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32 Cards in this Set
- Front
- Back
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When was it mandated in the USA to have 2 categories of drugs? (OTC vs Prescription)
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1951
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What are the three main aspects in the Durham Humphrey amendment to the 1938 FDA act?
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- Proof of effectiveness
- Cosmetics regulated - Food standards |
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List the steps in drug discovery
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- Identify targets
- Find leads - Develop leads - Pick a candidate - Make a drug - Formulate - Toxicology - Clinical Trials - Regulatory approvals |
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What is the purpose of the Kaplan-Meier plot?
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Show the efficacy of a given drug vs the placebo.
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Lipinski observed that most drugs are _____, ______ and _______.
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Relatively small, fat soluble, simple organic compounds.
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List the three aspects of Lipinski's rule of five.
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1. No more than 5H bond donors.
2. No more than 10H bond acceptors. 3. Molecular weight no more than 500 kDa. |
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The spanish fly cantarrhid is _____
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an irritant
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What drug is extracted from the periwinkle?
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Vincristine, an anti-cancer drug.
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Every year, US prescription drug sales grow by ___%
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about 5.1%.
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How do you calculate the number of years required to double the sales of a given product?
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70/(% increase/year) = number of years
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The FDA catalogues drugs in a variety of different ways. List them.
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New molecular entity (1), New derivative (20, New formulation (3), New combination (4), already marketed drug products if the patent is expired (5) and new use for a drug product (6).
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What is the name of the market for non-medicinal components of medication?
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Excipient market.
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What is the most widely used pain-relieving medication in the world? How many tablets are sold every year?
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Aspirin, with 58 billion tablets a year.
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When were willow trees used for the first time?
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Around 2200BC by the Sumerians, who knew it had a therapeutic effect against joint pain.
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What was Reverend Edward Stone's reasoning in the reintroduction of the powdered willow bark?
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The Doctrine of Signatures. Since willow trees grew in mushy areas where fevers were known to develop, then they must have a function in treating them.
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What is the active comound of the willow bark and when was it isolated?
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Salicin. 1829.
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Who isolated salicyclic acid?
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Pirra, 1838.
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Salicylic acid, a compound used in the 1800s against pain, fever and inflammation, was too much of an irritant. Who synthesized a compound that was less of an irritant, when, what was the name of the compound?
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Hoffman, 1897. Acetylsalicylic acid.
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How many companies have the right to sell acetylsalicylic acid as aspirin in the USA?
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Any company can do that. Bayer lost patent rights to ASA and to the name Aspirin.
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How many companies have the right to sell acetylsalicylic acid as aspirin in Canada?
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One, Bayer.
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Discuss the effects on ASA on Thromboxane A2 and the consequences of that in regards of heart disease.
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Thromboxane A2, a type of prostanglandin involved in clotting, is inhibited by ASA. Through inhibition of TA2, clotting decreases, which is beneficial in someone suffering from blood clots.
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Is there a benefit in taking ASA daily if you are not at risk of heart disease? Discuss.
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No. It is of benefit only if you have already suffered from a heart attack, or if you are at risk. Moreover, daily ASA consumption may lead to major bleedings.
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Discuss the anti-cancer properties of ASA against colon cancer, if any.
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There are no direct effects of ASA on colon cancer. Since ASA increases the chances of major rectal bleedings, patients rush to the ER where an unrelated colon cancer is discovered.
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What is salicylism?
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Disorder due to excessive consumption (12-25 tabs) of ASA. Leads to tinnitus.
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How does ASA work?
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It blocks the conversion of arachidonic acid into prostaglandins, which are normally the nerve stimulators to signal for pain. ASA blocks this conversion by inhibiting the cyclooxygenase enzyme (COX).
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What are the two main roles of prostaglandins?
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Lead to feeling pain, trigger inflammation.
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Why is it important not to take ASA in the last 3 months of pregnancy?
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Prostaglandins promote uterine contractions.
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True or false : Both ASA and Acetaminophen/Paracetamol are effective against inflammation.
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False. Acetaminophen/Paracetamol isn't.
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True/False : Acetaminophen is associated with liver failure.
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True. It is the number one cause of poisoning associated with OTC meds.
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In North America, what is the most sold OTC pain reliever?
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Acetaminophen, followed by ASA, Ibuprophen, Naproxen Sodium respectively.
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Name the roles of the Cox-1 and Cox-2 enzymes.
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Cox-1 has protective functions on the stomach, Cox-2 catalyzes the conversion of arachidonic acid into prostaglandins.
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Name a drug that is specific for the Cox-2 enzyme, and state why it is specific.
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Celebrex. It has a tail that prevents it from binding to Cox-1.
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