Humans have been practicing various forms of pain management for thousands of years. Stone Age people tried to banish pain by presenting religious offerings and sacrificing animals. Some Native American cultures sucked on pain pipes held against the skin to extract the pain. In Ancient Egypt, electric eels were taken from the Nile and laid on wounds. In 400 BC, the Ancient Greeks, on the advice of Hippocrates, used willow bark and the chewing of willow leaves to help women during childbirth — and they weren’t too far off the mark. Willows contain a form of salicylic acid, the active ingredient of aspirin.

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Opiates have also been used for thousands of years, an analgesic originally derived from the opium poppy. Morphine, the active substance, was named after Morpheus, the Greek god of dreams. Opiates represented an entirely new class of pain relief. They were extremely powerful, but also highly addictive.

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During the 16th Century, early chemists created laudanum, opium prepared in an alcoholic solution. In the 19th century morphine was extracted in its pure form. By the 1830s, drug dependency reached disturbing proportions, leading to the mobilization of British warships along the Chinese coast in an effort to suppress opium traffic.

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Aspirin goes back for millennia, but it wasn’t properly formulated until 1897 by Frederick Bayer and Felix Hoffman. Codeine, a naturally occurring methylated morphine, was first isolated in France in 1830 by Jean-Pierre Robiquet to replace raw opium in medications. It was primarily used as a cough remedy, but it’s still used today in such products as Tylenol 3. Chemists developed heroin in an effort to create something less addictive than morphine — but ended up developing a product with twice the addictive qualities.

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By the late 20th century, a new breed of painkillers hit the market — synthetic opiates. Common names include Vicodin (1984), OxyContin (1995), and Percocet (1999).

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Today, there are many different types of pain relievers. The most popular over-the-counter medications include Nonsteroidal anti-inflammatory drugs (NSAIDs) and Acetaminophen​.

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Nonsteroidal anti-inflammatory drugs (NSAIDs) and How They Work

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NSAIDs are among the most widely used analgesic substances in the world. However, the consumption of these products is associated with various adverse and life-threatening side effects such as heart-attack, stroke, and internal bleeding. These chemicals act on bodily processes that cause inflammation, pain, and fever. Examples include aspirin (the most widely used drug in the world), ibuprofen, naproxen, and indomethacin. They represent a diverse class of drugs and are among the most commonly used pain relievers worldwide. It’s estimated that NSAIDs are used by 30 million people every day.

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Pain relievers, like ibuprofen and aspirin, block the production of a very special class of tuning chemicals called prostaglandins. Our cells release arachidonic acid when they’re damaged; the enzymes COX-1 and COX-2 convert the arachidonic acid into prostaglandin H2, which then turns into a series of other chemicals that do such things as raise our body temperature, cause inflammation and lower our pain threshold. NSAIDs interfere with this process, raising our pain threshold. Aspirin performs this task by blocking the way arachidonic acid fits within the COX-1 and COX-2 enzymes, deactivating them.

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Acetaminophen (also called paracetamol) is derived from coal tar and is a mild analgesic that does little to treat inflammation, but increases the body's pain threshold. It is commonly used to treat headaches and is a major ingredient in many cold and flu remedies. The Food and Drug Administration warns that taking 25% above the daily maximum dose over several days can cause liver damage. During the last decade, more than 1,500 Americans died after taking too much of it. 

 

Endocannabinoid System Discovery

 

Using CBD dates back to the 19th century. Queen Victoria would use cannabis to alleviate menstrual cramps. In the early 1980's, studies hinted that CBD could alleviate certain types of pain, anxiety and nausea but it still didn't get much attention until almost a decade later. Research on the cannabis plant led directly to the discovery of a new chemical signaling system in the human body which is now recognized as playing a crucial role in regulating our physiology. Would it surprise you to know that cannabinoids exist in the human body? Endocannabinoids are proteins produced in the human body to help govern the physiological process of pain modulation, immune function, inflammation regulation and more.

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In 1988 the first cannabinoids receptor (molecule on the outside of a cell that receives a signal for the cell to do something specific) known as CB1, was discovered in humans. The receptors reside primarily in the brain. The function of the CB1 receptor is for appetite, immune function, muscle control, pain, inter-ocular pressure, cognition, reward mechanism and thermoregulation.

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In 1993, a second cannabinoid receptor was found in the macrophage (type of white blood cell) cells in the spleen suggesting a role in immune function, cell proliferation, inflammation and pain. In 1998, GW Pharmaceuticals based in Great Britain began to cultivate cannabis for medical trials to extract CBD for use in medicine.

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More recent science shows that different cannabinoids hold tremendous therapeutic promise. In 2008 it was reported that Beta-caryophyllene (BCP) selectively binds to the CB2 receptor and inhibits pro-inflammatory pathways. This discovery and rich scientific literature that suggests a role in potentially treating conditions through both topical and oral administration has led to new thinking about the role BCP plays in human health.

 

Newly discovered G-Protein Coupled Receptors called GPR18, GPR55 and GPR119 regulate bone density, insulin release and energy intake. Phytocannabinoids such as Beta-caryophyllene (BCP) plays an active role in regulating GPR Receptors. New studies of BCP are showing potent therapeutic benefits in managing pain as well as topically with its antifungal and antibacterial properties.

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NSAIDS, Cannabinoids or Both for the Relief of Pain?

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For many people with chronic pain and other conditions that cause pain and inflammation, it is quite common to take NSAIDs to find relief from their condition. However, a number of studies have shown that NSAIDs have adverse side effects. If taken for an extended period of time, they may cause stomach pain and heartburn, stomach ulcers, liver disease, headaches and allergic reactions such as rashes and wheezing In certain instances, NSAIDs might even make a person more prone to bleeding.

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If you’re taking NSAIDs to relieve body pain and inflammation, you might be wondering how you can reduce the severity or find relief from your symptoms without taking these harmful medicines. Fortunately, there are alternatives to NSAIDs. One of them is Beta-caryophyllene (BCP), an effective cannabinoid with no known side adverse effects. BCP has been shown to be capable of treating and preventing pain and inflammatory disorders. For instance, if you want to treat an inflamed muscle or joint, simply apply and massage a BCP-rich cream into the affected area to relax your muscles and find relief.

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There's new evidence emerging regularly that Cannabinoids hold tremendous promise on the pain treatment front.

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