Proton Pump Inhibitors

PROTON PUMP INHIBITORS

Q. 1

Action of Proton pump inhibitors are most effective when they are given:

 A

After meals

 B

Shortly before meals

 C

Along with H2 blockers

 D

During prolonged fasting periods

Q. 1

Action of Proton pump inhibitors are most effective when they are given:

 A

After meals

 B

Shortly before meals

 C

Along with H2 blockers

 D

During prolonged fasting periods

Ans. B

Explanation:

Proton pump inhibitors should be taken 15-30 minutes before meals.

This allows absorption of the medication to provide availability to the proton pumps when they are activated by the meal.

This drug when taken before meals provide the best intragastric pH control.

PPIs are inactive at neutral pH. At pH < 5 the drug rearranges into two charged cationic forms (a sulfenic acid and a sulphenamide configuration). They react covalently with SH group of the H+ K+ ATPase enzyme and inactivate it irreversibly. Acid secretion resumes when new H+ K+ ATPase molecules are synthesized.

Ref: Advanced Therapy in Gastroenterology and Liver Disease By Theodore M. Bayless, 5th Edition, Page 56 ; Essentials of Medical Pharmacology By K D Tripathi, 5th Edition, Page 593


Q. 2

What is the treatment of choice in duodenal ulcer without any complication of hemorrhage?

 A

Highly selective vagotomy

 B

Trunkal vagotomy

 C

Proton pump inhibitors

 D

None

Q. 2

What is the treatment of choice in duodenal ulcer without any complication of hemorrhage?

 A

Highly selective vagotomy

 B

Trunkal vagotomy

 C

Proton pump inhibitors

 D

None

Ans. C

Explanation:

Proton pump inhibitors like Omeprazole can produce relief  in patients with duodenal ulcer. 

Perforation complicates duodenal ulcer about half as often as bleeding and most perforated ulcers are on the anterior surface of the duodenum.

The patient population tends to be elderly (mean age 60–70), chronically, ill patients often (40–50%) taking ulcerogenic medication.

Helicobacter pylori is implicated in 70–92% of all perforated duodenal ulcers even if those secondary to Non-Steroidal Antiinflammatory Drugs are included.

The second most common cause of perforated duodenal ulcer is the ingestion of Non-Steroidal Antiinflammatory drugs.

 The traditional management of a perforated duodenal ulcer has been a Graham Omental Patch and a thorough abdominal lavage.

Q. 3

. Clostridium difficale infection occurs after ‑

 A

After prolong antibiotic therapy 

 B

Pantoprazole increases the risk

 C

Associated with use of rectal thermometer

 D

All

Q. 3

. Clostridium difficale infection occurs after ‑

 A

After prolong antibiotic therapy 

 B

Pantoprazole increases the risk

 C

Associated with use of rectal thermometer

 D

All

Ans. D

Explanation:

Ans. is ‘a’ i.e., After prolong antibiotic therapy, ‘b’ i.e., Pantoprazole increases the risk, ‘c’ i.e.,

Associated with use of rectal thermometer 

Quiz In Between


Q. 4

Acetyl salicylate & phenobarbitone are better absorbed from stomach because they are-

 A

Weak acids remain non-ionic in gastric pH

 B

Weak acids remain ionic in gastric pH

 C

Strong acids fully ionised in gastric pH

 D

Weak bases which are ionised at gastric pH

Q. 4

Acetyl salicylate & phenobarbitone are better absorbed from stomach because they are-

 A

Weak acids remain non-ionic in gastric pH

 B

Weak acids remain ionic in gastric pH

 C

Strong acids fully ionised in gastric pH

 D

Weak bases which are ionised at gastric pH

Ans. A

Explanation:

Ans. is ‘a’ i.e., Weak acids remain non-ionic at gastric pH

Remember simple funda :

When the medium is same drugs can cross the membrane:

i) Acidic drugs can cross the membrane in acidic medium, i.e., acidic drugs are unionized at acidic pH and are lipid soluble —> so, in stomach acidic drugs are absorbed.

ii) Basic drugs can cross the membrane in basic medium, i.e., basic drugs are unionized at alkaline pH and are lipid soluble —> so, in intestine basic drugs are absorbed.


Q. 5

Omeprazole act by inhibiting –

 A

Nall+ATPase

 B

NalCATPase

 C

Calcium channels

 D

1-11K+ATPase

Q. 5

Omeprazole act by inhibiting –

 A

Nall+ATPase

 B

NalCATPase

 C

Calcium channels

 D

1-11K+ATPase

Ans. D

Explanation:

Ans. is ‘d’ i.e., HICATPase


Q. 6

Which of following is a proton pump inhibitor

 A

Magnesium carbonate

 B

Ranitidine

 C

Omeprazole

 D

Sucralfate

Q. 6

Which of following is a proton pump inhibitor

 A

Magnesium carbonate

 B

Ranitidine

 C

Omeprazole

 D

Sucralfate

Ans. C

Explanation:

Ans. is ‘c’ i.e., Omeprazole

Quiz In Between


Q. 7

Proton pump inhibitors are most effective when they are given –

 A

After meals

 B

Shortly before meals

 C

Along with H2 blockers

 D

During prolonged fasting periods

Q. 7

Proton pump inhibitors are most effective when they are given –

 A

After meals

 B

Shortly before meals

 C

Along with H2 blockers

 D

During prolonged fasting periods

Ans. B

Explanation:

Ans. is ‘b’ i.e., Shortly before meals

o Bioavailibility of all PPIs is reduced by food; they should be taken in empty stomach, followed 1 hour later by a meal to activate 1-1+ ATPase and make it more susceptible to the PPI.

o PPIs should be administered approximately 1 hour before a meal (usually breakfast) so that the peak serum concentration coincides with the maximal activity of proton pump secretion.


Q. 8

Drug of choice for Zollinger-Ellison syndrome

 A

Antihistaminics

 B

Proton pump inhibitors

 C

Dopamine agonists

 D

Antacids

Q. 8

Drug of choice for Zollinger-Ellison syndrome

 A

Antihistaminics

 B

Proton pump inhibitors

 C

Dopamine agonists

 D

Antacids

Ans. B

Explanation:

Ans. is ‘b’ i.e., Proton pump inhibitors

“Proton pump inhibitors are the drug of choice for Zollinger Ellison syndrome; they have decreased the need for total gastrectomy”.


Q. 9

Which group of drugs is most effective for the healing of Non steroidal Anti Inflammatory Drug (NSAID) induced gastric ulcer-

 A

Prostaglandin analogues

 B

H2-receptor antagonists

 C

Proton pump inhibitors

 D

Antacids

Q. 9

Which group of drugs is most effective for the healing of Non steroidal Anti Inflammatory Drug (NSAID) induced gastric ulcer-

 A

Prostaglandin analogues

 B

H2-receptor antagonists

 C

Proton pump inhibitors

 D

Antacids

Ans. C

Explanation:

Ans. is ‘c’ i.e., Proton pump inhibitors

o Drug of choice for NSAIDs induced peptic ulcer —> PPIs

o Most specific drug for NSAIDs induced peptic ulcer —> Prostaglandin analogue.

Quiz In Between


Q. 10

All of the following are true regarding a patient with acid peptic disease except

 A

Misoprostol is the drug of choice in patients on NSAIDS

 B

DU is preventable by the use of single night time H2 blockers

 C

Omeprazole may help ulcers refractory to H2 blockers

 D

Misoprostol is DOC in pregnant patients

Q. 10

All of the following are true regarding a patient with acid peptic disease except

 A

Misoprostol is the drug of choice in patients on NSAIDS

 B

DU is preventable by the use of single night time H2 blockers

 C

Omeprazole may help ulcers refractory to H2 blockers

 D

Misoprostol is DOC in pregnant patients

Ans. D

Explanation:

Answer is D (Misoprostol is Drug of choice in pregnant patients)

Stimulant effect of Misoprostol on the uterus makes it contraindicated in women of child bearing age.

  • The prostaglandin analogue misoprostol is effective in the prevention of NSAID induced gastric and duodenal ulcer° and is the only agent approved by the FDA for this purposeQ CMDT-2001/609
  • Misoprostol causes a dose dependent diarrhea and its stimulant effect on the uterus makes it contraindicated in women of child bearing age°. Katzung 8th/1068
  • H2 receptor antagonist : whereas previous recommendations were to administer these agents at least twice a day, a single bed time dose may be just as effective and may elicit better compliance – Katzung

For uncomplicated peptic ulcers, H2 receptor antagonists may be administered twice daily or once daily at bed time, with equivalent efficacy- CMDT 2001

  • Proton pump inhibitors (Omeprazole) : They are superior to H2 receptor antagonists and to misoprostol in the healing of NSAID induced gastric ulcer.

– Compared to H2 Receptor antagonists, proton pump inhibitor provide faster pain relief and more rapid ulcer healing.

  • Alternate pharmacological approaches to failure of an H2 blocker include :

– using a higher dose of the same H2 blocker.

– switching to another H2 receptor antagonist

switching to a proton pump inhibitere (Omeprazole)


Q. 11

Omeprazole effects are due to:   

March 2013

 A

Prostaglandin analogue

 B

H, antihistamines

 C

Proton pump inhibitor

 D

Ulcer protective mechanism

Q. 11

Omeprazole effects are due to:   

March 2013

 A

Prostaglandin analogue

 B

H, antihistamines

 C

Proton pump inhibitor

 D

Ulcer protective mechanism

Ans. C

Explanation:

Ans. C i.e. Proton pump inhibitor

Omeprazole

  • It is a proton pump inhibitor used in the treatment of:

–        Dyspepsia,

–        Peptic ulcer disease (PUD),

–        Gastroesophageal reflux disease (GORD/GERD),

–        Laryngopharyngeal reflux (LPR) and

–        Zollinger-Ellison syndrome.


Q. 12

Unfavorable interaction of drug and substrate in human beings are all except:

 A

Omeprazole reduces stomach acid

 B

Methotrexate inhibiting folate

 C

Barbiturates decreases B 12 absorption

 D

Retinoic acid inhibits vitamin E

Q. 12

Unfavorable interaction of drug and substrate in human beings are all except:

 A

Omeprazole reduces stomach acid

 B

Methotrexate inhibiting folate

 C

Barbiturates decreases B 12 absorption

 D

Retinoic acid inhibits vitamin E

Ans. A

Explanation:

Ans. a. Omeprazole reduces stomach acid

Omeprazole reduces stomach acid secretion:

This interaction is beneficial for patients suffering from GERD without having any associated complications.

  • Rest three interactions has a bad impact on the normal healthy individuals.
  • Methotrexate inhibiting folate
  • Barbiturates decreases 13,2 absorption
  • Retinoic acid inhibits vitamin E

Quiz In Between


Q. 13

Despite their short half-lives (2 hours), Proton pump Inhibitors (PPIs) cause a prolonged suppression of acid secretion (up to 48 hours) because:

 A

They are prodrugs and undergo activation gradually

 B

They exit from the plasma and enter acid secretory canaliculi and stay there, blocking the secretion of acid for a long time

 C

They irreversibly inhibit the proton pump molecule and hence, acid secretion requires synthesis of new proton pumps

 D

They are available as enteric coated capsules, from which drug is gradually released

Q. 13

Despite their short half-lives (2 hours), Proton pump Inhibitors (PPIs) cause a prolonged suppression of acid secretion (up to 48 hours) because:

 A

They are prodrugs and undergo activation gradually

 B

They exit from the plasma and enter acid secretory canaliculi and stay there, blocking the secretion of acid for a long time

 C

They irreversibly inhibit the proton pump molecule and hence, acid secretion requires synthesis of new proton pumps

 D

They are available as enteric coated capsules, from which drug is gradually released

Ans. C

Explanation:

Ans. c. They irreversibly inhibit the proton pump molecule and hence, acid secretion requires synthesis of new proton pumps

  • “Proton pump inhibitors (PPIs) are prodrugs that require activation in an acidic environment. After absorption into the systemic circulation, the prodrug diffuses into the parietal cells of the stomach and accumulates in the acid secretory cancliculi. Here, it is activated by the proton catalyzed formation of a tetracyclic sulfenamide, trapping the drug so that it cannot diffuse back across the canalicular membrane. The activated form then binds covalently with the sulfhydryl groups of cysteines in the Irr-ATPase, irreversibly inactivating the pump molecule. Acid secretion resumes only after new pump molecules are synthesized and inserted into the luminal membrane, providing a prolonged (up to 24 to 48 hour) suppression of acid secretion, despite the much shorter plasma half-lives (0.5-2 hour) of the parent compounds. Because they block the final step in acid production, the PPIs are effective in acid suppression regardless of other stimulating factors.”- Goodman and Gilman 12/e p1311

Proton Pump Inhibitors

  • Most potent antisecretory agents, substituted benzimidazoles, also known as the proton pump inhibitorse.
  • Covalently bind to the catalytic subunit of the proton pump and negate all types of acid secretione
  • PPIs provide more complete inhibition of acid secretion than the H2-receptor antagonistse
  • Inhibition of acid secretion is also more prolonged because of the irreversible inhibition of the enzyme caused by the covalent bond to the proton pump°.
  • PPIs are more effective during the day, generally prescribed before breakfast°.
  • PPIs require an acidic environmente within the gastric lumen in order to become activated and bind to the proton pump at the secretary canaliculus
  • Utilization of antacids or 112-receptor antagonists in combination with PPIs could have deleterious effects by promoting an alkaline environment and thereby preventing activation of the PPP.
  • Consequently antacids and 112-receptor antagonists should not be used in combination with PPIse.

Q. 14

Which proton pump inhibitor can be used IV

 A

Omeprazole

 B

Rabeprazole

 C

Pantoprazole

 D

Fomeprazole

Q. 14

Which proton pump inhibitor can be used IV

 A

Omeprazole

 B

Rabeprazole

 C

Pantoprazole

 D

Fomeprazole

Ans. C

Explanation:

Ans. is ‘c’ i.e., Pantoprazole

  • Pantaprazole – it is more acid stable and has higher oral bioavailability. It is also available for i.v. administration; particularly employed in bleeding peptic ulcer and for prophylaxis of acute stress ulcers.

Quiz In Between



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