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Lodine (Etodolac)
description: Drug Infonet: "Lodine (etodolac) is a pyranocarboxylic acid,
chemically designated as (±) 1,8
diethyl-1,3,4,9-tetrahydropyrano-[3,4-b]indole-1 -acetic acid. Lodine is a
racernic mixture of R- and S-etodolac. The structural formula for etodolac is
shown below: The empirical formula for etodolac is C17H21NO3. The molecular
weight of the base is 287.37. It has a pKa of 4.65 and an n-octanol; water
partition coefficient of 11.4 at pH 7.4. Etodolac is a white crystalline
compound, insoluble in water but soluble in alcohols, chloroform, dimethyl
sulfoxide, and aqueous polyethylene glycol.The inactive ingredients present in
the capsules are cellulose, gelatin, iron oxides, lactose, magnesium stearate,
povidone, sodium lauryl sulfate, sodium starch glycolate, and titanium
dioxide.The inactive ingredients present in the tablets are cellulose, FD&C
Yellow #10, FD&C Blue #2, FD&C Yellow #6, hydroxypropyl methylcellulose,
lactose, magnesium stearate, polyethylene glycol, polysorbate 80, povidone,
sodium starch glycolate, and titanium dioxide.Lodine is available in 200 and 300
mg capsules and 400 mg tablets for oral administration."
http://www.druginfonet.com/lodine.htm#DESCRIPTION
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Lodine
(Etodolac) pharmacology: Rx List: "Etodolac is a nonsteroidal
anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and
antipyretic activities in animal models. The mechanism of action of etodolac,
like that of other NSAIDs, is not known, but is believed to be associated with
the inhibition of prostaglandin biosynthesis.Pharmacokinetics The activity of
Lodine XL is due to the parent drug, etodolac. The free fraction is less than 1%
and is independent of concentration over the therapeutic range. Etodolac is not
dialyzable. Etodolac is extensively metabolized in the liver, with renal
elimination of its metabolites. The terminal half-life ranges between 7.3 and
8.3 hours. Less than 1% of the dose is excreted unchanged in urine.Absorptions
Lodine and Lodine XL both contain etodolac, but differ in their release
characteristics. The systemic availability of etodolac from Lodine XL is
generally greater than 80%. After administration of 400 mg of Lodine XL, a Cmax
of 8.6 µg/mL was observed 3 to 12 hours post dose. Peak concentrations are dose
proportional for both total and free etodolac following Lodine doses up to 400
mg every 12 hours, but following a 600 mg dose, the peak is about 20% higher
than predicted on the basis of lower doses. After oral administration of Lodine
XL in doses of 800 mg once daily, peak concentrations are dose proportional for
both total and free etodolac whereas peak concentrations following 1200 mg
Lodine XL once daily were about 20% lower than that predicted by lower doses.
Table 1 shows the comparison of pharmacokinetic parameters for etodolac and
Lodine XL."
http://www.rxlist.com/cgi/generic/etodolac_cp.htm
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Less and more
common side effects of Lodine (Etodolac): Natural Essentials: "More common
side effects may include: Abdominal pain, black stools, blurred vision, chills,
constipation, depression, diarrhea, dizziness, fever, gas, increased frequency
of urination, indigestion, itching, nausea, nervousness, rash, ringing in ears,
painful or difficult urination, vomiting, weaknessLess common side effects may
include:Abdominal bleeding, abnormal intolerance of light, anemia, asthma, blood
disorders, congestive heart failure, dry mouth, fainting, flushing, hepatitis
and other liver problems, high blood pressure, high blood sugar in some
diabetics, hives, inability to sleep, inflamed blood vessels, inflammation of
mouth or upper intestine, kidney problems, including kidney failure, loss of
appetite, peptic ulcer, rapid heartbeat, rash, severe allergic reactions, skin
disorders including increased pigmentation, sleepiness, Stevens-Johnson syndrome
(peeling skin), sweating, swelling (fluid retention), thirst, visual
disturbances, yellowed skin and eyes"
http://www.naturalessentials.com/lodine.htm
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Pharmacokinetic
Summary of Lodine (Etodolac): Sunnybrook and Woman's College Health Sciences
Centre's: "In clinical trials, most adverse reactions observed were mild and
transient. Fluid retention and edema have been observed as has gastrointestinal
discomfort. In patients treated for three to six months the incidence of upper
GI ulcers, gross bleeding or perforation is approximately 1% and this increases
to 2-4% after one year of treatment[4]. The recommended dose of etodolac for
acute pain is 200 to 400 mg every 6 to 8 hours, as needed, not to exceed a total
daily dose of 1200 mg[4].Etodolac is a pyranocarboxylic acid non-steroidal
anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic
activities. Etodolac is more than 99% bound to plasma proteins. The free
fraction is less than 1% and is independent of etodolac total concentration.
Less than 1% of etodolac is excreted unchanged in the urine[1]."
http://www.icomm.ca/shsc/kinetics/etodolac.html
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Clinical information about
Lodine (Etodolac): Doctor's Guide: "Clinical trials have established that
Lodine XL is effective in managing the pain and inflammation associated with
osteoarthritis and rheumatoid arthritis. In one study of Lodine XL used for the
treatment of rheumatoid arthritis (RA), 500 mg of Lodine XL taken as two tablets
once daily was found to be effective in relieving the symptoms of RA, especially
morning stiffness -- which is significant because it indicates that Lodine XL
500 mg was working to relieve inflammation throughout the night. This is an
important benefit of Lodine XL -- it can relieve arthritis symptoms around the
clock"
http://www.pslgroup.com/dg/58112.htm
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Special warnings
about Lodine (Etodolac): Health Square: "Peptic ulcers and bleeding can
occur without warning. You may have other problems with bleeding as well. Call
your doctor if you have any signs or symptoms of stomach or intestinal ulcers or
bleeding, blurred vision or other eye problems, skin rash, weight gain, or fluid
retention and swelling. This drug should be used with caution if you have kidney
or liver disease; and it can cause liver inflammation in some people. Do not
take aspirin or any other anti-inflammatory medications while taking Lodine,
unless your doctor tells you to do so. If you are taking Lodine over an extended
period of time, your doctor should check your blood for anemia. This drug can
increase water retention. Use with caution if you have heart disease or high
blood pressure."
http://www.healthsquare.com/newrx/LOD1232.HTM
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Clinical Trials: Studies
in pain relief of Lodine (Etodolac) comprehensive drug info included: Wyeth
Info: "Controlled clinical trials in analgesia were single-dose,
randomized,double-blind,parallel studies in three pain models, including dental
extractions. The analgesic effective dose for Lodine established in these acute
pain models was 200 to 400 mg. The onset of analgesia occurred approximately 30
minutes after oral administration. Lodine 200 mg provided efficacy comparable to
that obtained with aspirin (650 mg). Lodine 400 mg provided efficacycomparable
to that obtained with acetaminophen with codeine (600 mg + 60 mg). The peak
analgesic effect was between 1 to 2 hours. Duration of relief averaged 4 to 5
hours for 200 mg of Lodine and 5 to 6 hours for 400 mg of Lodine as mea-sured by
when approximately half of the patients required remedication."
http://www.wyethinfo.com/etodolac.htm
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Etodolac (Etogesic Rx) a
pain reliever for dogs with arthritis: Vet Info: "Etodolac (Etogesic Rx) is
a non-steroidal anti-inflammatory (NSAID) medication. It is a relatively new
medication and it is considered to be less likely to upset the gastrointestinal
tract than older NSAIDs, such as aspirin. This medication can be used long term
but it is recommended to use the lowest dose that will work to control the pain
when long term use is necessary. A similar medication, carprofen (Rimadyl Rx)
has been associated with liver problems in a small number of dogs and it is
possible that this effect could surface for etodolac, as well. If there are any
signs of decreased appetite, loss of appetite, lethargy or anything that
concerns you while your dog is on this medication it would be best to
discontinue it and call your vet as soon as symptoms are noted."
http://www.vetinfo.com/detogesic.html
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