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Pharmacology > GI I - Acid Peptic Diseases and GERD > Flashcards

GI I - Acid Peptic Diseases and GERD Flashcards

1
Q

Key pathogenic agent in peptic ulcers? Functions?

A

H. Pylori is the key pathogenic agent and it both stimulates acid secretion and destroys stomach protective mechanisms

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2
Q

3 main drug categories to treat peptic ulcers

A

Druge that:

a. Decrease acid secretion
b. Neutralize stomach acid
c. Promote mucosal defence against acid

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3
Q

3 stomach cells and what do they secrete?

A

a. Enterochromaffin-like cell: histamine
b. Parietal cell: stomach acid
c. Superficial epithelial cell: cytoprotective mucus and bicarbonate

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4
Q

Histamine antagonists:

  1. What receptor?
  2. Functions?
A

Histamine antagonists:

  1. H2 receptor
  2. Blocks histamine but also blocks the potentiated actions of histamine and causes reduces secretion of acid
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5
Q

Prostaglandins:

  1. What two prostaglandins are important?
  2. What is their function?
  3. Agonist?
  4. Antagonist?
A

Prostaglandins:

  1. PGE2 and PGI2
  2. Protection: stimulate production of mucin and bicarb.
  3. Misoprostol
  4. NSAIDS
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6
Q

4 types of drugs with their role in the gastric lumen and role?

A

a. Proton pump inhibitors
b. Antacids: “soak up” H+ ions
c. H. Pylori medications
d. Cryoprotection: stimulate mucin and HCO3-

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7
Q

Proton Pump Inhibitors:

  1. These are ___ that require activation in an ___ environment.
  2. Type of binding? Duration?
  3. Most ___ suppressors. Reduce by what %?
A

Proton Pump Inhibitors:

  1. These are prodrugs that require activation in acid
  2. Covalent and irreversible binding; long duration of action
  3. Most potent suppressors. Reduce by 80-95%
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8
Q

Proton Pump Inhibitors:

Drugs?

A

Proton Pump Inhibitors:

a. Omeprazole
b. Esomeprazole
c. Rabeprazole
d. Lansoprazole
e. Pantoprazole

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9
Q

Proton Pump Inhibitors:

Conversion of drug to a ____ in the acidic secretory canaliculi of the ___ cell. The ___ interacts covalently with ___ groups in the proton pump, thereby ___ inhibiting its activity.

A

Proton Pump Inhibitors:

Conversion of drug to a sulfenamide in the acidic secretory canaliculi of the parietal cell. The sulfenamide interacts covalently with sulfhydryl groups in the proton pump, thereby irreversibly inhibition its activity.

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10
Q

Proton Pump Inhibitors:

Therapeutic uses?

A

Proton Pump Inhibitors:

a. Promote healing of ulcers
b. Treat GERD
c. Treat erosive esophagitis
d. Treat pathological hypersecretory conditions (Zollinger-Ellison)
e. Reduce risk of duodenal ulcers with H. pylori infection

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11
Q

Proton Pump Inhibitors:

  1. Lansoprazole specific FDA approval for?
  2. Omeprazole is safe and effective for treatment of ____ ___ and ___ in who?
A

Proton Pump Inhibitors:

  1. Lansoprazole - treatment and prevention of recurrence of NSAID-associated gastric ulcers
  2. Omeprazole is safe and effective treatment of erosive esophagitis and GERD in CHILDREN
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12
Q

Proton Pump Inhibitors:

General side effects?

Significant-ish side effect?

A

Proton Pump Inhibitors:

SE: nausea, abdominal pain, constipation, flatulence, and diarrhea

Significant: Hypergastrinemia - rebound hyperacidity and tumors

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13
Q

Proton Pump Inhibitors:

Drug interactions: what drugs?

A

Proton Pump Inhibitors:

Interaction with warfarin, diazepam, and cyclosporine

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14
Q

Proton Pump Inhibitors:

What drugs cannot be combined with warfarin?

A

Proton Pump Inhibitors:

Omeprazole, esomeprazole, rabeprazole, lansoprazole

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15
Q

Proton Pump Inhibitors:

What drugs cannot be combined with diazepam?

A

Proton Pump Inhibitors:

Omeprazole and esomeprazole

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16
Q

Proton Pump Inhibitors:

What drugs cannot be combined with cyclosporine?

A

Proton Pump Inhibitors:

Omeprazole and rabeprazole

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17
Q

H2 receptor antagonists:

  1. Interaction with H2 receptor? What membrane?
  2. Suppress secretion by ___%.
  3. Predominantly inhibit? When is this good?
A

H2 receptor antagonists:

  1. Reversible competitive inhibition on the basolateral membrane
  2. Suppress secretion by 70%
  3. Predominantly inhibit basal acid secretion - good during sleep
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18
Q

H2 receptor antagonists:

Drugs?

A

H2 receptor antagonists:

a. Cimetidine
b. Rantidine (most common)
c. Famotidine (most common)
d. Nizatidine

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19
Q

H2 receptor antagonists:

Therapeutic uses? (3)

A

H2 receptor antagonists:

Therapeutic uses:

a. Promote healing of ulcers
b. Treatment of uncomplicated GERD
c. Prevention of stress ulcers

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20
Q

H2 receptor antagonists:

Side effects?

What is common and likely accounts for loss of effectiveness? Occurs after how long?

A

H2 receptor antagonists:

SE: diarrhea, HA, drowsiness, fatigue, muscle pain, constipation

Tolerance can develop within 3 days and decrease effectiveness

21
Q

H2 receptor antagonists:

Why has cimetidine declined for clinical use?

A

H2 receptor antagonists:

Cimetidine inhibits CYPs which decrease its use

22
Q

Prostaglandin Analogs:

  1. PGs stimulate?
  2. PGs decrease?
  3. PGE2 also stimulates?
A

Prostaglandin Analogs:

  1. Stimulate Gi pathway in gastric mucosa
  2. Decrease intracellular cAMP and H+ secretion
  3. PGE2 also stimulates mucin pdtn, bicarbonate secretion, and increases mucosal blood flow
23
Q

Prostaglandin Analogs:

Drug?

A

Prostaglandin Analogs:

Misoprostol

24
Q

Prostaglandin Analogs:

Misoprostol:

This is a synthetic analog of ____. It can reduce basal and food stimulated acid secretion by ___%.

A

Prostaglandin Analogs:

Misoprostol

Synthetic analog of PGE1. Reduce by 75-90%

25
Q

Prostaglandin Analogs:

  1. Misoprostol therapeutic use?
  2. Why is it rarely used?
A

Prostaglandin Analogs:

  1. Prevents NSAID-induced mucosal injury and nonsurgical abortion
  2. Rarely used bc of adverse effects and need for 4 times daily dosing.
26
Q

Prostaglandin Analogs:

  1. Adverse effects?
  2. Contraindications?
A

Prostaglandin Analogs:

  1. Diarrhea
  2. Contraindicated in IBS and pregnant women (promotes uterine contraction)
27
Q

Coating agents:

In the presence of gastric acid, ___ mediated hydrolysis of ___ proteins contributes to mucosal ___ and ulceration. What can inhibit this process?

A

Coating agents:

In the presence of gastric acid, pepsin-mediated hydrolysis of mucosal proteins contributes to mucosal erosion and ulceration. This can be inhibited by sulfated polysaccharides

28
Q

Coating agents:

Drug?

A

Coating agents:

Sucralfate

29
Q

Coating agents:

  1. Sucralfate is a combination of?
  2. MOA?
A

Coating agents:

  1. Combo of octasulfate of sucrose and Al(OH)3
  2. At low pH it undergoes extensive cross-linking and creates a viscous polymer that sticks to damaged tissue and provides physical protection
30
Q

Coating agents:

  1. May also stimulate ___ synthesis and ____ __ ___ locally.
  2. Use?
A

Coating agents:

  1. May also stimulate PG synthesis and epidermal growth factor locally.
  2. NOT used for peptic acid disease but other conditions in the alimentary tract (such as oral mucositis or proctitis and bile reflux)
31
Q

Coating agents:

Adverse Effects?

Contraindications?

A

Coating agents:

SE: constipation

Contraindicated in patients with renal failure (to avoid aluminum overload) and aluminum-containing antacids

32
Q

Antacids:

Main action?

A

Antacids:

Function is to relieve symptoms

33
Q

Antacids:

Speed of reaction of Mg++ hydroxides?

Speed of reaction of Al+++ hydroxides?

A

Antacids:

Mg++ is rapidly reacting

Al+++ is slowly reacting

34
Q

Antacids:

What agents are high in Mg++ only?

A

Antacids:

Mg++ only = Milk of magnesia

35
Q

Antacids:

What drugs are high in Al+++ only?

A

Antacids:

Al+++ = Riopan plus double strength and magaldrate

36
Q

Antacids:

CaCO3 rapidly and effectively neutralizes gastric H+:

However what can its released products cause?

A

Antacids:

CaCO3:

Releases CO2 = belching, nausea, abdominal distention, and flatulence

Releases Calcium = can induce rebound acid secretion

37
Q

Antacids:

What drugs are high in CaCO3?

A

Antacids:

CaCO3 = maalox quick dissolve, calcium rich rolaids, and tums

38
Q

Antacids:

What causes constipation?

What causes diarrhea?

A

Antacids:

Constipation = Al+++

Diarrhea = Mg++

39
Q

Antacids:

What drugs have both Mg++ and Al+++?

A

Antacids:

Both Mg++ and Al+++

a. gelusil
b. mylanta

40
Q

Antacids:

What is simethicone and what does it do?

A

Antacids:

Simethicone is a surfactant that may decrease foaming and esophageal reflux

41
Q

Antacids:

Drugs high in simethicone?

A

Antacids:

Drugs high in simethicone:

a. Gelusil
b. mylanta

42
Q

Antacids:

Adverse effects of Al+++ and Mg++? Thus should not be taken with?

A

Antacids:

Adverse effects (other than constipation/diarrhea):

May chelate drugs in the GI tract causing the formation of insoluble (thus unabsorbable) complexes.

These should not be taken with other drugs!!!!!

43
Q

Antacids:

Some antacids contain ___ which is contraindicated! Why?

A

Antacids:

Some contain aspirin and its contraindicated because it can increase severity or generate ulcers

44
Q

Bismuth compounts:

Example of drug?

What are they prescribed in combination for?

What do they promote production of in an ulcer?

A

Bismuth compounts:

Pepto bismol

Prescribed with abx for H. pylori because they are antibacterial

Promote mucin and bicarb production in ulcers

45
Q

GERD:

What can occur when the LES is damaged?

GERD is a ____ disorder that requires ___ term therapy.

A

GERD:

Damage: erosive esophagitis, pain, dyspepsia, and barrets esophagus that can lead to esophageal cancer that is INCURABLE

GERD is a chronic disorder that requires long term therapy

46
Q

GERD:

Stage 1:

Episodes? Other symptoms?

Management?

A

GERD:

Stage 1:

Less than 2-3 episodes per week. No other symptoms

Lifestyle modification and antacids/H2 antagonists as needed

47
Q

GERD:

Stage II:

Episodes per week? Other symptoms?

Treatment?

A

GERD:

Stage II:

Greater than 2-3 episodes per week; w/ or w/o esophagitis

Treat with proton pump inhibitors

48
Q

GERD:

Stage III:

Episodes? Symptoms?

Managements?

A

GERD:

Stage III:

Chronic, unrelenting symptoms, immediate relapse off therapy. Esophageal complications

Proton pump inhibitors once or twice a day

Pharmacology (24 decks)

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