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MCPHS MedChem Ex 1
MCPHS MedChem Ex 1 Summer 07
| Question | Answer |
|---|---|
| What are nuclear receptors? | AHR, RXR, PXR, CAR: turned on by ligand to autoinduce CYP expression |
| What CYP does AHR induce? | 1A1 & 1A2, induced by hydrocarbons, conversion of pro-CA compounds |
| PXR does what? | nucear receptor that induces 3A4, ligand is RIF, st. Johns, statins, (causes met of hormones) |
| CAR does what? | Nuclear Receptor induces 2B6, 2C9, 3A4 (Ligands: phenobarbital, -azoles, androstanol) |
| Gilberts Syndrom? | Genetic decrease in UGT1A1 gene causing HyperBilirubinemia, decreased glucuronidation, increased Cp of many drugs as a result |
| Terfenadin(seldane)? | Converted to Fexofenadine (allegra) by Cyp 3A4, but Ery & -azoles Inhibit, ADR is incr. QT & CHF |
| Quinidine Inhibits? | 2D6 (many substrates) |
| Lopinavir combo drug? | Kaletra = lopinavir + Ritinavir (offsets clearance of lopinavir by 3A4) |
| ROS does what to GSH? | makes GSSH, and GSH is no longer available to clear NAPQI, blocks glutathione pathways |
| ETOH does what? | Stabilizes mRNA Inducing 2E1 driving up NAPQI productions w/APAP OD |
| Metabolism is Inhibited by? | Piperonyl butoxide, cimetidine, etoh, GFJ, diallyl sulfide (garlic) |
| Metabolism is Induced by? | Barbituates, PAHs, OrganoChlor, etoh, antibiotics |
| Finneys Formula? | 1/LD50 (mix) = [( %A/LD50A) + (%B/LD50B)] Predicted/Observed = deg. of potentiation |
| centrilobular has? | FMOs and CYPs |
| periportal has? | glutathione, O2, Alcohol Dehydrogenase |
| NAPQI increased by which CYPs | 1A2, 2E1, 3A4 |
| Antidote for APAP OD? | Acetadote (N-acetyl Cysteine) |
| APAP is also called? | paracetamol |
| apap od = ? | 10-15 g = 20 - 30 caps at 500 mg |
| Cats dont do what process? | Cats do not perform glucuronidation So, no APAP |
| What CYPs most effected by liver disease? | 1A, 2C19, 3A (2D6, 2C9, 2E1 are less effected by liver disease) |
| Which CYPs do what? | 1 = PAHs & Aryl Amines, 2 = Drugs & Steroids, 3 = Drugs |
| What does Antizol do? | Inhibits Alcohol Dehydrogenase (4-methyl pyrazol) |
| Antidote for 1080 f-acetate poisoning) | Alcohol (IV), or Antizol "forepizole" 8000x more pot than ETOH |
| What is Questran? | "Cholestyramine" traps digitoxin/kepone, pesticides in EHC |
| Sites of CA/Tox targets? | CA: olfactory, intestines, hepatic Tox: LIver, Kidney, Lungs |
| Ave consumptions? | Air 9000 L/d, H2O 2 L/d |
| RfD = ? | RfD = Noael / (UF x MF) = ADI |
| Epigenetic means? | non-genotoxic |
| Ames test? | uses salmonilia to determine mutagenic agents in biotests, potential to cause CA |
| TI & Mos = ? | TI = LD50/ED50 MoS = LD01/ED99 |
| Q1 star? | CA slope factor (goes through zero, no threshold for CA) |
| Atorvastatin & GFJ (3A4 inhibition) = ? | liver failure |
| Terfenadine & GFJ (3A4 inhibition) = ? | CHF |
| Cimetadine does what? | Inhibits many P450s |
| 3A4 Induction? | Barbituates, Ery, RIF, Griseofulvine, glucocorticoids (causes inactivation of Estrogen & Progesterone) |
| Warfarin Clearance Inhibitors are? | APAP, GFJ, Quinidine, Cimetidine, Smoke, Sildenafil, Clotrimazole (causes incr PT & Bleeding) |
| Warfarin Clearance Inducers? | st. Johns, Alcoholism, Barbituates, RIF, Phenytoin, griseofulvin (causes decreased PT & Stroke) |
| Warfarin is Detox (cleared) By which CYPs? | 2C (9/19 & 8/18), 1A2, 3A4 |
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