Pharmacodynamics Flashcards
What is pharmacodynamics
the effect of a drug on the body
What are the 4 drug receptor types
Ligand-gated ion channels
G-protein-coupled receptors
Kinase-linked receptors
Nuclear receptors (DNA coupled)
Attributes of ligand-gated ion channels
Milliseconds
Hyperpolarization or depolarization
Nicotinic ACh receptor
Attributes of G-protein-coupled receptors
Seconds
Crosses membrane 7 times
Muscarinic ACh receptor
Attributes of Kinase-linked receptors
Hours
Joins together for an intracellular response/ binds to impact a different receptor
Cytokine receptors
Attributes of nuclear receptors
Hours
occurs intracellularly requires a lipophilic ligand
Estrogen
What is a receptor
a component on or in a cell that a substance can bind to
primary location where drugs bind to have their effect
What does a drug target
Receptors
Enzymes
Non-human cells
What are all the different drug-receptor interactions
Specific Selective Agonist Antagonist Competitive antagonist Non-competitive antagonist Partial agonist
What is specificity
drug only binds to one type of receptor
Ex: A not B
What is selectivity
drug prefers to bind to one subtype of a receptor but can still bind to others
Ex: B1 mostly, B2 sometimes
What is an agonist
OPTIMUS PRIME DRUG
drugs that occupy receptors and activate them
What is an antagonist
MEGATRON DRUG
drugs that occupy receptors and block receptor activation by agonists
What is a competitive antagonist
Agonist and antagonist compete to bind to the receptor
highest concentration wins
What is a non-competitive antagonist
Near or irreversible binding to receptor
More than one attachment point on the receptor for both the agonist and antagonist so the activation is blocked
What is a partial agonist
Doesn’t fit the receptor perfectly but well enough
Lower dose=agonist effect
Higher dose=antagonist effect
Where do opioid receptors and ligand reactions occur
mu and kappa receptors
What is a dose response curve based on
individual or homogenous population
What is Emax
the maximal response from a drug
all receptors are saturated
may cause toxicity
What is ED50
the effective dose to get 50% of the expected response
AKA Kd or EC50