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65 Cards in this Set

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Review Gastric Acid Secretion
Need to look at Amanda's LO's when she puts them up.
Review of Mucosal defense mechanism in the Stomach
Noxious (harmful) factors: HCL, pepsin, others
Defense factors: mucus, cells, bicarbonate, prostaglandins, other
Drugs used in Acid-Peptic Disease
1. Drugs that decrease gastric acidity: Antacids, H2 receptor blockers, Proton pump inhibitors
2. Drugs that increase mucosal defenses: Sucralfate, Misoprostil, Bismuth compounds
Antacids
Aluminum hydroxide, Aluminum hydroxide-magnesium hydroxide combo, Calcium carbonate.
Mechanism: decreases gastric acidity by reacting with HCL and increasing the gastric pH.
Drug interactions: decreases absorption of some drugs but chelating or binding to them.
Nonprescription use in intermittent heartburn, dyspepsia
Aluminum hydroxide
Antacid.
Adverse effects: Diarrhea (so give with magnesium), problems in renal insufficiency.
Use: heartburn, dyspepsia
Aluminum hydroxide - magnesium hydroxide combination
Antacid
Adverse Effects: Magnesium hydroxide causes diarrhea(its an osmotic laxative so give with Aluminum which causes constipation), problems in renal insufficiency.
Use: heartburn, dyspepsia
Calcium carbonate
Antacid
Adverse Effects: high doses with certain dairy products (Ca containing) can cause milk-alkali syndrome = hypercalcemia, metabolic alkalosis, renal insufficiency.
Uses: heartburn, dyspepsia
H2 Receptor Blockers
Cimetidine, Ranitidine (-itidine)
Mechanism: decreases gastric acidity by being competitive inhibition of H2 receptors on parietal cells causing decreased HCl secretion. Greater decrease of nocturnal/fasting secretion than stimulated secretion.
-Oral, IV. Eliminated by metabolism, renal secretion.
Uses: GERD, Peptic ulcer Disease, Prevent UGI bleeding in critically ill patients
Drug interactions: alter the pH of gastric contents which can alter absorption of some drugs.
Cimetidine
H2 receptor blocker.
Decrease HCl secretion
Adverse effects: GI effects, possible gynecomastia in males, galactorrhea in females (nipple discharge), increase prolactin release, altered mental status (confusion) especially in severely ill patients.
Uses: GERD, peptic ulcer dz, prevent UGI bleeding
Ranitidine
H2 receptor blocker.
Decrease HCl secretion
Adverse effects: GI effects, altered mental status (confusion) especially in severely ill patients.
Uses: GERD, peptic ulcer dz, prevent UGI bleeding
Proton Pump Inhibitors
Omeprazole, Esomeprazole, Lansoprazole (-prazole)
Mechanism: decreases gastric acidity via covalent binding and irreversible inhibition of H+/K+ ATPase -> decreased HCl secretion. Decreases acid secretion in both fasting and stimulated stages.
Oral, some IV
Adverse effects: Increased gastrin (bc decreased feeback inhibition). Drug interactions
Uses: GERD, peptic ulcer disease (including H. pylori ulcers w/ antibacterials), pathological hypersecretory condittions (Zollinger-Ellison Syndrome)
Omeprazole
Proton pump inhibitor
Adverse effects: Increased gastrin (bc decreased feeback inhibition).
Uses: GERD, peptic ulcer disease (including H. pylori ulcers w/ antibacterials), pathological hypersecretory condittions (Zollinger-Ellison Syndrome)
Esomeprazole
Proton pump inhibitor
Adverse effects: Increased gastrin (bc decreased feeback inhibition).
Uses: GERD, peptic ulcer disease (including H. pylori ulcers w/ antibacterials), pathological hypersecretory condittions (Zollinger-Ellison Syndrome)
Lansoprazole
Proton pump inhibitor
Adverse effects: Increased gastrin (bc decreased feeback inhibition).
Uses: GERD, peptic ulcer disease (including H. pylori ulcers w/ antibacterials), pathological hypersecretory condittions (Zollinger-Ellison Syndrome)
Sucralfate
Mechanism: Increases mucosal defenses via converted to thick paste that binds to ulcer and thought to form physical barrier
Adverse Effects: constipation (2%), some aluminum absorped (can cause toxicity in renal insufficiency), may decrease absorption of some drugs
Uses: limited use now, peptic ulcer disease
Misoprostil
Prostaglandin analog.
Decreases acid secretion; increases secretion of mucus and bicarbonate; increases mucosal blood flow.
Adverse Effects: Diarrhea, abdominal cramps, contraindicated in pregnancy (increases uterine contraction).
Uses: Decreases risk of NSAID-induced ulcers in high-risk patients.
Bismuth Compounds
Bismuth subsalicylate (peptobismol), bismuth subcitrate potassium.
Mechanism of action unknown.
Adverse Effects: Darkening of stool and tongue
Uses: Nonprescription- dyspepsia, diarrhea, traveler's diarrhea, component of some H. pylori regimens.
Drugs that Increase GI motility
Metoclopramide, Erythromycin
Metoclopramide
Increases GI motility.
Mechanism: Dopamine antagonist. Normally stimulation of D2 receptors in the GI tract inhibits GI motility. (blocks this so increased motility). Blockade of dopamine receptors also causes prokinetic effect (increases LES tone and gastric emptying), also causes antiemetic effect.
Oral, IV
Adverse Effects: restlessness, drowsiness, insomnia, anxiety, agitation, extrapyramidal effects (parkinson-like), tardive dyskinesia, increased prolactin.
Use: Diabetic gastroparesis
Erythromycin
Increases GI motility.
Mechanism: stimulates motilin receptors. Motilin increases contraction in upper GI tract.
Use: Diabetic gastroparesis
Laxatives
1.Bulk forming
2. Stool surfactant agents (softeners) -Docusate
3. Osmotic - magnesium hydroxide, lactulose, polyethylene glycol electrolyte solution
4. Stimulants - Senna, bisacodyl
5. Chloride channel activator - lubiprostone
6. Opioid agonists - loperamide
Bulk forming laxatives
Metamucil, Citrucel, FiberCon (don't have to know these)
Absorb water --> distend colon --> increase peristalsis
Docusate
Stool Surfactant agent (stool softener, laxative)
Magnesium Hydroxide
Osmotic laxative.
nonabsorbable sugars or salts in GI lumen pulls water out of cells into lumen.
Risk of hypermagnesemia in renal insufficiency.
Lactulose
Osmotic Laxative.
nonabsorbable sugars or salts in GI lumen pulls water out of cells into lumen.
Polyethylene glycol electrolyte solution
Osmotic Laxative
Use for cleansing bowel for endoscopy.
Senna
Stimulant laxative.
Mechanism unknown.
Anthraquinones -natural product
Adverse Effect:"melanosis coli" -brown pigmentation of colon mucosa
Bisacodyl
Stimulant laxative
Mechanism unknown
Diphenylmethane type.
Lubiprostone
Chloride channel activator laxative.
Increases fluid secretion --> increased motility.
Uses: chronic constipation, women with IBS with constipation.
Methylnaltrexone
Opioid receptor antagonist.
opioids cause constipation.
Methylnaltrexone blocks peripheral receptors "without impacting opioid-mediated analgesic effects on the CNS"
Antidiarrheal Drugs
1. Opioid Agonists - loperamide
2. Colloidal bismuth compounds
3. Kaolin and pectin
4. Bile salt-binding resins
5. Octreotide
Loperamide
Antidiarrheal drug - Opioid agonist
-Poor entry to CNS
Colloidal bismuth compounds
Antidiarrheal drug
Kaolin and Pectin
Antidiarrheal drug
Thought to absorb toxins and fluid
Bile salt-binding resins
Antidiarrheal drug for people with increased bile salts in lumen causing diarrhea.
Octreotide
Antidiarrheal drug.
Synthetic peptide with actions similar to somatostatin -decrease hormone release, decrease secretion of fluid into the GI tract, decrease motility
Uses: Decrease endocrine tumor effects (carcinoid, VIPoma)
Drugs used to treat Irritable bowel syndrome
IBS - abdominal pain with predominantly diarrhea or constipation.
1. Antispasmodics (anticholinergics)
2. Serotonin 5-HT3 receptor antagonist - alosetron
3. Chloride Channel activator - lubiprostone
Antispasmodics (Anticholinergics)
Dicyclomine, Hyoscyamine
Treatment of IBS.
Parasympathetic stimulates GI motility so block this.
Alosetron
Serotonin 5-HT3 receptor antagonist.
Treatment of IBS. - decreases pain and diarrhea.
Adverse Effect: Infrequent but serious GI toxicity, including ischemic colitis and constipation with serious complications. Participation in special Prescribing Program required.
Uses: "indicated only for women with severe diarrhea-predominant IBS"
Antiemetic drugs
Vomiting Center can be triggered by many things including Chemoreceptor trigger zone nearby, CNS, GI, Solitary Tract nucleus (5-HT3, D2, M, H1, NK1, CB1), etc.
1. Serotonin 5-HT3 receptor antagonists - ondansetron
2. Corticosteroids
3. Neurokinin-1 receptor Antagonists - Apretitant
4. Phenothiazines - Prochlorperazine, Promethazine
5. Metoclopramide
6. Antihistamines (H1) and anticholingeric drugs - diphenylhydramine, meclizine, scopolamine
7. Benzodiazepines
8. Cannabinoids - Dronabinol
Ondansetron
Antiemetic drug - Serotonin 5-HT3 receptor antagonist.
Blocks 5-HT3 receptors peripherally and centrally in vomiting center, CTZ, solitary tract nucleus, and area postrema.
Oral, IV. Hepativ metabolism
Adverse Effects:Headache, constipation, Increased QT interval.
Uses: Chemotherapy-induced emesis, Postoperative emesis.
Corticosteroids
Dexamethasone
Antiemetic Drug
-mechanism unknown
Use: Chemotherapy-induced nausea and vomiting
Aprepitant
Antiemetic drug - Neurokinin-1 (NK1) receptor antagonist.
(substance P receptor antagonist)
Blocks central NK1 receptors; "inhibits both the acute and delayed phases of cisplatin- induced emesis"
Oral, hepatic metabolism
Adverse Effects: fatigue, dizziness, diarrhea, drug interactions
Uses: Prevention of chemotherapy-induced emesis
Prochlorperazine
Antiemetic drug - Phenothiazine
Inhibits dopamine and muscarinic receptors --> antiemetic effect
Also inhibits histamine receptors --> sedative effect
Promethazine
Antiemetic drug - Phenothiazine
Inhibits dopamine and muscarinic receptors --> antiemetic effect
Also inhibits histamine receptors --> sedative effect
Metoclopramide
Antiemetic Drug (also increases GI motility)
Blocks dopamine receptors --> antiemetic
Adverse effects: extrapyramidal effects (parkinson-like)
Uses: Chemotherapy-induced emesis
Diphenylhydramine
Antiemetic Drug -antihistamine and anticholinergic
Use: Motion sickness
Meclizine
Antiemetic Drug - Antihistamine, minimal anticholinergic effect
Use: Motion sickness
Scopolamine
Antiemetic Drug - Muscarinic Antagonist
Use: Motion sickness
Benzodiazepines
Antiemetic Drug
Dronabinol
Antiemetic Drug - Cannabinoids
Mechanism unknown.
Adverse Effect: CNS effects
Use: Chemotherapy-induced nausea and vomiting "in patients who have failed to respond adequately to conventional antiemetic treatments"
Drugs used to treat Inflammatory Bowel Disease
IBD - ulcerative Colitis or Crohn's disease.
1. Aminosalicylates - sulfasalazine, mealamine
2. Glucocorticoids
3. Purine analogs - azathioprine, 6-mercaptopurine
4. Methotrexate
5. Anti-TNF antibodies - infliximab, adalimumab, certolizumab
6. Anti-integrin Therapy - natalizumab
Sulfasalazine
Aminosalicylates - Treats IBD
Converted by bacteria to 5-ASA in distal GI
Mechanism unknown
Some absorbed in small intestine; >85% sulfapyridine formed from sulfasalazine absorbed in colon
Adverse effects: GI upset, headaches, hypersensitivity reactions, reversible oligospermia, decreased folate absorption
Uses: ulcerative colitis, Chrohn's disease (although efficacy is less striking)
Mesalamine (5-ASA)
Aminosalicylates - Treats IBD
Multiple formulations - delayed release, pH sensitive coating.
Mechanism unknown.
25% absorbed in colon.
Adverse effects: nephrotoxicity, interstitial nephritis
Uses: ulcerative cololitis, Crohn's Disease
Glucocorticoids
Prednisone, Prednisolone, Budesonide
Use: Treatment of inflammatory bowel disease (Crohn's or ulcerative colitis)
Azathioprine
Purine analog - Treats IBD
Converted to 6-mercaptopurine --> active nucleotides interfere with multiple reactions in purine synthese
Adverse effects: Myelosuppression, hepatotoxicity, immunosuppression
Use: Moderately severe to severe disease
6-Mercaptopurine
Purine analog - Treats IBD
active nucleotides interfere with multiple reactions in purine synthese
Adverse effects: Myelosuppression, hepatotoxicity, immunosuppression
Use: Moderately severe to severe disease
Methotrexate
Treats IBD
-Inhibits dihydrofolate reductase --> decreases DNA, RNA and protein sysnthesis (Also an anti-cancer drug)
-Toxicities: myelosuppression, GI and hepatic
Infliximab
Anti-TNF antibodies.
Tumor necrosis factor is an important cytokine in IBD.
-Chimeric monoclonal antibody that binds TNF.
IV
Adverse Effects: Increased risk of infection (reactivation of TB), infusion reactions (can be severe), serum sickness-like reaction, development of antibodies to the drug (may decrease response and increase risk of infusion reaction), reports of lymphoma and other malignancies
Uses: Mod to sever Crohn's disease or ulcerative colitis in patients not responding to conventional therapy
Adalimumab
Human monoclonal antibody administered subcutaneously.
Treats Crohn's disease
Certolizumab
Fab fragment conjugated with polyethylene glycol
Administered subcutaneously
Treats Crohn's disease
Natalizumab
Humanized Mab that binds alpha4-integrin, an adhesion molecule; decreases extravasation of some cells to inflammatory area.
Approved for Chron's dz.
Adverse Effects: increases the risk of progressive multifocal leukoencephalopathy, an opportunistic viral infection of the brain that usually leads to death or severe disability.
Restricted distribution program.
Indicated for inducing and maintaining clinical response and remission in adult patients with moderately to severely active Crohn's disease with evidence of inflammation who have had an inadequate response to, or are unable to tolerate, conventional CD therapies and inhibitors of TNF alpha.
Should not be used in combination with immunosuppressants (6-MP, azathioprine, cyclosporine, or methotrexate) or inhibitors of TNFalpha.
Pancrelipase
Contains amylases, lipases, proteases; porcine derived.
Adverse Effects: Fibrosing colonopathy, increased uric acid, allergic reactions
Uses: Exocrine pancreatic insufficiency (cystic fibrosis)
Ursodiol
Treats certain patients with cholesterol gallstones below a certain size
Drugs to treat Variceal bleeding
Octreotide, Beta blockers