anti inflammatories and related drugs (pharm at UVic) Flashcards
which NSAIDs are nonselective COXinhibitors
ibuprofen
diclofenac
aspirin
naroxen
which NSAIDs are selective COX2 inhibitors
celecoxib
which conditions are treatee by ASA, NSAIDS, acetaminophen
Bursitis Dysmenorrhea Fibromyalgia Gout Migraine Osteoarthritis RA Juvenile RA
which organ are NSAIDs hard on
kidneys
what is the prototype analgesic-antipyretic-antiinflm drug
ASA
other than ASA what drugs are analgesic-antipyretic-antiinflm drug
NSAIDs
acetaminophen
Drugs used to prevent or treat gout and migraine
are COX1 or COX 2 pathologic prostaglandins
what do they do
inflm
- vasodilation
- inc cap perm
- edema
- pain
leukocytosis\
activation of WBC to rel inflm cytokines
what does COX1 do and what are these aka
physiologica prostaglandins (aka)
GI protection
- dec gastric acid secretion
- inc mucus prod
- maint of GI mucosal perfusion
renal protection
-maint of renal perfusion
maint of renal fx
relaxes sm muscle tone
- vasodilation
- bronchodilation
regs platelet aggregation
what is primary dysmenorrhea d/t?
how is this involved/produced and what effect does it have?
**inc prostaglandins and vasopressin in primary dysmenorrhea -> **inc muscle contractions (cramping) and pain (make the uterine muscles contract and help the uterus shed the lining that has built up during the menstrual cycle. )
the prostaglandins are made in the uterus
if pain during menses why is this? in r/t prostaglandins
too many prostaglandins produced
what other conditions can prostaglandins produce
Prostaglandins can also cause headaches, nausea, vomiting and diarrhea.
TX of primary dysmenorrhea (meds)
NSAIDs (prostaglandin inhibitor) eg aspirin or ibuprofen
-naproxen sodium is stronger but requires a prescription
-extended cycle oral contraceptive (prevents excessive growth of uterine lining)
Tx of primary dysmenorrhea nonpharm
Therapies for primary dysmenorrhea include rest, heating pad to the lower abdomen or back, proper nutrition, aerobic exercise and medication. Nutrition therapy includes a well-balanced diet with an adequate intake of calcium (1000 mg. per day) and fluid intake of two quarts of water each day. Vitamin E about 500 units a day, Vitamin B1 about 100mg a day and Vitamin B6, 200 mg. each day, may occasionally be helpful.
when taking NSAIDs is it best with or without food
take w food to prevent GI upset
taking NSAIDS for dysmenorrhea what part of cycle is best?
specific dose?
- gen started 1-3 days prior to menstruation
- sometimes nec to take one of several NSAIDs until one with ma efficacy is found
how does hormonal alteration for dysmenorrhea alter pain
hormonal contraception prevents ovulation which dec thickness of uterine lining resulting in fewer prostaglandins
what is Depo-Provera and a consideration for this
it is a BC shot you get q10-12 wks
-MUST get adequate Ca2+ 1000mg
what kind of half-life do NSAIDs have
varies from short (less than hr) to longer than 12hrs
protein binding and NSAids
what % are bound
heavily bound
60-90%
metb of NSAIDs and ASA
in liver
**what side effects do almost all NSAIDS cause
***Virtually all NSAIDs can cause dyspepsia and GI toxicity including ulceration. Except celecoxib
aside from Gi upset what is a major consideration for almost all NSAIDs
what is exception to this
All except the nonacetylated salycilates? can effect bleeding time
is the effect that NSaids have on bleeding time reversible? which drug is the exception?
generally reversible except for aspirin which lasts the life of the platelet
where is Cox1 made
COX-1 is formed in all tissues and cells, especially platelets, endothelial cells, GI tract, and kidneys
where is COX-2 found
COX-2 is present brain, bone, kidneys, GI tract and female reproductive system
which dugs act on COX 1 or 2? what is the end result on the goal substance?
Aspirin, NSAIDs and acetaminophen inactivate cyclooxygenases, effectively blocking prostaglandin formation.
Does aspirin or NSAIDs
- act both centrally and periph to black pain impulses
- act periph to block pain impulses
aspirin-act both centrally and periph to black pain impulses
NSAIDs–act periph to block pain impulses
Does aspirin or NSAIDs
Act on hypothalamus to decrease temperature and reset thermostat
both do this
Does aspirin or NSAIDs
Prevents prostaglandins from increasing pain and edema
both do but I think NSAIDs more…it was **Prevents prostaglandins from increasing pain and edema
what is the antiplatelet activity of aspirin vs NSAIDs
which is longer acting
aspirinAntiplatelet effects by preventing synthesis of throboxane A2
NSAID-Antiplatelet effects bind reversibly with platelet COX-1 (shorter acting than aspirin)
Indications: celecoxib
elecoxib used to treat familial adenomatous polyposis
(some kind of lg intestine thing)
indications of NSAIDs and other antipyretic, anti inflm meds
Treat mild-moderate pain (may be combined with oral opioid)
- *Anti-inflammatory
- *Antipyretic
- *Antiplatelet - low dose cardioprotective
what is relationship of NSAIDs to eyes
may be used for eye disorders
but all NSAIDs cause dry eyes
contraindications
general
GI disorders
Hypersensitivity
Renal disease
*contraindication for aspirin
Aspirin is *****contraindicated for children in presence of viral infection due to association with Reye’s Syndrome
**celecoxib contra when..
pt is allergic to sulfonamides
what are the general categories of NSAIDs eg ..acid
- propionic acid derivatives
- acetic acid..
- mefenamic acid
- oxicam
- diclofenac
- celecoxib
which of these is ibuprofen and what the max dose
- propionic acid derivatives
- acetic acid..
- mefenamic acid
- oxicam
- diclofenac
- celecoxib
its a type of propionic acid derivative
the max is 2x400-3x200mg/day
so…800mg/day max?
what are the consequences of the acetic acid derivatives
- indomethacine and sulindac
- -GI ulceration, bone marrow depression, hemolytic anemia, mental confusion, depression and psychosis
Mefenamic acid (Ponstan): Oxicam drugs:
whih has a long half life and which causes GI upset
Mefenamic acid (Ponstan): GI upset Oxicam drugs: long half-lives
what is another major concern w celecoxib ** and wht is the dose
dose 100-400mg/day, iincreased risk of cardiovascular events such as MI and stroke with COX-2 inhibitors.
what is max dose for acetaminophen
4g
what are the names of the drugs used to treat gout and hyperuricemia
Allopurinol (Zyloprim)
Colchicine
Probenecid (Benemid)
Sulfinpyrazone (Anturan)
how do allopurinol and colchicine work (tx of gout)
Allopurinol prevents formation of uric acid by inhibiting xanthine oxidase.
Colchicine decreases inflm by decreasing the movement of leukocytes into body tissues containing urate crystals. It has no analgesic or anti-pyretic effects.
howdo probenecid and sulfinpyrazone work
Probenecid (Benemid) increases the urinary excretion of uric acid. This uricosuric action is used therapeutically to treat hyperuricemia and gout.
Sulfinpyrazone (Anturan) is a uricosuric agent similar to probenecid. It is not effective in acute gout but prevents or decreases tissue changes of chronic gout.
what is arthrotec and a consideration with this
arthrotec contains diclofenac and misoprostol (since this s protective of the stomach)
BUT! this will induce abortion so need to know if pregnant or trying to get pregnant
what are the two ways that drugs to treat migraines will help with them
medications used to treat acute pain,
medications used to prevent migraine headaches from occurring.
how should we think of a migraine
a neurovascular headache
