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1

what are the usage of these types of drugs:
1.therapeutic
2.diagnostic
3. prophylactic

1. thera=to treat certain conditions
2. diag=to assess current state of health
3. prophylactic=to prevent disease state

2

what are pharmacodynamics
-2 things

entails the biochemical and physiological effects of drugs (what a drug does) AND their mechanism of action (how the drug has an effect and the correlation of drug action w/ their chem structure)

3

what are the 6 drug targets

1. receptors
2. ion channels
3. enzymes
4. transporters (symporters/antiporters)
5. nucleic acids
6. idiosyncratic targets
-ions, GI contents, etc

4

what is an agonist? what are the 2 types

activates the target
full=mimics response of natural ligant
partial=lower efficacy than full agonist

5

what is an antagonist?
how can it bind

neutral: prevents the target from signalling
-can bind competivielty (to active site) or non competivetly (somewhere to prevent active site being accessed)

6

what is an inverse agonist

reduces basal receptor activity below baseline

7

what does the dose responsive curve (DR) give information about

potency and efficacy
-exsists both for therapeutic and side effects of a drug

8

what is potency
what is efficacy

potent=the more potent the less drug you need
-related to concentration of a mg, NO EFFECT

efficacy=the more efficacious, the greater the maximal effect
-related to maximal therapeutic effects

9

what is ED50?
what is LD50?

ED50=dose needed to be effective in 50% of indiv
LD50(TD50)= dose needed to kill 50% of subjects, T=toxic

10

what is the therapeutic index
what is the ideal number for this

LD50/ED50
ideally want this ratio to be infinite
wnat ED50 < < < < < < LD 50

11

what is the therapeutic window

concentration range wehre drug is effective w/o side effects
-large TI is good and means

12

what does a large therapeutic index mean

a much greater dosage is required for toxic or lethal effects compared to the dosage for therapeutic benefits

13

what is pharmacokinetics

examines the processes affecting the fate of drugs in the body

14

what are the steps to pharmakokinetics

absorption
distribution
metabolism
elimination

15

what are route of administration of drugs

oral
parenteral (IV, IM, SC)
sublingual (under tonue)
inhalation
topical/transdermal patch
rectal

16

what are the advantages and disadvantages to oral delivery

advantages
-easy
-high compliance
disadvangtage
-first pass metabolism
-may be modified by digestive enzymes or stomach acid

17

what is bioavailability

amount of administered drug that actually enters the circulation

18

what affects bioavailabilty

absorption
first-pass metabolism

19

what are the key factors of drug distribution

-chemical structure of drug (ease of transport through membrane)
-blood flo w
-plasma protein binding (albumin)

20

what cna albumin affect

distribution
metabolism
elimination

21

what is aparent volume of distrubution

dose/ [drug]

22

what kind of avd does blood only have?
blood+tissues?
fat?

blood only=low AVD
blood+tissues=high AVD
fat=very high AVD

23

wehre does most metabolism happen

liver

24

what is the first pass effect

most oral drugs undergo processing/metabolism in the liver prior to having access to its target

25

what is phase 1 and phase 2 or metabolism

phase 1: oxidation by CYP450 enzymes
-results in active metabolite
phase 2: conjugation

drug=> phase 1=> derivative=> phase 2

26

how does elimination happen

1. kidney=> urine through glomerular filtratoin ( bile=> feces
3. sweat
4. respiration

27

what is elimination kinetics affected by

metabolism and elimination rate

28

what is first order elimination kinetics
what is zero order

first: constant t half life, takes 4-5 half lives to remove drug from body
-plasma [drug] decreases exponentially w/ time
-most drugs

zero: no half life, rate of elimination constant
-constant amount of drug metabolized per unit of time
-eliminate faster
-larger dosage=longer time

29

what is clearance

the volume of blood or plasma filtered per unit of time to account for the drop of drug concentration

30

how can clearance be measured

not measured directly, determined by drop in concentration with time