Laxatives

PHCL 3XX

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 Learning Objectives
• Define constipation
• Justify the use of laxatives in constipation
• Describe the mechanisms of action of each
of the laxative groups
• Outline the main clinical considerations
associated with laxative use

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 Laxatives:
• Laxative – results in the production of a soft formed stool
over a period of 1 or more days
• Catharsis – results in prompt, fluid evacuation of the
bowel, more intense

Indications for laxative use:

• Pain associated with bowel movements
• To decrease amount of strain under certain conditions
• Evacuate bowel prior to procedures or examinations
• Remove poisons
• To relieve constipation caused by pregnancy or drugs

Contraindications:
• Inflammatory bowel diseases
• Acute surgical abdomen
• Chronic use and abuse 3
 Classification of Laxatives
Bulk laxatives
– Non-absorbable Laxatives act by:
carbohydrates • Stimulating
– Osmotically active peristalsis
laxatives or
• Irritant (stimulant) laxatives = • Soften bowel content
purgatives
– Small bowel irritants
– Large bowel irritants
• Lubricant laxatives
– Paraffin
– Glycerol 4
 Bulk laxatives
• Increase in bowel volume triggers stretch
receptors in the intestinal wall . This causes
causes reflex contraction (peristalsis) that
propels the bowel content forward
– Carbohydrate-based laxatives
• Insoluble and non-absorbable
• Non digestable; take several days for effect
• Expand upon taking up water in the bowel
• Must be taken with lots of water
– Vegetable fibers (e.g. Psyllium, lineseed)
– Bran (milling waste product)
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 Osmotically active laxatives
• MoA:
– increase the amount of water in the large bowel, either by drawing fluid from
the body into the bowel or by retaining the fluid they were administered with.

• Partially soluble, but not absorbable

• Adverse Effects:
– flatulence, cramps, and abdominal discomfort

• Eamples
1. Lactulose (Duphalac®)
2. Macrogols (Forlax®):
3. Saline-based (mostly sulfates)
4. Effect in 1-3 hrs => used to purge intestine (e.g. surgery, poisoning)
• MgSO4 (= Epsom salt)
• Na2SO4

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 Irritant laxatives
• Increases peristalsis via intestinal nerve stimulation
• Cause irritation of the enteric mucose
=> more water is secreted than absorbed => softer bowel
content and increased peristaltic due to increase volume

Small intestine irritants

• Ricinoleic acid (Castor oil)
– Active ingredient of Ricinus communis
– The oil (triglyceride) is inactive
– Ricinoleic acid released from oil through lipase
activity

Ricin:
– Lectin from the beans of R.communis
– Potent toxin: inhibits protein synthesis
– Potential bioterrorism agent (LD ~100g)

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 Irritant laxatives-
large intestine irritants
• Anthraquinones
– Active ingredient of
• Senna sp. (Folia and fructus
sennae),
• Rhamnus frangulae (cortex
frangulae) and
• Rheum sp. (rhizoma rhei):
– contain inactive glycosides =>
active anthraquinones released
in colon and take 6-10 hours to
act
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 Irritant laxatives-
large intestine irritants (Cont’d)
• Synthetic compounds
– Diphenolmethanes
• Derivatives of phenolphtalein

– Bisacodyl (Dulcolax)
• Oral administration: effect in 6-8
hrs
• Rectal administration: effect in 1 hr
• Often used to prepare for intestinal
surgery

– Sodium picosulfate (FRUCTINE)

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 Laxatives: Indications
Laxative Group Use
Bulk forming Acute and chronic
constipation
Irritable bowel syndrome
Diverticulosis
Lubricant Acute and chronic
constipation
Softening of fecal impaction;
facilitation of BMs in
anorectal conditions

Mosby items and derived items © 2005, 2002 by Mosby, Inc. 10

Laxatives: Indications (cont'd)
Laxative Group Use
Hyperosmotic Chronic constipation
Diagnostic and surgical
preps
Constipation
Saline
Diagnostic and surgical
preps
Removal of helminths and
parasites

Mosby items and derived items © 2005, 2002 by Mosby, Inc. 11

Laxatives: Indications (cont'd)
Laxative Group Use
Irritant (Stimulant) Acute constipation
Diagnostic and surgical
bowel preps

Mosby items and derived items © 2005, 2002 by Mosby, Inc. 12

 Laxative abuse
• Laxative abuse:
Most common cause of constipation is laxative abuse!
– Longer interval needed to refill colon is misinterpreted as
constipation => repeated use
– Enteral loss of water and salts causes release of
aldosterone
=> stimulates reabsorption in intestine, but increases
renal
excretion of K+ => double loss of K+ causes hypokalemia,
which in turn reduces peristalsis. This is then often
misinterpreted as constipation => repeated use 13
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 Non-pharmacological recommendations for
Therapy of Constipation

• Add fiber, whole grains to diet

• Drink more liquids
• Exercise regularly
• Avoid stress

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