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80 Cards in this Set
- Front
- Back
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NSAIDs mostly have 4 A properties, what are they?
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Analgesia
Antipyresis (lower fever) Antiinflammatory Antiplatlet |
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In addition to gout, these drugs are important drugs in the treatment of other arthritic type disorders, including rheumatoid and osteoarthritis.
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NSAIDs
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Swollen tender joints
Nocturnal pain Early morning stiffness that lasts more than 30 minutes Acute physical disability what is this? |
Rheumatoid Arthritis
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Most common arthritic disease
About 60 million Americans Males and females about equally what is this? |
Osteoarthritis (OA)
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Osteophytes are a cardinal feature of what?
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Osteoarthritis (OA)
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Primary mode of action for NSAIDs?
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Inhibits cyclooygenase enzymes (COX) resulting in inhibition of prostaglandin (PG) synthesis
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please diagram where NSAIDs work in the inflammatory process
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COX 1 vs COX 2
There all the time (constitutive)? |
COX 1
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COX 1 vs COX 2
inducible (not there all the time) |
COX 2
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COX 1 vs COX 2
Protective and maintenance function? |
COX 1
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COX 1 vs COX 2
Proinflammatory and mitogenic function |
COX 2
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COX 1 vs COX 2
PGs in Stomach Intestine Kidney Platelet |
COX 1
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COX 1 vs COX 2
PGs in inflammatory sites Synoviocytes macrophages |
COX 2
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NSAIDs for which COX are going to cause GI bleeds with chronic use?
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COX 1
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Acetylsalicylic acid [ASA] inhibits which cox?
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BOTH! non-selective
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Acetylsalicylic acid [ASA] is a salicylate or non-salicylate
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salicylate
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is Acetylsalicylic acid [ASA] reversible?
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no, it is irreversible
must make new COX |
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Relieves mild to moderate pain by peripheral and central effects (↓ PGE2) – moderate doses
Lowers elevated temperature by interfering with hypothalamic control mechanisms – moderate doses this describes what drug? |
Acetylsalicylic acid [ASA]
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how does Acetylsalicylic acid [ASA] lower elevated body temp?
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by interfering with hypothalamic control mechanisms
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what does cetylsalicylic acid [ASA] do to bleeding time?
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prolongs it (anti-platelet effect)
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list which effect seen by cetylsalicylic acid [ASA] requires the highest dose (rank from low to high)
anti-inflammatory, anti-platelet, analgesic |
anti platelet
analgesic effect anti-inflammatory |
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what is the major adverse effect of aspirin (cetylsalicylic acid [ASA])?
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GI effect
due to loss of protective prostaglandin effect |
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asthmatics may have an asthma attack if using this drug, due to inhibition of COX enzymes forming leukotrienes, leading to bronchoconstriction
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cetylsalicylic acid [ASA]
(aspirin) |
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acute MILD toxicity from aspirin (cetylsalicylic acid [ASA]) is known as what?
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Salicylism
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with high concentrations of cetylsalicylic acid [ASA] what can happen to acid-base balance?
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mild uncoupling of oxidative phosphorylation --> increased respiration --> decreased pCO2 --> resp. alkalosis --> renal compensation -->increased bicarb elimination -->compensated resp alkalosis (pH normal, decreased bicarb decreased pCO2).
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Dehydration via sweating, lungs and kidneys
Hyperthermia Uncoupling of oxidative phosphorylation CNS effects Irritability and psychosis Respiratory depression Convulsions and coma Cardiovascular collapse Death usually as a result of respiratory failure this is adverse effects of what? |
severe salicylate poisoning
too much aspirin |
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please describe the acid/base inbalance in SEVERE aspirin overdose
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Inhibition of resp center ---> decreased resp --> increased pCO2 --> resp acidosis (decreased pH and bicarb, increased pCO2) plus inhibition of Krebs cycle and severe uncoupling of oxid. phos. (decreased ATP) --> metabolic acidosis, hyperthermia and hypokalemia
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should you use aspirin for fever reduction of children?
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NEVER
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Reduction of risk of re-infarction and stroke – major use
Fever reduction (antipyresis) Analgesia (mild to moderate) Acute rheumatic fever RA and OA (large doses required) these are therapeutic uses of what drug? |
aspirin
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aspirin in combination with these 2 drugs lead to increased bleeding
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warfarin and heparin
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What type of drug is Diflunisal? what drug is it similar to? what makes it different from the one it is similar to?
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NSAID
Aspirin NO ANTIPYRETIC EFFECT |
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Non-acetylated salicylates vs. salicylates
lower GI effect? |
Non-acetylated salicylates
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mechanism of action for Non-acetylated salicylates
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inhibit COX to decrease PG
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what is the major difference in Non-acetylated salicylates
and salicylates |
Non-acetylated salicylates
are REVERSIBLE while the others are irreversible |
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what will block the anti-platelet effect of aspirin?
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Ibuprofen (Non-acetylated salicylates)
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do Non-acetylated salicylates
cause acid base problems with high doses? what about aspirin? |
Non-acetylated salicylates: NO
aspirin: yes |
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which would you rather use for anti-inflammatory effects:
Non-acetylated salicylates or aspirin why? |
Non-acetylated salicylates
because it has less GI effects |
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this is one of the more toxic NSAIDs, should only be used for short periods of time, and really should only be used if you have to. Used to treat gout
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Indomethacin
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what is one special use of Indomethacin?
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to close a patent ductus arteriousus in neonates
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what is the limitation of Ibuprofen?
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short duration
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what drug may negate aspirin’s cardioprotective effects by antagonizing aspirin’s irreversible platelet inhibition?
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Ibuprofen
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what is the major difference between naproxen and Ibuprofen?
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naproxen is better for chronic conditions because it is longer lasting
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what kind of drug is naproxen?
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NSAID
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how is nabumetone eliminated?
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by kidneys, must reduce doses if they arent working well
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what type of drug is nabumetone?
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NSAID
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this is one of the few injectible NSAIDs that is used for pain relief and not anti-inflammatory
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Ketorolac
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what are the 2 selective COX 2 inhibitors?
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Celecoxib
Meloxicam |
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of the 2 COX2 inhibitors, which one is MORE selective for COX2? (what are the 2 drugs?)
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Celecoxib: more selective for COX 2
Meloxicam- "COX 2 preferred" |
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what is the Black Box warning of Meloxicam and Celecoxib?
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Increased risk of MI
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Celecoxib is what kind of drug?
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COX2 specific NSAID
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Meloxicam is what kind of drug?
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COX2 specific NSAID
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what can be given with a NSAID to help lower GI bleeding? how does it do this?
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Misoprostol is a prostiglandin analog that gets absorbed in the GI and decreases gastric acid production while stimulating bicarb and mucin production
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is acetaminophen an NSAID?
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NO!
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does acetaminophen have anti-inflammatory effects? why?
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NO!
it inhibits COX2 mostly in the CNS so it is used for analgesic and antipyretic effects |
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How is acetaminophen eliminated?
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mostly by phase 2 reaction
but also some by hepatic CYP450 (note: Phase 2 reactions are metabolic processes aimed at attaching polar and ionizable groups to phase 1 metabolites in order to form water soluble products which are devoid of activity and easily excreted from the body) |
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main uses for acetaminophen?
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pain and fever
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if you overdose on acetominophen to the point of toxicity, what will happen?
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dose dependent hepatic necrosis
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Please diagram how acetominophen is normally broken down and how toxicity occurs
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Patients such as...
Children with viral infections Patients on anticoagulants Gouty patients on uricosurics would be treated with? |
acetaminophen
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what are DMARDS?
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Disease Modifying Anti-Rheumatic Drugs
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What is the gold standard in treatment of RA?
*****MUST KNOW |
Methotrexate (MTX)
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what kind of drug is Methotrexate (MTX)? what is it used for?
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DMARD
for RA |
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what drug is used as an antimalarial?
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Hydroxychloroquine
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Hydroxychloroquine is used for what
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Antimalarial
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Gold salts can be used to treat what?
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Most effective early in the rapid progressive stages of RA
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Pencillamine is a 3rd or 4th line drug for what? What is its action?
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Decreases bone destruction in RA
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what is a second line treatment if a person can't use methotrexate? what disease are these for?
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Leflunomide
for RA |
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how does Etanercept work?
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forms a 'decoy' TNFalpha receptor to decrease the inflammatory response
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what is Etanercept used for?
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RA, lowers inflammation by TNFalpha by forming a decoy receptor
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how is Etanercept administered?
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injection
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if you see a drug ending in mab, what is it?
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monoclonal antibody to TNF alpha
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what is the action of Infliximab
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monoclonal antibody to TNF alpha
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what is the action of adalimumab
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monoclonal antibody to TNF alpha
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what is the action of golimumab
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monoclonal antibody to TNF alpha
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Progressive Mulitfocal Leukoencephalopathy (PML) is a side-effect seen in what drugs?
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the mabs
Infliximab , adalimumab and golimumab |
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you have a patient on a TNF inhibitor (either Infliximab , adalimumab and golimumab) and you see edema in the ankles, what do you need to worry about happening (a side effect)
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Heart failure
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Anakinra does what
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IL-1 receptor antagonist.
Blocks inflammatory and immunologic reactions of IL-1 produced in RA. |
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Abatacept does what
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inhibits T-cell activation, thus decreasing the production of TNFα.
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what does Capsacin do? what is it used for?
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Stimulates release of substance P from afferents…Deplete stores to decrease pain sensation
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