levallorphan

Trade name: lorfan

Small moleculeapproved

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

Phase 1
0
Phase 2
0
Phase 3
0
Phase 4
0

Timeline

1950s

  1. Dec 13, 1955

    Roche — First NDA Organization

  2. Dec 13, 1955

    Roche — NDA Organization

  3. Apr 30, 1956

    Earliest FDA Approval

  4. Apr 30, 1956

    Roche — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedApr 30, 1956

Chemistry & pharmacology

Loading structure…

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

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

Organizations

Marketing (2)

OrganizationOrg typeRelationshipDate
RocheFor profitNDADec 13, 1955
RocheFor profitMKTGApr 30, 1956