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Recent Advances

Recent Advances = New drugs:

  1. Aprepitant/Fosaprepitant:
    1. This drug is blocker of action of substance P on its receptor neurokinin 1(NK1)
    2. NK1 receptor is present both periphery as well as centrally in CNS
    3. This drug blocks the interaction of sub P with this receptor and approved for the treatment of nausea and vomiting caused by anticancer drugs which is not controlled by 5-HT3 antagonist.
    4. This drug is lipid soluble, and cross BBB
    5. Given by oral route.
  2. Dronabinol and Nebilone
    1. These are two new drugs which are cannabinoid receptor agonist (CB1)
    2. They have been approved for the treatment of chemotherapy induced nausea and vomiting.

Drugs for Peptic Ulcer

Reduction of gastric acid secretion


a) H2 antihistamines: Cimetidine Ranitidine,

Famotidine, Roxatidine

b) Proton pump inhibitors: Omeprazoie,

Lansoprazole, Pantoprazole, Rabeprazole,


c) Anticholinergics: Pirenzepine, Propanthe-

line, Oxvphenonium

(d) Prostaglandin analogue: Misoprostol

Neutralization of gastric acid (Antacids)


(a) Systemic: Sodium bicarbonate, Sodium Citrate

(b) Nonsystemic: Magnesium hydroxide, Mag.trisilicate,                    Aluminium hydroxide. Magaldrate, Calcium carbonate

Ulcer Protectives

Sucralfate, Collloidal bismuth subcitrate (CBS), Alginic acid

Anti-H.Pylori drugs

Amoxicillin, Clarithromycin, Metronidazole, Tinidazole, Tetracycline

  1. Antacids
    Two types
    1. Non systemic
      1. Aluminum hydroxide (Constipation causing)
      2. Magnesium hydroxide (Diarrhea causing)
    2. Systemic
      1. Sodium bicarbonate, Sodium citrate


  • Neutralize gastric acidity

Advantage of antacids

  1. Fastest acting antiulcer drugs
  2. Used for:
    1. ‘Breakthrough pain’
    2. ‘On demand’ acid neutralization

Combination of antacids- RATIONALE

A combination of two or more is frequently used. These may be superior to any single agent on the following account:

(a) Fast (Mag. Hydrox.) and slow (Alum. Hydrox.) acting components yield prompt as well as sustained effect.

(b) Mag. salts are laxative, while alum. salts are constipating: combination may annul each other’s action and bowel movement may be least affected.

(c) Gastric emptying is least affected: while alum. salts tend to delay it, mg/cal salts tend to hasten it.

(d) Dose of individual components is reduced; systemic toxicity (dependent on fractional absorption) is minimized.


Disadvantage of antacids

  1. Rebound acidity                  
  2. Drug interaction          
  3. Stomach distention (HCO3-)
  4. Low efficacy        
  5. High rate of relapse

Milk Alkali Syndrome: Large quantities of milk were prescribed with CaCO3 (or NaHCO3) for peptic ulcers. Such regimen often produced syndrome characterized by Headache, anorexia, weakness, abdominal discomfort, abnormal Ca2+ deposits and renal stones due to concurrent hypercalcemia and alkalosis.

  1. H-2 blockers
    a. Act upon parietal cells of stomach     
    b. Block production of gastric acid


  1. Well absorbed
  2. Short acting
  3. Enzyme inhibitors (cimetidine)
  4. Ranitidine is not an enzyme inhibitor
  5. Pro-drugs
  6. Ranitidine-shortest acting
  7. Famotidine-more potent than ranitidine
  8. Loxatidine - longest acting


  1. Duodenal ulcer
  2. Gastric ulcer
  3. Zollinger Ellison Syndrome
  4. GERD
  5. Prophylaxis of aspirational pneumonia
  6. Stress induced gastric ulcers (DOC)
    1. Curling’s ulcers
    2. Cushing’s ulcers

Not effective for:

  1. Bleeding peptic ulcers
  2. DOC PPIs

Side effects

  1. Gastrointestinal upset
  2. Gynecomastia
    1. Cimetidine
  3. Aspiration pneumonitis
  4. Hypotension
    1. IV ranitidine

Rannitidine Over Cimetidine

  • About 5 times More Potent than cimetidine. Though its pharmacokinetic profile and t1/2 of 2-3 hr is similar to cimetidine, a longer duration of action with greater 24 hr acid suppression is obtained clinically because of higher potency.
  • No antiandrogenic action, does not increase prolactin secretion or spare estradiol from hepatic metabolism, no effect on male sexual function or gynaecomastia.
  • Lesser permeability into the brain: lower propensity to cause CNS effects. In fact, little effect outside g.i.t. has been observed. Does not significantly inhibit hepatic metabolism of other drugs; drug interactions mostly have no clinical relevance.
  • Overall incidence of side effects is lower: headache, diarrhea/constipation, dizziness have an incidence similar to placebo.
  1. Proton pump inhibitors
    1. Sulfanilamide derivatives
    2. Inhibit H+K+ATPase at parietal cells of stomach
    3. Latency of 2-3 days
    4. Block final common pathway
    5. Therefore have high efficacy


  1. Well absorbed; prodrugs
  2. Food decrease action
  3. Converted into sulfanilamides
  4. Form covalent bonds
  5. Short half life; long acting
  6. Highly protein bound
  7. Metabolism-CYP 2C8, CYP 2C9, 2C19

Individual agents


CYP inhibitor


Optical isomer of omeprazole


Anti-H.Pylori effect


Least drug interaction


Fastest, longest, most efficacious



  1. GERD
  2. Erosive esophagitis
  3. Bleeding Peptic ulcer
    1. Gastric
    2. Duodenal
  4. Zollinger Ellison Syndrome
  5. Prophylaxis of Aspirational pneumonia
  6. NSAID induced ulcer
    1. Prophylaxis
    2. Treatment

Side effects

  1. GI upset          
  2. Increased gastrin levels               
  3. Atrophic gastritis

Drug interactions

  1. Omeprazole inhibits metabolism of Warfarin-Bleeding
  1. Antichloinergics
    Pirenzepine: It is a selective M1 anticholinergic that has been used in Europe for peptic ulcer. Gastric secretion is reduced by 40-50% without producing intolerable side effects, but side effects occur with slight excess. It has not been used in India and USA
  2. Gastroprotective drugs (GPs)
    1. Misoprostol
      1. PGE1 analogue
      2. Mucoprotective / CYTOPROTECTIVE
        Increases mucosal blood flow
      3. USE: NSAIDs induced ulcers
      4. S/e
        1). Dose dependent diarrhea      
        2). Bronchospasm       
        3). Oxytocic-C/I-pregnancy
    2. Sucralfate

                i.    Sugar polymer


MOA: It preferentially and strongly adheres to ulcer base, especially duodenal ulcer; has been seen  endoscopically to remain there for - 6 hours. It precipitates surface proteins at ulcer base and acts as a physical barrier preventing acid, pepsin and bile from coming; in contact with the ulcer base Dietary proteins get deposited on this coat, forming another layer

Inactive at pH above 4

  1. Therefore not given with antacids, H2 blockers or PPIs
  2. Used mainly for stress ulcer prophylaxis
  1. Colloidal Bismuth Subcitrate
    1. Anti-inflammatory
    2. Increases mucosal regeneration
    3. Ulcer healing
    4. Anti H-Pylori property
    5. S/e
      1. Black colored stools
      2. Osteodystrophy  
  2. Alginic acid
    i. Complex carbohydrate          
    ii. Forms a cytoprotective layer on stomach
    iii. Used in orthostatic ulcers  

Management Of Gerd

STAGE 1: Sporadic uncomplicated heart burn, often in setting of known precipitating factor, often not chief complaint, less than 2-3 episode per week, no additional symptoms

Lifestyle modification

Antacids and/or Antihistaminics as needed

STAGE 2: Frequent symptoms, with or without esophagitis. Greater than 2-3 episodes per week


STAGE 3: Chronic unrelenting symptoms, immediate relapse off therapy, esophageal complications (e.g., stricture, Barrett’s metaplasia)

PPI once or twice daily


Treatment Of H.Pylori Infection

Triple therapy . 14 days: Proton pump inhibitor + clarithromycin 500 mg +  metronidazole 500 mg/amoxicillin 1 g twice a day.

(Tetracycline 500 mg can be substituted for amoxicillin or metronidazole.)

Quadruple therapy . 14 days: Proton pump inhibitor twice a day + metronidazole 500 mg three times daily +  (bismuth subsalicylate 525 mg + tetracycline 500 mg four times daily)


H2 receptor antagonist twice a day +  (bismuth subsalicylate 525 mg + metronidazole 250 mg + tetracycline 500 mg) four times daily


Proton pump inhibitors: Omeprazole: 20 mg, Lansoprazole: 30 mg,  Rabeprazole: 20 mg, Pantoprazole: 40 mg, Esomeprazole: 40 mg

H2 receptor antagonists: Cimetidine: 400 mg, Famotidine: 20 mg, Nizatidine: 150 mg, Ranitidine: 150 mg


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