Laxatives and Purging Agents

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Laxatives Overview - The Gut Go-Getters

  • Laxatives: Promote defecation; ease stool passage. Purgatives: Stronger, cause fluid evacuation.
  • Constipation: Infrequent (<3/week), hard, or difficult-to-pass stools.
  • Key Indications:
    • Functional constipation; Opioid-induced constipation (OIC)
    • Bowel prep (surgery/colonoscopy)
    • Hepatic encephalopathy (lactulose: ↓NH₃)
    • Avoid straining (post-MI, anorectal conditions)
  • General Contraindications:
    • Undiagnosed abdominal pain, nausea, vomiting
    • Bowel obstruction, perforation, fecal impaction
  • Classification:
    • Bulk-forming: Psyllium, Ispaghula (absorb water, ↑mass)
    • Osmotic: Lactulose, PEG, Mg salts (osmotic water retention)
    • Stimulant: Bisacodyl, Senna (↑motility, alter transport)
    • Stool Softeners/Lubricants: Docusates, Liquid paraffin (soften/lubricate)

⭐ Lactulose, a non-absorbable disaccharide, is key in hepatic encephalopathy by reducing ammonia production and absorption in the colon.

Bulk-Forming Agents - Gentle Giants

Mechanisms of Action for Different Laxative Types

  • Mimic dietary fiber; non-digestible hydrophilic colloids.
  • Examples:
    • Psyllium (Ispaghula)
    • Methylcellulose
    • Calcium polycarbophil
    • Wheat dextrin
  • Mechanism of Action (MOA):
    • Absorb water in gut → swell → form bulky, emollient gel.
    • ↑ Stool volume → distends colon → stimulates peristalsis.
    • Onset: 12-72 hours.
  • Adverse Drug Reactions (ADRs):
    • Bloating, flatus.
    • ⚠️ Esophageal/intestinal obstruction or impaction if taken with insufficient fluid.
  • Clinical Uses:
    • First-line for chronic constipation.
    • Irritable Bowel Syndrome with Constipation (IBS-C).
    • Diverticulosis.
    • Safe in pregnancy & for long-term use.

⭐ Psyllium can also bind bile acids, leading to a modest reduction in LDL cholesterol. 📌 "Bulk up with water, or you'll be stuck!"

Osmotic Laxatives - Water Wonders

These agents draw water into the bowel, softening stool and promoting motility.

  • MOA: Create osmotic gradient → ↑ intraluminal water → stimulate peristalsis.
  • Types & Examples:
    • Saline:
      • Magnesium Salts: Sulfate (Epsom), Hydroxide (Milk of Magnesia), Citrate.
      • Sodium Phosphate (⚠️ Nephropathy risk).
    • Non-absorbable Sugars/Alcohols:
      • Lactulose: Disaccharide.
      • Sorbitol, Mannitol.
      • Polyethylene Glycol (PEG): Large polymers. 📌 "PEG pulls H₂O!"
  • Key Uses:
    • Lactulose: Hepatic encephalopathy (↓ $NH_3$).
    • PEG: Bowel prep (colonoscopy), chronic constipation.
    • Saline laxatives: Rapid evacuation.
  • ADRs:
    • Electrolyte imbalance (e.g., ↑$Mg^{2+}$, ↑$PO_4^{3-}$, ↓$K^+$).
    • Dehydration, cramping, flatulence.

⭐ Lactulose, metabolized by gut flora to acidic byproducts, lowers colonic pH, trapping ammonia as NH3 (converting to NH4+), thus reducing systemic ammonia levels in hepatic encephalopathy.

Osmotic Laxative Mechanism in Colon

Stimulants & Softeners - Active Accelerators

  • Stimulants (Irritants): ↑ intestinal motility via nerve stimulation.
    • Anthraquinones (Senna, Cascara):
      • MOA: Hydrolysed to emodin; stimulates colon.
      • ADRs: Melanosis coli (reversible), cathartic colon (prolonged use). Melanosis Coli: Colonoscopy View
    • Diphenylmethanes (Bisacodyl, Sod. Picosulfate):
      • Bisacodyl: Enteric-coated (avoid antacids/milk).
      • Sod. Picosulfate: Prodrug, colonic bacteria activate.
      • ADRs: Cramps, electrolyte imbalance.
    • Castor Oil:
      • MOA: Hydrolysed to ricinoleic acid (irritant). Acts on small intestine.
      • ADRs: Uterine contraction (⚠️ CI: Pregnancy).
  • Stool Softeners & Lubricants:
    • Docusates (DOSS):
      • MOA: Anionic surfactant; softens stool.
      • Use: Prevent straining.
    • Liquid Paraffin (Mineral Oil):
      • MOA: Lubricates feces.
      • ADRs: Lipid pneumonitis (aspiration), ↓ fat-soluble vitamin absorption.
  • Newer Agents: Lubiprostone (ClC-2), Linaclotide (GC-C), Prucalopride (5-HT₄).

⭐ Bisacodyl should not be taken within 1 hour of antacids or milk as these can disrupt its enteric coating, leading to gastric irritation.

High‑Yield Points - ⚡ Biggest Takeaways

  • Bulk-forming laxatives (e.g., psyllium) mimic fiber; require adequate fluids.
  • Osmotic laxatives (e.g., lactulose, PEG) draw water into colon; lactulose reduces ammonia in hepatic encephalopathy.
  • Stimulant laxatives (e.g., senna, bisacodyl) increase motility; chronic use risks cathartic colon.
  • Stool softeners (e.g., docusate) facilitate water mixing, preventing straining.
  • Lubiprostone & Linaclotide are for chronic constipation and IBS-C.
  • Opioid-induced constipation treated with PAMORAs like methylnaltrexone.
  • Avoid castor oil in pregnancy due to uterine stimulation.

Practice Questions: Laxatives and Purging Agents

Test your understanding with these related questions

Colonoscopy performed on a 25 year old woman with eating disorder showed dark brown to black pigmentary deposit in the lining of the large intestine. Histopathology of biopsy revealed pigment laden macrophages within the lamina propria. On probing, the woman revealed use of laxatives for 9 months to lose weight. What could be the probable laxative agent that could have caused these findings?

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Flashcards: Laxatives and Purging Agents

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_____ is indicated for the reversal of opioid-induced constipation in patients on chronic opioid therapy.

TAP TO REVEAL ANSWER

_____ is indicated for the reversal of opioid-induced constipation in patients on chronic opioid therapy.

Methylnaltrexone

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