This document discusses the classification, mechanisms of action, and uses of various laxatives and purgatives. It covers bulk forming laxatives like fiber, stool softeners like docusate, and stimulant laxatives like bisacodyl and anthraquinones found in senna and cascara. It also discusses osmotic laxatives like magnesium salts and lactulose. The document provides details on the treatment of constipation and diarrhea, including the use of oral rehydration solutions, antimicrobial drugs, and nonspecific antidiarrheal medications.

1. Dr Anuj
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2.  Laxatives are used
1) To treat constipation
2) To avoid undue straining atdefecation
3) Before or after any anorectal surgery
4) In bedridden patients
Laxatives have mild activity and are usually stool
softeners.
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3.  Purgatives are used for complete colonic cleansing
prior to GI endoscopic procedures, pre-post MI
bed ridden patients , also to prepare bowel before
surgery or abdominal X-ray, may be needed for
neurologically impaired patients.
 Purgative either provide semisolid stool or lead to
watery evacuation
 In low doses these can be used as laxative also
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4. CLASSIFICATION
1. Bulk forming:- Dietary fibre : Bran Psyllium,Ispaghula
2. Stool softener :- Docusates (DOSS), Liquidparaffin
3. Stimulant purgative
a) Diphenylmethanes:- Phenolphthalein, Bisacodyl
b) Anthraquinones(Emodins) :- Senna, Cascara sargada
c) 5HT4 agonist:- Prucalopride
d) Fixed oil :- Castoroil
5. Osmotic purgatives :-
Magnesium salts : sulfate ,hydroxide
Sodium salts: sulfate phaophate
Sod. Pot. Tartrate
Lactulose
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5. Bulk forming
 Luminally active, hydrophilic indigestible vegetablefibres
 Stimulates peristalsis and defecation reflexes by increasing
faecal bulk
 Adequate water must be taken with all Bulk forming agents
 Effect appears within 1-3days
 S/E Bloating and flatus causing abdominaldiscomfort
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6. Stool softener : Docussates(Dioctyl sodium sulfosuccinate)
 Also known as surfactantlaxatives
 Luminally active agents , an anionic surfactant , softens
stool by decreasing surface tension of fluids in the bowel.
 100-400 mg oral per day in divided doses
 Indicated when straining at defecation is avoided
 Latency period 1-3 day
 Bitter in taste can causenausea
 Cramps and abdominal pain mayoccur
 Hepatotoxicity may occur after prolongeduse
 Increases absorption of liquid paraffin , hence shouldnot
be given together
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7. Stimulant purgative
 Stimulate peristalsis by irritant action on intestinal mucosa
 Also stimulate colonic electrolyte and fluid secretion by altering
absorptive and secretory activity of mucosal cells.
 Inhibit Na+ K+ ATPase at the bosolateral membrane ofvillous
cells
 Secretion is enhanced by activation of cAMP in crypt cells as well
as by increasing PG synthesis
 Laxative action of bisacodyl and cascara is dependent upon NO
synthesis/action in colon
 Larger dose of stimulant purgative can lead to purgation
resulting in fluid and electrolyte imbalance, hypokalemia.
 Regular and long term use – colonic atony
 Can reflexly stimulategravid uterus- C/I in Pregnancy
 Oter C/I- Subacute or Chronic intestinal obstruction
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8. Bisacodyl: (DULCOLAX 5 mg)
 Partly absorbed and reexcreted inbile.
 Activated in intestine bydeacetylation.
 Primary site of action is colon- Irritate mucosa,
produce inflammation & increase secretion
 Effect appears within 6-8hrs.
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9. Anthraquinones: Senna, Cascara sargada
 Senna : Leaves and pods of Cassiaspp.
 Cascara sargada: bark of buck thornetree
 Degraded by colonic bacteria to liberate anthrol form
which either acts locally or absorbed into circulation and
excreted in bile to act on smallintestine
 Takes 6-8 hrs to produceaction
 Active principle of these drugs act on myenteric plexus to
increase peristalsis and decreasesegmentation
 Senna has been found to stimulate PGE2 secretion in rats
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10.  Prucalopride :- selective 5HT4 receptoragonist
for tt of chronic constipation in women
 Tegaserod :- 5HT4 receptor partial agonist ,
 Used for tt of constipation predominant IBS
Withdrawn from market due to cardiovascular risk
 Lubiprostone: PG analogue, activates Chloride channel in
small intestine to promote intestinal secretions and
motility
 used for tt of constipation predominantIBS
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11. Osmotic purgatives
 These are soluble inprganic salts , that increases the faecal
bulk by retaining water osmotically and distend the bowel
increasing peristalsis indirectly.
 Act on small aswell as large intestine
 Magnesium salts release Cholecystokinin which further
helps in increasing intestinal secretions and peristalsis.
 Milk of Magnesia is most commonly used , other salts have
an unpleasant taste
 30 ml of its 8% w/w suspension is given in morning, effects
comes within 2-3 hrs.
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12.  Usually preferred for bowel preparation before surgery,
colonoscopy, in food/drug poisoning and as after purge in
tt of tapeworm infestation
 Should not be used for prolonged period in pt with renal
insufficiency due to risk ofhypermagnesaemia.
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13. Lactulose(DUPHALAC 10gm/15ml syp)
 Semisynthetic disaccharide of fructose and lactose, neither
digested nor absorbed in small intestine-retainswater
 Broken down in the colon by bacteria to osmotically more
active product
 Produces soft, formed stool in 1-3days.
 Flatulence and flatus is common , cramps occur in
few,some pt may feel nauseated due to peculiar sweet taste
 Also used for tt of hepatic encephalopathy in dose of 20gm
TDS orally
 Lactulose is degraded tolactic acid and converts NH3 to
ionised NH4+ salts which is then excreted.
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14. Questions
 Active principle of these drug act on myenteric plexus
 Anthraquinones (Senna & cascarasargada)
 Lactulose is used in ttof
 Hepatic encephalopathy
 It turns urine pink ifalkaline
 Phenolphthalein
 Cholecystokinin is release by
 Magnesium salts
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15.  Alvimopan
peripherally acting μ opioid receptor antagonist for the
tt of postoperative ileus and constipation after surgery
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16. TREATMENT OF DIARRHOEAS
 Too frequent, often too precipitate passage of poorly
formed stool
 WHO “ 3 or more loose or watery stools in a 24 hr
period”
 Cause
 ↓ed electrolyte and water absorption
 ↑ed secretion by intestinal mucosa
 ↑ed luminal osmotic load
 Inflmm of mucosa & exudation into lumen
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17. 1. Treatmrnt of fluid depletion, shock andacidosis
2. Maintainance of Nutrition
3. Drug therapy
 Oral rehydration if fluid loss is mild 5-7%BW
 IV rehydration only when fluid loss is > 10% of BW
 Dhaka fluid
 NaCl -85 mM=5gm
 KCl- 13MM=1gm,
 NaHCO3 48mM =4gm in 1 ltr of water
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18.  New formula WHO-ORS
 NaCl: 2.6g
 KCl: 1.5G
 Trisod. Citrate : 2.9 g
 Glucose : 13.5 g
 Water : 1 L
Total osmolarity 245 mOsm/L
 Zinc in pediatricdiarrhea
 Maintainance of nutrition
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19. Drug Therapy
1. Special antimicrobial drug
2. Probiotics
3. Drugs for Inflammatory boweldisease
4. Nonspecific antidiarrhoeal drug
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20.  antimicrobial drug are of no value in diarrhoea due to
noninfectious causes
1. IBS
2. Coeliac disease
3. Pancreatic enzyme deficiency
4. Tropical Sprue
5. Thyrotoxicosis
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21.  antimicrobial drug are useful in severe cases of
1. Travellers diarrhoea :- Cotrim, Norflox, Doxy, Rifaximin
2. EPEC :- Cotrim, FQ
3. Shigella enteritis :- Cipronorflox
4. Nontyphoid salmonella :- FQ Cotrim
5. Yersinia :- Cotrim Cipro
 Antimicrobial drug are regularly usefulin
1. Cholera :- Fluid replcement, Tetracyclin, Cotrim,
2. C. jejuni:- Norflox and otherFQ
3. Clostridium difficile:- Metronidazole, Vancomicin
4. Amoebiasis, giardiasis :- Metron , Diloxfuroate
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22. •Drugs for IBD(Inflammatory bowel disease)
 chronic relapsing inflammatory disease of ileum colon or both a/w
systemic manifestation
Drugs used can be groupedin
 5-ASA compounds
 Corticosteroids
 Immunosuppressants
 TNF-α inhibitors
A. Ulcerative colitis:-Aminosalicylates(sulfasalazine),glucocorticoids,
cyclosporine,azathioprine , 6-mercaptopurine
B. Crohn’s disease :-
AntiTNF-α drugs( Infliximab adalimumab, Certolizumab),
Methotrexate, Antibiotics( metron cipro), Anti integrin monoclonal
antibody (Natalizumab)
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23. ❖ 5-ASA compounds( Sulfasalazine)
Azo bond split by colonic bacteria to release 5-ASA & sulfapyridine
5-ASA :- exerts antiinflammatoryeffect
sulfapyridine :- serves to carry 5-ASA to colon without being
absorbed proximally.
 Mesalazine
 Olsalazine
 Balsalazide
❖ Corticosteroid :- 40-60 mg/day
❖ Immunosoppressant :- Azathioprine (purineantimetabolite)
Methotrexate(DHFRase inhibitor)
Cyclosporine
TNF-α inhibitors :- Infliximab
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24. Nonspecific antidiarrhoeal drugs
1. Antisecretory drugs
2. Antimotility drugs
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25. Antisecretory drugs
 Racecadotril:- (Thiorphan)Enkephalinase inhibitor
↓ intestinal hypersecretion without affecting motility
lowers mucosal cAMP due to enhanced ENK action
indicated in short term treatment of acute secretary diarrhoea
(REDOTIL 100 mg cap)
 Bismuth subsalicylate
 Anticholinergics
 Octreotide
 Opioids
α2 adrenergic receptor agonist :-clonidine
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26. Antimotility drugs
 Opioid drugs which increase small bowel tone and
segmenting activity,
 ↓ propulsive movements,
 ↓ intestinal secretions ,
 enhancing absorptions
 Diphenoxylate (2.5mg) + atropine(0.025mg):- LOMOTIL
 Loperamide
opiate analogue with major peripheral μ opioid and weak additional
anticholinergic property
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27. Probiotics in Diarrhoea : (ECONORM,
BIFILAC, ENTEROGERMINA)
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28.  Drug used for tt of dirrhoea in diabetic pt
 Clonidine
 Drug used to treat secretarydiarrhoea
 Octreotide
 Variceal blleeding can be controlledby
 Octreotide
 Alosetron ,a drug useful in pt of Irritable bowel
syndrome with diarrhea actsthrough
 5-HT3 receptor antagonist
 An effective antidiarrhoeal agent that inhibits
peristalsis movt
 Diphenoxylate
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