Consider This 10.11 COX-2 Inhibitors
In 1992 researchers discovered that there were two separate types of COX enzymes, COX-1 and COX-2. The COX-2 enzyme is responsible for the production of the prostaglandins that regulate inflammation, pain, and fever, thereby reducing these symptoms. The COX-1 enzyme catalyzes the production of the prostaglandins responsible for maintaining proper kidney function and for keeping the stomach lining intact. Aspirin blocks the activity of both COX enzymes so it has the unwanted side effects of stomach aches and bleeding.
After this discovery, new "super aspirins" that would affect only the COX-1 enzymes were developed. Touted as drugs that would cause fewer gastrointestinal problems, they entered the market with great fanfare. They became instant blockbuster drugs, selling in the billions of dollars per year. Use the Web to find the names of two of these drugs. Why have they disappeared from the pharmaceutical radar screen? |
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Consider This 10.13 Drugs by Chance
Modern methods of drug discovery involve structure-activity relationship studies, computer modeling, etc. Sometimes side effects of a drug may open the door for its usefulness in treating other illnesses. Screening programs where chance is built into the methodology. There are many examples where a new drug was discovered by "chance." Use the resources of the Web to find an example of a drug that was discovered by unusual circumstance. |
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Consider This 10.14 Friend or Foe?
Make two lists of drugs for each of the two broadly classified groups–those that bring about a desired physiological response and those that kill foreign invaders. Propose three drugs for each list, using examples not given in the text. |
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Consider This 10.15 3D Drugs
See for yourself how drug molecules appear in three dimensions. a. Select several compounds from the list of top 50 selling pharmaceuticals and examine their three-dimensional structures. How do these computer representations differ from the structural formulas of drugs shown in this chapter? b. What advantages do the computer representations have over two-dimensional drawings? What are their limitations compared with "real" molecules? Are there any disadvantages? |
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Consider This 10.18 Chiral Switch
In principle, the strategy of chiral switching should afford a therapeutic advantage for the single isomer drug over the racemic mixture. But is this always the case? Use the Web to identify one drug (other than Ritalin) that has made the chiral switch and report on the relative merits of the single isomer versus the racemic mixture. |
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Your Turn 10.19 Structural Similarities of Steroids
Here are pairs of steroids whose structures are given either in the text or in Figures Alive! for this chapter. a. Identify the structural similarities in each pair.
| estradiol and progesterone | corticosterone and cortisone | | cholic acid and cholesterol | prednisone and cortisone | | estradiol and testosterone | | b. Write the chemical formula for five of the drugs in part a. |
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Consider This 10.25 Citizen Petitions
The Washington Post article mentioned in the Section 10.10 listed the hot-selling antidepressant drug Wellbutrin XL as an example of the misuse of a citizen petition. Search the Web using keywords such as "citizen petition," "generic drug," "pharmaceutical company," and "FDA." Find one petition and research it. Explain the nature of the petition, who filed it, and why. Then state your opinion. Was the petition filed because of a bona fide safety issue, or was it designed to stave off generic competition? |
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Consider This 10.26 Using Common Sense
Many people are of the opinion that it is best to take only the medicines indicated for a particular illness. Yet some companies selling OTC preparations seem to throw in everything but "the kitchen sink," hoping to give their product some sort of "value-added" feature. Check the contents of several cold remedies found at your local drug or grocery store (or go online to find the same information). In particular, look at several cough remedy preparations. Do you find the use of both guaifenesin and dextromethorphan in one product? List the names of the products that do, and then explain why a product containing both of these medicines makes no sense. |
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Consider This 10.29 Low Potential for Abuse?
The sedatives diazepam (Valium) and alprazolam (Xanax) are currently listed as schedule IV drugs, indicating that they have a low potential for abuse. Search the Web for information on addiction to these powerful sedative drugs. Do you agree with the current scheduling? Explain. |
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Consider This 10.30 Is Your State Going to Pot?
The legality of medical marijuana seems to shift like dunes of sand. Use the Web to determine your home state's current position on the use of marijuana for medicinal purposes. Is this position in conflict with that of the U.S. federal government? Be sure to have up-to-date information on the federal government's position. Do you agree or disagree with both your home state and the U.S. government on this issue? List the sources of your information. |
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Consider This 10.32 Who Is Right? Wrong?
Use the Web to investigate several sites that discuss the abuse of OxyContin. Also find sites that describe the legal woes that Purdue Pharma has encountered. Do you think that the drug manufacturer bears some responsibility in this matter? Write an essay taking one side or another or present your stance in a class discussion. |