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Pharmacology Exam 2
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cytokine receptors ligands
growth hormone
epo
interferons
Cytokine receptor cascade
protein tyrosine kinase non intrinsic
JAK binds non covalently to the receptor and tyr are phosphorylated
STAT binds each JAK
STATs dimerize and regulate transcription of genes
Regulation of ion channels
phosphorylation
endocytosis
verapamil
inhibits voltage gated Ca2+ channels in heart muscle
reduces arrhythmia
reduces blood pressure
Propranolol
binds B-adrenoreceptors
reduces blood pressure
EC50
concentration required to achieve 50% of the drugs maximal effect
ED50
dose of a drug required to produce 50% of a drug's maximal effect
Potency
amount of drug needed to produce 50% of the drug's maximal effect
depends on drug affinity (Kd)
depends on efficiency of the drug receptor interaction response
Potency of drug on graph
left = most potent
right = least potent
low Kd
high affinity
Drug on a chart with maximal efficacy
tallest line on the chart
Clinical effectiveness depends on
potency (ec50)
maximal efficacy
ability of drug to reach the relevant receptors
is effectiveness or potency more desired?
effectiveness > potency
____ the potency of a drug should be stated in dosage units in terms of particular outcomes.
therapeutic purposes
Relative potencey
ratio of equi-effective doses that may be used in comparing one drug to another
Maximal efficacy
limit of the dose response
hight of the line on the graph
Therapeutic efficacy
effect that can be achieved in the patient
depends on drug-receptor interactions
Quantal dose effect plots
shaded boxes indicate the frequency distribution of doses required to produce a specified effect
ED50
Median effective dose at which 50% of individuals exhibit the specified quantal effect
TD50
Median Toxic Dose is the dose required to produce a particular toxic effect in 50% of the animals.
LD50
Median lethal dose is the dose that causes death in 50% of the animals
If the ED50 of two drugs for producing a specified quantal effect are 5 and 500 mg then:
the first drug can be said to be 100 times more potent than the second for that effect
measure which relates the dose of a drug required to produce a desired effect to that which produces an undesired effect
therapeutic index
therapeutic index is usually defined as
ratio of TD50 to the ED50
idiosyncratic drug response
individual exhibit an unusual response to the drug
When responsiveness diminishes rapidly after administration of a drug, the response is said to be
tachyphylaxis
Four mechanisms which may contribute to variation in drug responsiveness among patients
alteration in concentration of dose that reaches the receptor
variation in concentration of an endogenous receptor ligand
alteration in number or function of receptors
changes in components of response distal to the receptor
Multi drug resistance genes
MDR
major mechanism by which tumor cells develop resistance to anticancer drugs
drugs are ____ rather than specific
selective
Measurement of selectivity of a drug
compare binding affinities
compare ED50s for different effects of a drug in vivo
selectivity is usually considered by separating effects into two categories
therapeutic effects vs. toxic effects
Author
Rx2013
ID
39181
Card Set
Pharmacology Exam 2
Description
Drug receptor concepts II and III
Updated
2010-10-03T01:23:53Z
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