Fentanyl
General Information
Introduction
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. The patches work by releasing fentanyl into body fats, which then slowly release the drug into the bloodstream over 48 to 72 hours, allowing for long-lasting relief from pain.
History
Fentanyl was first synthesized by Paul Janssen in 1960. Fentanyl was introduced in patch form in the mid 1990s, shortly followed by lollipop form. As of 2012 fentanyl was the most widely used synthetic opioid in clinical practice.
Dosage
Approximately 100 micrograms of fentanyl is equivalent to 10mg of morphine. Rate of absorption is dependent on a number of factors. Body temperature, skin type, amount of body fat, and placement of the patch can have major effects. Fentanyl is available as a patch, nasal spray, lollipop lozenge (percopop), or inhaler.
Patch
Bioavailability: nearly 100%
Duration: 8-72 hours
Medium (typical) dose: 400 μg
Patches are available in doses ranging from 1.25mg to 10mg
The patch may be taken orally, but it is not recommended.
Lollipop Lozenge
Oral Bioavailability: 33%-50%
Duration: 8-12 hours
Typical dose: 400 μg
High dose: 1600 μg
Available in dosages from 200 μg to 1600μg
Insufflated
Fentanyl powder may be snorted, but it is not recommended.
Smoked
The gel inside patches can be smoked. The powder also may be smoked, although it is not recommended.
Injected
Fentanyl powder may be injected, but it is not recommended.
Effects
The effects of fentanyl are similar to that of heroin.
Positive
- Analgesia
- Euphoria
- Feelings of relaxation
Neutral
- Hallucinations
- Sedative effects
- Changes in focus, attention
Negative
- Respiratory depression
- Diarrhea
- Nausea
- Constipation
- Dry Mouth
- Somnolence
- confusion
- weakness
- Sweating
- headache
- Fatigue
- Dizziness
- Nervousness
- Anxiety
- Urinary retention
After effects
- Risk of post-acute withdrawal effects, including depression, anxiety disorder, psychosis, or even suicidal ideation in extreme cases
Harm Reduction
Fentanyl is considered one of the safest opioid medications on the market, as well as the least physically harmful to the body with long-term or life-term use. Still, fentanyl has caused overdoses and deaths, especially when mixed with other drugs.
Illicitly synthesized fentanyl powder has also appeared on the United States market. Because of the extremely high strength of pure fentanyl powder, it is very difficult to dilute appropriately, and often the resulting mixture may be far too strong and, consequently, very dangerous.
Sometimes fentanyl is sold as heroin. Some dealers may mix fentanyl powder with heroin to increase potency or compensate for low-quality heroin. If you have any concerns about your drug, please test it.
- Avoid driving and operating heavy machinery
- Risk of Post-acute withdrawal effects
- Strong addiction potential due to short effects
- Risk of overdose/death
Chemistry and Pharmacology
Fentanyl is a potent μ-opioid receptor agonist with relatively little effect on κ or δ receptors compared to most opioids. Being very lipid soluble, it penetrates the blood-brain barrier quickly and efficiently, which accounts for its high potency compared to traditional opioids. When taken orally, fentanyl undergoes extensive first-pass metabolism by CYP3A4 to non-active metabolites, and as such, CYP3A4 inhibitors (such as grapefruit juice) could potentially be very dangerous when coadministered with fentanyl.
Images
Legal
In most countries, fentanyl is illegal to sell without a license and illegal to buy or possess without a license or prescription.
Europe
America
Regulated as a schedule II opiate.
Canada
Regulated as schedule I.
Australia
Fentanyl is a border controlled substance under Criminal Code Act 9.1.314 and is additionally controlled by several states and territories.