levallorphan
Trade name: lorfan
Approved
Apr 30, 1956
Levallorphan (brand name Lorfan), is an opiate antagonist of morphine family. Levallorphan was formerly used in general anesthesia, mainly to reverse the respiratory depression produced by opioid analgesics and barbiturates used for induction of surgical anaesthesia whilst maintaining a degree of analgesia. Levallorphan was also used in combination with opioid analgesics to reduce their side effects, mainly in obstetrics. The combination of levallorphan with pethidine was used so frequently, a standardized formulation was made available, known as Pethilorfan, by Roche Products Ltd in later 1950s. Is known to be used for narcotic overdose. Levallorphan is similar to naloxone but differs from naloxone in that it also possesses some agonist properties. It acts as an antagonist and partial agonist of the mu opioid receptor (MOR). Levallorphan can produce severe mental reactions at sufficient doses including hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety, confusion, dizziness, disorientation, derealization, feelings of drunkenness, and bizarre, unusual, or disturbing dreams. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 1 marketing orgs
Timeline
Indications
Mechanism of action
- Mu opioid receptorANTAGONIST
OPRM antagonist
- Kappa opioid receptorPARTIAL AGONIST
OPRK1 partial agonist
Approval history
- approvedApr 30, 1956
Chemistry & pharmacology
SMILES
C=CCN1CC[C@]23CCCC[C@H]2[C@H]1Cc1ccc(O)cc13- Mol. weight
- 283.41 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Discontinued
Oral
No
Parenteral
Yes
Topical
No
Sources
- ChEMBLCHEMBL1254682 ↗
- WikipediaLevallorphan ↗
- NCATS353613BU4U ↗
- ChEMBLCHEMBL2062276 ↗
Also known as
- levallofano
- levallofano
- levallorphan
- levallorphan
- levallorphan
- levallorphan
- levallorphan
- levallorphan
- levallorphan
- levallorphan
- levallorphan
- lévallorphane
- lévallorphane
- levallorphan tartrate
- levallorphan tartrate
- levallorphan tartrate
- levallorphan tartrate
- levallorphanum
- levallorphanum
- levalorfano
- levalorfano
- lorfan
- lorfan
- lorfan
- lorfan
- lorfan
- naloxiphan
- naloxiphan
- naloxiphan
- naloxiphan
- naloxiphane tartrate
- naloxiphane tartrate