Lofentanil Stats & Data
CCC(=O)N(c1ccccc1)C1(CCN(CCc2ccccc2)CC1C)C(=O)OCIMYHGORQCPYVBZ-NLFFAJNJSA-NPharmacology
DrugBankDescription
Lofentanil is an analog of fentanyl and is one of the most potent opioids available today. It displays most similarity to carfentanil (4-carbomethoxyfentanyl) and is considered to be slightly more potent than this drug.
Effect Profile
CuratedStrong euphoria, itching/nausea, and pain relief with low sedation
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Based on general opioid patterns and limited analog data: tolerance can rise quickly with continuous exposure and decays over weeks. Estimates are approximate and carry low confidence.
Cross-Tolerances
Harm Reduction
drugs.wikiLofentanil is among the most potent opioids known; DrugBank describes it as slightly more potent than carfentanil, underscoring that microgram‑scale mismeasurement can be fatal. Volumetric dilution and analytical verification are essential if this substance is encountered; ordinary milligram scales are wholly inadequate. Opioid and other CNS depressant combinations (especially benzodiazepines and alcohol) markedly increase the risk of respiratory arrest. Fentanyl‑class agents can cause sudden chest wall/diaphragmatic rigidity (“wooden chest syndrome,” WCS), often within 1–3 minutes after rapid IV administration; bag‑mask ventilation may be ineffective until naloxone and/or neuromuscular blockade with advanced airway management are provided by clinicians. Because naloxone is shorter‑acting than many fentanyl analogs, re‑sedation (renarcotization) can occur; observation and repeated dosing or infusion may be necessary. Routine drug‑checking FTIR has a ~5% limit of detection and can miss trace high‑potency opioids; pairing with fentanyl test strips improves detection of fentanyl and some analogs but cannot identify which analog or quantify potency. Lofentanil shows meaningful κ‑opioid receptor activity in vitro, which may contribute to dysphoria and sedation at analgesic doses, narrowing the safety margin. Human pharmacokinetics for lofentanil are not established; avoid redosing based on subjective effects, and assume a prolonged and variable duration. Small but statistically significant QTc changes have been observed with fentanyl in clinical settings; while torsades is uncommon with fentanyl-class agents (in contrast to methadone), caution is warranted in patients with long‑QT risks or on QT‑prolonging drugs. Buprenorphine can precipitate acute withdrawal in people physically dependent on full μ‑agonists; initiation should be medically supervised. Even trace contamination with lofentanil can render a non‑opioid sample lethally potent; a negative fentanyl strip does not guarantee absence of other ultra‑potent analogs, and a positive result does not quantify dose.
References
Drugs.wiki References
- DrugBank – Lofentanil (DB09174) overview; potency note vs carfentanil; identifiers
- European J. Pharmacology 1992 – Pharmacological profiles of fentanyl analogs (lofentanil high affinity; not strictly μ‑selective)
- BMC Pharmacology 2006 – κ‑opioid receptor ligand profiles (lofentanil Ki≈8.2 nM; κ agonism)
- TripSit Wiki – Opioids page (RC fentanyls microgram risk; avoid CNS depressant combos)
- Wooden Chest Syndrome case/review – management and timing; naloxone vs duration
- Wooden Chest Syndrome review (mechanism, rapid rigidity with fentanyl/analogs)
- Case report: very‑low‑dose fentanyl causing WCS
- Drugchecking.community – FTIR ~5% limit of detection; pair with test strips
- Drugchecking.community – Fentanyl test strips resource (sensitivity, limitations)
- Fentanyl and QTc – ED prospective study (small, significant QTc prolongation)
- Opioid agents and arrhythmia – review (dose‑dependent QT effects for fentanyl‑class; far higher risk with methadone)
- Drugs‑Forum Wiki – Fentanyl (notes lofentanil slightly > carfentanil)
- PubChem – Lofentanil compound entry (identity)