User:Mr. Ibrahem/Fentanyl
From Wikipedia, the free encyclopedia
Fentanyl, also spelled fentanil, is an opioid used as a pain medication and together with other medications for anesthesia.[3] Fentanyl is also used as a recreational drug, often mixed with heroin or cocaine.[5] It has a rapid onset and its effects generally last less than two hours.[3] Medically, fentanyl is used by injection, nasal spray, skin patch, or absorbed through the cheek (transmucosal) as a lozenge or tablet.[3][6]
Clinical data | |
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Pronunciation | /ˈfɛntənɪl/ or /ˈfɛntənəl/ |
Trade names | Actiq, Duragesic, Fentora, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a605043 |
License data | |
Pregnancy category |
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Dependence liability | High[1] |
Routes of administration | Buccal, epidural, IM, IT, IV, sublingual, skin patch |
Drug class | Opioid |
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Pharmacokinetic data | |
Bioavailability | 92% (transdermal) 89% (intranasal) 50% (buccal) 33% (ingestion) 100% (intramuscular)/> 55% (inhaled) |
Protein binding | 80–85% |
Metabolism | Liver, primarily by CYP3A4 |
Onset of action | 5 minutes[2] |
Elimination half-life | IV: 6 mins (T1/2 α) 1 hours (T1/2 β) 16 hours (T1/2 ɣ) Intranasal: 6.5 hours Transdermal: 20–27 hours[3] Sublingual/buccal (single dose): 2.6–13.5 hours[3] |
Duration of action | IV: 30–60 minutes[2][4] |
Excretion | Mostly urinary (metabolites, <10% unchanged drug)[3] |
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Chemical and physical data | |
Formula | C22H28N2O |
Molar mass | 336.479 g·mol−1 |
3D model (JSmol) | |
Density | 1.1 g/cm3 |
Melting point | 87.5 °C (189.5 °F) |
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Common side effects include vomiting, constipation, sedation, confusion, hallucinations, and injuries related to poor coordination.[3][7] Serious side effects may include decreased breathing (respiratory depression), serotonin syndrome, low blood pressure, addiction, or coma.[3][7] 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.[8]
Fentanyl was first made by Paul Janssen in 1960 and approved for medical use in the United States in 1968.[3][9] In 2015, 1,600 kilograms (3,500 lb) were used in healthcare globally.[10] As of 2017[update], fentanyl was the most widely used synthetic opioid in medicine.[11] Fentanyl patches for cancer pain are on the World Health Organization's List of Essential Medicines.[12] In 2016, fentanyl and analogues were the most common cause of overdose deaths in the United States at more than 20,000, about half of all opioid-related deaths.[13][14][15] Most of these overdose deaths were due to illegally made fentanyl.[16]
For a 100 microgram vial, the average wholesale cost in the developing world was US$0.66 in 2015.[17] In 2017, the price in the United States was US$0.49 for that same amount.[18] In the US, the 800 mcg tablet was 6.75 times more expensive as of 2020 than the lozenge.[19][20] In 2017, it was the 250th most commonly prescribed medication in the United States, with more than 1.7 million prescriptions.[21][22]