adme

Question 1

paracetamol MOA

Answer 1

central inhibition of cox2 and postagladin synthase

antipyresis via inhibition of PGE2

Question 2

progress of paraetamol toxicity

Answer 2

hepatic toxicity progresses to hepatic failure , enepalopathy and death within days

Question 3

what nabqi does on a cellular level

Answer 3

covalently bind cellular proteins altering cell function resulting in cell injury and death

Question 4

why is it that in paracetamol overdose glutathione is unable to detoxify all nabqi

Answer 4

glutathione reserve falls below 30%

Question 5

Na acteryl cysteine

Answer 5

restores glutathioneallowing napqi detoxification

direct antioxidant thereforeimoprove organ function and

Question 6

opioids MOA

Answer 6

opioid actions are mediated through interacctions with mu delta and kappa receptor.

myu rceptor is the primary site of action of opioid analgesics

Question 7

mu delta and kappa receptors

Answer 7

g protein coupled receptors that are located in the brain and the spinal cord

Question 8

opipid reeptor agonist, side effects

Answer 8

respiratiory depression (anti-tussive)

deddation

euphoria

Question 9

opioid toxicity through overdose

Answer 9

causes respiratory depression which can lead to apnea

cessation of breathing

Question 10

naloxone

Answer 10

antidote for opioid overdose

mu rceptor antagonist -reverses all signs of opioid intoxication

Question 11

pharmcoology of morphine metabolite. m6g

Answer 11

active metabolite

relative potency depnent on route of administraiton

70-360 x more poretnt folliow icv administation

Question 12

pharmaoclogy of morpgine metabolite. m36

Answer 12

inactive metabolite

Question 13

metabolites of morphine and renal impariement

Answer 13

metabolites accumulate in renal impairment

Question 14

m6g as an analgesic

Answer 14

similar analgesic effect of morphine

fewer side effects.
-less respiratory depression

significant reductions in incidences of nausea and anti emetic

Question 15

pharmacohenomics, safety and efficacy

Answer 15

genetric polymorphisms in the enzymes responsible for phase 1 and 2 metabolism alter the safety aand efficacy of drugs

Question 16

phase 1 metabolism of codeine to morphine

Answer 16

cyp2d6

Question 17

poor metabolizers

Answer 17

poor emtabolised habe a decreased activation of cyp2d6 dependent analgesics

poor metabolisers do not get any analgesic benfits from codeine

sme frequency of side effects as normal metabolisers

Question 18

ultrarapid emtabolisers

Answer 18

potential for increased risk of production of morphne from codeine

increased risk of opioid related adr

lead to serious complicaiton of opiod toxicity which can be fatal

Question 19

tramadol metabolism

Answer 19

11 metabolites identified

m1 has the analgesic activity

Question 20

pharmacological effects tramadol and its metabolites

Answer 20

+- tramadol:weak opioid agonist and serotonin reupake inhibitor

–trmadol:noradrenaline reuptake inhibitor

+-m1:700x greater affinity for mor than parent compound

–m1: mop analgesic activity

Question 21

opmr1 115 allele

Answer 21

polymorphisms of the mu opioid receptor gene (opmr1) varies opioid response

increase in medication
decrease in pain relief

Question 22

how can rapid metbaolisers stl benefit from opioids

Answer 22

benefit from a lower dose of opioids