Lecture set 4 Flashcards
Drug dose and clinical responses in patients
Time Action Curve
Two important questions for every drug
How quickly is the drug going to act
How long will the drug react
We cannot see toxicity on a Time-action curve
We can know how quickly the drug acts by seeing the onset of effect
We know how long it will react by looking between the MEC for adverse and MEC for desired response which gives us our therapeutic window
Quantal vs graded drug response
Quantal
Used to measure all or none responses
It responds to the max or none at all
Ex. take a hypnotic to go to sleep you’re either asleep or you’re not
Binary
Threshold
Minimum effective dose of the drug which evokes an all or none pharmacological response
Graded
Time action curve
Response is graded not all or none
Showing progressively increasing effects
EX heart rate
Center of symmetry which is our ED50
Similarities of Graded and Quantal
Similarities
Sigmoid in nature
Potency and selectivity
Differences
Graded - progressive increases of effect
Quantal - all or none
ED50
The dose required to produce the stated effect in 50% of the population
LD50
The dose required to produce death in 50% of the population
Therapeutic index or ratio
The relative safety of a drug expressed as LD50/ED50
The larger the ratio the greater the relative safety
Calculate and compare the therapeutic index between drugs
TI= TD50/ED50 (TD50 also can be LD50)
Describe the factors that modify the effects of drugs
Drug tolerance
Condition of decreasing responsiveness
Opioids famous example
Concentration at site of action
Physiological variables
Pathological factors
Genetic factors
Desensitization
biological factors as well
- age
-sex
Compare and contrast drug disposition tolerance and pharmacologic tolerance
Drug tolerance
2 ways to develop tolerance
Decrease in effective concentration of the agonist
Drug disposition
Metabolic tolerance
Downregulation of receptors
Change in receptor affinity
Apply cross-tolerance to disease management
Tolerance to one drug in a class and occurs with other drugs in a class
EX: tolerance to vicodin means tolerance to morphine
Understand the basis for on target and off target adverse effects
?
Deconvolute physiological response in multicellular/ multi receptor context