Lecture 1: intro

Question 1

What is a mechanism of action?

Answer 1

a cell signaling system or process that is changed/impacted by the way a drug interacts with a target molecule

Question 2

what is a ligand

Answer 2

drug

any substance that brings about a change in biological function through its chemical actions.

Question 3

what is a receptor

Answer 3

target molecule

a macromolecule (target molecule) in the membrane or inside of the cell that binds with a drug molecule.

Question 4

what can a drug act as when it binds to a receptor

Answer 4

an agonist (or activator)
or
an antagonist (or inhibitor)

Question 5

what are the criteria for drug (ligand) attachment to target molecule (receptor)

Answer 5

size, electrical charge, shape, atomic composition

Question 6

describe the fit and effect of natural chemicals, agonist drug, and antagonist drugs at receptor site

Answer 6

Before Drug (natural chemical)- fits into receptor site and produces normal cellular activity

Agonist Drug- fits into receptor sites BETTER and produces enhanced cellular activity

Antagonist drug- fits into receptor site like a blocker and creates no cellular response, inhibits activity

Question 7

How do drugs interact with receptors?

Answer 7

By means of chemical forces or bonds

Question 8

Strong bonds =

Answer 8

covalent

Question 9

ionic bonds =

Answer 9

electrostatic

Question 10

weak bonds

Answer 10

hydrophobic

Question 11

what determines affinity for a ligand to bind

Answer 11

the strength of the bond it holds- the stronger the bond the more attraction it has for the receptor site

Question 12

What is drug selectivity

Answer 12

degree to which a drug acts on a given site relative to other sites
—how well a drug works at one site compared to another

Question 13

Relatively nonselective drugs:

Answer 13

affect many different tissues or organs (e.g.,atropine- muscle relaxer- eyes, digestive tract, etc)

Question 14

Relatively selective drugs:

Answer 14

affect targeted areas (e.g., NSAIDs such as aspirin andibuprofen only targets areas of inflammation)

Question 15

Highly selective drugsaffect

Answer 15

a single organ or system (e.g.,digoxin- heart, increases pump efficiency for congestive heart failure, sleep aids -brain)

Question 16

Define poisons

Answer 16

drugs that have almost exclusively harmful effects.
- warfarin- used as a blood thinner but is also in rat poison so they bleed to death

Question 17

what kind of drugs are synthesized within the body

Answer 17

hormones

Question 18

Define toxins

Answer 18

poisons of biologic origin, synthesized by plants or animals.

Question 19

Inorganic poisons

Answer 19

poisons such as lead or arsenic.( consist of metallic and non metallic compounds)

Question 20

what chemical shape are more than half of all useful drugs

Answer 20

chiral- 4 unique attachment sites

Question 21

How are drugs normally sold/ what are the common ideas of them

Answer 21

• often sold as racemic mixtures of enantiomers (S and R isomers)
• often one enantiomer is more active than the other
• often one is more susceptible than the other to drug-metabolizing enzymes
• as result, duration of action of one enantiomer may be quite different than the other
  -one usually active while the other is inactive

Question 22

what can’t drugs do

Answer 22

drugs cannot change the basic nature of biologic functions or create new functions
- cant exceed normal biological speed of doing things

Question 23

what can drugs speed up/slow down

Answer 23

drugs can speed up or slow down biochemical reactions but can only affect at the rate that existing biologic functions proceed
- after the maximum dose of a drug it may not help

Question 24

how will a drug reach its site of action from administration site

Answer 24

a useful drug must have the necessary properties to be transported from its site of administration to its site of action (whether it is oral, rectal, gel- must have correct chemical properties to make it into blood or path it needs to go to)

Question 25

what does a practical drug need to reach its target site and be productive

Answer 25

a practical drug should be inactivated or excreted at a reasonable rate so that its action will have enough effect once it is in its target area ( should be inactive until it reaches place you want it to occur)

Question 26

Pharmacodynamics is

Answer 26

determines the amount and variation of drug responses on the body - the actions of the drug on the body (MoA, therapeutic effect, toxic effect).

Question 27

what does pharmacodynamics involve

Answer 27

receptor binding, post receptor effects, and chemical interactions

Question 28

how are many drugs classified

Answer 28

based on the basis of their primary receptor affinity

Question 29

Examples of pharmodynamics

Answer 29

- receptors, effectors - dose-response curves - agonists, antagonist - signaling mechanisms - receptor regulation

Question 30

Pharmacokinetics (PK or ADME) describes

Answer 30

the effects of the body on drugs. - It determines the onset, duration, and intensity of a drug’s effect.

Question 31

examples of Pharmacokinetics (actions of the body on the drug)

Answer 31

- movement of drug in body - absorption - distribution - metabolism - elimination

Question 32

What is biodisposition

Answer 32

a term used to describe the processes of metabolism and excretion.

Question 33

PK and particular patients

Answer 33

- PK aids in the choice and administration of drugs for particular patients - Patients PK depends on patient related factors (age, genetics, etc) and chemical properties -individual physiology can affect PK

Question 34

what can be used to predict the PK parameters in populations?

Answer 34

patient related factors

Question 35

PK-PD chart

Answer 35

Question 36

Black box warnings are

Answer 36

meant to draw attention to a medication's serious or life-threatening side effects or risks

Question 37

What are indications

Answer 37

reason to use a specific drug saying that the use of a drug is for a specific disease " diabetes is an indication for insulin"

Question 38

What are contraindictions

Answer 38

condition that serves as a reason NOT to take a certain medication (would cause harm to patient) cautions

Question 39

off-label

Answer 39

When the indication, dose, or form of a drug is not FDA approved to treat an illness or symptoms -might use if all other options exhausted- get consent and document everything !!

Question 40

Chemical name

Answer 40

name given when drug is first discovered - describes the atomic or molecular structure of the drug. -usually too complex for general use

Question 41

Generic name

Answer 41

(official name) - is assigned, in the United States, by an official body—the United States Adopted Names (USAN) Council. -off patent

Question 42

Brand name

Answer 42

(trademark name) - company name drug - gives company proprietary rights to drug ( doesn't last forever, once expires then can be sold by other companies by different names off the shelf) -under patent protection -often related to drugs intended use (lopressor lowers blood pressure)

Question 43

once a drug is FDA approved what is it given

Answer 43

a generic (official) name and a brand (trademark) name

Question 44

when a drug is off patent how can it be marketed

Answer 44

by brand or generic name

Question 45

if a company files for approval to market an off patent drug what are the conditions

Answer 45

the company must use the same generic name but can create their own brand name - FDA must agree to proposed brand name to eliminate prescription mistakes due to similar/same drug names

Question 46

What is a prototype drug

Answer 46

a drug(s) that typifies the most important characteristics of the group of drugs.