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Pharmacology-PA
GI Lecture #2
| Question | Answer |
|---|---|
| 1. What drug is a Cyto-Protective Agent? | Sucralfate (carafate) |
| 2. What is Sucralfate (carafate)? | Complex of Aluminum Hydroxide & Sulfated Sucrose |
| 3. What is the mechanism of Action of Sucralfate (carafate)? | It coats the ulcerated mucosa by binding to positively charged groups in proteins and glycoproteins of necrotic tissue |
| 4. Does Sucralfate (carafate) absorb systemically? | No |
| 5. Does Sucralfate (carafate) requires acidic pH to dissolve & coat the ulcerative tissue? | Yes |
| 6. Can Sucralfate (carafate) be given with H2-antagonist, PPIs, or antacids? | No, bc it requires acidic pH to dissolve and coat the ulcerative tissue. |
| 7. Is the Administration-difficult for Sucralfate (carafate)? | Yes |
| 8. How should Sucralfate (carafate) not be given? | Should not be given with food |
| 9. How should Sucralfate (carafate) be given? | Give 1hr before or 3hr after meal |
| 10. What is the Dose of Sucralfate (carafate)? | 1gm/ 4times daily or 2 gm/ 2times daily |
| 11. Is the Sucralfate (carafate) tablet large and difficult to swallow? | Yes |
| 12. How long should Sucralfate (carafate) be administered? | Must be given for 6-8 weeks |
| 13. What are the side effects of Cyto-Protective Agent (Sucralfate)? | Constipation; dark stool; dry mouth |
| 14. Is Cyto-Protective Agent (Sucralfate) very safe in pregnancy? | Yes |
| 15. What drug is a Prostaglandin Agonists (PGE1)? | Misoprostol |
| 16. Is Misoprostol a methyl analog of PGE1? | Yes |
| 17. Does Misoprostol inhibit secretion of mucus and bicarbonate? | Yes |
| 18. What drug is approved for the prevention of ulcer induced by NSAIDS? | Misoprostol |
| 19. What is Misoprostol’s role in ulcer treatment? | difficult to define |
| 20. T/F Routine clinical prophylaxis of NSAID, which induces ulcers, may not be justified as PPIs being effective. | True |
| 21. T/F In patients requiring NSAIDs, Misoprostol or PPI prophylaxis is cost effective. | True |
| 22. How should Misoprostol be administered? | Should be given 4 time/ day ( inconvenient) |
| 23. What are the side effects of Misoprostol? | Up to 20% develop diarrhea & cramps |
| 24. Is Misoprostol a category X drug that induces labor? | Yes |
| 25. T/F Antacids are weak bases that react with gastric acid to form water & salt (Neutralize acid). | True |
| 26. T/F Antacids stimulate prostaglandin production. | True |
| 27. T/F Antacids bind injurious substances. | True |
| 28. Do Antacids vary in palatability & price? | Yes |
| 29. What are the Antacids? | Sodium-bicarbonate, Aluminum-hydroxide, magnesium-hydroxide and calcium carbonate |
| 30. Do Antacids provide large neutralizing capacity? | Yes |
| 31. What is the 1st dose given of Antacids? | A 1st dose of 156 meq antacid is given 1 hr after meal |
| 32. What does the 1st dose effectively do? | It effectively neutralizes gastric acid for 2 hr |
| 33. What is the 2nd dose given of Antacids? | The 2nd dose is given 3 hr after eating |
| 34. What does the 2nd dose help to do? | It helps to maintains the effect for over 4 hr after the meal |
| 35. T/F By altering gastric and urinary pH or delaying gastric emptying, antacids can affect absorption, dissolution, bioavailability and renal elimination of other drugs. | True |
| 36. What drugs sometimes chelate (binding) other drugs to form insoluble complexes that can prevent absorption? | Antacids |
| 37. What are the ADR of Sodium-bicarbonate (NaHCO3)? | systemic alkalosis, fluid retention |
| 38. What are the ADR of Calcium Carbonate (CaCO3)? | hypercalcemia, nephrolithiasis |
| 39. What are the ADR of Aluminum-Hydroxide (Al(OH)3)? | constipation, hypophosphatemia |
| 40. What are the ADR of Magnesium-Hydroxide (Mg(OH)2)? | diarrhea, hypermagnesemia |
| 41. T/F Since Aluminum hydroxide can be constipating and Magnesium hydroxide can produce diarrhea, they are sometimes used in combination? | True |
| 42. T/F Calcium-carbonate containing antacids work rapidly & very effectively but large dose may cause calciuria-possible stone formation? | True |
| 43. Are high dose antacids very inconvenient to administer? | Yes |
| 44. Are tablet antacids generally weak in their neutralizing capability and need a large number of tablets for this high-dose regimen? | Yes |
| 45. Is the Sodium content in the Antacids an issue with congestive heart failure? | Yes |
| 46. What is the Mechanism of Antacids? | To neutralize acid |
| 47. What are the common side affects of Antacids? | Mg - diarrhea, belching and flatulence; Al – constipation; Ca – constipation |
| 48. What is the Mechanism of Action of H2 receptor antagonist? | To Block histamine receptor |
| 49. What is the common side effects of H2 receptor antagonist? | Cytochrome 450 interactions metabolism of drugs |
| 50. What is the Mechanism of Action of Prostaglandins? | Agonist |
| 51. What are the common side effects of Prostaglandins? | Diarrhea, cramps, abortion |
| 52. What is the mechanism of Action of H+/K+ ATPase inhibitors? | Block acid pump |
| 53. What are the common side effects of H+/K+ ATPase inhibitors? | Hypergastrinemia enterochromaffin cell (ECL) hyperplasia |
| 54. What is the mechanism of action of Sucrafate? | To Coat ulcerated mucosa |
| 55. What is the common side effect of Sucrafate? | Constipation |
| 56. What % of Gastric Ulcers are associated with H. pylori? | 60-70% |
| 57. What % of Duodenal Ulcers associated with H. pylori? | 90% |
| 58. T/F Antibiotics for H. Pylori eradication is less expensive than chronic anti-secretory therapy. | True |
| 59. T/F Antibiotics for H. Pylori eradication significantly reduces the risk of ulcer recurrence & re-bleeding. | True |
| 60. Is it necessary to continue antisecretory therapy for more than 2 weeks following antibiotic treatment after H. pylori eradication? | No. |
| 61. T/F Until recently, the recommended duration of therapy for H.pylori eradication was 10 -14 days. | True |
| 62. T/F There are a number of recent studies evaluated seven-, five-, & even one-day regimens. | True |
| 63. Has it been proven that potential benefits of shorter regimens include better compliance, fewer adverse drug effects, & reduced cost to the patient? | No, it has not been proven yet. |
| 64. What are the most commonly reported adverse events? | nausea, vomiting, & diarrhea |
| 65. What drug has a bitter or metallic taste in the mouth that is associated with eradication regimens? | Clarithromycin |
| 66. What drug may cause temporary grayish-black discoloration of the stools? | Bismuth subsalicylate |
| 67. In the Treatment regimen for H. pylori eradication of Omeprazole 20mg BID + Amoxicillin 1g BID + Clarithromycin500 mg BID, what is the Duration and eradication rate? | Duration is 14 days and Eradication Rate is 80-86% |
| 68. In the Treatment regimen for H. pylori eradication of Lansoprazole 30mg BID + Amoxicillin 1g BID + Clarithromycin500 mg BID, what is the Duration and eradication rate? | Duration is 10-14 days and Eradication Rate is 86%. |
| 69. In the Treatment regimen for H. pylori eradication of Bismuth subsalicylate 525mg QID + Metronidazole 250mg QID + Tetracycline 500mg + Histamine H2 blocker, what is the Duration and eradication rate? | Duration is 14 days (H2 blocker alone for an additional 14 days taken once or twice daily) and Eradication Rate is 80%. |
| 70. For the eradication of Helicobacter pylori for the treatment regimen of Bismuth subsalicylate 524mg QID + amoxicillin 2g QID + metronidazole 500mg QID + lansoprazole 60mg once, what is the Duration, Population studied and eradication rate? | Duration: 1 day, Population studied: H. Pylori (+) patients with dyspepsia, and Eradication Rate: 95% |
| 71. In the short-course therapy for eradication of Helicobacter pylori for the treatment regimen of Lansoprazole 30mg BID + Amoxicillin 1g BID + Clarithromycin500 mg BID, what is the Duration, Population studied and eradication rate? | Duration: 7 day, Population studied: H. Pylori (+) patients with dyspepsia, and Eradication Rate: 90% |
| 72. For the eradication of Helicobacter pylori for the treatment regimen of Clarithromycin250 mg BID + amoxicillin 1g BID + metronidazole 400mg BID + lansoprazole 30mg BID, what is the Duration, Population studied and eradication rate? | Duration: 5 day, Population studied: H. Pylori (+) patients with dyspepsia for 3 months or endoscopically confirmed ulcers, and Eradication Rate: 89% |
| 73. For the eradication of Helicobacter pylori for the treatment regimen of Clarithromycin250 mg BID + amoxicillin 1g BID + metronidazole 400mg BID + ranitidine300mg BID, what is the Duration, Population studied and eradication rate? | Duration: 5 day, Population studied: H. Pylori (+) patients with dyspepsia for 3 months or endoscopically confirmed ulcers, and Eradication Rate: 89% |
| 74. For the eradication of Helicobacter pylori of the treatment regimen of Lansoprazole 30 mg BID for 2 days (pretreatment) + amoxicillin 1g BID + metronidazole 400mg BID + clarithromycin 250mg BID + lansoprazole 30mg BID, what is the Dur., P.S and ER? | Duration: 5 day, Population studied: H. Pylori (+) patients with dyspepsia for 3 months or endoscopically confirmed ulcers, and Eradication Rate: 81% |
| 75. T/F Resistant H. pylori has been documented in cases of failed eradication therapy based on biopsy & culture results. | True |
| 76. T/F Resistance represents a serious problem in patients at high risk for complications of H.pylori infection. | True |
| 77. What is the Resistance rate for Clarithromycin? | It is currently 2-30% |
| 78. What is the resistance rate for metronidazole? | It is 15-66% |
| 79. T/F Primary resistance to clarithromycin is a strong predictive risk factor for treatment failure, whereas primary resistance to metronidazole does not always lead to treatment failure. | True |
| 80. What triple drug therapy responds well for 70 % of patients failing one or more regimens? | Pantoprazole, amoxicillin, & levofloxacin for 10 days |
| 81. What is the quadruple drug therapy that is a meta-analysis of the current literature on treatment of resistant for H. pylori showed benefit in treatment? | Clarithromycin + ranitidine + bismuth + amoxicillin (1 g twice daily) therapy, as well as a combination of PPIs (standard dosage for 10 days) + bismuth + Metronidazole + tetracycline |
| 82. What are the Risk factors for recurrence? | Non-ulcer dyspepsia, Persistence of chronic gastritis after eradication therapy, Female gender, Intellectual disability, Younger age, High rates of primary infection, Higher urea breath test values |
| 83. T/F Recurrence rates worldwide vary but are lower in developed countries. | True |
| 84. T/F In the primary care setting, physicians may choose to treat recurrences with an alternative eradication regimen, depending on symptoms & risk factors for complications of infection. | True |
| 85. T/F It is too early to know whether shorter courses of eradication therapy will be associated with a higher resistance rate. | True |
| 86. What area is the chemoreceptor trigger zone (CTZ) for vomiting (emesis)? | It is in the area postrema (AP) at the caudal end of the fourth ventricle. |
| 87. Where is the CTZ located? | This is located on the dorsal surface of the medulla oblongata |
| 88. T/F The CTZ is one of the “circumventricular organs” that interface between the brain parenchyma and the cerebrospinal fluid (CSF)- containing ventricles. | True |
| 89. What does the AP lack? | Lacks the “blood-brain” diffusion barrier to large polar molecules and can respond to emetic toxins in the blood as well as in the CSF. |
| 90. What are the Nausea/Vomiting (Antiemetics)? | Dopamine antagonists, Serotonin (5-HT3) antagonists, Antihistamines & Anticholinergics, Cannabinoids, Corticosteroids, Sedatives |
| 91. What is the result of preventing neurotransmitters from reaching their respective receptors in the brain and gastrointestinal tract? | Its becomes effective in preventing and treating emesis. |
| 92. What drug classes’ receptors are capable of preventing nausea and vomiting? | Drug classes that antagonize dopaminergic (D2), serotonergic (5-HT3), neurokinin-1 (NK1), histaminic (H1), and muscarinic (M) receptors |
| 93. What are the D2 Antagonists? | Prochlorperazine, Droperidol, Metoclopramide |
| 94. What is the dose for Prochlorperazine (compazine)? | 5-10mg q 4-6 hours PO/IM |
| 95. What is the dose for Droperidol D2>>H1/5HT antagonist? | 1-2.5mg q 3-6h IV |
| 96. What is the dose for Metoclopramide (reglan) D2 and 5HT3/4 antagonist? | 10-20mg q6h PO or 0.5mg/kg q6h IV |
| 97. What are the indications for D2 antagonists? | Vomiting uremia, radiation, viral gastroenteritis and severe morning sickness in pregnancy (if sufficiently severe) |
| 98. What is the drug of choice of D2 antagonists? | Viral Gastroenteritis |
| 99. What is the mechanism of how Trimethobenzamide (Tebamide) represses CTZ? | mechanism unknown |
| 100. What drug is the most potent antiemetic not having serotonergic, dopaminergic, or histaminergic effects, which means less side effects? | Trimethobenzamide (Tebamide) |
| 101. What is the dose of Trimethobenzamide (Tebamide)? | 250mg tid PO |
| 102. What are the ADR of Dopamine Antagonists? | Extrapyramidal effects, Drowsiness, Hypotension, Restlessness, Diarrhea, Depression |
| 103. What is Cyclizine used for? | Motion Sickness |
| 104. What is Cinnarizine used for? | Motion sickness, vestibular disorders (e.g. Meniere’s disease) |
| 105. What is Promethazine (also an anticholinergic) used for? | Severe morning sickness of pregnany (if absolute essential) |
| 106. What are the Serotonin 5HT3 Antagonists drugs? | Ondansetron, Granisetron, Dolasetron |
| 107. What is the dose for Ondansetron (Zofran)? | 0.15mg/kg IV 15 minutes before chemotherapy, then q4h for 2 doses, 8mg tid PO |
| 108. What is the dose for Granisetron? | 10mcg/kg IV once |
| 109. What is the dose for Dolasetron? | 1mg bid PO, 100mg or 1.8 mg/kg IV |
| 110. What are the 5-HT3 receptor antagonists Odansetron (Zofran) primarly used to treat and prevent? | chemotherapy induced nausea and vomiting (CINV). |
| 111. How is Odansetron (Zofran) given? | It is given intravenously about 30 minutes before beginning therapy. |
| 112. Is Odansetron (Zofran) also effective in controlling postoperative (PONV) and post-radiation nausea and vomiting? | Yes |
| 113. Is Odansetron (Zofran) a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis? | Yes |
| 114. What are the ADR for Serotonin 5HT3 Antagonists? | Headache, Dizziness, Constipation |
| 115. Are Agents in Serotonin 5HT3 costly? | Yes |
| 116. What are the drugs of Anticholinergics/Antihistamines? | Diphenhydramine, Scopolamine, Dimenhydrinate, Meclizine |
| 117. What is the dose for Diphenhydramine? | 25-50mg q4-6h PO/IM/IV |
| 118. What is the dose for Scopolamine? | Patch: 1.5mg q 3days (transdermal) |
| 119. What is the dose for Dimenhydrinate? | 50mg q4h PO |
| 120. What is the dose for Meclizine (antivert)? | 25-50mg q24h PO |
| 121. T/F Antihistamine efficacy is similar to dimenhydrinate but has less side effects. | True |
| 122. T/F Diphenhydramine is Diphenhydramine hydrochloride (Benadryl /Unisom and Nytol as sleeping pills). | True |
| 123. T/F Diphenhydramine is a (OTC) antihistamine/ anticholinergic? | True |
| 124. What are the actions of Diphenhydramine? | antiemetic, sedative, and hypnotic. |
| 125. T/F Diphenhydramine is used for the treatment of extra pyramidal side effects of typical antipsychotics, such as the tremors. | True |
| 126. What drug is used in Dramamine to prevent nausea and emesis? | Diphenhydramine |
| 127. What are the indications of Dimenhydrinate? | Nausea and motion sickness |
| 128. Dimenhydrinate is a salt of two drugs, what are the salts? | diphenhydramine and 8-chlorotheophylline (a chlorinated derivative of the theophylline) |
| 129. What drug is very closely related to caffeine and theobromine (a mild CNS stimulant)? | Theophylline |
| 130. T/F Drowsiness is induced by diphenhydramine, which outweighs the stimulation caused by chlorotheophyllinate, so the desired stimulation insufficient. | True |
| 131. What drug has anticholinergic properties used in very minute doses? | Scopolamine |
| 132. What drug is used in treatment of motion sickness? | Scopolamine |
| 133. What does the patch of Scopolamine do? | It has a slow release of only 330 micrograms (μg) per day. |
| 134. What can the overdose of Scopolamine cause? | Delirium, delusions, paralysis, dangerous elevations of body temperature, stupor and death. |
| 135. What are ADR of Anticholinergics/Antihistamines? | Drowsiness, Dry mouth, Constipation, Urinary retention |
| 136. What drugs are the most effective for nausea and vomiting due to motion sickness? | Anticholinergics/Antihistamines |
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