Outlines for Anti-Ulcer Drugs

 Anti-Ulcer Drugs: Classification

Anti-ulcer drugs reduce acid, protect mucosa, or eradicate causes like H. pylori. Main classes:

1. H2 blockers,

2. PPIs (Proton Pump Inhibitors)

2. Anticholinergics

3. Prostaglandin analogues

4. Antacids

5. Ulcer protectives

Mnemonic trick: "HAPPy Stomach" – H2 blockers, Anticholinergics, PPIs (Proton Pump Inhibitors), Prostaglandins, Antacids/Protectives.
Tip: Visualize a "happy stomach party" with these guests neutralizing acid.

Related discovery: H. pylori (discovered 1982 by Marshall & Warren; Nobel 2005) causes 90% duodenal ulcers – key for eradication regimens.

1. H2 Receptor Antagonists (Cimetidine, Ranitidine, Famotidine)

MOA: Block histamine H2 receptors on parietal cells → ↓ gastric acid.
Uses: Peptic ulcer, GERD, Zollinger-Ellison syndrome.
AE: Headache, dizziness; Cimetidine: gynecomastia (anti-androgen).
DI: Cimetidine inhibits CYP450 → ↑ warfarin, theophylline levels.

Mnemonic: "C-R-F Blocks Acid" (Cimetidine-Ranitidine-Famotidine). Trick: Cimetidine = "Cime-TITS" (gynecomastia). Ranitidine/Famotidine safer (no major DI).
Tip: Rank potency: F > R > C (Family strongest).

2. Proton Pump Inhibitors (PPIs: Omeprazole, Pantoprazole, Rabeprazole, Lansoprazole, Esomeprazole)

MOA: Irreversibly block H+/K+ ATPase (proton pump) → max acid suppression (up to 99%).
Uses: Refractory ulcers, GERD, H. pylori eradication.
AE: Headache, diarrhea; long-term: osteoporosis, infections, B12 deficiency.
DI: Inhibit CYP2C19 → ↑ diazepam, clopidogrel (weakened).

Mnemonic: "O-PRA-L-E" (Omeprazole-Pantoprazole-Rabeprazole-Ansoprazole-Esomeprazole). Trick: "OPRA Leans on Pump" (blocks proton pump). Esomeprazole = "S"-omeprazole (S-isomer, strongest).
Tip: PPIs > H2 blockers (Pumps are final step). Discovery note: Omeprazole first PPI (1984, AstraZeneca).

3. Anticholinergics (Pirenzepine, Propantheline, Oxyphenonium)

MOA: Block muscarinic receptors → ↓ acid secretion, motility.
Uses: Peptic ulcer (adjunct).
AE: Dry mouth, blurred vision, constipation, tachycardia.
DI: Additive with other anticholinergics.

Mnemonic: "PPO" (Pirenzepine-Propantheline-Oxyphenonium). Trick: "Pirates Propel Oxy" (block vagal stimulation).
Tip: Rarely used now (side effects); selective like Pirenzepine better.

4. Prostaglandin Analogues (Misoprostol)

MOA: Mimics PGE1 → ↑ mucus/bicarb, ↓ acid.
Uses: NSAID-induced ulcers.
AE: Diarrhea, abdominal pain (abortifacient – avoid pregnancy).
DI: None major.

Mnemonic: "Misoprostol Protects Stomach." Trick: "Misery-postol" (diarrhea misery).
Tip: Pair with NSAIDs.

5. Antacids

MOA: Neutralize HCl → ↑ pH.
Types:

Type	Examples	Notes
Systemic	NaHCO3, Na citrate	Absorbed; alkalosis risk.
Non-systemic	Mg(OH)2, Mg trisilicate, Al(OH)3, Magaldrate	Poorly absorbed; Mg=diarrhea, Al=constipation.

AE/DI: Diarrhea (Mg), constipation (Al); ↓ absorption of tetracyclines, fluoroquinolones.
Mnemonic: "SMAM" (Systemic: Sodium; Non: Mag/Al). Trick: "Mag Loose, Al Tight" (Mg laxative, Al constipating).
Tip: Space 2 hrs from other drugs.

6. Ulcer Protectives (Sucralfate, Colloidal Bismuth Subcitrate – CBS)

MOA: Sucralfate = Al salt + sucrose → barrier on ulcer; CBS coats + anti-H.pylori.
Uses: Ulcer healing.
AE: Constipation (Sucralfate).
DI: ↓ other drug absorption.

Mnemonic: "SuCralfate Coats ulcers; BiSmuth Shields."
Tip: Take empty stomach.

H. pylori Eradication Regimen (Triple/Quadruple therapy, 10-14 days): PPI + 2 antibiotics (Clarithromycin + Amoxicillin/Metronidazole) ± Bismuth. Discovery: Barry Marshall self-infected (1984) proved H.pylori causation.

Drugs for Constipation: Laxatives Classification & Key Drugs

Classes: Bulk-forming, Stool softeners, Stimulants, Osmotics.

Class	Examples	MOA	Uses	AE	DI
Bulk-forming	Ispaghula, Methylcellulose	↑ bulk → peristalsis	Chronic constipation	Bloating	↓ drug absorption
Stool softener	Liquid paraffin	Lubricates/softens stool	Post-op, hemorrhoids	Aspiration (lipid pneumonia)	↓ fat-soluble vit absorption
Stimulant	Bisacodyl, Phenolphthalein, Senna, Tegaserod, Castor oil	↑ motility/secretions	Acute constipation	Cramps, dependence	Electrolyte loss
Osmotic	Lactulose	Retains water → osmosis	Hepatic encephalopathy, constipation	Flatulence, diarrhea	None major

Mnemonic: "B-S-S-O" (Bulk-Softener-Stimulant-Osmotic). Trick: "Big Soft Sausage Osmosis" (visualize colon flow).
Tip: Start with bulk/osmotic; stimulants last resort. Discovery: Lactulose (1920s synthesis; 1960s use for encephalopathy).

Drugs for Diarrhea: Antidiarrheals Classification & Key Drugs

Classes: Absorbents, Aminosalicylates, Somatostatin analogues, Opioids.

Drug	MOA	Uses	AE	DI
Absorbents (Ispaghula, Psyllium)	Absorb water	Mild diarrhea	Bloating	↓ other absorption
Aminosalicylates (Sulfasalazine, Mesalazine)	Anti-inflammatory (IBD)	Ulcerative colitis	Rash, headache	Sulfa allergy
Octreotide	Somatostatin analogue → ↓ secretions/motility	Endocrine tumors, VIPomas	Gallstones	↓ insulin
Opioids (Codeine, Diphenoxylate, Loperamide)	μ-opioid agonist → ↓ motility	Acute diarrhea	Constipation, drowsiness (systemic)	CNS depressants; Loperamide non-CNS

ORS & Zinc: ORS (glucose-electrolyte solution) → Na/glucose cotransport rehydrates. Zinc (10-20mg/day, kids) shortens duration 25%. Discovery: ORS (1968, WHO; Nobel 2006 to Kaprekar et al. for mechanism).
Mnemonic: "A-S-O-O" (Absorbents-Sulfasalazine-Octreotide-Opioids). Trick: "Lope-rope" ties gut (Loperamide).
Tip: Avoid opioids in bloody/infectious diarrhea; Loperamide safest (no addiction).

                                                    END OF THE CHAPTER

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