General Principles of Pharmacology part 3

Question 1

define biotransformation

Answer 1

change in chemical structure caused by living system

Question 2

another name for biotransformation

Answer 2

drug metabolism

Question 3

what is the produce of biotransformation called

Answer 3

metabolite

Question 4

where does biotransformation primarily occur

Answer 4

liver

Question 5

produrg

Answer 5

activate an inactive drug

Question 6

general characteristic of metabolite

Answer 6

more pole
more water soluble
excreted faster than parent drug

Question 7

what are 4 results of biotransformation

Answer 7

produg
inactivate an active drug (main)
active drug to active metabolite
active drug/metabolite to toxic metabolite

Question 8

what are 2 general classes of biotransformation reactions, generally what do they do

Answer 8

Phase 1 - add Hydrogen or Oxygen

Phase 2 - add cofactor

Question 9

what reactions occur in phase 1

Answer 9

oxidation
reduction
hydrolysis

Question 10

what reactions occur in phase 2

Answer 10

conjugation or synthesis

Question 11

location of microsomal enzymes

Answer 11

smooth endoplasmic reticulum

Question 12

microsomal enzymes are oxidative enzymes are also known as

Answer 12

mixed function oxidases (MFO)

P450 (CYP)

Question 13

CYP cytochrome P450 ezymes are what type of oxidase

Answer 13

terminal oxidase

Question 14

for microsomal enzymes, what characteristic must the substrate have

Answer 14

lipophillic

Question 15

microsomal enzymes have what kind of acitivity

Answer 15

inducible

Question 16

genetic polymorphism

Answer 16

genes can be different for people

Question 17

where are nonmicrosomal enzymes located

Answer 17

cytosol
mitochondria
blood (esterases)

Question 18

are nonmicrosomal enzymes induciable

Answer 18

generaally not

Question 19

name 6 factors that affect rate of biotransformation

Answer 19

enzyme activity inducers/inhibitors 
age
liver 
nutritional 
genetics 
gender

Question 20

name 2 primary routes of drug excretion

Answer 20

biliary

renal

Question 21

name secondary routes of excretion

Answer 21

sweat, saliva, breast milk, exhalation

Question 22

define drug elimination

Answer 22

drug is no longer able to produce a pharmacological effect and can include excretion

Question 23

where does central vein blood go from liver

Answer 23

general circulation

Question 24

where are 2 places drugs can go from portal vein in liver

Answer 24

bile canaliculus

central vein

Question 25

drugs that go through bile canaliculus in liver go where

Answer 25

small intestines

Question 26

drugs going from bile canaliculus to S.I., have what characteristics

Answer 26

increase molecular weight

Question 27

explain enteroheptatic cycling

Answer 27

Bile canaliculus
Small intestines
portal system - lipophilic
back to liver

Question 28

what does enterheptatic cycling do to drug

Answer 28

prolongs interaction of drug

Question 29

the amount of drug filtered in glomerular kidney depends on what

Answer 29

filteration rate
molecular rate
degree of binding to plasma protein

Question 30

can weak acids and weak bases be filtered in glomerular kidne

Answer 30

yes

Question 31

what are the 2 bidirectional transport systems for drugs in proximal nephron

Answer 31

anionic form

cationic form

Question 32

prominent direction in proximal portion of nephron

Answer 32

peritubular fluid into proximal tubular cells then in lumen

Question 33

how should drugs be administered to infants due to the proximal nephron

Answer 33

modified dosage

anionic and cationic transport system not fully developmed

Question 34

what type of transport occurs in proximal tubule of nephron

Answer 34

active

Question 35

distal nephron: amount of unionized drug that undergoes non-ionic back diffusion is dependent on

Answer 35

P.C.
equilibrium constant
[H+] of tube and luminal fluid
urine flow rate

Question 36

what is the exchange of H and Na in distal tubule

Answer 36

H in (makes urine acidic)
Na out

Question 37

When H enter distal tubule what does it do to the weak acid? then what process does it do

Answer 37

it unionized weak acid

non-ionic back diffusion

Question 38

When H enter distal tubule what does it do to the weak bases?

Answer 38

it ionizes weak bases