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59 Cards in this Set
- Front
- Back
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What are two Gold Preparation drugs?
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Gold Sodium Thiomalate and Auroanofin
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What is Gold Sodium Thiomalate used for?
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Supresses or prevents arthritis and synovitis
Used for RA for Pts. who are not getting satisfactory results from NSAIDs |
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What is the MOA of Gold Sodium Thiomalate?
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May inhibit the maturation and function of mononuclear phagocytes (the things destroying the tissue)
And decreases the concentrations of Rheumatoid Factor and Immunoglobulins in Pts who have RA Immunosuppresion |
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How is Gold Sodium Thiomalate given and how is it metabolized/excreted?
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Usually given by IM but is available by PO
It is highly bound to plasma (95%), and has a long T 1/2, which becomes longer with continued dosing Excreted by the kidney |
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What are the side effects of Gold Sodium Thiomalate?
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Erythema (redness of the skin due to congested capilaries) to severe Exfoliative Dermatitis
Stomatitis, Pharyngitis, Trachxetis, Gastritis, Colitis, Vaginitis, Glossitis Preteinuria, Hematuria, Nepxrosis, Glomerulonphritis (reversible) Thrombocytopeni, Lecopenia, Agranulocytosis, Aplastic Anemia (Rare but usually fatal) A lot risks b/c it is an immunosupresent >chance of infection |
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What are the Contraindications of Gold Sodium Thiomalate?
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Renal Disease*
Hepatic dysfunction History of Hematological disorders During Pregancy or breast feeding Poorly tolerated by the elderly |
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What are two antimalarials?
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Hydroxychloroquine and Chloroquine
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What are Antimalarials used for?
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RA and Lupus Erythematosus with Pts. who have not responded to NSAIDs
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What is the MOA of the Antimalarials?
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Unknown but thought to be due to stabilization of Leukocyte Membranes
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How are Antimalarials Metabolized?
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Well absorbed following PO, but even faster with IM or SC
Extensive biotransformation Excreted by the kidney |
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What are the side effects of of Antimalarial drugs?
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More severe then when given for Malaria b/c higher doses are given
Retinal Damage (irreversible), CNS (nervousneess, vertigo, convulsions, ataxia), Extraoccular muscle palsies, Blood Dycrasias (Insepcified disorder of the blood, GI |
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What is the use and Mechanism of Penicillinamine?
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Mainly used for Heavy metal poisening but also for Severe RA
It is an Immunosupressive |
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What are the side effects of Penicllinamine?
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GI, Hematologic (aplastic anemia), and Dermatologic
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What are the two cytoxic drugs?
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Methotrexate (the GOLD standard) and Leflunomide
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What is Methotrexate used for and what is its MOA?
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This is the gold standard for DMARDs, it is used for severe, active RA
Immunosuppresor that inhibits the replication and the function of T cells and possibly B cells b/c of a relatively selective action on the DNA synthesis (Dihydrofolate inhibitor) |
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What are the side effects of Methotrexate?
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Hepatic fibrosis and cirrhosis (liver function) and Acute or chronic nonseptic pneumonitis
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What is the MOA of Leflunomide?
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Dihydroorotate inhibitor, with antiproliferative activity an Anti-Inlammatory activity
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What can Leflunomide be used with?
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May be combined with NSAIDs and/or Low dose corticosteroids
Use w/ other DMARDs has NOT been studied (so dont do it) |
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What are the side effects of Lefulnomide?
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Hepatotoxicity and potenially teratogenic effects
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What is the MOA of Azathioprine and what is it used for?
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Immunosuppressive
Severe Refractory RA (HIV?) |
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What are the side effects of Azathioprine?
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Leukopenia, Thrombocytopenia and GI (weak; nausea and vomiting)
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What are the 4 Immunologic Agent drugs and how are they all given and what is the cost?
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Etanercept, Infliximab, Adalimumab, Anakinera
All injectibles and very expensive due to production costs |
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What is the use of Etanercept and how is it given?
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For severe RA, that has been refractory to Methotrexate, may be given in combination with Methotrexate, also used for Active Ankylosing Spondylitis
Given 2 injections/week (6 month supply is $10,000) |
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What is the MOA of Etanercept?
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Binds to and inactivates TNF
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What are the side effects of Etanercept?
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Respiratory infection (common), headache, rxn at injection site, Rhinitis, Potential formation of autoimmune ABs
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What is Infliximab used for?
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Severe, active RA that is refractory to Methotreaxate
UNIQUE in that it also treats Crohns Disease |
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What is the MOA of Infliximab?
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Binds to and inactivates TNF-Alpha
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What are the side effects of Infliximab?
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Serious infection (b/c of the immunosuppresion), Hematologic (especially pancytopenia b/c possibly fatal)
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What is the Warning/ADR given from the FDA regarding TNF blockers?
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7 fold increase in the incidence of Lymphoma
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What is the MOA, ADR and use for Adalimumba?
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Another version of of the TNF-Alpha inhibitor/inactivator
Side effects similar to Infliximab Used for Severe RA and Active Crohn's disease |
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What is the use for Anakinra?
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Used for severe, active RA
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What can Anakinra be used with and what can it NOT be used with?
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In conjunction with Methotreate and other DMARDs
DO NOT use in conjunction with other Immunologic agents (i.e. Etanercept o drugs ending in -mab) due to life threatening infection b/c of total immune suppresion |
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What is the MOA of Anakinra?
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Competitively inhibits IL-1 binding
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What are the side effects of Anakinra and what is the biggest of these contraindications?
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Seriuos infection (40%) and injection site rxn (70%), THE BIG ONE is not to use concurrently with live vaccines
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What are the two Uricosuric Agents and what are they used for?
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Probenicid and Sulfinpyrazone
To Treat renal gout |
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What are the uses of Probenicid?
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To treat renal gout
Also used to increase the T 1/2 of Penicillin |
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What is the MOA of Probenicid?
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Increases excretion of Uric Acid by inhbiting the reabsorbtion or Urate in the PCT
Inhibits the transport of organic acids across the renal tubule |
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How are the final concentration of substances in urine measured?
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Degree of filtration and degree of reabsorbtion
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What is the metabolism of Probenicid?
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Completely absorbed after oral administration, highly bound to plasma proteins
Completely REabsorbed by renal tubules Metabolized VERY slowly by liver, hence long lasting and NO extensive dosing needed |
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What are the side effects of Probenicid and what is been linked to overdose?
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GI (give caution w/Pt. with peptic ulcer history), Mild skin rash, Nephrotic Syndrome (toxic rxn), overdose has been linked to CNS stimulation which leads to convulsions and death via respirtory failure
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What are the contraindications/interactionsof Probenicid?
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Increases T 1/2 of penicillin and Indomethacin (Indomethacin can be used to treat Gout in lower doses that when used as an NSAID
Coadministration os Salicylates which causes uricocuric action blunted; negative additively |
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What is the MOA Sulfinpyrazone?
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Inhibits renal tubular reabsorbtion of Uric Acid
A metabolite of an analogue of Phenylbutazone (NSAID) |
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What is the Metabolism of Sulinpyrazone?
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Orally absorbed
Highly bound to plasma proteins 50% metabolized in the liver 50% excreted unchanged |
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What are the side effects of Sulfinpyrazone?
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GI, Rash, Fever, Risk of depression of hematopoiesis function (periodic blood count CBC recomended)
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What are the contraindications/interactionsof Sulfinpyrazone
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Pts with Diabetes (interacts with hypoglycemic agents), Increases T 1/2 of Warfarin and inhibits Platlet aggreation, DO NOT combine with Salicylates b/c is mutually antagonistic
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What is the one Uric Acid Synthesis Inhibitor and what does it do?
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Allopurinol
Used to treat metabolic gout |
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What is the MOA of Allopurinol?
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It is a noncompetitive inhibitor of xanthine oxidase thus reducing the synthesis of uric acid
It is metabolized by xanthine oxidase to form alloxanthine which has a higher affinity for xanthine oxidase than hypoxanthine |
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What is the metabolism of Allopurinol?
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NOT bound to plasma proteins which means essentially 100% free, what you give is what you get
Slowly excreted in the urine by glomerular filtration |
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What are the side effects of Allopurinol?
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GI, Skin rash, Acute attacks of gout, may bind to lens and cause cataracts
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What are the contraindications/interactionsof Allopurinol?
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Reduce dose of Chemotherapeutic Agents if given concomitantly
Increases the effect of Cyclophosphamide Inhibits the metabolism of PROBENECID and Oral anticoagulants (Do NOT give together and keep a close watch on Diabetes II pts) |
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What are the three antiinflammatory agents?
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Colchicine, Indomethacin, Naproxen
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What is the MOA Colchicine?
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Binds to tubulin and prevents its polymerization into microtubules
Interferes with leukocyte migration and phagocytosis Inhibits formation of leukotriene B4 (which causes pain) |
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What has Colchicine been used for?
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In the intial day 1 treatment of Gout
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What is the metabolism of Colchicine?
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Absorbed after oral administration
Metabolites are excreted in intestinal tract and urine Can be detected in leukocytes and urine for 9 days after single dose |
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What are the side effects of Colchicine?
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There related to dose and duration
Common: Diarrhea, nausea and vomiting Long term Administration: Aplastic anemia, myopathy, alopecia |
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What are the symptoms of Colchicine at toxic levels?
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Affects the medulla: decrease body temp., depresses respiratpry center, Induces hypotension
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What are the contraindications/interactionsof Colchicine?
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Contraindicated in serious GI, Renal, Hepatic or Cardiac disorders
Increases response to CNS depressents (benzo's), and to sympathomimetic agents (stimulates sympathetic response) |
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What is Indomethacin used for?
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Reduces pain, fever, swelling, redness, and tenderness
Used as intial treatment of gout or as an alternative when colchicine is unsuccesful Most used drug for acute Gout atacks SEVERE SIDE EFFECTS |
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What is Naproxen used for?
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Reduces inflammatory changes (e.g. swelling, heat) within 24-48 hrs
provides relief of pain and tenderness Used as an adjuvant |
