Quantitative Analysis of Drug-Receptor Interactions Flashcards
Cardinal Rule in Pharmacology
Cant create a new drug effect
Can only alter cell fxn or increase/decrease existing drug effect
Clinical vs Pharmacological effect
Clinical effect can be observed
3 most important properties of a drug
SEQu: Safety, Efficacy, Quality
Properties of a Drug receptor
Stereospecificity/Stereoselectivity
Reversibility
Saturability
2 Consequences of Up regulation
Hyperreactivity and Supersensitivity
How can you obliterate the effect of a competitive antagonist
Increase the concentration of the agonist
3 Types of Bonds Involved in DRI
Covalent - usually irreversible
Electrostatic - most common
Hydrophobic - in highly lipid soluble drugs
Graph of Graded Response Curve using Arithmetic Scale?
Hyperbola, has ceiling effect
Graph of Graded Response Curve using Log scale? Plot Elements?
Sigmoid Curve;
Slope, Max Effect, Log dose, Potency, Variability
Variability implies
…using a range of doses
due to differences in age, weight, etc
What is the response curve for:
Temporary competitive antagonism?
Pseudo-irreversible competitive antagonism?
Response curve shifted to the right, EC(50) is increased; (THE COBRA)
Response curve is depressed or tilted, depression of maximal response; (LYING BUDDHA)
Efficacy VS Potency
Efficacy - effect that is not dose dependent; up-down movement of graph, up being higher
Potency - effect is dose dependendent, left right movement of graph, nearer Y axis being higher
Potency
Drug concentration/dose required to produce 50% of that drug’s max effect
Importance of potency begins when ease of administration ends
Quantal Response Curve:
Variability depends on?
Gives info regarding?
Frequency o response or how many indivs in the popl’n will respond to the drug dose
Info on the margin of safety to be expected
Explain the Counterfeit incorporation mechanism
Purine and pyrimidine analogs being incorporated into Nucleic Acids thereby cheating the rapidly multiplying cancer cells
