Medicinal Chemistry: The Basis of Drug Discovery

This week was far more interesting to me due to the focus shift to chemistry. I am learning that I definitely prefer chemistry over biology. Learning about specific chemical reactions in the body and the structure of drugs was something that interests me. Learning about new drugs and learning their effects on the body is also incredibly interesting. I also enjoyed this week and learning about how drugs are metabolized and how they exit the body. My question this week is about an example that was shown in one of the videos. It showed Codeine being metabolized to morphine. does the codeine cause the effect or does the metabolite morphine cause it?

When someone refers to metabolism in medicinal chemistry terms, they are not referring to the number of calories burned at rest, or the use and replacement of organic material in the body. The are referring to the methods of how a drug is removed from the body. When a drug is taken by someone, it enters the bloodstream and is transported to other part of the body. Then, the body want to get rid of it, as its a foreign substance the body doesn't recognize. It does so by one or more chemical reactions to make it less possible to mix in with the plasma and then easier to filter by the kidneys.  How the drug is metabolized and what the body changes the initial substance to is very important for the safety of drugs. If the drug metabolizes to something extremely dangerous and toxic, and doesn't  metabolized again to something else that drug cant be given. this just another thing that must be considered and another challenge that must be overcome.

Week 10 video 1 -phase 1 metabolic reactions specifically oxidation -sp3 hybridized carbons includes dealkylation and alcohol oxidation -sp2 hybridized carbón mostly alkenes and aromatic rings in videos mostly aromatic rings -heteroatoms (non carbon) -starting in nitrogen dealkylation oxidation -visualized as a removal of a carbon group from a nitrogen atom -used with small alkyl groups, and carry prefix nor- -same can happen on oxygen atoms, the carbon Group is removed -involves small alkyl groups and uses prefix desmethyl -alcohol oxidation is very common -primary alcohols oxidize to a carboxylic acid -secondary alcohols to a ketone -sp2 hybridization ex benzene -when nitrogen are oxidized form a n-oxide -sulfur also is very easily oxidized -forms sulfoxide which can turn to sulfones Video 2 -phase 1 covers oxidation, reduction, and hydroleses -reductions are the opposite of oxidations -ketones/aldehydes to alcohols -the ketone of warfarin is reduced to provide ...

My reaction to the learning was interest. I realized that the majority of this class has been math, which I find boring. However, learning about metabolism was very interesting. The topics i find interesting is the real chemistry and biology, not so much the math and graphs. I also learn the things that I want to learn better. The part about the graphs and the concentration limits was somewhat interesting, and the equations and calculations part was pretty boring. My question for this week is about overdosing. When someone overdoses, what is happening in their body? why does that much of a substance make your body stop functioning?

When creating a drug that will be administered orally, the window between the minimum required for a proper effect and the maximum to avoid adverse effects must be considered. When this drug is swallowed, the concentration in the plasma rises, then as metabolism begins to take effect, it decreases again. This continues for each time the drug is taken, slowly adding up until the max begins to plateau. The goal is to always be above the minimum efficacy and below the maximum amount to not feel adverse effects. Another consideration is to the half-life of the drug. The goal for the half-life is 8 hours, and changes can be made to the molecule to effect the half-life. When talking about metabolism, most people think about calories. When talking about drugs, however, it has to do with the process of getting the drug out of the body. This can be done through two phases. In phase one, the single molecule undergoes a chemical change that makes it easier for the kidneys to filter the blood. In ...