15: P450s Flashcards
Cytochromes Perform Oxidation-Reduction (RedOx) Reactions in Phase _____
Bound to the lipid membranes of the _____ endoplasmic reticulum
Most are found in the liver, but exist in lung, kidney, heart, and brain also since they all have _____ endoplasmic reticuli.
Cytochromes Perform Oxidation-Reduction (RedOx) Reactions in Phase 1
Bound to the lipid membranes of the smooth endoplasmic reticulum
Most are found in the liver, but exist in lung, kidney, heart, and brain also since they all have smooth endoplasmic reticuli.
Oxidation is the _____ of electrons or an increase in oxidation state by a molecule, atom, or ion.
Reduction is the _____ of electrons or a decrease in oxidation state by a molecule, atom, or ion.
Oxidation is the loss of electrons or an increase in oxidation state by a molecule, atom, or ion.
Reduction is the gain of electrons or a decrease in oxidation state by a molecule, atom, or ion.
Prodrug - a medication that is administered in an inactive or less than fully active form, and is then converted to its _____ form through a normal metabolic process
Prodrug - a medication that is administered in an inactive or less than fully active form, and is then converted to its active form through a normal metabolic process
Induction – Biotransformation by Induced CYP enzymes results in either increased _____ of prodrugs or _____ elimination of drugs. CYP enzymes become induced and work faster due to the presence of a substrate.
Induction – Biotransformation by Induced CYP enzymes results in either increased activity of prodrugs or enhanced elimination of drugs. CYP enzymes become induced and work faster due to the presence of a substrate.
Inhibition – results in _____ bioavailability of a drug or _____ activity of a prodrug since CYP enzyme acitivity decreases. So prodrug stays prodrug & has no activity & unmetabolized drug can exert its effects for a longer time.
Inhibition – results in increased bioavailability of a drug or decreased activity of a prodrug since CYP enzyme acitivity decreases. So prodrug stays prodrug & has no activity & unmetabolized drug can exert its effects for a longer time.
Polymorphism – a genetic change that exists for at least _____% of the population. CYP polymorphism occurs when the biotransforming properties of an enzyme are altered.
Polymorphism – a genetic change that exists for at least 1 % of the population. CYP polymorphism occurs when the biotransforming properties of an enzyme are altered.
Substrate – A substance (drug/medication/ prodrug) acted on by an _____
Substrate – A substance (drug/medication/ prodrug) acted on by an enzyme
CYP1A _____ acts on caffeine & Theophylline. Smoking and charred foods are inducers of CYP1A _____. Grapefruit juice is an inhibitor of CYP1A _____.
CYP1A2 acts on caffeine & Theophylline. Smoking and charred foods are inducers of CYP1A2. Grapefruit juice is an inhibitor of CYP1A2.
CYP2C _____ acts on phenytoin & warfarin*. Rifampin is an inducer of CYP2C _____. Macrolides are inhibitors of CYP2C _____.
There are 1-2% polymorphisms in CYP2C _____ in african amerians and asians and 1-3% polymorphisms in whites.
CYP2C9 acts on phenytoin & warfarin*. Rifampin is an inducer of CYP2C9. Macrolides are inhibitors of CYP2C9.
There are 1-2% polymorphisms in CYP2C9 in african amerians and asians and 1-3% polymorphisms in whites.
CYP2C _____ acts on diazepam*. St. Johns wort is an inducer of CYP2C _____. Fluoxetine is an inhibitor of CYP2C _____.
20% of african americans have polymorphisms in CYP2C _____, 15-20% asians have polymorphisms in CYP2C _____, & 3-5% whites have polymorphisms in CYP2C _____.
CYP2C19 acts on diazepam*. St. Johns wort is an inducer of CYP2C19. Fluoxetine is an inhibitor of CYP2C19.
20% of african americans have polymorphisms in CYP2C19, 15-20% asians have polymorphisms in CYP2C19, & 3-5% whites have polymorphisms in CYP2C19.
CYP2D_____ acts on codeine*. Rifampin is an inducer of CYP2D_____. Quinidine & haloperidol are inhibitors of CYP2D_____.
There are polymorphisms in CYP2D_____ in all races, but some more than others: whites 5-10%, ethiopians 30%, southern european 10%.
CYP2D6 acts on codeine*. Rifampin is an inducer of CYP2D6. Quinidine & haloperidol are inhibitors of CYP2D6.
There are polymorphisms in CYP2D6 in all races, but some more than others: whites 5-10%, ethiopians 30%, southern european 10%.
CYP2E_____ acts on paracetamol/ acetaminophen
CYP2E1 acts on paracetamol/ acetaminophen
CYP3A_____ acts on trefenadine & verapamil. St. Johns wort is an inducer of CYP3A_____. Ketoconazole & itraconazole are inhibitors of CYP3A_____.
CYP3A4 acts on trefenadine & verapamil. St. Johns wort is an inducer of CYP3A4. Ketoconazole & itraconazole are inhibitors of CYP3A4.
Mnemonic: A looks like 4
CYP enzymes have _____ in their core.
CYP enzymes have iron in their core.
Codeine is the most famous prodrug, it is converted to morphine by CYP2D_____.
Rifampin is an _____ of CYP2C9 & is given for tuberculosis. If a patient begins taking Rifampin while taking Codeine, CYP2C9 is _____ by Rifampin & works overtime and there is increased production of morphine so morphine toxicity (toxidrome).
Patient will get lethargic and sleepy after taiking pain medication if taking _____.
Codeine is the most famous prodrug, it is converted to morphine by CYP2D6.
Rifampin is an inducer of CYP2C9 & is given for tuberculosis. If a patient begins taking Rifampin while taking Codeine, CYP2C9 is induced by Rifampin & works overtime and there is increased production of morphine so morphine toxicity (toxidrome).
Patient will get lethargic and sleepy after taiking pain medication if taking Rifampin.
