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37 Cards in this Set

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what are NSAIDs and how do they work?
Non-steroidal anti-inflammatory Drugs reversibly inhibit the synthesis of cyclooxygenase and thus prostaglandins and thromboxanes; releive symptoms of pain, stiffness, swelling, and inflammation by inhibiting COX (cyclooxygenase) enzyme that converts arachidonic acid into prostaglandins
Name the 4 main therapeutic uses of NSAIDs.
1)Anti-inflammatory; 2) Analgesia; 3)Antipyretic; 4) Antiplatelet activity
Name the only NSAID that is irreversibly inhibited by cyclooxygenase.
aspirin
what do prostaglandins cause?
edema, cellular exudation, and pain (arachidonic acid (cox 1) -> prostaglandins)
What NSAIDs have antipyretic properties?
ibuprofen, naproxen, and salicylates (aspirin)
How do COX 1 and COX 2 differ?
COX 1 is predominately responsible for the production of cytoprotective prostaglandins formed by gastric mucosa; COX2: more involved in forming inflammatory mediators. (thus COX 2 selective inhibitors were thought to be anti-inflammatory without the GI effects)
What does it mean to be a selective COX inhibitor?
there are 3 types of cyclooxygenase iosenzymes: COX 1- prostaglandin production (prostaglandins have a protective role in the GI tract and prevent acid insult); COX 2 turn arachidonic acid into prostanoids which are more responsible for inflammation (COX 2 inhibitors don't upset the GI mucosa and are selective to only be anti-inflammatory and thus are great for joint pain)
list the contraindications for taking NSAIDs.
Hypersensitivity; Triad Asthma; Nasal Polyps; Angioedema; Bronchospasms; History of Gastric Dz or Ulcers
list the side-effects of NSAIDs.
Gastropathy; Platelet inhibition; Edema; Headache; Impaired wound healing (Phar Recall: Epigastric Distress, N/V; Cardiac D/O; Coagulation D/O; Renal Tox; Hypersensitivity; Reye's Syndrome (aspirin in kids)
List the drugs that have interactions with NSAIDs.
Digoxin, diuretics, warfarin, lithium, methotrexate, cyclosporine
___ mask the symptoms of gastropathy but they don't have a protective effect.
H2 blockers
This prostaglandin E1 analogue may be used to protect the stomach lining (not used much anymore) from long-term NSAID damage by stimulating the production of mucin and bicarbonate.
misoprostol - gives 40% users diarrhea - contraindicated in preg.- causes uterine contractions
This drug is a mucosal protective agent that is used to treat peptic ulcer disease by binding to necrotic ulcer tissue and acts as a barrier to acid, pepsin, and bile.
sucralfate - needs acidic environment to work - don't use with H2 blockers or PPI
How are NSAIDs metabolized?
converted to water-soluble conjugates in the liver and cleared by the kidney. If the liver is compromised, the T1/2 will increase.
How are all NSAIDs cleared?
kidneys; thus if renally compromised then must adjust the medication based on GFR
How do you calculate GFR?
using the Cockcroft-Gault formula: GFR: (140-age) x (weight in kg)/serum creatinine in mg/dl x 72
Name some NSAIDs in the Salicylate category.
aspirin (acetylsalicylic acid); Bufferin, Salicyl salicylate (salsalate); Magnesium Trisalicylate; Difunisal (no tinnitus); Anacin (+caffeine); Ascriptin (+maalox); Ecotrin (enteric coated); Excedrin (+acetaminophen); Alka-seltzer(+NaHCO3)
This NSAID category contains naproxen, indomethacin, sulindac, ketorolac, tolmetin, and nabumetone.
indoleACETIC ACIDS
These drugs do not interfere with anti-HTN diuretics.
sulindac, naproxen
This acetic acid NSAID has no effect on GFR and doesn't interefere with diurectics (anti-HTN).
sulindac
Th acetic acid NSAID, _____ and the propionic acid, _____ are approved for use in children.
acetic acid: tolmetin sodium; propionic acid: naproyxn
This acetic acid NSAID is used with misoprostol in RA and OA patients that are at risk for developing gastropathies.
diclofenac sodium
this acetic acid NSAID has a rapid onset and doesn't cause any sodium retention edema.
diclfenac potassium
this propionic acid is used very commonly (it's trade name is Motrin or Advil).
ibuprofen - (ibuprofen + hydrocodone = vicoprofen)
this propionic acid NSAID has a higher association with causing nephrotic syndrome than any other NSAIDs.
fenoprofen calcium
ketoprofen comes in many different forms and is in what category of NSAIDs?
propionic acid
the propionic acid drug naproxyn sodium is sold as what trade name?
Aleve
name the NSAIDS that are under the sub-class of Fenamates aka Fenamic Acid.
meclofenamate sodium (25% get diarrhea); mefenamic acid (Ponstel)
name the 2 NSAIDs that are under the pyranocarboxylic acid category.
etodolac and ketorolac tromethamine
This pyranocarboxylic acid NSAID may help promote healing of cartilagenous erosions.
etodolac
This pyranocarboxylic acid NSAID excellent analgesic and is commonly used as an alternative to opioid (for short-term only).
ketorolac tromethamine (comparable doses: TORADOL, morphine, and meperidine)
this oxicam has a long-half and takes 7-12 days to reach a steady state level.
piroxicam
this naphthylalkanone NSAID has the lowest incidence of gastropathy of all NSAIDs and has a half-life of 29hours.
nabumetone (Relafen)
Describe the COX 2 inhibitor Celecoxib (CELEBREX).
Metabolized by P450 and elimated through the liver; much lower incidence of gastroduodenal ulcers (7.5% vs. 35% in naproxyn, 23% ibuprofen; 10% in diclofenac); NO platelet inhibition
What are the C/I and Drug Interactions with celecoxib?
C/I: allergy to sulfonamides and avoid in late pregnancy to allow closure of the ductus arteriosus; DRUG INTERACTIONS: ACE inhibitors (decreases anti-HTN effects) and Fluconazole (causes a 2x increase in celecoxib levels)
This COX2 inhibitor was withdrawn from the market because of possible CV problems in 2004. It has many drug interactions. Name them.
rofecoxib(Vioxx); Drug Interactions: aspirin, ACE inhibitors, Cimetidine (increases rofecoxib levels); furosemide-loop diuretic (reduces effect), lithium (increases lithium); methotrexate (increases metho); rifampin (co-admin produced a 50% red. in roecoxib); warfarin (increases the INR)
List the NSAIDs in order of increasing injury as seen by endoscopic evaulation.
nabumetone, piroxicam, ibuprofen, naproxen, indomethacin, then tolmentin.