Antacid Drugs

Overview – Antacid Drugs

Antacid drugs are used to treat gastric acid–related disorders such as gastroesophageal reflux disease (GORD/GERD), dyspepsia, and peptic ulcer disease. Treatment options include direct acid neutralisers, acid secretion inhibitors, and cytoprotective agents that enhance mucosal defences.


1. Acid Neutralisers

Antacids

Mechanism of Action:

  • Directly neutralise gastric acid in the stomach lumen
  • Provide symptomatic relief in acid reflux and indigestion

Common Antacid Ingredients:

  • Aluminium salts (e.g. Al(OH)₃)
  • Calcium salts (e.g. CaCO₃)
  • Magnesium salts (e.g. Mg(OH)₂)
  • Sodium bicarbonate (NaHCO₃)
  • Magnesium-Aluminium combinations → balance bowel effects

Side Effects:

CompoundCommon Side Effects
Aluminium SaltsConstipation, Al+ accumulation (renal impairment), hypophosphataemia
Calcium SaltsConstipation, rebound hyperacidity, milk-alkali syndrome
Magnesium SaltsDiarrhoea, Mg+ accumulation (renal impairment)
Sodium BicarbonateMilk-alkali syndrome, avoid in sodium-restricted patients
Mg-Al CombosMinimise GI effects (balanced bowel effects)

Alginates

Mechanism of Action:

  • Increase mucus viscosity and adherence to oesophageal mucosa
  • Form a protective barrier that prevents acid reflux
  • Often combined with antacids

Side Effects:

  • Bloating → altered eating behaviour
  • May affect absorption of oral drugs via pH alteration

2. Inhibitors of Acid Production

H₂ Histamine Receptor Antagonists

Mechanism of Action:

  • Block H₂ receptors on parietal cells
    → ↓ cAMP → ↓ gastric acid secretion

Classical Agents:

  • Ranitidine
  • Cimetidine
  • (Also: Nizatidine, Famotidine)

Side Effects:

  • Diarrhoea
  • Dizziness
  • Muscle pain
  • Alopecia
  • Rash

Proton Pump Inhibitors (PPIs)

Mechanism of Action:

  • Prodrug activated in acidic environment
  • Irreversibly inhibits H⁺/K⁺ ATPase (proton pump)
    → Profound acid suppression

Classical Agents:

  • Omeprazole
  • (Also: Esomeprazole, Lansoprazole, Pantoprazole, Rabeprazole)

Side Effects (Uncommon):

  • Headache
  • Diarrhoea
  • Rash

3. Cytoprotective Agents

Bismuth-Chelate

Mechanism of Action:

  • Coats ulcers, adsorbs pepsin
  • Directly toxic to Helicobacter pylori
  • Enhances local prostaglandin synthesis → ↑ mucus, ↓ acid
  • Stimulates bicarbonate secretion

Side Effects:

  • Nausea, vomiting
  • Black tongue/feces

Sucralfate

Mechanism of Action:

  • Strong negative charge → binds to proteins → forms physical gel barrier
  • ↓ diffusion of H⁺ through mucus
  • Enhances prostaglandin production, mucus & bicarbonate secretion

Side Effects:

  • Constipation
  • Dry mouth, headache, nausea

Misoprostol (Prostaglandin E1 Analogue)

Mechanism of Action:

  • Stimulates PGE₂ receptors:
    • Goblet cells → ↑ mucus
    • Parietal cells → ↓ acid
    • Increases mucosal blood flow
  • Enhances mucus & bicarbonate secretion

Side Effects:

  • Diarrhoea
  • Abdominal cramps
  • Contraindicated in pregnancy (can induce uterine contractions)

Summary – Antacid Drugs

Antacid drugs and related agents offer multi-pronged treatment for gastric acid-related conditions. While antacids neutralise acid directly, H₂ antagonists and PPIs inhibit acid production, and cytoprotective agents bolster mucosal defences. Choosing the right agent depends on the underlying pathology and patient-specific factors such as renal function and pregnancy status. For a broader context, see our Pharmacology & Toxicology Overview page.

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