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23 Cards in this Set

  • Front
  • Back

Define structure activity relationship

The steric arrangement of the drug molecule with the receptor and how that contributes to specificity of drug action

Name 5 properties of receptors

1. Specificity?


2. Expected to bind a normal body component


3. May have subtypes


4. Can be desensitized


5. Propagate signal via changing ion transport (iontrophic) or activating second messengers (metabotrophic)

Name 3 types of noncovalent bonds

1. Ionic bonds


2. Hydrogen bonds


3. Hydrophobic bonds (Van der Waals)

Define threshold

The drug concentrated need to elicit an effect

Define max efficacy

The drug concentration beyond which no increase in concentration will lead to a higher percentage of effectiveness

Define partial agonist

A drug not causing a maximal response

When can summation and potentiation/synergism be determined with drugs?

When the doses are less than maximally efficacious and receptors remain open to be occupied

Define surmountable antagonism

Competitive antagonism: A blocks the effect of B at B's usual threshold and range of effective doses; but an increase in B (shift B's curve to the right) will overcome the effect of A

Define Insurmountable antagonism

Noncompetitive antagonism: A decreases the effectiveness of B and no increase in B's concentration can lead to a situation where maximum efficacy is restored (curve shape changes and efficacy is decreased)

Define Therapeutic Index

LD50/ED50




**Always have this one**

Define Margin of Safety

LD01/ED99




**May not always have this one**

What are some advantages (3) of dose-response curves?

1. Identification of drug properties (intrinsic activity, maximal efficacy, threshold, range of therapeutic and toxic doses, risk-benefit)


2. Comparison of agonists, partial agonists for efficacy and potency


3. Studies of drug interactions (how does an antagonist affect an agonist)

What are some pitfalls (3) of the dose-response curve?

1. Low-dose extrapolations are hard to do


2. Only one response can be determined at a time


3. Toxicity is not necessarily the same as lethality

Elimination includes:

Biotransformation to inactive druge + excretion

What are two aspects of cell membranes that affect drug absorption?

1. Membrane composition


2. Membrane permeability

Name 5 ways that drugs cross membranes. What are the 2 most likely methods?

1. Filtration


2. Diffusion (concentration gradient important)


3. Facilitated diffusion (non-energy requiring carrier)


4. Active transport


5. Phagocytosis




** Filtration and diffusion are most likely**

Name some aspects of the drug that contribute to absorption.

1. Concentration gradient


2. Size (MW, Protein binding)


3. Formulation (vehicle of drug)


4. Lipid-water (o/w) partition coefficient (solubility)


5. Drug ionization (solubility)


6. Protein binding in blood (more protein binding will decrease availability for absorption)

What form of ionization is necessary for a drug to diffuse across a membrane?

Unionized

Ionized drugs are considered to be _______

Ion trapped

If a drug is acidic, then the drug will be unionized when the tissue pH is ________ than the drug's pKa.

Less

If a drug is a weak base, then the drug will be unionized when the tissue pH is ______ than the drug's pKa.

Greater

Pharmacokinetics includes:

Movement of the drug through the body as a concentration versus time function

Absorption, Distribution, Biotransformation, Excretion


Pharmacodynamics includes:

The mechanism of the drug action especially at the cellular level