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83 Cards in this Set
- Front
- Back
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What is Celecoxib?
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Celecoxib (Celebrex)
Selective COX-2 inhibitor Sulfa allergy due to Sulfonamide side chain Generally safe on GI |
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What is Zileuton?
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Zileuton (Zyflo)
5-LOX Inhibitors Block CysKT series synthesis, which mediate airway inflamation Adjunctive anti-asthmatic medications |
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What is Montelukast?
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Montelukast (Singulair)
CysLT Receptor Blocker Given for asthma prophylaxis, NOT acute asthma attack |
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What is Zafirlukast?
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Zafirlukast (Accolate)
CysLT Receptor Blocker Given for asthma prophylaxis, NOT acute asthma attack |
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What is Acetaminophen?
Max dose? Antidote? |
Acetaminophen (Tylenol)
Non-Salicylate Not anti-inflammatory No sulfa Weak inhibitor of COX Has more of a Central action or blocking PGs transmission of pain signals to hypothalamus Max Dose= 4g/ day Toxic effects: skin rash, hepatic damage, renal tubular necrosis Antipyretic of choice in children N-acetylcysteine is antidote in poisoning |
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Name the Acidic-Enolic Acids
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Oxicams:
Piroxicam (Feldene) Meloxicam (Mobic) |
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What is Piroxicam?
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Piroxicam (Feldene)
Acidic-Enolic Acid Contain sulfa groups, if allergic switch to propionic acids COX-1 and COX-2 inhibitor |
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What is Meloxicam?
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Meloxicam (Mobic)
Acidic-Enolic Acid Contain sulfa groups, if allergic switch to propionic acids COX-1 and COX-2 inhibitor |
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What is Meclofenamate Na?
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Mefenamic Acid (Meclomen)
Fenamic Acid Derivative considered Acidic-Carboxylic Acid |
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What is Sulindac?
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Sulindac (Clinoril)
NSAID Prodrug; contains sulfa atom Liver=active sulfide metabolite Kidney= inactive sulfone metabolite Advantage: used in kidney impaired patients (dosed BID) |
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What is Indomethacin?
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Indomethacin (Indocin)
Most potent NSAID considered Acidic-Carboxylic Acid Acetic Acid CNS dysfunction commonly prescribed for gout attack (don't use SR form) Uses: Gout and Patent Ductus Arteriosus |
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What is Tolmetin sodium?
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Tolmetin sodium (Tolectin)
considered Acidic-Carboxylic Acid |
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What is Diclofenac sodium?
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Diclofenac sodium (Voltaren, Cataflan)
considered Acidic-Carboxylic Acid Sodium salt= Voltaren Potassium salt= Cataflan Caution: monitor FLTs |
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What is Ketorolac?
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Ketorolac (Toradol)
Acetic Acid indicated used only as a peripheral analgesic for short term (max 5 days) prolonged use causes kidneys to shut down |
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What is Etodolac?
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Etodolac (Lodine)
ACIDIC=Carboxylic Acid Pyranocarboxylic acid Less GI upset |
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What is Naproxen?
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Naproxen (Naprosyn)
Propionic Acid Long t1/2 |
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What is Flurbiprofen?
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Flurbiprofen (Ansaid)
Propionic Acid NSAID |
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What is Ibuprofen?
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Ibuprofen (Motrin, Advil)
Propionic Acid First NSAID available OTC; contains isobutyl substitute Max Dose: 1.2 g/ day |
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What is Naproxen Sodium?
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Naproxen Sodium (Anaprox, Aleve)
Propionic Acid Long t1/2 Aleve= 220mg Naproxen= 200mg |
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What is Ketoprofen?
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Ketoprofen (Orudis)
Propionic Acid derivative contains ketone group give to patients allergic to sulfa |
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What is acetylsalicylic acid?
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acetylsalicylic acid (Aspirin)
1st NSAID discovered Salicylic Acids- Salicylates Irreversible COX-1 and COX-2 inbhibitor acetyl group= blood thinning salicylate anion= active moiety Uses: analgesic, antipyretic, anti-inflammatory, and anti-platelet Contraindicated in asthma (LT synthesis may increase) and child with fever (Reyes) |
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What is Salsalate?
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Salsalate (Disalcid)
Salicylic Acids- Salicylates DOES NOT contain acetyl group less GI irritation no effect on platelets take with full glass of water |
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What is Diflunisal?
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Diflunisal (Dolobid)
Salicylic Acids- Salicylates structurally related to salicylates but not an ester of salicylic acid USES: analgesic, anti-inflammatory, but NOT antipyretic Long t 1/2 (BID dosing) |
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What is Mesalamine?
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Mesalamine (Asacol, Pentasa, Rowasa)
Salicylic Acids- Salicylates local effects for inflammatory bowel disease, crohn's disease, and ulcerative colitis forms: enteric coated or enema |
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What is Sulfasalazine?
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Sulfasalazine (Azulfidine)
NSAID Salicylic Acids- Salicylates Prodrug; active moiety is mesalamine Also DMARD in treating RA; last line treatment of RA; also used to treat ulcerative colitis and Crohn's desease |
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What is Gemeprost?
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Gemeprost
PGE1 analog |
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What is Misoprostol?
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Misoprostol (Cytotec)
PGE1 analog Used in medical abortion (with mifepristone-RU486); also used in gastric protection in patients treated with NSAIDs |
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What is Alprostadil?
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Alprostadil (Caverject)
PGE1 analog Used in ED as intracarvenosal injection and maintenance of patent ductus arteriosus |
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What is Dinoprostone?
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Dinoprostone
PGE2 analog Oxytocic-Labor induction |
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What is Carboprost?
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Carboprost
PGF2 alpha analog used in post-partum hemorrhage (uterine bleeding, menorrhagia) |
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What is Latanoprost?
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Latanoprost (Xalantan)
PGF2 alpha analog Eye drops for open-angle glaucoma; increases blood aqueous humor outflow outside from the eye bulb |
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What is Bimatoprost?
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Bimatoprost (Lumigan)
PGF2 alpha analog Eye drops for open-angle glaucoma; increases blood aqueous humor outflow outside from the eye bulb used in cosmetics as latisse for eyelash enhancement |
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What is Epoprostenol?
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Epoprostenol (Remodulin)
PGI2 analog USE: PAH injection |
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Okay to take Aspirin with food or milk?
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YES. helps reduce SE and should be taken with 1-2 large glasses of water
enteric coated products also available |
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What is the #1 recommended drug for OA?
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Acetaminophen (Tylenol)
Max= 1 gram 3-4 times daily prn if on warfarin max= 2 g/ day USE: Osteoarthritis |
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What is the most potent NSAID?
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Indomethacin (Indocin)
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What is the first NSAID discovered?
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Aspirin (ASA)
USE: Osteoarthritis |
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What is Tramadol?
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Tramadol (Ultram, Tramal)
Non-narcotic opiod analgesic MOA: affects 5HT, GABA, and NA systems in the CNS can cause CNS depression especially with alcohol Serotonin syndrome with MAOIs and SSRIs very low risk for dependency/addiction USE: Osteoarthritis |
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What is Triamcinolone acetonide?
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Triamcinolone acetonide (Kenalog)
Corticosteroid used to treat osteorthritis; only used as topical agents via direct intra-articular injection; short term relief; onset takes >24 hours; combine with local anesthetic for immediate relief USE: Osteoarthritis |
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What is Methylprednisolone acetate?
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Methylprednisolone acetate (Depo-Medrol)
Corticosteroid used to treat osteorthritis; only used as topical agents via direct intra-articular injection; short term relief; onset takes >24 hours; combine with local anesthetic for immediate relief USE: Osteoarthritis |
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What is Capsaicin?
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Capsaicin (Qutenza patch)
Depletes Substance P, TRPV1 agonist; only used as topical agent; potent skin and mucosal irritant USE: Osteoarthritis |
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What is Lidocaine?
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Lidocaine
local anesthetic and anti-arrhythmic (Class 1B) USE: Osteoarthritis |
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What are Glucosamine and Chondroitin?
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Glucosamine and Chondroitin are Hyluronic Acid Derivatives
NOT drugs components of natural joint cartilage; trophic and lubricant for joints, serve to nurture the joint bones |
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Drugs Classes used to treat Rheumatoid arthritis
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1. Salicylates and NSAIDS
2. Corticosteroids 3. Disease Modifying Anti Rheumatic Drugs (DMARDS) 4. Biologic Response Modifiers (BRMs) |
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What is prednisone?
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Prednisone (Deltasone)
Corticosteriod used for Rheumatoid Arthritis anti-inflammatory and immunosuppressive effects MOA: inhibit leukotriene and prostaglandin synthesis, generalized leukocyte and lymphocyte suppression adverse effects if given systemically: osteoporosis, cataracts, glaucoma, NA and fluid retention, edema, HT, risk of infections, neurological symptoms |
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What is Methylprednisolone?
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Methylprednisolone (Medrol)
Corticosteriod used for Rheumatoid Arthritis anti-inflammatory and immunosuppressive effects MOA: inhibit leukotriene and prostaglandin synthesis, generalized leukocyte and lymphocyte suppression adverse effects if given systemically: osteoporosis, cataracts, glaucoma, NA and fluid retention, edema, HT, risk of infections, neurological symptoms |
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Name the short acting Glucocorticoids
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1. Cortisone
2. Hydrocortisone |
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Name the Intermediate acting Glucocorticoids
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1. Prednisone
2. Prednisolone 3. Triamcinolone 4. Methylprednisolone |
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Name the Long acting Glucocorticoids
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1. Dexamethasone
2. Betamethasone |
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Name the Disease Modifying Anti-Rheumatic Drugs (DMARDs)
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Hydroxychloroquine
Azathioprine Methotrexate Sulfasalazine Doxycycline Minocycline Leflunomide |
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What is Penicillamine?
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Penicillamine (Depen, Cuprimine)
NOT an antibiotic, just a by product of penicillin hydrolysis; used to treat Wilson's disease (Elevated Cu levels) MOA: inhibit collagen formation, inhibit T lymphocyte function, decrease IgM Rheumatoid Factor levels in synovial fluid |
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What is Hydroxychloroquine?
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Hydroxychloroquine (Plaquenil)
DMARD used to treat RA, Lupus, and Malaria MOA: inbhibits chemotaxis of leukocytes, macrophages, and eosinophils, inhibits prostaglandin effects Adverse effects: Ocular Toxicity (irreversible) |
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What is Azathioprine?
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Azathioprine (Imuran)
DMARD used to treat RA Purine synthesis inhibitor MOA: inhibits nucleic acid synthesis-immune cell proliferation; metabolized to 6-MP, which is converted to TIMP that gets incorporated into nascent DNA strand and stops DNA synthesis; G-MP metabolized by XO Caution: must reduce the dose of Azathioprine or 6-Mercaptopurine to 1/4 original dose when given with allopurinol b/c severe life threatening bone marrow suppression Pregnancy category D |
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What is Methotrexate?
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Methotrexate (MTX, Rheumatrex)
DMARD used for RA Gold standard for RA structural analog of folic acid (folate antagonist) MOA: irreversibly blocks DHFR preventing reduction to active tetrahydrofolate; blocks pyrimidine sysnthesis (DNA/RNA) cell proliferation Macrophage activation is also inhbited Side effects: bone marrow suppression damage, damage to GI mucosa, and skin rash/alopecia |
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What is Sulfasalazine?
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Sulfasalazine (Azulfidine)
DMARD Last line treatment for RA Primary use: ulcerative colitis and crohn's disease MOA: sulfapyridine moiety |
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What is Doxycycline?
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Doxycycline (Doryx, Vibramycin)
Tetracycline Class DMARD used for RA antibiotics-bacterial protein synthesis inhibitors; decreases collagenase activity and bone resorption |
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What is Minocycline?
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Minocycline (Minocin)
Tetracycline Class DMARD used for RA antibiotics-bacterial protein synthesis inhibitors; decreases collagenase activity and bone resorption |
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What is Leflunomide?
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Leflunomide (Arava)
DMARD used for RA immunomodulatory-immuosuppressive agent MOA: inhibits DHODH, blocks pyrimidine (DNA and RNA) synthesis-immune cell proliferation Caution: increases liver enzymes; LFT needed; pregnancy category X |
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What is Infliximab?
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Infliximab (Remicade)
Biologic Response Modifiers Monoclonal antibody against TNF alpha; binds it and prevents it from activating its receptor human-mouse chimeric Ab therefore immunogenic IV only immunosuppressive |
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Name the Biologic Response Modifiers used to treat RA
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1. Infliximab
2. Etanercept 3. Adalimumab 4. Certolizumab 5. Golimumab 6. Anakinra 7. Rituximab 8. Abatacept 9. Tocilizumab 10. Belimumab |
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What is Etanercept?
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Etanercept (Enbrel)
Biologic Response Modifier (BRM) used for RA Soluble form of TNF alpha receptor; binds and sequesters TNF alpha and does not allow it to bind and activate its endogenous membrane receptor SC once or twice weekly very low risk for immunogenicity risk of immunosuppressive infections USE: RA |
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What is Adalimumab?
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Adalimumab (Humira)
Biologic Response Modifier (BRM) Monoclonal antibody against TNF alpha; binds TNF alpha directly and prevents it from activating its receptor Fully humanized Ab, no risk for immunogenicity SQ only once biweekly USE: RA |
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What is Certolizumab?
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Certolizumab (Cimzia)
Biologic Response Modifier (BRM) Monoclonal antibodies against TNF alpha USE: RA |
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What is Golimumab?
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Golimumab (Simponi)
Biologic Response Modifier (BRM) Monoclonal antibodies against TNF alpha USE: RA |
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What is Anakinra?
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Anakinra (Kineret)
Biologic Response Modifier (BRM) Recombinant IL-1R antagonist fully humanized; analog of natural sIL-1R SC once daily risks of serious infections; coadministration with TNF alpha blocker contraindicated |
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What is Rituximab?
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Rituximab (Rituxan)
Biologic Response Modifier (BRM) Anti-CD20 chimeric monoclonal antibody; CD20 important cell surface receptor for B cell activation; blocks B cell proliferation, activation, delpetes B cells IV once biweekly for RA risk of serious infections; DO NOT administer with TNF alpha blocker |
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What is Abatacept?
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Abatacept (Orencia)
Biologic Response Modifier (BRM) Recombinant CTLA4-IgG1 fusion protein important cell surface receptor for T cell activation; blocks T cell proliferation-activation IV for RA Risk of serious infections; DO NOT give with TNF alpha blocker or Anakinra |
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What is Tocilizumab?
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Tocilizumab (Actemra)
Biologic Response Modifier (BRM) Recombinant humanized anti-IL-6R antibody; IL-6 the third most important pro-inflammatory immunoactivating cytokine after TNF alpha and IL-1 risk of serious infection; DO NOT give with other BRMs |
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What is Belimumab?
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Belimumab (Benlysta)
Biologic Response Modifier (BRM) Fully humanized recombinant anti-BlyS monoclonal antibody; BlyS is a powerful B cell stimulator, so Belimumab blocks B cell activation Approved for SLE, not yet for RA |
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What are 4 ways to treat acute gout attacks?
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1. Colchicine
2. NSAIDs 3. Corticosteroids 4. ACTH |
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What is Colchicine?
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Colchicine (Colcrys)
Anti-inflammatory NOT analgesic or uricosuric agent MOA: inhibits assembly of microtubules, preventing polymerization, blocking cell proliferation and causing: 1.inhibition of leukocyte migration 2. inhibition of cell mitosis 3. decreases kinin and leukotrienes= decreased inflammation OD= bloody diarrhea, shock, hematuria, and fatal CNS depression |
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What is Indomethacin?
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Indomethacin (Indocin)
MOA: inhibis COX-1 and COX-2 and also inhibits urate crystal phagocytosis agent most used today to treat gout highest potential for CNS dysphoria/dysfunction |
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What Corticosteroids are used in Gout
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Prednisone and Triamcinolone
anti-inflammatory and immunosuppressive |
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How does ACTH help with Gout?
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Adrenocorticotropic hormone (ACTH)
stimulates glucocorticoid synthesis |
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Name the Uricosurics?
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Probenacid
Sulfinpyrazone |
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What is Probenacid?
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Probenacid (Benamid)
Uricosuric- completes with URAT1 in proximal tubule to decrease the net reabsorption or uric acid is an organic acid so it competes with other acids like salicylates... ASA is contraindicated Drink Lots of water Do NOT take lots of Vitamin C NO alcohol useless in renal insufficiency |
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What is Sulfinpyrazone?
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Sulfinpyrazone (Anturane)
Uricosuric- completes with URAT1 in proximal tubule to decrease the net reabsorption or uric acid is an organic acid so it competes with other acids like salicylates... ASA is contraindicated Drink Lots of water Do NOT take lots of Vitamin C NO alcohol useless in renal insufficiency |
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What is Allopurinol?
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Allopurinol (Zyloric, Zyloprim)
MOA: Inhibit xanthine oxidase= reduces uric acid formation xanthine analog- a suicide inhibitor of XO XO metabolizes 6-MP drugs therefore reduce dose of these drugs to 1/4 or else fatal bone marrow suppression will develop interferes with TMPT phenotyping in oncologic treatments; drug interaction with warfarin and theophylline |
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What is Feboxustat?
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MOA: Inhibit xanthine oxidase= reduces uric acid formation
non-xanthine XO inhibitor- lacks drug interactions |
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Name the XO inhibitors used in Gout
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Allopurinal (Zyloric)
Febuxostat (Uloric) |
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Name the Uricases used to treat RA?
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1. Rasburicase (Elitek)
2. Pegloticase (Krystexxa, Puricase) |
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What is Rasburicase?
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Rasburicase (Elitek)
Recombinant urate oxidase enzyme; converts urate to allantoin (very water-soluble and no propensity for crystal formation) Can be immunogenic |
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What is Pegloticase?
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Pegloticase (Krystexxa, Puricase)
PEGylated porcine uricase; converts urate to allantoin (very water-soluble and no propensity for crystal formation) far less immunogenic than rasburicase and with improved bioavailability |
