Pharm Flashcards
Cox 1 actions
renal function bronchodilation/constriction acute prostaglandin production gastric cytoprotection platelet aggregation
cox 2 actions
renal function
bronchodilation/constriction
sustained prostaglandin production
COX1 and COX2 shared functions
renal function
bronchodilation/constriction
COX1 only functions
gastric cytoprotection
platelet aggregation
PGE1
vasodilation
maintenance of patent ductus arteriosus
PGE2
vasodilation diuresis- Na and K loss in urine patent ductus arteriosus gastric cytoprotection pain sensitization fever uterine and GI smooth muscle contraction relaxation of respiratory smooth muscle
PGF2
vasoconstriction
increased aqueous humor drainage
uterine, GI, and respiratory smooth muscle contraction
changes in vessel diameter
vasodilation- PGE1, PGE2, PGI2
vasoconstriction- PGF2, TXA2
uterine changes
contraction- PGE2, PGF2
relaxation- PGI2
GI contraction
PGE2
PGF2
respiratory changes
contraction- PGF2, TXA2, leukotrienes C, D, E
relaxation- PGE2, PGI2
PGI2
vasodilation- diuresis, NA and K loss in urine
gastric cytoprotection
pain sensitization
fever
relaxation of uterine and respiratory smooth muscle
prevents spontaneous platelet aggregation- inhibits TXA2
gastric cytoprotection
PGE2
PGI2
pain sensitization
PGE2
PGI2
leukotrienes (LTB4)
fever
PGE2
PGI2
TXA2
vasoconstriction
contraction of respiratory smooth muscle
platelet aggregation
platelet aggregation
inhibit- PGI2
promote- TXA2
LTC4, LTD4, LTE4
bronchoconstriction
increased vascular permeability
LTB4
chemoattraction
pain sensitization
EP1
fever
EP2
vascular smooth muscle relaxation
EP3
vascular smooth muscle relaxation decreased gastric acid secretion increased gastric mucus secretion uterine contraction fever
EP4
vascular smooth muscle relaxation
pain sensitization
budesonide
short half life
used in asthma inhalers
easily penetrates airway mucosa
dexamethasone
very potent
long half life
oral, parenteral, topical
multipurpose
fluticasone
asthma inhalers and nasal sprays
medium potency
short half life
hydrocortisone (cortisol)
low potency OTC for skin
also used PO and parenteral
used for adrenal insufficiency replacement
medium half life
mometasone
medium potency
asthma and skin
not metabolized in skin, so can cause local side effects
systemically absorbed
*not as commonly used as budesonide or fluticasone
prednisone
long half life
prodrug metabolized by liver
PO only
used for inflammatory conditions
prednisolone/methylprednisolone
active metabolite of prednisone
used in hepatic disease patients
PO, inject, eye drops
no bioactivation required
triamcinolone
oral, injection, topical
potency depends on formulation
causes skin issues like mometasone
ibuprofen
COX1
pain, fever, OA, RA, dysmenorrhea
topical for MSK and dental
pediatric- fever
naproxen
COX1
similar to ibuprofen
LONG half life
used 2x daily for arthritis
piroxicam
COX1
OA, RA
long half life- once daily
noncox mediated anti-inflammatory effects
high doses more likely to cause peptic ulcers than other NSAIDs
indomathacin
COX1
extensive toxicities with severe sideffects
used to reverse acute disorders- pericarditis, patent ductus closure, acute gout attack
few, night time doses
sulindac
COX1 RA, OA, gout polyp regression in familial adenomatous polyposis prodrug less GI irritation high CNS effects enterohepatic recycling
ketoralac
COX1 analgesic- better than morphine used with opioids and reduces required opioid dose not anti-inflammatory high risk renal toxicity do not use more than 5 days renal impairment- contraindication
nabumetone
COX1 and COX2 OA, RA, pain non acid NSAID metabolized to weak acid to be activated >24 hour half life pseudoporphyria and photoinsensitivity
etodolac
COX2
OA, RA
less GI ulceration
diclofenac
OA, RA
less likely to cause GI ulcerations
topical gel for localized arthritis
more likely to elevate liver enzymes
celecoxib
cox 2 selective
OA, RA
promote regression of polyps
lower GI ulceration, but can delay healing of existing ulcers
increased risk of Cardiovascular adverse efects
meloxicam
cox 2 selective
OA, RA
low doses have fewer GI sed effects
activity is dose dependent
