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Phentolamine mesilate

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Phentolamine mesilate Basic information

Product Name:
Phentolamine mesilate
Synonyms:
  • REGITIN
  • REGITIN MESYLATE
  • PHENTOLAMINE MESILATE
  • PHENTOLAMINE MESYLATE
  • PHENTOLAMINE METHANESULFONATE
  • PHENTOLAMINE METHANESULFONATE SALT
  • VASOMAX
  • m-(n-(2-imidazolin-2-ylmethyl)-p-toluidino)-phenomonomethanesulfonate(sal
CAS:
65-28-1
MF:
C18H23N3O4S
MW:
377.46
EINECS:
200-604-6
Product Categories:
  • Adrenoceptor
  • Erectile Dysfunction
  • ACTIVE PHARMACEUTICAL INGREDIENTS
  • Diagnostic
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • API
  • Pharmaceutical raw material
  • Regitine
  • pharmaceutical
  • 65-28-1
Mol File:
65-28-1.mol
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Phentolamine mesilate Chemical Properties

Melting point:
180-182 °C(lit.)
Density 
1.2256 (rough estimate)
refractive index 
1.6320 (estimate)
storage temp. 
2-8°C
solubility 
ethanol: 26 mg/mL
form 
powder
color 
white to off-white
Water Solubility 
50 mg/mL
Merck 
14,7264
Stability:
Aq. Solutions Cannot be Stored
InChI
InChI=1S/C17H19N3O.CH4O3S/c1-13-5-7-14(8-6-13)20(12-17-18-9-10-19-17)15-3-2-4-16(21)11-15;1-5(2,3)4/h2-8,11,21H,9-10,12H2,1H3,(H,18,19);1H3,(H,2,3,4)
InChIKey
OGIYDFVHFQEFKQ-UHFFFAOYSA-N
SMILES
N(CC1=NCCN1)(C1C=CC(C)=CC=1)C1C=CC=C(O)C=1.S(=O)(=O)(O)C
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Safety Information

Hazard Codes 
Xn,Xi
Risk Statements 
20/21/22-36/37/38
Safety Statements 
26-36
RIDADR 
3249
WGK Germany 
3
RTECS 
SL5430000
HazardClass 
6.1(b)
PackingGroup 
III
HS Code 
29332900
Toxicity
LDLo scu-rat: 275 mg/kg NIIRDN 6,667,82

MSDS

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Phentolamine mesilate Usage And Synthesis

Chemical Properties

Phentolamine mesylate is a white, odourless powder which is soluble in water and alcohol.

Uses

Phentolamine mesilate is an adrenergic blocking agent and antihypertensive. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of raynaud disease and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.

brand name

Regitine (Novartis) [Name previously used: Phentolamine Methanesulfonate.].

General Description

Phentolamine Mesylate belongs to the class of alpha adrenergic antagonist drugs. It is used in the treatment of pheochromocytoma-related hypertension, erectile dysfunction and in the diagnosis of pheochromocytoma and norepinephrine-related dermal necrosis.

Biochem/physiol Actions

α-Adrenergic receptor antagonist; peripheral vasodilator.

Clinical Use

Alpha-adrenoceptor blocker:
Hypertensive crisis

Safety Profile

Poison by intravenous and subcutaneous routes. Experimental reproductive effects. When heated to decomposition it emits toxic fumes of SOx and NOx.

Drug interactions

Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Antidepressants: additive hypotensive effect with MAOIs - avoid.
Antihypertensives: enhanced hypotensive effect.
Avanafil, vardenafil, sildenafil and tadalafil: enhanced hypotensive effect - avoid concomitant use.
Diuretics: enhanced hypotensive effect.
Linezolid: additive hypotensive effect.
Moxisylyte: possibly severe postural hypotension.

Metabolism

Phentolamine is extensively metabolised.
Only about 10-13% of an intravenous dose is excreted unchanged in the urine, and the fate of the remainder of the drug is unknown.

storage

Store at +4°C

Mode of action

Phentolamine Mesylate is the mesylate salt of a synthetic imidazoline with alpha-adrenergic antagonist activity. As a competitive alpha-adrenergic antagonist, phentolamine binds to alpha-1 and alpha-2 receptors, resulting in a decrease in peripheral vascular resistance and vasodilatation. This agent also may block 5-hydroxytryptamine (5-HT) receptors and stimulate release of histamine from mast cells.

Phentolamine mesilate Preparation Products And Raw materials

Raw materials

Phentolamine mesilateSupplier

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