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MSK exam 1 med chem
MSK exam 1 med chemistry
| Question | Answer |
|---|---|
| the allosteric binding pocket is inaccessible in | COX-1 |
| which amino acid covers allosteric pocket | isoleucine |
| between cox 1 and cox 2 which is the better target | COX- 2 |
| cox-1 expression is | Constitutive |
| cox-2 expression is | Inducible |
| Thromboxane (TXA2) | Platelet aggregation & vasoconstriction |
| Thromboxane (TXA2) produced by | COX-1 |
| Prostaglandin E2 (PGE2) | Pain, fever, inflammation, gastric mucosal, renal blood flow |
| Prostaglandin E2 (PGE2) produced by | COX-1 |
| Prostacyclin I2 (PGI2) | inhibition of platelet aggregation, vasodilation |
| Prostacyclin I2 (PGI2) produced by | COX- 2 |
| Phospholipase A2 (PLA) hydrolyzes the .... | ester bond in the membrane phospholipid |
| Archidonic acid is stored in the membrane as part of ... | Phospholipids |
| Arachidonic acid is also called | Eicosatetraenoic acid |
| for a weak acid if pH < pKa | mostly unionized |
| for a weak acid if pH > pKa | mostly ionized |
| how many carbon atoms does arachidonic acid have | 20 |
| Aspirin (ASA) MOA | inhibit prostaglandin synthesis by irreversible inhibition of COX |
| Aspirin (ASA) covalently acetylates | Ser530 of COX-1 and Ser516 of COX-2 |
| Low dose aspirin (81mg) has | Cardioprotective effect |
| drugs affecting aspirin | other NSAIDS & Anticoagulants |
| aspirin increase risk of ______ with viral infection or live virus vaccine | Reye's syndrome |
| NSAIDS adverse effects BOX WARNING | Increase risk of CV adverse effects & GI adverse effects |
| NSAIDS other adverse effects are | decrease renal function, increase renal function, premature closer of ductus arteriosus in fetus |
| for Arylalkaonic acid separation of acidic group and flat aromatic ring by ____ | one carbon is optimal for activity |
| for Arylalkaonic acid R= H are ? | acetic acid derivatives |
| for Arylalkaonic acid R= CH3 are? | Propionic acid derivatives |
| for Arylalkaonic acid the carboxylic acid(acidic group) is required for? | binding with COX active site |
| General NSAIDs bind to albumin due to ___ | acidic nature of drug |
| which NSAIDs can reach high concentration in the synovial fluid | indomethacin and diclofenac |
| General NSAIDs are | CNS penetration |
| General NSAIDs bio activation or inactivation of drug by | CYP2C9 |
| General NSAIDs are excreted through the | Renal |
| General NSAIDs t1/2 for short acting (<6hrs) are___ | ibuprofen, diclofenac, ketoprofen, indomethacin |
| General NSAIDs t1/2 for long acting (>6hrs) are ___ | Sulindac, naproxen, nabumetone, celecoxib, meloxicam, piroxicam |
| NSAIDs + Anticoagulant = | increase risk of bleeding |
| NSAIDs + Diuretic= | decrease diuretic effect |
| NSAIDs + ACEi/ARB = | decreases antihypertensive effect |
| NSAID + Antidepressant = | increase risk of intracranial bleeding |
| NSAIDs+ Lithium and high doses of methotrexate = | increase serum concentration; possible toxicity |
| NSAID+ cyclosporine = | Increased risk of nephrotoxicity |
| Indomethacin( Indocin) is | psuedo irreversible inhibitor to COX and has high oral BA |
| Indomethacin( Indocin) is lipophilic or hydrophobic | lipophilic |
| Indomethacin( Indocin) drug you want to avoid in | In Psych conditions |
| Indomethacin( Indocin) cautions with | elderly population |
| Indomethacin( Indocin) AE is high for | CNS adverse effects |
| is sulindac (Clinorel) is a | prodrug |
| drug diclofenac (flexor,cataram,voltaren) if glutathione isn't enough it'll cause | hepatotoxicity |
| diclofenac (flexor,cataram,voltaren) has 2 chlorophyll groups making this drug | very potent |
| Nabumetone (Relafem) is a | non acidic prodrug |
| Nabumetone (Relafem) converts to | an active acidic adding the carboxylic group which is now 6-MNA |
| Ibuprofen has to get metabolized by | CYP2C9 |
| naproxen t1/2 is | 12-15 hours |
| naproxen dose is | twice daily |
| why is it important for oxicam enolate to have a negative charged | to interact with arg120 of COX |
| Piroxicam (Feldene) t1/2 îs | 38hours |
| dose Piroxicam (Feldene) | once daily |
| Piroxicam (Feldene) îs a CYP2C9 metabolize to be | inactivated |
| Meloxicam (Mobic) has | Some COX -2 selectivity at lower doses |
| Meloxicam (Mobic) t1/2 | is 15 - 20 hours |
| dose Meloxicam (Mobic) | once daily |
| Meloxicam (Mobic) îs a CYP2C9 metabolize to be | inactivated |
| the Antidote for over dose on acetaminophen | N acetylcysteine |
| why is folate supplement given with methotrexate | to reduce incidence of MTX related adverse effects |
| methotrexate can increase what enzymes | liver |
Created by:
arcervantes