Ellen - Pharmacology 2: Gi Drugs

Front 1

Name 13 antacid drugs :)

Back 1

ALUMINUM HYDROXIDE, MISOPROSTOL, calcium carbonate, OMEPRAZOLE, CIMETIDINE, Pentagastrin, ESOMEPRAZOLE, LANSORPAZOLE, RANITIDINE, MAGNESIUM, sodium bicarbonate, magnesium oxide, SUCRALFATE

Front 2

Name 7 laxatives

Back 2

Bisacodyl, lactulose, docusate, MAGNESIUM HYDROXIDE, mineral oil, methylcellulose, polyethylene glycol 

Front 3

Name 5 antidiarrheals.

Back 3

Atropine, LOPERAMIDE, bismuth subsalicylate, octreotide, diphenoxylatel clonidine

Front 4

Name 6 prokinetic drugs

Back 4

Bethanechol, TEGASEROD, cisapride, ERYTHROMYCIN, neostigmine, METOCLOPR

Front 5

Name 5 H.pylori treatments

Back 5

Bismuth subsalicylate, tetracycline, clarithromycin, metronidazole, amoxicillin

Front 6

Name 5 drugs used to tx inflammatory bowel disease.

Back 6

Steroids (hydrocortisone, prednisone, prednisolone, budesonide), infliximab, balgalazide, mesalamine, sulfasalazine

Front 7

What are the causes of peptic ulcers?

Back 7

Decreased mucosal resistance to acid.
Gastrin-secreting tumors (Zollinger-Ellison syndrome)
Helicobacter pylori

Front 8

What's the approach used to tx peptic ulcers?

Back 8

Neutralize excess acid.
Block acid secretion (H2, M3 and G receptor antagonists).
Repair mucosa.
Antibacterial therapy.

Front 9

What is Zollinger-Ellison syndrome?

Back 9

a rare disorder that causes gastrin- secreting tumors in the pancreas and duodenum, and ulcers in the stomach and duodenum due to excessive production of acid.

Front 10

What percent of Zollinger-Ellison cases are associated with genetic disorders?

Back 10

25%

Front 11

What are the prototype antacids (7)?

Back 11

Mg(OH)2, Al(OH)3, NaHCO3, KHCO3, MgO, MgCl2 and Ca2+ salts

Front 12

What are the adverse effects of antacids?

Back 12

Na salts cause systemic alkalosis and fluid retention, alkalinization of urine.
Al salts cause constipation.
Mg salts cause diarrhea.
Ca salts cause acid rebound.

Front 13

What are the protoype Anticholinergics (3)? How do they work to tx ulcers?

Back 13

Atropine, propantheline (M3), pirenzepine (M1).
Block M-receptors, decrease H+ secretion

Front 14

What are the adverse effects of Anticholinergics?

Back 14

Poor selectivity: interfere with M-receptor mediated regulation of salivary secretion, GI propulsion, heart rate and ocular accommodation.

Front 15

Name 4 prototype H2 receptor antagonists? Mechanism to tx ulcers?

Back 15

Cimetidine, ranitidine, famotidine, nizatidine
Block H2-receptors, decrease H+ secretion.

Front 16

Adverse effects of H2 antagonists?

Back 16

Cimetidine inhibs drug metabolism
High doses have antiandrogenic effect (ZES pts)
Impotence
Mental disorders.

Front 17

Name 1 prototype Gastrin blockers. Mechanism of action in tx of ulcers?

Back 17

Octreotide.
Inhibits secretion of peptide hormones. Effective in Zollinger-Ellison syndrome

Front 18

Adverse effects of Octreotide?

Back 18

Could impair renal function.

Front 19

Name 4 prototype Proton pump inhibitors? Mechanism to tx ulcers?

Back 19

Omeprazole, lansoprazole, rabeprazole, pantoprazole
Covalently bind and inhibit H+,K+-ATPase, decreasing H+ secretion. Useful in ZES pts.

Front 20

Adverse effects of Proton pump inhibitors?

Back 20

Headache, diarrhea and abdominal pain.
Gastric mucosal hyperplasia, due to enhanced synthesis of gastrin.

Front 21

Name one prototype drug in stomach mucosal protection? Mechanism?

Back 21

Misoprostol (prostaglandin agonist)
Stimulates mucus and bicarbonate secretion.
Inhibit gastric acid secretion by parietal cells.

Front 22

Name one prototype stomach ulcer protective drug? Mechanism?

Back 22

Sucralfate, colloidal bismuth compounds
Protect mucosal barrier from acid-pepsin attack by forming a protective layer.
Bind/inhibit pepsin, bind to bile salts.

Front 23

What's the triple therapy used to tx H.pylori ulcers?

Back 23

1. Antimycotics and/or antibiotics (metronidazole, clarithromycin, amoxicillin, tetracycline)
2. Antisecretory drugs: H2-antagonists (cimetidine, ranitidine) Proton pump inhibs (omeprazole)
3. Bismuth salts: bismuth subsalicylate

Front 24

What's GERD caused by and how's it treated?

Back 24

Lower esophageal sphincter disorder
Prokinetic drug therapy

Front 25

What are the causes of constipation?

Back 25

Functional disorders.
Dietary changes.
Drug treatment.
Low-residue diet.

Front 26

Ways to treat constipation?

Back 26

Prokinetic drugs + laxatives.
Return to normal diet.
Discontinue drug treatment.
Include fiber-rich food.

Front 27

What is Bethanechol? Mechanism of action in GI?

Back 27

M2 receptor agonist
Increases contraction of the GI smooth muscle = prokinetic

Front 28

Adverse GI effects of Bethanechol?

Back 28

Excessive secretory activity of salivary, gastric, pancreatic and intestinal cells.

Front 29

What are the 5 different groups of prokinetic drugs?

Back 29

M2 receptor agonists
AChE inhibitors
DA receptor blockers
5-HT receptor agonists
Motilin agonists

Front 30

Name 3 AChE inhibitors used as prokinetics. What's their mechanism of action?

Back 30

Block degradation of acetylcholine

Front 31

Adverse GI effects of AChE inhibitors?

Back 31

Excessive secretory activity of salivary, gastric, pancreatic and intestinal cells.
Cramps

Front 32

What's Metoclopramide?

Back 32

DA receptor blocker used as a prokinetic drug.

Front 33

Mechanism of GI action of Metoclopramide?

Back 33

Blocks presynaptic D2-receptors, increase release of Ach from nerve terminals.
Increases the tone of the lower esophageal sphincter (important in reflux esophagitis).
Antiemetic effects.

Front 34

Adverse effects of Metoclopramide?

Back 34

Fatigue, insomnia, altered motor coordination. Hyperprolactinemia could cause galactorrhea and menstrual disorders

Front 35

Name 2 5-HT receptor agonists used as prokinetics.

Back 35

Cisapride (no longer in use), tegaserod

Front 36

Mechanism of action for 5-HT receptor agonists on the GI tract?

Back 36

Activate presynaptic 5-HT4 receptors, increase release of Ach.
Increase tone of the lower esophageal sphincter (gastro-esophageal reflux).

Front 37

Adverse GI effects of 5-HT receptor agonists?

Back 37

Enhanced salivation, lacrimation, sweating, urination, defecation.
Could exacerbate peptic ulcer and asthma

Front 38

How is Erythromycin used as a prokinetic?

Back 38

Motilin agonist- Activates neural and smooth muscle motilin receptors. Effective in postoperative and diabetic gastroparesis.

Front 39

Adverse effects with using erythromycin as a prokinetic?

Back 39

Occasional epigastric pain, abdominal cramps, nausea and emesis.
Long-term medication could reversibly promote hepatotox (jaundice, fever, leukocytosis and eosinophilia).

Front 40

What prototype secretory drugs are used in the treatment of constipation?

Back 40

Castor oil (ricinoleic acid), diphenoxylate docusate.
Natural: cascara, senna, aloe.
Synthetic: phenolphthalein and bisacodyl

Front 41

What is the mechanism of action for secretory drugs (castor oil/diphenoxylate) used in the treatment of constipation?

Back 41

Open Cl- and Na+ channels, and ion efflux stimulates water movement into the GI lumen

Front 42

Adverse effects of secretory drugs (castor oil/diphenoxylate) used in the treatment of constipation?

Back 42

Could produce electrolyte imbalance.
Long-term use leads to habituation, damage to the myenteric plexus and colonic atony

Front 43

Name 4 prototype saline laxatives.

Back 43

Mg(OH)2 , lactulose, Na3PO4 and Na2SO4.

Front 44

Mechanism of action for saline laxatives?

Back 44

Poorly absorbable ions, leading to osmosis-driven water transfer into the intestinal lumen.
Distension activates stretch receptors and produces physiological stimulus for peristalsis

Front 45

Adverse effects of saline laxatives?

Back 45

Occasionally produce explosive watery bowel movements.
Upon prolonged usage absorption of Na causes blood and urine alkalinization.

Front 46

Name 3 prototype emolients (stool softeners). Mechanism of action?

Back 46

Mineral oil, glycerin, docusate salts.
Nonabsorbable lubricants of the lower bowel in conditions of irritated anal tissues

Front 47

Adverse effects of emolients?

Back 47

Mineral oil is itself absorbed from the GIT or inhaled into the lungs, and may produce inflammatory responses, e.g. lipoid pneumonia.
Docusate may increase GI absorption of other laxatives and lead to liver toxicity.

Front 48

What are the acute and chronic causes of diarrhea?

Back 48

Acute: bacterial/viral infection.
Chronic: inflammation or functional bowel disease.
Laxatives abuse.

Front 49

What are the treatments for diarrhea?

Back 49

Bismuth subsalicylate.
Opioid therapy.
Remove source.
Fluid and electrolyte replacement

Front 50

What's Bismuth subsalicylate? Mechanism in the GI?

Back 50

An antisecretory agent that decreases fluid secretion with high activity against enterotoxigenic strains (E. coli). Antibacterial activity.

Front 51

Name 4 prototype opioid receptor agonists used in the tx of diarrhea.

Back 51

morphine, codeine, loperamide, diphenoxylate

Front 52

Antidiarrheal mechanism of action of opioids?

Back 52

Inhibit release of Ach, decrease propulsion.
Decrease net fluid secretion, promote fluid absorption

Front 53

Adverse effects of opioids?

Back 53

Constipation
Respiratory depression at high doses (not prescribed for chronic use)

Front 54

What's Dicyclomine and how's it used in the GI tract?

Back 54

muscarinic antagonist. Used to tx diarrhea by reducing contractile activity and alleviating GI spasms and pylorospasm.

Front 55

Adverse effects of Dicyclomine?

Back 55

Dry mouth, blurred vision, tachycardia, urinary retention, cutaneous vasodilation and paralysis of stomach and intestines with constipation.

Front 56

What are the bulk/gel forming substances used to tx diarrhea? (6)

Back 56

Bran, methylcellulose, psyllium, hydrated aluminum silicate, pectin, kaolin.

Front 57

Mechanism of action of the bulk/gel forming substances in the tx of diarrhea?

Back 57

Nonabsorbable compounds form large hydrophilic mass
Increase resistance to intestinal lumen flow
Increase firmness of stool

Front 58

Adverse effects of the bulk/gel forming substances?

Back 58

May interfere with absorption of some drugs.
Kaolin absorbs bacterial toxins and could cause diarrhea

Front 59

What's the cause of ulcerative colititis? What about Crohn's disease?

Back 59

Unknown (both)
Suspected viral or bacterial infection.
Immune disorders

Front 60

What part of the GI is effected in ulcerative colitis?

Back 60

The mucosa of the colon and (sometimes) the anus

Front 61

What part of the GI is effected in Crohn's disease?

Back 61

The entire intestinal wall in the ileum, rectum and colon (mainly - can effect the whole GI tract though)

Front 62

Symptoms of ulcerative colitis?

Back 62

Bloody diarrhea, weight loss and abdominal pain.

Front 63

Symptoms of Crohn's disease?

Back 63

Chronic diarrhea, crampy abdominal pain, loss of appetite and weight.

Front 64

What are the 5 mediators of acute inflammation?

Back 64

Prostaglandins
Leukotrienes
Histamine
Serotonin
Bradykinin

Front 65

What are the 2 mediators of chronic inflammation?

Back 65

TNFa
Interleukins

Front 66

Name 2 corticosteriods used to tx ulcerative colitis/crohn's disease. Mechanism?

Back 66

Hydrocortisone, prednisone.
Reduce expression of COX2
Inhibit PLA2 activity.
Immunosuppressive effects.

Front 67

Adverse effects of Corticosteroids?

Back 67

Enhanced susceptibility to infections and cancer, ulcer, hyperglycemia, osteoporosis, edema, hypokalemia, Cushings syndrome.

Front 68

Name 4 Salicylates used to tx ulcerative colitis/crohn's disease. Mechanism?

Back 68

Mesalamine (5-ASA), sulfasalazine, olsalazine, balsalazide.
Poorly absorbed inhibitors of COX2 (inhib production of prostaglandin and leukotriene)

Front 69

Adverse effects of Salicylates?

Back 69

Upper GIT irritation after oral intake.
N/V, headache, abdominal discomfort, watery diarrhea

Front 70

Name 3 Cytostatic drugs
used to tx ulcerative colitis/crohn's disease. Mechanism?

Back 70

Azathioprine, 6-mercaptopurine and methotrexate.
Antimetabolites: suppress immune response

Front 71

Adverse effects of Cytostatic drugs?

Back 71

Bone marrow suppression, leukopenia and thrombocytopenia,
Liver and GIT toxicity
Cystitis, pulmonary fibrosis.

Front 72

What is INFLIXUMAB (REMICADE)?

Back 72

chimeric human/murine antibody that inactivates membrane-bound TNFalpha.
Effective in tx of Crohn’s disease

Front 73

Adverse effects of INFLIXUMAB (REMICADE)?

Back 73

Nausea, autoimmune diseases and malignancies.
IV administration of antibodies could produce flu-like symptoms with fluid retention and possible pulmonary edema.
Antibodies against the murine epitope may develop.