functional group like -OH, -NH2, -SH.
oxidation-add O, remove H
reduction-remove
O, add Hhydrolysis - add H2O
Phase II - Synthetic
make very polar
Generally act in tandem
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Презентация на тему Биотрансформации
Содержание
- 2. CLEARANCE OF DRUGSDefinitionWhy needed?Either UnchangedMetabolitesPolarity of compounds
- 3. BIOTRANSFORMATIONDefinitionSitesLiverGITKidneysOthersLungsSkin
- 4. PhasesPhase I - Nonsyntheticmake polar by unmasking
- 5. Nonsynthetic or Phase I Reactions: Site
- 6. Oxidation Reduction Hydrolysishydroxylations aromatic, aliphatic, nitrogendealkylations(N-, S-, P)deaminationsN-, S-, P-
- 7. Nonsynthetic or Phase I Reactions: Cyt P450
- 8. Nonsynthetic or Phase I Reactions: Cyt P450
- 9. Nonsynthetic or Phase I Reactions: Cyt P450
- 10. Enzyme InductionEnhance synthesis: Phenobarbital, SteroidsReduce rate of degradation: ‘Substrate Stabilization’Clotrimazole, Ethanol
- 11. Enzyme InhibitionBinding/Inactivation of heme iron: Imidazoles, MacrolidesInactivation of the enzyme protein: suicide inhibitors:Chloramphenicolcombination of above: Secobarbital
- 12. Synthetic or Phase II Reactions:Involves high energy
- 13. Results of BiotransformationBiotransformed Drug or PoisonIn general
- 14. Clinical RelevanceIndividual DifferencesAge & SexGenetic FactorsDiet & Environmental factorsDrug interactionsDiseases
- 15. Скачать презентацию
- 16. Похожие презентации
CLEARANCE OF DRUGSDefinitionWhy needed?Either UnchangedMetabolitesPolarity of compounds
Слайд 4
Phases
Phase I - Nonsynthetic
make polar by unmasking a
functional group like -OH, -NH2, -SH.
O, add Hhydrolysis - add H2O
Phase II - Synthetic
make very polar
Generally act in tandem
Слайд 6
Oxidation
Reduction
Hydrolysis
hydroxylations
aromatic, aliphatic, nitrogen
dealkylations(N-, S-, P)
deaminations
N-, S-, P- oxidations
S-replacements
epoxidations
others
azo
reduction
nitro reduction
disulfide reduction
others
esters
amides
oxidoreductases
oxidases
monoamine oxidases
mixed function oxidasesoxidoreductases
reductases
esterases
amidases
peptidases
lipases
Nonsynthetic or Phase I Reactions:
Слайд 10
Enzyme Induction
Enhance synthesis:
Phenobarbital, Steroids
Reduce rate of degradation:
‘Substrate Stabilization’
Clotrimazole, Ethanol
Слайд 11
Enzyme Inhibition
Binding/Inactivation of heme iron:
Imidazoles, Macrolides
Inactivation of
the enzyme protein: suicide inhibitors:
Chloramphenicol
combination of above:
Secobarbital
Слайд 12
Synthetic or Phase II Reactions:
Involves high energy intermediates
Glucuronidation,
Acetylation, Methylation, Glutathione/ Glycine/ Sulfate/ Water Conjugation.
Transferases in microsomes
or cytosolRole of nutrition in regulation of drug conjugation
Слайд 13
Results of Biotransformation
Biotransformed Drug or Poison
In general -
nonsynthetic
reactions
precede synthetic reactions
can produce active metabolites
synthetic reactions
produce inactive
metabolitesDrug or
Poison
Слайд 14
Clinical Relevance
Individual Differences
Age & Sex
Genetic Factors
Diet & Environmental
