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Phentolamine

Generic Name
Phentolamine
Brand Names
Oraverse
Drug Type
Small Molecule
Chemical Formula
C17H19N3O
CAS Number
50-60-2
Unique Ingredient Identifier
Z468598HBV
Background

Phentolamine is a reversible, non-selective alpha-adrenergic blocker that induces vasodilation. While initially introduced to the market for the treatment of hypertension, this clinical use was halted due to cardiovascular and gastrointestinal adverse effects with the prolonged use of large oral doses of phentolamine. It has several therapeutic uses, including the treatment of hypertensive episodes, prevention of norepinephrine-induced extravasation, diagnosis of pheochromocytoma, reversal of soft-tissue anesthesia, and treatment of pharmacologically-induced mydriasis. Phentolamine is administered intravenously, intramuscularly, submucosally, and topically.

Indication

1.用于预防和治疗嗜铬细胞瘤所致的高血压发作,包括手术切除时出现的阵发性高血压,也可根据血压对本品的反应用于协助诊断嗜铬细胞瘤;

2.治疗左心衰竭;

3.治疗去甲肾上腺素、去氧肾上腺素、间羟胺等静脉给药外溢,用于防止皮肤坏死;

4.临床还用于治疗男性勃起功能障碍(ED)。最新研究表明,本品与罂粟碱、前列地尔三联用药,可降低引起平滑肌收缩的交感神经张力,使阴茎动脉平滑肌松弛,增加阴茎动脉血流,有利勃起。

Associated Conditions
Mydriasis, Necrosis caused by norepinephrine extravasation, Pheochromocytoma, Sloughing Skin, Soft Tissue Anesthesia (Numbness), Hypertensive episodes

Safety and Efficacy of Ophthalmic Phentolamine Mesylate to Reverse Pharmacologically Induced Mydriasis

Phase 2
Completed
Conditions
Mydriasis
Dilation
Interventions
Other: Phentolamine Mesylate Ophthalmic Solution Vehicle (Placebo)
First Posted Date
2019-07-18
Last Posted Date
2023-08-29
Lead Sponsor
Ocuphire Pharma, Inc.
Target Recruit Count
32
Registration Number
NCT04024891
Locations
🇺🇸

West Bay Eye Associates, Warwick, Rhode Island, United States

🇺🇸

Kannar Eye Care, Pittsburg, Kansas, United States

🇺🇸

Athens Eye Care, Athens, Ohio, United States

and more 1 locations

Single Dose Study of Phentolamine Mesylate Eye Drops in Patients With Severe Night Vision Disturbances

Phase 2
Completed
Conditions
Disturbance; Vision, Loss
Decrease in Night Vision
Interventions
Other: Phentolamine Mesylate Ophthalmic Solution Vehicle (Placebo)
First Posted Date
2019-07-02
Last Posted Date
2024-02-15
Lead Sponsor
Ocuphire Pharma, Inc.
Target Recruit Count
24
Registration Number
NCT04004507
Locations
🇺🇸

Ophthalmic Consultants of Long Island, NY, Lynbrook, New York, United States

Safety and Efficacy of Ophthalmic Phentolamine Mesylate in Glaucoma

Phase 2
Completed
Conditions
Open Angle Glaucoma
Ocular Hypertension
Interventions
Other: Phentolamine Mesylate Ophthalmic Solution Vehicle (Placebo)
First Posted Date
2019-05-23
Last Posted Date
2023-09-13
Lead Sponsor
Ocuphire Pharma, Inc.
Target Recruit Count
39
Registration Number
NCT03960866
Locations
🇺🇸

Clayton Eye Clinical Research, Morrow, Georgia, United States

🇺🇸

Abrams Eye Center, Cleveland, Ohio, United States

🇺🇸

University of Michigan Kellogg Eye Center, Ann Arbor, Michigan, United States

and more 2 locations

Phentolamine Mesylate as a Reversal of Local Anesthesics

Not Applicable
Completed
Conditions
Anesthesia, Local
Interventions
First Posted Date
2018-11-14
Last Posted Date
2018-11-14
Lead Sponsor
León Formación
Target Recruit Count
90
Registration Number
NCT03740386

Role of Sympathetic Vasoconstriction on Insulin-Mediated Microvascular Recruitment and Glucose Uptake in Obesity

Phase 1
Active, not recruiting
Conditions
Healthy
Insulin Resistance
Obesity
Interventions
First Posted Date
2017-10-23
Last Posted Date
2025-05-13
Lead Sponsor
Vanderbilt University Medical Center
Target Recruit Count
36
Registration Number
NCT03318094
Locations
🇺🇸

Autonomic Dysfunction Center, Nashville, Tennessee, United States

A Study of the Pharmacokinetic and Pharmacodynamic Responses in Healthy and Altered Human Cardiovascular Systems

Phase 1
Terminated
Conditions
Drug-Related Side Effects and Adverse Reactions
Cardiovascular System Disease
Interventions
First Posted Date
2017-04-04
Last Posted Date
2021-03-22
Lead Sponsor
Cambridge University Hospitals NHS Foundation Trust
Target Recruit Count
18
Registration Number
NCT03098680
Locations
🇬🇧

Addenbrooke's Hospital, Cambridge, Cambridgeshire, United Kingdom

Adrenergic System in Islet Transplantation

Early Phase 1
Active, not recruiting
Conditions
Type1diabetes
Hypoglycemia
Hypoglycemia Unawareness
Islet Cell Transplantation
Interventions
First Posted Date
2017-03-15
Last Posted Date
2025-02-13
Lead Sponsor
University of Pennsylvania
Target Recruit Count
11
Registration Number
NCT03079921
Locations
🇺🇸

University of Pennsylvania - Institute for Diabetes, Obesity and Metabolism, Philadelphia, Pennsylvania, United States

Reversing the Effects of 0.5% Bupivacaine

Phase 4
Completed
Conditions
Anesthesia, Local
Interventions
First Posted Date
2016-12-16
Last Posted Date
2020-01-29
Lead Sponsor
Dalhousie University
Target Recruit Count
44
Registration Number
NCT02995291
Locations
🇨🇦

Dalhousie University Faculty of Dentistry, Halifax, Nova Scotia, Canada

Reversing the Effects of 2% Lidocaine

Not Applicable
Completed
Conditions
Soft Tissue Anaesthesia
Interventions
First Posted Date
2016-08-10
Last Posted Date
2016-10-14
Lead Sponsor
Dalhousie University
Target Recruit Count
38
Registration Number
NCT02861378
Locations
🇨🇦

Dalhousie University Faculty of Dentistry, Halifax, Nova Scotia, Canada

The Safety and Efficacy of Phentolamine Mesylate Ophthalmic Solution in Subjects With Severe Night Vision Disturbances

Phase 2
Completed
Conditions
Decrease in Night Vision
Disturbance; Vision, Loss
Night Vision Complaints
Interventions
First Posted Date
2012-10-10
Last Posted Date
2019-08-01
Lead Sponsor
Ocuphire Pharma, Inc.
Target Recruit Count
60
Registration Number
NCT01703559
Locations
🇺🇸

Celerion, Phoenix, Arizona, United States

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