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Study points to cause of safety concerns in widely used painkiller diclofenac (Genetics, sex, and age greatly shift safe oral use)
Medical Xpress / Washington State University / Clinical Pharmacology & Therapeutics ^ | April 24, 2023 | Judith Van Dongen / Deepak Ahire et al

Posted on 04/25/2023 7:23:48 AM PDT by ConservativeMind

Safety concerns related to the widely used painkiller diclofenac may be tied to a little-studied drug-metabolizing enzyme whose expression can vary as much as 3,000 times from one individual to the next.

Used to combat pain and inflammation associated with arthritis, diclofenac was an over-the-counter drug. The FDA restricted it to prescription-only use following reports of the drug causing heart damage.

Previous findings by the WSU team had found a high degree of variability in the expression of UGT2B17, an enzyme that is a known player in diclofenac metabolism. That study showed that the enzyme is present at much lower levels in women than in men, which the researchers thought could explain the increased risk of heart damage seen in women taking diclofenac.

They also found that the enzyme is mostly absent in children under the age of nine and discovered large ethnicity-based differences in the number of people who lack the gene for the enzyme altogether, which ranges from around 20% of Caucasians up to around 90% of Japanese people.

The researchers used human liver and intestinal samples along with computer-based modeling to quantify the degree to which this enzyme contributes to diclofenac metabolism relative to other related enzymes. They found it to be a major player, supporting the idea that low levels of the UGT2B17 enzyme may be the cause of heart damage tied to diclofenac use.

Ahire said that their study found that this enzyme metabolizes diclofenac mainly in the intestine, unlike other related enzymes that are active mostly in the liver. As a result, the effect the researchers are seeing is specific to diclofenac tablets taken by mouth, which provides for the quickest absorption and pain relief. Just under half of prescriptions written for the drug in the U.S. are for oral diclofenac, Prasad said.

(Excerpt) Read more at medicalxpress.com ...


TOPICS: Health/Medicine
KEYWORDS: diclofenac; painkiller
Kids under 9 years of age, women (overall) 20% of Caucasians and 90% of Japanese people have possible safety concerns with oral use of diclofenac.

Voltaren is the brand name.

1 posted on 04/25/2023 7:23:48 AM PDT by ConservativeMind
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To: Mazey; ckilmer; goodnesswins; Jane Long; BusterDog; jy8z; ProtectOurFreedom; matthew fuller; ...

The “Take Charge Of Your Health” Ping List

This high volume ping list is for health articles and studies which describe something you or your doctor, when informed, may be able to immediately implement for your benefit.

Email me to get on either the “Common/Top Issues” (20 - 25% fewer pings) or “Everything” list.

2 posted on 04/25/2023 7:24:24 AM PDT by ConservativeMind (Trump: Befuddling Democrats, Republicans, and the Media for the benefit of the US and all mankind.)
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To: ConservativeMind

Voltarin is the cream, I think its still otc.


3 posted on 04/25/2023 7:35:38 AM PDT by Husker24 (Pp)
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To: ConservativeMind

Been taking it for several years now on an as needed basis.


4 posted on 04/25/2023 7:39:48 AM PDT by peggybac (My will is what I wanted. God's will is what I got.)
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To: ConservativeMind

“... researchers at the Yale School of Medicine found that nearly a third of those approved from 2001 through 2010 had major safety issues years after the medications were made widely available to patients.”

It continues.

When approved, doctors puff themselves up and call themselves “evidence-based” doctors...

But the evidence is redefined to mean only a drug or procedure that the FDA allowed - until it did not, and it maimed or kills. That is swept under the carpet and a pharma rep visits the office to offer cash payments, trips, etc.

Meanwhile, vitamin C is evil.


5 posted on 04/25/2023 7:44:21 AM PDT by aMorePerfectUnion (Fraud vitiates everything)
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To: Husker24
Voltarin is the cream, I think its still otc.

The cream version recently became an OTC. The pill version still required a prescription.

I use the cream for should and joint pain. It takes several days for it to work, but it does relieve the pain. Now, I use it occasionally when it feels like the pain is returning.

My Sister's doctor told her it also thins the blood, so excess use should be avoided.

6 posted on 04/25/2023 7:51:44 AM PDT by TomGuy
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To: ConservativeMind

Pain relief My A$$ !!! That crap is useless as politicians and ant piss.


7 posted on 04/25/2023 7:52:41 AM PDT by mabarker1 ( (Congress- the opposite of PROGRESS!!! A fraud, a hypocrite, a liar. I'm a member of Congress !7)
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To: mabarker1

It’s not useless to everyone. I just knew I was headed for shoulder surgery until my GP prescribed it. It took a couple of weeks, about a tube and a half, but I regained full use of my shoulder.


8 posted on 04/25/2023 8:00:00 AM PDT by EandH Dad (sleeping giants wake up REALLY grumpy)
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To: mabarker1

My doc prescribed it for me for shoulder pain. Didn’t do much for me and never re-uped the prescription after the first bottle. May still have it in a drawer someplace.


9 posted on 04/25/2023 8:12:16 AM PDT by moovova ("The NEXT election is the most importan.t election of our lifetimes!“ LOL...)
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To: EandH Dad

I’m talking about the pills.


10 posted on 04/25/2023 8:12:32 AM PDT by mabarker1 ( (Congress- the opposite of PROGRESS!!! A fraud, a hypocrite, a liar. I'm a member of Congress !7)
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To: moovova

Same here. I’ve got enough Rx’s that have been filled and were a waste of time. I could open a pharmacy with the crap I’ve been prescribed that doesn’t work.


11 posted on 04/25/2023 8:15:29 AM PDT by mabarker1 ( (Congress- the opposite of PROGRESS!!! A fraud, a hypocrite, a liar. I'm a member of Congress !7)
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To: ConservativeMind

this is affected by sex? but what if the person identifies as the opposite sex?

...

LMAO


12 posted on 04/25/2023 8:16:50 AM PDT by TexasFreeper2009
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To: mabarker1
Same here. I’ve got enough Rx’s that have been filled and were a waste of time. I could open a pharmacy with the crap I’ve been prescribed that doesn’t work.

I just give the meds to middle-school children.

13 posted on 04/25/2023 8:17:57 AM PDT by Lazamataz (The firearms I own today, are the firearms I will die with. How I die will be up to them.)
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To: Lazamataz

LOL 🤪


14 posted on 04/25/2023 1:01:50 PM PDT by mabarker1 ( (Congress- the opposite of PROGRESS!!! A fraud, a hypocrite, a liar. I'm a member of Congress !7)
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To: Lazamataz

You’re justa sharing -caring kinda guy👍💊


15 posted on 04/25/2023 1:02:49 PM PDT by mabarker1 ( (Congress- the opposite of PROGRESS!!! A fraud, a hypocrite, a liar. I'm a member of Congress !7)
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To: mabarker1

It works for me within a few minutes after I apply it. It had been prescribed for years as a topical cream for horses and I saw it worked so well for them that I decided to try it on myself. It’s great for my carpal tunnel syndrome.


16 posted on 04/25/2023 5:32:18 PM PDT by ottbmare (the OTTB mare)
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