Intro I and II, Drug Development

Question 1

Define chemical name

Answer 1

specific compound’s structure; long

Question 2

Define generic name

Answer 2

derived from chemical name; shorter-ish

Question 3

Describe schedule I substance and examples

Answer 3

substances with no currently accepted medical use and high potential for abuse

Ex. heroin, LSD, marijuana, MDMA

Question 4

Describe schedule II substances and examples

Answer 4

substances with a high potential for abuse w/ use potentially leading to severe psychological of physical dependence; accepted medical use

Ex. methylphenidate, methamphetamine, oxycodone, morphine, methadone, hydromorphone, fentanyl, cocaine

Question 5

Describe schedule III substances and examples

Answer 5

moderate to low abuse potential compared to schedule II

Ex. anabolic steroids, testosterone, codeine, ketamine

Question 6

Describe schedule IV substances and examples

Answer 6

Schedule IV: lower abuse potential and risk of dependence compared to schedule III

Ex. diazepam, lorazepam, phenobarb, propoxyphene, tramadol

Question 7

Describe schedule V substances and examples

Answer 7

lowest abuse potential

Ex. low dose opioids in cough meds, lamotil, pregabalin

Question 8

Define pharmacokinetics (PK). What is it composed of?

Answer 8

what the body does to the drug

absorption, distribution, metabolism, excretion (ADME)

Question 9

Define pharmacodynamics (PD). What is it composed of?

Answer 9

what the drug does to the body

MOA, dose response, effects, SE

Question 10

Describe absorption, passive diffusion

Answer 10

H2O and water soluble substance and small lipids move w/ concentration gradient

Question 11

Describe absorption, active transport

Answer 11

minerals, some sugars, and most amino acids move against a concentration gradient w/ an input of energy

Question 12

What factors affect distribution

Answer 12

-tissue permeatbility
-BF
-binding plasma proteins
-binding to subcellular components

Question 13

What organ is a major site of drug elimination?

Answer 13

kidney

Question 14

Define clearance rates for excretion

Answer 14

ability of all organs and tissues to eliminate drug or ability of single organ/tissue to eliminate drug

Question 15

Define half-life of excretion

Answer 15

amount of time required for 50% of drug remaining in body to be eliminated

Question 16

Phase I drug metabolism; what happens and what is involved

Answer 16

oxidation (CYP 450) and reduction

polar (water soluble) metabolite often still active

Question 17

Phase II drug metabolism; what happens

Answer 17

conjugation of reactive groups inserted in phase I

large polar metabolite by adding endogenous hydrophilic groups to form water-soluble inactive compounds

Question 18

Components of phase II drug metabolism

Answer 18

Glucuronidation, sulphate, glycine, acetylation, methylation

Question 19

Define bioavailability

Answer 19

amount of substance that enters the bloodstream and is available for the body to use

Question 20

Define bioequivalence

Answer 20

two different versions of a drug that work the same way

Question 21

What are major organs of drug metabolism and excretions?

Answer 21

liver and kidneys

Question 22

What factors affect the variations to drug response?

Answer 22

-disease
-genetics
-age
-diet
-gender
-drug interactions
-environmental
-obesity
-exercise
-cigs/alcohol

Question 23

Define dose response

Answer 23

provides info about dosage range over which drug is effective

Question 24

Define potency

Answer 24

quantity of drug necessary to produce of given effect

Question 25

Define efficacy

Answer 25

maximum response that can be achieved with a drug

Question 26

Define median effective dose

Answer 26

E50

dose 50% of population responds to drug in specific manner

Question 27

Define median toxic

Answer 27

T50

dose 50% of group exhibits AR’s

Question 28

Define median lethal dose

Answer 28

L50

dose causes death in 50% of the group; not used in human trials

Question 29

Define agonist/full agonist

Answer 29

affinity or efficacy

Question 30

Define partial agonist

Answer 30

do not evoke max response and does not fully activate receptor

Question 31

Define antagonist

Answer 31

affinity only (but may have efficacy by inhibiting inhibitory neuron)

Question 32

Define additive effects

Answer 32

2 chemical effects = sum of 2 chemicals taken separately

Question 33

Define synergistic effects

Answer 33

2 chemical effects > sum of separate effect at same doses

Question 34

Define tolerance, dependence, addiction

Answer 34

T: decreased rxn to drug after repeated use

D: person dependent on drug to fx

A: inability to control drug use

Question 35

Describe the 3 main stages of the progress of drug development

Answer 35

-preclinical testing (animal trials provide info about PK and PD, dosage and toxicity)
-human clinical trials
-post marketing surveillance

Question 36

What are the 4 phases of drug development

Answer 36

I: is it safe? PK?
II: does it work?
III: does it work double-blind?
IV: post marketing surveillance

Question 37

Define investigational new drug (IND), new drug app (NDA), FDA

Answer 37

Investigational new drug: a drug that is not approved by FDA

New drug application: app to get approval from FDA

Food and drug admin: approves drugs

Question 38

List the various routes of admin (6)

Answer 38

oral, sublingual/buccal rectal, inhalation, injection, topical

Question 39

Oral vs parenteral route of admin

Answer 39

parenteral skips 1st pass

first pass: drug metabolized BEFORE reaching circulation (goes through digestive system)