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PDA I
Shankars PGt, PGx Lectures
| Question | Answer |
|---|---|
| Deals with single genes? | PGt |
| Deals with whole genes? | PGx |
| whats pharmacogentics | variabity in heredity factors as it relates to drug response in different population |
| what pharmacogenomics | study of the genome (DNA) as it related to drug response |
| Causes of variation to drug response? there are 7 factors. he gave us 5 in lecture..what are they | Geneticss, Age, Sex, Nutritional status, Physiological status, Pathological states, and drug interactions |
| do you think with incresing age, your metabolic enzymes will be increased or decreased? | Decreased..your getting older and ratter..things wont work as good |
| If someon excercises alot, do you expect blood to perfuse better or worse? | better. will effect how much drug gets to the site and how quickly |
| Kidney and Liver and involved in what process? | In detoxification and Execretion of metabolites of the active drug. |
| Pahtological states means what | disease state |
| drug interactons mostly occur with people on few drugs...or multiple drugs | multiple drugs |
| Pk of a drug | what body does to the drug (ADME - your body does all this) |
| PD of a drug | what drug does to the body (think of the receptors) |
| What is Succinylcholine | neuromusclar blocking agent used in surgeical procedures. For muscle relaxation. (CHOLINE- think muscle!) |
| What degrades Succinylcholine? | Cholinesterases does! (it comes from liver and plasma) |
| If someone has succinylcholine Apnea. Do they recover faster or slower from this relaxant? | Recover SLOWER. Normal people's drug concentration drops quickly after taking out the IV. |
| LONGER muscle relaxation and apnea..they must have this problem? | Their cholinesterases arent working properly |
| What Dibucaine used for? | for a test,to see how ur cholinesterases functioin |
| What does Apnea Mean | Trouble breathing |
| What do N-acetltansferases do? | they metabolize common drugs and detox carcinogens |
| Where does Acetylation occur? | In liver and gut mucosa |
| What type of rxn is Acetylation? | its a Conjuntion rxn |
| How many types of N-acetyltransferases are there? | two |
| Which one metabolizes isoniazid, caffeine, and anti-infectives | Nat2 |
| Which metabolizes p-aminosalicylate and P-aminobenzoic acid | Nat1 |
| What do Nat1 and Nat2 actually do? | Its transfer an acetyl group from Acetyl CoA to an amine--and forms and Amide |
| N-acetylltransfrases form what final functional group | Amides |
| Which acetylators have both slow and fast | NAT2 does---(way to remember: caffine metabalizes FAST and antiinfects/isoniazide metabolizes SLOW |
| Acetylation is responsible for confervting to what form to excrete? | To ionic forms |
| what form in the urine is excreted OUT faster? | Ionic form |
| What form is more ionic? Primary amine or amide? | Primary amine is more ionic |
| Give two exxamples of drugs that get Acetylaed? | Chlorenphenicol and Aminoglycosides |
| What happens when groups are acetylated? (not sure if i said this correctly ask shankar) | drugs no longer bind the 30S subunit |
| Resistance to chlorenfphicol and aminoglycosides can occur as they become ......what? | amino groups get acetylated |
| If you have gave someone Isoniazide- which NAT would metabolize it | NAT2 |
| If NAT2 was defected/not working, and you give somosomone P-aminobenzoic acid ..what would happen | nothing, NAT metaboizes Pamino-acid |
| If you give someone isonizide and their NAT2 was defective what would happen | Could get toxic levels because the isonizide is not being metabolized |
| Why is it important to have normal levels of Nat2 | Bc of toxicity issues. and can properly metabolize drugs |
| Sulfonamide compounds are metabolied by which NAT | Nat 1 |
| Which CYP is very common in metabolizing drugs | CYP 2D6 |
| What population of people has lower CYP2D6 | Whites and some Asians |
| What imhibits CYP2D6 | Prozac (fluxetine) |
| Drug interactin when cyp2d6 is inhibited..with what type of drug | Antidepressant |
| Warfarin inhibits what enzyme? | epoxide reductase |
| What CYP metabolizes warfarin? | CYP2C9 |
| 2C9*2 and 2C9*3 are associated with what? | with excessive anticoagultoin and bleeding during warfarin thearpy |
| What is the most polymorphic type of CYP | 2d6 |
| Tricyclin antidepressants depend on wht CYP? | CYP2D6 |
| What drug works on Epoxide Reductase? | Warfarin |
| what does 2C9 do? | metabolizes warfarin |
| Azathrioprine what does it treat | R.A. |
| Mercaptopurine what does it treat | acute lmphoblastic leukemia |
| what enzyme converts Thiopurines to the Toxic thioguanine nucleotides? | HPRT |
| What inactivates Thiopurines? | Adding a methyl group |
| Who adds the methyl group on thiopurines? | TPMT (thiopurine methyl transferase) |
| Do you konw the thiopurine biotransformation pathway? | you better. Two key enyzmes are TPRT and TPMT |
| if TPMT isnt working..shifts in what direction? | south, to make toxic Guanines |
| If givening Allpurinol- what enzyme is inhibited | XO |
| is BCR gene 9 or 22 | 22 |
| is ABL gene 9 or 22 | 9 |
| how can we try and treat CML, two ways (phenotype attack!) | Stem cell replacement and interferon alpha cytarabine |
| what drug can we use to taget CML...genotypically? | Gleevac |
| in CML what happens to your cells | they keep dividing..its cancer |
| if you have mutant forms of Chromo 9 and 22...what happens | resistance forms |
| The BCR-ABL protein makes a protien that does what? | it disrupts the normal function of granulocytic leukocytes--causing CML |