Basic principles of Pharm lecture 1

Question 1

Agonist

Answer 1

Binds to a receptor and activates a response you would normally see from the native ligand bound to the receptor (can have greater or lesser effect than native ligand)

Question 2

Antagonist

Answer 2

inhibits response of receptor (inhibits native ligand from binding)

Question 3

Most prevalent protein in our plasma?

Answer 3

Albumin

Question 4

pharmacodynamics

Answer 4

effect of drug on body

Question 5

pharmacokinetics

Answer 5

effect of body on drug (how does the body break down the drug? how does the drug change?) (Absorption, Distribution, Metabolism, Elimination)

Question 6

pharmacogenomics

Answer 6

how genome effects the drug

Question 7

list 3 main types of bonds from strongest to weakest

Answer 7

Covalent, Electrostatic (ionic, hydrogen, van der waals), and Hydrophobic (lipid soluble drugs)

Question 8

list 3 main types of bonds from most to least specificity

Answer 8

Hydrophobic (lipid soluble durgs), Electrostatic (ionic, hydrogen, van der waals), and covalent

Question 9

Stereoisomerism

Answer 9

2 Drug with exact same chemical components but are mirror images of each other. They have a central Carbon.

Question 10

Racemic mixtures

& example

Answer 10

A mix of 2 stereoisomers (ex: R-Ketamine and S-Ketamine)

Question 11

Orthosteric drugs

Answer 11

Bind at the same active site of a receptor as the native ligand

Question 12

Allosteric drugs

Answer 12

Bind somewhere other than the active site of a receptor causing a conformational change. (can be agonist or antagonist in nature)

Question 13

non-specific receptor binding…

Answer 13

…is linear (see slide 30 on Basic Principles of Pharmacology powerpoint)

Question 14

Specific receptor binding…

Answer 14

…is logarithmic (it rises quickly and then levels off because specific receptors can eventually become saturated or used up). (see slide 30 on Basic Principles of Pharmacology powerpoint)

Question 15

Drug concentration response curve (drug concentration vs drug effect):
Emax-
EC50-

Answer 15

Emax- the max effect the drug will produce

EC50- the dose where we see 50% of the effect

Question 16

Drug concentration response curve (drug concentration vs receptor-bound drug)
Kd-
Bmax-

Answer 16

Kd- the concentration in which 50% of receptors are bound

Bmax- total saturation of all receptors (rarely achieved)

Question 17

what is the difference between a competitive/orthosteric inhibitor and an allosteric inhibitor

Answer 17

Competitive/orthosteric inhibitors bind to the same active site as the agonist and can be over powered. Allosteric inhibitors bind to a different place on the receptor and can’t be over powered.