Oral Transmucosal Fentanyl | What Is Fentanyl Citrate?

Fentanyl citrate refers to the citrate salt of fentanyl, a powerful synthetic opioid. Oral fentanyl includes any form of the drug that’s ingested through the mouth, including sublingual tablets or sprays, transmucosal lollipops or lozenges, and buccal soluble films.

If you research the synthetic opioid drug fentanyl, you’ll soon encounter two very different reports:

• fentanyl is one of the most widely prescribed and used medical painkillers in the world with special applications for treating breakthrough cancer pain
• fentanyl is a deadly illicit drug smuggled into the United States from oversea drug labs, and is a leading factor behind surging overdose death rates

Unfortunately, both accounts are accurate and describe the same substance in different forms with radically different impacts.

Fentanyl Citrate History

Fentanyl, produced medically as a fentanyl citrate, is a fully synthetic opioid drug originally discovered in Belgium by Paul Janssen of Janssen Pharmaceutica in 1959.

Janssen was reviewing a number of chemicals with similar structures to the synthetic opioid meperidine, searching for any that might offer pain relief and central nervous system sedation.

Fentanyl was one such drug, and proved to be extremely potent, with a strength up to 100 times greater than morphine by weight.

Following testing and clinical trials, fentanyl was used as a general anesthetic under the trade name Sublimaze in 1968 and continues to play an important role in anesthesia, analgesia (pain relief) and pain management today, especially for opioid-tolerant patients.

Fentanyl Citrate Legal Status

Like other opioid drugs, fentanyl is classified by the DEA/FDA as a schedule II controlled substance with a high potential for abuse and adverse effects including psychological or physical dependence.

If a person is convicted of improperly possessing a schedule II substance, including even a single dose of fentanyl, they face federal imprisonment for between 5 and 40 years for the first offense, and between 10 and life on the second offense.

Forms Of Fentanyl Citrate

While a large number of brand-name products containing fentanyl have been discontinued in recent years, the drug is widely available in a large number of different pharmaceutical formulations for use in treating a variety of different types of pain.

Specific forms of pharmaceutical fentanyl include:

• a variety of fentanyl injection preparations including intravenous, intramuscular, and subcutaneous forms
• transdermal fentanyl skin patches, which are small transparent films that adhere to and transfer the drug through the skin and into the
• bloodstream over the course of several days
• sublingual fentanyl tablets, which dissolve on the floor of the mouth under your tongue and are absorbed through the skin
• sublingual fentanyl sprays (Subsys), which are sprayed under the tongue and are absorbed through the skin
• oral transmucosal fentanyl citrate (OTFC) lozenges (Actiq), which look like lollipops and administer the drug through the skin on the inner lining of the mouth
• fentanyl buccal tablets (Fentora), which dissolve between the cheek and gums
• fentanyl buccal soluble films (Onsolis), which are placed in the mouth and allowed to dissolve and absorb through the skin
• intranasal sprays (Lazanda), applied through the nose

Oral Transmucosal Fentanyl Citrate

This diverse range of drug administration options, many of which focus delivery of the drug through the oral mucosa (or skin inside the mouth), are extremely important for the medical treatment of breakthrough pain and chronic pain.

Breakthrough pain is defined as an episode of sudden, severe pain that overwhelms the effects of standard opioid analgesics. It sometimes impacts those dealing with persistent pain, especially cancer patients and those with severe arthritis, fibromyalgia, and other serious conditions.

By providing fentanyl in easy-to-access, rapid onset, high-bioavailability forms like nasal sprays and lozenges, health care providers are able to reduce a patient’s pain intensity and effectively deal with these pain episodes as they arise.

Note that patients must generally attempt intravenous morphine, oral morphine, or oxycodone before fentanyl is prescribed.

Fentanyl Citrate Side Effects

As with other opioid drugs, fentanyl use is associated with certain common side effects including:

• constipation
• confusion
• feeling cold
• drowsiness
• dizziness
• dry mouth
• trouble sleeping
• decreased appetite
• sweating
• nausea
• anxiousness

Less-common adverse events can include:

• hallucinations or paranoia
• depression
• slurred speech
• chest pain
• unsteadiness
• fever
• sleep apnea
• respiratory depression
• difficulty urinating
• hypotension (low blood pressure)

Fentanyl Citrate Overdose

Fentanyl’s overdose toxicity is exceptionally high due to the drug’s extreme potency. If you suspect a fentanyl overdose has occurred, based on any of the following symptoms, immediately contact your local emergency department and apply the medication naloxone if available.

Fentanyl citrate overdose signs and symptoms can include:

• breathing problems
• slow or unsteady heart rate
• blue skin or fingertips
• difficulty speaking or moving
• pinpoint pupils
• loss of awareness

If you or a loved one struggle with opioid misuse or dependence, please consider contacting Northeast Addictions Treatment Center today.