Gastrointestinal Drugs - Gi Drugs

Front 1

Review Gastric Acid Secretion

Back 1

Need to look at Amanda's LO's when she puts them up.

Front 2

Review of Mucosal defense mechanism in the Stomach

Back 2

Noxious (harmful) factors: HCL, pepsin, others
Defense factors: mucus, cells, bicarbonate, prostaglandins, other

Front 3

Drugs used in Acid-Peptic Disease

Back 3

1. Drugs that decrease gastric acidity: Antacids, H2 receptor blockers, Proton pump inhibitors
2. Drugs that increase mucosal defenses: Sucralfate, Misoprostil, Bismuth compounds

Front 4

Antacids

Back 4

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

Front 5

Aluminum hydroxide

Back 5

Antacid.
Adverse effects: Diarrhea (so give with magnesium), problems in renal insufficiency.
Use: heartburn, dyspepsia

Front 6

Aluminum hydroxide - magnesium hydroxide combination

Back 6

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

Front 7

Calcium carbonate

Back 7

Antacid
Adverse Effects: high doses with certain dairy products (Ca containing) can cause milk-alkali syndrome = hypercalcemia, metabolic alkalosis, renal insufficiency.
Uses: heartburn, dyspepsia

Front 8

H2 Receptor Blockers

Back 8

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.

Front 9

Cimetidine

Back 9

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

Front 10

Ranitidine

Back 10

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

Front 11

Proton Pump Inhibitors

Back 11

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)

Front 12

Omeprazole

Back 12

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)

Front 13

Esomeprazole

Back 13

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)

Front 14

Lansoprazole

Back 14

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)

Front 15

Sucralfate

Back 15

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

Front 16

Misoprostil

Back 16

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.

Front 17

Bismuth Compounds

Back 17

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.

Front 18

Drugs that Increase GI motility

Back 18

Metoclopramide, Erythromycin

Front 19

Metoclopramide

Back 19

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

Front 20

Erythromycin

Back 20

Increases GI motility.
Mechanism: stimulates motilin receptors. Motilin increases contraction in upper GI tract.
Use: Diabetic gastroparesis

Front 21

Laxatives

Back 21

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

Front 22

Bulk forming laxatives

Back 22

Metamucil, Citrucel, FiberCon (don't have to know these)
Absorb water --> distend colon --> increase peristalsis

Front 23

Docusate

Back 23

Stool Surfactant agent (stool softener, laxative)

Front 24

Magnesium Hydroxide

Back 24

Osmotic laxative.
nonabsorbable sugars or salts in GI lumen pulls water out of cells into lumen.
Risk of hypermagnesemia in renal insufficiency.

Front 25

Lactulose

Back 25

Osmotic Laxative.
nonabsorbable sugars or salts in GI lumen pulls water out of cells into lumen.

Front 26

Polyethylene glycol electrolyte solution

Back 26

Osmotic Laxative
Use for cleansing bowel for endoscopy.

Front 27

Senna

Back 27

Stimulant laxative.
Mechanism unknown.
Anthraquinones -natural product
Adverse Effect:"melanosis coli" -brown pigmentation of colon mucosa

Front 28

Bisacodyl

Back 28

Stimulant laxative
Mechanism unknown
Diphenylmethane type.

Front 29

Lubiprostone

Back 29

Chloride channel activator laxative.
Increases fluid secretion --> increased motility.
Uses: chronic constipation, women with IBS with constipation.

Front 30

Methylnaltrexone

Back 30

Opioid receptor antagonist.
opioids cause constipation.
Methylnaltrexone blocks peripheral receptors "without impacting opioid-mediated analgesic effects on the CNS"

Front 31

Antidiarrheal Drugs

Back 31

1. Opioid Agonists - loperamide
2. Colloidal bismuth compounds
3. Kaolin and pectin
4. Bile salt-binding resins
5. Octreotide

Front 32

Loperamide

Back 32

Antidiarrheal drug - Opioid agonist
-Poor entry to CNS

Front 33

Colloidal bismuth compounds

Back 33

Antidiarrheal drug

Front 34

Kaolin and Pectin

Back 34

Antidiarrheal drug
Thought to absorb toxins and fluid

Front 35

Bile salt-binding resins

Back 35

Antidiarrheal drug for people with increased bile salts in lumen causing diarrhea.

Front 36

Octreotide

Back 36

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)

Front 37

Drugs used to treat Irritable bowel syndrome

Back 37

IBS - abdominal pain with predominantly diarrhea or constipation.
1. Antispasmodics (anticholinergics)
2. Serotonin 5-HT3 receptor antagonist - alosetron
3. Chloride Channel activator - lubiprostone

Front 38

Antispasmodics (Anticholinergics)

Back 38

Dicyclomine, Hyoscyamine
Treatment of IBS.
Parasympathetic stimulates GI motility so block this.

Front 39

Alosetron

Back 39

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"

Front 40

Antiemetic drugs

Back 40

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

Front 41

Ondansetron

Back 41

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.

Front 42

Corticosteroids

Back 42

Dexamethasone
Antiemetic Drug
-mechanism unknown
Use: Chemotherapy-induced nausea and vomiting

Front 43

Aprepitant

Back 43

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

Front 44

Prochlorperazine

Back 44

Antiemetic drug - Phenothiazine
Inhibits dopamine and muscarinic receptors --> antiemetic effect
Also inhibits histamine receptors --> sedative effect

Front 45

Promethazine

Back 45

Antiemetic drug - Phenothiazine
Inhibits dopamine and muscarinic receptors --> antiemetic effect
Also inhibits histamine receptors --> sedative effect

Front 46

Metoclopramide

Back 46

Antiemetic Drug (also increases GI motility)
Blocks dopamine receptors --> antiemetic
Adverse effects: extrapyramidal effects (parkinson-like)
Uses: Chemotherapy-induced emesis

Front 47

Diphenylhydramine

Back 47

Antiemetic Drug -antihistamine and anticholinergic
Use: Motion sickness

Front 48

Meclizine

Back 48

Antiemetic Drug - Antihistamine, minimal anticholinergic effect
Use: Motion sickness

Front 49

Scopolamine

Back 49

Antiemetic Drug - Muscarinic Antagonist
Use: Motion sickness

Front 50

Benzodiazepines

Back 50

Antiemetic Drug

Front 51

Dronabinol

Back 51

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"

Front 52

Drugs used to treat Inflammatory Bowel Disease

Back 52

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

Front 53

Sulfasalazine

Back 53

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)

Front 54

Mesalamine (5-ASA)

Back 54

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

Front 55

Glucocorticoids

Back 55

Prednisone, Prednisolone, Budesonide
Use: Treatment of inflammatory bowel disease (Crohn's or ulcerative colitis)

Front 56

Azathioprine

Back 56

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

Front 57

6-Mercaptopurine

Back 57

Purine analog - Treats IBD
active nucleotides interfere with multiple reactions in purine synthese
Adverse effects: Myelosuppression, hepatotoxicity, immunosuppression
Use: Moderately severe to severe disease

Front 58

Methotrexate

Back 58

Treats IBD
-Inhibits dihydrofolate reductase --> decreases DNA, RNA and protein sysnthesis (Also an anti-cancer drug)
-Toxicities: myelosuppression, GI and hepatic

Front 59

Infliximab

Back 59

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

Front 60

Adalimumab

Back 60

Human monoclonal antibody administered subcutaneously.
Treats Crohn's disease

Front 61

Certolizumab

Back 61

Fab fragment conjugated with polyethylene glycol
Administered subcutaneously
Treats Crohn's disease

Front 62

Natalizumab

Back 62

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.

Front 63

Pancrelipase

Back 63

Contains amylases, lipases, proteases; porcine derived.
Adverse Effects: Fibrosing colonopathy, increased uric acid, allergic reactions
Uses: Exocrine pancreatic insufficiency (cystic fibrosis)

Front 64

Ursodiol

Back 64

Treats certain patients with cholesterol gallstones below a certain size

Front 65

Drugs to treat Variceal bleeding

Back 65

Octreotide, Beta blockers