Drugs For Peptic Ulcer Question And Answers

Drugs For Peptic Ulcer

 

Question 1. Write Classification And Uses Of Drugs Inhibiting Gastric Acidity.
Or
Mention Classification And Uses Of Acid Antisecretory Drugs.
Or
Write A Short Note On Drugs Decreasing The Gastric Acidity.
Or
Classify The Drugs Used For Peptic Ulcer.
Answer:

Classification Of Drugs

1. Reduction Of Gastric Acid Secretion

• H₂ antihistaminics: Cimetidine, ranitidine, famotidine, roxatidine, and loxatidine.
• Proton pump inhibitor: Omeprazole, lansoprazole, pantoprazole, rabeprazole and esomeprazole.
• Anticholinergic agents: Pirenzepine, propantheline, and oxyphenonium
• Prostaglandin analogs: Misoprostol.

Read And Learn More: Pharmacology Question And Answers

2. Neutralization of gastric acid (Antacids)

• Systemic antacids: Sodium bicarbonate, sodium citrate
• Nonsystemic antacids: Aluminum hydroxide, magnesium hydroxide, magnesium trisilicate, magaldrate, calcium carbonate

3. Ulcer protective: Sucralfate, Colloidal Bismuth substrate

4. Ulcer healing drugs: Carbenoloxone

5. Anti-H. pylori drugs: Amoxicillin, clarithromycin, metronidazole, tinidazole, and tetracycline.

Drugs Inhibiting Gastric Acidity Uses

• They are used to prevent gastric acid secretion.
• They are used in controlling pain during gastric ulcers and duodenal ulcers.
• They are used in preventing bleeding from gastric ulcers.
• They are used in gastroesophageal reflux disease.
• They are used in controlling hyperacidity during ZollingerEllison syndrome.

Question 2. Write A Short Note On The H₂ Receptor Antagonist.
Or
Describe The Pharmacology Of Omeprazole.
Answer:

H₂  receptor antagonist/H₂ blockers competitively block the effects of histamine on H₂ receptors. They include cimetidine, ranitidine, famotidine, roxatidine, and loxatidine.

• They inhibit basal, food-stimulated, and nocturnal gastric acid secretion and are effective in promoting the healing of peptic ulcers and preventing their recurrence.
• These drugs are used for the treatment of peptic ulcer disease, Zollinger-Ellison syndrome, gastroesophageal reflux disease, and the prevention of stress-induced ulcers.
• Cimetidine was the first  H₂ blocker to be introduced.
• The interaction of H₂ receptor antagonists with H₂ receptors has been found competitive in the case of cimetidine, ranitidine, and roxatidine and non-competitive in the case of loxatidine.
• They are highly selective and have no effect on H₁ -mediated responses.

Question 3. Write A Short Note On Ranitidine.
Answer:

Ranitidine is a H₂ blocker. It is introduced subsequent to cimetidine as nonimidazole.

• Ranitidine is 5 times more potent than cimetidine.
• It has nonandrogenic action and does not produce any effect on male sexual function or gynecomastia.
• It has lesser permeability into the brain.
• It does not significantly inhibit the hepatic metabolism of other drugs.
• Its overall incidence of side effects i.e. headache, diarrhea, and dizziness is lower. Rashes are infrequent.

Ranitidine Dosage

Orally

• For ulcer healing 300 mg at bedtime. For maintenance 150 mg at bedtime.
• Parenterally: 50 mg IM or slow IV in. every 6–8 hours.

Ranitidine Uses

• In peptic ulcer, i.e. duodenal and gastric ulcer
• In stress ulcers
• In gastritis
• In Zollinger-Ellison syndrome
• In gastroesophageal reflux disease
• It is used preoperatively to reduce the risk of aspiration pneumonia.

Question 4. Write A Short Note On Omeprazole.
Answer:

Omeprazole is a proton pump inhibitor that inhibits a common step in gastric acid secretion.

• Omeprazole is inactive at neutral PH and active at a pH of less than 5.

Omeprazole Mechanism Of Action

Omeprazole is a prodrug that generates an active form at acidic pH. Omeprazole is absorbed in the small intestine move in blood and diffuses in the canaliculi of the parietal cell and converts to sulfonamide which is the active form of the drug.

The active form binds covalently with the SH group of H⁺-K⁺-ATPase (proton pump) and irreversibly inactivates it. So because of irreversible inhibition, gastric acid secretion is inhibited for 24 hours irrespectively of their half-life.

Omeprazole Uses

• Omeprazole 20 mg OD is more effective than H₂ blockers on ulcers. Continued treatment can prevent relapse. It also controls bleeding from peptic ulcers.
• It is more effective than H₂ blockers in healing of esophageal lesions.
• It controls hyperacidity in Zollinger-Ellison syndrome.
• It is the choice of drug for peptic ulcer due to any etiology even NSAID induced.
• It is used in stress ulcers.

Omeprazole Adverse Effects

• Headache
• Diarrhea
• Abdominal pain
• Long-term use of proton pump inhibitors decreases vitamin B₁₂ absorption and increases the risk of infection and osteoporosis.
• Chronic use can cause hypergastrinemia which can cause gastric tumor
• Gynecomastia and erectile dysfunction.

Question 5. Describe The Pharmacological Basis Of Omeprazole In Peptic Ulcers.
Or
Describe The Pharmacological Actions And Adverse Reactions Of Anyone With Peptic Ulcer.
Answer:

Omeprazole is a prodrug that generates an active form at acidic pH. Omeprazole is absorbed in the small intestine move in blood and diffuses in the canaliculi of the parietal cell and converts to sulfonamide which is the active form of the drug.

The active form binds covalently with the SH group of H⁺-K⁺-ATPase (proton pump) and irreversibly inactivates it. So because of irreversible inhibition, gastric acid secretion is inhibited for 24 hours irrespectively of their half-life.

Omeprazole inhibits all phases of gastric acid secretion and is the most powerful acid-suppressive agent that’s why it is used in the treatment of peptic ulcer.

Question 6. Compare And Contrast Ranitidine And Omeprazole.
Answer:

Question 7. Write A Short Note On Antacids.
Or
Write In Brief About Antacids.
Answer:

These are the weak bases, which chemically react with gastric acid to form salt and water and reduce gastric acidity immediately.

Antacids Mechanism Of Action

Antacids Classification

Systemic antacids: Sodium bicarbonate, sodium citrate

Nonsystemic antacids: Aluminum hydroxide, magnesium hydroxide, magnesium trisilicate, magaldrate, calcium carbonate

Description Of Antacids

• Systemic antacids are water soluble, their duration of action is short, and they are potent acid neutralizers.
• Non-systemic antacids are insoluble and poorly absorbed. They reach the stomach to form corresponding chloride salt. When it reaches the intestine chloride salt reacts with bicarbonate and bicarbonate is not available for absorption so there is no systemic alkalosis.
• Most of the antacids have either magnesium hydroxide or aluminum hydroxide or calcium carbonate alone or in combination with their main components.
• They are effective in relieving the pain of peptic ulcers. Magnesium-containing antacids can cause diarrhea while aluminum and calcium-containing antacids cause constipation.
• Antacids do not decrease acid production and hence potency of antacids is expressed in terms of their acid-neutralizing capacity.
• Antacids are potent drugs in gastroesophageal reflux disease.
• A combination of two or more antacids is frequently used. They are more effective, for Example. the acid in, digene, elusive, and machine.

Question 8. Compare The Mechanism Of Action, Efficy, And Doses Of Aluminum Hydroxide And Ranitidine.
Answer:

Question 9. Write A Short Note On Famotidine.
Answer:

• Famotidine is an H₂ blocker.
• It blocks the effects of histamine on H₂ receptors and gastric acid secretion is inhibited.
• It binds tightly to H₂ receptors and exhibits a longer duration of action.
• It is five times more potent than ranitidine. It has no antiandrogenic action.
• It has a low affinity for cytochrome P 450 enzyme and drug metabolism modifying property is minimal.
• The duodenal ulcer healing rate is similar to better than cimetidine.
• Drug interactions are negligible.

Famotidine Adverse Effects

The adverse effects are low only headache, dizziness, bowel upset, and rashes are reported.

Famotidine Uses

• In peptic ulcer, i.e. duodenal and gastric ulcer
• In stress ulcers
• In gastritis
• In Zollinger-Ellison syndrome
• In gastroesophageal reflux disease
• It is used preoperatively to reduce the risk of aspiration pneumonia.

Question 10. Enumerate Drugs Used In The Management Of Peptic Ulcer Justifying The Reasons For Use. What Drugs Are To The Avoided In Peptic Ulcer Patients?
Answer:

Drugs Used In The Management Of Peptic Ulcer With Reasons For Their Use

Antacids

These drugs are weak bases that can neutralize gastric HCl. Aluminum hydroxide, legal rate, and magnesium hydroxide are nonsystemic antacids. These are slower but longer-acting drugs.

Drugs Decreasing Acid Secretion

• Proton pump inhibitors (PPIs): These are prodrugs that act by irreversibly inhibiting H⁺ K⁺ ATPase in gastric parietal cells. The drugs in this group are omeprazole, pantoprazole, esomeprazole, Iansoprazole and rabeprazole. PPIs are administered orally in the early morning empty stomach (just before breakfast). These drugs have short half-life but can inhibit acid secretion for more than 24 hours.
• H2 receptor antagonists: These drugs competitively inhibit H₂ receptors in parietal cells, thus inhibiting acid secretion. Acetylcholine and gastrin act partly by causing the release of histamine, therefore acid-secreting capacity of these agents also is decreased by H₂ blockers. Drugs in this group are cimetidine, ranitidine, famotidine, and loratadine.
• Anticholinergics: Pirenzepine and telenzepine are selective M1, blockers that are preferred antimuscarinic agents for peptic ulcer disease as these are devoid of anticholinergic adverse effects.

Drugs Increasing Protective Factors

Prostaglandins act as anti-ulcer agents by stimulating the release of mucus and bicarbonate and by increasing the mucosal blood flow.

Prostaglandins also inhibit H⁺ K⁺  ATPase and decrease the production of acid. Misoprostol is the most effective drug.

Ulcer Protective Agents

These drugs form a covering over the ulcer bed that prevents its exposure to gastric acid. Sucralfate and colloidal bismuth subcitrate are two important ulcer-protective drugs.

• Sucralfate: It is an aluminum salt of sulfated sucrose. It acts only in an acidic medium.
• Colloidal bismuth subcitrate: It forms an acid-resistant coating over the ulcer. It also dislodges H. pylori from the surface of gastric mucosa and kills it.

Ulcer Healing Drugs

Carbenoloxone causes the epithelization of ulcers without decreasing acid production. It can cause sodium and water retention.

Anti-H. Pylori Drugs

H. pylori infection can be detected by “urea breath test”. It is responsible for the relapse of peptic ulcer disease. Drugs used for H.

pylori are metronidazole, tinidazole, amoxicillin, clarithromycin, tetracycline, colloidal bismuth subcitrate, omeprazole, and lansoprazole. These are used as a three-drug combination (triple therapy) for 2 weeks.

Drugs To Be Avoided In Peptic Ulcer Patients

The drugs to be avoided in peptic ulcer patients are:

1. NSAIDs
2. Cholinergic drugs
3. Histamine drugs

• NSAIDs that are to be avoided are aspirin, ibuprofen, diclofenac, etc.
• Cholinergic drugs are to be avoided.
  • Antimuscarinic drugs: Atropine.
  • Neuromuscular locality agent: D Tubocuranine.
  • Ganglion blocking agent: Trimethaphane
• Histaminergic drugs: 5 Hydroxytriptamine, dopamine, morphine, and diazepam.

Question 11. Write A Short Note On Proton Pump Inhibitors.
Or
Write A Long Answer On Proton Pump Inhibitors.
Answer:

Proton pump inhibitors are absorbed in the small intestine move in blood and diffuse in canaliculi of parietal cell and converts to sulfonamide which is the active form of the drug. The active form binds covalently with the SH group of H+-K+-ATPase (proton pump) and irreversibly inactivates it. So because of irreversible inhibition, gastric acid secretion is inhibited for 24 hours irrespectively of their half-life.

• Proton pump inhibitors are the most powerful inhibitors of gastric acid secretion.
• These drugs inhibit both fasting and stimulated acid secretion.
• Proton pump inhibitors act in the final step of acid secretion, so they stop the acid production following the stimulation.
• Proton pump inhibitors should be given orally 30 minutes before meals because food stimulates the secretion of acid which is necessary for activation of proton pump inhibitors. But food also decreases the absorption of proton pump inhibitors as acid secreted by it produces acidic pH, due to this proton pump inhibitors are given as enteric-coated tablets to prevent acid in the stomach.
• Esomeprazole, pantoprazole, and lansoprazole have high oral bioavailability as compared to omeprazole.
• Parenteral formulations are present for esomeprazole, lansoprazole, pantoprazole and rabeprazole.

Proton Pump Inhibitors Uses

• Peptic ulcer: Omeprazole 20 mg and lansoprazole 30 mg are given once daily. Duodenal ulcers require 4-week therapy and gastric ulcers require 6 to 8 weeks of therapy.
• In acute bleeding ulcers: IV esomeprazole, lansoprazole, and pantoprazole can be given which suppresses acid secretion and promotes healing.
• In H. pylori-associated ulcers: Combined therapy of two or three anti-microbials with proton pump inhibitor is more effective.
• Stress ulcers: Prophylactic use of IV proton pump inhibitors decreases the incidence of stress ulcers in critically ill patients.
• In NSAID-induced ulcers: Proton pump inhibitors are the most effective drugs.
• In aspiration pneumonia: Proton pump inhibitors are the drugs used preoperatively to decrease the risk of aspiration pneumonia.
• In Zollinger­Ellison syndrome: Proton pump inhibitors are the choice of drugs. Higher doses are needed for the healing of ulcers.
• In gastroesophageal reflux disease: Proton pump inhibitors are the drug of choice in gastroesophageal reflux disease and are given once daily.

Proton Pump Inhibitors Adverse Effects

• Headache
• Diarrhea
• Abdominal pain
• Long-term use of proton pump inhibitors decreases vitamin B₁₂ absorption and increases the risk of infection and osteoporosis.
• Chronic use can cause hypergastrinemia which can cause gastric tumor
• Gynecomastia and erectile dysfunction are reported with omeprazole.

Proton Pump Inhibitors Drug Interactions

• Omeprazole inhibits the metabolism of drugs like warfarin, phenytoin, and diazepam.
• Proton pump inhibitors decrease the bioavailability of itraconazole, iron salt, etc.

Question 12. Explain The Pharmacological Basis For Magnesium Hydroxide Antacid Combined With Aluminum Hydroxide Antacid.
Or
Explain Why Magnesium And Aluminium Containing Antacids Are Given In Combination?
Answer:

Magnesium hydroxide antacid is combined with aluminum hydroxide antacid because:

• Magnesium hydroxide is fast acting whereas aluminum hydroxide has slow but sustained action. The combination of both provides a rapid and sustained acid-neutralizing capacity.
• Aluminum can relax gastric and intestinal smooth muscle producing delayed gastric emptying and constipation whereas magnesium causes an increase in bowel motility and acts as a laxative.

Thus the field combinations of magnesium and aluminum counteract the adverse effects of each other on bowel movements.

The combination leads to a reduction in the dose of the individual components and thus, lowering of systemic toxicity of the drugs.

Question 13. Describe Drugs Used To Treat Duodenal Ulcer.
Answer:

Physicians treat duodenal ulcers with several types of medications, including the following:

• H₂-blockers reduce the amount of acid the stomach produces by blocking histamine, a powerful stimulant of acid secretion, for Example. ranitidine, famotidine
• Proton pump inhibitors more completely block stomach acid production by stopping the stomach’s acid pump—the final step of acid secretion, for Example. omeprazole, pantoprazole
• Mucosal protective agents shield the stomach’s mucous lining from the damage of acid but do not inhibit the release of acid, for Example. Sucralfate

When treating H. pylori, these medications or procedures are often used in combination with antibiotics, for Example. Amoxicillin + Tinidazole + Omeprazole; Amoxicillin + Tinidazole + Lansoprazole.

Question 14. Write Pharmacological Basis Of Use Of H₂ Blockers In Peptic Ulcer.
Answer:

H₂ receptor antagonist/ H₂ blockers competitively block the effects of histamine on H₂ receptors.

They inhibit basal, food-stimulated, and nocturnal gastric acid secretion and are effective in promoting the healing of peptic ulcers and preventing their recurrence.

Question 15. Enumerate The Drugs Used In The Treatment Of Peptic Ulcers.
Answer:

Drugs Used In Peptic Ulcer

• Drugs that neutralize gastric acid secretion, i.e. antacids
  • Systemic antacids: Sodium bicarbonate, sodium citrate
  • Nonsystemic antacids: Aluminum hydroxide, magnesium hydroxide
• Drugs that reduce gastric acid secretion:
  • H₂ blockers: Ranitidine, famotidine, loxatidine and roxatidine.
  • Proton pump inhibitor: Omeprazole, lansoprazole and pentoprazole.
  • Antimuscarinic agents: Pirenzepine, telenzepine
  • Prostaglandin analogs: Misoprostol, enprostol
• Ulcer protection: Sucralfate, Colloidal Bismuth substrate
• Ulcer healing drugs: Carbenoloxone
• Anti-H. pylori drugs: Amoxicillin, clarithromycin, metronidazole, tinidazole, and tetracycline.
• Since omeprazole is one of the drugs which is used in the treatment of peptic ulcers.

Question 16. Classify The Drugs Blocking Histamine Receptors. Write Their Uses And Adverse Effects.
Answer:

Drugs blocking the histamine receptors are of two types, i.e. H₁ blockers and H₂ blockers.

Classification Of Drugs Blocking Histamine Receptors

1. Drugs blocking H₁ histaminic receptors

• High Sedative:
  • Diphenhydramine
  • Dimenhydrinate
  • Promethazine
  • Hydroxyzine.
• Moderately Sedative
  • Pheniramine
  • Cyproheptadine
  • Meclizine
  • Buclizine
  • Cinnarizine.
• Mild sedative
  • Chlorpheniramine
  • Methdilazine
  • Mepyramine
  • Dimethindene
  • Triprolidine
  • Mebhydrolin
  • Cyclizine
  • Clemastine.
• Second Generation (Non-Sedative)
  • Fexofenadine
  • Loratidine
  • Desloratadine
  • Cetrizine
  • Levocetirizine
  • Azelastine
  • Mizolastine
  • Ebastine
  • Rupatadine.

2. Drugs blocking H₂ histaminic receptors: Cimetidine, ranitidine, famotidine, roxatidine, and loxatidine.

Uses Of H₁ Blockers

• Allergic disorders: Antihistaminics do not suppress antigen: antibody reaction, but block the effects of released histamine are only palliative. They effectively control certain immediate types of allergies, for Example. itching, urticaria, seasonal hay fever, allergic conjunctivitis, and angioedema of lips, eyelids, etc.
• Other conditions involving histamine: Histaminics block symptoms produced by histamine liberators; afford symptomatic relief in insect bites and ivy poisoning.
• Pruritides: Many conventional antihistamines have antipruritic action independent of H₁ antagonism. Though relief is often incomplete, older antihistaminics remain the first choice of drugs for idiopathic pruritus.
• Common cold: Antihistaminics do not affect the course of the illness but may afford symptomatic relief by reducing rhinorrhea and sedative actions.
• Motion sickness: Promethazine, diphenhydramine, dimenhydrinate, and cyclizine have prophylactic value in milder types of motion sickness; should be taken one hour before starting the journey.
• Vertigo: Cinnarizine is the H₁ antihistamine having additional anticholinergic, anti-5-HT, sedative, and vasodilator properties which have been widely used in vertigo. It modulates calcium fluxes and attenuates the vasoconstrictor action of many endogenous substances.
• Preanesthetic medication: Promethazine has been used for its anticholinergic and sedative properties.
• Cough: Antihistaminics like chlorpheniramine, diphenhydramine, and promethazine are constituents of many popular cough remedies. They have no selective cough suppressant action but may afford symptomatic relief through sedative and anticholinergic properties.
• Parkinsonism: Promethazine and some others afford mild symptomatic relief in early cases.
• Acute muscle dystonia: Caused by anti-dopaminergic antipsychotic drugs is promptly relieved by parenteral promethazine or hydroxyzine. This is again based on the central anticholinergic action of the drugs.
• As sedative, hypnotic, anxiolytic: Antihistamines with CNS depressant action have been used as sedative and to induce sleep, especially in children.

Uses Of H₂ Blockers

• Duodenal ulcer: They produces rapid and marked pain relief. Ulcers heal at 4 weeks.
• Gastric ulcer: Healing rates are lower. H₂ blockers can heal NSAID-associated ulcers.
• Stress ulcers and gastritis: Stressful situations like hepatic coma, severe burns, trauma, etc. are associated with gastric erosions and bleeding. IV infusion prevents gastric lesion and hemorrhage.
• Zollinger-Ellison syndrome: It is a gastric hypersecretory state due to a rare tumor secreting gastrin. H₂ blockers control hyperacidity and symptoms in many patients.
• Gastroesophageal reflux disease: H₂  blockers afford symptomatic relief and facilitate the healing of esophageal erosions by reducing the acidity of gastric contents.
• Prophylaxis of aspiration pneumonia: H₂ blockers given preoperatively reduce the risk of aspiration of acidic gastric contents during anesthesia and surgery.

Adverse Effects Of H₁ Blockers

• Sedation, diminished alertness, and concentration, lightheadedness, motor incoordination, fatigue, and a tendency to fall asleep are the most common.
• Objective testing shows impairment of psychomotor performance. Patients should be cautioned not to operate motor vehicles or machinery requiring constant attention.
• Alcohol synergizes in producing these effects as do other CNS depressants.
• Few individuals become restless, nervous, and unable to sleep.
• Second-generation compounds are largely free of CNS effects.
• Dryness of mouth, alteration of bowel movement, urinary hesitancy, and blurring of vision can be ascribed to anticholinergic properties.
• Epigastric distress and headache are also common.
• A local application can cause contact dermatitis.
• Acute overdosages produce central excitation, tremors, hallucination, muscle incoordination, convulsion, flushing, hypotension, and fever.
• Death is due to respiratory and cardiovascular failure.

Adverse Effects Of H₂ Blockers

• Cimetidine leads to headache, dizziness, bowel upset, dry mouth, and rashes.
• Cimetidine produces CNS effects like confusional state, restlessness, convulsions, and coma that have occurred infrequently in elderly patients, in those with renal impairment, especially with large doses infused IV.
• Bolus IV injection of cimetidine can release histamine-caused bradycardia, arrhythmias, and cardiac arrest. It should always be given by slow infusion.
• Cimetidine (but not other H₂ blockers) has antiandrogenic action, increases plasma prolactin, and inhibits the degradation of estradiol by the liver. High doses given for long periods have produced gynecomastia, loss of libido, impotence, and a temporary decrease in sperm count.
• Transient elevation of plasma aminotransferases; but hepatotoxicity is rare.
• Ranitidine and roxatidine lead to headaches, diarrhea/ constipation, and dizziness.
• Famotidine leads to headache, dizziness, bowel upset, rarely disorientation, and rash.

Question 17. Write Short Note On Uses Of Sodium Bicarbonate.
Answer:

The following are the uses of sodium bicarbonate:

• It alkalinizes the urine and treats acidosis.
• Sodium bicarbonate neutralizes the acid formed due to the action of bacteria on food lodged between the teeth.
• It provides symptomatic relief for heartburn.

Question 18. Mention Four Proton Pump Inhibitors And Its Indications.
Answer:

Four proton pump inhibitors:

• Omeprazole
• Lansoprazole
• Pantoprazole
• Rabeprazole

Pump Inhibitors Indications

• Peptic ulcer: Omeprazole 20 mg and lansoprazole 30 mg are given once daily. Duodenal ulcers require 4-week therapy and gastric ulcers require 6 to 8 weeks of therapy.
  • In acute bleeding ulcers: IV esomeprazole, lansoprazole, and pantoprazole can be given which suppresses acid secretion and promotes healing.
  • In H. pylori-associated ulcers: Combined therapy of two or three anti-microbials with proton pump inhibitor is more effective.
  • Stress ulcers: Prophylactic use of IV proton pump inhibitors decreases the incidence of stress ulcers in critically ill patients.
  • In NSAID-induced ulcers: Proton pump inhibitors are the most effective drugs
• In aspiration pneumonia: Proton pump inhibitors are the drugs used preoperatively to decrease the risk of aspiration pneumonia.
• In Zollinger-Ellison syndrome: Proton pump inhibitors are the choice of drugs. Higher doses are needed for the healing of ulcers.
• In gastroesophageal reflux disease: Proton pump inhibitors are the drug of choice in gastroesophageal reflux disease and are given once daily.