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MedChem III--stack 5

Part 2 of NSAIDs (starts with fenamates)

Mefenamic Acid (Ponstel) Fenamate derivative
Meclofenamate Sodium (Meclomen) Fenamate derivative, contains 2 ortho position chlorines, less coplanar than mefenamic acid, therefore more potent
Indomethacin (Indocin) Aryalalkanoic acid derivative, inhibits COX enzymes and reduces the motility of polymorphonuclear leukocytes
Indomethacin Sodium Trihydrate (Indocin IV) Arylalkanoic acid derivative, has a 2-position methyl group which makes the phenyl ring non-coplanar with the indole ring, and enhances activity of the compound
Sulindac (Clinoril) Arylalkanoic acid derivative, COX inhibitor, contains a sulfoxide group, which is eventually reduced to sulfide, the active moiety, less SE's than indomethacin
Tolmetin Sodium (Tolectin) Analogue of indomethacin (arylalkanoic acid), contains an indole ring, has the same MOA as indomethacin
Ketorolac Tromethamine (Toradol) Arylalkanoic acid derivative, levorotatory isomer is the more active, more potent than indomethacin, has increased water solubility due to tromethamine salt
Etodolac (Lodine) Arylalkanoic acid derivative, but structure is modified--carboxylic acidgroup is separated by more than 1 carbon from the ring system, inhibits COX, has less SE's
Ketoprofen (Orudis, Oruvail) Profen, inhibits COX, leukotriene biosynthesis, reduces leukocyte migration to inflamed areas, stabilizes lysosomal membranes, may inhibit bradykinin activity
Suprofen (Profenal) Profen, restricted for ophthalmic use, used to prevent miosis during cataract extraction
Flurbiprofen Sodium (Ocufen) Profen, inhibits both COX and motility of leukocytes
Ibuprofen (Motrin, Advil, Nuprin) Profen, contains an aliphatic moiety, S(+) isomer is active, R(-) isomer can be converted to the active S(+)
Fenoprofen Calcium (Nalfon) Profens, both enantiomers are active, inhibits COX, phagocytosis, complement function, and stabilizes lysosomal membranes
Naproxen (Naprosyn) Naproxen Sodium (Anaprox) Profen, contains a fused naphthalene ring system, marketed as S(+) isomer onlyInhibits COX, neutrophil response to chemotaxis, and stabilizes lysosomal membranes, salt is more water soluble, so it reaches peak plasma concentration quicker
Diclofenac (Voltaren) Anthranilic acid derivative, resembles mefenamic acid, and meclofenate sodium, inhibits COX and may affect delay the release of arachidonic acid
Oxazoprin (Daypro) Anthranilic acid derivative, has 2 carbons between the carboxylic group and the aromatic ring, once daily administration
Piroxicam (Feldene) Oxicam derivative, fairly acidic, inhibits both COX and activation of neutrophils, can be dosed once daily
Meloxicam (Mobic) Oxicam, used for anti-inflammatory activity, selective for COX-2 at lower doses, can be dosed once daily
Celecoxib (Celebrex) Selective COX-2 inhibitor, increases incidence of myocardial events, slows the formation of colonic polyps--used as a cancer chemopreventive agent
Nabumetone (Relafen) Nonacidic ketone, analogue of naproxen, inhibits COX (especially COX-2), decreased incidence of GI side effects
Zileuton (Zyflo) Hydroxyurea derivative, inhibit 5-lipoxygenase, used for prevention and symptomatic treatment of asthma, inhibits CYP1A and CYP3A
Zariflukast (Accolate) Leukotriene antagonist, selective, competitive antagonist of cysteine-leukotriene receptors (CYSLT1), used for prevention and long-term management of asthma
Aurthioglucose (Solganal) Gold Sodium Thiomalate (Myochrystine) Gold DMARD, administered IM, variety of toxic effects to the skin, mucous membranes, kidneys, and blood
Auranofin (Ridaura) Gold DMARD, orally effective, better tolerated than parenteral gold preparations, thought to inhibit lysosomal enzymes and reduce the immune response
Created by: 100000197460889