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Drugs for Pain, Inflammation and Arthritic Disorders
Terms in this set (50)
Describe the joint inflammation associated with RA.
SYMMETRIC, usually affecting SM joints of the hands, wrists and feet. Rheumatoid nodules on EXTENSOR surfaces of joints of UE.
RA is triggered by which type of mechanisms?
AUTOIMMUNE mechanisms that lead to destruction of synovial / connective tissue
Pts with RA show increased levels of ________ via serum immunoassay testing.
How do NSAIDs relieve FEVER?
They inhibit prostaglandin synthesis in the hypothalmus; temp will NOT be reduced below normal body temp.
Which "NSAID" is said to potentially inhibit COX-3, resulting in decreased anti-inflammatory action?
What are the NSAIDs listed in Chapter 30 (that we have to know)?
*COX 2 inhibitor
Which NSAIDs should be avoided for use in children?
Aspirin & other salicylates due to REYE SYNDROME - increased risk in children infected with VIRUSES
What are the ADEs of NSAIDs that affect the GIT?
GI bleeding, peptic ulcers, renal/hepatic dysfunction
Which NSAID produces fewer GI problems than other COX inhibitors?
T or F - NSAIDs can be used in combination with another NSAID for supplemental analgesia.
FALSE. Acetaminophen CAN be used concurrently with another NSAID, but generally combo of 2 NSAIDs should be avoided. = increase risk of GI ADEs + increase serum levels of other NSAIDs.
T or F. NSAIDs are safe for use in pts with bipolar disorder who are managed with LITHIUM.
FALSE. Most NSAIDs inhibit renal excretion of lithium and increase serum levels that can lead to TOXICITY.
Low doses of which NSAID can safely be used for analgesia and antipyresis in pregnancy?
Acetaminophen (Tylenol). All others are associated with potential ADEs on the fetus.
Acetaminophen is different from other NSAIDs in terms of its activity because it lacks ______________.
Significant ANTIPLATELET / ANTIIFLAMMATORY activity.
Which type of COX inhibition does ASA form?
Covalent, IRREVERSIBLE inhibition of COX, providing longer lasting effect on thromboxane synthesis.
In cases of ASA overdose, _____________ of the urine by ____________________ can be used to increase ionization and elimination.
ALKALINIZATION, SODIUM BICARBONATE.
The rate of excretion of ASA is affected by urine pH.
What is the ADE associated with giving NSAIDs in conjunction with potassium sparing drugs?
NSAIDs can cause K+ retention, leading to hyperkalemia.
ASA undergoes _______________ order metabolism at therapeutic doses and _____________ order metabolism at excessive doses.
Elderly at greatest risk for ASA toxicity.
What are the pharmacological and ADEs / toxic effects of ASA with each increased dose?
Therapeutic = Antiplatelet, analgesic, antiinflammatory; gastric irritation, GI bleeding and peptic ulcers
High therapeutic = Anittinflammatory (rheumatic fever); tinnitus
Excessive = hyperventilation, resp alkalosis
High plasma salicylate = fever, rehydration, severe metabolic acidosis
Shock, coma, resp/renal failure, death
What is another name for acetaminophen that is derived from its chemical name?
Acetaminophen toxicity is associated with which organ specifically?
What is acetaminophen primarily metabolized by?
Conjugation with sulfate and glucuronide
Long term use of acetaminophen is associated with an increased risk of ________________?
T or F. NSAIDs are safe for use in all trimesters of pregnancy.
FALSE. NSAIDs (with the exception of low doses of acetaminophen) should be avoided, especially in the 2nd and 3rd trimesters.
ASA can be used prophylactically for which of the following?
A. Strep pharyngitis
C. ASA can also be used as prophylaxis against CVA and thromboembolism because it prevents platelet aggregation.
What is the antidote for acetaminophen toxicity?
N-acetylcysteine (Mucomyst). Acetylcysteine is the immediate precursor to glutathione in the pentose phosphate pathway. Glutathione is the body's "master anti-oxidant", capable of protecting and repairing hepatocytes. Given within FOUR hours of overdose.
Which of the following NSAIDs has the longest 1/2 life?
C. Naproxen administered bid. it has a 14h 1/2 life.
What NSAID is used in the Tx of patent ductus arteriosus in infants?
Indomethacin. It inhibits the synthesis of prostaglandins allowing for the closure of the ductus arteriosus.
Celecoxib has all of the following effects EXCEPT:
C. Inhibit platelet aggregation
C. Inhibit platelet inhibition. Platelets only contain the COX-1 isozyme and celecoxib is a COX-2 inhibitor.
What are the ADEs of celecoxib?
CV events, ABD pain, diarrhea, dyspepsia.
CI concomitant administration with fluconazole, fluvastatin, and zafirlukast.
What is the utility of DMARDs limited by?
Toxicity and loss of efficacy over time.
What are the "salts" associated with the Tx of RA?
Gold sodium thiomalate
What is the hypothesized MOA of gold salts in the Tx of RA?
Antimitochondrial activity and cell apoptosis
When do pts usually start to benefit from the Tx of RA with gold salts?
3-6 months after initiation of therapy
What are the ADEs associated with gold salts?
GI / renal
Flushing / skin rash
Hypotension / tachycarida
Stomatitis (inflammation of mucous membranes of the mouth and lips)
Which ADEs require discontinuation (d/c) of golds salts if observed?
Skin rash and stomatitis.
How are glucocorticoids used in the Tx of RA?
A SHORT course can be used in the initiation of therapy and/or for disease FLARE-UPS.
What are the "other" DMARDs used in the Tx of RA?
What is the single most effective DMARD available today?
T or F. Methotrexate is CI in pregnancy.
TRUE. Methotrexate inhibits human folate reductase leading to decreased folate.
+ folate supplement with use
What are some ADEs of leflunomide?
Diarrhea, REVERSIBLE ALOPECIA, hepatotoxicity when used with MTX
CI in pregnancy - X
Pts undergoing hydroxychloroquine Tx must be monitored for what ADEs?
Adverse OCULAR effects:
What DMARD is reserved for RA refractory to MTX and other DMARDs?
What is the BBW for all TNF blockers?
Risk of Legionella pneumonia and Listeria infections.
What is the niche use of the TNF alpha blocking agent, infliximab?
Intravenous Tx of CROHN'S disease and RA.
What are the ADEs of indomethacin?
Increased incidence of GI/CNS effects, higher than any other NSAID.
Serious HEMATOLOGICAL TOXICITY.
What are the uses for Sulindac, a prodrug, noted for its renal sparing effect?
Tx of RA
Tx of adenomas in polyp disease
What is the NSAID that is comparable to morphine in its analgesic effects and can be given via parenteral, opthalmic and intranasal routes?
Comparable to morphine without the ADEs of N/V and drowsiness.
Ketorolac is available in which forms for administration?
Only for 5 or fewer days!
What are the ADEs associated with Ketorolac in patients with renal/hepatic disease?
Increased risk of severe renal or hepatic impairment in patients with renal/hepatic disease.
What is ophthalmic solution for ketorolac used for?
Tx of allergic conjunctivitis
Tx of post operative ocular inflammation
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