Term
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Definition
| Chronic autoimmune disease with frequent acute attacks |
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Term
| COX inhibitors common problems |
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Definition
| GI upset, platelet fxn, elderly, renal dysfunction, cross sensitivity, CNS problems, blood dyscrasias, asthma, drug interactions |
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Term
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Definition
| phenylacetic acid derivative, some question use because of strong pro-MI effects |
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Term
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Definition
| Plaquenil, an antimalarial drug, increasing use, 400 to 200 mg/day PO, effective anti-inflammatory agent, inhibits neutrophils and eosinophils, 4-12 weeks to see effects, can combine with NSAIDs (sulfasalazine), Side effects: GI, retinal damage, dermatological, do not use with psoriasis or porphyria, liver damage, neurologic disorders, hematologic disorders, alcoholism |
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Term
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Definition
| Azulfidine, 500 mg to 2 g/day, metabolized to 5-amino-salicylate and sulfapyridine, MOA: anti-inflam, reaches high concentration in serous fluids, sulfapyridine and/or sulfasalazine produce beneficial effects; SE: anorexia, diarrhea, GI, headache, N/V, rash, urticaria, pruritis, blood dyscrasias rare, reduce folate absorption, Do not use with sulfa or celebrex allergy |
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Term
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Definition
| Rheumatrex, 10-15 mg/wk, going to 30 mg/wk usually PO, first choice drug used early and late RA; MOA: inhibits purine synthesis, inhibits DHFR, increase extracellular adenosine (anti-inflammatory), add folinic acid, dose related hepatotoxicity in 40%; SE: well tolerated, GI, liver, teratogenic, Higher doses: pulm tox, infections, lymphomas, BM suppr, hepatic fibrosis, pneumonitis |
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Term
| Triple drug therapy for RA |
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Definition
MSH
1. methotrexate up to 20 mg/wk
2. try hydroxychloroquine (200 mg bid) plus sulfasalazine (500 mg bid)
3. try all three in combination
*Can add NSAID and/or prednisone to above |
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Term
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Definition
| Arava, 100 mg/day x 3, then 20 mg/day PO, increasing in use; MOA: inhibits pyrimidine synthesis, antiprolif effect on T cells, reduces auto-antibody formation by B cells; SE: diarrhea, alopecia, CYP450 inhibition, carcinogenic, teratogenic, not combined with MTX (liver damage) |
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Term
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Definition
| tumor necrosis factor alpha, cytokine important in immune response, triggers inflammation and joint destruction |
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Term
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Definition
| cytokine produced by many immune cells, promotes inflammation, joint destruction, acts on IL-1 receptor |
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Term
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Definition
| target of IL-1, activation leads to increased inflammation |
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Term
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Definition
| target of IL-6, a pro-inflammatory cytokine over-produced in RA |
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Term
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Definition
| on T cells, stimulation by CD28 leads to activation of T cells |
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Term
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Definition
| binds to CD80, CD86, inhibiting their activation of T cells |
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Term
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Definition
| protein expressed on B cells involved in activation of B cells |
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Term
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Definition
| responsible for secreting autoantibodies (among other things) |
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Term
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Definition
| secrete cytokines and chemokines involved in immune response |
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Term
| Immunosuppressive agent side effects |
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Definition
GI problems, headache, rash, cough - common
increased risk of infections, teratogenic, blood dyscrasias, increased cancer, allergic reactions |
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Term
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Definition
| cancer risk similar to MTX, concern of possible appearance of PML (rare, usually fatal, untreatable viral infection of CNS), increased lymphomas in children/adolescents |
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Term
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Definition
| Enbrel, 25 mg SC twice a week, soluble human TNF receptor; MOA: binds TNF, prevents it from activating real TNF receptor, usually combined with MTX, shortest DOA of class (advantage with adverse reaction) |
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Term
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Definition
| Remicade, 3 or 10 mg/kg IV every 4-12 weeks, anti-TNF antibody (mouse-human chimera), binds TNF, usually combined with MTX; SE: immunosuppressive SE plus infusion rxns, don't use in HF (hypotension), used in Crohn's |
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Term
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Definition
| Humira, 40 mg every 2 weeks SC, anti-TNF antibody, similar to infliximab except all human, SE similar to others except don't use in MS (incr demyelination), approved for juvenile idiopathic arthritis (4 years +) |
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Term
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Definition
| Simponi, 50 mg SC once a month, human anti-TNF antibody, similar to infliximab except human |
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Term
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Definition
| Kineret, human interleukin-1 receptor antagonist, 100 mg/day SC, treatment of moderate to severe active RA that is non-responsive to one or more DMARDs, not first line; SE: serious infection, lymphomas, blood dyscrasias, Do not combine with anti-TNF drugs |
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Term
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Definition
| Actemra, 4 mg/kg IV/4 wks, can increase to 8 mg/kg, humanized anti-IL-6 receptor antibody, comp inhibits binding of IL-6 to its receptor, used in non-responders; SE: infections, immune rxns, elevated liver enzymes, elevated LDL, HTN, GI perforations |
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Term
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Definition
| Orencia, 500-1000 mg/day based on weight; MOA: binds CD80 and CD86 on APCs, inhibits full activation of T cells (usually requires binding of CD28 to CD80 or 86 on APCs, used in moderate to severe RA nonresponsive to other DMARDs; SE: serious infections, infusion rxns, Do not combine with TNF inhibitors or Anakinra (increased infections), not in people with COPD |
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Term
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Definition
| Rituxan, 2 X 1000 mg IV, 2 wks apart, anti-CD20 monoclonal antibody, inhibits activation of B cells, approved for RA with MTX when TNF inhibitors not adequate; SE: serious infections, infusion rxns, PML |
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Term
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Definition
| Minocin, 100 mg bid, experimental, effective early (first 6-12 months), SE: minimal, inhibits metalloproteinase (which degrades collagen) |
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Term
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Definition
| Ridaura, prototype, gold salts, accumulate in body (synovium), long lasting, takes 10 wks before effect, plasma protein bound, renally excreted (highest shortly after admin), IM dosing schedule 10mg 1st wk, 25 mg 2nd/3rd wks, 50 mg weekly, 50 mg 2 to 4 wk intervals up to 1yr; SE: dermatitis, BM suppr, renal tox, hepatitis, enteritis, stomatitis, metallic taste |
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Term
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Definition
| Depen, Cuprimine, 125-250 mg/day to 1000 mg/day, effective alternative to gold, rarely used due to SE, long-term use - serious tox, proteinuria, cutaneous lesions, blood dyscrasias, renal tox, pulm tox, myasthenia gravis |
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Term
| glucocorticoids - prednisone |
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Definition
| 5-7.5 mg/day to start, highly effective, used in combo with other agents, long term tox is high |
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Term
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Definition
| Alloprim, Zyloprim, prototype, xanthine oxidase competitive inhibitor, analog of hypoxanthine; reduces urate synthesis, more xanthine/hypoxanthine excreted as % of urine purines, also substrate of XO, oxypurinol is active metabolite (noncomp XO inhibitor), dissolves tophi, prevents progession of gouty arthritis by lowering serum urate, reduce nephropathy, increase acute attacks in early stage of therapy (suppr by colchicine), avoid starting during acute attack |
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Term
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Definition
| Uloric, non-purine, non-comp inhibitor of oxidized/reduced form of XO, alt to allopurinol, used for hyperuricemia with gout attacks, more effective in lowering urate to 6 than allo, but equal overall; SE: abnormal liver fxn, nausea, joint pain, rash |
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Term
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Definition
| Elitek, recombinant urate oxidase (uricase), converts urate to inactive and soluble allantoin, used for tumor lysis syndrome in peds with lymphoma/leukemia, IV infusion over 30 min, not used for chronic gout; SE: BBW for severe anaphylaxis and hemolytic anemia (G6PD deficiency), methemoglobinemia, keep blood samples chilled (false urate levels) |
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Term
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Definition
| Krystexxa, recombinant urate oxidase (uricase), converts urate to inactive and soluble allantoinpegloticase is newly pegylated recomb porcine uricase approved for refractory chronic gout (increased half life (12 days) and reduced antigenicity |
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Term
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Definition
| uricosuric agent, increase rate of excr of uric acid, inhibits URAT-1 mediated reabs in proximal tubule (high doses, >5g/day, dose dependent), used for gout, take lots of fluids to prevent renal stones, maintain urinary pH >6 (increase urate solubility), inneffective in renal insuff, don't use in nephrolithiasis, combo with colchicine or NSAIDs early in therapy; SE: well tolerated, GI irritant, salicylates reduce effic, may block penicillin excr, |
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Term
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Definition
| Cozaar, ARB, moderate uricosuric, option for intolerant patients to probenecid and hypertensive |
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Term
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Definition
| Indomethacin, sulindac, naproxen approved, relieves pain and inflammation, used for acute gouty arthritis within 24 hrs of symptom onset, high doses for 3-4 days, tapered for 7-10 days (aspirin contraindicated), sulindac safer congener also less potent, infant patent ductus arteriosus closure; SE: narrow index, GI, pancreatitis, hepatitis, frontal headache, dizziness/mental confusion (elderly) |
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Term
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Definition
| prednisone, used if NSAIDs ineffective/not tolerated, systemic therapy with high doses, rapidly tapered over 10-14 days, intra-articular admin useful if only 1 or 2 joints affected |
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Term
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Definition
| Colcrys, anti-mitotic effects, interfere with microtubule formation (disrupts fxn of neutrophil cytoskel), prevents neutrophil activation/degran/migration that mediates gout symptoms, enterohepatic recirculation exposes GI tract, CYP3A4, dose reduced in hepatic/renal, elderly, taking 3A4/P-glycoprotein inhibitors, used for second-line therapy, 2 doses taken 1 hr apart for acute gout, gout prevention (off label), fixed dose combo with probenecid; SE: narrow index, GI, myelosuppression, min of 3 but pref 7-14 days between courses to avoid cumulative tox |
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Term
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Definition
| block Na channels along axons (only when the channel is open) in a voltage and time-dependent manner, blocks from the inside of cell, no loss of consciousness, reversible |
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Term
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Definition
| pain, temp, light touch, deep pressure, muscle proprioception, motor nerve |
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Term
| Rapid onset local anesthetics |
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Definition
| lidocaine, mepivacaine, chlorocaine, etidocaine |
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Term
| Slow onset local anesthetics |
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Definition
| bupivacaine, procaine, tetracaine |
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Term
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Definition
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Term
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Definition
| bupivacaine, etidocaine, tetracaine |
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Term
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Definition
| lidocaine, mepivacaine, prilocaine |
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Term
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Definition
| longer DOA, reduces tonic somatic motor activity influencing alpha and gamma motor neurons, related to TCA, serotonergic, noradrenergic (also anticholinergic/antimuscarinic), short-term treatment of skeletal muscle spasms, not for spasticity; SE: anticholinergic; High Doses: areflexia, flaccid paralysis, resp depression, tachycardia, hypotension |
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Term
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Definition
| Robaxin, related to TCA, short DOA, may be due to general CNS depression, short-term treatment of spasms, not effective for spasticity; SE: discoloration of urine; High doses: CNS depression, respiratory depression; Parenteral Admin: syncope, hypotension, bradycardia, seizures, hemolysis |
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Term
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Definition
| central acting, pre/post synaptic GABAb receptor agonist, Ca influx to presynaptic terminals inhibited, glutamate and aspartate release suppressed, on post synaptic it activates K channels and 2nd messenger involving AA, reduces substance P, decrease spasticity caused by MS and spinal injury, also used for hiccups, neuropathic pain, episodes of intense pain in areas of face, monitor liver, aprupt stop can cause seizures |
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Term
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Definition
| diazepam, valium, GABAa receptor agonist, increases Cl conductance resulting in pre-synaptic inhibition in spinal cord, adjunct to baclophen in patients with spinal cord lesions and cerebral palsy, also treats muscle spasm, 2 active metabolites (nordazepam and oxazepam) |
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Term
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Definition
| zanaflex, alpha 2 adrenergic receptor agonist, decreases spasticity in MS and spinal injury, inhibits release of excitatory amino acid in spinal interneurons, elevated liver transaminases, monitor liver, don't use with antihypertensives or clonidine |
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Term
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Definition
| neurontin, acts on N-type Ca channels to reduce neuropathic pain |
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Term
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Definition
| botox, myobloc, centrally acting, decrease spasticity with cerebral palsy, stroke, brain injury, adv MS, dystonia, excessive sweating, inhibits pre-syn ACh release causing localized chemodenervation, focal muscle paralysis begins in 24-72 hrs after injection, can last for 12-16 wks, antibodies can develop, Do not use with excessive weakness |
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Term
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Definition
| Dantrium, muscle acting, acts on fast muscle fibers to block contraction, reduces depolar release of Ca from SR, decrease spasticity in patients with upper motor neuron lesions, stroke, or spinal cord injury, treats malignant hyperthermia and neuroleptic malignant syndrome, reaches peak after 3-6 hrs, metabolized by liver, Do not use with AML (low tolerance for muscle weakness), hepatotox, monitor liver |
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Term
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Definition
| pump surgically implanted under skin, connected to small flexible catheter directly into intrathecal space, advantages are lower dose and fewer side effects; Uses: cerebral palsy, anoxic brain injury, MS, stroke, spinal cord injury, arteriovenous malformation, spinal infection |
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Term
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Definition
| alkane, not pungent, MAC 0.77, medium onset, non-inflammatory, relatively potent, moderate onset/recovery; Disadvantages: unpredictable hepatitis, myocardial depression, malignant hyperthermia, highly metabolized, reduces renal BF/GFR, reduces hepatic BF |
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Term
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Definition
| ether, pungent, MAC 1.68, medium onset |
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Term
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Definition
| ether, pungent, MAC 1.15, medium onset, widely used in USA for maintenance, lower BP, tachycardia, malignant hyperthermia, reduces GFR, reduces hepatic BF |
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Term
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Definition
| ether, pungent, MAC 6.0, rapid onset |
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Term
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Definition
| ether, not as pungent, inhalation used for induction of anesthesia in children, MAC 2.05, rapid onset, not irritating to airways, used for outpatient procedures, exothermic rxn with soda lime (nephrotoxic), lower BP, no tachycardia (ischemia), malignant hyperthermia |
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Term
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Definition
| MAC 104, rapid onset, excellent analgesia, non-inflammatory, little tox, use as adjunct, Diadvantages: no skeletal muscle relax, weak anesthetic, post-anesthetic hypoxia, not suitable alone, not used in 1st trimester, teratogenic |
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Term
| General anesthetic Metabolism rank order |
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Definition
| halothane > enflurane > sevoflurane > isoflurane > desflurane > nitrous oxide |
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Term
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Definition
| uncontrolled release of Ca from SR, mutations in skeletal muscle ryanodine receptor calcium-release channel, mutations on alpha1 subunit of DHPR (voltage gated calcium channel), Patient Exhibit: tachycardia, hypercarbia, tachypnea, acidosis, muscle rigidity, hypoxemia, ventricular arrhythmias, hyperkalemia, rise in body temp |
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Term
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Definition
| non-barb, most common IV anesthetic in US, reduces opening time of Na channels, similar onset to thiopental, but faster elimination, induction time 11 sec, DOA 8 min, metabolized, SE: hypotension, lowers TPR, depr respiration, post-op N/V less (antiemetic), induction and maintenance of anesthesia, excitation in 10%, turns urine green |
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Term
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Definition
| Ketalar, non-barb, congener of phencyclidine (PCP), used in patients with risk for hypotension, bronchospasm, peds procedures, analgesic/amnesic and unresponsive but eyes open and spontaneous breathing (dissociative anesthesia), increase BP, HR, CO, increase RR, bronchodilator, stimulates sympathetic, N/V |
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Term
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Definition
| Amidate, non-barb, substituted imidazole, active D-isomer, poorly soluble, formulated in 35% propylene glycol (antifreeze, safe), induction of anesthesia with limited cardiac reserve, less resp depression than barbs, N/V |
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Term
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Definition
| Pentothal, barb, induction time <60 sec, DOA 5 min, longer half life than propofol, metabolized, SE: hypotension, decr myocard contractility, lowers TPR, depr respiration, anti-analgesic at low doses, purely amnestic, induction of anesthesia, urine output may fall, Don't use with porphyria |
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Term
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Definition
| Brevital, barb, similar to thiopental |
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Term
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Definition
| ligand-gated ion channel, inhibitory post-synaptic receptor for spinal reflexes and startle responses |
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Term
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Definition
| ligand-gated ion channel, excitatory synaptic receptor, involved in memory, nociception, autonomic fxn |
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Term
| serotonin type 3 receptors |
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Definition
| ligand-gated ion channel, excitatory synaptic receptor, arousal, emesis |
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Term
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Definition
| ligand-gated ion channel, excitatory synaptic receptor, perception, memory, learning, nociception |
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Term
| voltage-activated K channels (inhibit) |
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Definition
| nerve conduction, cardiac action potential |
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Term
| voltage-activated Na channel (inhibit) |
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Definition
| nerve conduction, cardiac action potential |
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Term
| voltage-activated Ca Channel (inhibit) |
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Definition
| cardiac inotropy and chronotropy, vascular tone |
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