What is Fentanyl?

Overdose, Side Effects, and Half-Life

What is Fentanyl?

Overdose, Side Effects, and Half-Life

Introduction

Fentanyl-involved overdose deaths continue to rise in the US. In 2016, 29% of all drug overdose deaths mentioned the involvement of fentanyl.1

Likewise, of 70,237 drug overdose deaths in 2017, more than two-thirds involved opioids. Synthetic opioids, including fentanyl, accounted for nearly 60% of all opioid overdose deaths.2

The death rate involving fentanyl and similar drugs increased by a whopping 45% from 2016 to 2017.2 With this, fentanyl has overtaken heroin as the leading cause of drug overdose deaths in the US.

Illicitly manufactured fentanyl is the major driver of overdose fatalities in recent years.

What is Fentanyl?

Fentanyl is a potent synthetic opioid available only on a prescription. It is a member of a group of pain medications known as narcotic analgesics.

Different forms of the drug are currently available. These include oral tablets, lozenges, and lollipops. Nasal sprays, transdermal patches, and solution for injection are also available.

Narcotic analgesics work by increasing the levels of a brain chemical – dopamine. Increased dopamine levels help relieve pain, promote euphoria, and decrease pain perceptions.

Fentanyl is 50 to 100 times more potent than morphine.3

Its therapeutic index (TI) is nearly four times that of morphine and over 50 times that of meperidine. TI measures the relative safety of a drug.4 The greater the value of TI, the safer is a drug.

Fentanyl History: Revisiting the Birth of America’s Top Killer Drug

Both morphine and meperidine were well-known opioid analgesics during the early 1950s. However, both the drugs were poorly absorbed into the brain. Thus, they took longer to show the pain-relieving effects.

Early Development

Paul Janssen and his team synthesized fentanyl in 1960. They were looking for an alternative to morphine and meperidine.5 Paul was a Belgian doctor and founder of Janssen Pharmaceutica. Paul and his team were looking for more powerful and rapidly acting pain medication. Between 1953 and 1957, they developed several new molecules. The most notable of these molecules was phenoperidine.

Animal studies revealed that phenoperidine was 25 times more powerful than morphine. Likewise, it was more than 50 times more powerful than meperidine.

The Janssen Company marketed phenoperidine in many European countries but not the US since they did not have permission to market there.

In the late 1950s, the team developed several phenoperidine-like molecules.

Eventually, they developed fentanyl in 1960. Animal studies showed it was ten times more powerful than phenoperidine. Initially, only the injectable form was considered effective for pain relief.

FDA Approval

The US FDA approved fentanyl in 1968 if it was combined droperidol. In 1972, the US FDA approved a vial containing only fentanyl.

Since the 1990s, the fentanyl patch has been widely used to manage both chronic cancer and noncancer pain.

In the last two decades, over twelve fast-acting preparations have become available.

Uses of Fentanyl

Fentanyl has several uses. Doctors prescribe it for treating severe pain in cancer patients. Likewise, they also prescribe it for patients who have undergone major surgery.

It may also be used to treat chronic pain in patients who do not respond to other opioid pain medications.

As a sedative, it is used as a drip in intubated patients to assist ventilation. Sometimes, it may be used before or during surgery to calm a patient down.

Sometimes, doctors may use it in combination with antipsychotic medications to treat epilepsy.

Fentanyl Side Effects: Things to Know

Side effects may be experienced while taking prescribed doses. The side effects can be worse when someone abuses or misuses the drug.

Anyone who is taking fentanyl in the prescribed doses may experience:

Some people may also complain of:

Most of these side effects usually go away on their own. However, some effects may persist and can lead to complications. If any side effects persist or become worse, talk to your doctor immediately.

The patches may cause skin rashes, itching, and swelling at the site of application.

Fentanyl Abuse and Addiction

The National Institute on Drug Abuse (NIDA) defines fentanyl abuse as “the use of fentanyl without a prescription, in a way other than as prescribed, or for the experience or feelings elicited.”6

The American Academy of Pain Medicine (AAPM) defines addiction as “a primary, chronic, neurobiological disease, with genetic, psychosocial, and environmental factors influencing its development and manifestations. It is characterized by behaviors that include one or more of the following: impaired control over drug use, compulsive use, continued use despite harm, and craving.”6

In simple terms, addiction is a long-term brain disease in which an individual compulsively uses a drug despite its harm. The pattern of drug use is continuous. Moreover, the individual has little control over its use.

Long-term fentanyl abuse can lead to its addiction. This is because it is one of the most addictive prescription drugs. However, one should keep in mind that addiction from prescription fentanyl is rare.

In most cases, addiction develops from its recreational use. The US market has been flooded with illegally manufactured fentanyl, worsening the opioid epidemic.

Fentanyl Overdose: A Quick Look at the Stats

A drug overdose occurs when an individual accidentally or deliberately consumes a large amount of the drug within a short period.

Fentanyl is a relatively safe drug. Nonetheless, overdose deaths are increasing at an alarming rate.

The rate of drug overdose deaths involving fentanyl and related substances increased by 100% each year from 2013 through 2016. In 2013, the rate was 0.6 per 100,000, whereas, in 2014, it was 1.3. Likewise, it more than doubled to 5.9 in 2016 from 2.6 in 2015. This is according to the National Vital Statistics Report. The report was published on December 12, 2018.1

The same report also noted that fentanyl overdose deaths were mentioned in:

Fentanyl Overdose Deaths 2011-2016

1,662 in 2011

1,615 in 2012

1,919 in 2013

4,223 in 2014

8,251 in 2015

18,335 in 2016

By the end of 2017, nine out of every ten overdose deaths in Massachusetts involved fentanyl.7

Signs

Below are the signs of an overdose8:

Sudden breathing difficulties

Confusion

Loss of consciousness

Excessive sweating and reduced body temperature

Bluish discoloration of the skin and nails

Coma and death due to impaired blood supply to the brain

Overdose Treatment and Prevention

Treatment

Naloxone is an antidote for fentanyl overdose. For better outcomes, treatment with naloxone should begin as early as possible.

Naloxone is known as an opioid antagonist. It prevents the drug from binding to opioid receptors in the body. That way, it blocks the effects of fentanyl and other opioids.

Naloxone is available without a prescription in most states in the US. Some authorities also urge people who use fentanyl or other opiates to carry naloxone with them. 9

Prevention

Strictly follow the directions for use

Do not mix fentanyl with alcohol, sleeping pills, or other medications

If you are using it for the first time, or are returning to use after detox, remember that the risk of overdose may be higher

Sources of Illegal Fentanyl

A major portion of the illegal drug comes from China.10

A thousand grams of fentanyl is available in China for about $4000. The same amount can be potentially lethal for 500,000 people.11

A 2018 study suggests the “recreational” drug market gets most of its fentanyl from two major sources.12

First, from illegal manufacturing facilities, both inside and outside the country. The manufacturers may also mix it with heroin or cocaine to increase potency.

Second, from fentanyl-containing medicines such as the patches. Drug abusers may inject or inhale fentanyl obtained from the patches. Interestingly, some may eat the whole patch or insert it into the rectum.

Keeping a patch in the mouth dramatically increases absorption into the bloodstream. That way, the contents of a 50 mg patch can produce blood levels equivalent to those produced by 5000 mg of oral fentanyl.13

Fentanyl Withdrawal Symptoms

If you have been using fentanyl for some time, stopping it abruptly can cause a set of unpleasant effects. These effects are known as withdrawal symptoms. Withdrawal symptoms indicate the dependence of an individual on a drug.

These symptoms can begin within a few hours of stopping the drug