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GI & Inflammation

Pharmacology: GI & Inflammatory Drugs

QuestionAnswer
1. Which enzyme breaks down serotonin? 2. Main metabolite of serotonin 1. MAO type A 2. 5HIAA
Mechanism of action. Receptor involved. Clinical use. 1. buspirone 2. sumatriptan 1. partial agonist (competitive antagonism) of the presynaptic 5HT-1a autoreceptor; anxiolytic 2. agonist at 5HT-1b/1d receptor cranial artery vasoconstriction; migraine and cluster headache
1. What is the cause of emesis during chemotherapy and radiation? 2. Which receptor is involved? 3. Drug that antagonizes receptor. Used as anti-emetic 1. serotonin from enterochromaffin cells in the small intestine is released 2. and binds 5HT3 receptors in the area postrema 3. ondansetron
What role do prostaglandins play in: 1. stomach 2. renal vasculature 3. uterus 4. ductus arteriosus 1. cytoprotective 2. dilate renal vasculature 3. contract uterus 4. maintain ductus arteriosus
Mechanism of action of: 1. Colchicine 2. Allopurinol 3. Probenecid 1. binds to tubulin →↓ microtubular polymerization 2. inhibits xanthine oxidase 3. inhibits proximal tubular reabsorption of urate
1. Drug used for acute gout 2. Long term treatment for patients that overproduce uric acid 3. Long term treatment for patients that underexcrete uric acid 1. colchicine, indomethacin 2. allopurinol 3. probenecid
What is the common side effects of the biological response modifying drugs used in rheumatoid arthritis? since they inhibit the T cell response, patients are susceptible to T cell infections (need a PPD test before starting this therapy)
1. When is COX1 active? 2. When is COX2 active? 1. constitutively active 2. inducible during inflammation
1. Which leukotriene is involved in chemotaxis of neutrophils and macrophages? 2. Zileuton MOA 3. Zafirlukast MOA 1. LTB4 2. Lipoxygenase inhibitor 3. LT-receptor antagonist
1. Prostaglandin analog used in treatment of NSAID-induced ulcers? 2. Which PG does this drug mimic? 1. Misoprostol 2. PGE1
1. Which PG analog maintains patency of ductus arteriosus (PDA)? 2. Which PG does it immitate? 3. Which PG antagonist is used to close a PDA? 1. Alprostadil (Misoprostol also works because it is a PGE1 analog too) 2. PGE1 3. Indomethacin
1. Which prostaglanin drug analog causes uterine smooth muscle contraction? 2. Which prostaglandin acts as a platelet stabilizer and vasodilator? 1. dinoprostone 2. PGI2 (prostacyclin)
Which intracellular messenger do the following act through: 1. TXA2 2. PGI2 1. phospholipase C 2. adenylyl cyclase
1. How does high therapeutic dose of acetylsalicylic acid affect acid-base balance? 2. How does ASA toxicity affect acid-base balance? 1. mild uncoupling of oxidative phosphorylation → need more O2→↑ respiration→↓ pCO2→ respiratory alkalosis 2. respiratory suppression →respiratory and metabolic acidosis
1. Which is often the first sign of salicylate toxicity? 2. Selective COX2 inhibitor 1. tinnitus 2. Celecoxib
How does acetylsalicylic acid effect uric acid elimination? compete with uric acid for secretion resulting in hyperuricemia leading to uricosuria
1. What effect does acetaminophen have on fever, pain and inflammation? 2. Which method of metabolism does acetaminophen go through? 3. What is given to manage hepatotoxicity? 1. analgesic and antipyretic but not antiinflammatory 2. liver glucuronyl transferase or CYP450 followed by glutathione 3. N-acetylcysteine to replenish the glutathione
How do NSAIDs effect renal blood flow? PGE2 maintains patency of the afferent renal arteriole; with NSAID use, the arteriole closes and less blood reaches the kidney
1. What is the mechanism of action of ibuprofen/naproxen? 2. How do ibuprofen/naproxen compare to ASA in analgesia? 1. reversible inhibitors of COX1 and COX2 2. more effective than ASA
1. Why is acetaminophen better suited for osteoarthritis than rheumatoid arthritis? 2. Which drug is implicated in Reye's syndrome? 1. acetaminophen is an effective analgesic/antipyretic and not an effective antiinflammatory 2. Aspirin
1. Current drug of choice in rheumatoid arthritis? 2. Mechanism of action 1. Methotrexate 2. inhibits dihydrofolate reductase to prevent B and T lymphocyte cell division
Mechanism of action of Leflunomide 1. inhibits dihydro-orotate dehydrogenase → ↓ pyrimidine synthesis 2. causes p53 dependent cell cycle arrest in G1
Antirheumatic drug that inhibits: 1. pyrimidine synthesis 2. purine synthesis 1. leflunomide 2. azathioprine
Mechanism of action of cimetidine and ranitidine. 1. antagonizes the H2 histamine receptor in parietal cells 2. leads to decreased activity of the K+/H+ antiporter
Mechanism of action of omeprazole direct inhibitor of the parietal cell proton antiporter (K+/H+)
how do prostaglandins analogs that contain "pros" affect pregnancy? PGs with "pros" can trigger labor contractions (example carboprost)
Mechanism of action as an antirheumatic drug 1. hydroxychloroquine 2. penicillamine 1. ↑ pH of lysosomes to stabilize them and ↓ chemotaxis 2. binds metals and cystein to inhibit T cells and macrophage proliferation
Mechanism of action as an antirheumatic drug 1. Etanercept 2. Inflixamab 3. Anakinra 4. Adalimumab 1. recombinant TNF receptor 2. chimeric IgG antibody to TNF 3. IL-1 receptor antagonist 4. human IgG antibody to TNF
polymerizes on the GI luminal surface to form a protective gel-like coating of ulcer beds Sucralfate
The area postrema contains receptors for which 3 substances? What are the receptors? Which cause emesis? 1. D2 for dopamine - causes emesis 2. 5HT3 for serotonin - causes emesis 3. CB1 for cannabis - prevents emesis
1. NK1 receptors in the spinal cord bind which substance? 2. Which drug antagonizes NK1 receptors? What is its use? 1. substance P, bradykinin 2. aprepitant; anti-emetic in chemotherapy
1. gout medication with side effect of diarrhea and GI pain 2. Long term use of this drug can cause: 1. colchicine 2. alopecia, myelosuppression, peripheral neuropathy (antimitotic properties effect proliferating cells)
1. Which drug should be used to treat gout in patients with recurrent uric acid stones? 1. allopurinol; want to decrease uric acid secretion (so no uricosuric agents)
Sulfasalazine is a prodrug used in which in which two disorder? What activity confers its dual use? Sulfasalazine is converted into: 1. 5-ASA used in ulcerative colitis 2. sulfapyridine used in rheumatoid arthritis
1. Mechanism of action of Glatiramer acetate 2. What drug is used to reverse myelosuppression caused by methotrexate 1. antagonizes myelin basic protein specific T cells by causing Th1 to Th2 immune deviation 2. leucovorin
How do blood pressure medications precipitate gout diuretics, particularly thiazides → hypovolemia → uric acid resorption
Rheumatoid arthritis drug that causes mouth ulcers and hepatotoxicity Methotrexate (stomatitis and hepatotoxicity)
1. How does allopurinol interact with 6-mercaptopurine? 2. How does allopurinol interact with azathioprine? 1. 6-MP is inactivated by xanthine oxidase(XO); allopurinol inhibits XO leading to 6-MP build-up 2. azathioprine is metabolized to 6-MP
Which drug class is used in Pagets disease of bone to decrease activity of osteoclasts and osteoblasts bisphosphonates (etidronate, pamidronate)
Treatment of hepatic encephalopathy Lactulose: degraded by colonic bacteria to lactic acid which traps NH3 in colon by converting it to NH4+
Patient with peptic ulcer, gastritis, complaining of decreased libido and gynecomastia. Which drug was he given? H2 blocker (Cimetidine, ranitidine)
Triple therapy of H. pylori ulcers 1. Metronidazole 2. Amoxicillin (or Tetracycline) 3. Bismuth
Serotonin antagonist that is a powerful antiemetic. Ondansetron
Mechanism and use of Metoclopramide D2 receptor antagonist that stimulates gastric emptying
What effect does diphenoxylate have on peristalsis: inhibits peristalsis (opioid similar to meperidone)
Created by: amichael87