Inhibitors of Gastric Acid secretion
Proton Pump Inhibitors (PPIs)
Gastric Acid Secretion
Receptors
H2 histamine receptors
Gs
Histamine
M3 Muscarinic
Gq
Ach
EP3 Prostaglandin receptors
Gi
PG Prostaglandin
MOA
Inhibit H+/K+ ATPase proton pump that controls H+ secretion from the parietal cell
PKs
Pro-drug activated in acidic env
Rapidly absorbed, highly protein bound
Metabolised by CYP450 2C19 and CYP 3A4
Drugs
Omeprazole
Lansoprazole
Pantoprazole 🥇
Rabeprazole
Esomeprazol
ADs
CYP 2C19 genotype hav greater efficiacy and adverse effects
Indications
- Gastric and duodenal ulceration
- H. pylori eradicatoin (Triple Therapy)
- Dyspepsia
- GORD
- NSAID ass ulceration
7. Zollinger - Ellison syndrome
Tumors cause too much acid, resulting in peptic ulcers
- Nausea
- Abdominal pain
- Constipation
- Diarrhoea
- Risk of bone fracture
- Susceptibility to certain infx (C.dif and HAP) 🍫⛲
Interactions
Esomeprazole + Omeprazole - Clopidogrel
- Hypomagnesia 🧲
Decreased efficacy of clopidogrel
H2RA Histamine H2 Receptor Antagonists
Drugs
Cimetidine
Ranitidine
Famotidine
Nizatidine
MOA
Competitive antagonism of H2 receptors
Prevents ↑cAMP and gastric acid secretion
Indications
- Gastric / duodenal ulceration
- H. pylori eradication
- Dyspepsia
- GORD
- NSAID ass ulceration
- Zollinger-Ellison syndrome
Adverse Effects
- GIT disturbance
- Headache
- Dizziness
- Altered LFTs
- Bradycardia
- Confusion
- Depression
- Hallucinations
- ↑ Prolactin
- Galactorrhoea
- Impotence
- CYP450 inhibiton - Cimetidine
Interactions
Cimetidine - Warfarin (CYP2C9), Phenytoin (CYP3A4), Theophylline (CYP1A2)
Cimetidine inhibits drug metabolism
- Secondary hypergastrinaemia
Prostaglandin Analogues
Drug
Misoprostol
MOA
E1 Prostaglandin analogue
Antisecretory and cytoprotective properties vie EP3 receptor
Increases mucin and bicarbonate secretion
Indications
- Gastric / duodenal ulceration
- NSAID ass ulceration
Adverse Effects
Nausea and vomiting
Abdominal pain
Diarrhoea
Abdnormal vaginal bleeding
Women of childbearing age must take contraception
Contraindicated in pregnancy
Exacerbates inflammatory bowel disease (IBD)
Chelates & Complexes
Sulcralfate
Bismuth Chelates
Indications
Gastic / duodenal ulceration
Indications
Gastric / duoudenal ulcers
H. pylori eradication
Antacids
Drugs
Aluminium hydroxide (MAALOX)
Magnesium carbonate (ANDRES ANTACID TAB)
Indications
Symptom relief in ulcer dyspepsia
Non erosive GORD
Adverse Effects
Aluminium hydroxide : Constipation
Magnesium carbonate : Diarrhoea
H. Pylori Eradication
1st Line 🥇
Triple Therapy
- PPI (Pantoprazole 🥇)
- Amoxicillin
- Metronidazole
Penicillin allergy
Amoxicillin → Lymecycline
2nd Line 🥈
- PPI
- Levofloxacin
- Amoxicillin
Penicillin allergy
Amoxicillin → Clarithromycin
Treatment of Dyspepsia
- Inhibitors of Gastric Acid Secretion
- Antiacids
- Mucosal Protectants / Chelates & Complexes
Laxatives
Causes of Constipation
β Blockers
Ca+ channel blockers
Neuroleptics
SSRIs
SNRIs
Tricyclic antidepressants
Ostrogens
Codeine
Levodopa
Managment of Constipations
🥇Dietary fibre , fluids, exercise
🥈Laxatives
Types
- Bulk forming laxatives
- Stimulant laxatives
- Faecal softeners
- Osmotic Laxatives
Bulk forming Laxatives
- Peripheral opioid receptor antagonists
Methylcellulose
Ispaghula
Steruclia
Stimulant laxatives
Sennoside
Bisacodyl
Na Picosulphate sachet
Faecal Softeners
Na+ Lauryl Sulfoacetate
Na+ Citrate
Glycerol enema
Sorbic acid enema
Osmotic Laxatives
Lactulose
Macrogols
Peripheral Opiod Receptor Antagonists
Naloxegol
Methylnaltrexone bromide solution
Antidiarrheals
Definition of Acute Diarrhoea
Lasts less than 14 days but symptoms improve within 2-4 days
Causes
Infection
Chronic GIT condition (IBD)
Drugs
β blockers
Antibiotics
HIV protease inhibitors
SSRIs
PPIs
Oestrogens
Methyldopa
Misoprostol
Methotrexate
Management
- Rehydration - Dioralyte
- Loperamide
- Diphenoxylate
- Cholestyramine
Loperamide
MOA
Piperidine derivative
Opiate agonist slows GIT moltility
Reduces GIT secretions
Adverse Effects
QT prolongation
Torsades de points
Cardiac arrest
Diphenoxylate
Piperidine derivative
Given in combo w/ anticholinergic agent
Cholestyramine
MOA
Ion-exchange resin
Indication
Diarrhoe due to ileal resection
Crohn's
Diabetic vagal neuropathy