Rheumatology Pharmacotherapy Lecture PDF Flashcards
Acetaminophen function
Analgesic and antipirectic, does not possess anti-inflammatory activity (not an NSAID)
NSAIDs, Aspirin, and acetaminophen mech of action
-prostaglandin synthesis inhibitors by blocking COX 1 and/or 2 (1 helps with GI protection, platelet function, and kidney function while 2 is associated with inflammation, pain, and fever)
3 major actions of NSAIDS including ASA are….
- anti-inflammation (
- analgesia (raise threshold)
- antipyretic (activation of macrophages that then release interleukins 1 and 2 which are pyrogens)
Methyl salicylate function (oil of wintergreen, bengay)
Poison when taken orally but topical prep in creams is counterirritant often for muscle pain in athletes by increasing blood flow and warmth at applicaiton site
Other effects of NSAIDS including ASA (3)
- platelet inhibition (thromboxane enhances platelet aggregation and aspirin irreversibly inhibits production inhibiting platelet aggregation at low consistent*** levels)
- migraine induced headache prophylaxis
- antidysmenorrheal effect
NSAIDs long term use ADR’s (6)
- dyspepsia
- epigastric pain
- peptic ulceration
- renal side effects including failure
- respiratory acidosis at very high dose
- increase risk of thrombotic events (opposite of aspirin)
Gastric damage by NSAIDs can be mitaged by administering a ____ alongside
proton pump inhibitor
In contrast to aspirin, nonaspirin NSAIDS do not protect against ____ and ____
MI and stroke
Aspirin triad
Aspirin hypersensitivity
Asthma
Nasal polyps
Reyes syndrome
Primary childhood disorder with death rate of 25%, develops after apperent recovery from flu or chicken pox chracterized by vomiting, liver abnormalities, and encephalopathy progressing to delirium and coma, often due to aspirin use
NSAID use and pregnancy
Not recommended especially during lat trimester to cause premature closure of ductus arteriosus
Symptoms of salicylism from excess aspirin use (4)
- tinnitus
- headache
- delirium
- hyperventilation
Acetaminophen (tylenol) toxicity
At very high levels leads to production of macromolecules that are very hepatotoxic when daily dose is exceeded or individual with hepatitis
Nondrug therapies for RA treatment (remember RA cannot be cureD) (3)
- physical therapy
- occupaitonal therapy
- surgery
3 categories of drugs for treatments of RA
- NSAIDS (symptomatic relief doesn’t slow progression)
- disease modyfing antirheumatic drugs (slow acting anti-rehumatic drugs inclduing nonbiologic and janus kinase inhibitors
- glucocorticoids (great for flareups but chronic use has many neg side effects)
Current recommendations for treatment of rheumatoid arthritis
-start disease modifying antirheumatic drugs (DMARD) within 3 months of diagnosis (this hopes to delays joint degeneration)
Intraarticular injections
Use of something like methyrednisalone for relief of RA for several months as long as not used more than 2-3 times a year in cases where only 1 or 2 joints are affected
Corticosteroids ADRs (5)
- adrenal suppression
- cushings
- osteoporosis
- cataracts
- glaucoma
Methotrexate function
fastest acting of DMARDs, PO in low dose decreases symptoms and improves long term outcome of RA, often used intially
Methotrexate ADR’s (4)
- hepatic fibrosis
- bone marrow suppression
- immunosuppressive
- teratogenic in pregnancy
Hydroxychloroquine (plaquenil) function
Antimalerial drug that is moderately effective for mild rheumatoid arthritis and can produce remission of RA, reserved for those not responding to NSAIDS, takes up to 3-6 months to develop effects
Hydroxychloroquine (plaquenil ADR’s (2)
- retinal damage
- hemolysis in G6PD deficiency
Sulfasalazine (azulfidine) function
Drug used to treat inflammatory bowel disease and RA
Azathioprine (imuran), cyclosporine, and gold salts function
Approved by FDA for rheumatoid arthritis treatment but used infrequently due to serious adverse side effects, may still be used in refractory cases
When are biologic DMARDs and janus kinase inhibitor used?
In those that need moderate or high disease treatment of RA or who do not respond
Etanercept (enbrel) drug class and function
TNF inhibitor, used for RA in combo with methotrexate in those who do not respond to first line treatments alone
Etanercept (enbrel) contraindication (1)
-septic patients or those with hypersensitivity
Infliximab (remicade) drug class and function
TNF inhibitor, first approved for treatment of crohn’s now approved for use in combo with methotrexate to treat RA in patients who do not respond to methotrexate alone, also to treat ankylosing spondylitis, psoriasis
Adalimumab (humira) function
Similar immunosuppressant function as infliximab but easier to administer as it is only used every 2 weeks
Rituximab (rituxan) drug class and fucntion
B lymphocyte depleting agent, selectively depletes B cells which play role in autoimmune response and in the chronic synovitis associated with RA
T cell activation inhibitor example, function
Abatacept (orencia), reduces RA symptoms and decreases disease progression
3 examples of drugs that are interleukin receptor antagonists preventing the cytokines being overproduced in patients with RA that contribute to joint destruction
- tocilizumab
- sarilumab
- anakinra
Tofacitinab (xeljanz) drug class and function
Janus kinase inhibitors, used for treatment of adults with moderate to severe active RA who have not had adequate response or who are intolerant of methotrexate
Gouty arthritis is associated with hyperuricemia which is uric acid level greater than ___mg/dL
6-7
Drugs to relieve acute gouty attacks (2)
- NSAIDS
- colchicine
Drugs used to lower long term levels of uric acid in patients with chronic gout (2)
- allopurinol and febuxostat
- probenecid and lesinurad
If a patient is not on uric acid lowering therapy at time of gout attack, then…..
It is not time to intiiate therapy. If patient is on uric acid lowering therapy at time of attack, should not be discontinued
Common NSAID agents used for treatment of gout (4)
- indomethacin
- naproxen
- diclofenac
- ibuprofen
Causes of elevated uric acid levels
- decreased clearance of uric acid from kidney (90%)
- overproduction of uric acid
Lifestyle changes for gout (3)
- diet not huge influence
- decrease obesity
- decrease alcohol consumption
Whenever starting a uric acid lowering treatment, there is risk of preciptating a ___, therefore this is avoided by coadministration of ___ alongside uric acid lowering therapy
gout flare, steroids/colchicine/nsaid
Colchicine function
Antinflammatory whose effects are specific for gout, ineffective for other inflammatory disorders, use has declined because of better alternatives
Colchicine ADR’s (3)
- GI issues
- drug interactions with statins
- myelosuppression
Allopurinol drug class and function
Xanthine oxidase inhbitor, used to reduce blood levels of uric acid, indicated for primary hyperuricemia of gout, as well as 2ndary hyperuricemia due to blood dyscrasias such as polycythemia vera and leukemia, can increase risk of incidence of attacks in intial months of treatment hence need concurrent treatment with colchicine or NSAID
Febuxostat (uloric) function
Identical to allopurinol in treatment of reduction of uric acid levels in blood for primary hyperuricemia of gout
Pegloticase (krystexxa) drug class and function
Recombinant form of uric acid oxidase IV agent for highly symptomatic patients with severe tophaceous gout who have not responded to other agents, very expensive and has many infusion reactions (urticaria, dyspepsia, chest discomfort, erythema)
Pseudogout
Results when calcium pyrophosphae dihydrate crystals deposited into bone and cartilage are released into synovial fluid inducing acute inflammation, may present as acute monarthritis or oligoarthritis, usually affecting knee, treated via NSAIDs, colchicine, glucocorticoids
