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1

PPI

  • Bioavailability of all agents is decreased by what? 
  • How is this fixed?****

 

  • Bioavailability of all agents is decreased by what? 
  • How is this fixed?****

 

  • Food***
  • Administer approximately 30 - 60 mins BEFORE a meal (usually breakfast)***

(Know this)

2

PK of PPIs

  • Acid inhibition lasts up to __ hours. 
  • How many hours are required for synthesis of new H+/K+-ATPase pump molecules
  • Undergo which rapid 1st pass systemic effect?
  • Which type of clearance neglible? 

Acid inhibition lasts up to 24 hours. 

 

hours required for synthesis of new H+/K+-ATPase pump molecules: 18 hours

 

1st pass hepatic

3

PK of PPIs

  • Dose reduction in pts w/ what condition?

  • Severe liver impairment

4

Which nerve stimulates postganglionic neurons of the enteric nervous system to release acetylcholine (ACh), which binds to M3 receptors on parietal cells and ECL cell?

Vagus

5

3 SE of PPIs

  • Diarrhea**
  • HA
  • Abdominal pain

6

PPI adverse effects

  • Acid is important in releasing what from food?
  • Acid also promotes absorption of what 3 food bound minerals?*** 
    • What should you monitor?
    • What could you supplement with?

  • Releasing B12 from food
  • 3 food-bound minerals: iron, Ca, Mg*** (know this)
  • Monitor: bone density
  • Ca supplements

7

Adverse effects of which agent?

  • Community-acquired respiratory infections and nosocomial pneumonia
  • 2- to 3-fold increased risk for hospital- and community-acquired Clostridium difficile infection
  • Salmonella, Shigella, E coli, Campylobacter

PPI

8

PPI Drug Interactions

  • Decreased gastric acidity may alter absorption of what 4 drugs? Which drug especially?**

  • Ketoconazole
  • Itraconazole
  • Digoxin***
  • Atazanavir

"A KID"

9

PPI Drug Interactions

Omeprazole may inhibit the metabolism of what 3 drugs? 

  • Warfarin***
  • Diazepam
  • Phenytoin

"Omeprazole went to War w/ P. diddy"

10

PPI Drug Interactions

  • Which 2 PPIs have no significant drug interactions?

  • Rabeprazole
  • Pantoprazole

"A rabbi wearing pants is getting no action..."

11

PPI Drug Interactions

  • Metabolized by P450 cytochromes
  • What is the "prodrug" which requires activation by the hepatic P450 CYP2C19?
  • PPIs could reduce activation of what drug?

  • Clopidogrel
  • Clopidogrel

12

PPI Drug Interactions

  • Which 2 PPIs are preferred bc/ of minimal CYP2C10 inhibition?

Rabeprazole & Pantoprazole

"Rabbi wearing Pants"

13

Mucosal Protective Agents

  • Gastroduodenal mucosa evolved defense mechanisms to protect itself against the noxious effects of what 2 substance?

  • acid & pepsin

14

What substance appears to be important in stimulating mucus and bicarbonate secretion and mucosal blood flow?

Mucosal prostaglandins

15

What are the 3 Mucosal Protective Agents

•Sucralfate

•Prostaglandin analogs

•Bismuth

16

Which Mucosal Protective Agent?

•Salt of sucrose complexed to sulfated aluminum hydroxide

•forms a viscous, tenacious paste that binds selectively to ulcers or erosions for up to 6 hours

Sucralfate

17

Which Mucosal Protective Agent?

Negatively charged sucrose sulfate binds to positively charged proteins in the base of ulcers or erosion

•Forms a physical barrier that restricts caustic damage

Stimulates mucosal prostaglandin and bicarbonate secretion

Sucralfate

18

Which Mucosal Protective Agent?

  • Used to prevent stress-related bleeding

Sucralfate

19

Adverse effects of which Mucosal Protective Agent?

  • Small amount of aluminum is absorbed
  • Do not be used for prolonged periods in patients with renal insufficiency

Sucralfate

20

Prostaglandin Analogs

  • What are the 2 primary prostaglandins?

E & F

21

What is the name of a prostaglandin analog? (Methyl Analog of PGE1)

Misoprostol

22

Misoprostol (prostaglandin analog)

  • Metabolized to what?
  • Serum half life is how long?
  • Excreted how?

  • Metabolized to a metabolically active free acid
  • Half life: less than 30 mins
  • Excreted in the urine

23

T/F

  • Dose reduction of Misoprostol is NOT needed in pts w/ renal insufficiency

True

24

Prostaglandin Analogs: Misoprostol

Pharmacodynamics

  • Has what 2 properties? 
  • Binds to prostaglandin receptor on parietal cells, reducing histamine stimulated _____ production and causing modest acid inhibition
  • Prostaglandins stimulate what 3 things?

 

Prostaglandin Analogs: Misoprostol

Has what 2 properties? 

Acid inhibitory & Mucosal protective properties

Binds to prostaglandin receptor on parietal cells, reducing histamine stimulated cAMP production and causing modest acid inhibition

Prostaglandins stimulate what 3 things?

1. Intestinal electrolyte & fluid secretion

2. Intestinal motility 

3. Uterine contractions

25

Which medication? 

 

Reduces the incidence of NSAID-induced ulcers 

Misoprostal

(Prostaglandin Analog)

26

Adverse reactions of which medication? 

 

uterine contractions

do not use in pregnancy/childbearing women unless they have a neg. serum pregnancy test and on effective contraceptive measures

Misoprostol 

(Prostaglandin Analog)

27

What are the 2 bismuth compounds? 

  • bismuth subsalicylate
  • bismuth subcitrate potassium

28

Which bismuth compound? 

  • combination prescription product that also contains metronidazole and tetracycline for the treatment of H pylori.

bismuth subcitrate potassium

29

Bismuth

 

  • Over 99% of bismuth appears where? 
  • What substance is (like ASA), readily absorbed and excreted in the urine

 

  • in the stool
  • Salicylate

30

Bismuth Compounds

  • May stimulate what 3 things?
  • Which bismuth reduces stool frequency and liquidity in acute infectious diarrhea? 

  • secretion of: prostaglandin, mucus, bicarbonate
  • Bismuth subsalicylate