Pharmacology Sem VII University of Mumbai

2.  Common complaint in clinical practice.
 Definition of constipation includes the following :
▪ Infrequent bowel movements (typically three times or fewer
per week) .
▪ Difficulty during defecation .
▪ The sensation of incomplete bowel evacuation.
 Rome III criteria are widely used to diagnose chronic
constipation.

3. the large amount of stool throughout the colon on this
radiograph.

4.  Eating foods low in fiber.
 Not drinking enough water (dehydration).
 Not getting enough exercise.
 Changes in your regular routine, such as traveling or eating or
going to bed at different times.
 Eating large amounts of milk or cheese.
 Stress.
 Resisting the urge to have a bowel movement.

5.  more of criteria listed below:
▪ Straining efforts in course of defecation at least in 25% of
defecations
▪ Solid stool at least in 25% of defecations
▪ Feeling of incomplete evacuation at least in 25% of defecations.
▪ Feeling of anorectal obstruction at least in 25% of defecations.
▪ Need in hand manipulation to facilitate the defecation at least in
25% of defecations
▪ Less than 3 defecations per week.
 Criteria fulfilled for the last 3 months with symptom onset.

6.  Causes of constipation can be divided into primary and secondary.
 Most common - Primary or functional constipation is not due to any
underlying cause.
 Secondary causes:
▪ Immobility
▪ Improper Diet
▪ Endocrine & Metabolic Disorders
▪ Neurological Disorders
▪ Psychological Conditions
▪ Structural Abnormalities
▪ Medications

7.  These are drugs that promote evacuation of bowels. A
distinction is sometimes made according to the intensity of
action.
 a) Laxative or aperient: milder action, elimination of soft but
formed stools.
 b) Purgative or cathartic: stronger action resulting in more
fluid evacuation.

8. Class of Drug Examples
Bulk forming Dietary fibre : Bran , Psyllium ( Plantago) Ispaghula,
Methylcellulose
Stool softener Docusates (DOSS) , Liquid paraffin
Stimulant purgatives a) Diphenylmethanes : Phenolphthalein, Bisacodyl ,
Sodium picosulphate
b) Anthraquinones ( Emodins) : Senna , Cascara
,sagrada
c) 5-HT4 agonist : Prucalopride
d) Fixed oil : Castor oil
Osmotic purgatives • Magnesium salts : sulphate , hydroxide
• Sodium salts : sulphate , phosphate
• Sod.pot. Tartrate
• Lactulose

9.  Residual product of flour industry which consist of 40% of
dietary fiber.
 Consist of un-absorbable – cellulose , lignin, pectins,
glycoproteins & other polysaccharides.
 MECHANISM OF ACTION:-
▪ Absorbs water in the intestines, swells, increases water
content of faeces- softens it and facilitates colonic transit.
▪ Dietary fiber supports bacterial growth in colon which
contribute to faecal mass.

10.  First line approach for most patients of simple constipation.
 Reduces Recto sigmoid intraluminal pressure.
 Relieves symptoms of irritable bowel syndrome (IBS) including
pain, constipation as well as diarrhoea.
 DRAWBACKS :
▪ Unpalatable
▪ Large quantity (20-40 g/day) needs
▪ Does not soften faeces already present in colon or rectum
▪ Should not be used in patients with gut ulcerations, adhesions.

12.  They contain natural colloidal mucilage
 MECHANISM OF ACTION:
▪ Forms a gelatinous mass by absorbing by water
▪ Largely fermented in colon increase bacterial mass & softens
the faeces.
 USES: Useful in both constipation & diarrhea
 DRAWBACKS: If taken dry ,can cause esophageal impaction
 DOSE: 3-12 g refined husk freshly mixed with water or milk
and taken daily –acts in 1-3 days.

13. Psyllium & Isabgol seed

14.  It is a anionic detergent, softens the stool by decreasing
the surface tension of fluids in bowel.
 Emulsifies the colonic content and increases penetration
of water into the faeces.
 DOSE: 100-400 mg/day
 USES: Indicated when straining at stools must be avoided.
 DRAWBACKs :
▪ Can disrupt the mucosal barrier and enhance absorption
of many non- absorbable drugs .
▪ e.g liquid- paraffin –should not be combined with it .
▪ Cramps and abdominal pain can occur.
▪ Bitter; liquid preparation may cause nausea

15.  It is a viscous liquid
 A mixture of petroleum hydrocarbon
 USES - Soften stools and is said to lubricate by coating them
 DOSE :
15-30ml/day-oil as such or in emulsified form
 DRAWBACKS :
Unpleasant to swallow
Small amount passes in to intestinal mucosa →may
produce foreign body granuloma in intestinal submucosa.
Carries away fat soluble vitamins with it into the stools;
deficiency may occur on chronic use

16.  Activated in intestine by deacetylation
 Site of action is in colon: irritate the mucosa, produce mild
inflammation → stimulate peristalsis.
 DOSE:
Phenolphthalein: 60-130 mg
Bisacodyl: 5-15 mg
 DRAWBACKS:
Allergic reaction- skin rashes, fixed drug eruption ,Stevens
Johnson syndrome have been reported.
Phenolphthalein has been found to produce tumours in mice and
genetic damage; the US-FDA has ordered its withdrawal from market.

17.  Senna is obtained from leaves of certain Cassia sp.
 Cascara, sagrada is the powdered bark of the buck-thorn tree.
 These contain anthraquinone -glycosides ,also called Emodins.
 MECHANISM OF ACTION:-
In the colon bacteria liberate the active anthrol form, which either acts
locally or is absorbed into circulation.
The active principle acts on the myenteric plexus to increase peristalsis.
 DOSE: 12- 18 mg
 DRAWBACKS:
Skin rashes are seen occasionally
Regular use for 4-12 months causes mucosal pigmentation (melanosis).

18.  It is a selective 5-HT4 receptor agonist marketed recently in UK,
Europe and Canada for chronic constipation, when other laxative
fail.
 It activates 5-HT4 receptor on intrinsic enteric neurons to
promoting propulsive contraction in ileum and more prominently in
colon .
 Enhance release of excitatory transmitter Ach Colonic transit and
stool frequency is improved - predominant irritable bowel
syndrome.
 DOSE:- 2 mg OD.
 SIDE EFFECT:- Headache, dizziness, fatigue, abdominal pain &
diarrhea.

19.  Bland vegetable oil the seeds of Ricinus communis
 MECHANISM OF ACTION:
1. It mainly contain triglyceride of ricinoleic acid which is a polar long
chain fatty acid.
2. Castor oil hydrolyzed in the ileum by lipase to ricinoleic acid. Which acts
primarily in the small intestine to stimulate secretion of fluid and
electrolytes and speed intestinal transit.
 DOSE: 30 ml oil
 DRAWBACKS:
1. unpalatable
2. Frequent cramping, possibility of dehydration and after constipation
(due to complete evacuation of colon).

20.  Solute that are not absorbed in the intestine retain water osmotically and distend
the bowel –increasing peristalsis indirectly.
 Magnesium salt also release cholecystokinin which augment motility and
secretion.
 DOSE:
1. Mag.hydroxide (as 8% w/w suspension-milk of magnesia) 30ml.
2. Mag.sulfate : 5-15g.
3. Sod.sulfate : 10-15g.
4. Sod.phosphate: 6-12g
5. Sod.pot.tartrate: 8-15g
6. Salt taken in above mentioned doses, dissolved in 150-200 ml of water
 DRAWBACK: Unpleasant, vomiting, produce watery stool & after constipation

21.  It is a disaccharide of fructose and lactose which is
neither digested nor absorbed in the small
intestine-retains water.
 It increase faecal bulk by hydrophilic action and
also due to osmotic action.
 DOSE: 10 mg BD with plenty of water
 DRAWBACK:
 Flatulence and flatus is common, cramp also
occur.
 Nausea due to its peculiar sweet taste.

23.  Also called: IBS, spastic colon
 An intestinal disorder causing pain in the stomach, wind,
diarrhoea and constipation.
 The cause of irritable bowel syndrome isn't well understood. A
diagnosis is often made based on symptoms.
 Symptoms include abdominal pain, bloating, diarrhoea and
constipation.
 Some people can control their symptoms by managing diet,
lifestyle and stress. Others will need medication and
counselling.

24.  Also called: piles
 Swollen and inflamed veins in the rectum and anus that cause
discomfort and bleeding.
 Haemorrhoids are usually caused by straining during bowel
movements, obesity or pregnancy.
 Discomfort is a common symptom, especially during bowel
movements or when sitting. Other symptoms include itching and
bleeding.
 A high-fibre diet can be effective, along with stool softeners. In some
cases, a medical procedure to remove the haemorrhoid may be
needed to provide relief.

25.  Gastrointestinal diseases affect the gastrointestinal (GI) tract from the
mouth to the anus.
 There are two types: functional and structural. Some examples include
nausea/vomiting, food poisoning, lactose intolerance and diarrhea.
 six of the most common gastrointestinal problems –
1. Gastroesophageal Reflux Disease (GERD)
2. Chronic Diarrhea.
3. Chronic Constipation.
4. Gastroenteritis.
5. Ulcers.
6. Hemorrhoids.

26.  Hardened stool that's stuck in the rectum or lower colon due to
chronic constipation.
 Faecal impaction often occurs in people who've been
constipated for a long time. Fibre added to the diet, exercise
and laxatives may prevent impaction.
 Symptoms include stomach cramps, bloating and stool leakage.
 A doctor may insert one or two fingers to break up the stool in
the rectum. A warm mineral enema then softens the stool, to
aid in its elimination.

27.  gastrointestinal condition in which digested material is prevented
from passing normally through the bowel.
 It can be caused by fibrous tissue that compresses the gut, which
can develop many years after abdominal surgery. It can also be
caused by certain medication.
 Symptoms may include severe abdominal pain, nausea, vomiting
and an inability to pass wind or stools.
 Treatment includes avoiding solid foods, using pain and nausea
medication and close monitoring. A tube can be inserted to help
relieve pressure. Depending on the severity of the obstruction,
surgery may be required.

29.  https://www.slideshare.net/DrResuNehaReddy/drugs-for-
constipation-and-diarrhea
 https://www.niddk.nih.gov/health-information/digestive-
diseases/constipation
 https://medlineplus.gov/constipation.html
 https://emedicine.medscape.com/article/184704-overview