Basics

Question 1

The branch of medicine concerned with the uses, effects and modes of action of drugs is called what?

Answer 1

Pharmacology (toxicology is concerned with dosages)

Question 2

How the body acts on a drug is called what?

Answer 2

Pharmacokinetics (ADME)

Question 3

How the drug acts on the body is called what?

Answer 3

Pharmacodynamics (usually receptors)

Question 4

What is an agonist?

Answer 4

Drug or natural ligand that activates the receptor. Sometimes selective, sometimes not

Question 5

What does an antagonist do?

Answer 5

Interferes with agonist by binding to the receptor without activating it. Typically shifts dose-response curve to the right. Often competitive

Question 6

What does an allosteric activator do?

Answer 6

Binds receptor at a separate site from the agonist and potentiates its effect

Question 7

What does an allosteric inhibitor do?

Answer 7

Binds receptor at a separate site from the agonist to decrease its affect. Non competitive and often reversible

Question 8

Rank the types of agonists from greatest to leasts response

Answer 8

Full agonist > Partial agonist > Antagonist > inverse agonist

Question 9

The effective concentration for 50% of the total response is called what?

Answer 9

EC50

Question 10

The concentration required to bind 50% of receptors is called what?

Answer 10

Kd

Question 11

Competitive inhibition affects the _________ for a max response while non-competitive inhibition affects the __________

Answer 11

concentration, max response

Question 12

The greatest effect a drug can elicit is called the ________ while the beginning of an effect is called the ________

Answer 12

Plateau, Threshold

Question 13

What are 3 types of drug-receptor interactions?

Answer 13

1-Additive (1+1=2)
2-Synergistic (1+1=5)
3-Antagonistic (1+1=1/2)

Question 14

What are two additional forms of antagonists?

Answer 14

• Chemical (does not involve receptor)

- Physiological (involves regulatory pathways with different receptors)

Question 15

The number of receptors required to reach maximum response is called?

Answer 15

Efficacy

Question 16

The relative concentration of two or more drugs to produce the same drug effect is called what?

Answer 16

Potency

Question 17

How is therapeutic index calculated?

Answer 17

Toxic dose/Therapeutic dose= Therapeutic index

*bigger number means there is a bigger window of dosage. Also true of margin of safety

Question 18

What are the 3 main ways to administer drugs parenteral? (not by way of intestine or G.I. tract)

Answer 18

1-Intravenous (very fast)
2-Intramuscular (prompt absorption, large volume possible)
3-Subtunaeous (adsorption less rapid, smaller volume)

Question 19

What are the 3 main ways to administer drugs enterally? (by way of intestine or G.I. tract)

Answer 19

1-Buccal or sublingual (fast absorption)
2-Oral (most common and convenient, 30 minutes till effect)
3-Rectal (less absorption, alternative to other administration options)

Question 20

What are 3 other ways to administer drugs other than parenteral and enteral?

Answer 20

1-Inhalation (very fast, within 5 minutes)
2-Topical (apply to a surface)
3-Transdermal (15 min onset, slow and sustained release)

Question 21

A substance that brings about a change in biologic function through chemical actions is a?

Answer 21

Drug

Question 22

The subset of drugs used for therapeutic benefit are called?

Answer 22

Medicine

Question 23

Chemicals not synthesized in the body are called?

Answer 23

Xenobiotics

Question 24

What are 4 factors that affect absorption?

Answer 24

1-Route of administration
2-blood flow
3-Drug characteristics
4-Cell membrane characteristics

Question 25

What two chemical properties of drugs are very important for absorption?

Answer 25

- Lipid soluble or water soluble | - Size of molecule (small go more places)

Question 26

What are two things that affect the bioavailability of a drug?

Answer 26

1-dissolving of drug by GI tract 2-destruction of drug by liver *intravenous administration results in 100% bioavailability

Question 27

The apparent space in the body available to contain a drug calculated through volume distribution using what equation?

Answer 27

Volume of Distribution=Amount of drug in body/Concentration of drug

Question 28

What equation is used to determine half-life using Volume of distribution?

Answer 28

T1/2=0.693 Vd/Cl

Question 29

The rate of process of elimination of a drug is measure by clearance using what equation?

Answer 29

Clearance= Rate of elimination/Concentration of the drug

Question 30

What are two families of Drug transporters?

Answer 30

1-Solute Carrier Transporters (OCT's and OAT's) | 2-ATP binding cassette transporters

Question 31

Assuming 1st order kinetics, how many half lives does it take to eliminate 95% of a drug?

Answer 31

4.5 half lives

Question 32

Constant amount of drug eliminated is ____________ where as elimination proportional to concentration is _________

Answer 32

Zero order, first order

Question 33

What are the two stages of metabolism?

Answer 33

Phase I Phase II *not necessarily in that order

Question 34

Purified liver endoplasmic reticulum containing two types of oxidases are called?

Answer 34

Microsomes

Question 35

What are the two main types of mixed function oxidases found in microsomes?

Answer 35

- P450 reductase (NADPH-cyp450-oxireductase) | - P450 (Cyp450)

Question 36

Phase I of hepatic metabolism includes what?

Answer 36

- oxidation, reduction, hydrolysis | * if the phase I metabolite is hydrophilic enough it is excreted

Question 37

Phase II of hepatic metabolism includes what?

Answer 37

Making the drug more hydrophilic through rxns such as glucuronidation, glutathione conjugation, and acetylation

Question 38

The study of underlying genetic factors in drug response is called what?

Answer 38

Pharmacogenomics