Gout Medication

Picture of Generic ColchicineGout medications do have a place in the War on Gout . . . LAST place!

You know that I’m all about treating gout naturally, without pharmaceuticals.  But, I’ve written this article as a kind of “public service announcement” so that my website can answer all your gout related questions.  This does NOT mean that I advocate the use of pharmaceuticals . . . disclaimer out of the way . . . here we go.

Now keep in mind, these are ONLY the pharmaceutical type of gout medications . . . this list does NOT include the hundreds of natural gout medicines that are effectively used worldwide.

Detailed Chart of Gout Medications

Gout medications basically fall into two categories: 

  1. Prevention
  2. Treatment.

Gout Medications Used For Prevention

There are four categories of medicines used for gout prevention:

  1. Xanthine Oxidase Inhibitors – which work to limit the production of uric acid
  2. Uricosurics – which work to increase the elimination of uric acid via the kidneys
  3. Uricolytics – which act as a substitute for the enzyme “uricase” which humans no longer have, that converts uric acid into allantoin so that it can be more easily excreted
  4. Other Therapeutic Options – including experimental possibilities

Xanthine Oxidase Inhibitors

Xanthine oxidase inhibitors work by blocking an enzyme called “xanthine oxidase” which is responsible for the conversion of hypoxanthine into xanthine, and eventually into uric acid . . . causing a decrease in uric acid levels in your blood and urine.  Basically these drugs work to minimize the conversion of purines into uric acid.

There are two xanthine oxidase inhibitor gout medications available today, and they are very similar in how they work:  Allopurinol and Febuxostat.

ALLOPURINOL

The gout medicine “Allopurinol” is the oldest and most widely used gout medication in the world today. It works in the body by mimicking hypoxanthine (a type of purine) because it has the exact same structure as hypoxanthine.

It is prescribed for many different medical conditions, but in the case of gout it is prescribed for people who overproduce uric acid, because it decreases the formation of uric acid.

Allopurinol is the generic name of this gout medicine, and it is available under the following brand names:  Zyloprim®, Aloprim® Allohexal®, Allosig®, Milurit®, Alloril®, Progout®, Zyloric®, Zyrik® and Aluron®

Febuxostat

The gout medicine “Febuxostat” is a newer drug that works as a “non-purine selective inhibitor” of xanthine oxidase, which means it works by blocking the active receptor sites on the xanthine oxidase enzymes.

Febuxostat has been proven in clinical studies to lower uric acid levels in the blood more potently than allopurinol, with fewer effects on the enzymes which are involved in purine and pyrimidine metabolism.

Febuxostat is the generic name for this gout medicine, and it is available under the following brand names:  Uloric®, Adenuric®, and Febutaz®

Uricosurics

Uricosuric gout medications are drugs that increase the excretion of uric acid in the urine, instead of inhibiting its production (like the xanthine oxidase inhibitors described above).   Uricosuric gout medicines lead to reduced levels of uric acid in blood. Although they are better tolerated (have fewer side effects) than xanthine oxidase inhibitors, they are also less effective.

There are four uricosuric gout medications available today:  Probenecid, Sulfinpyrazone, Benzobramone, and Lesinurad.

Probenecid

The gout medicine “Probenecid” works by increasing the portion of uric acid that gets excreted in urine, versus the portion that gets retained in the blood.  Let me explain:  As the kidneys filter uric acid out of the blood, some percentage of it gets “reabsorbed” back into the blood.  Probenecid limits the resorption of uric acid by interfering with the organic ion transporter (OAT) in the kidneys.

Probenecid is prescribed for people who have chronic gouty arthritis as well as tophaceous gout.  It has also been shown to be effective at lowering hyperuricemia resulting from the use of diuretics.

Probenecid is the generic name for this gout medicine, and it is available as the following brand names: Benemid®, Benuryl®, Probalan®, Probecid®, Proben®

Sulfinpyrazone

The gout medicine “Sulfinpyrazone” works in a very similar way as Probenecid, in that it limits the resorption of uric acid in the kidneys.  The difference is that Sulfinpyrazone does this by inhibiting the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4) in the kidneys.

Currently the branded and generic forms of Sulfinpyrazone have been discontinued in the US for unknown reasons. The FDA has stated that the discontinuation is not for safety reasons.

Sulfinpyrazone is the brand name of this gout medicine, and its brand names are:  Anturan® and Anturane®.

Benzbromarone

The gout medicine “benzbromarone” is a uricosuric drug that was approved in the 1970’s for use in many countries in Europe, Asia, and South America . . . but not in the United States, due to concerns about liver toxicity.  A small but significant number of patients on this drug developed liver injury, and some developed liver failure and died.

Benzbromarone is still prescribed on a “named patient basis” in much of Europe, which means it is not approved for use in the general population. A doctor can override this restriction on a case by case basis if deemed appropriate.

Benzbromarone is highly effective at reducing uric acid levels in the blood, and clinical trials as recent as 2008 have shown its effectiveness to be superior to Allopurinol, Probenecid and other uricosuric drugs.

Lesinurad

The upcoming gout medication “Lesinurad” is currently in phase 3 of clinical trials (as of Feb. 2013) and has been shown to reduce uric acid levels in the blood when taken both alone and alongside xanthine oxidase inhibitors.  It works primarily by inhibiting the URAT1 transporter, and to lesser degree by inhibiting the OAT4 transporter, in order to limit the resorption of uric acid in the kidneys.

Once approved, Lesinurad is expected to be prescribed for people only after their uric acid levels have not been sufficiently reduced through the use of Allopurinol or Febuxostat alone.

 . . .

Hi Bert

 

Just to let you know, and I was surprised how quick you answered my email.  I meant to Thank You, in the last email.  4 Days ago I could hardly walk, and thanks to you I’m walking, without any medication.  I did do another treatment, but I’m still a little sore in my toe and ankle, and now little in both wrists, which I did not have yesterday.  Just wondering what I should do now?  I’m going out today to pick some of the ingredients today.

 

Thanks Again,
Glen

. . .

Uricolytics – Uricase

Uricolytic gout medications are drugs that work by helping convert uric acid into allantoin.  Allantoin results from the breakdown of uric acid, and is 5-10 times more soluble than uric acid.  Thus, it is excreted more readily than uric acid through the urine, whic results in lower levels of uric acid in the blood.

All mammels, except humans and higher-apes, have an enzyme in the liver called uricase, which converts uric acid into allantoin, and this is how they keep their uric acid levels in moderation.  However, humans and higher-apes seem to have lost this enzyme (uricase) through the course of evolution.

The uricolytic gout medications function as substitutes for the lost enzyme uricase, and promote the conversion of uric acid to allantion so it is excreted better.  In contrast to drugs which prevent uric acid production, the uricolytic drugs work by reducing uric acid stores, both in the blood and in tophi.

Currently, there are two types of uricolytic gout medicines available:  Rasburicase and Pegloticase.

Rasburicase

The gout medicine “Rasburicase” was originally developed for the prevention or management of hyperuricemia in pediatric cancer patients experiencing Tumor Lysis Syndrome. Case studies have shown that Rasburicase can lower blood uric acid levels in gout patients, but the drawback is that Rasburicase is highly “immunogenic”.  This means that after 1 or 2 doses are given, the person’s body recognizes Rasburicase as a “foreign substance” and renders it neutral so that it no longer works.  The immunogenic effect also creates severe hypersensitivity reactions.

Raburicase was hoped to be helpful to people experiencing “refractory gout”, which is gout that does not respond to other urate lowering drugs.  However, because of the immunogenic problems, its use was discontinued and has since been replaced by a similar drug, Pegloticase.

Rasburicase is the generic name of this gout medicine, and its brand name is Elitek®

Pegloticase

The gout medicine “Pegloticase” was developed to overcome the immunogenic problems found with Rasburicase, using a process called “pegylation” which is the alteration of proteins by the addition of several chains of polyethylene glycol.  Pegylation is a strategy to mask the antigenicity of foreign proteins and permit their administration as therapeutic agents.

Pegloticase is prescribed for people with “refractory gout” where their uric acid levels are not being lowered by the more commonly used drugs Allopurinol or Febuxostat.  Pegloticase is also being prescribed for people with tophaceous gout, since it has shown the ability reduce and resolve tophi lumps.

Pegloticase is the generic name for this gout medicine, and it is available under the brand name Krystexxa®.

Other Therapeutic Gout Medications

The following medicines are not typically prescribed for gout, however they have been shown to lower uric acid blood levels.  Thus, they are sometimes prescribed for dual purposes as discussed below.

There are 3 gout medications in this category:  Losartan, Fenofibrate, and Rilonacept.

Losartan as a Gout Medicine

The potential gout medicine “Losartan” is an angiotensin receptor blocker that is normally prescribed for people with high blood pressure.  However, it was found to also be moderately effective at lowering uric acid levels in the blood.  It achieves this result through a uricosuric action, because it acts to inhibit the URAT1 transporter in the kidneys which reduces the resorption of uric acid back into the blood.

As such, Losartan is sometimes prescribed as a gout medicine for people who also have hypertension.

Lozartan is the generic name for this hypertension + gout medication, and it is available under the trade name:  Cozaar ®.

Fenofibrate

The potential gout medicine “Fenofibrate” is a triglyceride-lowering drug that is normally prescribed for people with high cholesterol levels.  However, in 1980 it was found to also have moderately potent uricosuric effects, meaning that its use also resulted in lowered blood uric acid levels.  The uricosuric benefits appear to be modulated through the UGT2B7 A-327G genes.

As such, Fenofibrate is sometimes prescribed as a gout medicine for people who also have hypertriglyceridemia, or high cholesterol levels.

Fenofibrate is the generic name for this cholesterol + gout medicine, and it is available under the following brand names:  Tricor®, Lipofen®, Triglide®, Lofibra®, Fenoglide®, Antara®.

Rilonacept

The potential gout medicine “Rilonacept” is a “fusion protein” drug that is normally prescribed for people with CAPS (cryopyrin-associated periodic syndromes).  However, it was shown in early studies to reduce the incidence of gout flares brought on by the initiation of urate-lowering drug therapy.

It is well known that when a person begins to take Allopurinol their risk of having a gout attack goes UP for the first few months.  Rilonacept is being explored as a drug to prevent those gout attacks that occur as a result of starting on Allopurinol.

However, in May of 2012 the FDA Advisory Panel voted 11-0 against the approval of rilonacept for the treatment of gout, stating that “the benefits did not outweigh the risks”.

Rilonacept is the generic name for this potential gout medicine, and it is currently available as a drug for people with CAPS under the trade name:  Arcalyst®.

Gout Medications Used for Treatment

The so-called “treatment” of active gout flares is accomplished through anti-inflammatory gout medications. These work by reducing the inflammatory response, and thus are basically treating the symptoms of gout, not the cause. There are 4 types of anti-inflammatories used today for treating (not preventing) gout attacks:

  1. NSAIDS:  Non-steroidal Anti-inflammatory Drugs
  2. Colchicine
  3. Corticosteroids
  4. Anakinra

NSAIDs

NSAIDS, or Non-Steroidal Anti-Inflammatory Drugs, are widely prescribed to treat acute inflammation in patients who can safely take them. However, the pain relieving effects of NSAIDs for the treatment of gout attacks are known to vary from patient to patient.  Some people do get pain relief, and others do not, from the use of NSAIDS.  And some have dramatic adverse reactions to NSAIDS.

NSAIDS reduce inflammation by creating a series of events, like a chain-reaction:  First the NSAID inhibits an enzyme called cyclo-oxygenase (COX), which in turn limits the production of prostaglandin, which then has a reduced ability to initiate the rest of the inflammatory response.

Two different COX enzymes have been identified, called COX 1 and COX 2.  The COX 1 Inhibitors are older drugs, and while they do create the anti-inflammatory benefit they also have more undesired side effects.  The COX 2 Inhibitors are newer drugs, and are more targeted to create the anti-inflammatory benefit with fewer undesirable side effects.

NSAIDS fall into two categories, as listed below with both the generic names and (brand names):

Non-selective COX Inhibitors

The following Non-Selective COX Inhibitors will inhibit both the COX 1 and COX 2 enzymes, and thus will have more side effects than the Selective COX 2 Inhibitors.  They are listed below with their generic names and their (brand names):

  • Acetylsalicylic acid (Aspirin)
  • Indomethacin (Indocin)
  • Ibuprofen (Motrin, Advil, Nuprin)
  • Naproxen Sodium (Aleve, Anaprox, Midol Extended Relief, Naprosyn)
  • Ketorolac (Toradol, Sprix)
  • Sulindac (Clinoril)
  • Pioxicam (Feldene)
  • Diflunisal (Dolobid)

Indomethacin is a Non-Selective COX Inhibitor, and has become the “drug of choice” that most doctors like to prescribe, even though it is “non-selective” and many people do not tolerate it well.

Selective COX 2 Inhibitors

The following Selective COX 2 Inhibitors will inhibit ONLY the COX 2 enzyme, thus will have fewer sides effects than the Non-Selective types.  They are listed below with their generic names and their (brand names):

  • Celecoxib (Celebrex)
  • Meloxicam (Mobic)
  • Valdecoxib (Bextra)
  • Nabumetone (Relefen)
  • Etodolac (Lodine)

Colchicine

Colchicine is a gout medication that is derived from an herb called Autumn Crocus.  The exact way that colchicine works to help with gout is not completely understood, but it is theorized that it interrupts the cycle of monosodium urate crystal deposition in joint tissues.  This then interrupts the inflammatory response that creates the pain of an acute gout attack.

Colchicine decreases the inflammatory response through a binding of the micro-tubular proteins, which interfere with granulocyte mobility.  Thus, Colchicine is prescribed for relief of pain in acute gouty attacks.

Colchicine is the generic name of this gout medicine, and it is available under the brand names:  Colcrys®, and Proben-C® which is a combination of Probenecid and Colchicine.

Corticosteroids

Corticosteroids are potent gout medications which can be used to reduce the inflammation and pain of an acute gout attack, but typically are only prescribed if:

  1. NSAIDS and Colchicine are found to be ineffective
  2. The severity of the gout attack warrants the risks of the significant side effects that come with steroid use

Corticosteroids can be given either by oral pills, intra-muscular injection (directly into a muscle), intravenous injection (directly into a vein), intra-articular injection (directly into the joint).  Also, adrenocorticotropic hormone (ACTH) can be given via intramuscular injection, which works indirectly through the adrenal axis. However, ACTH has not been shown to be more effective than systemic corticosteroids for treatment of gout inflammation.

The short-burst corticosteroid regimen used to treat an acute flare of gout is generally well tolerated, but is associated with the same adverse effects seen with long-term steroid use.

In gouty events that only involve 1 or 2 joints, intra-articular corticosteroids are an effective treatment option, as long as there is no infection present in the joint.

Corticosteroids are available through numerous generic formulations, each with their own brand names.  Following is a partial list of the generic corticosteroids, with their brand names in parentheses:

  • Triamcinolone Acetonide (Kenalog®)
  • Triamcinolone hexacetonide (Aristospan®)
  • Prednisone (Deltasone®)
  • Hydrocortisone (Cortef®)
  • Methylprednisolone (Medrol®)

Anakinra (IL1)

Anakinra is an “interleukin-1 receptor antagonist” drug that is normally prescribed for people with rheumatoid arthritis, in order to control inflammation and cartilage degradation.  However, Anakinra has also been found to help relieve the painful inflammation associated with gout attacks.

In 2007 an open-labeled pilot study was conducted on 10 patients who had “refractory acute gout”, meaning that their inflammation did not respond to other anti-inflammatory drugs.  They were given Anakinra daily for 3 days in a row, and by the 2nd day of treatment the pain was substantially reduced in all 10 patients, without side effects. Clinical signs of inflammation had disappeared in 9 of 10 patients by the 3rd day of treatment.

As such, further controlled clinical studies are proceeding in order for Anakinra to be approved as a gout medicine by the FDA.

Anakinra is the generic name for this potential gout medication, and it is currently available as a drug for rheumatoid arthritis under the brand name:  Kineret®.

Summary of Gout Medications

As I said at the beginning of this article, gout medications do indeed have a place in the War on Gout . . . LAST place! All of the gout medications above come with detrimental effects to your overall health, which can and should be avoided at all costs.  I strongly encourage you to become very proactive in managing your gout with natural methods.

To learn more about how I manage my gout naturally, check out my book Kill Your Gout NOW!

 

 + References

Harris, M (1999). Gout and Hyperuricemia. American Family Physician. Retrieved from
https://www.aafp.org/afp/1999/0215/p925.html

Rothschild, B(2013). Gout and Pseudogout Treatment & Management. Emedicine.medscape.com. Retrieved from https://emedicine.medscape.com/article/329958-treatment

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