lecture 11 drugs and the gut Flashcards
hydrolysis
breaking down drugs using water
reduction
loss of oxygen
oxidation
gain of ooxygen
intrinsic clearance
clearing unbound drug
drug that can change prothrombin time
paracetamol
flow of blood in the liver
periportal to perivenous
which way does bile flow
opposite way to the blood
what is on the other side of the endothelial cells
space of disse
where is oxygen high in the liver
peiportal end
where is glycolysis
hepatocytes
where is urea formed
periportal region
where is ammonia changed in the liver
perivenous end
what is ammonia changed into
glutamine
where is oxidative phosphorylation and gluconeogenesis
periportal end
how can we excrete drugs
bile or urine
what must an oral drug be to enter the blood
lipid soluble
what does hepatic drug extraction depend on
blood flow
ability of the enzymes
main enzyme of drug metabolism
cytochrome p450
first pass effect
oxidation, hydrolysis, hydroxylation, and deamination
what does first pass do
makes drugs more polar
what is phase 2
detoxification and conjugation
what is phase 2 for
makes drugs more water soluble
phase 3 is for
elimination
how and what is aspirin changed into
salicylic acid by hydrolysis
what is asparin conjugated to
glycine
phase 1 reactions are ctalysed by
cytochrome p450
low affinity drugs for C p450
metabolised slower and so have prolonged action
reduced renal clearance is associated with
reduced renal function
what can affect the conjugation
malnutrition
outcomes of hepatic metabolism of drugs
active agent, inactive compound, toxic metabolite and carcinogen
cortosol prodrug
cortisone
prednisolone prodrug
perdnisone
6 mercaptopurine prodrug
azathiapurine
what colour does rifampacin turn urine
orange
drug that can cause hepatitis
helothene
how does halothene cause hepatitis
forms free radicals
drug that can cause liver fibrosis
methotrexate
methotrexate is used for
RA and cancer
toxic metabolite of paracetamol
NAPQI
what would you give someone who has taken too much paracetamol and why
glutathione for conjugation