Pharmaceutical Chemistry
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What is a drug?
Any substance that alters the biochemical process of the body
What is pharmacology?
The study of the effect of drugs on living organisms
What drugs said to be?
pharmacologically active
What are substances that have beneficial effect on the body said to be?
medicines
What do medicines contain?
a small amount of the active ingredient and other substances such as starch and colouring.
What do most medicines produce?
unwanted side-effects
How do drugs work?
By binding to receptors on the surface of cells
What is a receptor?
part of a very large protein molecule that can interact with a specific, biologically active molecule that occurs naturally in the body.
Decribe how biologically active molecules can interact with receptors.
the active molecule will fit the shape, size and structure of the receptor site.
What two functions can drug have?
to act as a catalyst for a specfic biochemical reactions, or act as enzyme inhibitors by blocking the active site of the enzyme
What does the structural fragment of the drug which confers pharmacological activity consist of?
functional groups which bind to the receptor site
What position must the functional groups on both the drug and receptor site be in?
correct relative positions
What does bonding between functional groups in the active molecule and functioknal groups in the complex protein involve?
weak forces such as hydrogen bonding and weak electrostatic interactions
What happens if the correct molecule binds to the receptor site?
it activates the cell and triggers a biological response within the cell. The active molecule then leaves the site without being chemically changed
What does an agonist do?
interact with a receptor to produce a response similar to the body’s natural active compound
What does an antagonist do?
interacts with a receptor to produce no response because it prevents the action of the body’s natural active compound
What are most medicines and drugs?
complex molecules containing a variety of functional groups. Some of these groups may not be essential for binding to the receptor.
For chemists trying to design new, more effective medicines, what is it useful to know?
the minimum structural requirements for a molecule to be pharmacologically active
What is the structural fragment of the molecule that confers pharmacological activity called?
pharmacophore
How can the pharmacophore be identified?
by comparing the structures of a number of medicines with similar pharmacological activity
How can asthma attacks be releived?
By inhaling a bronchodilator, which widen the airways. The natural substance which performs this function is adrenaline, which is produced at nerve-endings to stimulate muscle activity.
Why can adrenaline not be used for asthma attacks?
it has undesirable side-effects such as increasing blood pressure, heart rate and brain activity
What was designed to be more effective than adrenaline?
salbutamol
Why is salbutamol more effective than adrenaline?
Doesn’t cause the side effects that adrenaline does. It also lasts longers in the body as it is less easily metabolised.