🗊 BIOTRANSFORMATION DR. NASIR ALI AFSAR

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  BIOTRANSFORMATION  DR. NASIR ALI AFSAR  , слайд №1  
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BIOTRANSFORMATION
DR. NASIR ALI AFSAR
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BIOTRANSFORMATION DR. NASIR ALI AFSAR

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CLEARANCE OF DRUGS
Definition
Why needed?
Either 
Unchanged
Metabolites
Polarity of compounds
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CLEARANCE OF DRUGS Definition Why needed? Either Unchanged Metabolites Polarity of compounds

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BIOTRANSFORMATION
Definition
Sites
Liver
GIT
Kidneys
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BIOTRANSFORMATION Definition Sites Liver GIT Kidneys

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Phases
Phase I - Nonsynthetic
make polar by unmasking a functional group like -OH, -NH2, -SH.
oxidation-add O, remove H
reduction-remove O, add H
hydrolysis - add H2O
Phase II - Synthetic
make very polar
Generally act in tandem
Описание слайда:
Phases Phase I - Nonsynthetic make polar by unmasking a functional group like -OH, -NH2, -SH. oxidation-add O, remove H reduction-remove O, add H hydrolysis - add H2O Phase II - Synthetic make very polar Generally act in tandem

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Nonsynthetic or Phase I Reactions: Cyt P450
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Nonsynthetic or Phase I Reactions: Cyt P450

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Enzyme Induction
Enhance synthesis: 
Phenobarbital, Steroids
Reduce rate of degradation: 
‘Substrate Stabilization’
Clotrimazole, Ethanol
Описание слайда:
Enzyme Induction Enhance synthesis: Phenobarbital, Steroids Reduce rate of degradation: ‘Substrate Stabilization’ Clotrimazole, Ethanol

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Enzyme Inhibition
Binding/Inactivation of heme iron: 
Imidazoles, Macrolides
Inactivation of the enzyme protein: suicide inhibitors:
Chloramphenicol
combination of above: 
Secobarbital
Описание слайда:
Enzyme Inhibition Binding/Inactivation of heme iron: Imidazoles, Macrolides Inactivation of the enzyme protein: suicide inhibitors: Chloramphenicol combination of above: Secobarbital

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Synthetic or Phase II Reactions:
Involves high energy intermediates
Glucuronidation, Acetylation, Methylation, Glutathione/ Glycine/ Sulfate/ Water Conjugation.
Transferases in microsomes or cytosol
Role of nutrition in regulation of drug conjugation
Описание слайда:
Synthetic or Phase II Reactions: Involves high energy intermediates Glucuronidation, Acetylation, Methylation, Glutathione/ Glycine/ Sulfate/ Water Conjugation. Transferases in microsomes or cytosol Role of nutrition in regulation of drug conjugation

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Clinical Relevance
Individual Differences
Age & Sex
Genetic Factors
Diet & Environmental factors
Drug interactions
Diseases
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Clinical Relevance Individual Differences Age & Sex Genetic Factors Diet & Environmental factors Drug interactions Diseases

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  BIOTRANSFORMATION  DR. NASIR ALI AFSAR  , слайд №15
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