pharmacology of drugs affecting git
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Pharmacology of drugs affecting GIT. 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. Defensive factors. - PowerPoint PPT PresentationTRANSCRIPT
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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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PepsinSmoking
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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AlmagelCombined 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 cornStigma of corn
Common immortelleCommon immortelle
Dog-roseDog-rose
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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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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