranitidine 5. roxatidine
27
What PPI reduce intragasric acidity?
1. lansoprazole 2. omeprazole and esomeprazole 3. pantoprazole 4. raberprazole
28
What drugs are RARELY used to treat ulcers b/c they slow gastric emptying and prolong exposure of the ulcer to acid?
Muscarinic receptor ANTAGONISTS Atropine pirenzipine *also have a more severe SE htan H2 blockers
29
How does ACh trigger acid secretion?
ACh acts on M1 (ECL) and M3 (Parietal cell) leading to acid secretion
30
What type of receptors are muscarinic receptors?
M1 and M3> G protein linked> activate phospholipiase C and D> increase in IP3
31
What is the MOA of atropine and pirenzipine?
compeptive inhibitors of ACh
32
Which muscarinic receptor antagonist is M1 selective?
pirenzipine
33
What are the SE of atropine and pirenzipine?
``` ABCD'S Anorexia blurry vision constipation/confusion dry mouth sedation/stasis of urine ```
34
What drugs are NOT used to tx ulcers?
Muscarinic receptor antagonists
35
Overdose of atropine will cause...
CNS: hallucinations/ confusion tachycardia hot, dry skin
36
What drugs are H2 receptor antagonists?
CIMETIDINE famotidine nizatidine ranitidine
37
What do H2 receptor antagonists do?
Decrease ALL forms of gastric acid secretion (esp nocturnal)
38
Why are H2 receptor antagonists OTC?
they ahve few SE except cimetidine and can be given orally
39
What is the primary effect of H2RAs?
They are competitive antagonists of H2 and are highly selective (no H1 activity)
40
What is the secondary effect of H2 receptor antagonists?
Decrease intracellular cAMP> basal and nocturnal secretion d/t other agents
41
What is the t1/2 of H2RA?
Usually 1-4 hrs but they have extensive hepatic metabolism and are excreted renally
42
Which H2RA is hte best tolerated?
Famotidine (highest potency + smallest dose)
43
What are the SE of H2RA?
No SE when given ORALLY to HEALTHY pt
44
Why is it bad to give a pt rapid IV infusion of H2RA?
bradycardia and hypotension *there are H2 receptors in the heart so you have to give a slow infusion
45
What drug drug interactions are seen with H2RA?
1. decreased ethanol metabolism (esp in women) | 2. Compete for tubular secretion w/ weak bases (metronidazole)
46
High doses of Cimetidine can cause...
1. decrease binding of DHT to androgen receptors decreased estrogen metabolism incerased prolactin--> gynecomastia and impotence in men galactorrhea in women 2. inhibition of cyp450 (increases effectiveness of other drugs)
47
Which drug has a therapeutic advanatage esomeprazole or omeprazole?
Esomeprazole is exclusively the S isomer (omeprazole is the racemic mixture) and is metabolized more slowly and reproducibly
48
What are the most effective agents for reducing intragastric acidity b/c they IRREVERSIBLY block the final common pathway in acid secretion---the H/K ATPase in the parietal cell?
``` PPI: esomeprazole/omeprazole lansoprazole pantoprazole rabeprazole ```
49
What drugs are good for treating GERD and ZE syndrome?
PPI
50
Why do PPIs need a coating?
they are prodrugs that become labile in acid and must pass through the stomach to be absorbed
51
Where are PPIs absorbed/concentrated?
SI then circulate throughout the body> concentrate in teh acidified compartments> protonated> active form
52
What should you give a PPI?
give drug 1/2 hr before meal so the concentration is highest when the pumps are active
53
What are the SE of PPIs?
No sig SE Some pts may experience HA, diarrhea, nausea, rash
54
What is the danger of stopping PPIs in a pt who has been using them for a long time?
rebound acid hypersecretion
55
What concerns are associated w/ long term use of PPIs?
1. Decreased B12, FE, Ca, Zinc absorption> hip fx 2. increased respiratory and enteric infections (increased pH) 3. ECL hyperplasia (hypergasrinemia) Normally a decreased gastric pH> increases SS release> and leads to a decrease in gastrin
56
What is used to buffer stomach acid?
``` Weak bases: Aluminum hydroxide Ca carbonate Mg hydroxide Na Bicarbonate ```
57
What weak bases are systemically absorbed?
NaHCO3 the most | CaCO2 some
58
What drugs have a fast rate of dissociation?
NaHCO2 and CaCO2
59
What weak bases create gas and can cause belching?
CaCO2 and NaHCO3
60
aluminum hydroxide
Efficient and low systemic absorption CONSTIPATION (not effective when given alone) Decreases PO4 absorption> increased Ca loss> osteomalacia
61
magnesium hydroxide
Efficient and low systemic absorption (like Al OSMOTIC DIARRHEA Renal insufficiency> hypermagnesemia> CNS and cardiotoxicity
62
Calcium carbonate
Rapid onset of action and long duration Belching/gastric distention, rebound acid secretion MILD SYSTEMIC ALKALOSIS
63
Na Bicarbonate
Extremely RAPID onset of action bleching, gastric distention, short duration of action SEVERE METABOLIC ALKALOSIS ALKALINIZES URINE
64
What drug interactions are associated w/ weak bases?
1. increase gastric pH (can increase or decrease absorption) 2. binds drugs (decrease absorption) 3. increases gastric emptying (decreased absorption) 4. systemic absorption (alkalinize urine)
65
What is simethicone?
antifoaming agent that decreases gas pain *also affects absorption
66
What is the difference between antacids, H2 blockers and PPIs?
Antacids: rapid onset, short duration, INTERMITTENT DYSPEPSIA (don't prevent ulcer recurrence) H2 blockers: rpaid onset, intm duration, some prevention PPI: slow onset, ong duration, EXCELLENT prevention
67
What is the drug of choice for ZE syndrome, GERD and ulcer treatment?
PPIs
68
What is sucralfate?
Al (OH3) and sulphated sucrose (NOT an antacid)
69
What is the MOA of sucralfate?
attaches to ulcer surface (acts like a band aid)
70
Sucralfate is used to tx?
stress induced ulcers in the ICU
71
What does sucralfate require and what should it not be taken with?
acidic environment to be converted to paste interacts w/ PPI and H2 blocker
72
What are the SE of sucralfate?
constipation | binds other drugs
73
What does misoprostol do?
replaces prostaglandins
74
What percent of ulcers are caused by NSAIDs?
5%
75
Why does misoprostol owrk?
PGE is less involved w/ inlammation and misoprostol t1/2 is 30-40 min compared to acetaminophen and ibuprofen (2hrs)
76
What are the pharmikokinetics of misoprostol?
rapid absorption and metabolism | excreted in urine
77
What are the SE of misoprostol?
diarrhea, severe nausea, cramping, abdominal pain
78
What drug can also be used as an aborficant b/c it stimulates uterine contractions?
MIsoprostol
79
What is triple therapy?
PPI + )clarithryomyacin for 5 days followed by amoxicillin or tinidazole for 5 days)
80
What is quadruple therapy?
PPI + tetracycline + metornidazole + bismuch subsalicylate for 14 days
81
What is a last choice therapy for ulcers?
PPI+ amoxicillin + rifabutin + cipro for 10 days
82
At a low pH will you get more gastric absorption of WA or WB?
More of WA
83
At a high pH will you get more gastric absorption of WA or WB?
WB will increase (PPI, H2 blocker, antacid)
84
At a low pH will you get more excretion of WA or WB?
MOre WB
85
At a high pH will you get more excretion of WA or WB?
More WA (antacids)

GI- Week 2 (11 decks)

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