Week 0 + 1

Question 1

Drug Development Part 1

Answer 1

In-vitro and In-Vivo testing:
Basic Research, early discovery, pre clinical
Meant to establish drug safety and efficacy

Question 2

Drug Development Part 2

Answer 2

Human testing: Clinical Development
Phase 1: 10s of people
Phase 2: 100s of people
Phase 3: 1000s of people

Question 3

Drug Development Part 3

Answer 3

Data Review=> FDA Review

Question 4

Drug Development Part 4

Answer 4

Surveillance: Post-market monitoring

Question 5

What protein allows SARS-CoV-1 to infect humans that some animals do not have?

Answer 5

ACE2R Receptor

Question 6

What enzyme, if blocked, would inhibit viruses from infecting humans?

Answer 6

RNA dependent polymerase

Question 7

What is Log P

Answer 7

Measure of lipophilicity of a molecule. Known as the octanol/water partition coefficient. Octanol is a representative of a lipophilic environment. Log P correlates to drug absorption and distribution in the body

Question 8

To classify a drug as soluble in water. The log P must be?

Answer 8

Less than 0.5

Question 9

Lipinski’s rule of Five

Answer 9

Provides a basis of whether a chemical compound is likely to become a drug.

1. A molecular weight under 500
2. Fewer than 10 H-bond acceptors
3. Fewer than 5 H-bond donors
4. A C log P value less than 5

Question 10

Define a hydrogen bond donor (HBD)

Answer 10

A functional group that provides the hydrogen required for a hydrogen bond (When a hydrogen is bonded to another element)

Question 11

Define a hydrogen bond acceptor (HBA)

Answer 11

Functional group that provides the electron-rich atom required to interact with a hydrogen in a hydrogen bond (A good hba has to be electronegative and have a lone pair of electrons) Such an Oxygen having extra electrons

Question 12

Percentage of drugs approved in clinical trials

Answer 12

0.01%

Question 13

Percentage of drug trials that become approved via passing each step?

Answer 13

Less than 10%

Question 14

What is the Investigational New Drug Application (IND)

Answer 14

A document for drug trials

Question 15

Phase 1 of drug trials

Answer 15

Tests healthy volunteers (unless for cancer pts, then phase 1 studies pts with cancer)
Absorption, distribution, metabolism, or excretion of drug
Side effects
Dosage and best route of administration determined
Approx. 70% of drugs move to the next phase

Question 16

Phase 2 of drug trials

Answer 16

Studies efficacy and side effects
Given to pts w/ disease or condition
Provides additional safety data
Approx. 70% of drugs move to next phase

Question 17

Phase 3 of drug trials

Answer 17

Determine efficacy and monitor adverse reactions
Provides most of the safety data
Common side effects become more present
More likely to determine long-term or rare side effect
Approx 25-30% of drugs move to the next phase

Question 18

Phase 4 of drug trials

Answer 18

Determine safety and efficacy

Carried out once drug is approved by FDA

Question 19

define pharmacokinetics

Answer 19

movement of the drug in the body

defined as the study of time course of Absorption, Distribution, Metabolism, and Excretion (ADME) of drugs

Question 20

define pharmacodynamics

Answer 20

power of the drug in the body

Question 21

what is Absorption heavily dependent on

Answer 21

route of administration

Question 22

Distribution

Answer 22

process of drug travelling to numerous locations in the body to and from the blood and various tissues

Question 23

Metabolism

Answer 23

where drug is modified, usually by specialized enzymatic systems

Question 24

Metabolism- major site of metabolism?

Answer 24

liver

Question 25

Metabolism- define biotransformation

Answer 25

alteration of chemical structure of drug

Question 26

Metabolism- Drug metabolism converts _______ compounds into more readily excreted ________ compounds

Answer 26

lipophilic, hydrophilic

Question 27

Excretion

Answer 27

process of a compound being removed from the body

Question 28

major site for excretion?

Answer 28

kidney

Question 29

define endocytosis

Answer 29

xport of macromolecules

Question 30

Fick’s law

Answer 30

rate of diffusion across membrane is proportional to the diff in concentration on each side of the membrane
*calculated by flux

Question 31

Define Flux

Answer 31

Flux: Mass/Area*Time =>
J= K*D/h * (Co - Ci)
J= flux
K= partition coefficient
D= diffusion coefficient
h= thickness of barrier
Co - Ci= concentration gradient

Question 32

Henderson Hasselbach Equation:

Answer 32

Acid: pH= pKa +log ({A-}/{HA})
Base: pH= pKa +log ({B}/{BH+})

Question 33

facilitated diffusion

Answer 33

energy not required

solute flow from high to low electrochemical potential with help of a transport molecule

Question 34

active transport

Answer 34

energy required

solute flows from low to high electrochemical potential