GI Drugs Flashcards
Proton pump inhibitors
H2-receptor blockers
Sucralfate
Antacids
Drugs used in acid-peptic diseases
Drugs used in acid-peptic diseases
Proton pump inhibitors
H2-receptor blockers
Sucralfate
Antacids
Proton pump inhibitors
Omeprazole
Lansoprazol
Etc
Omeprazole
Proton pump inhibitor
Lansoprazol
Proton pump inhibitor
Proton pump inhibitors
Mechanism of action
Irreversible blockade of H+/K+ATPase pump in active parietal cells of stomach
Irreversible blockade of H+/K+ATPase pump in active parietal cells of stomach
Proton pump inhibitors
Mechanism of action
Proton pump inhibitors
Effects
Long-lasting reduction of stimulating and nocturnal acid secretion
Long-lasting reduction of stimulating and nocturnal acid secretion
Proton pump inhibitors
Effects
Proton pump inhibitors
Clinical applications
Peptic ulcer
Gastroesophageal reflux disease
Erosive gastritis
Peptic ulcer
Gastroesophageal reflux disease
Erosive gastritis
Proton pump inhibitors
Clinical applications
Proton pump inhibitors
Toxicities
Reduction of stomach acid may reduce absorbtion of some drugs and increase that of others
Reduction of stomach acid may reduce absorbtion of some drugs and increase that of others
Proton pump inhibitors
Toxicities
H2-receptors blockers
Cimetidine
Etc
H2-receptors blockers
Cimetidine
Etc
H2-receptors blockers
Effects
Effective reduction of nocturnal acid but less effective against stimulated secretion, very safe.
Effective reduction of nocturnal acid but less effective against stimulated secretion, very safe.
H2-receptors blockers
Effects
Sucralfate
Effects
Polymerizes at site of tissue damage (ulcer bed) and protectsagainst further damage; very insoluble with no systemic effects; must be given 4 times daily
Polymerizes at site of tissue damage (ulcer bed) and protectsagainst further damage; very insoluble with no systemic effects; must be given 4 times daily
Sucralfate
Effects
Antacids
Effects
Popular OTC medication for symtomatic relief of heartburn; not as usful as PPI and H2 blockers in peptic diseases
Popular OTC medication for symtomatic relief of heartburn; not as usful as PPI and H2 blockers in peptic diseases
Antacids
Effects
Drugs stimulating motility
Metoclopramid
Domperidone
Cholibomimetics: Neostigmine
Macrolides: Eryhromycin
Metoclopramid
Domperidone
Cholibomimetics: Neostigmine
Macrolides: Eryhromycin
Drugs stimulating motility
Drugs stimulating motility
Metoclopramid
Domperidone
Mechanism of action
D2-receptor blocker
Removes inhibition of acetylcholine neurons in enteric nervous system
D2-receptor blocker
Removes inhibition of acetylcholine neurons in enteric nervous system
Drugs stimulating motility
Metoclopramid
Domperidone
Mechanism of action
Drugs stimulating motility
Metoclopramid
Domperidone
Effects
Increases gastric emptying and intestinal mobility
Drugs stimulating motility
Metoclopramid
Domperidone
Effects
Increases gastric emptying and intestinal mobility
Drugs stimulating motility
Metoclopramid
Domperidone
Clinical applications
Gastric paresis (e.g, in diabetic) Antiemetic
Gastric paresis (e.g, in diabetic) Antiemetic
Drugs stimulating motility
Metoclopramid
Domperidone
Clinical applications
Drugs stimulating motility
Metoclopramid
Domperidone
Toxicities
Parkinsonian symtoms due to block of central nervous system (CNS) D2 receptors
Parkinsonian symtoms due to block of central nervous system (CNS) D2 receptors
Drugs stimulating motility
Metoclopramid
Domperidone
Toxicities
Laxatives
Magnesium hydroxide, other nonabsorbable salts Bulk-forming laxatives Stimulants laxatives Stool surfactans Chlorid channal activator Opioid receptor antagonists 5-HT4 agonists
Magnesium hydroxide, other nonabsorbable salts Bulk-forming laxatives Stimulants laxatives Stool surfactans Chlorid channal activator Opioid receptor antagonists 5-HT4 agonists
Laxatives
Magnesium hydroxide, other nonabsorbable salts and sugars
Mechanism of action
Osmotic agents increase water content of stool
Osmotic agents increase water content of stool
Magnesium hydroxide, other nonabsorbable salts and sugars
Mechanism of action
Magnesium hydroxide, other nonabsorbable salts and sugars
Effects
Usally cause evacuation within 4-6 h, sooner in large doses
Usally cause evacuation within 4-6 h, sooner in large doses
Magnesium hydroxide, other nonabsorbable salts and sugars
Effects
Magnesium hydroxide, other nonabsorbable salts and sugars
Clinical applications
Simple constipation
Bowel prep for endoscopy
(especially PGE solutions)
Simple constipation
Bowel prep for endoscopy
(especially PGE solutions)
Magnesium hydroxide, other nonabsorbable salts and sugars
Clinical applications
Magnesium hydroxide, other nonabsorbable salts and sugars
Toxicities
Magnesium may be absorbed and cause toxicity in renal imparment
Magnesium may be absorbed and cause toxicity in renal imparment
Magnesium hydroxide, other nonabsorbable salts and sugars
Toxicities
Bulk-forming laxatives
Methylcellulose
Psyllium
Etc
( increase volume of colon, stimulat evacuation)
Methylcellulose
Psyllium
Etc
( increase volume of colon, stimulat evacuation)
Bulk-forming laxatives
Stimulants (laxatives)
Senna
Cascara
(Stimulate activity; may cause cramping)
Senna
Cascara
(Stimulate activity; may cause cramping)
Stimulants (laxatives)
Stool surfactants
Docusate
Mineral oil
(Lubricate stool, ease passage)
Docusate
Mineral oil
(Lubricate stool, ease passage)
Stool surfactants
Chloride channal activators (laxatives)
Lubiprostone
Prostanoic acid derivate
(Stimulates chloride secration into intestine, increasing fluid content)
Lubiprostone
Prostanoic acid derivate
(Stimulates chloride secration into intestine, increasing fluid content)
Chloride channal activators (laxatives)
Opioid receptor antagonists (laxatives)
Alvimopan
Methylnaltrexone
(Blocks intestinal U-opioid receptors but do not enter CNS, so analgesia is maintained)
Alvimopan
Methylnaltrexone
(Blocks intestinal U-opioid receptors but do not enter CNS, so analgesia is maintained)
Opioid receptor antagonists (laxatives)
5-HT4 agonists (laxatives)
Tegaserod
Activates enteric 5-HT4 receptors and increase intestinal mobility
Tegaserod
Activates enteric 5-HT4 receptors and increase intestinal mobility
5-HT4 agonists (laxatives)
Antidiarrheal drugs
Loperamide
Diphenoxylate
Colloidal bismuth compounds
Kaolin+pectin
Loperamide
Diphenoxylate
Colloidal bismuth compounds
Kaolin+pectin
Antidiarrheal drugs
Loperamide
Mechanism of action
Activates U-opioid receptors in enteric nervous system
Activates U-opioid receptors in enteric nervous system
Loperamide
Mechanism of action
Loperamide
Effects
Slows mobility in gut with negliable CNS effects
Slows mobility in gut with negliable CNS effects
Loperamide
Effects
Loperamide
Clinical applications
Nonspecific, noninfectious diarrhea
Nonspecific, noninfectious diarrhea
Loperamide
Clinical applications
Loperamide
Toxicities
Mild cramping but little or no CNS toxicity
Mild cramping but little or no CNS toxicity
Loperamide
Toxicities
Diphenoxylate
Effects
Similar to loperamid, but high doses can cause CNS opioid effects and toxicity
Similar to loperamid, but high doses can cause CNS opioid effects and toxicity
Diphenoxylate
Effects
Colloidal bismuth compounds
Subsalicylate and citrate salts available
OTC preparations popular and have some value in travelers’ diarrhea due to adsorption of toxins
Subsalicylate and citrate salts available
OTC preparations popular and have some value in travelers’ diarrhea due to adsorption of toxins
Colloidal bismuth compounds
Kaolin+pectin
Adsorbent compounds available OTC in some contries
Adsorbent compounds available OTC in some contries
Kaolin+pectin
Drugs for irritable bowel syndrome (IBS)
Alosetron (5-HT3 antagonist)
Anticholinergics
Chloride channal activators
Alosetron (5-HT3 antagonist)
Anticholinergics
Chloride channal activators
Drugs for irritable bowel syndrome (IBS)
Alosetron
Mechanism of action
5-HT3 antagonist of high potency and duration of binding
5-HT3 antagonist of high potency and duration of binding
Alosetron
Mechanism of action
Alosetron
Effects
Reduces smooth muscle activity in gut
Reduces smooth muscle activity in gut
Alosetron
Effects
Alosetron
Clinical applications
Approved for severe diarrhea-predominant IBS in women
Approved for severe diarrhea-predominant IBS in women
Alosetron
Clinical applications
Alosetron
Toxicities
Rare but serious constipation
Ischemic colitis
Infarction
Rare but serious constipation
Ischemic colitis
Infarction
Alosetron
Toxicities
Antiemetic drugs
Ondasetron, other 5-HT3 antagonists Aprepitant Corticosteroids Antimuscarinic Antihistaminics Phenothizines Cannabinoids
Ondasetron, other 5-HT3 antagonists Aprepitant Corticosteroids Antimuscarinic Antihistaminics Phenothizines Cannabinoids
Antiemetic drugs
Ondasetron, other 5-HT3 antagonists
Mechanism of action
5-HT3 blockade in gut and CNS with shorter duration of binding than alosetron
5-HT3 blockade in gut and CNS with shorter duration of binding than alosetron
Ondasetron, other 5-HT3 antagonists
Mechanism of action
Ondasetron, other 5-HT3 antagonists
Effects
Extremely effective in preventing chemotheraphy induced and postoperative nausea and vomiting
Extremely effective in preventing chemotheraphy induced and postoperative nausea and vomiting
Ondasetron, other 5-HT3 antagonists
Effects
Ondasetron, other 5-HT3 antagonists
Clinical applications
First-line agents in cancer chemotherapy; also useful for postop emesis
First-line agents in cancer chemotherapy; also useful for postop emesis
Ondasetron, other 5-HT3 antagonists
Clinical applications
Aprepitant
Mechanism of action
NK1-receptor blocker in CNS
NK1-receptor blocker in CNS
Aprepitant
Mechanism of action
Aprepitant
Effects
Interferes with vomiting reflex
No effect on 5-HT, dopamin or steroid receptors
Interferes with vomiting reflex
No effect on 5-HT, dopamin or steroid receptors
Aprepitant
Effects
Aprepitant
Clinical applications
Effective in reducing both early and delayed emesis in cancer chemotherapy
Effective in reducing both early and delayed emesis in cancer chemotherapy
Aprepitant
Clinical applications
Aprepitant
Toxicities
Fatigue
Dizziness
Diarrhea
CYP interactions
Fatigue
Dizziness
Diarrhea
CYP interactions
Aprepitant
Toxicities
Antimuscarinic (scopolamine)
Effective in emesis due to motion sickness; not other types
Effective in emesis due to motion sickness; not other types
Antimuscarinic (scopolamine)
Antihistaminics ( antiemetic )
Moderate efficacy in motion sickness and chemotherapy-induced emesis
Moderate efficacy in motion sickness and chemotherapy-induced emesis
Antihistaminics ( antiemetic )
Phenothiazines ( antiemetic )
Act primary through block of D2 and muscarinic receptors
Act primary through block of D2 and muscarinic receptors
Phenothiazines ( antiemetic )
Cannabinoids
Dronabinol is available for use in chemotherapy- induced nausea and vomiting, but associated with CNS marijuana effects
Dronabinol is available for use in chemotherapy- induced nausea and vomiting, but associated with CNS marijuana effects
Cannabinoids
Drugs used in inflammatory bowel disease (IBD)
5-Aminosalicylates, eg mesalamine
Sulfasalazine
Purine analogs, eg, 6-mercaptopurine, methtrexate
Anti-TNF antibodies, eg infliximab, others
Corticosteroids
5-Aminosalicylates, eg mesalamine
Sulfasalazine
Purine analogs, eg, 6-mercaptopurine, methtrexate
Anti-TNF antibodies, eg infliximab, others
Corticosteroids
Drugs used in inflammatory bowel disease (IBD)
5-Aminosalicylates
Mesalamine
Mesalamine
5-Aminosalicylates
Mesalamine
Mechanism of action
Mechanism uncertain
May be inhibition of eicosanoid inflammatory mediators
Mechanism uncertain
May be inhibition of eicosanoid inflammatory mediators
Mesalamine
Mechanism of action
Mesalamine
Clinical applications
Mild to moderately severe Crohn’s disease and ulcerative colitis
Mild to moderately severe Crohn’s disease and ulcerative colitis
Mesalamine
Clinical applications
Anti-TNF antibodies
Infliximab
Others
Infliximab
Others
Anti-TNF antibodies
Infliximab
Mechanism of action
Bind tumor necrosis factor and prevents it from binding to its receptors
Bind tumor necrosis factor and prevents it from binding to its receptors
Infliximab
Mechanism of action
Infliximab
Effects
Suppression of several aspects of immune function, especially TH1 lymphocytes
Suppression of several aspects of immune function, especially TH1 lymphocytes
Infliximab
Effects
Infliximab
Clinical applications
Moderately severe to severe Crohn’s disease and ulcerative colitis
Moderately severe to severe Crohn’s disease and ulcerative colitis
Infliximab
Clinical applications
Pancreatic supplements
Pancrelipase
Pancreatin
Pancrelipase
Pancreatic supplements
Pancrelipase
Mechanism of actions
Replacement enzymes from animal pancreatic extracts
Replacement enzymes from animal pancreatic extracts
Pancrelipase
Mechanism of actions
Pancrelipase
Effects
Improves digestion of dietary fat, protein, and carbohydrate
Pancrelipase
Effects
Improves digestion of dietary fat, protein, and carbohydrate
Pancrelipase
Clinical applications
Pancreatic insufficiency due to cystic fibrosis, pancreatitis, pancreatectomy
Pancreatic insufficiency due to cystic fibrosis, pancreatitis, pancreatectomy
Pancrelipase
Clinical applications
Bile acid therapy for gallstones
Ursodiol
Ursodiol
Bile acid therapy for gallstones
Ursodiol
Mechanism of action
Reduces cholesterol secretion into bile
Reduces cholesterol secretion into bile
Ursodiol
Mechanism of action
Ursodiol
Effects
Dissolves gallstones
Dissolves gallstones
Ursodiol
Effects
Ursodiol
Clinical applications
Gallstones in patients refusing or not eligible for surgery
Gallstones in patients refusing or not eligible for surgery
Ursodiol
Clinical applications
Orlistat
Non-amphetamine drug for treatment of obesity
Non-amphetamine drug for treatment of obesity
Orlistat