drugs

Question 1

Tmax

Answer 1

time to get to peak concentration

Question 2

C max

Answer 2

peak concentration

Question 3

increasing rate of absorption will

Answer 3

make the drug reach peak conc faster

Question 4

what will increasing dose do

Answer 4

increase peak conc- C max

but wont increase time- T max

Question 5

the area under the conc/time curve =

Answer 5

amount of drug that reaches systemic circulation

and biologics available

Question 6

factors affecting oral bioavailability

Answer 6

• formulation- tablet, capsule, systemic
• ability to pass membrane
• gastrointestinal effects- gut motility, food, illness
• first pass metabolism

Question 7

what effects membrane permeability

Answer 7

SIZE

solubility

ionisation

IONISED DRUG DON’T CROSS MEMBRANE

Question 8

lipid soluble drugs will…

Answer 8

pass right across membrane

Question 9

first pass metabolism

Answer 9

metabolism of a drug before it reaches systemic circulation

often causes problems for oral route

Question 10

protein bound drugs are…

Answer 10

inactive

Question 11

protein binding is ____ and effected by

Answer 11

reversible

effected by:

renal failure

pregnancy

other drugs

Question 12

prodrugs are activated by

Answer 12

metabolism

Question 13

what type of compounds can be excreted

Answer 13

water soluble

Question 14

lipid compounds after use get

Answer 14

reabsorbed

Question 15

main stages of phase 1 metabolism

Answer 15

hydrolysis

oxidation

reduction

increases polarity

Question 16

main enzyme of phase 1 metabolism

Answer 16

cytochrome p450

helps to determine drug specificity

Question 17

phase 1: CYP3A4 metabolises

Answer 17

many drugs inc diazepam and methadone

and found in gut for presystemic metabolism

“3A”LLLdrugs

Question 18

phase 1: CYP2D6 metabolises

Answer 18

antidepressants and antipsychotics

codeine-morphine

“CYP2”Depressants

Question 19

phase 1: CYP1A2 metabolises

Answer 19

theophylline

CYP1A2- the 1 looks like T for theophylline

Question 20

phase 2 metabolism invlolves

Answer 20

conjugation

increases water solubility and enhances excretion

Question 21

what does phase 2 metabolism include

Answer 21

adding:

glucuronic acid

glutathione

sulphate

acetate to metabolite

inactivating molecule

Question 22

things that induce metabolism

Answer 22

smoking and alcohol

phenytoin

st johns wort

Question 23

things that inhibit metabolism

Answer 23

erythromycin

clarithromycin

grapefruit juice

Question 24

IV drugs and absorption

Answer 24

none absorbed

100% bioavailability

Question 25

sublingual route is good for

Answer 25

drugs with high fast pass metabolism

(under tongue, buccal cavity)

Question 26

rectal administration route bypasses

Answer 26

pre synaptic metabolism

Question 27

IM injection pros

Answer 27

long duration of action

Question 28

pros of percutaneous creams ointments and patches

Answer 28

bypasses presystemic metabolism

Question 29

inhaled drugs effects

Answer 29

little local

systemic absorption

Question 30

types of adverse drug reactions

Answer 30

• Augmented- too high a dose and response
• Bizarre- rare, allergy
• Chronic- long term side effects
• Delayed- carcinogenic
• End of treatment- withdrawal, rebound
• Failure of treatment

Question 31

predisposing factors for ADRs

Answer 31

taking multiple drugs

intercurrent diseases- liver or renal impairments

race age sex etc