Omm; 4.2.07; Nsaids Part I, Kek

Front 1

what are NSAIDs and how do they work?

Back 1

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

Front 2

Name the 4 main therapeutic uses of NSAIDs.

Back 2

1)Anti-inflammatory; 2) Analgesia; 3)Antipyretic; 4) Antiplatelet activity

Front 3

Name the only NSAID that is irreversibly inhibited by cyclooxygenase.

Back 3

aspirin

Front 4

what do prostaglandins cause?

Back 4

edema, cellular exudation, and pain (arachidonic acid (cox 1) -> prostaglandins)

Front 5

What NSAIDs have antipyretic properties?

Back 5

ibuprofen, naproxen, and salicylates (aspirin)

Front 6

How do COX 1 and COX 2 differ?

Back 6

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)

Front 7

What does it mean to be a selective COX inhibitor?

Back 7

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)

Front 8

list the contraindications for taking NSAIDs.

Back 8

Hypersensitivity; Triad Asthma; Nasal Polyps; Angioedema; Bronchospasms; History of Gastric Dz or Ulcers

Front 9

list the side-effects of NSAIDs.

Back 9

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)

Front 10

List the drugs that have interactions with NSAIDs.

Back 10

Digoxin, diuretics, warfarin, lithium, methotrexate, cyclosporine

Front 11

___ mask the symptoms of gastropathy but they don't have a protective effect.

Back 11

H2 blockers

Front 12

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.

Back 12

misoprostol - gives 40% users diarrhea - contraindicated in preg.- causes uterine contractions

Front 13

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.

Back 13

sucralfate - needs acidic environment to work - don't use with H2 blockers or PPI

Front 14

How are NSAIDs metabolized?

Back 14

converted to water-soluble conjugates in the liver and cleared by the kidney. If the liver is compromised, the T1/2 will increase.

Front 15

How are all NSAIDs cleared?

Back 15

kidneys; thus if renally compromised then must adjust the medication based on GFR

Front 16

How do you calculate GFR?

Back 16

using the Cockcroft-Gault formula: GFR: (140-age) x (weight in kg)/serum creatinine in mg/dl x 72

Front 17

Name some NSAIDs in the Salicylate category.

Back 17

aspirin (acetylsalicylic acid); Bufferin, Salicyl salicylate (salsalate); Magnesium Trisalicylate; Difunisal (no tinnitus); Anacin (+caffeine); Ascriptin (+maalox); Ecotrin (enteric coated); Excedrin (+acetaminophen); Alka-seltzer(+NaHCO3)

Front 18

This NSAID category contains naproxen, indomethacin, sulindac, ketorolac, tolmetin, and nabumetone.

Back 18

indoleACETIC ACIDS

Front 19

These drugs do not interfere with anti-HTN diuretics.

Back 19

sulindac, naproxen

Front 20

This acetic acid NSAID has no effect on GFR and doesn't interefere with diurectics (anti-HTN).

Back 20

sulindac

Front 21

Th acetic acid NSAID, _____ and the propionic acid, _____ are approved for use in children.

Back 21

acetic acid: tolmetin sodium; propionic acid: naproyxn

Front 22

This acetic acid NSAID is used with misoprostol in RA and OA patients that are at risk for developing gastropathies.

Back 22

diclofenac sodium

Front 23

this acetic acid NSAID has a rapid onset and doesn't cause any sodium retention edema.

Back 23

diclfenac potassium

Front 24

this propionic acid is used very commonly (it's trade name is Motrin or Advil).

Back 24

ibuprofen - (ibuprofen + hydrocodone = vicoprofen)

Front 25

this propionic acid NSAID has a higher association with causing nephrotic syndrome than any other NSAIDs.

Back 25

fenoprofen calcium

Front 26

ketoprofen comes in many different forms and is in what category of NSAIDs?

Back 26

propionic acid

Front 27

the propionic acid drug naproxyn sodium is sold as what trade name?

Back 27

Aleve

Front 28

name the NSAIDS that are under the sub-class of Fenamates aka Fenamic Acid.

Back 28

meclofenamate sodium (25% get diarrhea); mefenamic acid (Ponstel)

Front 29

name the 2 NSAIDs that are under the pyranocarboxylic acid category.

Back 29

etodolac and ketorolac tromethamine

Front 30

This pyranocarboxylic acid NSAID may help promote healing of cartilagenous erosions.

Back 30

etodolac

Front 31

This pyranocarboxylic acid NSAID excellent analgesic and is commonly used as an alternative to opioid (for short-term only).

Back 31

ketorolac tromethamine (comparable doses: TORADOL, morphine, and meperidine)

Front 32

this oxicam has a long-half and takes 7-12 days to reach a steady state level.

Back 32

piroxicam

Front 33

this naphthylalkanone NSAID has the lowest incidence of gastropathy of all NSAIDs and has a half-life of 29hours.

Back 33

nabumetone (Relafen)

Front 34

Describe the COX 2 inhibitor Celecoxib (CELEBREX).

Back 34

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

Front 35

What are the C/I and Drug Interactions with celecoxib?

Back 35

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)

Front 36

This COX2 inhibitor was withdrawn from the market because of possible CV problems in 2004. It has many drug interactions. Name them.

Back 36

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)

Front 37

List the NSAIDs in order of increasing injury as seen by endoscopic evaulation.

Back 37

nabumetone, piroxicam, ibuprofen, naproxen, indomethacin, then tolmentin.