action
Ibuprofen inhibits the cyclooxygenase enzyme.
This is the (action/effect) of the Ibuprofen drug.
effect
Ibuprofen relieves pain & fever and reduces inflammation.
These are the (actions/effects) of the Ibuprofen drug.
Drug action
The mechanism by which a drug produces an effect
Drug effect
The biological response after a drug is administered
subtherapeutic, therapeutic/beneficial, harmful
Drug effect may be:
toxic & lethal
two types of harmful effects of drugs
receptor-mediated, nonreceptor-mediated
Drug action may be:
receptor
a specialized macromolecule involved in cell signaling that binds a ligand
protein or glycoprotein
nature of receptors
enzyme-linked receptor
receptors with a kinase domain
G-protein-coupled receptors (GPCRs)
largest family of receptors
guanine nucleotide-binding protein
G-protein
Ion channel receptor
modulated the passage of ions and hydrophilic molecules
ligand-gated, voltage-dependent
types of ion channel receptor
ligand-gated ion channel receptor
opens in response to a chemical signal/ligand
voltage-dependent ion channel receptor
opens in response to voltage, i.e. when the membrane gets depolarized
transcription factor receptor
receptors for fat-soluble signaling molecules
cytosol
transcription factor receptors are located in the ___ and migrates to the nucleus after binding with the ligand
transcription factor
what is the receptor class of the steroid hormone estrogen?
ionic bond
formed by the attraction between 2 ions of opposite charge
ionic bond
the most commonly occurring bond
hydrogen bond
arises from the ability of a proton (H+) to accept an electron pair from a donor (e.g. oxygen) & another donor (oxygen or N)
van der waals
form a very weak bond between dipoles or induced dipoles
covalent bond
tight and practically irreversible
covalent bond
rare during drug-receptor interactions except in toxic situations
ionic bond, hydrogen bond, van der waals
the principal bond forces involved in drug action
20-40°C
at what temperatures do the principal bond forces become easily reversible?
50-100 kcal/mol
What amount of energy is required to break covalent bonds?
cell signaling
relates to cell communication and the intracellular responses generated in response to drugs and endogenous ligands
reception
during this process, a chemical message/ligand binds to a cell surface receptor
transduction
a cascade of reactions that elicit cellular response
signal transduction
a mechanism by which cell surface receive information & amplify this information through action of second messengers
second messengers
molecules produced in response to ligand-receptor binding that translate the extracellular signal into a response that may be further propagated or amplified within the cell
response
may vary from activating a gene or an enzyme, or rearranging the cytoskeleton
neutralization reactions, nonspecific perturbation of cell membrane, binding with small molecules and ions (chelation)
non receptor-mediated drug action
enzyme-linked, G-protein-coupled, Ion channel
cell-surface receptors
transcription factor receptors
intracellular/cytoplasmic receptors