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19 Cards in this Set
- Front
- Back
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biotransformation |
it is the metabolic conversation of drugs so its easily excreted lipid soluble to water soluble from lipid soluble to water solubleactive to inactivenon ionised to ionised lipid soluble to water solubleactive to inactivenon ionised to ionised lipid soluble to water solubleactive to inactivenon ionised to ionised active to inactive non ionised to ionised |
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main site of biotransformation |
main site liver also occurs in kidney git liver skin plasma and lungs |
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metabolism is controled by? |
cellular enzyme |
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phase 1 of biotransformation |
non synthetic reaction occurs via oxidation reduction and hydrolysis 1. inactivation of nearly all drugs 2. conversation of active drug like phenacitin to active metabolite like paracetamol 3. from inactive drug like cartisone to active cartisole 4. conversation into toxic compound like methanol to formaldehyde |
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phase 2 of biotransformation |
synthetic and conjugation conjugation with endogenous compounds via activity of transferases results of inactivation of drugs |
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conjugation of compound with? |
d acetyl acid glucuronic acidacetyl acidglycinmethyl groups glycin methyl groups |
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glucoronic acid |
chloramphanicol morphine |
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acetic acid |
sulphonomides hydralazine isoniazid |
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glycine |
salicylates |
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methyl groups |
catecholamine and histamine |
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factors affecting hepatic microsomal activity |
drugs age gender pathological conditions genetic factors starvation |
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drugs- enzyme activators (inducers) |
phenobarbitone rifampicin smoking diphenylhydetoin androgen griseofulvin griseofulvin |
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enzyme induction result in? |
decrease activity if some drugs oral anticoagulants, oral contraceptives and corticosteroids due to increase metabolism |
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type of enzyme inhibitors? |
cimetidine grapefruit progesterone oestrogen chloramphenicol tolbutamide sodium valproate |
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what does enzyme inhibitors do |
they increase the effects of drugs |
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gender |
male hormone stimulate drug metabolsm female hormone are inhibitors |
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age |
neonate cannot conjugate with glucuronic acid chloramphenicol causes grey baby syndrome |
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pathological conditions |
liver disease and cancer |
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genetic factors |
succinyle (muscle relaxent) choline apnea |
