13-gidrugs-120605125040-phpapp01 (1)
description
Transcript of 13-gidrugs-120605125040-phpapp01 (1)
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PharmacologyPharmacologyPharmacologyPharmacology
Drugs that Affect the
Gastrointestinal System
Drugs that Affect the
Gastrointestinal System
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TopicsTopicsTopicsTopics
• Peptic Ulcer Disease
• Constipation
• Diarrhea
• Emesis
• Digestion
• Peptic Ulcer Disease
• Constipation
• Diarrhea
• Emesis
• Digestion
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Peptic Ulcer DiseasePeptic Ulcer DiseasePeptic Ulcer DiseasePeptic Ulcer Disease
Factors thatIncrease Acidity
Factors thatIncrease Acidity
Factors thatProtect Against
Acidity
Factors thatProtect Against
Acidity
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Peptic Ulcer DiseasePeptic Ulcer DiseasePeptic Ulcer DiseasePeptic Ulcer Disease
• Factors Increasing– H. pylori
– NSAIDs
– Acidic agents
– Pepsin
– Smoking
• Factors Increasing– H. pylori
– NSAIDs
– Acidic agents
– Pepsin
– Smoking
• Factors Decreasing– Mucus production
– Buffers
– Blood flow
– Prostaglandins
• Factors Decreasing– Mucus production
– Buffers
– Blood flow
– Prostaglandins
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Regulation of Gastric Acid Regulation of Gastric Acid SecretionSecretionRegulation of Gastric Acid Regulation of Gastric Acid SecretionSecretion
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HH22 Receptor Antagonists Receptor AntagonistsHH22 Receptor Antagonists Receptor Antagonists
• Inhibits gastric acid secretion
• No effect on H1 receptors
• cimetidine (Tagamet®)
• ranitidine (Zantac®)
• famotidine (Pepcid®)
• nizatidine (Axid®)
• Inhibits gastric acid secretion
• No effect on H1 receptors
• cimetidine (Tagamet®)
• ranitidine (Zantac®)
• famotidine (Pepcid®)
• nizatidine (Axid®)
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HH22 Receptor Antagonists Receptor AntagonistsHH22 Receptor Antagonists Receptor Antagonists
• Indications:– PUD– GERD– Prevention of aspiration pneumonia
• Indications:– PUD– GERD– Prevention of aspiration pneumonia
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Proton Pump InhibitorsProton Pump InhibitorsProton Pump InhibitorsProton Pump Inhibitors
• K+H+ATPase (Proton Pump)
• Irreversible inhibition– Must synthesize new enzyme– Long duration
• omeprazole (Prilosec®)
• lansoprazole (Prevacid®)
• K+H+ATPase (Proton Pump)
• Irreversible inhibition– Must synthesize new enzyme– Long duration
• omeprazole (Prilosec®)
• lansoprazole (Prevacid®)
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AnticholinergicsAnticholinergicsAnticholinergicsAnticholinergics
• pirenzepine (Gastrozepine®)
• Other anticholinergics have too many side effects and are not used
• pirenzepine (Gastrozepine®)
• Other anticholinergics have too many side effects and are not used
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Prostaglandin AnalogProstaglandin AnalogProstaglandin AnalogProstaglandin Analog
• misoprostol (Cytotec®)– Approved for treating PUD due to long term
NSAID use
• misoprostol (Cytotec®)– Approved for treating PUD due to long term
NSAID use
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AntacidsAntacidsAntacidsAntacids
• Increase pH of gastric environment
• Hydroxides– Aluminum – Magnesium
• Carbonates– Calcium
• Increase pH of gastric environment
• Hydroxides– Aluminum – Magnesium
• Carbonates– Calcium
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AntacidsAntacidsAntacidsAntacids
• Most OTC drugs are combinations– DiGel®
– Amphojel®
– Maalox®
– Milk of Magnesia®
– Mylanta®
• Most OTC drugs are combinations– DiGel®
– Amphojel®
– Maalox®
– Milk of Magnesia®
– Mylanta®
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AntibioticsAntibioticsAntibioticsAntibiotics
• Aimed at eliminating H. pylori
• bismuth (Pepto-Bismol®)
• metronidazole (Flagyl®)
• amoxicillin (Amoxil®)
• tetracycline (Achromycin V®)
• Aimed at eliminating H. pylori
• bismuth (Pepto-Bismol®)
• metronidazole (Flagyl®)
• amoxicillin (Amoxil®)
• tetracycline (Achromycin V®)
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Stool FormationStool FormationStool FormationStool Formation
Water absorbed in colon (~90%)– Excessive absorption
• Constipation: hard, dehydrated stool
• Increases strain on defecation
• Harmful for subset of patients– Recent episiotomy, colostomy, hemorrhoids,
cardiovascular disease
– Inadequate absorption• Diarrhea: soft, non-formed, liquid stool
Water absorbed in colon (~90%)– Excessive absorption
• Constipation: hard, dehydrated stool
• Increases strain on defecation
• Harmful for subset of patients– Recent episiotomy, colostomy, hemorrhoids,
cardiovascular disease
– Inadequate absorption• Diarrhea: soft, non-formed, liquid stool
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TermsTermsTermsTerms
LaxativeLaxative Production of soft, formed stool over 1 or more days
Production of soft, formed stool over 1 or more days
CatharticCathartic Rapid, intense fluid evacuation of bowel.
Rapid, intense fluid evacuation of bowel.
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LaxativesLaxativesLaxativesLaxatives
• Bulk forming
• Surfactants
• Stimulants
• Osmotics
• Bulk forming
• Surfactants
• Stimulants
• Osmotics
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Bulk Forming LaxativesBulk Forming LaxativesBulk Forming LaxativesBulk Forming Laxatives
• Absorb water• Soften and enlarge
stool• Fecal swelling
promotes peristalsis
• Absorb water• Soften and enlarge
stool• Fecal swelling
promotes peristalsis
• methylcellulose (Citrucel®)
• psyllium (Metamucil®)• Polycarbophil
• methylcellulose (Citrucel®)
• psyllium (Metamucil®)• Polycarbophil
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Surfanctant LaxativesSurfanctant LaxativesSurfanctant LaxativesSurfanctant Laxatives
• Lowers surface tension– Facilitates water
penetration
• Lowers surface tension– Facilitates water
penetration
• Docusate salts– Colace®
– Modane Soft®)
• Docusate salts– Colace®
– Modane Soft®)
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Stimulant LaxativesStimulant LaxativesStimulant LaxativesStimulant Laxatives
• Stimulate peristalsis• Increases water and
electrolytes secretion into intestinal lumen
• Decreases water and electrolyte reabsorption
• Stimulate peristalsis• Increases water and
electrolytes secretion into intestinal lumen
• Decreases water and electrolyte reabsorption
• Phenylolpthalein – (Ex-Lax®, Feen-a-
Mint®, Correctol®)
• bisacodyl (Ducolax®)
• Phenylolpthalein – (Ex-Lax®, Feen-a-
Mint®, Correctol®)
• bisacodyl (Ducolax®)
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Osmotic LaxativesOsmotic LaxativesOsmotic LaxativesOsmotic Laxatives
• Poorly absorbed salts remain in fecal matter
• Pull water into lumen
• Poorly absorbed salts remain in fecal matter
• Pull water into lumen
• Magnesium hydroxid (Milk of Magnesia®)
• Magnesium hydroxid (Milk of Magnesia®)
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AntidiarrhealAntidiarrhealAntidiarrhealAntidiarrheal
• Diarrhea is usually a compensatory action…– Treatment aimed at cause, no symptom
• Opioid receptors in GI tract decrease motility– Increase time for water reabsorbtion
• Diarrhea is usually a compensatory action…– Treatment aimed at cause, no symptom
• Opioid receptors in GI tract decrease motility– Increase time for water reabsorbtion
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Antidiarrheal AgentsAntidiarrheal AgentsAntidiarrheal AgentsAntidiarrheal Agents
• paregoric/opium tincture
• diphenoxylate (Lomotil®)
• defenoxin (Motofen®)
• loperamide (Imodium®)
• paregoric/opium tincture
• diphenoxylate (Lomotil®)
• defenoxin (Motofen®)
• loperamide (Imodium®)
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Vomiting StimulusVomiting StimulusVomiting StimulusVomiting Stimulus
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AntiemeticsAntiemeticsAntiemeticsAntiemetics
• Serotonin (5HT) Antagonists
• Dopamine (DA) Antagonists
• Anticholinergics (muscarinic blockers)
• Cannabinoids
• Serotonin (5HT) Antagonists
• Dopamine (DA) Antagonists
• Anticholinergics (muscarinic blockers)
• Cannabinoids
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Serotonin AntagonistsSerotonin AntagonistsSerotonin AntagonistsSerotonin Antagonists
• Used to treat side effects of chemotherapy-induced emesis
• condansetron (Zofran®)
• Doesn’t affect dopamine receptors no extrapyramidal effects
• Granisetron (Kytril®)
• Used to treat side effects of chemotherapy-induced emesis
• condansetron (Zofran®)
• Doesn’t affect dopamine receptors no extrapyramidal effects
• Granisetron (Kytril®)
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Dopamine AntagonistsDopamine AntagonistsDopamine AntagonistsDopamine Antagonists
• Phenothiazines– prochloraperazine (Compazine®)– promethazine (Phenergan®)
• Butyrophenones– haloperidol (Haldol®)– droperidol (Inapsine®)
• metoclopramide (Reglan®)
• Phenothiazines– prochloraperazine (Compazine®)– promethazine (Phenergan®)
• Butyrophenones– haloperidol (Haldol®)– droperidol (Inapsine®)
• metoclopramide (Reglan®)
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CannabinoidsCannabinoidsCannabinoidsCannabinoids
• Tetrahydrocannabinol (THC)– Active ingredient in marijuana– Dronabinol (Marinol®)– Nabilone (Cesamet®)
• Tetrahydrocannabinol (THC)– Active ingredient in marijuana– Dronabinol (Marinol®)– Nabilone (Cesamet®)
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Digestion AidsDigestion AidsDigestion AidsDigestion Aids
• Useful for inactive vagal stimulus/bypassed duodenum
• Pancreatin (Entozyme®)
• Pancrelipase (Viokase®)
• Useful for inactive vagal stimulus/bypassed duodenum
• Pancreatin (Entozyme®)
• Pancrelipase (Viokase®)