isoprenaline
Approved
Feb 19, 1948
Isoproterenol (trade names Medihaler-Iso and Isuprel) is a medication used for the treatment of bradycardia (slow heart rate), heart block, and rarely for asthma. Isoproterenol is a non-selective β adrenoreceptor agonist and TAAR1 agonist that is the isopropylaminomethyl analog of epinephrine. Isoprenaline's effects on the cardiovascular system (non-selective) relate to its actions on cardiac β1 receptors and β2 receptors on smooth muscle within the tunica media of arterioles. Isoprenaline has positive inotropic and chronotropic effects on the heart. β2 adrenoceptor stimulation in arteriolar smooth muscle induces vasodilation. Its inotropic and chronotropic effects elevate systolic blood pressure, while its vasodilatory effects tend to lower diastolic blood pressure. The overall effect is to decrease mean arterial pressure due to the β2 receptors' vasodilation. The adverse effects of isoprenaline are also related to the drug's cardiovascular effects. Isoprenaline can produce tachycardia (an elevated heart rate), which predisposes patients to cardiac arrhythmias. — NCATS
Clinical trial activity
15 trials · 18 clinical orgs · 39 marketing orgs
Earliest trial started Dec 1, 1996 (NCT00748059)
Timeline
1940s
- Feb 19, 1948
Earliest FDA Approval
- Feb 19, 1948
Sanofi-Aventis — Marketing Organization
- Feb 19, 1948
Sanofi-Aventis — NDA Secondary Org
1950s
- Mar 9, 1956
3M — NDA Secondary Org
- May 25, 1956
Bausch Health Companies — NDA Secondary Org
1970s
- Nov 15, 1974
Hospira — Marketing Organization
- Nov 15, 1974
Baxalta — Marketing Organization
- Nov 15, 1974
Baxter — Marketing Organization
- Jun 25, 1975
AbbVie — NDA Secondary Org
- Jan 6, 1976
International Medication — Marketing Organization
1980s
- Sep 10, 1985
Armour & Company — Marketing Organization
1990s
- Jan 1, 1996
Earliest Phase 1 Sponsor(trial)
2000s
- Jan 1, 2006
Earliest Phase 2 Sponsor(trial)
2010s
- Aug 2, 2017
Nexus Pharmaceuticals — Marketing Organization
- Jun 12, 2018
Cipla — Marketing Organization
- Jun 18, 2018
Amphastar Pharmaceuticals — Marketing Organization
- Oct 17, 2018
Amneal Pharmaceuticals — Marketing Organization
2020s
- Feb 9, 2021
Aurobindo Pharma — Marketing Organization
- Feb 9, 2021
Eugia Pharma — Marketing Organization
- Feb 16, 2021
Micro Labs Ltd India — Marketing Organization
- May 19, 2021
Amring Pharmaceticals — Marketing Organization
- Nov 19, 2021
Avet Lifesciences — Marketing Organization
- Sep 6, 2022
Mylan — Marketing Organization
- Sep 6, 2022
PHARMOBEDIENT — Marketing Organization
- Sep 20, 2022
STI Pharma, LLC — Marketing Organization
- Sep 20, 2022
PENN LIFE — Marketing Organization
- Oct 19, 2022
Sankyo — Marketing Organization
- Oct 19, 2022
Daiichi Sankyo — Marketing Organization
- Apr 14, 2023
Zydus Discovery DMCC — Marketing Organization
- Apr 26, 2023
Hikma — Marketing Organization
- Aug 6, 2024
Somerset Pharmaceuticals — Marketing Organization
- Oct 3, 2024
Gland Pharma Ltd — Marketing Organization
- Dec 10, 2025
Deva Holding A.S. — Marketing Organization
- May 18, 2026
Aspiro — Marketing Organization
Indications
Approved for
Studied for
- Atrial Fibrillation · Phase 2
- Autonomic Nervous System Diseases · Phase 1
- Dopamine beta-Hydroxylase · Phase 1
- Healthy Volunteers · Phase 1
- Hematuria · Phase 2/Phase 3
- Hypotension, Orthostatic · Phase 1
- Kidney Calculi · Phase 2/Phase 3
- Lipoma · Phase 1/Phase 2
- Neoplasms · Phase 2/Phase 3
- Obesity · Early Phase 1
- Orthostatic Intolerance · Phase 1
- Out-of-Hospital Cardiac Arrest · Phase 4
- Ureteroscopy · Phase 2
- Vasodilation · Early Phase 1
Mechanism of action
- Adrenergic receptor betaAGONIST
Adrenergic receptor beta agonist
Combination products
duo-medihaler
with phenylephrine
mucomyst w/ isoproterenol
with acetylcysteine
Approval history
- approvedFeb 19, 1948
Chemistry & pharmacology
SMILES
CC(C)NCC(O)c1ccc(O)c(O)c1.CC(C)NCC(O)c1ccc(O)c(O)c1.O.O.O=S(=O)(O)O- Mol. weight
- 556.63 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Discontinued
Oral
No
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL3989521 ↗
- WikipediaIsoprenaline ↗
- NCATSL628TT009W ↗
- ChEMBLCHEMBL1160723 ↗
- ChEMBLCHEMBL1200447 ↗
- ChEMBLCHEMBL1711 ↗
- ChEMBLCHEMBL434 ↗
Also known as
- 1-(3,4-dihydroxyphenyl)-2-isopropylaminoethanol
- 1-(3,4-dihydroxyphenyl)-2-isopropylaminoethanol
- 1-(3,4-dihydroxyphenyl)-2-(isopropylamino)ethanol
- 1-(3,4-dihydroxyphenyl)-2-(isopropylamino)ethanol
- 3,4-dihydroxy-alpha-[(isopropylamino)methyl]benzyl alcohol
- 3,4-dihydroxy-alpha-[(isopropylamino)methyl]benzyl alcohol
- aerolone
- aerolone
- alpha-(isopropylaminomethyl)protocatechuyl alcohol
- alpha-(isopropylaminomethyl)protocatechuyl alcohol
- dl-isoprenaline hcl
- dl-isoprenaline hydrochloride
- dl-isoproterenol
- imuprel
- isoprenalin
- isoprenalina
- isoprenalina
- isoprenaline
- isoprenaline
- isoprenaline
- isoprenaline
- isoprenaline
- isoprenaline
- isoprenaline
- isoprenaline
- (+-)-isoprenaline
- (+-)-isoprenaline
- (±)-isoprenaline
- (±)-isoprenaline
- isoprenaline sulfate
- isoprenalinum
- isoprenalinum
- isopropylarterenol hcl
- isopropylarterenol hcl
- isopropylarterenol sulfate
- isopropylarterenol sulfate
- isopropyl noradrenaline
- isopropyl noradrenaline
- isoproterenol
- isoproterenol
- isoproterenol
- isoproterenol
- isoproterenol
- isoproterenol
- (+-)-isoproterenol
- (+-)-isoproterenol
- (±)-isoproterenol
- (±)-isoproterenol
- isoproterenol hcl
- isoproterenol hcl
- isoproterenol hcl
- isoproterenol hydrochloride
- isoproterenol hydrochloride
- isoproterenol hydrochloride
- isoproterenol hydrochloride
- isoproterenol sulfate
- isoproterenol sulfate
- isoproterenol sulfate
- isoproterenol sulfate
- isuprel
- isuprel
- isuprel
- l-isoprenaline hcl
- l-isoprenaline hcl
- medihaler-iso
- medihaler-iso
- n-isopropyl-beta-dihydroxyphenyl-beta-hydroxyethylamine
- n-isopropyl-beta-dihydroxyphenyl-beta-hydroxyethylamine
- n-isopropylnoradrenaline
- n-isopropylnoradrenaline
- n-isopropylnorepinephrine
- n-isopropylnorepinephrine
- n-isopropyl-β-dihydroxyphenyl-β-hydroxyethylamine
- n-isopropyl-β-dihydroxyphenyl-β-hydroxyethylamine
- norisodrine
- norisodrine
- norisodrine aerotrol
- norisodrine aerotrol
- vapo-iso
- vapo-iso
- α-(isopropylaminomethyl)protocatechuyl alcohol
- α-(isopropylaminomethyl)protocatechuyl alcohol
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06473116 | Phase 4 | Mar 31, 2025 | University of Southern Denmark |
| NCT05219799 | Early Phase 1 (Phase 1) | Feb 28, 2023 | University of Missouri |
| NCT03019081 | N/A | Jan 1, 2017 | Brain & Behavior Research Foundation, Laureate Institute for Brain Research |
| NCT02726620 | N/A | Jan 1, 2017 | Utrecht University, Vanderbilt University |
| NCT02725060 | N/A | Feb 1, 2016 | University of Oklahoma, Vanderbilt University |
| NCT02615119 | N/A | Oct 1, 2015 | Laureate Institute for Brain Research, National Institute of Mental Health (NIMH) |
| NCT02286934 | Phase 1 | Sep 1, 2014 | National Institute of Food and Drug Safety Evaluation, Korea, Seoul National University |
| NCT02524145 | N/A | Mar 1, 2013 | The University of Texas, Dallas |
| NCT03032965 | Phase 2 | Oct 1, 2011 | University of Michigan |
| NCT01377636 | N/A | Aug 1, 2009 | New York University |
| NCT00624416 | Phase 1/Phase 2 (Phase 2) | Oct 1, 2007 | Neothetics, Inc, University of Vermont |
| NCT00428428 | Phase 2/Phase 3 (Phase 3) | Feb 1, 2007 | Fredericia Hospital, Fredericia & Kolding Hospitals |
| NCT00323843 | Phase 2 | Jun 1, 2006 | Fredericia Hospital |
| NCT00226551 | N/A | Aug 1, 1999 | Hebrew University |
| NCT00748059 | Phase 1 | Dec 1, 1996 | Vanderbilt University |
Organizations
Research & Development (18)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Vanderbilt University | Academic/Hospital | 3 | 3 | 2 | 1996 |
| Fredericia Hospital | Academic/Hospital | 2 | 2 | 2 | 2006 |
| Laureate Institute for Brain Research | Academic/Hospital | 2 | 2 | 1 | 2015 |
| Brain & Behavior Research Foundation | Academic/Hospital | 1 | 0 | 1 | 2017 |
| Fredericia & Kolding Hospitals | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Hebrew University | Academic/Hospital | 1 | 1 | 1 | 1999 |
| National Institute of Food and Drug Safety Evaluation, Korea | Academic/Hospital | 1 | 0 | 1 | 2014 |
| National Institute of Mental Health (NIMH) | Government | 1 | 0 | 1 | 2015 |
| Neothetics, Inc | For profit | 1 | 0 | 1 | 2007 |
| New York University | Academic/Hospital | 1 | 1 | 1 | 2009 |
| Seoul National University | Academic/Hospital | 1 | 1 | 1 | 2014 |
| The University of Texas, Dallas | Academic/Hospital | 1 | 1 | 1 | 2013 |
| University of Michigan | Academic/Hospital | 1 | 1 | 1 | 2011 |
| University of Missouri | Academic/Hospital | 1 | 1 | 1 | 2023 |
| University of Oklahoma | Academic/Hospital | 1 | 0 | 1 | 2016 |
| University of Southern Denmark | Academic/Hospital | 1 | 1 | 1 | 2025 |
| University of Vermont | Academic/Hospital | 1 | 1 | 1 | 2007 |
| Utrecht University | Academic/Hospital | 1 | 0 | 1 | 2017 |
Marketing (42)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| 3M | For profit | NDA2 | Mar 9, 1956 |
| AbbVie | For profit | NDA2 | Jun 25, 1975 |
| Abbott | For profit | NDA2 | — |
| Abraxis | For profit | MKTG | — |
| Alpharma | For profit | MKTG | — |
| Amneal Pharmaceuticals | For profit | MKTG | Oct 17, 2018 |
| Amneal Pharmaceuticals | For profit | SYN | Oct 17, 2018 |
| Amphastar Pharmaceuticals | For profit | MKTG | Jun 18, 2018 |
| Amring Pharmaceticals | For profit | MKTG | May 19, 2021 |
| Armour & Company | For profit | MKTG | Sep 10, 1985 |
| Aspiro | For profit | MKTG | May 18, 2026 |
| Aurobindo Pharma | For profit | MKTG | Feb 9, 2021 |
| Avet Lifesciences | For profit | MKTG | Nov 19, 2021 |
| Bausch Health Companies | For profit | NDA2 | May 25, 1956 |
| Baxalta | For profit | MKTG | Nov 15, 1974 |
| Baxter | For profit | MKTG | Nov 15, 1974 |
| Cipla | For profit | MKTG | Jun 12, 2018 |
| Daiichi Sankyo | For profit | MKTG | Oct 19, 2022 |
| Deva Holding A.S. | For profit | MKTG | Dec 10, 2025 |
| Dey | For profit | MKTG | — |
| Eli Lilly | For profit | NDA2 | — |
| Eugia Pharma | For profit | MKTG | Feb 9, 2021 |
| Fisons | For profit | NDA2 | — |
| Gland Pharma Ltd | For profit | MKTG | Oct 3, 2024 |
| Hikma | For profit | MKTG | Apr 26, 2023 |
| Hospira | For profit | MKTG | Nov 15, 1974 |
| International Medication | For profit | MKTG | Jan 6, 1976 |
| Mead Johnson | For profit | NDA2 | — |
| Micro Labs Ltd India | For profit | MKTG | Feb 16, 2021 |
| Mylan | For profit | MKTG | Sep 6, 2022 |
| Nexus Pharmaceuticals | For profit | MKTG | Aug 2, 2017 |
| Nexus Pharmaceuticals | For profit | SYN | Aug 2, 2017 |
| PENN LIFE | For profit | MKTG | Sep 20, 2022 |
| PHARMOBEDIENT | For profit | MKTG | Sep 6, 2022 |
| Parke-Davis | For profit | MKTG | — |
| STI Pharma, LLC | For profit | MKTG | Sep 20, 2022 |
| Sankyo | For profit | MKTG | Oct 19, 2022 |
| Sanofi-Aventis | For profit | MKTG | Feb 19, 1948 |
| Sanofi-Aventis | For profit | NDA2 | Feb 19, 1948 |
| Smith, Kline & French | For profit | NDA | — |
| Somerset Pharmaceuticals | For profit | MKTG | Aug 6, 2024 |
| Zydus Discovery DMCC | For profit | MKTG | Apr 14, 2023 |