Pharmacokinetics 2 Flashcards
Phase I metabolism
• Generally oxidation, reduction or hydrolysis – Introduce/reveal a reactive chemical group
– “Functionalisation”
• Products often more reactive
Phase II metabolism
- Synthetic, conjugative reactions
* Hydrophilic, inactive compounds generated (usually)
Cytochrome P450 Enzymes
Mixed function monooxygenases
Throughout the body, extensively in the liver 57 human genes coding for CYP P450 enzymes
functions of cytochrome P450 enzymes
biosynthesis of steroids, fatty acids and bile acids
metabolism of endogenous and exogenous substrates
Simvastatin metabolised by CYP3A4 in
the gut wall and liver
Metabolism of non-depolarising NMJ blockers - vecuronium
Liver – eliminated via the urine and bile
Metabolism of non-depolarising NMJ blockers - atracurium
spontaneous degradation in plasma
Metabolism of non-depolarising NMJ blockers - mivacurium
plasma cholinesterase
Possible sources of excretion include
- Breath
- Urine
- Saliva
- Perspiration • Hair
- Feces • Milk • Bile
Cmax
horizontal from peak
Tmax
vertical from peak
Absorption half life
half the height of peak to the left and time at which this occurs
Plasma clearance half life
half the height of the peal to the right and the time at which this occurs
“Steady state”
Plasma concentration increases during infusion until rate of input equals rate of output