Term
| NSAIDs are effective against what type of pain? |
|
Definition
| Low to moderate intensity |
|
|
Term
|
Definition
| Analgesics, Antipyretics (via IL-1 block), anti-inflammatory, primary dysmenorrhea, PDA, colon cancer prevention. |
|
|
Term
|
Definition
| GI ulceration and intolerance, Blockage of platelet aggregation (via inhibition of TXA2), inhibition of uterine motility, inhibition of prostaglandin-mediated renal effects--> nephritis and papillary necrosis, Hypersensitivity (asthma, urticaria, angioedema, cross reactivity) |
|
|
Term
| The only analgesic that causes irreversible inhibition of platelet aggregation |
|
Definition
|
|
Term
| Use and Mechanism of Action of Aspirin |
|
Definition
Use: analgesic, antipyretic, anti-inflammatory
MOA: inhibit PG synthesis by irreversible acetylation of COX |
|
|
Term
| How long does aspirin's effect on platelets last? |
|
Definition
| The entire platelet life (8-10days) |
|
|
Term
| Side effects of COX inhibitors not seen in Selective COX 2 inhibitors |
|
Definition
| GI ulceration, inhibition of platelet fct |
|
|
Term
Aspirin
Route of Administration
Half life
Elimination
Side Effects
Use |
|
Definition
ROA: Oral
t 1/2: 15-30 min
Excreted as salicyluric acid by kidney
Tinnitus or deafness (early sign of toxicity)
Transient decrease in renal fct, GI intolerance, hepatotoxicity, Salicylate intoxication, hypersensitivity
Use: juvenile rheumatoid arthritis, MI, colon cancer prevention
|
|
|
Term
|
Definition
Disturbance of acid-base balance leading to respiratory alkalosis and metabolic acidosis
Sx: Headache, dizzy, ringing in ear, mental confusion, drowsiness and sweating |
|
|
Term
| Contraindications of Aspirin use |
|
Definition
| Gout, ulcer, asthma, influenza (Reye's Syndrome) |
|
|
Term
|
Definition
Diflurophenyl derivative of salicylic acid
More potent anti-inflammatory fct than aspirin but no antipyretic and poor penetration to CNS
Less auditory side effects than aspirin |
|
|
Term
|
Definition
Salicylate used for local effect on IBD
Asacol (effective in ulcerative colitis) |
|
|
Term
Acetaminophen
Use:
Route of Admin:
t 1/2:
Side Effect:
|
|
Definition
Use: Analgesic and antipyretic. NOT ANTI-INFLAMMATORY
ROA: Oral
t 1/2: 1-4 hr
Side Effects: Fatal hepatic necrosis due to toxic metabolite
|
|
|
Term
|
Definition
| Antidote for hepatic toxicity seen in acetominophen. Gives a cysteine to help make glutathione, which detoxifies N-acetyl-Beta-benzoquinone imine. |
|
|
Term
Indomethacin
ROA:
Use:
t 1/2:
Side Effects: |
|
Definition
ROA: Oral rapid absorption in GI
Use: Acute gout and ankylosing spondylitis, tx PDA in premature infants
t 1/2: 2-3 hour
Side Effects: Nausea, vomiting, anorexia, abdominal pain, frontal headache associated with dizziness, confusion and depression.
|
|
|
Term
| What prohibits renal secretion of Indomethacin |
|
Definition
|
|
Term
Sulindac
Use:
t 1/2:
Side effects: |
|
Definition
Pro-drug with sulfide derivative as active metabolite
Suppress polyp formation in colon cancer, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis
t 1/2: 7 hours for pro-drug and 18 hours for active
Side effects: Renal stone
Less ulceration, GI irritation and blood loss than with aspirin. |
|
|
Term
Tolmetin
Use:
Side Effects:
|
|
Definition
Heteroaryl Acetic Acid Derivative
Use: juvenile rheumatoid arthritis
Side Effects: Epigastric pain, N/V |
|
|
Term
Diclofenac
MOA:
Route:
T 1/2:
Side effects: |
|
Definition
Reduce synthesis of both PGs and leukotrienes
Oral
2 hour
Increased hepatic transaminase, not recommended for children, nursing mothers, or pregnant women
Less likely than aspirin to cause peptic ulcer and GI bleed |
|
|
Term
|
Definition
NSAID with analgesic activity. PG synthesis inhibition.
Use: <5 days for management of moderately to severe acute pain
|
|
|
Term
Ibuprofen
Use:
Route:
t 1/2:
|
|
Definition
Mild inflammatory and analgesic drug with reduced gastric irritation
Route: Oral, protein bound, extensively metabolized in liver
t1/2: 2 hr |
|
|
Term
Naproxen
Use:
Route:
t 1/2:
Side effects: |
|
Definition
Use: Only propionic acid derivative approved for ankylosing spondylitis and juvenile RA as well as acute gout. 20x more potent than aspirin
Route: Oral; high protein bound excreted entirely in urine
t 1/2: 14 hour
Side effects: Crosses the placenta and appears in milk of lactating women |
|
|
Term
Ketoprofen
MOA:
t 1/2
Side effects |
|
Definition
MOA: Inhibits COX and lipoxygenase
t 1/2: 2 hr
Side Effects: GI, CNS |
|
|
Term
|
Definition
Propionic Acid Derivative
t 1/2 40-60 hours |
|
|
Term
|
Definition
| Aspirin, Diflunisal, Mesalamine |
|
|
Term
| Para-Aminophenol Derivatives |
|
Definition
|
|
Term
|
Definition
|
|
Term
| Heteroaryl Acetic Acid Derivatives |
|
Definition
| Tolmetin, Diclofenac, Ketorolac |
|
|
Term
| Arylproprionic Acid Derivatives |
|
Definition
| Ibuprofen, Naproxen, Ketoprofen, Oxaprozin |
|
|
Term
|
Definition
|
|
Term
|
Definition
t 1/2: 50-60 hr
COX inhibitor |
|
|
Term
|
Definition
Inhibits COX-2>>>COX -1
t 1/2: 20 hr
Tx: osteoarthritis |
|
|
Term
|
Definition
Alkanone
Only nonacid NSAID in use
Ketone prodrug converted to acetic acid derivative
Preferentially inhibits COX-2
t 1/2: 24 hour
GI ulceration much lower than other NSAIDS |
|
|
Term
|
Definition
| Celecoxib, Rofecoxib, Valdecoxib |
|
|
Term
|
Definition
COX-2 selective inhibitor
First one on the market. At therapeutic concentrations COX-1 is not inhibited.
Causes less ulcers than naproxen or ibuprofen and does not affect platelet aggregation
TX: osteo- and rheumatoid arthritis |
|
|
Term
|
Definition
Inhibits T cell activation
Tx: Adult rheumatoid arthritis and juvenile idiopathic arthritis in patients who are refractory to other regimens of NSAIDs
IV injection |
|
|
Term
|
Definition
Chimeric monoclonal antibody for CD20 B lymphocytes
Used when other NSAIDs fail.
Side effect: fatal infusion rxn within 24 hours of IV |
|
|
Term
|
Definition
Binds to TNF and blocks interaction with TNF receptors
t 1/2: 4.5 days
Route: Sub Q
Use: When other NSAIDS are refractory |
|
|
Term
|
Definition
Binds to TNF-alpha and blocks interaction with p55 and p75 cell surface TNF receptors
Given SC
t 1/2: 10-20 days so given every other week
Side effects: TB, invasive fungal diseases and other opportunistic infections |
|
|
Term
|
Definition
Neutralizes TNF-alpha by binding to soluble and membrane bound ones and inhibiting the binding to receptors.
Increased risk of infections including progression.
T 1/2: 9-12 days
Given IV every 8 weeks |
|
|
