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15 Cards in this Set

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what is pegylation
a process of attaching the strands of the polymer PEG to molecules such as peptides, proteins, and antibody fragments, that can help improve safety and efficiency of therapeutics
what does pegylation produce
alterations in the physiochemical properties such as conformation, electrostatic binding, hydrophobicity
what do the physical and chemical changes caused by pegylation do
increase systemic retention of therapeutic agents
what can pegylation influence
binding affinity of the therapeutic moiety to the cell receptors and can alter the absorption and distribution patterns
what are the advantages of pegylation by increasing the weight of the molecule
improved drug solubility
extended circulating life
increased drug stability
enhanced protection from proteolytic degradation
reduced dosage frequency
what can influence the binding affinity of the therapeutic moiety to the cell receptors
pegylation
what is the pathway of drug metabolism
Drug > phase 1 >

Active metabolite > phase 2 > conjugate > excreted

Inactive metabolite> excreted
what are the phase 1 reactions
oxidation
reduction
hydrolysis
hydration
isomerisation
dethioacetylation
what are the phase 2 reactions
glucuronidation/glucosidation
sulfation
methylation
acetylation
amino acid conjugation
glutathione conjugation
FA conjugation
condensation
what is the most important enzyme in phase 1
CYP450
what is CYP450 classified as
haem containing enzyme (haemoprotein)
where are CYP450
in the ER
what does CYP2C19 do
metabolizes proton pump(zole) inhibitors, fluoxetine, sertraline, nelfinavir
what are proton pump inhibitors for
treatment of ulcers
if you don't have TPMT what will happen when given Thiopurines
adverse drug effect (leukopenia)