Treatment of
Constipation
Dr. Lokeshwar Chaurasia
Assistant Professor
Dept. Of Pharmacology
JMC-TH
Physiology of defecation
Pendular movement-Alternating
contraction and relaxation of the
longitudinal muscles, causing a portion of
s. intestine to shorten and lengthen.
Function: moves chyme back and forth
Segmental- Contraction of circular
muscle
Function: mixes chyme
Peristaltic-peristalsis help in propulsion
Normally food leaves the stomach in ½ to 2.5 hrs
and its residue reaches to caecum by approx. 5-6
hrs
Approx. 18-24 hrs is required before the process
of evacuation starts.
Complete clearance takes in approx. 5-6 days
Absorption takes place in s. intestine and caecum.
So, Laxative which act in s. intestine, likely
produce fluid loss
Where as laxative which act only on colon
produce less fluid loss and also don’t interfere
with absorption of food
Introduction
Constipation – Functional impairment of
inherent capacity of colon to propel
normally formed stool at regular interval
An infrequent production of hard stool or a
sense of incomplete evacuation
Decreased frequency of defecation with
discomfort or difficulty
Not moving your bowels on a regular
basis or feeling like you still need to move
your bowels.
Constipation: Definition
Rome Criteria:
Straining ≥ 25% of the time
Hard stools ≥ 25% of the time
Incomplete evacuation ≥ 25% of
the time
< 3 bowel movements per week
Constipation can be self-corrected to some extent
by:-
a. An increase in the roughage (fibrous
content) in the daily diet.
b. An increase in daily fluid intake
c. An increase in physical activity
d. Not neglecting the nature’s call
e. Adjusting the daily routine
f. Selecting alternate drugs that cause less
constipation as side effects
g. Correcting the underlying pathology.
If this fails to overcome the constipation,
laxatives and the purgatives can be used.
Their effectiveness
Aperient (to get rid of) < Laxatives (to
loosen) < Emollient (to smooth & soften)
< Evacuant (to empty) < Purgative (to
clean) < Cathartic (to utterly clean)
Drugs causing constipation
1) NSAIDs 7) TCA
8) Antacids containing
2) Opiates: Orally
administered opiates
calcium carbonate or
have greater inhibitory aluminum hydroxide
effect than parenterally 9) Barium sulfate
administered agents 10)CCB
3) Anticholinergics 11)Clonidine
4) Antihistamines 12)Ganglionic blockers
5) Antiparkinsonian agents 13)Iron preparations
(e.g., benztropine or 14)Muscle blockers (D -
trihexyphenidyl) tubocurarine,
6) Phenothiazines succinylcholine)
Laxative promotes and facilitate bowel
evacuation by acting locally to stimulate
intestinal peristalsis ,to soften bowel contents ,or
both
A distinction is made according to intensity of
action
Laxative or aperient-milder action,elimination
of soft and formed stool
Purgative or cathartic-stronger action
resulting in more fluid evacuation
Many drug at low dose act as laxative and at
high dose as purgative
Classification of laxatives
1. Bulk-forming laxatives
Bran, methylcellulose, Ispaghula
2. Stool softners
Docusate sodium, liquid paraffin
3. Osmotic purgatives
Magnesium sulfate, Magnesium hydroxide, Sodium
sulfate, Lactulose
4. Stimulant purgatives
Phenolphthalein, Bisacodyl, Castor oil, Cascara
sagrada, Senna
Differences
LAXATIVE PURGATIVE
Elimination of soft Strong action-result in
and formed feces more fluid evacuation
Mild dose-laxative High dose-purgative
Action 1-3 days Action within1-3 hrs to
Use- to return at 6-8 hrs
normal evacuation of For clinical
stool examination
To remove worm
1- Bulk-forming agents(active after 12-36hrs)
Drugs: (taken as granules, powders or tablets)
1.Methylcellulose 2. Bran
Mechanism of action of bulk-forming agents:
hydrophilic colloids- absorb water in the
intestine- swells-increase water content of feces-
soften it –and facilitate colonic transit
They increase stool bulk and water content
(make stools bulky (→ stimulate peristalsis) and
soft → easy to pass) (similar to natural fiber)
BULK FORMING LAXATIVE: MOA
Bulk-forming agents (cont.)
Indications:
1. They are the first-line treatment of constipation
2. Conditions where dietary intake of fibers can not be
increased
Precautions:
Adequate fluid intake to avoid intestinal
obstruction
Adverse effects of bulk-forming laxatives:
1.Abdominal distension
2.Intestinal obstruction when not consumed with
sufficient fluid
2. Fecal softeners/emollient
laxatives
A.Docusate salts (weak laxatives) - Anionic detergents
Mechanism of action:
1.Reduces water surface tension of stools →
increases penetration of fluids into feces → soft
bulky stools
2.Stimulate intestinal fluid secretion (by altering
mucosal permeability)
Dosage forms:
3.Oral form (active within 1-3 d)
4.Rectal form has a rapid onset of action but is
contraindicated in hemorrhoids and anal
Uses:
1. Used in hospitalized patients following
myocardial infarction or surgery, when
straining at defecation should be avoided.
2. They have little role in the management of
chronic constipation, except when the
patient is fluid-restricted or incapable of
increasing his or her dietary fiber or activity.
Fecal softeners/emollient laxatives (cont.)
B. Mineral oil:
Mechanism of action:
1. Indigestible and with minimal absorption.
Coat stool and allow easier passage.
2. Inhibit colonic absorption of water →
increasing stool weight and decrease stool
transit time.
Dosage forms:
Oral or rectal. Laxative effect is noted after 2 or
3 days of oral use.
Indications: Similar to docusates
Fecal softeners/emollient laxatives (cont.)
Mineral oil:
Adverse effects:
1. May be absorbed systemically → foreign-body
reaction in lymphoid tissue.
2. May be aspirated (in debilitated or recumbent
patients) → lipoid pneumonia
3. Decreases absorption of fat-soluble vitamins
(A, D, E, and K)
4. When given orally, mineral oil may leak from
the anal sphincter.
3.Osmotic Purgatives:
These are solutes that are not absorbed in the
intestine, osmotically retain water & increase the
bulk of intestinal contents.
They increase peristalsis & expel a fluid stool.
Magnesium hydroxide, magnesium sulphate, sodium
sulphate, etc
Magnesium ions release cholecystokinin which
augments motility and secretion, contributing to their
purgative action.
Lactulose is a synthetic disaccharide that is not
absorbed, holds water & acts as an osmotic
purgative.
Flatulence & cramps may accompany.
In the colon, lactulose is fermented to lactic &
acetic acids which inhibit the growth of
ammonia-producing bacteria.
Also inhibits the absorption of ammonia by
lowering pH & thus lowers blood ammonia level.
It can hence be used in hepatic coma as hepatic
coma is worsened by ammonia.
4. Stimulant purgatives:
They are powerful purgatives,acting on large
bowel, produce gripping pain, irritate intestinal
mucosa and stimulate motor activity.
They are given in an inactive form →
hydrolyzed in the GIT into active forms → GIT
irritation → modify permeability of the mucosal
cells → ↑ fluid and electrolyte secretion in the
GIT → distension → evacuation of soft (or liquid)
bulky stools.
They probably cause direct stimulation of the
When Cascara sagrada & senna are given
orally, active anthraquinones are liberated in
the intestine which stimulate the myenteric
plexus in the colon.
Evacuation takes 6-8 hrs
Prolonged use may result in melanotic
pigmentation of the colon.
Contraindicated in breastfeeding as active
metabolites may get excreted through breast
milk.
Bisacodyl when administered oral, 5 mg (the
laxative effects after a dose occurs after 6 – 12
hours; & as rectal suppository, 10 mg, (the
laxative effect occurs within 30 to 60 min).
Adverse effects include inflammation, mucosal
damage and abdominal cramps.
Phenolphthalein acts on the colon after 6-8
hrs to produce soft, semiliquid stools.
It undergoes enterohepatic circulation which
prolongs its action.
Allergic rxns including pink coloured skin
eruptions limit its use.
Phenolphthalein has been found to produce
genetic damage and tumours in mice so
the US-FDA has ordered its withdrawal from the
market
Castor oil is hydrolysed in the intestine to
ricinoleic acid which is a local irritant &
increased intestinal motility.
Powerful and one of the oldest purgative.
Stool is semiliquid.
It is generally not preferred these days.
Laxative abuse syndrome
Mechanism:
1. With the use of strong purgatives, the colon may be so thoroughly evacuated that a
bowel movement may not occur normally until a few days later. This delay reinforces
the need for more laxative. Eventually the patient may require daily laxatives to
maintain bowel function.
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