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Phentolamine
Oraverse (phentolamine) is a small molecule pharmaceutical. Phentolamine was first approved as Regitine on 1982-01-01. It is used to treat extravasation of diagnostic and therapeutic materials, malignant hypertension, and necrosis in the USA. The pharmaceutical is active against alpha-1D adrenergic receptor, alpha-1B adrenergic receptor, and alpha-1A adrenergic receptor. In addition, it is known to target alpha-2A adrenergic receptor, alpha-2C adrenergic receptor, and alpha-2B adrenergic receptor.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
cardiovascular diseasesD002318
signs and symptoms pathological conditionsD013568
wounds and injuriesD014947
Trade Name
FDA
EMA
Oraverse (generic drugs available since 1998-03-11, discontinued: Regitine)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Phentolamine mesylate
Tradename
Company
Number
Date
Products
ORAVERSESeptodontN-022159 RX2008-05-09
1 products, RLD, RS
Show 1 discontinued
Labels
FDA
EMA
Brand Name
Status
Last Update
oraverseNew Drug Application2018-12-05
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
extravasation of diagnostic and therapeutic materials—D005119—
malignant hypertensionEFO_1001031D006974—
necrosis—D009336—
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent
Expires
Flag
FDA Information
Phentolamine Mesylate, Oraverse, Septodont Holding
75692302023-10-17U-967
72296302023-07-31DP
75757572023-07-31DP
ATC Codes
C: Cardiovascular system drugs
— C04: Peripheral vasodilators
— C04A: Peripheral vasodilators
— C04AB: Imidazoline derivatives, peripheral vasodilators
— C04AB01: Phentolamine
V: Various drug classes in atc
— V03: All other therapeutic products
— V03A: All other therapeutic products
— V03AB: Antidotes
— V03AB36: Phentolamine
HCPCS
Code
Description
J2760
Injection, phentolamine mesylate, up to 5 mg
Clinical
Indications Phases 4
No data
Indications Phases 3
No data
Indications Phases 2
No data
Indications Phases 1
No data
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common namePHENTOLAMINE
INNphentolamine
Description
Phentolamine is a substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension. It has a role as an alpha-adrenergic antagonist and a vasodilator agent. It is a member of imidazoles, a member of phenols, a tertiary amino compound and a substituted aniline.
Classification
Small molecule
Drug class—
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
Cc1ccc(N(CC2=NCCN2)c2cccc(O)c2)cc1
Identifiers
PDB—
CAS-ID50-60-2
RxCUI8153
ChEMBL IDCHEMBL597
ChEBI ID8081
PubChem CID5775
DrugBankDB00692
UNII IDZ468598HBV (ChemIDplus, GSRS)
Target
Agency Approved
ADRA1D
ADRA1D
ADRA1B
ADRA1B
ADRA1A
ADRA1A
Organism
Homo sapiens
Gene name
ADRA1D
Gene synonyms
ADRA1A
NCBI Gene ID
146
Protein name
alpha-1D adrenergic receptor
Protein synonyms
adrenergic, alpha -1D-, receptor, adrenergic, alpha-1A-, receptor, Alpha-1A adrenergic receptor, Alpha-1D adrenoceptor, Alpha-1D adrenoreceptor, Alpha-adrenergic receptor 1a
Uniprot ID
Q9NPY0
Mouse ortholog
Adra1d (11550)
alpha-1D adrenergic receptor (P97714)
Alternate
ADRA2A
ADRA2A
ADRA2C
ADRA2C
ADRA2B
ADRA2B
Organism
Homo sapiens
Gene name
ADRA2A
Gene synonyms
ADRA2R, ADRAR
NCBI Gene ID
150
Protein name
alpha-2A adrenergic receptor
Protein synonyms
adrenergic, alpha-2A-, receptor, Alpha-2 adrenergic receptor subtype C10, alpha-2-adrenergic receptor, platelet type, Alpha-2A adrenoceptor, Alpha-2A adrenoreceptor, Alpha-2AAR, alpha-2AAR subtype C10
Uniprot ID
Q9BZK1
Mouse ortholog
Adra2a (11551)
alpha-2A adrenergic receptor (Q3URE6)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
Mock data
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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1 adverse events reported
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