PHARMACODYNAMIC PRINCIPLES

in terms of drug receptor theory, when no ligand is present the equilibrium lies far to the right and a few on the left

this is a decrease in total receptor number in the cell due to endocytosis and subsequent degredation of the receptors

this agonist can bind to and activate the receptor, but produces a sub-maximal effect

which is the dose that kills 50% of subjects?

a drug that acts on the same receptor as an agonist but produces an opposite effect of an agonist

a drug binds to a different region of the receptor

in a quantal dose-response relationship, the % of population affected increases as the dose is increased

graded doses of a drug given to an individual usually result in a lesser magnitude of response as the dose increases

quantal dose-reponse plots outcome occurence un a population against the drug dose

this agonist produces maximal efficacy

if the dose difference between ED and LD is low then the drug has a ______ safety margin

agonists have a higher affinity for _______ and hence, produce a response

cells are more sensitive to a hormone or neurotransmitters

occurs because of long term administration of an antagonist

ED₉₉ - 10mg dose is effective in _____ of the population

what drugs is considered a full agonist?

there is a graded dose response in a(n) ________ and a quantal dose-response in a(n) _________

what equation is this?

receptor desensitization can be characterized as decreased responsiveness with repeated or chronic exposure to agonist

which is the dose that produces desired effect in 50% of the population?

what possesses affinity and intrinsic efficacy?

few antagonist drugs can act as agonist on one receptor and antagonist on another receptor

if the safety margin is 900% it is a ________ drug

what dose-response relationship is this?

this relationship describes a drug effect as either present or absent (binary)

what has affinity but lacks intrinsic efficacy?

competitve antagonism is irreversible

for constitutively active receptors a proportion of receptors adopt 'R' conformation in the absence of any ligand

what equation is this used for?

a dose response can be ______ or _______

caused by long exposure to agonists

a drug binds to the same site as an endogenous ligand

what dose-response relationship is this?

which is associated with functional super sensitivity to subsequent antagonist administration

this is known as increased expression of receptors on the cell membrane

this is the relationship between the chemical structure of a molecule and its biological activity

this relationship describes a drug effect which increases in proportion to increasing drug dose

non-competitive antagonists are irreversible no matter the concentration

what is this associated with?

what drug is considered a partial agonist?