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Article Summary

History Of Fentanyl

Fentanyl was introduced in the 1960s. Since then, it has quickly become one of the most popularly used opioids for intraoperative analgesia. From the early 1990s onwards, patches containing the drug are available for use in the management of chronic, moderate, and severe pain for all types of cancer, as well as for persistent and intense pain arising from other non-cancerous ailments.

In the course of the last 20 years, over 6 rapid onset trans-mucosal Fentanyl medications have been discovered, developed, produced, launched, and approved for breakthrough pain syndromes.

But why is Fentanyl used to treat pain in clinical practice? And why do people abuse the drug? Recent data indicates that the popularity of the drug has been due to its minimal effects on the cardiovascular system. It could also be attributed to the fact that this substance does not increase plasma histamine.

Additionally, Fentanyl works relatively slowly in the onset of action and the duration of its effects is quite short. In the same way, the drug can easily and inexpensively be synthesized and prepared for the marketplace.

Apart from all the above, this substance is familiar with most of the clinicians who work in perioperative and pain medicine all around the world - but more so in the United States.

Today, it is among the most important opioid drugs used for managing pain. In particular, Fentanyl is now available for transmucosal, transdermal, and intravenous administration. Its physical characteristics, familiarity, potency, and flexibility all go a long way in explaining why it is such a valuable drug for the management of pain.

Origins Of Fentanyl

A powerful synthetic opioid, Fentanyl has been gaining widespread attention particularly in modern mass media. This could be as a result of the role it has played in the dependence, addiction, overdose, and death of many people all around the country. It was, for instance, believed to have caused the death of Prince, a world renowned music legend.

But what is this drug? Where does it come from, and where it originate? These are all questions that many people ask especially because it seems like Fentanyl came from nowhere before the headlines were filled with news of the drug and the massive addiction problem it causes to users.

Consider the following answers:

What is Fentanyl?

At its most basic, Fentanyl can be defined as a potent and powerful opioid analgesic that is quite similar to morphine but with effects that could be anywhere between 50 and 100 times stronger. As such, the drug is classified by the DEA (Drug Enforcement Authority) as a Schedule II substance meaning that it has an incredibly high potential for misuse and addiction. However, it is used as a prescription medication for its therapeutic pain relief benefits, in a variety of brand names including Duragesic, Sublimaze, and Actiq.

In the hospital or clinical setting, patients might be given a Fentanyl prescription for the treatment of severe pain - such as in the management of the pain caused by cancer as well as following surgery. The drug is also used to treat chronic pain especially for patients who have developed resistance to other less powerful opioids.

On the street, Fentanyl (or when it is mixed with heroin) is called Goodfella, Friend, and China Girl. Most of these formulations are made illegally in illicit labs, meaning that they might be more dangerous than the prescription versions.

Although Fentanyl can be safe and effective in treating severe pain in the medical setting, those who abuse it illegally can find that it is quite dangerous. At the moment, there are over 12 different illicit types of the drug.

One of the reasons behind the dangers of these formulations is because their effects tend to last for a shorter duration than, say, heroin. When a drug is as powerful as Fentanyl and acts for a short term, it might prove to be more addictive meaning that the potential for abuse and eventual overdose tends to be much higher.

Fentanyl Abuse

Before reviewing the origins of Fentanyl and where it comes from, it is important to have a rough idea of its effects and well as signs of abuse. When you use this drug in ways other than those recommended by a genuine prescription, it might cause an euphoric high and complete relaxation.

However, if you take large doses of the drug, you may experience sedation, nausea, confusion, and extreme drowsiness. Fentanyl can additionally contribute to other serious consequences, including but not limited to respiratory arrest or distress and coma.

In the same way, although you might feel high the first time you take this drug, it may cause depression especially when you start coming down from this initial high filled with euphoric feelings.

In the long term, abusing Fentanyl can also cause the quality of your life to deteriorate. You might, for instance, lack the ability to make lucid and sound decisions or show good judgement. Additionally, you may develop tolerance to it, meaning that you will have to start taking higher doses to enjoy its desired effects.

Where Does Fentanyl Originate?

Fentanyl was first developed by the Janssen Pharmaceutical Company in 1959. At the time, the drug was mostly used as a pain reliever and anesthetic for medical purposes and in clinical settings.

In the 1960s, Fentanyl was applied medically as an anesthetic that was administered intravenously in the form of Sublimaze. However, the Fentanyl patch only came into mainstream use in the 1990s and started being used to treat chronic pain - such as the pain caused by various forms of cancer. Eventually, other ways of delivering the drug were introduced to the market. They included oral options like the Actiq lozenge or lollipop.

With regards to the Fentanyl that is used illegally, it might be difficult for you to know the origins. Most of the illicitly sold and used forms of the drug in the United States come from China. However, the drug did not originate in China. However, since there are relatively low pharmaceutical regulations in the country, it has quickly developed into one of the major suppliers of illicit chemicals and prescription drugs. Although some Fentanyl arrives in the US directly from China, there are many other shipments coming in through Canada and Mexico before reaching the United States.

Today, China also exports a variety of other Fentanyl products - including the drug in its raw form, counterfeit prescription medications (such as oxycodone) laced with this substance, and analogs.

Chinese exporters also have a variety of ways of getting the drug to the West. Some of them, for instance, mislabel their shipments. In 2015, for instance, agents working at the US border seized more than 200 pounds of the drug (among other synthetic opioids) before they were smuggled into the country through Mexico.

Although China has been making strides towards the prevention of the exportation of the drug, these efforts have not been entirely successful. However, the US has also introduced legislation to reduce illicit Fentanyl from getting into the country. Examples of these legislations include the Synthetics Trafficking and Overdose Prevention Act of 2017. Despite this, Fentanyl is still one of the most problematic narcotics - in general - and opioids - in particular - in the country.

More On The History Of Fentanyl

Fentanyl was first formulated, prepared, and developed by Paul Janssen in 1959 from a patent that his company (Janssen Pharmaceutica) held. Since this drug is a potent and powerful analgesic - that is close to 100 times as strong as morphine - it was first used as an anesthetic and pain reliever. This form of use was quickly adopted in many different medical settings.

By the 1960s, for instance, it was introduced to the market under the Sublimaze brand name for use as an anesthetic that could be administered intravenously. Sublimaze proved so popular that other Fentanyl analogues were developed. They included Remifentanil, Lofentanil, Alfentanil, and Sufentanil.

Eventually, the Fentanyl patch was finally developed in the mid-1990s. It was designed in such a way that it could deliver the drug as a transdermal formulation for helping patients manage their pain. Given the brand name Duragesic, this patch could now be worn right on the surface of the skin. It was useful for managing the chronic pain that is typically felt by people with cancer, for instance.

At the time, this patch was made using an inert alcohol gel that was infused with some pre-determined Fentanyl doses. The patch worked by releasing the drug into body fats. After that, it would move slowly through the bloodstream over a period of 2 to 3 days. In the process, it would deliver pain relief over the long term.

These patches - Duragesic in particular - underwent a series of clinical trials and rigorous testing before they were approved for use in the mainstream market. Eventually, they were introduced and are now popular in clinical and medical practice.

Following the success of Duragesic, other devices for delivering Fentanyl were developed. They included the Actiq lollipop and the Femora buccal tablets. Most of these oral formulations contained a mixture of fillers and Fentanyl citrate. Actiq, for instance, was designed to provide fast acting pain relief for long term pain sufferers.

Additional products containing this potent opioid included a buccal spray and an effervescent lozenge. Despite the introduction of these various modes of delivery, the Duragesic transdermal skin patch is still the most popularly and widely used Fentanyl product.

More recently, however, the FDA (Food and Drug Administration) approved another product containing this drug. Today, Onsolis can be used in the treatment of breakthrough pain. It works as a soluble film of the drug - that is on a disc - that you can place in the mouth where it is absorbed immediately. Onsolis is popular because it effectively avoids the possibility of crushing or inhaling the drug.

Fentanyl Misuse

The FDA approved the first formulation of Fentanyl (Sublimaze) in the 1960s for use as an anesthetic for intravenous application. Additional formulations of the drug that have received FDA approval include a dissolving film and tablet, a fast acting lollipop or lozenge for breakthrough pain, and a transdermal patch.

The abuse of prescription Fentanyl was described for the first time in the 1970s among clinicians. Today, it is a reportedly widely abused among people who misuse prescriptions of the drug.

From 2005 to 2007, there was an increase in the number of deaths related to illegally manufactured Fentanyl. The drugs were eventually traced back to an illicitly operated lab in Mexico. The laboratory was shut down, leading to a sharp decline in the number of drug overdose related to the drug.

However, there has been an upsurge in the illicit production and manufacture of Fentanyl - most of which comes to the United States from China, Canada, and Mexico. This increase in the available of the drug is reflected in the substantial rise in seizures of the drugs by law enforcement officials.

In particular, there were less than 1000 seizures as of 2013. By 2015, however, there were more than 13000 seizures. Research shows that this increasing availability of illegally manufactured Fentanyl has corresponded and mirrored the simultaneous increase in overdose deaths related to synthetic opioids.

More recently, Tom Petty's death was officially ruled as an overdose arising from a combination of different pain relief medications including Fentanyl. The same drug was also attributed to the death of Prince, a music legend of international repute.

Although most people may not be immediately familiar to Fentanyl in the same way that they know other commonly cited substances like OxyContin and Percocet, the drug is far from uncommon.

One of the reasons that Fentanyl is so widely misused and leads to such high incidences of addiction, overdose, and fatal deaths is because it is quite potent - certainly 50 to 100 times as potent as morphine. It is also anywhere between 25 to 50 times as potent as heroin. This is why the federal government currently classifies it as a Schedule II controlled substance.

Concluding Thoughts

Overall, using Fentanyl regularly for the treatment and management of pain is not the best option. This is because the drug is so potent that is commonly prescribed in terms of micrograms instead of as milligrams. It also tends to hit patients quickly - in as few as 5 minutes - before wearing off quite as fast (and lasting for about 2 - 4 hours).

Originally, Fentanyl was used to make death experiences less painful. As such, it was never designed for use in the course of life for managing pain. Since it is so over-prescribed and - as a direct result - highly sought after by those who are addicted to it, the only remedy is to stop using it.

In case you have a problem with this drug, the best solution is to seek treatment at an inpatient rehabilitation facility. Through medication assisted therapy, counseling, as well as other forms of therapy, you will eventually be weaned of the drug and it will no longer be a problem for you.

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