ANTIDIARRHEAL AGENTS
Diarrhea
 Abnormal frequent passage of loose stool
or
 Abnormal passage of stools with increased
frequency, fluidity, an...
 Diarrhea is the condition of having three 
or more loose or liquid bowel movements 
per day. 
 For adults on a typical Western diet,
stool weight >200 g/d can generally
be considered diarrheal.
Acute diarrhea
 Sudden onset in a previously healthy
person
 Lasts from 3 days to 2 weeks
 Self-limiting
 Resolves wit...
Chronic diarrhea
 Lasts for more than 3 weeks
 Associated with recurring passage of
diarrheal stools, fever, loss of app...
 Diarrhea can be caused by
 An increased osmotic load within the intestine
(resulting in retention of water within the l...
 Pharmacotherapy of diarrhea should be
reserved for patients with significant or
persistent symptoms.
 Nonspecific antid...
ORS
 Composition of ORS :
HOME WORK
Mechanism of Action
Adsorbents
 Coat the walls of the GI tract
 Bind to the causative bacteria or toxin,
which is then e...
 Clays such as kaolin (a hydrated aluminum silicate)
and other silicates such as attapulgite (magnesium
aluminum disilica...
Side Effects
Adsorbents
 Constipation, dark stools
 Confusion, twitching
 Hearing loss, tinnitus, metallic taste,
blue ...
Mechanism of Action
Anticholinergics
 Decrease intestinal muscle tone and
peristalsis of GI tract
 Result: slowing the m...
Side Effects
Anticholinergics
 Urinary retention, hesitancy, impotence
 Headache, dizziness, confusion, anxiety,
drowsin...
Antimotility and Antisecretory Agents
OPIOIDS
 Opioids continue to be widely used in the treatment of diarrhea.
 They ac...
Loperamide
 Loperamide a Piperidine butyramide derivative with µ-
receptor activity, is an orally active antidiarrheal ag...
Diphenoxylate and Difenoxin
 Diphenoxylate and its active metabolite Difenoxin
(diphenoxylic acid) are related structural...
A/E
 They are available in preparations containing small
doses of atropine (considered subtherapeutic) to
discourage abus...
BULK-FORMING AGENTS
 Hydrophilic and poorly fermentable colloids
or polymers such as Carboxymethyl
cellulose and Calcium ...
Antidiarrheal Agents: Interactions
 Adsorbents decrease the absorption
of many agents, including digoxin,
clindamycin, qu...
Nursing Implications
 Obtain thorough history of bowel patterns, general
state of health, and recent history of illness o...
 Anticholinergics should not be
administered to patients with a history
of glaucoma, urinary retention, cardiac
problems,...
Constipation
Constipation
 Difficult, incomplete sensation, or
infrequent evacuation of dry hardened
feces from the bowels
 It is sym...
 Constipation can be corrected by adherence to a fiber-
rich (20–30 g daily) diet, adequate fluid intake,
appropriate bow...
 When stimulant laxatives are used, they
should be administered at the lowest
effective dosage and for the shortest perio...
 The terms laxatives, cathartics, purgatives, and
evacuants often are used inter changeably.
 There is a distinction, ho...
Laxatives
 1)Bulk laxatives: by increasing the
volume of non-absorbable solid residues
 Eg: Hydrophilic Colloids, Bran, ...
 3)Fecal Softners: by altering the
consistency of feces
 Eg: DOSS (dioctyl sodium sulfosuccinate), Mineral
oils, Glyceri...
Bulk laxatives
 Include hydrophilic colloids(prepared from indigestible
parts of fruits, vegetables and seeds)
 Forms ge...
Osmotic laxatives
 Saline purgatives: Laxatives containing magnesium
cations or phosphate anions commonly are called sali...
 Abd. cramps can occur
 Quick onset of action
 Advised to take plenty of water
administration of hypertonic sol may ca...
 Uses:
 For preparation of bowel before surgery
and colonoscopy
 In food/drug poisoning
Lactulose
 Semisynthetic disaccharide of fructose and
galactosenot digested or absorbed in small
intestineretains water...
Fecal softeners
 Promote more water and fat in the stools

Lubricate the fecal material and intestinal walls
 Emulsifyi...
Stimulant laxative
 They increase the peristalsis by stimulation
of gut mucosa
 Causes abd cramps, prolonged use cause
a...
 Bisacodyl: given orally and also as
suppositorydefecation in 15-30min
 Phenolphthalein: given orally
 A/E:allergic ra...
Laxatives: Side Effects
 Bulk forming
 Impaction
 Fluid overload
 Emollient (stool softener)
 Skin rashes
 Decreased...
 Saline
 Magnesium toxicity (with renal insufficiency)
 Cramping
 Diarrhea
 Increased thirst
 Stimulant
 Nutrient m...
Laxatives: Nursing Implications
 Assess fluid and electrolytes before
initiating therapy
 Patients should not take a lax...
 A healthy, high-fiber diet and increased
fluid intake should be encouraged as an
alternative to laxative use
 Long-term...
Abuse and danger of laxative
 Repeated administration may produce:
 GI disturbaces like spastic colitis, dyspepsia, anor...
The End…..
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antidiarrheal agents

  1. 1. ANTIDIARRHEAL AGENTS
  2. 2. Diarrhea  Abnormal frequent passage of loose stool or  Abnormal passage of stools with increased frequency, fluidity, and weight, or with increased stool water excretion.
  3. 3.  Diarrhea is the condition of having three  or more loose or liquid bowel movements  per day. 
  4. 4.  For adults on a typical Western diet, stool weight >200 g/d can generally be considered diarrheal.
  5. 5. Acute diarrhea  Sudden onset in a previously healthy person  Lasts from 3 days to 2 weeks  Self-limiting  Resolves without sequelae
  6. 6. Chronic diarrhea  Lasts for more than 3 weeks  Associated with recurring passage of diarrheal stools, fever, loss of appetite, nausea, vomiting, weight loss, and chronic weakness
  7. 7.  Diarrhea can be caused by  An increased osmotic load within the intestine (resulting in retention of water within the lumen)  Excessive secretion of electrolytes and water into the intestinal lumen.  Exudation of protein and fluid from the mucosa.  Altered intestinal motility resulting in rapid transit (and decreased fluid absorption).
  8. 8.  Pharmacotherapy of diarrhea should be reserved for patients with significant or persistent symptoms.  Nonspecific antidiarrheal agents typically do not address the underlying pathophysiology responsible for the diarrhea; their principal utility is to provide symptomatic relief in mild cases of acute diarrhea.
  9. 9. ORS  Composition of ORS : HOME WORK
  10. 10. Mechanism of Action Adsorbents  Coat the walls of the GI tract  Bind to the causative bacteria or toxin, which is then eliminated through the stool.  Examples: bismuth subsalicylate (Pepto- Bismol), kaolin-pectin, attapulgite.
  11. 11.  Clays such as kaolin (a hydrated aluminum silicate) and other silicates such as attapulgite (magnesium aluminum disilicate) bind water avidly and also may bind enterotoxins.  However, this effect is not selective and may involve other drugs and nutrients; hence, these agents are best avoided within 2–3 hours of taking other medications.  A mixture of kaolin and pectin (a plant polysaccharide) is a popular over-the-counter remedy (kaolin-pectin) and may provide useful symptomatic relief of mild diarrhea.
  12. 12. Side Effects Adsorbents  Constipation, dark stools  Confusion, twitching  Hearing loss, tinnitus, metallic taste, blue gums
  13. 13. Mechanism of Action Anticholinergics  Decrease intestinal muscle tone and peristalsis of GI tract  Result: slowing the movement of fecal matter through the GI tract  Examples: Atropine
  14. 14. Side Effects Anticholinergics  Urinary retention, hesitancy, impotence  Headache, dizziness, confusion, anxiety, drowsiness  Dry skin, rash, flushing  Blurred vision, photophobia, increased intraocular pressure
  15. 15. Antimotility and Antisecretory Agents OPIOIDS  Opioids continue to be widely used in the treatment of diarrhea.  They act principally through either µ- or δ- opioid receptors on enteric nerves, epithelial cells, and muscle.  These mechanisms include effects on intestinal motility (µ receptors), intestinal secretion (δ receptors), or absorption (µ and d receptors).  Commonly used antidiarrheals such as Diphenoxylate, and Loperamide act principally via peripheral µ-opioid receptors and are preferred over opioids that penetrate the CNS.
  16. 16. Loperamide  Loperamide a Piperidine butyramide derivative with µ- receptor activity, is an orally active antidiarrheal agent.  The drug is 40–50 times more potent than morphine as an antidiarrheal agent and penetrates the CNS poorly.  It increases small intestinal and mouth-to-cecum transit times.  Loperamide also increases anal sphincter tone, an effect that may be of therapeutic value in some patients who suffer from anal incontinence.  In addition, loperamide has antisecretory activity against cholera toxin and some forms of Escherichia coli toxin
  17. 17. Diphenoxylate and Difenoxin  Diphenoxylate and its active metabolite Difenoxin (diphenoxylic acid) are related structurally to meperidine.  As antidiarrheal agents, diphenoxylate and difenoxin are somewhat more potent than morphine.  Both compounds are extensively absorbed after oral administration, with peak levels achieved within 1–2 hours.  Both drugs can produce CNS effects when used in higher doses (40–60 mg/day) and thus have potential for abuse and/or addiction.
  18. 18. A/E  They are available in preparations containing small doses of atropine (considered subtherapeutic) to discourage abuse and deliberate overdosage.  With excessive use or overdose, constipation and (in inflammatory conditions of the colon) toxic megacolon may develop.  In high doses, these drugs cause CNS effects as well as anticholinergic effects from the atropine (e.g., dry mouth, blurred vision)
  19. 19. BULK-FORMING AGENTS  Hydrophilic and poorly fermentable colloids or polymers such as Carboxymethyl cellulose and Calcium Polycarbophil absorb water and increase stool bulk.  They usually are used for constipation but are sometimes useful in mild chronic diarrhea in patients suffering with Irritable Bowel Syndrome (IBS-A).
  20. 20. Antidiarrheal Agents: Interactions  Adsorbents decrease the absorption of many agents, including digoxin, clindamycin, quinidine, and hypoglycemic agents.
  21. 21. Nursing Implications  Obtain thorough history of bowel patterns, general state of health, and recent history of illness or dietary changes, and assess for allergies  DO NOT give bismuth subsalicylate to children younger than age 16 or teenagers with chickenpox because of the risk of Reye’s syndrome.
  22. 22.  Anticholinergics should not be administered to patients with a history of glaucoma, urinary retention, cardiac problems, myasthenia gravis.
  23. 23. Constipation
  24. 24. Constipation  Difficult, incomplete sensation, or infrequent evacuation of dry hardened feces from the bowels  It is symptom, not a disease  Disorder of movement through the colon and/or rectum  Can be caused by a variety of diseases or drugs
  25. 25.  Constipation can be corrected by adherence to a fiber- rich (20–30 g daily) diet, adequate fluid intake, appropriate bowel habits and training, and avoidance of constipating drugs.  Constipation related to medications can be corrected by use of alternative drugs where possible, or adjustment of dosage.  If nonpharmacological measures alone are inadequate, they may be supplemented with bulk- forming agents or osmotic laxatives.
  26. 26.  When stimulant laxatives are used, they should be administered at the lowest effective dosage and for the shortest period of time to avoid abuse.  Habitual use of laxatives may lead to excessive loss of water and electrolytes; secondary aldosteronism may occur if volume depletion is prominent.
  27. 27.  The terms laxatives, cathartics, purgatives, and evacuants often are used inter changeably.  There is a distinction, however, between laxation (the evacuation of formed fecal material from the rectum) and catharsis (the evacuation of unformed, usually watery fecal material from the entire colon).  Laxatives are employed before surgical, radiological, and endoscopic procedures where an empty colon is desirable.
  28. 28. Laxatives  1)Bulk laxatives: by increasing the volume of non-absorbable solid residues  Eg: Hydrophilic Colloids, Bran, Methylcellulose, Psyllium, Ispaghula  2)Osmotic laxative: by increasing the water content  Eg: Saline purgatives:MgSo4 (Epsom salts), Mg(OH)2 (MOM), Lactulose
  29. 29.  3)Fecal Softners: by altering the consistency of feces  Eg: DOSS (dioctyl sodium sulfosuccinate), Mineral oils, Glycerin suppositories  4)Stimulant/Irritant Purgative/laxative: by increasing the motility and secretion  Eg: Senna, Cascara, Castor oil, Bisacodyl. Phenolphthalein
  30. 30. Bulk laxatives  Include hydrophilic colloids(prepared from indigestible parts of fruits, vegetables and seeds)  Forms gel in large intestinecause water retention and intestinal distension increase peristaltic activity  Are first line approach for most pts of simple constipation  Uses:  Habitual constipation in elderly pts  hemorrhoids pts
  31. 31. Osmotic laxatives  Saline purgatives: Laxatives containing magnesium cations or phosphate anions commonly are called saline laxatives: magnesium sulfate, magnesium hydroxide, magnesium citrate,sodium phosphate  Solutes that are not absorbed in intestineretain more water osmoticallydistend the bowelincrease peristalsisleads purgation about an hour later
  32. 32.  Abd. cramps can occur  Quick onset of action  Advised to take plenty of water administration of hypertonic sol may cause dehydration
  33. 33.  Uses:  For preparation of bowel before surgery and colonoscopy  In food/drug poisoning
  34. 34. Lactulose  Semisynthetic disaccharide of fructose and galactosenot digested or absorbed in small intestineretains water  In colonbacteria convert it into two component sugarfermentationlactic acid and acetic acidfunction as osmotic laxative  After lactulose administration, gut contents have low pH than normaldecrease activity of ammonia producing organismhence used in treatment of hepatic encephalopathy
  35. 35. Fecal softeners  Promote more water and fat in the stools  Lubricate the fecal material and intestinal walls  Emulsifying effect on fecesmake them retain more watersofter stooleasier to pass out  Abd cramps can occur  Uses: condition where straining at stool has to be avoided like hernia, piles, fissures, anal surgery
  36. 36. Stimulant laxative  They increase the peristalsis by stimulation of gut mucosa  Causes abd cramps, prolonged use cause atonic colon(sluggish bowel)  Used mainly for preparation of bowel for surgery, colonoscopy and abd X-rays
  37. 37.  Bisacodyl: given orally and also as suppositorydefecation in 15-30min  Phenolphthalein: given orally  A/E:allergic rashes in skin
  38. 38. Laxatives: Side Effects  Bulk forming  Impaction  Fluid overload  Emollient (stool softener)  Skin rashes  Decreased absorption of vitamins  Hyperosmotic  Abdominal bloating  Rectal irritation
  39. 39.  Saline  Magnesium toxicity (with renal insufficiency)  Cramping  Diarrhea  Increased thirst  Stimulant  Nutrient malabsorption  Skin rashes  Gastric irritation  Rectal irritation All laxatives causes electrolyte imbalance
  40. 40. Laxatives: Nursing Implications  Assess fluid and electrolytes before initiating therapy  Patients should not take a laxative if they are experiencing nausea, vomiting.
  41. 41.  A healthy, high-fiber diet and increased fluid intake should be encouraged as an alternative to laxative use  Long-term use of laxatives often results in decreased bowel tone and may lead to dependency
  42. 42. Abuse and danger of laxative  Repeated administration may produce:  GI disturbaces like spastic colitis, dyspepsia, anorexia and nausea  Nutritional deficiencies of calories, vitamins, minerals  Loss of fluids and electrolytes  Complete dependency on drugs
  43. 43. The End…..
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