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10 Cards in this Set

  • Front
  • Back

Pharmalogic receptor

Where drug action takes place


The receptor site is complementary to the shape of a drug molecule



two types of studies that have been used to discover such receptors

Studies of drug structure and the pharmacologic activity produced




Studies of relationships bw drugs that produce a response and that that oppose the action




Studies of the selective binding of radioactive-labeled drugs to cell membranes

Describe the formation of a drug receptor complex

Due to the formation of a chemical bond (usually temporary) bw the drug and the receptor to activate an effector mechanism of some kind.

Structure-activity relationship (S-AR) and explain how changes in the structure of a drug can change the specificity of response

Better understanding of the spatial nature of the site permits the design of drugs with molecular shapes that precisely fit a pharmacologic receptor at a specific location.

General concept of dose-response relationships

Is the proportional change in drug response to a changing drug dosage.


At some dosage level all pharmacologic receptors are complexed by the drug.

Median effective dose (ED50) of a drug

Is the dose that produces a specified intensity of effect in 50% of individuals.


Some people may be sensitive and respond to a low dose. Some people may be more resistant and need a higher dose.




Simply the midpoint value .

Drug potency


VS


Efficacy

Refers to the relative ability of a drug to evoke a particular response at a given dosage.


(Drug A reponds at low dose more potent then Drug B that responds at higher dose)


VS


Ability of a drug to produce a desired therapeutic response is its effectiveness, or intrinsic activity.


Toxicity

overdose

Median Lethal dose (LD50)

Dose that produces lethal effects in one-half of a test population.

Explain the concept of therapeutic index (T.I) and relate this to the safety of a drug.

ED50 and LD50 curves for the same drug. The distance on the graph bw the doses producing the desired therapeutic effect(ED50) and the lethal effect(LD50) represents the safety margin for the drug. This margin is T.I