21.drugs used in peptic ulcer
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Drugs used in Drugs used in peptic ulcer peptic ulcer
Drugs used in Drugs used in peptic ulcer peptic ulcer
Peptic Ulcer Peptic Ulcer
A localized loss of gastric as well as duodenal mucosa leads to the formation of peptic ulcer
Symptoms – heartburn, abdominal pain, bloating, loss of appetite and weight loss
ClassificationClassification ClassificationClassification
I. Reduction of gastric acid secretion - a) H2 receptor antagonists : Cimetidine,
Ranitidine, Famotidine
b) Proton pump inhibitors : Omeprazole, Lansoprazole, Pantoprazole
c) Anticholinergics : Pirenzepine, Telenzepine d) Prostaglandin analogue : Misoprostol
I. Reduction of gastric acid secretion - a) H2 receptor antagonists : Cimetidine,
Ranitidine, Famotidine
b) Proton pump inhibitors : Omeprazole, Lansoprazole, Pantoprazole
c) Anticholinergics : Pirenzepine, Telenzepine d) Prostaglandin analogue : Misoprostol
II. Neutralization of gastric acid
(Antacids) – a) Systemic : Sodium bicarbonate Sodium citrate
b) Nonsystemic : Magnesium hydroxide Magnesium trisilicate Aluminum hydroxide Calcium carbonate
II. Neutralization of gastric acid
(Antacids) – a) Systemic : Sodium bicarbonate Sodium citrate
b) Nonsystemic : Magnesium hydroxide Magnesium trisilicate Aluminum hydroxide Calcium carbonate
III. Ulcer protectives – Sucralfate, Colloidal bismuth subcitrate (CBS)
IV. Anti-H.pylori drugs - Amoxicillin, Clarithromycin, Metronidazole, Tinidazole, Tetracycline
III. Ulcer protectives – Sucralfate, Colloidal bismuth subcitrate (CBS)
IV. Anti-H.pylori drugs - Amoxicillin, Clarithromycin, Metronidazole, Tinidazole, Tetracycline
HISTAMINE
GR ST M?
M3H2GR
ATPase C
A
H+ K+ Cl-
Food
Gastrin G cells
SomatostatinD cells
Acetylcholine
+-
ECL cell
Parietal cellH2 blockersH2 blockersH2 blockersH2 blockers
HH22 Receptor Antagonists - Receptor Antagonists - Cimetidine, Ranitidine, FamotidineCimetidine, Ranitidine, Famotidine
HH22 Receptor Antagonists - Receptor Antagonists - Cimetidine, Ranitidine, FamotidineCimetidine, Ranitidine, Famotidine
Mechanism of action
• Competitive inhibition of H2 receptors -
Inhibits gastric acid secretion (60-70%)
• Suppresses all phases of acid secretion, mainly nocturnal acid secretion; pH ↑to
4-5
Mechanism of action
• Competitive inhibition of H2 receptors -
Inhibits gastric acid secretion (60-70%)
• Suppresses all phases of acid secretion, mainly nocturnal acid secretion; pH ↑to
4-5
Therapeutic uses
Peptic ulcer : Gastric and Duodenal ulcer
Gastroesophageal reflux disease (GERD)
Stress ulcers and Gastritis
Zollinger-Ellison syndrome
Therapeutic uses
Peptic ulcer : Gastric and Duodenal ulcer
Gastroesophageal reflux disease (GERD)
Stress ulcers and Gastritis
Zollinger-Ellison syndrome
Adverse effects Cimetidine - antiandrogenic effect
• Gynaecomastia, impotence – men
• Menstrual irregularities, galactorrhoea – women
Enzyme inhibitor - inhibits metabolism
of many co-administered drugs – toxicity
Adverse effects Cimetidine - antiandrogenic effect
• Gynaecomastia, impotence – men
• Menstrual irregularities, galactorrhoea – women
Enzyme inhibitor - inhibits metabolism
of many co-administered drugs – toxicity
HISTAMINE
GR ST M?
M3H2GR
ATPase C
A
H+ K+ Cl-
Food
Gastrin G cells
SomatostatinD cells
Acetylcholine
+-
ECL cell
Parietal cellH2 blockersH2 blockersH2 blockersH2 blockers
PPIsPPIs
PPIs: Omeprazole, PPIs: Omeprazole, Pantoprazole Pantoprazole Lansoprazole, Rabeprazole Lansoprazole, Rabeprazole
PPIs: Omeprazole, PPIs: Omeprazole, Pantoprazole Pantoprazole Lansoprazole, Rabeprazole Lansoprazole, RabeprazoleMechanism of action PPIs (prodrugs)
sulfenamide cation (activated form)
binds with sulfhydryl groups of the H+K+- ATPase - inactivate it irreversibly
Mechanism of action PPIs (prodrugs)
sulfenamide cation (activated form)
binds with sulfhydryl groups of the H+K+- ATPase - inactivate it irreversibly
Therapeutic usesTherapeutic usesTherapeutic usesTherapeutic uses
Peptic ulcer
H.pylori associated ulcers
NSAID induced ulcers
GERD
Zollinger-Ellison syndrome
Stress ulcers
Peptic ulcer
H.pylori associated ulcers
NSAID induced ulcers
GERD
Zollinger-Ellison syndrome
Stress ulcers
Adverse effects Adverse effects Adverse effects Adverse effects
Muscle & joint pain Rashes, leucopenia, headache Atrophic gastritis
Muscle & joint pain Rashes, leucopenia, headache Atrophic gastritis
Prostaglandin analoguesProstaglandin analoguesMisoprostol (PGEMisoprostol (PGE11))
Prostaglandin analoguesProstaglandin analoguesMisoprostol (PGEMisoprostol (PGE11))
“Cytoprotective action” - increases mucus &
bicarbonate secretion, increases mucosal blood flow
Therapeutic use NSAID induced ulcers
“Cytoprotective action” - increases mucus &
bicarbonate secretion, increases mucosal blood flow
Therapeutic use NSAID induced ulcers
Adverse effects Diarrhea, abdominal cramps,
uterine contractions & bleeding
Multiple daily dosing – poor patient compliance
Adverse effects Diarrhea, abdominal cramps,
uterine contractions & bleeding
Multiple daily dosing – poor patient compliance
Anticholinergics - Anticholinergics - Pirenzepine, Pirenzepine, Telenzepine Telenzepine
Anticholinergics - Anticholinergics - Pirenzepine, Pirenzepine, Telenzepine Telenzepine
Selective M1 receptor blockers
Inhibits acid secretion - heals peptic ulcer
Selective M1 receptor blockers
Inhibits acid secretion - heals peptic ulcer
AntacidsAntacids AntacidsAntacids
Basic substances which
neutralize gastric acid and raise
pH of gastric contents.
Basic substances which
neutralize gastric acid and raise
pH of gastric contents.
Sodium bicarbonateSodium bicarbonateSodium bicarbonateSodium bicarbonate
Reacts rapidly with HCl – produces CO2
and NaCl Demerits Distension and belching Metabolic alkalosis Fluid retention Acid rebound
Reacts rapidly with HCl – produces CO2
and NaCl Demerits Distension and belching Metabolic alkalosis Fluid retention Acid rebound
Magnesium hydroxide and Magnesium hydroxide and Aluminum hydroxide Aluminum hydroxide
Magnesium hydroxide and Magnesium hydroxide and Aluminum hydroxide Aluminum hydroxide
Reacts slowly with HCl No belching No metabolic alkalosis
Mg salts diarrhea , Al salts constipation
so both are administered together
Reacts slowly with HCl No belching No metabolic alkalosis
Mg salts diarrhea , Al salts constipation
so both are administered together
Antacid combinationsAntacid combinations Antacid combinationsAntacid combinations
Magnesium hydroxide – fast acting
Aluminum hydroxide – slow acting
Mg salts – diarrhea
Al salts – constipation
Dose reduction – reduced toxicity
Magnesium hydroxide – fast acting
Aluminum hydroxide – slow acting
Mg salts – diarrhea
Al salts – constipation
Dose reduction – reduced toxicity
Ulcer protectives –Sucralfate ,Ulcer protectives –Sucralfate , Colloidal Bismuth Subcitrate Colloidal Bismuth Subcitrate
Ulcer protectives –Sucralfate ,Ulcer protectives –Sucralfate , Colloidal Bismuth Subcitrate Colloidal Bismuth Subcitrate
Sucralfate
MOA – • At acidic pH < 4, it undergoes
extensive polymerization – forms a sticky gel over the ulcer base – protects it
Sucralfate
MOA – • At acidic pH < 4, it undergoes
extensive polymerization – forms a sticky gel over the ulcer base – protects it
Use – duodenal and gastric ulcers
Adverse effects – constipation, dry mouth & hypophosphatemia
Use – duodenal and gastric ulcers
Adverse effects – constipation, dry mouth & hypophosphatemia
Colloidal Bismuth Subcitrate Colloidal Bismuth Subcitrate (CBS)(CBS)
Colloidal Bismuth Subcitrate Colloidal Bismuth Subcitrate (CBS)(CBS)
• Detaches H.pylori from surface of mucosa Use – Eradication of H.pylori infection Adverse effects – blackening of stool & tongue
• Detaches H.pylori from surface of mucosa Use – Eradication of H.pylori infection Adverse effects – blackening of stool & tongue
Helicobacter
pylori
• Gram –ve bacilli
• Attaches beneath the mucus
• Cause back diffusion of H+ ions
• Present in 90% of cases with peptic ulcers
Helicobacter
pylori
• Gram –ve bacilli
• Attaches beneath the mucus
• Cause back diffusion of H+ ions
• Present in 90% of cases with peptic ulcers
Anti Anti H.pyloriH.pylori drugs drugsAnti Anti H.pyloriH.pylori drugs drugs
• Amoxicillin• Clarithromycin• Tetracycline• Metronidazole/Tinidazole
• PPIs, H2 blockers, CBS
• Amoxicillin• Clarithromycin• Tetracycline• Metronidazole/Tinidazole
• PPIs, H2 blockers, CBS
Drug regimens - triple Drug regimens - triple therapytherapy
Drug regimens - triple Drug regimens - triple therapytherapy
Lansoprazole 30 mg + Amoxicillin 1000 mg
+ Clarithromycin 500 mg
(All twice daily for 2 weeks)
Lansoprazole 30 mg + Amoxicillin 1000 mg
+ Clarithromycin 500 mg
(All twice daily for 2 weeks)
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