pentazocine
Trade name: talwin
Approved
Jul 24, 1967
Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic (opioid analgesic) drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain. Pentazocine is sold under several brand names, such as Fortral, Sosegon, Talwin NX. Pentazocine acts as an agonist of κ-opioid receptors and as an antagonist of μ-opioid receptors. This compound may exist as one of two enantiomers, named (+)-pentazocine and (−)-pentazocine. Side effects are similar to those of morphine, but pentazocine, due to its action at the kappa opioid receptor is more likely to invoke psychotomimetic effects. High dose may cause high blood pressure or high heart rate. — NCATS
Clinical trial activity
7 trials · 10 clinical orgs · 6 marketing orgs
Earliest trial started Sep 1, 2005 (NCT00125931)
Timeline
1960s
- Jul 24, 1967
Hospira — Earliest FDA Approval
- Jul 24, 1967
Hospira — NDA Secondary Org
- Jul 24, 1967
Hospira — NDA Organization
- Feb 3, 1969
Sanofi-Aventis — NDA Secondary Org
1990s
- Jan 21, 1997
Watson Pharmaceuticals — Marketing Organization
2000s
- Mar 17, 2000
Sun Pharmaceuticals — Marketing Organization
- Jul 11, 2001
Lupin — Marketing Organization
- Aug 2, 2002
Gavis Pharmaceuticals — Marketing Organization
- Jan 1, 2005
Earliest Phase 2 Sponsor(trial)
2010s
- Jan 1, 2013
Earliest Phase 1 Sponsor(trial)
Indications
Approved for
Mechanism of action
- Sigma opioid receptorMODULATOR
SIGMAR1 modulator
Mixed agonist/antagonist
Combination products
talacen
with acetaminophen
talwin compoun
with acetylsalicylic acid
talwin nx
with naloxone
Approval history
- approvedPriority reviewJul 24, 1967
Chemistry & pharmacology
SMILES
C[C@H]1[C@H]2CC3=CC=C(O)C=C3[C@]1(C)CCN2CC=C(C)C- Mol. weight
- 285.4238 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral, Parenteral
- Availability
- Prescription Only
Oral
Yes
Parenteral
Yes
Topical
No
Sources
- WikipediaPentazocine ↗
- NCATSRP4A60D26L ↗
- ChEMBLCHEMBL3989509 ↗
- ChEMBLCHEMBL1200349 ↗
- ChEMBLCHEMBL560 ↗
- ChEMBLCHEMBL100116 ↗
- ChEMBLCHEMBL1200327 ↗
- ChEMBLCHEMBL3989510 ↗
Also known as
- cis-(+/-)-pentazocine
- dl-pentazocine
- fortral
- fortral
- pentazocin
- pentazocin
- pentazocin
- pentazocina
- pentazocina
- pentazocine
- pentazocine
- pentazocine
- pentazocine
- pentazocine
- pentazocine
- pentazocine
- pentazocine
- pentazocine
- pentazocine
- pentazocine hcl
- pentazocine hcl
- pentazocine hcl
- pentazocine hydrochloride
- pentazocine hydrochloride
- pentazocine hydrochloride
- pentazocine hydrochloride
- pentazocine lactate
- pentazocine lactate
- pentazocine lactate
- pentazocine lactate
- pentazocinum
- pentazocinum
- sosegon
- sosegon
- talwin
- talwin
- talwin
- win-20228
- win-20228
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05565274 | N/A | Oct 31, 2022 | Federal Medical Centre, Yenagoa |
| NCT04539249 | N/A | Oct 31, 2020 | Federal Medical Centre, Yenagoa |
| NCT02208596 | Phase 4 | Sep 1, 2014 | Zhengzhou University |
| NCT01872494 | Phase 4 | May 1, 2013 | People's Liberation Army of China |
| NCT02070718 | Phase 1 | Jan 1, 2013 | National Center for Advancing Translational Science (NCATS), National Center for Complementary and Integrative Health (NCCIH), National Institute on Aging (NIA), National Institutes of Health (NIH), University of Washington |
| NCT00431184 | Phase 2 | Jan 1, 2007 | Mclean Hospital, Stanley Medical Research Institute |
| NCT00125931 | Phase 2 | Sep 1, 2005 | Mclean Hospital, Stanley Medical Research Institute |
Organizations
Research & Development (10)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Federal Medical Centre, Yenagoa | Academic/Hospital | 2 | 2 | 1 | 2020 |
| Mclean Hospital | Academic/Hospital | 2 | 2 | 1 | 2005 |
| Stanley Medical Research Institute | Academic/Hospital | 2 | 0 | 1 | 2005 |
| National Center for Advancing Translational Science (NCATS) | Government | 1 | 0 | 1 | 2013 |
| National Center for Complementary and Integrative Health (NCCIH) | Government | 1 | 0 | 1 | 2013 |
| National Institute on Aging (NIA) | Government | 1 | 0 | 1 | 2013 |
| National Institutes of Health (NIH) | Government | 1 | 0 | 1 | 2013 |
| People's Liberation Army of China | Government | 1 | 1 | 1 | 2013 |
| University of Washington | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Zhengzhou University | Academic/Hospital | 1 | 1 | 1 | 2014 |
Marketing (7)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Gavis Pharmaceuticals | For profit | MKTG | Aug 2, 2002 |
| Hospira | For profit | NDA2 | Jul 24, 1967 |
| Hospira | For profit | NDA | Jul 24, 1967 |
| Lupin | For profit | MKTG | Jul 11, 2001 |
| Sanofi-Aventis | For profit | NDA2 | Feb 3, 1969 |
| Sun Pharmaceuticals | For profit | MKTG | Mar 17, 2000 |
| Watson Pharmaceuticals | For profit | MKTG | Jan 21, 1997 |