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41 Cards in this Set
- Front
- Back
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(1) Biotransformation?
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The conversion of compounds from lipophilic substances to polar
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(2) 3 effects of biotransformation?
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1. terminates biological activity
2. facilitates drug removal 3. conversion of "pro" drug to active |
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(3) 4 sites of biotransformation?
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Liver, Kidney, GI, Lungs
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(4) Microsomes?
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isolated vesicles that are formed from lipophilic membrains that are dence in enzymes involved in biotransformation.
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(5) Phase 1 vs Phase 2 metabolism?
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Phase 1 - introduce or unmask functional group
Phase 2- conjugation of a polar group |
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(6) What metabolic reactions are CP450 dependent?
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Oxidations
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(7) What metabolic reactions are CP450 independent? (3)
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Dehydrogenation
Reduction Hydrolysis |
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(8) What is the electron source for P450?
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Cytochrome P450 Reductase/Flavoprotien reductase
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(9) What is the reducing sgent for P450?
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NADPH
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(10) What are the 4 steps for the c P450 cycle?
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1. Oxidized p450 binds substrate
2. NADPH gives electrons to flavoprotien reductase that reduces P450 3.O2 Binds the reduced P450 drug complex, a second electron is donated forming an activated oxygen" -P450 substrate complex 4. Release of H20. Second O atom transfered to subtrate. Oxidized P450 is regenerated. |
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(11) Oxidative Dealkylation?
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Losing an alkyle group (methyl goups included)
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(12) S and N Oxidation?
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Adding oxygen to N or S
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(13) Deanimation?
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losing an NH2 group usually for a mythle group.
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(14) how many families are in the C450 group?
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3
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(15) Which P450 is responsible for metabolizing 60% of drugs used?
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CYP3A4
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(16) 2 ways that inducers work on P450?
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Increase rate of P450 synthesis
Decrease rate of degredation of P450 |
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(17) 4 ways P450 is inhibited?
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1. Bind heme iron of P450
2. Bind heme iron and inactivation 3. Bind reactive intermediates 4. Generate metabolites that inactivate the enzyme. |
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(18) what is the endogenous reactants for glucoronidation?
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UDP glucuronic acid
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(19) what is the endogenous reactants for acetylation?
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Actyl CoA
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(20) what is the endogenous reactants for sulfate conjugation?
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Phosphoadenosyl Phosphosulfate PAPS
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(21) what is the endogenous reactants for methylation?
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S-Adesnosyl methionine
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(22) 7 examples of Phase 2 enzymes?
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1. UDP glucuonosyl tranferase
2. N-acetyletransferace 3. GSH-S-transferace 4. Acyl-CoA glycinetransferase 5. Sulfotransferase 6. transmethylases 7. Eposide hydrolase |
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(23) An increase in enzyme/organ fucntion leads to?
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Enhanced biotrasformation which means less drug and sub-therapeutic levels in the system.
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(24) 7 factros that affect biotransformation
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1. individual factors
2. genetic factors 3. diet adn envirnmental factors 4. age and sex 5. drugs 6. endogenous compunds 7. disease. |
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Coagulative necrosis is usually caused by?
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lack of oxygen
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A type of necrosis where you can still make out individual cells.
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coagulative necrosis
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mumificated tissue is a sign of which necrosis?
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Dry gangrenous necrosis
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Type of necrosis where individual cells cannot be made out and leads to absesses?
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liquifactive necrosis
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2 instances where tissue undergoes liquifactive necrosis?
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heart muscle and brain tissue
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Evidence of liquifactive necroisis of the brain is seen as?
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little holes.
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A big area of homogenized material is which necrosis?
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caseous necrosis.
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Teberculosis and seldomly fungul infections causes which necrosis?
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caseous necrosis
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pancreatitus can cause which for of necrosis?
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enzymatic fat necrosis
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Vessels that have undergone fibrinoid necrosis have what effect on the vessles?
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They swell and decrease the opening.
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what is usually deposited at sights of necrosis?
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calcium
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What is one thing that can cause raised blood calcium levels?
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hyperparathyroidism
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Anoxia?
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no oxygen
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A friction injury?
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abrasion
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patterned abrasions can be a sign off?
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abuse
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Blunt force injury, causes brusing
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contusion
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tearing away of tissue?
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Avulsion.
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