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Relafen (Nabumentone)
clinical pharmacology: Rx List: "After oral administration, approximately
80% of a radiolabelled dose of nabumetone is found in the urine, indicating that
nabumetone is well absorbed from the gastrointestinal tract. Nabumetone itself
is not detected in the plasma because, after absorption, it undergoes rapid
biotransformation to the principal active metabolite, 6-methoxy-2-naphthylacetic
acid (6MNA). Approximately 35% of a 1000 mg oral dose of nabumetone is converted
to 6MNA and 50% is converted into unidentified metabolites which are
subsequently excreted in the urine. Following oral administration of nabumetone,
6MNA exhibits pharmacokinetic characteristics that generally follow a
one-compartment model with first order input and first order elimination." ******************************************************
Side effects to
consider while taking Relafen (Nabumetone): Natural Essentials: "More common
side effects may include: Abdominal pain, constipation, diarrhea, dizziness,
fluid retention, gas, headache, itching, nausea, rash, ringing in ears Less
common side effects may include: Dry mouth, fatigue, inability to fall or stay
asleep, increased sweating, inflammation of the mouth, inflammation of the
stomach, nervousness, sleepiness, vomiting Rare side effects may include:
Agitation, anxiety, confusion, dark, tarry, bloody stools, depression, difficult
or labored breathing, difficulty swallowing, fluid retention, general feeling of
illness, hives, increase or loss of appetite, large blisters, pins and needles,
pneumonia or lung inflammation, sensitivity to light, severe allergic reactions,
skin peeling, stomach and intestinal inflammation and/or bleeding, tremor,
ulcers, vaginal bleeding, vertigo, vision changes, weakness, weight gain, yellow
eyes and skin" ******************************************************
Drug
information data for Relafen (Nabumetone): Health Square: "Stomach and
intestinal ulcers can occur without warning. Remember to get regular check-ups.
Make sure the doctor knows if you have kidney or liver disease. Relafen should
be used with caution. This drug can cause fluid retention and swelling. It
should be used with caution if you have congestive heart failure or high blood
pressure. Relafen can cause increased sensitivity to sunlight. Possible food and
drug interactions when taking this medication If Relafen is taken with certain
other drugs, the effects of either could be increased, decreased, or altered. It
is especially important to check with your doctor before combining Relafen with
blood-thinning drugs such as Coumadin and aspirin. Other drugs with which
Relafen could possibly interact include: Diuretics (HydroDIURIL, Lasix) Lithium
(Lithonate) Methotrexate" ******************************************************
Health
professional version information for Relafen (Nabumetone): University of
Iowa Nursing: "Indications: Acute and chronic treatment of signs and symptoms of
osteoarthritis and rheumatiod arthritis, and other inflammatory conditions. May
be used as an analgesic and an antipyretic. Onset: From 30 minutes to several
hours or longer Peak Plasma Concentrations: 2.5-4 hours, plasma protein binding
90+% Steady State: After repeated doses once a day for 5 days, steady state is
reached after the 5th dose at once daily dosing Metabolism: Nabumetone is
metabolized in the liver to active metabolite, and excreted by the kidney
Half-Life: 22-30 hours, Half lfie is about 24 hours on the average." ******************************************************
Relafen
(Nubumetone) Contraindications and drug interactions: Arthritis Insight:
"Contraindications: Those who have had a prior allergic reaction to other NSAIDs
should not take Nabumetone. Nabumetone should be avoided in those with a history
of peptic ulcer or GI bleeding. Use during the third trimester of pregnancy is
not recommended. Nabumetone is not recommended for use in nursing mothers. Drug
Interactions: Nabumetone can increase the effect of anti-coagulants.Nabumetone
should not be taken with any other NSAIDs.Because of the potent nature of this
medicine, be sure to tell your doctor about any other medicines you are taking,
including nonprescription medicines and vitamins" ******************************************************
Relafen (Nubumetone)
side effects questions and answers: Excite drugs and health: "Question: For
the past few years, I have experienced muscle/joint pain in my left hip during
the spring and fall. My doctor has prescribed Relafen twice a day to relieve
this. Within a day or two, I have begun to experience bouts of allergic,
histamine reations such as tearing, runny nose, severe mucas drainage and
uncontrollable coughing which have lasted up to several hours at a time. This is
accompanied by wheezing and often, ear aches. Typically, I end up with a sinus
infection and have to take antibiotics. This pattern has been with me for 3
years now. I have been diagnosed as being allergic to my environment.Today, I
looked up Relafen on the internet and was suprised to find that patients with
allergic type reactions such as asthma should not take this medication. Is it
possible that I am allergic to Relafen and, that, for what ever reason I have
the muscle/joint pain, when I take it I start this cycle? I have told my current
physician of the coincidence, he doesn't think they are related, but doesn't
discount the possibility. Eventually the symptoms dissapear and I return to my
normal activities with no obvious side effects. What would trigger the
muscle/joint pain in the spring and fall? I have had xrays and have no joint
obvious joint disease. If you have any suggestions or opinions, please advise
me. Thank you. Answer: The reaction you are referring to is an increase in
asthma with these class of drugs in susceptible individuals. Aspirin would have
the same effect. The tearing and other allergy symptoms would not be expected to
be caused by Relafen. Have you seen a Rheumatologist? Been tested for connective
tissue diseases? If not, I would." ******************************************************
Relafen
(Nubumetone) general information: Nurses PDR: "Classification: Nonsteroidal
anti-inflammatory agent See Also: See also Nonsteroidal Anti-Inflammatory Drugs
.Action/Kinetics: Time to peak plasma levels: 2.5-4 hr. t1/2 of active
metabolite: 22.5-30 hr.Uses: Acute and chronic treatment of osteoarthritis and
rheumatoid arthritis. Has also been used to treat mild to moderate pain
including postextraction dental pain, postsurgical episiotomy pain, and soft
tissue athletic injuries.Contraindications: Lactation.Special Concerns:Safety
and efficacy have not been determined in children." ******************************************************
Relafen
(Nubumetone) Special studies: Health and Age: "Gastrointestinal: Relafen
(nabumetone) was compared to aspirin in inducing gastrointestinal blood loss.
Food intake was not monitored. Studies utilizing 51 Cr-tagged red blood cells in
healthy males showed no difference in fecal blood loss after 3 or 4 weeks'
administration of Relafen 1000 mg or 2000 mg daily when compared to either
placebo-treated or nontreated subjects. In contrast, aspirin 3600 mg daily
produced an increase in fecal blood loss when compared to the Relafen -treated,
placebo-treated or nontreated subjects. The clinical relevance of the data is
unknown. The following endoscopy trials entered patients who had been previously
treated with NSAIDs. These patients had varying baseline scores and different
courses of treatment. The trials were not designed to correlate symptoms and
endoscopy scores. The clinical relevance of these endoscopy trials, i.e., either
G.I. symptoms or serious G.I. events, is not known. Ten endoscopy studies were
conducted in 488 patients who had baseline and post-treatment endoscopy. In 5
clinical trials that compared a total of 194 patients on Relafen 1000 mg daily
or naproxen 250 mg or 500 mg twice daily for 3 to 12 weeks, Relafen treatment
resulted in fewer patients with endoscopically detected lesions less than
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Last updated by Andrew Lopez, RN on Thursday, January 28, 2010 |
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