Fentanyl
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| PsychonautWiki | TripSit | Pharmacology | DrugCentral | DailyMed | ||
|---|---|---|---|---|---|---|
| Classification | ||||||
| Class / category | — | — | — | ≈ | ||
| Also known as | FentanylfentanilSublimazeActiqDurogesicDuragesicFentoraMatrifenHaldidOnsolisInstanylAbstralLazanda | fent | — | — | — | ≠ |
| Safety | ||||||
| Addiction potential | extremely addictive with a high potential for abuse | — | — | — | — | |
| Toxicity | potentially fatal at heavy dosagespotentially lethal when mixed with depressants like alcohol or benzodiazepinesunintentionally transporting the substance from the skin by touching the mouth, nose or eyes is dangerous | — | — | — | — | |
| Dangerous interactions | — | — | — | — | ||
| Dose · Insufflated | ||||||
| Threshold | 5 μg | — | — | — | — | |
| Light | 10–25 μg | 10–25 µg | — | — | — | ≠ |
| Common | 25–50 μg | 25–50 µg | — | — | — | ≠ |
| Strong | 50–75 μg | 50–75 µg | — | — | — | ≠ |
| Dose · Sublingual | ||||||
| Threshold | 5 μg | — | — | — | — | |
| Light | 10–25 μg | — | — | — | — | |
| Common | 25–50 μg | — | — | — | — | |
| Strong | 50–75 μg | — | — | — | — | |
| Heavy | 75 μg+ | — | — | — | — | |
| Dose · Transdermal | ||||||
| Threshold | 5 μg | — | — | — | — | |
| Light | 12–25 μg | — | — | — | — | |
| Common | 25–50 μg | 25–50 µg | — | — | — | ≠ |
| Strong | 50–100 μg | 50–100 µg | — | — | — | ≠ |
| Heavy | 100 μg+ | — | — | — | — | |
| Duration | ||||||
| Onset | 15–30 minutes | — | — | — | — | |
| Total | 1–4 hours | — | — | — | — | |
| Pharmacology | ||||||
| Receptor activity | — | — | — | OPRM1OPRD1Hrh1OPRK1MAOAKCNH2SIGMAR1SLC22A1 | — | |
| Half-life | — | — | The half life of fentanyl is 7 hours. The half life of fentanyl sublingual spray is 5-12 hours. Fentanyl kinetics were studied in patients with cirrhosis and in patients with normal hepatic and renal function undergoing surgery under general anaesthesia, the latter group served as the controls. Plasma fentanyl concentrations declined bi-exponentially in the controls with an average elimination half-life (T1/2 beta) of 263 min; total plasma clearance (Cl) as 10.8 mL/kg/min, and total apparent volume of distribution (V beta) 3.81 L/kg. No significant change was observed in patients with cirrhosis: T1/2 beta was 304 min, Cl 11.3 mL/kg/min and V beta 4.41 L/kg. These data suggest that the elimination half-life of fentanyl is not primarily influenced by the rate at which it is metabolized in the liver. Fentanyl was administered intravenously and transdermally to eight surgical patients to determine the systemic bioavailability and rate of absorption of the transdermally administered drug. Serum fentanyl concentrations reached a plateau approximately 14 hr after placement of the transdermal fentanyl delivery system. This plateau was maintained until removal of the system at 24 hr. The decline in serum fentanyl concentrations after removal of the transdermal system had a terminal half-life of 17.0 +/- 2.3 hr (mean +/- SD), considerably longer than the terminal elimination half-life seen after intravenous administration of fentanyl in the same patients (6.1 +/- 2.0 hr). ... ... In order to determine the bioavailability and absorption of fentanyl from OTFC, 12 volunteers were given intravenous fentanyl citrate or OTFC 15 ug/kg on each of two occasions. On a third occasion, the authors assessed oral administration (gastrointestinal absorption) by giving eight of the same volunteers the same dose of a solution of fentanyl citrate to swallow. In each study, arterial blood samples were taken over 24 hr for analysis of plasma fentanyl. After intravenous (iv) administration of fentanyl ... the terminal elimination half-life was 425 +/- 102 min. ... Following IV administration of fentanyl citrate in healthy individuals, the estimated initial distribution half-life was about 6 minutes, the second distribution half-life was about 1 hour, and the terminal half-life was about 16 hours. Studies of IV fentanyl suggest that clearance of the drug may be decreased and half-life increased in geriatric patients. Although the pharmacokinetic profile of fentanyl in healthy Caucasian adults 65 years of age or older (mean age: 71 years) generally was similar to that in adults 18-45 years of age following application of a fentanyl transdermal system labeled as delivering 100 ug/hour for 72 hours, the mean half-life of the drug was longer in geriatric individuals compared with younger adults (34.4 versus 23.5 hours). | — | — | |
| Protein binding | — | — | Fentanyl is 80-85% bound to plasma proteins. In one study, a 0.1µg/L solution of fentanyl was 77.9±1.1% bound to human serum albumin and 12.0±5.4% bound to α-1 acid glycoprotein. A 0.1µg/L solution of norfentanyl, the primary metabolite of fentanyl, was 7.62±1.2% bound to human serum albumin and 7.24±1.9% bound to α-1 acid glycoprotein. | — | — | |
Dose at a glance
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PsychonautWiki summary
This substance is extraordinarily potent (i.e. active in the microgram range). For this reason, it should be handled with extreme care and never be eyeballed. Fentanyl can also be fatal when combined with depressants such as opiates, benzodiazepines, barbiturates, gabapentinoids, thienodiazepines or other GABAergic substances.[1] It is strongly encouraged to wear gloves while handling, use volumetric dosing combined with a milligram scale, and to not consume either moderate or heavy dosages of other depressants in combination with this drug.
TripSit summary
Fentanyl is a synthetic opiate analgesic with a rapid onset and short duration of action. It is a strong agonist at the μ-opioid receptors and is historically used to treat breakthrough pain. Fentanyl is approximately 100 times more potent than Morphine, and is commonly used as a patch. Sometimes used as an adulterant for heroin, which has led to many overdose deaths.
Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.