Drug Biotransformation
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| two primary ways in which drugs are eliminated from the body | show 🗑
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| show | intestine
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| show | liver; first pass metabolism
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| Biotransformation | show 🗑
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| show | xenobiotics
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| show | derivative of drug structure; usually inactive or less active
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| biotransformation result in a metabolite that is no longer able to produce a therapeutic response | show 🗑
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| In some cases, the drug is inactive and the biotransformation results in | show 🗑
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| want to make the xenobiotics more polar to excrete | show 🗑
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| most drugs are biotransformed prior to excretion because they are not | show 🗑
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| show | less active or inactive as compared to parent drug; metabolite can no longer produce therapeutic response
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| in some cases biotransformation results in | show 🗑
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| show | prodrug; must be biotransformed to have therapeutic response
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| show | cant actually make more or less active
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| biotransformation occurs mainly in the | show 🗑
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| show | GI tract to enter bloodstream; once in bloodstream drugs are transported directly to liver via hepatic poral vein then to circulation
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| a considerable percentage of of an orally ingested dose is often metabolized | show 🗑
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| show | "first pass"- through liver
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| an active drug can go two routes | show 🗑
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| at site of action the chemical structure is not active | show 🗑
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| show | not "in the body"
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| orally ingested drugs go to --> | show 🗑
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| show | no way to tell; can be a barrier to get drug into bloodstream
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| show | CYP450's; superfamily thats responsible for majority of all drug biotransformations
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| cytochrome P450's are heme containing proteins that are capable of the following rxn's | show 🗑
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| enzyme involved in drug-drug interactions | show 🗑
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| show | Inducer; induction
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| show | inhibition
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| show | basically the high affinity drug will hog the active sites and the low affinity drugs wont be metabolized
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| when less enzymes are available what happens to drug concentration in bloodstream? | show 🗑
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| show | drugs that are affected by the actions of inhibitors and inducers
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| show | inhibitors; less enzymes= less metabolism
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| increases amount of enzymes | show 🗑
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| must abundant subfamily of human cytochrome enzymes | show 🗑
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| show | prodrugs; it is then transformed into an active substance either by chemical or metabolic means
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| designed to take advantage of absorption or metabolic properties to provide optimal drug therapy | show 🗑
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| show | true; ex:chloramphenicol succinate is chemically inactive until release into bloodstream (IV)
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| show | this helps keep the inactive form from stomach upset; it becomes active in the liver
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| show | inhibition; too many drugs and not enough enzymes
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| EX: a decrease in the active form of a drug occurs | show 🗑
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| show | Inducer; lots of enzymes to activate the prodrug
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| EX: a decrease in the plasma concentration of the active form of PROdrug | show 🗑
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| show | No metabolism because enzyme doesnt work
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| show | Phase I and Phase II
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| show | Phase I; introduce or expose a functional group on a compound to make more polar (hydrophilic)
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| Phase that generally results in loss of activity | show 🗑
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| show | Phase II; covalent linkage between functional group ON the parent drug and a highly polar conjugate; to make more hydrophilic
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| Phase I doesnt always happen, neither does Phase II | show 🗑
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| entero | show 🗑
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| Microflora in intestines can cleave the covalent bond made during Phase II biotransformations which does what? | show 🗑
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| Reversal of Phase II rxn | show 🗑
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| Phase I reactions (dealkylation)KNOW* | show 🗑
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| show | Aliphatic and aromatic hydroxylation- addition of OH group; can also result in a doubly bonded O
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| show | N and S; addition of O to N or S
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| show | remove amine; done via oxygen
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| show | breaking of a bond with addition of H2O
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| Phase II reactions Glucuronidation | show 🗑
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| show | add a sulfate (SO3--)
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| show | SCoA + RNH2 --> NHR plus CoASH
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| show | a tripeptide of glutamate, cysteine, and glycine that picks things up to help them be excreted
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| show | Primarily kidneys and liver in high concentrations; detoxification of xwnobiotics via Phase II conjugation
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| GSH is metabolized to what in order to be excreted? | show 🗑
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| show | glutathione S- transferases
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| Electrophilic substrate that wants electrons | show 🗑
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| Glutathione Adduct or Conjugate is what | show 🗑
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| Mercapturic Acid | show 🗑
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| show | 60% Glucuronide, 30% Sulfate -->both go toward renal excretion
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| Oxidized Acetaminophen becomes | show 🗑
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