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PHENTOLAMINE MESYLATE

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Overview

What is PHENTOLAMINE MESYLATE?

Phentolamine Mesylate for Injection, USP is an antihypertensive, available in vials for intravenous and intramuscular administration. Each vial contains phentolamine mesylate, USP, 5 mg, and mannitol USP, 25 mg, in sterile, lyophilized form.

Phentolamine Mesylate, USP is 4,5-dihydro-2-[N-(-hydroxyphenyl)-N-(-methylphenyl) amino methyl]-1- imidazole 1:1 methanesulfonate, and its structural formula is

Phentolamine mesylate, USP is a white or off-white, odorless crystalline powder with a molecular weight of 377.46. Its solutions are acid to litmus. It is freely soluble in water and in alcohol, and slightly soluble in chloroform. It melts at about 178°C.



What does PHENTOLAMINE MESYLATE look like?



What are the available doses of PHENTOLAMINE MESYLATE?

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What should I talk to my health care provider before I take PHENTOLAMINE MESYLATE?

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How should I use PHENTOLAMINE MESYLATE?

Phentolamine Mesylate for Injection, USP is indicated for the prevention or control of hypertensive episodes that may occur in a patient with pheochromocytoma as a result of stress or manipulation during preoperative preparation and surgical excision.

Phentolamine Mesylate for Injection, USP is indicated for the prevention or treatment of dermal necrosis and sloughing following intravenous administration or extravasation of norepinephrine.

Phentolamine Mesylate for Injection, USP is also indicated for the diagnosis of pheochromocytoma by the Phentolamine Mesylate for Injection, USP blocking test.

The reconstituted solution should be used upon preparation and should not be stored.Note:


What interacts with PHENTOLAMINE MESYLATE?

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What are the warnings of PHENTOLAMINE MESYLATE?

Azathioprine has been reported to cause temporary depression in spermatogenesis and reduction in sperm viability and sperm count in mice at doses 10 times the human therapeutic dose; a reduced percentage of fertile matings occurred when animals received 5 mg/kg.  

Myocardial infarction, cerebrovascular spasm, and cerebrovascular occlusion have been reported to occur following the administration of Phentolamine Mesylate for Injection, USP, usually in association with marked hypotensive episodes.

For screening tests in patients with hypertension, the generally available urinary assay of catecholamines or other biochemical assays have largely replaced the Phentolamine Mesylate for Injection, USP and other pharmacological tests for reasons of accuracy and safety. None of the chemical or pharmacological tests is infallible in the diagnosis of pheochromocytoma. The Phentolamine Mesylate for Injection, USP blocking test is not the procedure of choice and should be reserved for cases in which additional confirmatory evidence is necessary and the relative risks involved in conducting the test have been considered.


What are the precautions of PHENTOLAMINE MESYLATE?

General

Tachycardia and cardiac arrhythmias may occur with the use of Phentolamine Mesylate for Injection, USP or other alpha-adrenergic blocking agents. When possible, administration of cardiac glycosides should be deferred until cardiac rhythm returns to normal.

Drug Interactions

See , , .

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term carcinogenicity studies, mutagenicity studies, and fertility studies have not been conducted with Phentolamine Mesylate for Injection, USP .

Pregnancy Category C

Administration of Phentolamine Mesylate for Injection, USP to pregnant rats and mice at oral doses 24-30 times the usual daily human dose (based on a 60-kg human) resulted in slightly decreased growth and slight skeletal immaturity of the fetuses. Immaturity was manifested by increased incidence of incomplete or unossified calcanei and phalangeal nuclei of the hind limb and of incompletely ossified sternebrae. At oral doses 60 times the usual daily human dose (based on a 60-kg human), a slightly lower rate of implantation was found in the rat. Phentolamine Mesylate for Injection, USP did not affect embryonic or fetal development in the rabbit at oral doses 20 times the usual daily human dose (based on a 60-kg human). No teratogenic or embryo toxic effects were observed in the rat, mouse, or rabbit studies.

There are no adequate and well-controlled studies in pregnant women. Phentolamine Mesylate for Injection, USP should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Phentolamine Mesylate for Injection, USP, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

See


What are the side effects of PHENTOLAMINE MESYLATE?

Acute and prolonged hypotensive episodes, tachycardia, and cardiac arrhythmias have been reported. In addition, weakness, dizziness, flushing, orthostatic hypotension, nasal stuffiness, nausea, vomiting, and diarrhea may occur.


What should I look out for while using PHENTOLAMINE MESYLATE?

Myocardial infarction, history of myocardial infarction, coronary insufficiency, angina or other evidence suggestive of coronary artery disease; hypersensitivity to phentolamine or related compounds.

Myocardial infarction, cerebrovascular spasm, and cerebrovascular occlusion have been reported to occur following the administration of Phentolamine Mesylate for Injection, USP, usually in association with marked hypotensive episodes.

For screening tests in patients with hypertension, the generally available urinary assay of catecholamines or other biochemical assays have largely replaced the Phentolamine Mesylate for Injection, USP and other pharmacological tests for reasons of accuracy and safety. None of the chemical or pharmacological tests is infallible in the diagnosis of pheochromocytoma. The Phentolamine Mesylate for Injection, USP blocking test is not the procedure of choice and should be reserved for cases in which additional confirmatory evidence is necessary and the relative risks involved in conducting the test have been considered.


What might happen if I take too much PHENTOLAMINE MESYLATE?


How should I store and handle PHENTOLAMINE MESYLATE?

Store at 20º to 25ºC (68º to 77ºF); excursions permitted to 15º to 30ºC (59º to 86ºF) [see USP Controlled Room Temperature].Vials—The reconstituted solution should be used upon preparation and should not be stored. Store at 20° to 25°C (68° - 77°F) with excursions between 15° to 30°C (59° to 86°F) [USP Controlled Room Temperature]You can also call Precision Dose Inc. at 1-800-397-9228 or visit www.precisiondose.com. Distributed by: Precision Dose, Inc. South Beloit, IL 61080Revised: 10/2017Vials—The reconstituted solution should be used upon preparation and should not be stored. Store at 20° to 25°C (68° - 77°F) with excursions between 15° to 30°C (59° to 86°F) [USP Controlled Room Temperature]You can also call Precision Dose Inc. at 1-800-397-9228 or visit www.precisiondose.com. Distributed by: Precision Dose, Inc. South Beloit, IL 61080Revised: 10/2017Vials—The reconstituted solution should be used upon preparation and should not be stored. Store at 20° to 25°C (68° - 77°F) with excursions between 15° to 30°C (59° to 86°F) [USP Controlled Room Temperature]You can also call Precision Dose Inc. at 1-800-397-9228 or visit www.precisiondose.com. Distributed by: Precision Dose, Inc. South Beloit, IL 61080Revised: 10/2017Vials—The reconstituted solution should be used upon preparation and should not be stored. Store at 20° to 25°C (68° - 77°F) with excursions between 15° to 30°C (59° to 86°F) [USP Controlled Room Temperature]You can also call Precision Dose Inc. at 1-800-397-9228 or visit www.precisiondose.com. Distributed by: Precision Dose, Inc. South Beloit, IL 61080Revised: 10/2017Vials—The reconstituted solution should be used upon preparation and should not be stored. Store at 20° to 25°C (68° - 77°F) with excursions between 15° to 30°C (59° to 86°F) [USP Controlled Room Temperature]You can also call Precision Dose Inc. at 1-800-397-9228 or visit www.precisiondose.com. Distributed by: Precision Dose, Inc. South Beloit, IL 61080Revised: 10/2017Vials—The reconstituted solution should be used upon preparation and should not be stored. Store at 20° to 25°C (68° - 77°F) with excursions between 15° to 30°C (59° to 86°F) [USP Controlled Room Temperature]You can also call Precision Dose Inc. at 1-800-397-9228 or visit www.precisiondose.com. Distributed by: Precision Dose, Inc. South Beloit, IL 61080Revised: 10/2017


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Clinical Information

Chemical Structure

No Image found
Clinical Pharmacology

Phentolamine Mesylate for Injection, USP produces an alpha-adrenergic block of relatively short duration. It also has direct, but less marked, positive inotropic and chronotropic effects on cardiac muscle and vasodilator effects on vascular smooth muscle.

Phentolamine Mesylate for Injection, USP has a half-life in the blood of 19 minutes following intravenous administration. Approximately 13% of a single intravenous dose appears in the urine as unchanged drug.

Non-Clinical Toxicology
Myocardial infarction, history of myocardial infarction, coronary insufficiency, angina or other evidence suggestive of coronary artery disease; hypersensitivity to phentolamine or related compounds.

Myocardial infarction, cerebrovascular spasm, and cerebrovascular occlusion have been reported to occur following the administration of Phentolamine Mesylate for Injection, USP, usually in association with marked hypotensive episodes.

For screening tests in patients with hypertension, the generally available urinary assay of catecholamines or other biochemical assays have largely replaced the Phentolamine Mesylate for Injection, USP and other pharmacological tests for reasons of accuracy and safety. None of the chemical or pharmacological tests is infallible in the diagnosis of pheochromocytoma. The Phentolamine Mesylate for Injection, USP blocking test is not the procedure of choice and should be reserved for cases in which additional confirmatory evidence is necessary and the relative risks involved in conducting the test have been considered.

See , , .

Tachycardia and cardiac arrhythmias may occur with the use of Phentolamine Mesylate for Injection, USP or other alpha-adrenergic blocking agents. When possible, administration of cardiac glycosides should be deferred until cardiac rhythm returns to normal.

Acute and prolonged hypotensive episodes, tachycardia, and cardiac arrhythmias have been reported. In addition, weakness, dizziness, flushing, orthostatic hypotension, nasal stuffiness, nausea, vomiting, and diarrhea may occur.

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72
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Interactions

Interactions

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