what are the two main domains considered when studying drugs?
pharmacodynamics
pharmacokinetics
what is pharmacodynamics?
the action of drugs on the body, and the effects they produce
what specific things are considered in pharmacodynamics?
the mechanism of action, specific receptors the drug binds to, and what effectdrugs have on cells
what is pharmacokinetics?
the study of how drugs are absorbed, distributed, metabolized, and excreted by the body
what is pharmacokinetics in simple terms?
the action of the body on the drug
pharmacogenomics is much more recently developed
what is pharmacogenomics?
how genes affect a person's response to drugs, and how genes impact the effect of drugs
pharmacogenomics is important in personalised medicine
how is pharmacodynamics plotted?
drug concentration (mM) on the x axis, and the effect of the drug on the y axis
in an instance where the effect of a drug (i.e., muscle contraction) is measured against drug concentration, what would explain a plateau?
the musclecannotcontract past a certain point, no matter how increased the drug concentration is
plateaus occur at highconcentrations
what term is used to describe the plateau in a pharmacodynamics plot?
100%effect
the effect of a drug at 50% in a pharmacodynamics plot (i.e., dosage at 50%) gives a measure of the potency of a drug
therapeutic/toxic action is dependent on the amount of drug at the site of action
the majority of drugs bind to receptors, but they can also block them
why do some drugs block the reuptake of neurotransmitters?
to make them accumulate in the synaptic cleft
what are agonist drugs?
drugs that stimulate specific receptors that they bind to
what happens after an agonist binds to a receptor?
mimics the same effect of the endogenousmolecules that would normally act on the receptor
what does endogenous mean?
originating from within an organism
how does adrenaline work during the fight-or-flight response
epinephrine (adrenaline) binds to beta-adrenergic receptors, which increases the heart rate
adrenergicagonists act as agonists to adrenaline by binding to the same beta-adrenergic receptors and producing the same response (increased heart rate)
G-protein coupled receptors are activated by small molecules that bind to it, and activate the G-protein
give an example of something a G-protein can do once activated
stimulate an enzyme and produce a certain response
adenylatecyclase transforms ATP into cAMP
G-protein commonly stimulates adenylatecyclase, increasingcAMP, which can open/close channels
what determines whether an increase in cAMP will open or close channels?
the type of cell/tissue
tyrosine kinase is an important mediator of the cellsignallingcascade
tyrosine kinase receptors are still attached to the cell membrane
tyrosine kinases utilise ATP and become activated via phosphorylation
once tyrosine kinases are activated, they produce a certain effect (i.e., opening and closing channels)
tyrosine kinases are enzymes that transfer a phosphate group from ATP to the tyrosine residues of specific proteins inside a cell
tyrosinekinase functions as an "on" or "off" switch in many cellular functions
antagonists prevent the effect of endogenous agonists on receptors