antidiarrheal agents
TRANSCRIPT
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ANTIDIARRHEAL AGENTS
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Diarrhea
Abnormal frequent passage of loose stool
or
Abnormal passage of stools with increased frequency, fluidity, and weight, or with increased stool water excretion.
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Diarrhea is the condition of having three or more loose or liquid bowel movements per day.
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For adults on a typical Western diet, stool weight >200 g/d can generally be considered diarrheal.
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Acute diarrhea Sudden onset in a previously healthy person
Lasts from 3 days to 2 weeks
Self-limiting
Resolves without sequelae
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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
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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).
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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.
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ORS
Composition of ORS :
HOME WORK
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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.
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Clays such as kaolin (a hydrated aluminum silicate) and ot
her 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.
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Side Effects
Adsorbents
Constipation, dark stools
Confusion, twitching
Hearing loss, tinnitus, metallic taste, blue gums
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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
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Side Effects
Anticholinergics
Urinary retention, hesitancy, impotence
Headache, dizziness, confusion, anxiety, drowsiness
Dry skin, rash, flushing
Blurred vision, photophobia, increased intraocular pressure
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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.
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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
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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.
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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)
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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).
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Antidiarrheal Agents: Interactions
Adsorbents decrease the absorption of many agents, including digoxin, clindamycin, quinidine, and hypoglycemic agents.
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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.
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Anticholinergics should not be administered to patients with a history of glaucoma, urinary retention, cardiac problems, myasthenia gravis.
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Constipation
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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
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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.
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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.
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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.
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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
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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. Phenolphthale
in
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Bulk laxatives
Include hydrophilic colloids(prepared from indigestible parts of fruits, vegetables and seeds)
Forms gel in large intestinecause 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
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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 intestineretain more water osmoticallydistend the bowelincrease peristalsisleads purgation about an hour later
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Abd. cramps can occur
Quick onset of action
Advised to take plenty of water administration of hypertonic sol may cause dehydration
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Uses:
For preparation of bowel before surgery and colonoscopy
In food/drug poisoning
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Lactulose
Semisynthetic disaccharide of fructose and galactosenot digested or absorbed in small intestineretains water
In colonbacteria convert it into two component sugarfermentationlactic acid and acetic acidfunction as osmotic laxative
After lactulose administration, gut contents have low pH than normaldecrease activity of ammonia producing organismhence used in treatment of hepatic encephalopathy
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Fecal softeners
Promote more water and fat in the stools
Lubricate the fecal material and intestinal walls Emulsifying effect on fecesmake them retain more water
softer stooleasier to pass out
Abd cramps can occur
Uses: condition where straining at stool has to be avoided like hernia, piles, fissures, anal surgery
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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
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Bisacodyl: given orally and also as suppositorydefecation in 15-30min
Phenolphthalein: given orally
A/E:allergic rashes in skin
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Laxatives: Side Effects
Bulk forming Impaction Fluid overload
Emollient (stool softener) Skin rashes Decreased absorption of vitamins
Hyperosmotic Abdominal bloating Rectal irritation
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Saline
Magnesium toxicity (with renal insufficiency) Cramping Diarrhea Increased thirst
Stimulant
Nutrient malabsorption Skin rashes Gastric irritation Rectal irritation
All laxatives causes electrolyte imbalance
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Laxatives: Nursing Implications
Assess fluid and electrolytes before initiating therapy
Patients should not take a laxative if they are experiencing nausea, vomiting.
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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
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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
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The End…..