Pharmacology - answer✔the study of drugs and their interactions with living systems
Pharmokinetics - answer✔the study of drug interactions with the body (absorption, distribution,
metabolism, excretion -ADME)
Pharmacodynamics - answer✔the study of drug interaction with their receptors
Receptors - answer✔-The molecular target of a drug
-Think of the actions of drugs as being the result of their interaction with a target receptor
Pro-Drug - answer✔A compound which is not intrinsically active, and is activated by some
metabolic step after administration.
Off-Target Effects - answer✔-Drugs are usually not perfectly specific for one receptor type.
Sometimes they influence closely related receptors (H1 vs H2 receptors)
-Sometimes they influence completely unrelated receptors (H1 receptors vs potassium channels
in the heart)
-Adverse events arise due to effects that are unrelated to the desired mechanism of action of the
drug
Adverse events - answer✔-Undesirable drug effects can vary in severity
-Some off-target effects are mild/benign
-Some are very serious or lethal
Pharmacogenomics - answer✔The genetic background of a patient can significantly affect how
they respond of a drug
Drug Interactions - answer✔-It is very common for one drug/substance to adversely affect the
response to another
How do drugs exert their affect? - answer✔By binding to receptors in our bodies and triggering
a functional change
What field of pharmacology is important when considering drug safety and development? -
answer✔Pharmacokinetics
What was the antihistamine used in the 1980s and 90s to treat allergies? - answer✔Terfenadine
What was the initial thought of the function of terfenadine? - answer✔Terfenadine was a
specific h1 receptor antagonist - 'anti-histamine'
How does terfenadine really work? - answer✔Terfenadine is absorbed, passed through into the
liver which is where it is metabolized into fexofenadine which then blocks the H1 receptor
What is fexofenadine? - answer✔The antagonist of the H1 receptor which is derived from the
metabolism of terfenadine
What is terfenadine considered as? - answer✔a pro-drug
First pass metabolism - answer✔The amount of the drug that is processed or eliminated during
its first time through after it is absorbed in the gut and through the liver before it is delivered
through the circulatory system
What happens when terfenadine is not fully metabolized? - answer✔-The unprocessed
terfenadine will cause undesired effects on the heart.
-Terfenadine is a powerful blocker of certain proteins (hERG ion channels) that control electrical
activity and beating of the heart
What off-target effects of terfenadine can lead to? - answer✔-Lethal cardiac arrhythmia
(torsades de pointes)
-Death
What enzyme in the liver is involved with drug metabolism? - answer✔CYP3A4
What are risk factors involving the liver when taking terfenadine? - answer✔-Patients with
diminshed liver function, or taking certain antibiotics (erythromycin family) or antifungals were
at risk
-Drinking grape juice (CYP3A4 inhibitor)
What are the risk factors involving the heart when taking terfenadine? - answer✔-Some patients
will carry mutated versions of the genes encoding susceptible ion channel 'off-targets' in the
heart
-Some mutations will make them more sensitive to inhibition by terfenadine
What was the solution involving the use of Terfenadine? - answer✔To administer the
metabolite of terfenadine, which does not have cardiotoxic effects
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