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PMCOL 200 EXAM LATEST UPDATE
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PMCOL 200 EXAM LATESTUPDATE
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 is important when developing a drug? - Answer They are safe, effective, and used
,appropriately
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
What are the types modes of signal transmission? - Answer 1. Intracellular Receptors
, 2. Tyrosine Kinases
3. Ion Channels
4. G-Protein Coupled Receptors
Where are intracellular receptors located? - Answer inside the cell
What drugs target intracellular receptors? - Answer Hydrophobic lipid soluble
ex: steroid hormones
What is the mode of action of intracellular receptors? - Answer 1. Binding to the LBD
(Ligand Bind Domain) of a steroid hormone receptor
2. Displacement of HSP (heat shock protein)/chaperone
3. Expose DNA recognition domain
4. Activation of transcription of target genes
What type of onset does intracellular receptors have and how long do they last? -
Answer Slow Onset
Long Lasting
Not rapidly reversible
What does activation of G-protein receptor promote? - Answer GDP-GTP exchange of
the heterotrimeric G-protein
What is G-alpha bound to? - Answer Bound to the receptor and bound to GDP
What does the G-alpha unit have? - Answer GTPase activity that acts like a molecular
'timer' to terminate the signal
How does G-alpha terminate the signal? - Answer By hydrolyzing GTP back to GDP form
What can G-proteins do while active? - Answer They can influence 'effector' proteins
that alter cellular activity
What is G-beta-gamma bound to? - Answer The plasma membrane
What type of effect does the G-beta-gamma protein have? - Answer A direct effect that
can activate downstream effectors
How are G-protein coupled receptors categorized? - Answer Based on the subtype of
the G-alpha that is associated
What effects of having different G-alpha subtypes can do? - Answer Different subtypes
can influence different signaling cascades via effects on Adenylate Cyclase (AC) or
Phospholipase C (PLC)
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