Pharmacodynamics I Flashcards
Pharmacodynamics
How drugs interact with receptors
Pharmacokinetics
hint: ADME
The lifetime of a drug and how it interacts with the body: Absorption Distribution Metabolism Excretion
Pharmacogenomics/Pharmacogenetics
how genetics affects how a patient responds to a drug
- plays a role in how harmful/beneficial a drug may be for the patient
Receptors
What the drug binds to (what the drug targets)
ex. H1 histamine receptor
Prodrug
An inactivated form of a drug
- it needs to be changed/metabolized by the body into its active form in order to interact with the target receptor
Off Target Effects
When a drug affects another receptor than the one it was intended to affect
- some affect closely related receptors (ex. H1 & H2 receptors)
- some effects are wild/unexpected (ex. H1 receptor v.s K+ ion channels in the heart)
Adverse Events
When a drug has harmful/non-desired effects
T/F: All adverse events are unexpected.
False! Some can be expected as a ‘side effect’ due to the drug’s mode of action. Others can be unexpected (ex. off-target effects).
NNT and NNH stand for _______ and __________, respectively.
Numbers Needed to Treat
Numbers Needed to Harm
- both help quantify how beneficial a drug is
Isn’t pharmacology so cool??!
not bias, I promise….
Yes, it’s SUPER COOL. You better have gotten this flashcard right. Keep going, you got this!
Agonist
a drug/hormone/something that binds to a receptor and influences its activity
T/F: Antagonists are able to bind to receptors and create a biological effect themselves.
False! Antagonists cannot generate bio. effects on their own.
What are the properties of a steroid hormone when its receptor is inside the cell?
- receptor is inside cell –> steroid must be membrane permeable; hydrophobic
- if not lipid soluble, requires a transport carrier
Mode of action of an intracellular receptor? (steroid hormone receptor)
- binds to a LBD (ligand binding domain)
- this displaces HSP (heat shock protein) OR some other chaperone
key point: leads to activation of transcription/translation of protein
Better explanation –> check diagram in lec. notes
T/F: Steroid hormones result in slow biological effects but are long lasting.
True!!
What are 4 types of receptors that allow for a signal transmission?
1) Intracellular Receptors (we see these with steroid hormones)
2) G-protein coupled receptors
3) Transmembrane receptors (TKRs)
4) Ion Channels (Ligand Gated/ Voltage Gated)
What is a heat shock protein?
A heat shock protein is a type of molecular chaperone that covers the DNA binding domain in a intracellular receptor until a steroid binds to the ligand- binding domain.
Why are G- proteins called heterotrimeric?
There are three different subunits that make up a G- protein. The alpha, beta, and gamma subunits.
What are the 3 different types of G alpha sub units? What are they and what do they activate/inhibit?
Gs (activated adenylate cyclase) (AC)
Gi (inhibits adenylate cyclase) (AC)
Gq (activates phospholipase C (PLC)
Explain the signal transduction for how Adenylate Cyclase (AC) is activated and inhibited.