Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
15 Cards in this Set
- Front
- Back
|
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)
|
