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MedChem III--stack 5
Part 2 of NSAIDs (starts with fenamates)
Drug | Description |
---|---|
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 |