Gastro Pharm

Question 1

Xerostomia Tx
M3»M1, CYP3A3/4 interactions CYP2D6 ; contraindicated in asthma, closed angle glaucoma or iritis (caution w/ cardiac disease  change in conduction through the AVN, nephrolithiasis)
(cholingergic  bronchial smooth muscle constriction, will cause a change in visual acuity, & difficult w/ vision in transition to darkness

Answer 1

Cevimeline

Question 2

Xerostomia Tx

All muscarinic receptors, also avoid in psychosis owing to greater CNS activity (as well as contraindications above)

Answer 2

Pilocarpine

Question 3

Xerostomia Tx
free radical scavenger, given as a nephroprotective agent in cisplatin & to protect salivary glands in the protection during irradiation of the head & neck (can permanently damage the salivary glands)

Answer 3

Amifostine

Question 4

Magnesium-aluminum hydroxide

Answer 4

balance between constipation by aluminum & diarrhea by magnesium – Mylanta

Question 5

H2 Antagonist
lowest potency (1); inhibits P450 and slows metabolism of many drugs

Answer 5

Cimetidine

Question 6

H2 Antagonist

middle potency, name 2

Answer 6

Ranitidine

Nizatidine

Question 7

Strongest H2 Antagonist

Answer 7

Famotidine

Question 8

(Pepto-Bismal)–enhances secretion of mucus and HCO3, inhibits pepsin activity, chelates w/ proteins at the base of the ulcer crater and forms a protective barrier against acid and pepsin; inhibits H pylori; effective adjunct for tx PUC/ duodenal/ gastric ulcers, diarrhea

Answer 8

Bismuth subsalicylate

Question 9

forms a sticky, viscous gel that adheres to gastric epithelial cells protecting them from acid and pepsin; only agent in its class that requires an acidic pH for max activity; given 1 hr before meals and at bedtime to promote gastric healing; value in H2 blocker/ PPI induced pneumonia in bedridden patients; alkalinization of stomach reintroduces bacteria to stomach

Answer 9

Sucralfate

Question 10

PPI

oral, long duration, more powerful than H2 blockers - name 2

Answer 10

Omeprazole

Esomeprazole

Question 11

PPI, less effective in severe esophagitis

Answer 11

Lansoprazole

Question 12

PPI, less metabolized by P450

Answer 12

Rebeprazole

Question 13

Cytoprotective Agent; slowly metabolized analog of PGE1, stimulates mucus and HCO3 production, diarrhea in 40% patients; used in patients who must use NSAIDS
(mostly used for abortion)

Answer 13

Misoprostol

Question 14

Eradication of H pylori

Answer 14

Clarithromycin – macrolide, inhibits protein synthesis
Metronidazole –active against obligate anaerobes (more primary resistance 43%)
Tetracycline - second line for pt allergic to penicillin; stagger dose when given w/ bismuth; least primary resistance (<1%)
Amoxicillin- Effective against Gram Negative bacilli (resistance 3%)
Furazolidine – Nitrofuran antibacterial& antiprotozoal

Question 15

Enhances gastric motility, improves LES tone) - prokinetic agents

Answer 15

only Rx approved for gastroparesis

sensitization of smooth muscle muscarinic receptors

DA receptor blocker, serotonin blocker –> antiemetic effects

tardive dyskinesia

stimulates GI smooth muscle. Increases amplitude of esophageal contractions, accelerates gastric emptying, increases LES pressure (main anti-reflux is enhanced gastric emptying)

Question 16

local dopamine blocker (not FDA approved in US, but patients can purchase medicine from Canda); tx for gastroparesis

Answer 16

Domperidone

Question 17

partial 5HT-4 agonist (selective serotonin agonist), short-term tx of constipative IBS (increased rate of stroke, heart attack & worsening heart-related chest pain)

Answer 17

Tegaserod

Question 18

treatment of IBD: control inflammation, reduce morbidity, prevent complications, nutrition; given as enteric tablet, broken down by intestinal bacteria to sulfapyridine (causes SE  anemia, rash, importence) & 5-aminosalicyclic acid (5-ASA acts like a local anti-inflammatory agent)

Answer 18

Sulfasalazine

Question 19

monoclonal Ab against TNF-alpha; IV for Crohn’s; given with immunosuppressive therapy

Answer 19

Infliximab

Question 20

inhibits integrins from binding to intestinal lining

Answer 20

Natalizumab

Question 21

semisynthetic disaccharide; metabolized by enteric bacteria to organic acids such as lactic, formic, acetic acid – a fecal acidifier; acidification of the stool retards nonionic diffusion of ammonia from the colon to the blood because NG3 is the ammonium form which is non-diffusable; sinch lactulose is not absorbed, it produces an osmotic laxative effect

Answer 21

Lactulose

Question 22

Ribavirin, Telaprevir, Boceprevir, Peginterferon-a-2b

Answer 22

Hep C

Question 23

Tenofovir, entecavir, telbivudine, adefovir, lamivudine, emtricitabine

Answer 23

Hep B

Question 24

Lamivudine, Telbivudine class

Answer 24

L-nucleoside - Hep B

Question 25

Adefovir, Tenofovir

Answer 25

Acyclic Phosphonates - Hep B

Question 26

Entecavir

Answer 26

D-cyclopentane - Hep B

Question 27

nucleotide analog of adenosince 5 monophosphate; diphosphate form inhibits polymerase and terminates chain

Taken with high fat

AE: ARF, avoid NSAIDs, ask about bone pain
Patients predisposed dysfunction in apical pump so that drug cannot be extruded into lumen/ urine (increased renal toxicity) – OAT1 KOs have proximal tubule accumulation

Bone pain?

active against HIV and HBV

Answer 27

Tenofovir

Question 28

Guanosine nucleoside analog

food delays absorption

Answer 28

Entecavir

Question 29

L-isomer of thymidine

food- no effect

Answer 29

Telbivudine

Question 30

Adenosine-5 monophosphate - chain termination in diphosphate form

Answer 30

Adefovir

Question 31

L-isomers of cytosine; triphosphate form inhibits HBV

food - no effect

Answer 31

Lamivudine

Emtricitabine

Question 32

Serine protease inhibitors for Hep C-1

bind plasma proteins, take them with food, undergo hepatic metabolism, eliminated in stool

Answer 32

Telaprevir

Boceprevir

Question 33

First line for Hep C
high fat meal is beneficial for distribution;

enhanced host T cell function,

inhibition of host inodine monophosphate dehydrogenase (IMPDH) w/ depletion of guanosine triphosphate, essential for viral RNA synthesis

direct inhibition of RNA-dep RNA polymerase, may only transiently reduce HCV RNA but will normalize ALT

synergistic w/ interferon
Primary toxicity: hemolytic anemia (10-13%), extensive uptake into cells (indlucing erythrocytes), no CYP action, renal elimination; available as inhalation product

Answer 33

Ribivirin

Question 34

Serine protease for HepC1 that can cause rash & inhibits CYP3A4

Answer 34

Telapravir