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136 Cards in this Set
- Front
- Back
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At what phase is glucocorticoids effective in RA |
Early Phase |
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NSAID that is not acidic |
Nabumetone |
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Aspirin antiplatelet dose |
81-325mg |
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Days that aspirin inhibits platelet cox |
8-10 days |
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Aspirin duration of effect on cox other than platelet cox |
6-12 hours because synthesis of new COX replaces the inactivated enzyme |
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Uses of aspirin |
Decrease incidence of TIA Unstable Angina Coronary Artery Thrombosis with MI Thrombosis after CABG |
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Nonacetylated salicylates |
Magnesium Choline Salicylate Sodium Salicylate Salicyl Salicylate |
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Use of Nonacetylated Salicylates |
Px with asthma, bleeding tendencies and with renal dysfunction (Does not inhibit platelet aggregation) |
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Dose of nonacetylated salicylates |
3-4g/day |
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Location of COX-1 |
GI, Kidney, Platelet |
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Withdrawn cox-2 inhibitors because of CV thrombotic events |
Rofecoxib Valdecoxib |
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This drug interferes with celecoxib |
Warfarin (CYP2C9) |
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Meloxicam lowest therapeutic dose |
7.5mg/d |
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Phenylacetic acid derivative NSAID |
Diclofenac |
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Diclofenac + ______ = Diarrhea |
Misoprostol |
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Diclofenac + ________ = renal adverse effects |
Omeprazole |
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Dose of diclofenac that impairs renal blood flow and gfr |
150mg/d |
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Uses of diclofenac |
0.1% ophtalmic prep for prevention of post-op inflammation For intraocular lens implantation and strabismus surgery 3% gel solar keratoses Rectal supp for preemptive analgesia and post-op nausea |
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Diflunisal Use |
RA 500-1000mg daily in 2 divided doses (Rarely used today) |
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A racemic acetic acid derivative with an intermediate half life |
Etodolac |
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Analgesic dosage of etodolac |
200-400mg 3-4x daily |
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Dose of etodolac for OA and RA |
300mg 2-3x a day up to 500mg 2x a day initially followed by a maintenance of 600mg/d |
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A proprionic acid derivative with a possibly more complex mechanism of action than other NSAIDs |
Flurbiprofen |
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MOA of S(-) enantiomer of flurbiprofen |
Inhibits cox nonselectively Affect tnf-a and nitric oxide synthesis |
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Uses of flurbiprofen |
Topical ophthalmic-inhibition of perioperative miosis IV- perioperative analgesia in minor ear, neck, and nose surgery Lozenge- sore throat |
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Dose of ibuprofen equal to anti inflammatory effect of 4g of aspirin |
2400mg daily |
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Dose of ibuprofen in which it is analgesic but not anti inflammatory |
<1600mg/d |
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Uses of ibuprofen |
Oral and IV- closing of PDA (same effectiveness with indomethacin) Topical- primary knee OA (absorbed by muscle and fascia) Liquid gel 400mg- postsurgical dental pain |
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Why is ibuprofen better than indomethacin |
Decreases urine output less Less fluid retention |
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Contraindication of ibuprofen |
Nasal polyps Angioedema Bronchospastic reactivity to aspirin |
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Ibuprofen + aspirin = |
Antagonism of platelet inhibition Decreased anti-inflammatory effect |
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Effects of indomethacin |
Nonselective cox inhibition Inhibits phospholipas A and C Reduce neutrophil migration Decrease T-cell and B-cell proliferation |
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Propionic acid derivative that inhibita both COX and LOX |
Ketoprofen |
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Concurrent administration of _________ elevates ketoprofen levels |
Probenecid |
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Dosage of ketoprofen |
100-300mg/d |
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Nabumetone resembles what drug structure |
Naproxen |
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Half-life of nabumetone |
More than 24 hrs |
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Propionic Acid derivative NSAID with longest half-life |
Oxaprozin |
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Half life of Oxaprozin |
50-60 hours |
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Effects of piroxicam |
Nonselective COX inhibition Inhibits PMN leukocyte migration Decrease O2 radical production Inhibits lymphocyte function |
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Dose of piroxicam associated increased risk of peptic ulcer and bleeding |
>20mg/d |
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DOA of sulindac |
12-16 hrs |
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Half life of tolmetin |
1-2 hours |
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NSAIDs with greatest toxicity |
Tolmetin Indomethacin |
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Least toxic NSAIDs |
Salsalate Aspirin Ibuprofen |
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NSAID best for renal unsufficient patients |
Nonacetylated salicylates |
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NSAIDs associated with more liver function test abnormalities |
Diclofenac Sulindac |
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NSAID safest for px with high risk of GI bleeding but with higher risk for CV toxicity |
Celecoxib |
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What drugs can be added to augment the GI effect of NSAIDs |
Omeprazole or Misoprostol |
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How to choose NSAID |
Balance of efficacy Cost-effectiveness Safety and Numerous personal factors like other drugs being used, concurrent illness, and or compliance |
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Time before effect of DMARDs may become clinically evident |
2 weeks to 6 months |
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Enumerate csMARDS (conventional synthetic) |
Small molecule (MACCCLMS) Methotrexate Azathioprine Chloroquine and HCQ Cyclophosphamide Cyclosporine Leflunomide Mycophenolate Mofetil Sulfasalazine |
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Only targeted synthetic DMARD (tsDMARD) |
Tofacitinib |
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Enumerate bDMARDS |
Abatacept (T-cell modulator) Rituximab (B-cell cytotoxic) Anti-IL6 (tocilizumab) Anti IL-1 (anankira, rilonacept, canakinumab) TNF a -5 drugs |
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MOA of abatacept |
Inhibits activation of T-cells by binding to CD80 and 86, preventing the binding to CD28 |
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Dose of abatacept for RA |
Intravenous Day 0, week 2, week 4 followed by mothly infusion >60kg -500mg 60-100kg-750mg <100kg- 1000mg |
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Dose of Abatacept for JIA |
Intravenous Day 0, week 2, week 4, followed by monthly infusion 6-17 years old and <75kg- 10mg/kg 75-100kg- 750mg >100-1000mg |
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Half life of abatacept |
13-16 days |
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Dose of subcutaneous abatacept |
125mg once weekly |
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Time wherein most patients respond to abatacept after initiation of tx |
12-16 weeks |
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Drug with equivalent effect of abatacept |
Adalimumab |
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How to use abatacept in px with moderate-severe PJIA |
Monotherapy or in combi with MTX or other DMARD |
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Abatacept + Methotrexate = |
Achieving minimal disease activity as early as 2 months Significantly inhibiting radiographic progression at 1 year Improving patients physical function and symptoms |
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Other uses of Abatacept aside from RA and JIA |
SLE Sjogren syndrome Type 1 DM IBS Psoriasis vulgaris Psoriatic arthritis |
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Abatacept is most benefial to px with ______? Not RA or JIA |
Psoriatic Arthritis |
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Side effect of Abatacept |
Slight increased risk of infx (URTI, UTI) |
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Diseases to be screened before starting abatacept |
Latent TB and viral hepatitis |
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What should not be initiated while undergoing abatacept treatment? |
Vaccinations up to 3 months after termination |
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MOA of azathioprine |
Metabolized to 6-thioguanine which inhibits Inosinic acid synthesis B cell and T cell function Ig production IL 2 secretion |
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Production of 6-thioguanine from azathioprine is dependent on what enzyme |
Thiopurine Methyltransferase (TPMT) |
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Deficiency of TPMT are at high risk to |
Myelosuppression by excess concentrations of the parent drug |
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Dose of Azathiprine for RA |
2mg/kg/day |
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Azathioprine is indicated for px with |
RA Kidney transplant PA Reactive Arthritis Polymyositis SLE Maintenance of remission in vasculitis Behcet disease Scleroderma (less effective than cyclophosphamide) |
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Azithioprine toxicity |
Bone marrow suppression GI disturbances Increased risk of infx Lymphomas Rare: Fever Rash Hepatotoxicity signal acute allergic reactions |
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MOA of Chloroquine and Hydroxychloroquine |
Suppression of t-lymphocyte responses to mitogens Inhibition of leukocyte chemotaxis Stabilization of lysosomal enzymes Processing through the Fc-receptor Inhibition of DNA and RNA synthesis Trapping of free radicals |
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Percent of CQ or HCQ bound to protein |
50% |
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Drugs that are extensively tissue bound particularly in the melanin-containing tissues such as the eyes |
Chloroquine and Hydroxychloroquine |
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Half life of CQ and HCQ |
45 days |
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Dose of HCQ for RA |
Up to 6.4mg/kg/day |
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Dose of CQ for RA |
200mg/day |
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Time for RA to respond to CQ and HCQ |
3-6 months |
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Other uses of CQ and HCQ |
SLE Sjogren |
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Effect of CQ and HCQ in px with SLE |
Decreased mortality and skin manifestations, serositis, and joint pains of SLE |
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Dose of CQ and HCQ at which ocular toxicity occurs |
250mg/day - CQ >6.4mg/kg/day- HCQ |
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Opthalmologic monitoring for px taking CQ and HCQ should be every ____ |
12 months |
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Other toxicities of CQ and HCQ |
Dyspepsia Nausea Vomiting Abdominal Pain Rashes Nightmares |
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True or False: CQ and HCQ is safe for pregnant women |
TRUE |
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MOA of cyclophosphamide |
Converted to phosphoramide mustard which cross links DNA to prevent cell replication T-cell and B-cell suppression (30-40%) |
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What correlates with clinical response in rheumatic diseases? |
T cell suppression |
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Dose of cyclophosphamide |
2mg/kg/day |
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Cyclophosphamide is used to treat ___ |
SLE Vasculitis Wegeners granulomatosis |
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MOA of cylclosporine |
Inhibits IL-1 and IL-2 production Inhibits macrophage-t-cell interaction and t-cell responsiveness T-cell-dependent B-cell function is also affected |
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What increases bioavailability of cyclosporine? |
Grapefruit juice (CYP3A) |
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% by which grapefruit juice increases the bioavailability of cyclosporine |
62% |
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Cyclosporine is approved for |
Tx of RA and retards appearance of new bony erosions |
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Dosage of cyclosporine |
3-5mg/kg/day divided into two doses |
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Uses of cyclosporine |
RA SLE Polymyositis and Dermatomyositis Wegeners granulomatosis Juvenile chronic arthritis Refractory eye involvement im behcets disease |
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Common side effects of cyclosporine |
Leukopenia Thrombocytopenia Anemia (lesser extent) |
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High doses of cyclosporine will result to |
Cardiotoxicity and Neurotoxicity Sterility (chronic) especially women |
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A peptide antibiotic but is considered a csDMARD |
Cyclosporine |
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True or False: Cyclosporine is a peptide antibiotic but is considered a bDMARD |
False: csDMARD |
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Active metabolite of leflunomide |
A77-1726 |
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MOA of leflunomide |
converted to A77-1726 which inhibits dihydroorotate dehydrogenase, leading to a decrease in ribonucleotide synthesis and the arrest of stimulated cells in G1. Inhibits T-cell proliferation Reduces production of autoantibodies by B cells Secondary effects: Increased IL-10 receptor mRNA decreased IL-8 receptor type A mRNA, decreased TNF-a-dependent NF-KB activation |
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Half life of leflunomide |
19 days |
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Half life of metabolite of leflunomide |
19 days and is subject to enterohepatic recirculation |
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What enhances leflunomide excretion and increase total clearance by 50%? |
Cholestyramine |
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T or F: Leflunomide is as effective as methotrexate in RA |
True, including inhibition of bony damage |
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Side effects of leflunomide |
Diarrhea (25% (3-5 stop)) Liver enzyme elevation Mild alopecia Weight gain Increase BP |
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True or False: Leflunomide is safe for pregnant women |
False |
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First-line csDMARD for treating RA |
Methotrexate |
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csDMARD used in 50-70% of patients with RA |
Methotrexate |
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A synthetic nonbiologic antimetabolite used for the treatment of RA |
Methotrexate |
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MOA of methotrexate |
Inhibition of AICAR tranformylase and thymidylate synthetase. Leading to accumulation of AMP which is converted to adenosine, a potent inhibitor of inflammation. |
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Route of administration of methotrexate |
SC or IM |
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Half-life of methotrexate |
6-9 hours |
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What drug increases the tubular reabsorption of methotrexate? |
Hydroxychloroquine |
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What drug decreases the clearance of methotrexate? |
Hydroxychloroquine |
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Starting dose of methotrexate |
7.5mg weekly |
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Dosing regimen of methotrexate for RA |
7.5mg weekly then increased to 15-25mg weekly (increased effect up to 30-35mg) |
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Effect of methotrexate to RA |
decreases the rate of appearance of new erosions |
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Methotrexate is used in what diseases? |
RA Psoriasis PA AS Polymyositis Dermatomyositis Wegners granulomatosis Giant cell arthritis SLE Vasculitis |
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Most common toxicities of MTX |
Nausea and mucosal ulcers |
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Other side effects of MTX aside from nausea and mucosal ulcers |
Leukopenia Anemia Stomatitis GI ulcerations Alopecia |
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MTX is safe for pregnant women: T or F |
false |
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Active form of mycophenolate |
Mycophenolic acid |
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MOA of mycophenolate |
Converted to mycophenolic acid which suppresess T- and B-lymphocyte proliferation Inhibits E-selectin, P-selectin, and ICAM-1 |
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Indication of mycophenolate |
Treatment of renal disease due SLE and may be useful in vasculitis and Wegener's granulomatosis |
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Dose of Mycophenolate to treat RA |
2g/d (not sure if effective) |
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A chimeric monoclonal antibody biologic agent that targets CD20 B-lymphocyte |
Rituximab |
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MOA of rituximab |
Targets CD20 B-lymphocyte which reduces inflammation by decreasing the presentation of antigens to T lumphocytes and inhibits the secretion of pro-inflammatory cytokines |
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Dose of rituximab |
2 IV infusions of 1000mg separated by 2 weeks, may be repeated every 6-9 months, as needed. |
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Before treating patients with rituximab what should be given |
Acetaminophen Glucocorticoid (usually methylprednisolone 100mg) Antihistamine |
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Indications of Rituximab |
Tx for moderate-severe RA in combi with MTX in patients with and inadequate response to one or more TNF a antagonists Tx of adult patients with wegeners granulomatosis, microscopic polyangitis, and vasculitis in combi with glucocorticoids |
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Rituximab is associated with reactivation of what virus? |
HBV |
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Rituximab has been associated with TB and lymphoma: T or F? |
False |
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Patients taking rituximab needs CBC monitoring every? |
2-4 months in RA patients |
