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Midterm

Midterm Questions Durst.docx

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Department
Biopharmaceutical sciences
Course
BPS1101
Professor
Tony Durst
Semester
Fall

Description
BPS 2110. Sample questions. Question 1. Which area of the following areas pharmaceutical industry holds the most promise for new drugs in the next ten years? Support your choice. - New antibiotics are needed because bacteria are becoming resistant, and not many companies invest into making new antibiotics because they generate low profit - Drugs that are used for pain are always needed, so this is a good area to get involved in. - None of the drugs made today for dementia actually treat it, so this is a good field to focus in. - New cancer drugs are needed as new cancers are being discovered. - Personalized drugs are the future because people respond differently to different substances - Stem cell research is huge - New vaccines will always be needed because viruses change each year. Question 2. A tremendous need and opportunity exists for developing new drugs to slow down rate of decline of patients suffering from dementia eg, Alzheimers disease. Discuss the issues which made progress in this area slow at this time. What breakthrough(s) is (are) needed to change the situation? The drugs developed for Alzheimer’s disease do not cross the blood-brain barrier. Also, alzheimer’s disease couldn’t be predicted in a patient until symptoms started to occur, so it is hard to develop a drug that will cure alzheimer’s disease because it is hard to tell what the source of the disease is. It was later discovered that genetics can tell a lot about a predisposition to developing alzheimer’s disease – alzheimer’s genome project. From studying the genetics, you can prevent the disease better. Question 3. Give the names and headquarters country of three of the top ten pharmaceutical companies in the world. 1. Pfizer (USA) 2. Johnson&Johnson (USA) 3. Hoffman-Laroche (Switzerland) 4. Novartis (Switzerland) Question 4. Describe briefly the mode of action of Aspirin and explain why its action as an anti-inflammatory agent is accompanied in many patients by gastrointestinal bleeding. Aspirin is a drug that inhibits the formation of prostaglandins, which involves the enzyme COX. This enzyme has two variants – COX1 and COX 2, where COX1 mediates the formation of prostaglandins involved in important bodily functions such as the renewal of the stomach and esophagus lining, and COX2 is associated with inflammation. When aspirin is taken by the patient, both the enzymes are inhibited so that on one hand all inflammation is reduced, but the stomach and esophagus lining formation is also inhibited causing gastrointestinal bleeding. Question 5. COX2 inhibitors were initially expected to act as anti-inflammatory agents without the typical side effects associated with Aspirin [ASA] and the other NSAIDs such as Ibuprofen sold as Advil or Motrin. Explain the basis of this expectation. It was expected that if only the enzyme COX2 was inhibited and not COX1, that you could take the drug to reduce inflammation without suffering from gastrointestinal bleeding because COX1 would still be active to renew the lining. However, when the drug only inhibited COX2 activity, it increased the patient’s risk of developing colon cancer and was taken off the market. Question 6. Knowing the structure of lead structure published by the Dupont company, DuP697, and suggest two additional compounds that you would expect to have significant COX-2 vs COX-1 selectivity. Your compounds cannot have a sulfur containing ring since such compounds would obviously infringe on the Dupont patent. The compounds have to be similar to DuP697 in size to be able to fit in the COX-2 receptor to inhibit it but too big to fit in the COX-1 inhibitor. The structure can be altered by using a nitrogenous 5-membered central ring, and by changing the substituents on the aromatic rings from SO2CH3 to SO2NH2 or CF3 Question 7. Generic companies produce drugs whose patents have expired. In order to obtain permission from Health Canada to sell a particular drug what key property of the generic drug show compared to the originally approved drug. The drug must be bioequivalent. They must have the same active ingredients and must have equivalent bioavailability. Question 8. a) What key questions are addressed in a Phase 1 Clinical Trial? In a phase II Clinical trial? In a Phase III Clinical trial?
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