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ANTI - DIARRHEALS
BY- Sakshi Phaugat
Department - Mpharm (pharmacology) Ist year
Roll no. -2101700986008
DIARRHOEA
• Diarrhoea is too frequent, often too precipitate passage of poorly formed
stools.
• Diarrhoea is having 3 or more loose or liquid stools in one day, or more
frequently than normal.
• Diarrhoea episodes are often caused by a stomach bug ( gastroenteritis)and
clear up on their own in a few days.
DIARRHOEA(CONT’D)
• Acute Diarrhoea :
• Sudden onset in a previously healthy person
• Lasts from 3 days to 2 weeks
• Self-limiting
• Chronic diarrhoea:
• Lasts for more than 2 weeks
• Associated with the recurring passage of diarrheal stools ,fever , loss of appetite,
nausea, vomiting, weight loss, and chronic weakness.
SYMPTOMS
As well as the loose and watery stools of
diarrhoea, the other symptoms are also
occurs:
• Nausea
• vomiting
• Fever
• Headache
• Bloating and flatulence
• Abdominal cramps, with a colicky
pattern
• Stomach pains
• Loss of appetite
• Weakness
• dehydration
Causes of diarrhoea
• Acute diarrhoea
• Bacterial
• Viral
• Drug induced
• Nutritional
• protozoal
• Chronic diarrhoea
• Tumours
• Diabetes
• Addison’s disease
• Hyperthyroidism
• Irritable bowel
PATHOPHYSIOLOGY
• Four general pathophysiologic mechanisms disrupt water and electrolyte
balance, leading to diarrhea, and are the basis of diagnosis and therapy.
These are ( a) a change in active ion transport by either decreased sodium
absorption or increased chloride secretion ;
• (b) change in intestinal motility ; ( c ) increase in luminal osmolarity ;
• And (d ) increase in tissue hydrostatic pressure.
PHARMACOLOGY
• Pharmacology of diarrhea mainly contain :-
1. Rehydration therapy
2. Nutrition therapy
3. Drug therapy
ORAL REHYDRATION SALTS (WHO-
ORS)
• Rehydration with ORS is usually sufficient for management of moderate
dehydration from acute diarrhea, regardless of etiology, which can be safely
and effectively treated in over 90% of cases by the use of ORS. ORS is
absorbed in the small intestine even during diarrhea, thus replacing the water
and electrolytes lost in the feces
• A particular advantage of this is that ORS may be used as home treatment to
prevent dehydration.
NUTRITION THERAPY
• Patients with diarrhea should not be starved.
• Simple food like breast milk, boiled potato, rice, chicken soup, banana, etc.
should be given to the patient.
• When a patient has diarrhea then some of the main nutrients are lost:
sodium, potassium, water, proteins, vitamins, and calories.
• BLAND foods are given to the diarrhea patients.
Drug therapy
1. Specific antimicrobial
2. Probiotics
3. Drugs for IBD
4. Nonspecific antidiarrhoel
Antimicrobials – no value
• Irritable bowel syndrome
• Coeliac disease
• Pancreatic enzyme deficiency
• Topical sprue
• Thyrotoxicosis
• Rotavirus
• salmonella
Antimicrobials – useful (severe cases)
• Travellers diarrhoea – cotrimoxazole , norfloxacin, doxycycline, and
rifamixin.
• EPEC- cotrimazole, fluroquinolones
• Shigella enteritis – ciprofloxacin or norfloxacin , cotrimazole and ampicillin.
• Nontyphoid salmonella – FQs , cotrimoxazole or ampicillin
• Yersinia - cotrimoxazole
Antimicrobials – always useful
• Cholera – tetracycline , cotrimazole , FQs , ampicillin and erythromycin.
• Campylobacter jejuni- norfloxacin or erythromycin
• Clostridium difficile- metronidazole , vancomycin
• Amoebiasis and giardiasis – metronidazole , diloxanide furoate
Probiotics
• Live culture or lyophilized powders to restore and maintain gut flora.
• Recolonization of the gut by non- pathogenic , mostly lactic acid forming
bacteria.
• Probiotics significantly reduce antibiotic – associated diaarhoea , acute
infective diarrhoea and risk of travellers diarrhoea.
• Curd is an abundant source of lactic acid producing organisms.
Inflammatory bowel disease
• IBD is a chronic relapsing inflammatory disease of the ileum, colon, or both.
• crohn’s disease – lesions are patchy and transmural; may involve any part of
the g.i.t from mouth to the anus.
• Ulcerative colitis- it involves only the colon starting from the anal canal.
Drugs in IBD
• 5- aminosalicyclic acid compounds
• Corticosteroids
• Immunosuppressant
• TNF ά inhibitors
sulfasalazine
• 5ASA+sulfapyridine
• 5ASA inhibits COX, LOX decrease Pg and LT , cytokine,PAF, TNFά and
nuclear transcription factor
• Reduces frequency of stool , abdominal cramps and fever
• Used to maintain remission
• Sulfapyridine is responsible for rashes , fever , joint pain, haemolysis and
blood dyscrasias.
Mesalazine
• 5ASA delayed release preparation, release in jejunum, ileum, and colon.
• More useful in UC for remission.
• A/E- nausea, diarrhoea , abdominal pain and headache
• 5ASA - enema
Corticosteroids
• Prednisolone – induce remission in UC and CrD
• DOC for exacerbation
• Hydrocortisone enema for pro
• Used for short term and stopped after remission
Immunosuppressant
• Long term management , not suitable for acute exacerbation
• Azathioprine – steroid dependent, resistant and severe cases
• Methotrexate
• cyclosporine
TNFά inhibitors
• Severe active CrD ,fistulating CrD and severe UC not responding to steroids
or immunosuppressant
• Infliximab
• Adalimumab
• A/E- acute reactions, immune reactions and lowering of resistance to
infection
Non specific drugs
• Absorbents and adsorbents
• Antisecretory
• antimotility
Absorbants and adsorbants
• Bulk forming isaphghula , methylcellulose , carboxymethyl cellulose
• Diarrhoea phase of IBD
• Modify consistency and frequency,
• No effect on loss of water and electrolyte
Anti secretory- racecadotril
• Prodrug of thiorphan
• Prevent degradation of enkephalins of δ opoid receptor
• Decreases hypersecretion without affecting motility
• Short term treatment of secretory diarrhoea
• Safely given in children
Anti motility drugs
• μ receptors enhance absorption and decrease propulsive movements
• δ receptors promote absorption and inhibit secretion
• Increase resistance to luminal transit and allow more time for the absorptive
processes
• Only symptomatic relief in diarrhoea
Diphenoxylate
• Synthetic opoid
• Absorbed systemically and crosses BBB
• Atropine added in sub pharmaceutical doses to discourage abuse
• A/E – respiratory depression , paralytic ileus and toxic megacolon
• Contraindicated in <6 years
Loperamide
• Opiate analogue with μ agonistic and some weak anticholinergic effect
• Less absorbed from intestine – less BBB crossing
• Longer duration action than codeine and diphenoxylate
• Decrease motility and inhibit secretion
• A/E – abdominal cramps , rashes , paralytic ileus, toxic megacolon
• CI < 4 years
Antimotility drugs
• Useful in non infective , mild travellers diarrhoea and when diarrhoea is
exhausting in AIDS
• CI in infective diarrhoea , severe IBD
• Induce delibrate short term constipation – after anal surgery
New drugs
• The US FDA approved AEMCOLO ( RIFAMYCIN) an antibacterial drug
indicated for the treatment of adult patients with travellers diarrhea caused
by noninvasive strains of E.coli .
References
• Joseph T. dipiro ‘’ pharmacotherapy’’ , a pathophysiological approach ,6
edition.
• Essentials of medical pharmacology ,K.D Tripathi
• World Health Organization , http www.WHO.int accessed on 18 June
2022

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ANTI - DIARRHEALS.pptx

  • 1. ANTI - DIARRHEALS BY- Sakshi Phaugat Department - Mpharm (pharmacology) Ist year Roll no. -2101700986008
  • 2. DIARRHOEA • Diarrhoea is too frequent, often too precipitate passage of poorly formed stools. • Diarrhoea is having 3 or more loose or liquid stools in one day, or more frequently than normal. • Diarrhoea episodes are often caused by a stomach bug ( gastroenteritis)and clear up on their own in a few days.
  • 3. DIARRHOEA(CONT’D) • Acute Diarrhoea : • Sudden onset in a previously healthy person • Lasts from 3 days to 2 weeks • Self-limiting • Chronic diarrhoea: • Lasts for more than 2 weeks • Associated with the recurring passage of diarrheal stools ,fever , loss of appetite, nausea, vomiting, weight loss, and chronic weakness.
  • 4. SYMPTOMS As well as the loose and watery stools of diarrhoea, the other symptoms are also occurs: • Nausea • vomiting • Fever • Headache • Bloating and flatulence • Abdominal cramps, with a colicky pattern • Stomach pains • Loss of appetite • Weakness • dehydration
  • 5. Causes of diarrhoea • Acute diarrhoea • Bacterial • Viral • Drug induced • Nutritional • protozoal • Chronic diarrhoea • Tumours • Diabetes • Addison’s disease • Hyperthyroidism • Irritable bowel
  • 6. PATHOPHYSIOLOGY • Four general pathophysiologic mechanisms disrupt water and electrolyte balance, leading to diarrhea, and are the basis of diagnosis and therapy. These are ( a) a change in active ion transport by either decreased sodium absorption or increased chloride secretion ; • (b) change in intestinal motility ; ( c ) increase in luminal osmolarity ; • And (d ) increase in tissue hydrostatic pressure.
  • 7.
  • 8. PHARMACOLOGY • Pharmacology of diarrhea mainly contain :- 1. Rehydration therapy 2. Nutrition therapy 3. Drug therapy
  • 9. ORAL REHYDRATION SALTS (WHO- ORS) • Rehydration with ORS is usually sufficient for management of moderate dehydration from acute diarrhea, regardless of etiology, which can be safely and effectively treated in over 90% of cases by the use of ORS. ORS is absorbed in the small intestine even during diarrhea, thus replacing the water and electrolytes lost in the feces • A particular advantage of this is that ORS may be used as home treatment to prevent dehydration.
  • 10. NUTRITION THERAPY • Patients with diarrhea should not be starved. • Simple food like breast milk, boiled potato, rice, chicken soup, banana, etc. should be given to the patient. • When a patient has diarrhea then some of the main nutrients are lost: sodium, potassium, water, proteins, vitamins, and calories. • BLAND foods are given to the diarrhea patients.
  • 11. Drug therapy 1. Specific antimicrobial 2. Probiotics 3. Drugs for IBD 4. Nonspecific antidiarrhoel
  • 12. Antimicrobials – no value • Irritable bowel syndrome • Coeliac disease • Pancreatic enzyme deficiency • Topical sprue • Thyrotoxicosis • Rotavirus • salmonella
  • 13. Antimicrobials – useful (severe cases) • Travellers diarrhoea – cotrimoxazole , norfloxacin, doxycycline, and rifamixin. • EPEC- cotrimazole, fluroquinolones • Shigella enteritis – ciprofloxacin or norfloxacin , cotrimazole and ampicillin. • Nontyphoid salmonella – FQs , cotrimoxazole or ampicillin • Yersinia - cotrimoxazole
  • 14. Antimicrobials – always useful • Cholera – tetracycline , cotrimazole , FQs , ampicillin and erythromycin. • Campylobacter jejuni- norfloxacin or erythromycin • Clostridium difficile- metronidazole , vancomycin • Amoebiasis and giardiasis – metronidazole , diloxanide furoate
  • 15. Probiotics • Live culture or lyophilized powders to restore and maintain gut flora. • Recolonization of the gut by non- pathogenic , mostly lactic acid forming bacteria. • Probiotics significantly reduce antibiotic – associated diaarhoea , acute infective diarrhoea and risk of travellers diarrhoea. • Curd is an abundant source of lactic acid producing organisms.
  • 16. Inflammatory bowel disease • IBD is a chronic relapsing inflammatory disease of the ileum, colon, or both. • crohn’s disease – lesions are patchy and transmural; may involve any part of the g.i.t from mouth to the anus. • Ulcerative colitis- it involves only the colon starting from the anal canal.
  • 17. Drugs in IBD • 5- aminosalicyclic acid compounds • Corticosteroids • Immunosuppressant • TNF ά inhibitors
  • 18. sulfasalazine • 5ASA+sulfapyridine • 5ASA inhibits COX, LOX decrease Pg and LT , cytokine,PAF, TNFά and nuclear transcription factor • Reduces frequency of stool , abdominal cramps and fever • Used to maintain remission • Sulfapyridine is responsible for rashes , fever , joint pain, haemolysis and blood dyscrasias.
  • 19. Mesalazine • 5ASA delayed release preparation, release in jejunum, ileum, and colon. • More useful in UC for remission. • A/E- nausea, diarrhoea , abdominal pain and headache • 5ASA - enema
  • 20. Corticosteroids • Prednisolone – induce remission in UC and CrD • DOC for exacerbation • Hydrocortisone enema for pro • Used for short term and stopped after remission
  • 21. Immunosuppressant • Long term management , not suitable for acute exacerbation • Azathioprine – steroid dependent, resistant and severe cases • Methotrexate • cyclosporine
  • 22. TNFά inhibitors • Severe active CrD ,fistulating CrD and severe UC not responding to steroids or immunosuppressant • Infliximab • Adalimumab • A/E- acute reactions, immune reactions and lowering of resistance to infection
  • 23. Non specific drugs • Absorbents and adsorbents • Antisecretory • antimotility
  • 24. Absorbants and adsorbants • Bulk forming isaphghula , methylcellulose , carboxymethyl cellulose • Diarrhoea phase of IBD • Modify consistency and frequency, • No effect on loss of water and electrolyte
  • 25. Anti secretory- racecadotril • Prodrug of thiorphan • Prevent degradation of enkephalins of δ opoid receptor • Decreases hypersecretion without affecting motility • Short term treatment of secretory diarrhoea • Safely given in children
  • 26. Anti motility drugs • μ receptors enhance absorption and decrease propulsive movements • δ receptors promote absorption and inhibit secretion • Increase resistance to luminal transit and allow more time for the absorptive processes • Only symptomatic relief in diarrhoea
  • 27. Diphenoxylate • Synthetic opoid • Absorbed systemically and crosses BBB • Atropine added in sub pharmaceutical doses to discourage abuse • A/E – respiratory depression , paralytic ileus and toxic megacolon • Contraindicated in <6 years
  • 28. Loperamide • Opiate analogue with μ agonistic and some weak anticholinergic effect • Less absorbed from intestine – less BBB crossing • Longer duration action than codeine and diphenoxylate • Decrease motility and inhibit secretion • A/E – abdominal cramps , rashes , paralytic ileus, toxic megacolon • CI < 4 years
  • 29. Antimotility drugs • Useful in non infective , mild travellers diarrhoea and when diarrhoea is exhausting in AIDS • CI in infective diarrhoea , severe IBD • Induce delibrate short term constipation – after anal surgery
  • 30. New drugs • The US FDA approved AEMCOLO ( RIFAMYCIN) an antibacterial drug indicated for the treatment of adult patients with travellers diarrhea caused by noninvasive strains of E.coli .
  • 31. References • Joseph T. dipiro ‘’ pharmacotherapy’’ , a pathophysiological approach ,6 edition. • Essentials of medical pharmacology ,K.D Tripathi • World Health Organization , http www.WHO.int accessed on 18 June 2022