KG - Pharm 3, Exam 1, NSAIDS & DMARDS Flashcards
clinical signs inflammation?
- erythema, edema, tenderness, pain
- (rubor, calor, tumor, dolor)
three phases inflammation
- acute inflammation
- immune response
- chronic inflammation
ASA: moa
- NONSELECTIVE
- IRREVERSIBLE INHIBITOR COX-1 & COX-2
ASA: pharmacokinetics
- organic ACID
- fast, ORAL absorption
- HIGH CONCENTRATION IN STOMACH LUMEN (acidic)
- distribution throughout body - cross placental and BBB
- binds to plasma proteins
ASA: drug interactions
ASA competes w/ the following drugs for binding:
- T3, PEN G, thiopental, bilirubin, phenytoin, naproxen
(causes drug interaction)
ASA: metabolism
- low doses = first order kinetics
- high doses = zero order kinetics (above 600 mg)
- RENAL EXCRETION (alkalization of urine promotes excretion)
ASA: pharmacodynamics
- antiinflammatory
- analgesic
- antipyretic
- antiplatelet (irreversible inhibition of platelet COX enzymes)
ASA: uses
- mild/mod pain
- antipyresis
- anti-inflammatory
- MI/thrombosis prophylaxis
- long term use decr colon CA
ASA: adverse effects
- respiratory alkalosis
2. THEN, metabolic and respiratory acidosis
ASA: platelet effects
- inhibits platelet aggregation, so incr bleeding time
- effects last 8-10 days
ASA: avoided in pts w/ ___
- hypoprothrombinemia
- vit K def
- hemophilia
- severe hepatic damage
if a pt that takes ASA is going to have surgery, what should he/she do?
stop taking ASA AT LEAST ONE WEEK PRIOR to surgery
if a pt that takes ASA is pregnant, what should she do?
- avoid ASA prior to labor
ASA (low dose) & uric acid excretion
- decreases uric acid excretion
- elevates plasma urate concentration
(1-2 g ASA/day)
ASA (high dose) & uric acid excretion
- enhances uric acid secretion (uricosuria)
- lowers plasma urate concentration
(over 5 g/day)
ASA: side effects, cardiovascular
minimal in reg doses
ASA: side effects, lungs
ASPIRIN ASTHMA
- increased leukotriene synthesis
ASA: side effects, GI
- GI upset, gastritis, ulcer, bleeding
- to help, use buffering, food, misoprostol
ASA: side effects, kidneys
- renal damage, acute renal failure, interstitial nephritis
ASA & pregnancy
- NO TERATOGENIC effect
- stop aspirin before labor to prevent bleeding
salicylic acid & irritant effects (NOT ASA)
- destroys epithelial cells, irritant to mucosa
- used for removal of warts, corns, fungal infections, eczematous dermatitis
- methyl salicylates = irritating to skin and mucosa (oil of wintergreen)
ASA: avoid in patients w/ ___
- gastric ulcers
- hepatic damage
- hypoprothrombinemia
- vit K def
- hemophilia
- hypersensitivity to ASA/salicylates
when should ASA dose be decreased?
- long term therapy w/ oral anticoagulants & hypoglycemic agents (diabetes)
how much for acute salicylate poisoning?
- fatal = 20 g aspirin
- for methyl salicylate = 4-5 ml in children
Reye’s Syndrome?
- reason why don’t give ASA to kids
- cerebral edema in children w/ viral infection
DOC for Reye’s Syndrome?
acetaminophen
Celecoxib: moa
- SELECTIVE, REVERSIBLE COX-2 INHIBITOR
celecoxib: side effects
- less gastropathy (but still warning for GI bleed)
- INCREASED RISK CARDIOVASCULAR DISEASE
celecoxib: pharmacokinetics
- admin ORALLY
celecoxib: contraindications
- GI disease
- asthma
- breast feeding
- pregnancy
- renal failure
nonspecific reversible inhibitors of COX-1 & COX-2: info
- like ASA, but REVERSIBLE
- worst (but potent) = indomethacin
- first choice drug = ibuprofen (best side effect profile)
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, GI
- pain
- bleeding
- ulcer
- pancreatitis
- diarrhea
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, CNS
- HA
- dizziness
- confusion
- depression