FENTANYL CITRATE

Fentanyl citrate is an opioid. It is a pain medication used to treat "breakthrough" cancer pain when other therapies have failed to control the pain. This medicine is not for treating pain that is not cancer- related. Fentanyl works primarily by activating μ-opioid receptors.[3] It is around 100 times stronger than morphine, and some analogues such as carfentanil are around 10,000 times stronger. It has a rapid onset and its effects generally last less than two hours. It is also used as a recreational drug, often mixed with heroin or cocaine. Any Misuse of this medicine can cause addiction, overdose, or death. It is also used with general, regional, and spinal anesthesia. By 2017, fentanyl had become the most widely used synthetic opioid in medicine. Fentanyl citrate is sold and marketed under the brand name sublimaze, amongst others. Paul Janssen first made Fentanyl in 1960. It was approved for medical use in the United States in 1968. The World Health Organization’s List of Essential Medicines recommends fentanyl patches for cancer pain. Fentanyl was most common cause of overdose deaths in the United States at more than 20,000, about half of all opioid-related deaths.

Forms and Dosage

Fentanyl is administered through injection, nasal spray, skin patch, or absorbed through the cheek (trans mucosal) as a lozenge or tablet. For controlling moderate pain or severe pain, the recommended dose is 50 to 100 mcg over 1 to 2 minutes, given 30 to 60 minutes before surgery, for intraoperative or management of severe pain. This is strictly for use only in a monitored anesthesia care setting in the hospital, the same dose is also given as a part of the pain management in post- operative care. In the chronic severe pain management in opioid-tolerant patients who require daily, around-the-clock, long-term opioid treatment. In the management of severe breakthrough cancer pain in opioid-tolerant patients, the standard dosage for adults older than 16 years initially is a single 200-mcg lozenge placed between the cheek and lower gum as directed for breakthrough pain. tablets should be sucked, not chewed, over a period of 15 minutes. Repeat dose if the initial dose didn’t work, with a maximum of 2 lozenge units per breakthrough pain episode. Maximum dose is capped at 4 lozenge units/day.

The cost of Fentanyl

In the USA, a single dose of 200 mg liquid costs USD85, a 200 mcg lozenge costs $87USD. The 100 mcg, 72 hour pain patch costs $2.03 USD whereas the 250 mcg injection costs around $0.45 - $0.72. the 300 mcg nasal solution costs USD 1566 and each 200 mcg tablet costs USD 73. There are average prices of certain mainstream brands and units.

How does Fentanyl work?

Fentanyl, like other opioids, acts on opioid receptors. These receptors are G-protein-coupled receptors, which contain seven transmembrane portions, intracellular loops, extracellular loops, intracellular C-terminus, and extracellular N-terminus. As fentanyl binds, its actions inhibit downstream signaling, such as decreased cAMP production, decreased calcium ion influx, and increased potassium efflux resulting in blocked pathways in the central nervous system to increase pain threshold by changing the perception of pain, mediated by decreasing propagation of nociceptive signals that result in analgesic effects.

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