Class anti diarrheals

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Class anti diarrheals

  1. 1. Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC. 1
  2. 2.  Diarrhoea is an abnormal increase in the frequency and liquidity of stools  Too rapid evacuation of too fluid stools Diarrhea usually causes  Osmotic –lactase deficiency  Secretory –cholera, E. coli  Deranged intestinal motility-thyrotoxicosis  Altered mucosal morphology- viral gastroenteritis  Allergic diarrhoea –food allergy  Drug induced diarrhoea
  3. 3. Antimotility antisecretory agents Opioid agonists-Loperamide, diphenoxylate, difenoxin, racecadotril Anticholinergics –hyoscyamine and dicycloamine α2-adrenergic receptor agonist-clonidine Somatostatin analogue-Octreotide Adsorbant drugs- kaolin, pectin, bismuth subsalicylate And lactose Probiotics-lactobacillus sporogens
  4. 4. Antimotility agents & anti-secretory agents: LOPERAMIDE Mechanism of action: All the commonly used opioids act principally via peripheral  receptors and are preferred over opioids that penetrate central nervous system • More potent than morphine as an anti- diarrheal agent • Increases small intestinal and mouth to cecum transit time inhibition of presynaptic cholinergic nerves in the submucosal and myentric plexus 1. Intestinal motility-- receptors 2. Intestinal secretion--  receptors 3. Intestinal absorption---  &  receptors
  5. 5. •Increases anal sphincter tone •Anti-secretory activity against cholera toxin and some forms of E. coli toxin •Half- life 11 hours •Dose: 4mg initially followed by 2mg after each subsequent stool, up to 16mg/day. •Not recommended in children <2 years.
  6. 6.  A dipeptide  Racecadotril blocks enzyme encephalinase and increases local concentration of enkephalins in intestinal mucosa which then stimulate mu- and delta-receptors. Leads to anti-diarrheal effect  This drug can be used orally from children under 5 years old (including babies), but Loperamide is contraindicated in children < 5 years old.
  7. 7.  Trivalent bismuth suspended in a mixture of magnesium aluminium silicate clay.  Astringent, protective, adsorbent effect  In stomach: Combines with HCl Bismuth oxychloride + Salicylic acid  It can bind to toxins produced by v. cholerae, E. coli liberation of salicylic acid-prostaglandin synthesis inhibition intestinal inflammation
  8. 8.  Purified carbohydrate obtained from citrus fruits, tasteless  Forms viscous colloidal solution, coats the intestinal surface
  9. 9.  Cholestyramine, colestipol, colesevelam  -they decrease the excess fecal bile acids S/E-bloating flatulence, constipation D/I- binding to other drugs and cause malabsorption
  10. 10. Difenoxin- Active metabolite of diphenoxylate Both combined with 25 mcg of atropine to prevent abuse. Excess dose: CNS effects, anticholinergic effects, constipation, toxic megacolon Other opioids: 1. Paregoric: 2mg morphine/5mL. 2. Deodorized tincture of opium.
  11. 11.  Hyoscyamine and dicyclomine  Decrease bowel motility results in increase in fluid absorption, back from intestinal tract and in abdominal cramps
  12. 12. Clonidine Facilitates absorption, inhibits secretion of fluids and electrolytes Increases intestinal transit time Used in diabetic diarrhoea and opiod withdrawal
  13. 13.  14- amino acid peptide released in GIT, pancreas, D cells and enteric nerves  Inhibits secretion of gastrin, cholecystokinin, glucagon, growth hormone, insulin, 5-HT  Slows GI motility and inhibits gallbladder contraction  It inhibits secretion of anterior pituitary hormones  Stimulates intestinal fluid and electrolyte absorption  Inhibits intestinal fluid secretion  Inhibits release of gastrointestinal peptides.
  14. 14.  Given for: secretory diarrheas due to tumors--- VIPomas, Carcinoid, AIDS related diarrhea  inhibition of hormonal secretion and slows tumor progression  Low dose sc in patients with patients with small bowel bacterial overgrowth or intestinal pseudo- obstruction secondary to scleroderma  Dose: 50-250mcg subcutaneously three times daily.
  15. 15. Fluid and electrolyte Replacement Oral rehydration therapy WHO O.R.S Sodium Chloride 2.6 grams Trisodium dihydrate citrate 2.5 grams Potassium Chloride 1.5 grams Glucose 20 grams to be dissolved in one litre of clean drinking water
  16. 16. Cereal –based oral rehydration solution- decrease volume loss, shorten the duration of illness, It inhibits the response of crypt cell chloride channel to cAMP Digestive process supplies large number of glucose at the intestinal brush borders for transfer of glucose sodium ions from lumen into the blood less luminal back drag such effect may be seen in direct glucose ingestion Moderate dehydration and acidosis- can be corrected in 3-6hrs by ORS
  17. 17.  Includes ulcerative colitis and crohns disease  Includes drug therapy, dietary and lifestyle factors Aminosalicylates -Sulphasalazine, Mesalamine and Olsalazine – 5-ASA-5 amino salicylic acid topical anti- inflammatory agent Mesalamine –with pH sensitive coating release 5- ASA into the terminal ileum and colon also prevent formation of pro-inflammatory cytokines
  18. 18. Corticosteroids –Prednisone- Treatment for acute/severe exacerbations Patients not responding to ASA Foam based formulations coat the mucosa Severe-oral prednisolone-remission in 2 weeks Budesonide as enteric coated tablets used in Crohn’s disease
  19. 19. Immunosuppressant- Cyclosporine and Methotrexate-severe ulcerative colitis unresponsive to steroids Anti-TNF α agents- Adalimumab, Certolizumab Infliximab a new humanized antibody that targets tumour necrosis factor alpha, for crohn’s disease cross links with soluble and membrane bound TNF α  inhibits T cell and macrophage function  Alosetron –potent and selective 5-HT1 receptor antagonist  Tricyclic antidepressants- Amitriptyline
  20. 20. Antibiotics- Metronidazole and Ciprofloxacin Anti-integrin monoclonal antibody- NATALIZUMAB-humanised monoclonal antibody against integrin 300 mg /4wks IV infusion
  21. 21. THANKYOU Download slides from Authorstream/presentations/raghuprasada Slideshare/presentations/raghuprasada

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