Quiz 1 - Pharmacodynamics

Front 1

Agonist

Back 1

Stimulates and activates a receptor

Front 2

Antagonist

Back 2

Stops agonist from stimulating receptor

Front 3

EC50

Back 3

The concentration of drug that causes 50% of the maximal effect. It is a measure of drug POTENCY.

(50% Effective Concentration)

Front 4

Emax

Back 4

Efficacy Maximum, at which it is assumed all the receptors are occupied by the drug.

(At this point, higher concentrations of drug produce no effect)

Front 5

Full Agonist

Back 5

Can replicate the binding response of the body's physiological ligand

Front 6

Partial Agonist

Back 6

Unable to produce maximal effect, even if bound to all receptors.

Front 7

Inverse Agonist

Back 7

Stabilizes receptors in their inactive form

Front 8

Antagonist

Back 8

A ligand that can bind to a receptor and block or inactivate it, thus reducing agonist activity.

Front 9

Competitive Antagonist

Back 9

An antagonist that binds and prevents agonist from binding, inactivating the receptor.

- Shifts dose response curve of agonist to the RIGHT. (Because it takes a higher concentration of drug to get half of the Emax - lowered potency!)

Front 10

Allosteric Antagonist

(Non-Competitive Antagonist)

Back 10

Binds to a site on the receptor that is different than the agonist binding site, and causes a conformational change in the receptor, so the agonist can no longer bind.

Front 11

The ___________________ measures the relative safety of a drug, and gives a window of treatment.

Back 11

The therapeutic index measures the relative safety of a drug, and gives a window of treatment.

Front 12

How is the TI (therapeutic index) calculated?

Back 12

The Toxic Dose in 50% of population, divided by the Effective Dose in 50% of the population.

Front 13

PharmacoDynamics

Back 13

The effect of the DRUG on your body.

Front 14

Pharmacokinetics

Back 14

The physiological response your body has to a drug.

Front 15

KD

Back 15

Binding Affinity

The concentration of drug required to bind 50% of the receptors.

Front 16

Bmax

Back 16

Binding Maximum

The total number of receptors.

Front 17

Four Common Types of Receptors are:

1.

2.

3.

4.

Back 17

Four Common Types of Receptors are:

1. Ionotropic (ie: ligand gated)

2. Metabotropic (ie: G-PCRs)

3. Kinase Linked (both a receptor & enzyme)

4. Steroid

Front 18

Ligand

Back 18

An agent that binds to a receptor

Front 19

Spare Receptors

Back 19

Receptors that are leftover (spare!) because maximal effect (Emax) has been reached without all the receptors being utilized.

Front 20

With a constant blockade, a receptor may ______-regulate. This is usually by ______________ the number of receptors.

Back 20

With a constant blockade, a receptor may up-regulate. This is usually by increasing the number of receptors.

Front 21

With a constant stimulation, a receptor may ______-regulate. This is usually by ______________ the number of receptors.

Back 21

With a constant stimulation, a receptor may down-regulate. This is usually by decreasing the number of receptors.