Download Antiinflammatory Drugs

Antiinflammatory Drugs
Nonsteroidal Antiinflammatory Drugs (NSAIDs)
Aspirin (acetylsalicylic acid) -- only one that is an
irreversable inhibitor; less likely to cause
interstitial nephritis
Ibuprofin (IBU, Motrin, etc..) -- t1/2 is only 2 hrs.; better
tolerated than aspirin
Fenoprofin (Nalfon) -- longer acting than ibuprofin; t1/2
is about 13 hrs.
Ketoprofin (Orudis, Oruvail) -- inhibits both
lipoxygenase
AND cyclooxygenase
Diflunisal (Dolobid)
Sulindac (Clinoril)
Etodolac (Lodine)
Piroxicam (Feldene) -- long-acting
Nabumetone (Relafen) -- long-acting
Oxaprozin (Daypro) -- long-acting
Mefenamic acid (Ponstel)
Naproxen (Naprelan, Naprosyn, Anaprox)
Indomethacin (Indocin) -- more toxic, but often more
effective than the rest sometimes; used to
treat patent ductus arteriosus
Tolmetin sodium (Tolectin)
Phenylbutazone -- weak analgesic and antipyretic, but
it is a potent antiinflammatory agent; can
cause
agranulocytosis and aplastic anemia –
treatment is limited to 1 week
* Low dose aspirin gives analgesic and antipyretic effects
* High dose aspirin is required for antiinflammatory
actions
* Aspirin is not effective for visceral pain
*Low dose aspirin also inhibits platelet aggregation
* Antipyretic effect of NSAIDs is due to the inhibition of
interleukin-1 and other cytokine release
* Death from aspirin OD is due to respiratory and renal
failure (requires very high doses)
* Aspirin is contraindicated in pregnancy and in children
* Aspirin is highly protein bound and displaces
methotrexate, phenytoin, probenecid and others
Nonopioid analgesics
Acetaminophen -- active metabolite of phenacetin;
very little antiinflammatory activity; oxidation
by cyp-450 pathway releases a reactive
metabolite that causes centrilobular hepatic
necrosis, unless it’s detoxified by glutathione
Phenacetin -- not used any more because of its
toxicities
* N-Acetylcysteine can be used to treat acetaminophen
poisoning if it can be administered w/in 20 hrs of OD.
Arthritis drugs (slow-acting)
Gold salts -- reduse symptoms and slow progression of
rheumatoid arthritis; adverse effects include
dermatitis and diarrhea; may even cause
aplastic anemia; should follow NSAID treatment
Chloroquine -- used if NSAIDs are ineffective, or in
conjuction w/ NSAIDs; may cause blindness,
but this is very rare; contraindicated in
patients with psoriatic arthritis because of the
possibility of exfoliative dermatitis
D-Penicillamine -- reserved for patients unresponsive to
gold or chloroquine; antiinflammatory effects
take 3-4 MONTHS to set in; adverse effects are
severe and include leukopenia and/or
thrombocytopenia that may progress to (guess)
aplastic anemia
Methotrexate -- can cause a pneumonia-like condition
Corticosteroids -- do not alter the progressive destruction
of the bone and cartilage
Drugs to treat Gout
Colchicine -- drug of choice, except for its many
adverse effects: vomiting, abdominal pain,
alopecia, myopathy, agranulocytosis, and
(again) aplastic anemia; usually given IV
Indomethacin -- the drug most widely used to treat
acute gouty arthritis; limit treatment to 3 days
Phenylbutazone -- also limit treatment to 3 days
Allopurinol -- a substrate of xanthine oxidase, blocks
formation of uric acid from purines; used to
treat the primary hyperuricemia of gout;
often taken for life, usually well tolerated
Probenecid -- block proximal tubule reabsorption of
uric acid
Sulfinpyrazone -- also blocks uric acid reabsorption
* Aspirin is NOT used because in low doses it inhibits
the tubular secretion of uric acid (not good)
* Probenecid and sulfinpyrazone ALSO block uric acid
secretion at low doses; these should not be used in
patients excreting high levels of uric acid
* Allopurinol may actually precipitate and acute gouty
attack; this is prevented by co-administering colchicine
during the first few weeks of therapy
* Allopurinol also inhibits the metabolism of
probenecid
and oral anticoagulants
Vaccines
Bacterial vaccines
Pertussis -- from inactive B. pertussis
Cholera -- suspension of killed C. vibriae; boosters are
needed every 6 months
Typhoid -- acetone-killed S. typhi
M. tuberculosis -- the BCG vaccine
Plague -- suspension of inactivated Pasteurella pestis
Rickettsial vaccines
Epidemic typhus -- suspension of inactivated R.
prowazeki
from chicken egg embryos; frequent boosters
Rocky Mountain Spotted Fever -- egg grown suspension
of R. rickettsii
Viral vaccines
Influenza -- suspension of egg-grown Influenza virus;
only get partial protection
Poliomyelitis -- suspension of attenuated live virus types
1, 2, and 3; administered orally
Smallpox -- active Vaccina virus; it has been declared
eradicated by the WHO
Measles -- suspension of attenuated live Rubeola virus
Mumps -- suspension of attenuated live strains of the
mumps virus
Rubella
Yellow fever -- suspension of live attenuated virus from
chick embryos
Rabies -- phenol-inactivated tissue from infected
animals, in suspension; adverse effects are
resultant of an ineffective vaccination....
paralysis, encephalomyelitis, etc.
Passive immunizations
Diphtheria toxoid
Tetanus toxoid