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Pharmacology of drugs affecting GIT
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Peptic Ulcer Disease Imbalance between mucosal defensive factors and aggressive factors Major defensive – mucus and bicarbonate Major aggressive – gastric acid, H. pylori, nonsteroidal anti-inflammatory drugs, pepsin
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Defensive factors Prevent the stomach and duodenum from being harmed (self-digestion). Mucus – continually secreted, protective effect Bicarb – secreted from endothelial cells, neutralized hydrogen ions Blood flow – good blood flow helps to maintain mucosal integrity Prostaglandins – stimulate secretion of bicarb and mucus and help promote blood flow, suppress secretion of gastric acid
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Aggressive factors Helicobacter pylori – gram negative bacteria, can live in stomach and duodenum May breakdown mucus layer, inflammatory response to presence of the bacteria may breakdown defenses, also produces urease – forms CO2 and ammonia which are toxic to mucosa
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Pepsin Smoking NSAIDS – inhibit the production of prostaglandins
Decrease blood flow, decrease mucus production and bicarb synthesis, promote gastric acid secretion Gastric Acid – also needs to be present for ulcer to form – activates pepsin and injures mucosa
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Nondrug therapy Diet – change in eating pattern, 5-6 small meals a day
Smoking cessation, NSAID and ASA should be avoided whenever possible, avoid alcohol
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Antibacterial drugs Combinations must be used
Bismuth – disrupts cell wall of H. pylori, pepto-bismol Clarithromycin – inhibits protein synthesis Amoxicillin – disrupts cell wall, good when given with omeprazole Tetracyclin – inhibits protein synthesis Metronidazole – resistance,
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Histamine 2-receptor antagonists
Suppress secretion of gastric acid (activation of H2 receptors promotes secretion of gastric acid) Cimetidine - first available, oral, IV, IM May take up to twelve weeks for ulcer to be healed Therapeutic uses – ulcers, GERD, Zollinger-ellison syndrome, aspiration pneumonitis, heartburn, indigestion
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Proton Pump Inhibitors
Suppress secretion of gastric acid Omeprazole – prilosec – prodrug that converts to active form in parietal cells of stomach – inhibits enzyme that generates gastric acid Ulcers, GERD, Zollinger-Ellison syndrome May contribute to development of gastric tumors?
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Sucralfate Creates a protective barrier against acid and pepsin
Form sticky gel that coats ulcer portion Given every 6 hours Very few side effects – minimal systemic absorption
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misoprostol Cytotec – prevention of gastric ulcers caused by long-term NSAID therapy Replacement for endogenous prostaglandins
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Antacids Peptic ulcers and GERD Neutralize acid
Dosing – 7 times per day
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Almagel Combined drug which contains gel of aluminum hydroxide, magnesium oxide and D-sorbit 170 ml bottles
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Schemes of combined treatment of gastric ulcer
De-nol + amoxycillin De-nol + metronidazole Omeprazole + amoxycillin + clarythromycin De-nol + clarythromycin + metronidazole De-nol + controlok + amoxycilin + clarythromycin
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Laxatives Laxative effect – production of a soft formed stool over a period of 1 or more days Catharsis – prompt, fluid evacuation of the bowel, more intense Function of the colon – water and electrolyte absorption Bowel evacuation – individual Dietary fiber
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Indications for laxative use
Pain associated with bowel movements To decrease amount of strain under certain conditions Evacuate bowel prior to procedures or examinations Remove poisons To relieve constipation caused by pregnancy or drugs
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Just because laxatives are available without a prescription doesn't mean that they're without risk. Warning: Use of stimulant laxatives over a long period may lead to dependence and might permanently damage intestine and colon
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Classifications I – osmotic (high doses)
II – osmotic (low doses), stimulant except castor oil – most frequently abused III – bulk-forming, surfactant
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Bulk-forming Identical to fiber – soften fecal mass, increasing bulk
Temporary treatment of constipation, preferred for patients with inflammatory bowel diseases May help with diarrhea
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Adverse reactions Not absorbed – no systemic effects
Must take with sufficient water Intestinal, esophageal obstruction Metamucil, citrucel
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Surfactant laxatives Bisacodyl, castor oil
Stimulate intestinal motility Increase water and electrolytes in intestinal lumen Produce stool within 6-12 hours
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Bisakodil
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Guttalax
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Miscellaneous laxatives
Mineral oil Lactulose Glycerin suppository Polyethylene glycol-electrolyte solutions
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Laxative abuse Most common cause of constipation Teaching
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Choleretics of plant origin
Stigma of corn Common immortelle Dog-rose Choleretics of plant origin
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Tocopherole acetate (Tocopheroli acetas)
Vitamin E is produced in many forms: 5 %, 10 % and 30 % oil solution in 10, 20 and 50 ml bottles; elastic capsules with 0,1 and 0,2 ml of 50 % solution in oil; ampoules with 1 ml of 5 %, 10 % and 30 % oil solutions.
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Carsil Legalon
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Mechanism of action of legalon
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Is produced in 5 ml ampoules and in capsules
Essentiale Is produced in 5 ml ampoules and in capsules
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Lipostabil
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Pancreatin (Panсreatinum)
Is produced in 0,25 g and 0,5 g dragee (tablets).
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Panzynorm forte
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Festal, Enzistal, Mezym-forte
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No-spa, nicospan
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Baralgin
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Bil-berries St. John’s wort
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Pepper mint Chamomile
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