4) Constipation and IBS

Drugs used in treating
constipation and IBS
Prof. Hanan Hagar

Pharmacology Department
Medical College, KSU
What is constipation?
 infrequent defecation, often with straining

and the passage of hard, uncomfortable stools.
 May be accompanied by other symptoms:

Loss of appetite
Flatulence
Abdominal and rectal pain
Lethargy
Depression
Causes of constipations
 Decreased motility in colon:
 Decrease in water and fiber contents of diet.
 Difficulty in evacuation:
 Local painful conditions: anal fissures, piles
 Lack of muscular exercise
 Drug-induced:
 Anticholinergic agents
 Opioids
 Iron
 Antipsychotics
Treatment of Constipation
General Measures :
1. Adequate fluid intake.
2. High fiber contents in diet.
3. Regular exercise
4. Regulation of bowel habit.
5. Avoid drugs causing constipation.
6. Use drugs (laxatives or purgatives)
Medications used in constipations
Drugs that hasten the transit of food through

the gastrointestinal tract are called laxatives
or purgatives.
Classification of laxatives:
1. Bulk forming laxatives
2. Osmotic laxatives
3. Stimulant laxatives
4. Stool softeners (lubricants)
Classification of laxatives or purgatives
I) Bulk forming laxatives:

Increase volume of non-absorbable solid
residue.
II) Osmotic laxatives:

Increase water content in large intestine.
Classification of laxatives or purgatives
III) Stimulant or irritant laxatives:

Act by direct stimulation of nerve endings in
colonic mucosa.
IV) Stool softeners (lubricants):

Alter the consistency of feces  easier to pass
Bulk (fiber) Laxatives
Include:
Dietary fibers:
 Indigestible parts of vegetables & fruits
 Bran powder
Hydrophilic colloids
 Psyllium seed
 Methyl cellulose
 Carboxymethyl cellulose (CMC)

Mechanism of Action
Dietary fibers and hydrophilic colloids are non

absorbable substances  Increase the bulk of
intestinal contents by water retention  
mechanical pressure on the walls of intestine
 stimulation of stretch receptors 
 peristalsis  evacuation of soft stool.
Side Effects
• Delayed onset of action (1-3 days).
• Intestinal obstruction (should be taken with
enough water).
• Bloating, flatulence, distension
• Interfere with other drug absorption e.g. iron,
cardiac glycosides.
Osmotic Laxatives
 are water soluble compounds

 Poorly absorbable compounds (salts or sugars)
 They remain in the bowel, attract and retain

water by osmosis thereby increasing the
volume of feces   peristalsis  evacuation
of stool.
Osmotic Laxatives
Include:
1. Sugars : e.g. lactulose
2. Salts (Saline laxatives)
• Magnesium sulphate or hydroxide
• Sodium or potassium phosphate.
3. Polyethylene glycol (PEG)
Lactulose
 Semisynthetic disaccharide of fructose and
galactose.
 Non absorbable.
 In colon, metabolized by bacteria into
fructose and galactose.
 These sugars are fermented into lactic acid
and acetic acid that function as osmotic
laxatives.
Uses
 Prevention of chronic constipation
 Hepatic encephalopathy (Hyperammonemia)
 Hemorrhoids
Lactulose increases the H+ concentration in the

gut, This favors the formation of the non-
absorbable NH4+ from NH3, trapping NH3 in the
colon and reducing its back diffusion into blood.
Why lactulose is commonly used in liver
cirrhosis?
Mechanism:
Lactulose Lactic acid + Acetic Acid
acidification of the colon ammonia
absorption (NH4+)
Dose:
15 ml for constipation and 30 ml for liver cirrhosis
Side Effects
1. Delayed onset of action (2-3 days)
2. Abdominal cramps and flatulence.
3. Electrolyte disturbances.
Saline Laxatives
 Are poorly absorbable salts
 Increase evacuation of watery stool.
 Magnesium sulphate (Epson’s salt ).
 Magnesium hydroxide (milk of magnesia).
 Sodium phosphate or potassium phosphate.
 have rapid effect (within 1-3 h ).
 Isotonic or hypotonic solution should be used.
Uses
Treatment of acute constipation
Side Effects
 Disturbance of fluid and electrolyte balance
 May have systemic effects.
Contraindications
Sodium salts in congestive heart failure
Magnesium salts are contraindicated in:
 Renal failure
 Heart block
 CNS depression
 Neuromuscular block
Balanced Polyethylene Glycol (PEG)
 Isotonic solution of polyethylene glycol &
electrolytes (NaCl, KCl, Na bicarbonate).
 Is a colonic lavage solution
 Used for whole bowel irrigation prior to
colonoscopy or surgery (4L over 2-4 hours).
Advantages
 Limited fluid or electrolyte imbalance
 less flatulence and cramps
Stimulant Laxatives
are the most powerful group among laxatives and
should be used with care.
Mechanism of Action:
act via direct stimulation of enteric nervous
system  increased peristalsis & purgation.
Drugs
 Bisacodyl
 Castor oil
 Anthraquinone derivatives (senna, cascara,
aloes).
Bisacodyl
Is given orally, acts on colon
Onset of action = orally (6-12 h)/ per rectum (1 h)
Castor Oil
 Given orally
 5-20 ml on empty stomach in the morning.
 acts in small intestine
 Vegetable oil degraded by lipase  ricinoleic
acid + glycerin
 Ricinoleic acid is very irritating to mucosa.
 Onset of action = 2-6 h.
Anthraquinone glycosides
e.g. senna, cascara, aloe vera
 Act in colon
 Hydrolyzed by bacterial colon into sugar
+ emodin (The absorbed emodin has direct
stimulant action ).
 Emodin may pass into milk.
 Delayed onset of action (8-12 h).
 Bowel movements in 12 h (orally) or 2 h
(rectally as suppository).
 Given at night.
Common stimulant purgatives
Drugs Type Site of Action Onset of Action
Anthraquinone
Cascara colon 8-12 hours
Senna Anthraquinone colon 8- 12 hours
Aloe vera Anthraquinone colon 8-12 hours
Bisacodyl Diphenylmethane colon 6-8 hours
Castor Oil ricinoleic acid small intestine 2-6 hours

Side Effects
 Abdominal cramps may occur.
 Prolonged use  dependence & destruction
of myenteric plexus leading to atonic colon.
Contraindications
 Senna is contraindicated in breast feeding.
 Castor oil # in pregnancy  reflex
contraction of uterus  abortion.
Fecal Softeners
(Lubricants)/surfactants
 Are non absorbed drugs
 Act by either decreasing surface tension or by
softening the feces thus promoting defecation.
 Treat constipation in patients with hard stool
or specific conditions and for people who
should avoid straining .
Fecal Softeners
(Lubricants)/surfactants
Drugs
 Docusate
 Glycerin
 Paraffin oil
Docusate
• Sodium dioctyl sulfosuccinate
• One type of surfactants
 Act by decreasing surface tension of feces
 is given orally (12-72 hours) or enema (5-20
min).
Paraffin oil
 Is a mineral oil, given orally
 acts as lubricant thus softening the feces
and promoting defecation.
 Good for radiology preparation
 not palatable
 impairs absorption of fat soluble vitamins.
Glycerin
 Lubricant
 Given rectally (suppository)
Purgatives Site of action Onset time
Bulk purgatives Small & large 12-72 h

intestine Delayed
Saline purgatives Small & large 1-3 h
intestine Rapid
Lactulose colon 12-72 h
Delayed
Mineral oil colon 6 – 8 hours
Docusate Small and large Enema 5-20 minutes
intestine Orally 12 – 72 hours
Stimulants Small intestine See the previous table

Colon
Irritable bowel syndrome (IBS)
Chronic bowel disorder characterized by

abdominal discomfort (bloating, pain, distention,
cramps) associated with alteration in bowel
habits (diarrhea or constipation or both).
Symptomatic treatment of IBS
 Antispasmodics e.g. mebeverine
 Low doses of tricyclic antidepressants
(amitriptyline) act via
 Anticholinergic action
 Reduce visceral afferent sensation
 Laxatives in IBS with Constipation.
 Antidiarrheals in IBS with diarrhea
(diphenoxylate – loperamide).
 Alosetron (IBS-D)
 Tegaserod (IBS-C)
Alosetron
 Selective 5HT3 antagonist
 5-HT3 receptors antagonism of the enteric nervous
system of the gastrointestinal tract results into:
 inhibition of colon motility.
 inhibition of unpleasant visceral afferent pain
sensation (nausea, pain, bloating).
Uses of Alosetron
Used in IBS with severe diarrhea in women
who have not had success with any other
treatment.
Adverse effects
Constipation and ischemic colitis may occur.
People taking alosetron must sign a consent form
before starting to take the medicine.
Tegaserod
 5HT4 agonist.
 Stimulation of 5HT4 of enteric nervous system
of GIT  increases peristalsis.
 Short term treatment of IBS-associated with
constipation in women <55 years old with no
history of heart problems.
 Tegaserod has CVS side effects
 may still be used in limited emergency situations..
Summary
Bulking agents Oral, 48–72 hours Acute & chronic constipation
stool softeners oral, 24–72 hours; prevention of straining after

rectal, 5 --20 minutes rectal surgery and in acute
perianal disease
Osmotic laxatives oral, 24–72 hours - chronic constipation

(lactulose) -hepatic encephalopathy
- opioid constipation
Saline laxatives oral, 0.5–3 hours; short term treatment of

rectal, 30 minutes moderate-to-severe
constipation; acute
constipation; bowel preparation
for colonoscopy

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Drugs used in treating

constipation and IBS

Prof. Hanan Hagar

 infrequent defecation, often with straining

 May be accompanied by other symptoms:

 Local painful conditions: anal fissures, piles

 Lack of muscular exercise

Drugs that hasten the transit of food through

I) Bulk forming laxatives:

II) Osmotic laxatives:

III) Stimulant or irritant laxatives:

IV) Stool softeners (lubricants):

 Carboxymethyl cellulose (CMC)

Dietary fibers and hydrophilic colloids are non

 are water soluble compounds

 They remain in the bowel, attract and retain

Lactulose increases the H+ concentration in the

Lactulose Lactic acid + Acetic Acid

acidification of the colon ammonia

Drugs Type Site of Action Onset of Action

Senna Anthraquinone colon 8- 12 hours

Aloe vera Anthraquinone colon 8-12 hours

Bisacodyl Diphenylmethane colon 6-8 hours

Castor Oil ricinoleic acid small intestine 2-6 hours

Bulk purgatives Small & large 12-72 h

Stimulants Small intestine See the previous table

Chronic bowel disorder characterized by

stool softeners oral, 24–72 hours; prevention of straining after

Osmotic laxatives oral, 24–72 hours - chronic constipation

Saline laxatives oral, 0.5–3 hours; short term treatment of

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