Can CBD help with arthritis? 

  • A study in Neuroscience Letters in 2011 found that CBD might help reduce acute joint inflammation in animal models by affecting the way pain receptors respond to stimuli(1).
  • Data from a 2016 study in The European Journal of Pain indicated that a topical application of CBD could help relieve arthritis pain-related behaviors and inflammation in animal subjects without evident side-effects(2).
  • Researchers of a study published in the journal Pain in 2017 noted that local administration of CBD blocked osteoarthritis pain in rats(3). They concluded that CBD’s therapeutic benefits were due to its nerve-protective and anti-inflammatory properties on the joints.
  • A 2018 study in Arthritis Care & Research found that people who have rheumatoid arthritis (RA) are more likely to experience anxiety, depression, and bipolar disorder in their lifetimes than those who have not been diagnosed with the autoimmune disease(4).
  • A study published in the journal CNS and Neurological Disorders – Drug Targets noted that CBD, a Cannabis Sativa component with psychiatric benefits, had therapeutic uses as an anti-anxiety-like and an antidepressant-like compound(5).

Best CBD Oils for Arthritis

Editor's Pick

Spruce 750mg Lab Grade CBD Oil

Specifically formulated to be more palatable to CBD users
Spruce 750mg Lab Grade CBD Oil Bottle
  • Overall Clinical Score
    99%
    Editor's Pick
  • Score breakdown
    Value
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  • Summary

    Each bottle of the 750mg CBD oil tincture contains 25mg of CBD per dropper full. The oil is peppermint flavor to mask any unpleasant tastes related to CBD.

    Pro's
    Cons's
    •  Mid-strength
    •  Natural peppermint flavor
    •  Made from 100% organic and natural ingredients
    •  No other flavors
  • Features
    Discount pricing available?20% Off Coupon Code: CBDCLINICALS
    Source
    Source of Hemp
    Kentucky, USA & North Carolina, USA
    FormOil Tincture
    IngredientsOrganic Hemp Seed Oil, Full Spectrum CBD Oil
    Type
    Type of CBD
    Full Spectrum
    Extraction
    Extraction Method
    Moonshine extraction method
    How to take itUnder tongue
    Potency
    Potency - CBD Per Bottle
    750 mg per bottle
    Carrier OilOrganic Hemp Seed Oil
    Concentration
    CBD Concentration Per Serving
    25mg of CBD per dropper full (1ml)
    Drug TestContains 0.3% THC but there is a chance you may test positive for marijuana
    FlavoursPeppermint
    Price Range$89 ($75.65 for subscriptions, 15% discount from regular price)
    $/mg CBD
    Price ($/mg)
    $0.12/mg ($0.10/mg with subscription)
    Shipping
    Shipping/Time to delivery
    2-4 business days (first class USPS)
    Lab Tests
    Lab Testing Transparency
    Third Party Lab Tested post formulation for safety and potency, available on website
    ContaminantsOrganic, Non-GMO, no pesticides, no herbicides, no solvents or chemical fertilizers, No preservatives or sweeteners
    AllergensVegan, Gluten free
    Refund policyWithin 30 days
    Recommended forNew CBD users
    Countries servedUSA only (all 50 states)
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Best Organic

NuLeaf Naturals 900mg Full Spectrum Hemp CBD Oil

Perfect for anyone who are looking for CBD products that promote a healthy body and mind.
NuLeaf Naturals 900mg Full Spectrum Hemp CBD Oil
  • Overall Clinical Score
    99%
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  • Summary

    Natural remedy for various illnesses. NuLeaf Naturals’ CBD oil is a whole-plant extract containing a full spectrum of naturally occurring synergistic cannabinoids and terpenes.

    Pro's
    Cons's
    •  Pure CBD hemp
    •  All natural
    •  Approximately 300 drops total
    •  No other flavors
  • Features
    Discount pricing available?20% Off Coupon Code: CBDCLINICALS20
    Source
    Source of Hemp
    Colorado, USA
    FormOil Tincture
    IngredientsFull Spectrum Hemp Extract, Organic Virgin Hemp Seed Oil
    Type
    Type of CBD
    Full Spectrum CBD
    Extraction
    Extraction Method
    CO2 Method
    How to take itUnder the tongue for approximately 30 seconds before swallowing
    Potency
    Potency - CBD Per Bottle
    900mg per bottle
    Carrier OilOrganic Hemp Oil
    Concentration
    CBD Concentration Per Serving
    60mg per dropper full (1ml)
    Drug TestContains 0.3% THC but there is a chance you may test positive for marijuana
    FlavoursNatural
    Price Range$99 - $434
    $/mg CBD
    Price ($/mg)
    $0.08 - $0.13
    Shipping
    Shipping/Time to delivery
    2-3 Days via USPS
    Lab Tests
    Lab Testing Transparency
    Third Party Lab Tested post formulation for safety and potency, available on website
    ContaminantsNo additives or preservatives, Non-GMO, NO herbicides, pesticides, or chemical fertilizers
    AllergensNot specified
    Refund policyWithin 30 days
    Recommended forHealth-conscious persons
    Countries servedUSA (all 50 states) and over 40 countries including Australia, Azerbaijan, Beliza, Bosnia & Herzegovina, Brazil, Chile, China, Croatia, Czech Republic, Estonia, France, Hong Kong, Hungary, Ireland, Israel, Japan, Latvia, Lebanon, Lithuania, Macao, Malaysia, Malta, Netherlands, New Zealand, Oman, Paraguay, Poland, Portugal, Saudi Arabia, Serbia, Singapore, South Korea, Sweden, Switzerland, United Arab Emirates, United Kingdom, Uruguay, and many more.
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Best Customer Service

Sabaidee Super Good Vibes CBD Oil

4x the strength of a regular cbd oil
Sabaidee Super Good Vibes CBD Oil
  • Overall Clinical Score
    99%
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  • Score breakdown
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  • Summary

    Super Good Vibes CBD Oil provides the purest and highest quality Cannabidiol (CBD) on the market as well as other high quality phytocannabinoids, terpenes, vitamins, omega fatty acids, trace minerals, and other beneficial for your health elements, which all work together to provide benefits.

    Pro's
    Cons's
    •  Extra strong
    •  Significant benefits with just a few drops
    •  100% Natural ingredients
    •  No other flavors
  • Features
    Discount pricing available?15% Off Coupon Code: CBDCLINICALS15
    Source
    Source of Hemp
    Colorado, USA
    FormOil Tincture
    IngredientsCannabidiol (CBD), Coconut Medium-chain triglycerides (MCT) Oil, Peppermint oil
    Type
    Type of CBD
    Broad Spectrum
    Extraction
    Extraction Method
    CO2-extraction
    How to take itUsing 1-3 servings per day as needed is a good start to determine how much you need
    Potency
    Potency - CBD Per Bottle
    1000 mg per bottle
    Carrier OilCoconut MCT Oil
    Concentration
    CBD Concentration Per Serving
    33.5 mg per dropper (1ml)
    Drug TestContains 0.3% THC but there is a chance you may test positive for marijuana
    FlavoursPeppermint
    Price RangeSingle Bottle - $119.95, 2-Pack - $109.97 each, 3-Pack - $98.31 each, 6-Pack - $79.99 each
    $/mg CBD
    Price ($/mg)
    Single bottle - $0.010, 2-Pack - $0.011, 3-Pack - $0.009, 6-Pack - $0.007
    Shipping
    Shipping/Time to delivery
    3-5 Business days
    Lab Tests
    Lab Testing Transparency
    Third Party Lab Tested post formulation for safety and potency, available on website
    ContaminantsContaminant-free
    AllergensVegan and Gluten-free
    Refund policyWithin 30 days
    Recommended forPatients who are looking for serious CBD oil support
    Countries servedUSA only (all 50 states)
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Natural Alternative

cbdMD CBD Oil Tinctures

Uses USA hemp that is grown on non-GMO farms, and is both vegan and gluten-free
cbdMD CBD Oil Tinctures Products
  • Overall Clinical Score
    99%
    Natural Alternative
  • Score breakdown
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  • Summary

    cbdMD’s CBD oil tinctures are made using only CBD sourced from medical hemp and MCT oil as a carrier oil. Tinctures are offered in orange, mint, natural, and berry flavors. Safe for daily use, the oil tinctures are packaged with a built-in rubber dropper to adjust CBD dosage easily. The packaging is made to be easy to transport and discreet to use.

    Pro's
    Cons's
    •  Plenty of concentrations to choose from for all people with various kinds of needs
    •  Has vegan, organic, and gluten-free ingredients
    •  Affordable pricing
    •  Affordable pricing
    •  cbdMD uses MCT as its carrier oil so individuals who are allergic with coconuts should consider other brand options
  • Features
    Discount pricing available?15% Off Coupon Code: cbdMD15
    Source
    Source of Hemp
    Kentucky, USA
    FormOil Tincture
    IngredientsCannabidiol (CBD), MCT Oil, and Flavoring
    Type
    Type of CBD
    Broad Spectrum
    Extraction
    Extraction Method
    CO2 extraction method
    How to take itUnder tongue
    Potency
    Potency - CBD Per Bottle
    300 mg - 7500 mg / 30 ml bottle, 1000 mg - 1500 mg / 60 ml bottle
    Carrier OilOrganic Coconut MCT Oil
    Concentration
    CBD Concentration Per Serving
    30 ml: 300 mg - 10 mg per dropper (1ml), 750 mg - 25 mg per dropper (1ml), 1500 mg - 50 mg per dropper (1ml), 3000 mg - 100 mg per dropper (1ml), 5000 mg - 166.6 mg per dropper (1ml), 7500 mg - 250 mg per dropper (1ml), 60 ml: 1000 mg - 16.6 mg per dropper (1ml), 1500 mg - 25 mg per dropper (1ml)
    Drug TestContaining less than 0.3% THC, there are still trace amounts
    FlavoursNatural, Berry, Orange and Mint
    Price Range30 ml Bottles: $29.99 for 300 mg, $69.99 for 750 mg, $99.99 for 1500 mg, $149.99 for 3000 mg, $239.99 for 5000 mg, $339.99 for 7500 mg 60 ml Bottles: $74.99 for 1000 mg, $99.99 for 1500 mg
    $/mg CBD
    Price ($/mg)
    30 ml - $0.05 - $0.10, 60 ml - $0.06 - $0.07
    Shipping
    Shipping/Time to delivery
    2-5 Business days (via Fedex)
    Lab Tests
    Lab Testing Transparency
    Third Party Lab Tested post formulation for safety and potency, available on website
    Contaminants100% organic, non-GMO, and vegan-certified
    AllergensVegan, Gluten free
    Refund policyWithin 30 days
    Recommended forCBD users with different needs
    Countries servedUSA only (all 50 states)
Check Latest Prices

Why Some People Are Turning to CBD for Arthritis

Arthritis is the inflammation or swelling of one or more joints. It describes more than a hundred medical conditions that affect the joints, tissues around the joint, and other connective tissues. 

The Centers for Disease Control and Prevention (CDC) lists the following types of arthritis: osteoarthritis (OA), rheumatoid arthritis (RA), fibromyalgia, gout, and childhood arthritis(6). 

Although specific symptoms vary depending on the type of arthritis,  they usually include joint pain and stiffness(7). 

CBD for Joint Pain and Inflammation 

Rheumatoid arthritis, a chronic inflammatory disorder, can affect not only the joints. In some people, the condition can also harm a variety of body systems, including the skin, eyes, lungs, heart, and blood vessels(8).

A study done on animal subjects found that cannabinoids, particularly CBD (cannabidiol) and THC (tetrahydrocannabinol), are useful in the management of challenging-to-treat pain(9).  

Another study in Neuroscience Letters in 2011 found that CBD helped reduce acute joint inflammation in animal models by affecting the way pain receptors respond to stimuli(10).

CBD’s potent anti-inflammatory properties were also demonstrated in a 2018 study published in the Journal of Pharmacology and Experimental Therapeutics(11). 

Published by Neuropsychiatric Disease and Treatment, a clinical study examined Sativex, a combined cannabinoid medicine constituted by THC and CBD in a 1:1 ratio(12). 

Sativex mouth spray has shown its efficacy not only for helping with pain management in patients with chronic conditions, including pain due to nerve damage, advanced cancer pain, and rheumatoid arthritis but also for spasticity due to multiple sclerosis (MS)(13). 

Comparable results were obtained from another review published in The Cochrane Database of Systematic Reviews in 2018(14). 

A 2016 study from the European Journal of Pain showed, using rats as animal models, CBD applied on the skin might help lower pain and inflammation due to arthritis(15).

Researchers applied CBD gel to the rats for four consecutive days, with the animals receiving different doses per day. 

The researchers noted a reduction in inflammation and overall pain in the animals’ affected joints without noticeable side effects.

The rats that received low doses of CBD did not show improvement in their pain scores. Results found that 6.2 mg/day was a high-enough dose to reduce the rats’ pain and swelling symptoms.

Also, rats who received 62.3 mg/day had similar outcomes to the rats that received 6.2 mg/day. Thus, receiving a substantially larger dosage did not result in them having reduced pain.

The researchers believe that the pain-relieving and anti-inflammatory characteristics of CBD gel could potentially help individuals with arthritis. However, more human studies are needed(16).

A 2017 study from the journal Pain looked at the ability of CBD to prevent joint neuropathy and joint pain associated with osteoarthritis(17). 

Neuropathy is the damage or dysfunction of nerves that results in numbness, tingling, muscle weakness, burning, and pain in the affected area(18). 

Osteoarthritis, a common form of arthritis, occurs when the protective cartilage that cushions the ends of the bones wears down over time. With osteoarthritis, the joints can get painful, swollen, and hard to move(19).

The researchers of the said 2017 study found scientific evidence to support both of the neuropathic and osteoarthritic functions of CBD. 

They concluded that these abilities of CBD were due to its nerve-protective properties and anti-inflammatory properties on the joints.

CBD for Anxiety and Sleep Problems 

Having an autoimmune disorder, such as arthritis, may take a toll on the brain, as well as the body. 

A study published in Arthritis Care & Research in July 2018 found that people who have rheumatoid arthritis (RA) are more likely to experience anxiety, depression, and bipolar disorder in their lifetimes than those who have not been diagnosed with the autoimmune disease(20). 

Fighting the pain and expense of a long-term health problem can be a significant burden to carry, leading to sleep problems, changes in behavior, anxiety, and depression. 

CBD, meanwhile, has been shown to possess anti-anxiety and anti-depression characteristics that may help ease the increased burden of psychiatric disorders or associated symptoms in rheumatoid arthritis.

A study published in the journal CNS and Neurological Disorders – Drug Targets noted that CBD, a Cannabis Sativa component with psychiatric benefits, had therapeutic uses as an anti-anxiety-like and an antidepressant-like compound(21).

CBD’s potential for anxiety relief may also be attributed to its ability to help with sleep problems and reduce stress.

Studies have shown that CBD might help alleviate anxiety. Researchers of a 2019 study published in the Brazilian Journal of Psychiatry found that CBD’s anti-anxiety effect could help reduce the response to stressful environmental factors(22).

Authors of a 2019 study published in The Permanente Journal measured anxiety and sleep scores of the participants and noted that CBD could hold benefits for anxiety-related disorders(23).

Given CBD’s anti-anxiety and sleep-inducing, it may also be useful for individuals dealing with the emotional burden that comes with arthritis. 

How CBD Oil Works to Help with Arthritis

To understand how CBD works to help with arthritis, one must understand how the endocannabinoid system (ECS) works. 

The therapeutic effects of cannabinoids, like CBD, are realized by their active interaction with the body’s ECS and its cannabinoid receptors. 

The ECS is mainly responsible for regulating various body functions, including pain sensation, immune response, anxiety, sleep, mood, appetite, metabolism, and memory.

Researchers of a 2014 study in The European Journal of Neuroscience reported that the prevalence of receptors in the body and the critical role of the ECS in the regulation of pain, inflammation, and joint function further support the therapeutic use of cannabinoids for osteoarthritis(24).

Receptors CB1 and CB2 are the two main types of receptors found in specific parts of the human body. These receptors each have specific roles in the ECS.

CB1 receptors influence motor regulation, memory processing,  appetite, pain sensation, mood, and sleep(25).

Various studies of the cannabinoid receptors have shown that endocannabinoids attenuate and suppress the perception of pain(26).

Meanwhile, CB2 receptors are usually found on cells in the immune system and its associated structures.

When CB2 receptors are triggered, they trigger a response that fights inflammation, reducing pain, and minimizing damage to tissues.

These anti-inflammatory responses have been found useful in treating inflammation-related conditions, like chronic inflammatory demyelinating polyneuropathy (CIDP), Crohn’s disease, arthritis, and inflammatory bowel syndrome(27).

A 2019 study published in the journal Current Opinion in Rheumatology found that cannabinoids showed anti-inflammatory effects by activating CB2 receptors, which decrease cytokine production and immune cell mobilization(28). 

Cytokines are small proteins released by various cells in the body, including those of the immune system where they coordinate the body’s response against infection and disease.

In addition to its effects on CB1 and CB2 receptors, there is evidence that CBD impacts the TRPV-1(29) and GPR55(30) receptors. Both of these receptors are found in the skin and play a role in pain signaling and inflammation.

Also, CBD interacts with several other receptors in the body, such as the 5-HT1A receptor, which is linked to serotonin.

It is through this interaction with the neurotransmitter serotonin that these cannabinoids promote healing and balance(31). 

Research published in the Neurochemical Research Journal demonstrated that CBD might inhibit the reuptake of serotonin in the brain, making serotonin more available for the body(32).

Serotonin, also called the “feel good” chemical, influences a variety of body and psychological functions and impacts the levels of anxiety, mood, and happiness. 

The researchers believe that with better regulation of serotonin, CBD may help reduce anxiety and stabilize mood.

In the Translational PsychiatryJournal, a 2012 study demonstrated CBD’s potential ability to trigger the ECS to produce more of its natural cannabinoids, like anandamide, which regulates emotions(33). Results showed that anandamide levels increased in volunteers who were given CBD.

Increased anandamide levels in the brain protect against the effects of stress and reduce behavioral signs of fear and anxiety, according to a 2019 animal study published in the Journal of Neuroscience(34).

The Pros and Cons of CBD Oil for Arthritis

Pros

  • Human and animal studies have demonstrated that CBD possesses characteristics that may be beneficial in treating arthritis or its symptoms, including anxiety, sleep problems, depression, lethargy, and changes in mood and behavior.
  • CBD has been well-received by many distinguished health agencies, including the World Health Organization (WHO), stating that CBD “is generally well-tolerated with a good safety profile.”(35) 
  • CBD does not give the users a euphoric high, unlike its psychoactive cannabinoid counterpart, THC (tetrahydrocannabinol).
  • CBD is non-addictive, says Nora Volkow, director of the National Institute on Drug Abuse (NIDA) in a 2015 article(36). This characteristic makes CBD safe for daily consumption.
  • CBD oil can be purchased without a prescription in locations where they are legally available.

Cons

  • Cannabis has been a Schedule 1 drug, which has limited the type and scope of research needed to figure out how best to use it therapeutically.

Under the U.S. Federal Controlled Substances Act, Schedule 1 drugs have no currently accepted medical use and a high potential for abuse(37).

  • Studies are not substantial enough to determine whether or not CBD is a useful and effective treatment for conditions other than the ones already approved by the U.S. Food and Drug Administration (FDA).

To date, Epidiolex, a drug prescribed for epilepsy, is the only CBD product on the market that the FDA has approved(38).

  • There are risks involved in using CBD. According to the Mayo Clinic, possible side effects may include drowsiness, dry mouth, diarrhea, fatigue, and reduced appetite(39).
  • CBD has been shown to interact with other drugs. These drug interactions alter how the body breaks down certain medications, a 2017 research revealed(40). 
  • The lack of regulation on cannabis products in a dynamic CBD industry makes it difficult to determine if the CBD gummies, tinctures, patches, balms, and gelcaps contain what the product label claims.

A 2107 review published in the Journal of the American Medical Association revealed labeling inaccuracies among CBD products. Some products had less CBD than stated, while others had more(41).

How CBD Oil Compares to Alternative Treatments for Arthritis

Several herbal remedies are promoted today for treating arthritis, including Boswellia serrata, turmeric, ginger, devil’s claw, willow bark extract, and feverfew, says the Arthritis Foundation(42).

Some herbal remedies are available in the form of a cream, gel, patch, or compress that one can rub on or apply to the skin. 

  • Arnica and comfrey are useful for relieving arthritis pain. Creams made with the chili pepper extract, capsaicin, can also help with pain. However, they can cause side effects, like a burning sensation and skin irritation(43).
  • Capsaicin is a substance found in hot peppers. A study in Clinical Therapeutics found that, after four weeks of capsaicin treatment, rheumatoid arthritis and osteoarthritis patients showed mean reductions in pain of 57% and 33%, respectively(44).
  • Studies have shown that curcumin, the active component in turmeric, and ginger might be useful in reducing chronic pain associated with arthritis(45). 
  • Clinical trials with Boswellia gum-resin have shown that the herb could help improve symptoms in osteoarthritis and rheumatoid arthritis patients(46).

Meanwhile, CBD has been shown to possess characteristics that could be used for natural pain relief and combat inflammation.

Some CBD products come in the form of lotions, creams, and transdermal patches infused with capsaicin, turmeric, ginger, arnica, and Boswellia extracts. 

The natural extracts in CBD topicals combine with the natural pain-relieving benefits of CBD oil for targeted relief.

Massages can also help with arthritis. Regular massaging of arthritic joints is known to help reduce pain and stiffness and improve an individual’s range of motion. 

CBD oil tinctures may be used or combined with massage oils. Most CBD oils are infused with natural herb extracts that can add to CBD’s therapeutic benefits for arthritis symptoms.

Meanwhile, simple hot and cold treatments can make a significant difference when it comes to arthritis pain. CBD bath bombs may be used in bath and soaking therapies for added relief. 

Bath bombs infused with CBD and other therapeutic herbs can help provide relaxation and relief from physical tension and emotional stress. Long, warm showers or baths, particularly in the morning, can help ease stiffness in the joints. 

Meanwhile, an individual’s body weight can make a significant impact on the amount of pain experienced from arthritis. Extra weight puts added pressure on the joints, particularly the knees, hips, and feet. 

Reducing the stress on the joints by losing weight can improve one’s mobility, decrease pain, and prevent future damage to the joints. 

Studies have shown that CBD can help with weight management. In a study in the Brazilian Journal of Medical and Biological Research, researchers found that CBD might interfere with the secretion of cortisol, reducing blood levels significantly(47).

Researchers believe that chronic stress and persistently high cortisol levels may be associated with increased appetite and weight gain(48).

In a 2008 animal study published in the PLOS One Journal, it was noted that CBD inhibits a receptor in the brain so that ghrelin, which stimulates the appetite, is unable to act(49).

A study published in Nature Journal has reported that CBD could increase the levels of leptin in the brain(50). 

Leptin is the hormone that makes an individual feel full or satiated. The reduced cravings for unhealthy, calorie-dense foods may help individuals achieve their weight loss goals fast.

A healthy diet rich in omega-3 fatty acids may also help individuals deal with arthritis pain. 

Theramine, an amino acid blend, could be useful in reducing pain and inflammation linked to chronic back pain, according to a 2016 study in the American Journal of Therapeutics(51). 

Hemp oil produced from cannabis seed is an excellent source of essential amino acids and fatty acids(52).

How to Choose the Best CBD Oil for Arthritis

There are three types of CBD oil: full-spectrum, broad-spectrum, and CBD isolate.

The full-spectrum variety contains a complete range of cannabinoids, terpenes, flavonoids, and other compounds naturally present in cannabis, including other compounds and minerals, such as a variety of fatty acids and beneficial fiber. 

Terpenes are the compounds in cannabis plants that give it distinctive aromas and flavors, while flavonoids are responsible for the vivid colors in most plants.

The combination of all these components creates a synergy known as “entourage effect,” where all of the constituents working together are more efficient than their isolated elements(53).

CBD is not the only cannabinoid found in cannabis that has therapeutic benefits. Hence, when choosing a CBD product, one may opt for one that contains full-spectrum CBD oil.

Still, it is up to the discretion of the physician whether to suggest trying full-spectrum formulations. No research is available on their efficacy and safety outside of specific components in separate contexts(54).

Meanwhile, those with allergies to THC may choose broad-spectrum CBD oil, which is like full-spectrum CBD but THC-free or contains trace amounts (less than 0.3%) of THC. 

CBD isolates, on the other hand, carry only pure CBD. For people who are allergic to specific components of the hemp plant and do not want any THC in their system, CBD isolates are an option.

Regardless of the form of CBD oil products, careful consideration must be employed in selecting the best CBD oil that is suitable for one’s lifestyle and preferences.

The following factors are essential to ensure the safety and reliability of the CBD products purchased:

  • Research on the exact legal stipulations applicable to CBD in the area where it would be bought and used.
  • Purchase only non-GMO, organic hemp-derived CBD oil products from legitimate and reliable CBD brands known for their high-quality CBD oil products. The majority of CBD companies that manufacture the best CBD oil products grow their hemp from their own farm, or they purchase from licensed hemp producers.
  • Research product reviews before buying from an online store. When purchasing from a physical store or dispensary, check whether the store is authorized by the government to sell CBD.
  • Knowing the extraction methods used in making the CBD oil is also essential.

Researchers of a study indicate that the Supercritical-CO2 extraction process is recognized as safe by the U.S. Food and Drug Administration (FDA) in pharmaceutical manufacturing(55).

The supercritical CO2 extraction method allows for the highest purity and potency because the process does not extract any unwanted ingredients and impurities.

NuLeaf Naturals is only one of several companies that use the supercritical CO2 extraction method to extract CBD oil for their tinctures. The most natural carrier oils that may be used include MCT oil (medium-chain triglycerides from coconut oil), hemp seed oil, and extra-virgin olive oil.

Nuleaf extracts its CBD from hemp plants of the highest quality, grown on licensed farms in Colorado, USA. NuLeaf uses organic hemp oil as its carrier oil, for the most natural connection to the body’s endocannabinoid system and the most compatible oil for CBD.

  • One important thing to look for in CBD products is certification codes.

Several certification authorities approve certain products only after some thorough screening tests. A certificate of analysis (COA) is a laboratory report regarding the contents of a product.

In the case of CBD, a COA includes cannabinoid content and other tested compounds, such as pesticides, mold, and heavy metals. COAs ensure the customer knows what is in the product they are purchasing.

This piece of information does not only promote transparency, but it also ensures that the product contains what it claims. A reputable CBD company always ensures its products have passed lab testing and offers the most recent COAs of the products they provide.

After all, a COA is as much for the customer as it is for the manufacturer to make sure that consumers get only high-quality products. COAs ensure that consumers get only products of the highest quality with every purchase.

Apart from the COA, another certificate that is worth checking is the U.S. Hemp Authority Certification, which is the CBD industry’s initiative to provide high standards, best practices, and self-regulation. 

  • Compare company claims about their products’ potency with that of the third-party lab testing reports. Look for a certificate of analysis for every product purchased.
  • Consulting with a trusted medical professional experienced in the use of CBD is ideal before using any CBD product.

Additional Tips on Shopping for the Best CBD Oil Products

  • Consider CBD-rich, high-quality products derived from high-resin cannabis grown sustainably following with certified regenerative organic standards.
  • Be wary of CBD brands that claim their CBD is derived from the seed and stalk of hemp plants. CBD is not present in hemp seed, and there is barely any CBD in the stalk of the hemp plant.
  • Avoid CBD hemp oil vape cartridges containing flavor additives, toxic thinning agents (such as propylene glycol and polyethylene glycol), and other harmful ingredients.
  • Avoid poor quality CBD-infused gummies made with artificial colors and corn syrup. 
  • Reach out to CBD companies directly to ask questions. Try another brand if they do not communicate.

CBD Dosage for Arthritis

While there are no established clinical guidelines on dosing with CBD for arthritis treatment, the medical experts consulted by the Arthritis Foundation recommend the following for adults(56):

  • CBD extract is mixed with carrier oil. When taking CBD oil or tincture, it is essential to determine not only the amount of oil or tincture to take (the dose) but also the amount of CBD in each dose.
  • Go low and slow. Start with a few milligrams of CBD sublingually (under the tongue) twice a day. If relief is inadequate after one week, increase the dose by that same amount. 

If needed, gradually increase the dose over several weeks. Once relief has been achieved, continue taking that dose twice daily to maintain a stable level of CBD in the blood.

  • When using full-spectrum CBD oil, note that THC, even at low levels, may get the user high, creating cognitive, motor, and balance issues. 
  • If no relief from arthritis is achieved even after several weeks of using CBD alone or with a combination of CBD and very low THC, or if unwanted side effects are experienced when using a CBD product, immediately discontinue use and inform a doctor(57).

How to Take CBD Oil for Arthritis 

CBD-based products can be taken orally, applied to the skin, or inhaled. Each method of administration or consumption has its advantages and disadvantages for individuals with arthritis. 

Taking CBD by Mouth

CBD taken orally is swallowed or ingested in the form of capsules, food, or liquid, which are convenient and straightforward ways to take CBD oil (cannabidiol oil), especially for beginners.

CBD oil in these forms gets absorbed through the digestive tract. However, absorption is slow, and dosing is tricky due to the delayed onset (one to two hours) of effect, unknown stomach acids, and recent meals, among other factors.

Capsules can work for daily use after a safe, effective capsule dose has been established. Experts discourage taking CBD via edibles, like gummies and cookies, because dosing is unreliable.

CBD can also be absorbed directly into the bloodstream by holding liquid from a spray or tincture (a liquid dosed by a dropper) sublingually for 60 to 120 seconds. 

The taste may not be pleasant, but effects may be felt within 15 to 45 minutes and last for 4 to 6 hours(58).

CBD oil tinctures or drops may be practical for those who seek fast results and maximum dosage control. 

A syringe, marked dropper, or easily-calculated number of drops is used for consistent and accurate dosing. 

Topical CBD Application

A topical CBD cream, CBD transdermal patch, or CBD massage oil is ideal when dealing with pain or inflammation in a specific area of the body. 

When applied in this way, the CBD can target localized clusters of cannabinoid receptors, rather than interacting with the ECS as a whole.

The CBD in topicals goes to work instantly after rubbing the product onto the affected area, and relief can be felt in about 15 minutes. 

One option is to take CBD oil topically alone or combined with lotion or cream(59)

For topical products, look for keywords on the product labels that indicate that the product uses nanotechnology, encapsulation, or micellization of CBD. 

These words indicate that their solution can carry CBD through the dermal layers, rather than just staying on the skin.

Many CBD creams, salves, patches, and massage oils are also infused with other elements, such as essential oils, that may supplement CBD’s health benefits for pain relief.

Topical products may also include common over-the-counter ingredients such as menthol, capsaicin, or camphor, making it difficult to determine if a positive effect is due to the CBD or another ingredient.

Inhaling CBD

CBD can be inhaled via a vape pen. CBD oil vapes are one of the quickest ways to get CBD into the body since it enters the bloodstream through the lungs, without going through the digestive system. 

When vaping CBD, effects can be felt in minutes. However, the effects last for only 30 minutes to an hour or two. Also, with CBD vapes, it is difficult to determine precisely the amount of CBD is in each draw. 

As a 2018 study published in Molecules indicated, the primary limitations of inhaling are the variability in individuals’ inhalation techniques and respiratory tract irritation during inhalation(60).

Although labels for CBD oil vape products usually indicate the amount per inhale, this amount may vary in individuals. Thus, getting the dose right requires a bit of experimentation at first. 

Vaping is not for everyone. Experts are not sure whether or not vaping causes lung problems. However, they believe that the most likely culprit is a contaminant, not an infectious agent. 

Possibilities may also include chemical irritation or allergic or immune reactions to various chemicals or other substances in the inhaled vapors(61).

Also, inhalation of vapor oils and chemical byproducts carry unknown risks, particularly for people with inflammatory arthritis. 

The Centers for Disease Control and Prevention (CDC) is investigating vaping in association with widespread hospitalizations and deaths from severe pulmonary disease(62).

Individuals contemplating vaping CBD for the first time must proceed with caution and first consult with a doctor experienced in cannabis use.

Types and Symptoms of Arthritis

The Centers for Disease Control and Prevention (CDC) lists the following types of arthritis: osteoarthritis (OA), rheumatoid arthritis (RA), fibromyalgia, gout, and childhood arthritis(63). 

Osteoarthritis (OA) is the most common form of arthritis. Some experts call it a degenerative joint disease or “wear and tear” arthritis. It happens most frequently in the hands, hips, and knees.

The cartilage within a joint begins to break down, and then the underlying bone begins to change. These changes develop slowly, becoming worse over time. OA can cause pain, stiffness, and swelling. 

Rheumatoid arthritis (RA) usually attacks many joints at once. RA typically affects joints in the knees, hands, and wrists. 

With RA, the lining of the joint becomes inflamed, damaging the joint tissue. This damage can cause long-lasting or chronic pain, unsteadiness (lack of balance), and deformity (misshapenness).

An autoimmune disorder, RA occurs when the immune system mistakenly attacks the body’s tissues.

Autoimmune diseases are associated with an increased risk of high blood pressure and cardiovascular disease(64).

Fibromyalgia causes pain all over the body (also called widespread pain), sleep problems, fatigue, and mental and emotional distress. 

Individuals with fibromyalgia are more sensitive to pain than people without fibromyalgia. This heightened sensitivity is called abnormal pain perception processing.

Gout usually affects only one joint at a time, oftentimes the big toe joint. There are times when symptoms get worse, known as flares, and times when there are no symptoms, referred to as remission. 

Repeated periods of gout can lead to gouty arthritis, a worsening form of arthritis.

A common type of childhood arthritis is juvenile idiopathic arthritis (JIA), also called juvenile rheumatoid arthritis.

Childhood arthritis can lead to permanent physical damage to the joints. This damage can make it hard for the child to do everyday things like walking or dressing and can result in disability(65). 

The 2018 Farm Bill legalized industrial hemp and hemp-derived products at the federal level in the United States, removing them from the jurisdiction of the Drug Enforcement Administration (DEA). 

The law defined “agricultural hemp” as cannabis strains that contain less than 0.3% THC. Additionally, the Farm Bill explicitly legalized the “extracts, cannabinoids, and derivatives” of hemp. 

Many states and Washington, D.C. have passed cannabis-related laws, making medical marijuana with high levels of THC legal. 

Still, marijuana may require a prescription from a licensed physician(66).

To get more information on state laws and penalties, click here(67).

For a complete list of legal medical marijuana states and D.C., including the corresponding laws, fees, and possession limits, click here(68).

CBD Is Not the Same As Marijuana

CBD is the second most prevalent of the active ingredients of medical cannabis or medical marijuana. However, CBD, by itself, does not cause a “high.” 

While CBD is an essential component of marijuana, most CBD oil products on the market use cannabidiol oil derived directly from the hemp plant, which is a cousin of the marijuana plant. 

Conclusion

Human and animal studies have shown that CBD might be useful in alleviating arthritis symptoms, such as pain, inflammation, anxiety, and sleep problems. 

CBD has also been shown to help with weight management. Excess body weight puts added pressure on the joints, particularly the knees, hips, and feet. 

However, studies on CBD use for arthritis in humans are limited, and the long-term effects of CBD use remain unknown. 

More longitudinal research is needed to gather more scientific evidence and validate results from previous studies.

It is essential to consult with a medical professional experienced in cannabis use before starting a CBD regimen or combining CBD with current prescription medications.


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  35. WHO. Expert Committee on Drug Dependence. (2017, Nov 6-10). Cannabidiol (CBD). Retrieved from https://www.who.int/medicines/access/controlled-substances/5.2_CBD.pdf.
  36. Nora Volkow. NIDA. Researching Marijuana for Therapeutic Purposes: The Potential Promise of Cannabidiol (CBD). National Institute on Drug Abuse website. https://www.drugabuse.gov/about-nida/noras-blog/2015/07/researching-marijuana-therapeutic-purposes-potential-promise-cannabidiol-cbd. July 20, 2015. Accessed January 31, 2020.
  37. Malcom K. (2019, Oct 30). Should You Take CBD for Pain? Retrieved from https://healthblog.uofmhealth.org/health-management/should-you-take-cbd-for-pain.
  38. U.S. Food and Drug Administration. (2020, Jan 15). FDA Regulation of Cannabis and Cannabis-Derived Products, Including Cannabidiol (CBD). Retrieved from https://www.fda.gov/news-events/public-health-focus/fda-regulation-cannabis-and-cannabis-derived-products-including-cannabidiol-cbd.
  39. Bauer, B. (2018, Dec 20). What are the benefits of CBD — and is it safe to use? Retrieved from https://www.mayoclinic.org/healthy-lifestyle/consumer-health/expert-answers/is-cbd-safe-and-effective/faq-20446700.
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  43. ibid.
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  54. VanDolah HJ, Bauer BA, Mauck KF. Clinicians’ Guide to Cannabidiol and Hemp Oils. Mayo Clin Proc. 2019;94(9):1840–1851. DOI:10.1016/j.mayocp.2019.01.003.
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  58. ibid.
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  61. Shmerling, R. (2019, Dec 10). Can vaping damage your lungs? What we do (and don’t) know. https://www.health.harvard.edu/blog/can-vaping-damage-your-lungs-what-we-do-and-dont-know-2019090417734.
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More Info

Less Info

 Summary for UKPID

    GOLD SALTS

    (AURANOFIN; AUROTHIOMALATE)

    Kathryn Pughe, BSc (Hons) MRPharmS

    National Poisons Information Service (Newcastle Centre)

    Regional Drug & Therapeutics Centre

    Wolfson Building

    Claremont Place

    Newcastle upon Tyne

    NE1 4LP

    UK

    This monograph has been produced by staff of a National Poisons

    Information Service Centre in the United Kingdom.  The work was

    commissioned and funded by the UK Departments of Health, and was

    designed as a source of detailed information for use by poisons

    information centres.

    Peer review group: Directors of the UK National Poisons Information

    Service.

 

    Summary

    Name

         Generic             Auranofin

         Proprietary         Ridaura

         Generic             Sodium aurothiomalate

         Proprietary         Myocrisin

         Synonyms            Gold sodium thiomalate,

                             Sodium aurothiosuccinate

    Chemical Group/Family

         Drugs suppressing rheumatic disease

         BNF 10.1.3

    Reference Number

         Na aurothiomalate

         CAS 12244-57-4 (xNa, anhydrous)

         CAS 39377-38-3 (2Na monohydrate)

         Auranofin

         CAS 34031-32-8

         Product licence numbers:

         Myocrisin:     10 mg inj 0012/5114

                        20 mg inj 0012/5113

                        50 mg inj 0012/5006

         Ridaura:       0002/0082

    Presentation

         Myocrisin      Pale yellow solution

                        0.5ml amps in boxes of 10 x 10 mg

                        0.5ml amps in boxes of 10 x 20 mg

                        0.5ml amps in boxes of 10 x 50 mg

         Ridaura        Pale yellow, film coated square tablets

                        3 mg tabs in containers of 60

    Physico-Chemical Properties

    Chemical structure

         Myocrisin      C4H3AuNa2O4S

                        Disodium salt of (aurothio)succinic acid

 

         Auranofin      C20H34AuO9PS

                        2,3,4,6-Tetra-O-acetyl-1-thio-ß-D-glucopyranosato-

                        S-tri-ethylphosphine gold

    Physical state at room temperature

         Aurothiomalate      Fine, pale yellow powder with a slight odour

         Auranofin           Fine white powder

    Molecular weight

         Aurothiomalate

         (Hexomer)           2500 in 0.5M NaCl

         (Monomer)           390.1

         Auranofin           678.5

    pKa

         thiomalate          3.2

         carboxyl            4.2

         Auranofin           –

    Solubility

         Aurothiomalate      in alcohol     insoluble

                             in water       very soluble

         Auranofin           in alcohol     1 in 27

                             in water       1 in 5900

    USES

    Indications

         Sodium aurothiomalate – active progressive rheumatoid arthritis,

         and progressive juvenile chronic arthritis.

         Auranofin – active progressive rheumatoid arthritis when NSAIDs

         inadequate alone.

    Therapeutic Dosage

          Sodium aurothiomalate

         By deep im injection only.

         Adults: Initial test dose of 10 mg in first week followed by

         weekly doses of 50 mg until signs of remission occur. With full

         remission, the interval between injections should be

         progressively increased to 3, 4 and then, after 18-24 months, to

         6 weeks. If after reaching a total dose of 1g, excluding the test

         dose, no major improvement has occurred and the patient has not

         shown any signs of gold toxicity, six 100 mg injections may be

         administered at weekly intervals. If no signs of remission occur

         after this time, consider alternative treatments.

         Children: Weekly doses of 1mg/kg up to maximum weekly dose of 50

  1. This dose may be preceded by a smaller test dose of 1/10th or

         1/5th of the full dose for 2-3 weeks. Continue weekly doses until

         signs of remission appear then increase intervals to 2 weeks.

         With full remission increase interval to 3 then 4 weeks. I f no

         signs of remission after 20 weeks, consider alternative

         treatments. Treatment should be continued for 6 months. Expect

         response at 300-500 mg level. If patients respond, maintenance

         therapy should be continued with the dosage administered over the

         previous 2-4 weeks for 1-5 years.

          Auranofin

         Adults: Starting dose 3 mg twice daily, then 6 mg as single daily

         dose if well tolerated. Continue for minimum of 3-6 months to

         assess response. Increase to 3 mg three times a day if response

         inadequate after 6 months, if still inadequate after a further 3

         months, then discontinue

         Child: Not recommended

    Contraindications

          Sodium aurothiomalate

         Severe renal and hepatic disease; history of blood disorders or

         bone marrow aplasia; exfoliative dermatitis; systemic lupus

         erythematosus; necrotising enterocolitis; pulmonary fibrosis;

         pregnancy and breastfeeding; porphyria.

          Auranofin

         Not for use in patients with a history of gold-induced disorders

         as for sodium aurothiomalate.

    Abuses

         NIF

    HAZARD / RISK CLASSIFICATION

         NIF

    PHARMACOKINETICS

    Absorption

         Aurothiomalate      Intramuscular absorption 100%, not orally

                             absorbed

         Auranofin           Oral absorption 13-33%

    Distribution

         Aurothiomalate      Volume of distribution – 0.1Lkg-1

         Auranofin           Volume of distribution – NIF

    Metabolism

         Aurothiomalate      No presystemic metabolism, 95% plasma protein

                             bound

         Auranofin           No presystemic metabolism, 60% plasma protein

                             bound

    Elimination

         Aurothiomalate      70% excreted in urine, 30% in faeces

         Auranofin           85% excreted in faeces, 15% in urine

    Half-life

         Aurothiomalate      Initial 5.5 days; terminal 250 days

         Auranofin           17-25 days (plasma); total body 70 days

    Special Populations

    Pregnancy

    The safety of gold salts in pregnancy has not been established. Gold

    salts should not be used in women of child-bearing potential, unless

    the benefits outweigh the possible risks, as clinical experience is

    limited.

    Gold is teratogenic in rats and rabbits at high doses which produce

    maternal toxicity, increased frequencies of skeletal, CNS and other

    malformations were seen.

    There are no controlled studies of gold administration     during

    human pregnancy. Placental passage of gold salts has been documented

    in clinical reports.

    The frequency of malformations was not increased in a study of 119

    children born to women who had been treated with gold compounds during

    the first trimester of pregnancy. 26 patients in this series received

    gold treatment throughout pregnancy, 2 minor anomalies were seen but a

    causal association with gold has not been established.

    Hepatic disease

    Use with caution in patients with any degree of hepatic dysfunction.

    Intrahepatic cholestasis with eosinophilia may be seen after gold

    injections. The condition is self-limiting, and liver function tests

    return to normal within about 3 months.

    Renal disease

    Use with caution in patients with any degree of renal impairment.

    Elderly

    Monitor with extra caution due to decreased renal function

    Lactation

    Avoid if breastfeeding as significant amounts of gold excreted.

    TOXICOKINETICS

    EPIDEMIOLOGY OF POISONING

    Acute overdose is usually the result of administration errors with IM

    injections, and until 1984 therapeutic gold drugs were only available

    parenterally. Most toxic data are based on therapeutic toxicity.

    ADVERSE EFFECTS

    There is a high incidence of adverse reactions when gold salts are

    used for rheumatoid arthritis, incidence is between 5-50% (Eyring &

    Engleman, 1963; Davis & Hughes, 1974). The rate of serious reactions

    is approximately 3-5%. Anaphylactoid effects may occur after any

    course of therapy, usually within the first 10 minutes of

    administration.

    Problems with therapeutic use include mouth ulcers, skin reactions,,

    proteinuria, blood disorders (sometimes sudden onset and fatal).

    Rarely colitis, peripheral neuritis, pulmonary fibrosis,

    hepatotoxicity with cholestatic jaundice and alopecia can also occur.

    Diarrhoea and other gastrointestinal symptoms are associated with

    auranofin use.

    Proteinuria occurs in 2-20% of patients treated with injected gold and

    may be sufficiently severe to cause nephrotic syndrome in 10-30% of

    those affected. Proteinuria usually resolves on stopping treatment.

    Gold lung is a rare toxic side effect of gold therapy that may begin

    after administration of 300-1000 mg total gold dose. Dyspnoea appears

    suddenly over a period of 2-10 days. Chest x-rays show diffuse

    bilateral pulmonary shading (Gortenuti et al 1985), and a moderate

    eosinophilia may be present. The prognosis is good after withdrawal of

    treatment (McFadden et al 1989), although impairment of lung function

    may be permanent (Cohen 1988).

    Patients treated with gold salts should be asked to report immediately

    the appearance of pruritis, metallic taste, sore throat or tongue,

    buccal ulceration or easy bruising, purpura, epistaxis, bleeding gums,

    menorrhagia or diarrhoea.

    INTERACTIONS

    Increased risk of toxicity with other nephrotoxic and myelosuppressive

    drugs.

    MECHANISM OF ACTION / TOXICITY

    Acute:

    No deaths have been recorded. Adults have been given up to 500 mg (10

    times the therapeutic dose ) in a single dose with variable

    consequences. One patient took 27 mg auranofin daily for 10 days and

    developed an encephalopathy and peripheral neuropathy. The patient

    made a gradual recovery after auranofin was discontinued

    (manufacturer).

    Chronic:

    Effects would be expected to be extensions of toxic therapeutic

    effects.

    Features:

    Most of the reported cases of overdose have not developed  features.

    Early features of acute overdose have included a generalized skin

    rash, which settled within a few hours, and oedema of the eyelids in

    one case, and ventricular tachycardia in another. Acute renal failure

    is a potential problem but has not been reported. Abnormal LFTs with

    elevation of ALT and alkaline phosphatase were reported 3 weeks post-

    overdose in one case.

    MANAGEMENT

    Observation and supportive measures are probably all that are

    required. There is some doubt as to whether toxic reactions seen are

    due to direct effects of gold, or an indirect effect through the

    immune system.

    Decontamination

    Overdose with oral gold salts is not commonly seen and it is not known

    if activated charcoal is effective in minimizing drug absorption in

    such cases. Metallic gold is poorly adsorbed by activated charcoal.

    Supportive care

    D-Penicillamine has been used to treat skin reactions (Davis 1969)

    and thrombocytopenia (Bluhm et al 1962) in   cases where BAL and

    corticosteroids showed initial but not sustained results. It should be

    avoided in penicillin-allergic patients. Monitoring for proteinuria

    should be performed.

    Adults: 15-40mg/kg/day orally; max 250-500 mg four times a day before

    meals.

    Children: 20-30mg/kg/day orally once or twice daily before meals.

    Immunosuppressives such as cyclophosphamide have also been used to

    control toxic reactions. A dose of 100 mg daily for 6 months was used

    until platelets stabilised at 100,000 per cubic mm, and then the dose

    was reduced to 75mg daily (Kozloff et al 1979).

    Monitoring

    Haematology, liver and renal functions should be monitored.

    Gold urine levels during treatment vary      considerably. There seems

    to be no correlation between blood gold levels and toxicity or

    therapeutic effect. In a summary of 20 cases of toxicity, the

    cumulative toxic dose was from 230 mg to 10g of gold salt.

    Antidotes

    Some patients have been given dimercaprol (BAL) to chelate the

    gold but there is no evidence that it is of value.

    The dose of BAL is individualized. A common dosage schedule is 3-5

    mg/kg/dose every 4 hours by deep IM injection for the first 2 days,

    then 2.5-3/mg/kg/dose IM every 6 hours for 2 days, then 2.5-3 mg/kg IM

    every 12 hours for 7 days.

    Elimination

    techniques

    N-acetylcysteine (NAC) has been used to remove / redistribute gold and

    reduce haematological reactions (Godfrey et al 1982). Lorber et al

    (1973) demonstrated in vitro and in vivo chelation of gold by NAC,

    with up to a 54% increase over normal excretion in subjects tested.

    Dose: 2-9g in 100ml dextrose 5% or 0.45% sodium chloride iv over 2-6

    hours. Total dose per therapy ranged from 13 to 153g.

    D-Penicillamine was shown to enhance the urinary excretion of gold

    when tested in 9 patients (Erying & Engleman 1963).

    Investigations

    Haematology, liver and renal functions should be monitored.

    Management controversies 

    Use of dimercaprol: Patients with high gold levels not given

    dimercaprol do not appear to have had an adverse outcome, but there is

    insufficient data to make categoric statements. Chelation reduces the

    amount of circulating gold, but it is nearly impossible to remove all

    the gold from the system.

    CASE DATA

  1. AURANOFIN
  2. Auranofin overdose (27 mg/day for 10 days) has resulted in

    peripheral neuropathy and encephalopathy, which resolved upon drug

    withdrawal (Ridaura Prod Info, 1985).

  1. AUROTHIOMALATE
  2. Pik et al (1985) reported two acute overdose cases in which

    patients received 1000 mg and 500 mg of intramuscular aurothioglucose,

    respectively. Both patients were asymptomatic and recovered

    uneventfully without treatment. One patient, however, developed

    microhaematuria and granular casts without proteinuria which resolved

    spontaneously within four weeks.

  1. A 53 year old male was accidentally injected with an im dose of 450

    mg sodium aurothiomalate. Palpebral oedema and a cutaneous generalized

    rash were observed within 30 minutes. The gold blood levels reached

    29.7mg/L without significant toxicity. The patient was treated with

    BAL and recovered (Barelli et al 1987).

  1. A 32 year old patient developed ventricular tachycardia 3 hours

    after im injection of 500 mg of aurothiomalate (Sharf et al 1976).

    Author

    Kathryn Pughe, BSc (Hons) MRPharmS

    National Poisons Information Service (Newcastle Centre)

    Regional Drug & Therapeutics Centre

    Wolfson Building

    Claremont Place

    Newcastle upon Tyne

    NE1 4LP

    UK

    This monograph was produced by the staff of the Newcastle Centre of

    the National Poisons Information Service in the United Kingdom. The

    work was commissioned and funded by the UK Departments of Health, and

    was designed as a source of detailed information for use by poisons

    information centres.

    Peer review was undertaken by the Directors of the UK National Poisons

    Information Service.

    Last updated March 1997

    REFERENCES:

    Books:

  1.   ABPI Compendium of Data Sheets and Summaries of Product Characteristics. Datapharm Publications Ltd. 1996-97.
  1.   AHFS Drug Information. McEvoy GK (Ed.) 1997.
  2.   British National Formulary. Number 32 (September 1996). British Medical Association and Royal Pharmaceutical Society.
  1.   Dollery C. Therapeutic Drugs. Churchill Livingstone. 1991.
  2.   Ellenhorn MJ. Ellenhorn’s Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd Edition. Williams & Wilkins. 1997.
  1.   Martindale : The Extra Pharmacopoeia. 31st Edition. Reynolds JEF (Ed.) Pharmaceutical Press. 1996.

    Papers:

  1.   Barrelli A, Calimici A, Pala F. Gold salts acute poisoning: a case report. Vet Hum Toxicol 1987; 29(suppl 2): 108-110.
  1.   Bluhm GB, Sigler JW, Ensign DC et al. D-penicillamine therapy of thrombocytopenia secondary to chrysotherapy: a case report. Arthritis Rheum 1962; 5: 638.
  1.   Cohen MAH. Adverse reactions to gold compounds. Adverse Drug React Acute Poison Rev 1988; 4: 163-178.
  1.   Davis CM. D-penicillamine for the treatment for the treatment of gold dermatitis. Am J Med 1969; 46: 472-477.
  1.   Davis P & Hughes GRV. Significance of eosinophilia during gold therapy. Arthritis Rheum 1974; 17: 964-967.
  1.   Erying EJ & Engleman EP. Interaction of gold and penicillamine. Arthritis Rheum 1963; 6: 216-223.
  1.   Godfrey NF, Peter A, Simon TM et al. IV N-acetylcysteine treatment of hematologic reactions to chrysotherpay. J Rheum 1982; 9: 519-526.
  1.   Gortenuti G, Parrinello A, Vicentini D. Diffuse pulmonary changes caused by gold salt therapy. Report of a case. Diagn Imag Clin Med 1985; 54: 298-303.
  1.   Kozloff M, Votaw M & Penner JA. Gold-induced thrombocytopenia responsive to cyclophosphamide. South Med J 1979; 72: 1490-1491.
  1. Lorber A, Baumgartner WA, Bovy RA et al. Clinical application for heavy metal complexing potential of N-acetylcysteine. J Clin Pharmacol 1973; 13: 332-336.
  1. McFadden RG, Traher LJ, Thompson JM. Gold-naproxen pneumonitis. A toxic drug reaction? Chest 1989; 96: 216-218.
  1. Pik A, Cohen N, Yona E et al. Should gold overdose be invariably treated? J Rheumatol 1985; 12: 1174-1175.
  1. Rubinstein I et al. Aurothioglucose overdosage in five patients with rheumatoid arthritis. Clin Rheumatol 1987; 6: 583-587.
  1. Sharf J, Nahir M, Nirenberg L. Ventricular tachycardia caused by

         gold overdose. Arthritis Rheum 1976; 19: 137-138.

    Computer databases:

  1.   Poisindex System(R), Micromedex inc., Denver Colorado, Edition

         Expires 31/3/97.

  1.   Reprotox System(R), Micromedex inc., Denver Colorado, Edition

         Expires 31/3/97.

  1.   TOXBASE, National Poisons Information Service, 1997.

AZATHIOPRINE

VOL.: 26 (1981) (p. 47)

  1. Summary of Data Reported and Evaluation

5.1 Experimental data

Azathioprine was tested by intraperitoneal, subcutaneous and/or intramuscular administration in mice and by oral and intraperitoneal administration in rats. Suggestive evidence was obtained for the induction of lymphomas after intraperitoneal, subcutaneous or intramuscular injection in mice and for ear-duct carcinomas in rats after oral administration. Because of limitations in design and reporting, however, the results were considered to be inconclusive.

Studies in which azathioprine was tested in combination with other agents were inadequate for evaluation.

Azathioprine is embryolethal at doses nontoxic to the mother and can induce a variety of severe teratogenic effects in several animal species. It is mutagenic in bacteria and yeast in vitro and in Drosophila melanogaster and mice in vivo. At high concentrations, the drug is clastogenic to human lymphocytes in vitro.

5.2 Human data

Azathioprine has been widely used since the 1970s to prevent rejection following organ transplantation. It is also used to treat a variety of autoimmune diseases.

Use of azathioprine during pregnancy may reduce birth weight significantly. The data were insufficient to evaluate the teratogenic potential of this drug to humans. Azathioprine produces chromosomal abnormalities and increases in sister chromatid exchanges in the peripheral lymphocytes of non-cancer patients. No data were available to evaluate the mutagenic potential of this drug to humans.

There is evidence that azathioprine, often combined with prednisone, is associated with an increased incidence of non-Hodgkin’s lymphoma, squamous-cell cancers of the skin, hepato-biliary carcinomas, mesenchymal tumours, and perhaps certain other rare neoplasms. The risk of non-Hodgkin’s lymphoma is higher in organ transplant recipients; the presence of the graft may make some contribution to this increased incidence.

5.3 Evaluation

There is limited evidence for the carcinogenicity of azathioprine in mice and rats. There is sufficient evidence that azathioprine is carcinogenic in humans.

For definition of the italicized terms, see Preamble Evaluation.

Subsequent evaluation: Suppl. 7 (1987)

Last updated: 8 April 1998

See Also:

        Azathioprine (IARC Summary & Evaluation, Supplement 7, 1987)

        Azathioprine (PIM 053)

AZATHIOPRINE

(Group 1)

For definition of Groups, see Preamble Evaluation.

Supplement 7: (1987) (p. 119)

CAS No.: 446-86-6

Chem. Abstr. Name: 1H-Purine, 6-[(1-methyl-4-nitro-1H-imidazol-5-yl)thio]-

  1. Evidence for carcinogenicity to humans (sufficient)

Two large prospective epidemiological studies have shown that renal transplant patients, who usually receive azathioprine as an immunosuppressant, become at high risk for non-Hodgkin’s lymphoma, squamous-cell cancers of the skin, hepatobiliary carcinomas and mesenchymal tumours. While this is true for each of the various etiological entities resulting in the need for a transplant, these patients also have in common heavy exposure to foreign antigens [ref: 1]. Other patients who have received azathioprine as an immunosuppressant, including those with rheumatoid arthritis, systemic lupus and other ‘collagen’ disorders, inflammatory bowel disease and certain skin and renal diseases, have also been studied: the same array of malignancies was found to be in excess, although to a lesser extent [ref: 1,2]. For these patients, however, the picture is still not completely clear, because patients with rheumatoid arthritis constituted the largest category in the latter study [ref: 2], and some [ref: 3], but not all studies [ref: 4], have found that this disease conveys a risk for non-Hodgkin’s lymphoma in the absence of treatment.

  1. Evidence for carcinogenicity to animals (limited)

Suggestive evidence was obtained that lymphomas were induced in mice after intraperitoneal, subcutaneous or intramuscular injection of azathioprine, and that thymic lymphomas and squamous-cell carcinomas of the ear duct were induced in rats after oral administration, but there were limitations in the design and reporting of these studies [ref: 1,5].

  1. Other relevant data

There are conflicting reports of effects on the incidence of chromosomal aberrations in lymphocytes and bone-marrow cells of patients treated with azathioprine. In one study, the incidence of sister chromatid exchanges in lymphocytes of treated patients was not increased [ref: 6].

In animals treated in vivo, azathioprine induced dominant lethal mutations in mice; chromosomal aberrations in rabbit lymphocytes and Chinese hamster bone-marrow cells, and micronuclei in mice, rats and hamsters; it did not induce sister chromatid exchanges in Chinese hamster bone-marrow cells. Azathioprine induced chromosomal aberrations but not sister chromatid exchanges in human lymphocytes in vitro. It induced chromosomal aberrations in Drosophila and was weakly mutagenic to fungi and was mutagenic to bacteria [ref: 6].

Overall evaluation

Azathioprine is carcinogenic to humans (Group 1).

For definition of the italicized terms, see Preamble Evaluation.

Also see previous evaluation: Vol. 26 (1981)

References

  1. IARC Monographs, 26, 47-78, 1981
  2. Kinlen, L.J. (1985) Incidence of cancer in rheumatoid arthritis and other disorders after immunosuppressive treatment. Am. J. Med., 78 (Suppl. 1A), 44-49
  3. Isomäki, H.A., Hakulinen, T. & Joutsenlahti, U. (1978) Excess risk of lymphomas, leukemia and myeloma in patients with rheumatoid arthritis. J. chron. Dis., 31, 691-696
  4. Fries, J.F., Bloch, D., Spitz, P. & Mitchell, D.M. (1985) Cancer in rheumatoid arthritis: a prospective long-term study of mortality. Am. J. Med., 78 (Suppl. 1A), 56-59
  5. Cohen, S.M., Erturk, E., Skibba, J.L. & Bryan, G.T. (1983) Azathioprine induction of lymphomas and squamous cell carcinomas in rats. Cancer Res., 43, 2768-2772
  6. IARC Monographs, Suppl. 6, 86-88, 1987

Synonyms

Amuran

Azamun

Azathioprin

Azatioprin

Azothiaprine

Azathioprene

BW 57322

Imuran

Imurel

Imurek

Methyl-nitroimidazolylmercaptopurine

6-[(1-Methyl-4-nitroimidazol-5-yl)thio]purine

6-(1-Methyl-4-nitro-imidazole-5-yl)thiopurine

6-(1-Methyl-4-nitro-5-imidazolyl)mercaptopurin

Muran

NSC 39084

Last updated: 6 February 1998

See Also:

        Azathioprine (IARC Summary & Evaluation, Volume 26, 1981)

        Azathioprine (PIM 053)

INTOX Home Page

    Summary for UKPID

    PENICILLAMINE

    Dr Alan Worsley Bsc(hons) PhD MRPharmS

    National Poisons Information Service (Newcastle Centre)

    Regional Drug & Therapeutics Centre

    Wolfson Building

    Claremont Place

    Newcastle upon Tyne

    NE1 4LP

    UK

    This monograph has been produced by staff of a National Poisons

    Information Service Centre in the United Kingdom.  The work was

    commissioned and funded by the UK Departments of Health, and was

    designed as a source of detailed information for use by poisons

    information centres.

    Peer review group: Directors of the UK National Poisons Information

    Service.

    PENICILLAMINE (Distamine)

    Summary

    Type of product

    For the treatment of severe rheumatoid arthritis and cystinuria

    Ingredients/tablet

    Penicillamine 50, 125 and 250mg

    Fatal Dose

    Not Known- A 52 year old male presented at hospital 8 hours after

    ingesting 3.1g. Symptoms included vomiting, dehydaration, abdominal

    pain and tachycardia.

    Features

    Nausea and vomiting, abdominal pain, hyperpyrexia, thrombocytopaenia,

    neutropaenia, proteinuria, haematuria and tachycardia

    Management

    Empty the stomach if >500mg ingested, maintain a good diuresis.

    Monitor renal function and treat failure conventionally. Supportive

    Antidotes

    There are no specific antidotes

    Elimination techniques

    No data available

    REFERENCES

    ABPI Data Sheet Compendium. Datapharm publications Limited 1996-1997

    British National Formulary. Number 32 (September 1996). British

    Medical Associiation and Royal Pharmaceutical Society.

    Dollery C, Therapeutic Drugs. (Pt 2), Churchill Livingstone. 1994

    PENICILLAMINE

    Brand Name

         Distamine

    Generic Name

         Penicillamine

    Chemical Group/family

         Anti-rheumatic

         BNF 10.13

    Reference number

         CAS-52-67-5 (penicillamine)

         CAS-2219-30-9 (hydrochloride)

    Manufacturer/supplier

         Eli Lilly & Co Ltd,

         Dextra Court,

         Chapel Hill,

         Basingstoke, Hants.

         RG21 5SY

         Tel: 01256 315000

    Presentation

         Penicillamine 50mg, 125 mg, 250 mg tablets.

    Physicochemical properties:(Dollery)3

         3,3-Dimethyl-D-cysteine

    Molecular weight

         149.2

    pKa (COOH, NH, SH)

         1.8, 7.9, 10.5

    Solubility

         in alcohol         1 in 530

         in water           1 in 9

         octanol/water partition coefficient   –

    USES

    Indications

    Penicillamine is indicated in Wilson’s disease, cystinuria, rheumatoid

    arthritis, juvenile chronic polyarthritis, palindromic rheumatism,

    sero-negative polyarthritis, progressive systemic sclerosis, chronic

    active hepatitis.

    Therapeutic Dosage (BNF)2

    Adults

    Severe active rheumatoid arthritis, 500-750 mg daily maintenance (max

    1.5g daily)

    Wilson’s disease, 1.5-2.0g daily in divided doses.

    Cystinuria, 1-3g daily in divided doses (adjusted to maintain urinary

    cysteine below 200mg/litre.

    Chronic active hepatitis.

    Child

    Severe active rheumatoid arthritis15-20mg/kg maintenance.

    Wilson’s disease, up to 20mg/kg daily in divided doses.

    Cystinuria, minimum dose to maintain urinary cysteine below

    200mg/litre.

    Contraindications

    hypersensitivity (except in life threatening situations) systemic

    lupus erythematosus.

    Pharmacokinetics  (Dollery)3

         Oral absorption 40%

         presystemic metabolism –

         plasma half life

         mean 1-6h

         volume of distribution 0.8litre/kg

         plasma protein binding up to 85%

    Toxicokinetics

         No specific data available

    Adverse effects (Data Sheet)1

    Nausea, anorexia, fever and rash may occur early in therapy.

    Thrombocytopenia occurs commonly and neutropenia less often.

    Proteinuria occurs in 30% of patients and is dose related. Haematuria

    is rare.

    Haemolytic anaemia, nephrotic syndrome.

    Pregnancy

    Penicillamine crosses the placenta to the fetus and has been

    administered during pregnancy for the treatment of rheumatoid

    arthritis, cystinuria and Wilson’s disease4. Conflicting reports

    suggest that penicillamine should either be stopped during

    pregnancy5, or be continued during pregnancy with the treatment of

    Wilson’s disease, but discontinued in the treatment of rheumatoid

    arthritis6.

    The use of penicillamine has been observed in approximately 100

    pregnancies. Eight anomalies were observed, of which 5 cases were

    cutis laxa. The later three cases were not thought to be related to

    penicillamine, because they did not conclude connective tissue

    anomalies7.

    Breast Milk

    There are no reports that describe the use of penicillamine during

    lactation or if the drug is excreted in milk have been located.

    Authors of one review recomend avoiding penicillamine during

    lactation5.

    Interactions (BNF)2

    Antacids: reduced absorption of penicillamine

    Iron: reduced absorption of penicillamine

    Zinc:reduced absorption of penicillamine

    EPIDEMIOLOGY OF POISONING

    Limited specific data of penicillamine poisoning are available.

    A 52 year old male presented at hospital 8 hours after ingesting 3.1 g

    penicillamine. Symptoms included, vomiting, dehydration, abdominal

    pain and tachycardia.

    Side effects reported at therapeutic dosage include:

    Initially nausea, anorexia, fever and skin reactions; taste loss

    (mineral supplements not recommended); blood disorders including

    thrombocytopaenia, agranulocytosis and aplastic anaemia; proteinuria,

    rarely haematuria (withdraw immediately); haemolytic anaemia,

    nephrotic syndrome, lupus erythematosus-like syndrome, myasthenia

    Gravis-like syndrome, pemphigus, Goodpasture’s syndrome, and

    Stevens-Johnson syndrome also reported; in non-rheumatoid conditions

    rheumatoid arthritis-like syndrome also reported; late rashes (reduce

    dose or withdraw treatment).

    MANAGEMENT

    No specific details available

    Decontamination

    If ingestion is within 2 hours, 50-100grams (adults) or 25-50 grams

    (children) of oral activated charcoal may be administered. Lactulose

    (20ml) should be given to prevent constipation. There is no data to

    indicate whether or not this is effective in penicillamine poisoning.

    Supportive care

    General supportive care should be given

    Monitoring

    As no data are available on penicillamine poisoning vital signs should

    be monitored-pulse, blood pressure, respiration.

    Antidotes

    There are no specific antidotes

    Elimination techniques

    No data available

    Investigations

    No data is available on penicilllamine poisoning, but routine

    investigations including renal function tests, urinalysis and

    electrolytes could be carried out.

    Case Data

    Other Toxicological Data

         No data available

    Ecotoxicological Data

         No data available

    Hazard Warnngs

         No data available

    Waste disposal data

         No data available

    Author

    Dr Alan Worsley Bsc(hons) PhD MRPharmS

    National Poisons Information Service (Newcastle Centre)

    Regional Drug & Therapeutics Centre

    Wolfson Building

    Claremont Place

    Newcastle upon Tyne

    NE1 4LP

    UK

    This monograph was produced by the staff of the Newcastle Centre of

    the National Poisons Information Service in the United Kingdom. The

    work was commissioned and funded by the UK Departments of Health, and

    was designed as a source of detailed information for use by poisons

    information centres.

    Peer review was undertaken by the Directors of the UK National Poisons

    Information Service.

    Last updated January 1997

    REFERENCES

  1. ABPI Data Sheet Compendium. Datapharm Publications Limited. 1996-1997
  2. British National Formulary. Number 32 (september 1996). British Medical Association and Royal Pharmaceutical Society.
  3. Dollery C. Therapeutic Drugs. (Suppl 2), Churchill Livingstone.   1994
  4. Crawhall JC et al . BMJ (1967);2:216-8
  5. Ostensen M et Husby G. Scand J Rheumatol. (1985);14:1-7
  6. Miehle W. Z Rhematol (1988);47(suppl 1):20-3
  7. Gal P et Ravenel SD. J Clin Dysmorphol (1984);2:9-12
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