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81 Cards in this Set
- Front
- Back
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we
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are
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she
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is
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he
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you
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indications for use of acetaminophen?
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minor pain, anti-pyretic (NOT an anti-inflammatory or anti-coagulant or NSAID)
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indications for use of acetaminophen?
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minor pain, anti-pyretic (NOT an anti-inflammatory or anti-coagulant or NSAID)
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mechanism of action of acetaminophen?
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possibly weak COX-3 inhibitor
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side effects of acetaminophen and maximum daily dosages?
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possible mild increase in liver function tests (LFT: enzymes elevated if liver is damaged); 3g/day is max in adults, 4g/day = GI ulcers and bleeding occur rarely
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overdose treatment for acetaminophen?
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consider acetylcysteine (mucomist) to neutralize toxic metabolites
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mechanism of action of tramadol (ultram)?
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synthetic opioid agonist
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indications for use of tramadol (ultram)?
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unusual drug for patients who cannot tolerate opioids and need pain relief
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side effects (and special characteristics) of tramadol (ultram)?
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tolerance, dependance (does not require DEA #)
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first group NSAIDs that do not require a prescription?
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aspirin (acetylsalicylic acid, irreversible), choline magnesium trisalicylate (non-acetylated, non-enteric coated, irreversible), salsalate (like aspirin but without GI bleeding effects, irreversible), ibuprofen (motrin, reversible), naproxen (naprosyn, reversible)
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first group NSAIDs that do require a prescription?
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piroxicam (feldene, for rheumatoid arthritis), nabumetone (relafen, for osteoarthritis and rheumatoid arthritis), ketorolac (toradol, injectable NSAID)
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mechanism of action of first group NSAIDs?
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reversible or irreversible inhibition of COX 1/2
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side effects of first group NSAIDs?
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upper GI ulcers/bleeding, increased risk of cardiovascular problems
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risk factors for side effects from first group NSAIDs?
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> 60 years old, history of ulcers, also using steriods or anticoagulants
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mechanism of action of ketorolac (toradol)?
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NSAID, COX 1/2 inhibitor
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indications for use of ketorolac (toradol)?
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injectable for up to 5 days as treatment for moderate acute pain instead of opioid
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second group NSAIDs (and which ones are currently available and if not why they were withdrawn)?
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celecoxib (celebrex, currently available), rofecoxib (vioxx, withdrawn for increased risk of stroke/MI), valdecoxib (bextra, withdrawn for increased risk of stroke/MI), meloxicam (mobic, for OA, currently available but still increases risk of CV events)
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mechanism of action of second group NSAIDs?
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reversible COX 2 inhibitors
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mechanism of action of corticosteroids?
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irreversibly binds to glucocorticoid receptors (GR) alpha and beta in all cells; affect DNA transcription of many proteins; inhibit: COX 2 (anti-inflammatory), cytokines, cell adhesion molecules, NO synthetase (anti-immune); increase: annexin-1 (possibly anti-inflammatory)
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side effects of systemic corticosteroids?
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increased risk infection, cushingoid appearance (buffalo hump, moon face), lower bone density (osteopenia/osteoporosis), hyperglycemia, poor wound healing
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commonly given intra-articular corticosteroid?
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triamcinolone hexacetonide
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mechanism of action of colchicine?
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binds to tubulin thereby stopping the microtubules and stopping mitosis (anti-cancer); inhibits migration of granulocytes (anti-inflammatory); raises pH in cells (inhibits uric acid formation)
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indications for use of colchicine?
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prophylaxis of acute gout flare while treating elevated uric acid (e.g with allopurinol) or at first sign of gout flare up
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mechanism of action of allopurinol (zyloprim)?
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inhibits xanthine oxidase thereby stopping conversion of xanthine to uric acid (purines [adenosine and guanosine] are degraded into uric acid mostly in intestinal mucosal cells where they then enter blood and are excreted by kidneys)
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indications for use of allopurinol (zyloprim)?
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DOC for tophaceous gout and uric acid nephrolithiasis (kidney stones made of uric acid)
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side effects of allopurinol (zyloprim)?
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diffuse rashes, fever, elevated liver function tests (LFTs)
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mechanism of action of febuxostat (uloric)?
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same as allopurinol (xanthine oxidase inhibitor: stops uric acid formation in purine degradation)
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indications for use of febuxostat (uloric)?
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use in place of allopurinol for gout and uric acid kidney stones (nephrolithiasis) in patients with modest renal failure
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side effects of febuxostat (uloric)?
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elevated liver function tests (LFTs), rash
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mechanism of action of indomethacin (indocin)?
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NSAID
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indications for use of indomethacin?
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short term relief of gout attack
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when are corticosteroids used in gout patients?
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short course in a patient with one of: bleeding ulcers, renal failure, coagulopathies
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mechanism of action of probenecid?
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uricosuric (increases uric acid excretion in urine): lowers uric acid in serum by blocking renal tubular resorption
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indications for use of probenecid?
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patients with elevated serum uric acid who do not have renal failure or renal caliculi and who can intake lots of fluids
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side effects of probenecid?
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gastrointestinal symptoms, rash
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drugs commonly used for gout?
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colchicine (classic, not used much anymore), allopurinol (zyloprim), febuxostat (uloric), indomethacin (NSAID), probenecid (push uric acid out renally)
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mechanism of action of diazepam (valium)?
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benzodiazepine (increases GABA activity at GABA-a chloride channel)
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indications for use of diazepam (valium)?
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reflex muscle spasms from local pathology (inflammation of muscle/joint), spasticity from upper motor neuron lesion, acute seizure (including those in alcohol withdrawal)
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side effects of diazepam (valium)?
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sedation (especially in the elderly)
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mechanism of action of balcofen (lioresal)?
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GABA-b receptor agonist
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indications for use of balcofen (lioresal)?
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spasticity from multiple sclerosis, spinal cord injury, or other disease (either PO or IV); trigeminal neuralgia
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side effects of balcofen (lioresal)?
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sedation (but less than diazepam and no development of tolerance)
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mechanism of action of tinzanidine (zanaflex)?
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Alpha-2 agonist (like clonidine): act on alpha-2 adrenergic receptors in brain possibly reducing release of neuroexcitatory transmitters
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indications for use of tinzanidine (zanaflex)?
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reduce muscle tone/spasm (used in MS)
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side effects of tinzanidine (zanaflex)?
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dry mouth, drowsiness, hypotension
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mechanism of action of dantrolene (dantrium)?
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limits Ca++/calmodulin available to ryanodine receptor (RYR-1) on sarcoplasmic reticulum causing reduced muscle contrations
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indications for use of dantrolene (dantrium)?
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spasticity from upper motor neuron lesions (stroke, injury, cerebral palsy, multiple sclerosis), neuroleptic malignant syndrome from antipsychotic drugs (remember FEVER where r=rigidity), malignant hyperthermia (rare)
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side effects of dantrolene (dantrium)?
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weakness, sedation, hepatotoxicity
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mechanism of action of methotrexate (MTX, rheumatrex)?
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analog of folic acid and inhibits dihydrofolate reductase (DHFR) which stops activity of folic acid leading to reduction in DNA, RNA, protein synthesis
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indications for use of methotrexate (MTX, rheumatrex)?
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rheumatoid arthritis, Crohn's disease, psoriasis
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side effects of methotrexate (MTX, rheumatrex) and when it should not be used?
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leukopenia, gastrointestinal side effects, oral ulcers (stomatitis), elevated liver function tests (LFTs), teratogenic, lung abnormalities; do not use if creatinine > 2; for rheumatoid arthritis patients supplement diet with folate
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mechanism of action of botulinum toxin A (botox)?
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blocks release of acetylcholine from cholinergic nerve endings at neuromuscular junction
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indications for use of botulinum toxin A (botox)?
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focal dystonia/spasticity, strabismus, blepharospasm (closed eyelid spasms)
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side effects of botulinum toxin A (botox)?
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well tolerated but some people develop antibodies to it
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mechanism of action of cyclobenzaprine (flexoril)?
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related to TCAs: acts centrally in brain stem by interfering with synapses of motorneurons
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indications for use of cyclobenzaprine (flexoril)?
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acute muscle spasms due to muscular injury; sometimes used for fibromyalgia but little evidence for efficacy (not effective in cerebral palsy or spinal chord injury)
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side effects of cyclobenzaprine (flexoril)?
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confusion, dry mouth, antimuscarinic
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neuromuscular blocking agents (with their mechanisms of action) and indications for use?
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pancuronium (competetive nicotenic antagonist), rocuronium (quick 1-2 minutes, competetive nicotenic antagonist), mivacurium (competetive nicotenic antagonist), succenolinylcoline (nicotenic agonist leading to rapid receptor desensitation); indications: intubation, adjunctive to anesthesia, euthanasia after sodiumthiopental
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DMARDs?
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disease modifying anti-rheumatic drugs for rheumatoid arthritis
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mechanism of action of leflunomide (arava)?
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prodrug that inhibits dihydroorotate dehydrogenase (rate-limiting enzyme for pyrimadine synthesis)
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indications for use of leflunomide (arava)?
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rheumatoid arthritis, psoriatic arthritis (it's a DMARD)
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side effects of leflunomide (arava)?
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liver function tests tend to be increased (so they must be monitored), teratogenic, increased hepatotoxicity with methotrexate (MTX, rheumatrex)
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indications for use of TNF inhibitors?
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rheumatoid arthritis, psoriasis, akylosing spondylitis, irritable bowel syndrome, Crohn's disease
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side effects of TNF inhibitors?
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risk of infection (especially latent tuberculosis), increased risk of skin cancer
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considerations when treating with TNF inhibitors?
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cost more than $18k/year; avoid their use in patients with infection, congestive heart failure, or demyelinating disorders
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TNF inhibitors?
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etanercept, infliximab, adalimumab, certolizumab pegol, golimamab
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mechanism of action of anakinra?
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IL-1 receptor antagonist
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indications for use of anakinra?
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used in patients with rheumatoid arthritis when TNF inhibitors are not tolerated
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side effects of anakinra?
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increased infections, neutropenia
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agents rarely or never used for rheumatoid arthritis (and why)?
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cyclophosphomide (used for Wagner's granulomatosis but can cause severe vasculitis), azathioprine (risk of malignancies), penicillamine (too many side effects), cyclosporin (too many side effects), minocycline (antibiotic, needs more studies), gold (not very effective)
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refractory rheumatoid arthritis?
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rheumatoid arthritis that does not respond to traditional DEMARDs (methotrexate or leflunomide)
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what agents are used to treat refractory rheumatoid arthritis?
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abatacept (T-cell activation inhibitor), rituximab (anti-CD20 monoclonal antibody which depletes the CD20 B-cells); use these with methotrexate, both are very expensive
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what constitutes early mild rheumatoid arthritis?
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no joint erosions visible on x-ray
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agents used in early mild rheumatoid arthritis (and their side effects)?
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sulfasalazine (possible leukopenia [monitor blood counts]), hydroxichloroquine (rare retinal toxicity [need regular eye exams], photosensitivity [use sun screen])
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newest rheumatoid arthritis drug for patients failing use with other choices?
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tocilizumab
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mechanism of action of tocilizumab?
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IL-6 inhibitor
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side effects of tocilizumab?
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neutropenia, lipid abnormalities, liver function test abnormalities
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drugs used for fibromyalgia (and basic mechanisms of action)?
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pregabalin (lyrica, similar to gabapentin [GABA analog]), duloxatine (serotonin-norepinephrine reuptake inhibitor [SNRI]), milnaciprin (serotonin-norepinephrine reuptake inhibitor [SNRI])
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