Historical Aspects of Nitrate Therapy

Berlin, R

doi:10.2165/00003495-198700334-00003

Cited by 20 publications

(23 citation statements)

References 5 publications

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“…Glyceryl trinitrate, or nitroglycerin, was first synthesized by Ascanio Sombrero in Turin, Italy. In 1847, he noted that “a very minute quantity put on the tongue produced a violent headache for several hours” (2,3). Three year earlier, the French chemist Antoine Balard synthesized amyl nitrite (2).…”

Section: Early History Of the Use Of Nitrates In Coronary Artery Diseasementioning

confidence: 99%

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The Role of Nitroglycerin and Other Nitrogen Oxides in Cardiovascular Therapeutics

Divakaran

Loscalzo

2017

Journal of the American College of Cardiology

142

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The use of nitroglycerin in the treatment of angina pectoris began not long after its original synthesis in 1847. Since then, the discovery of nitric oxide as a biological effector and better understanding of its roles in vasodilation, cell permeability, platelet function, inflammation, and other vascular processes have advanced our knowledge of the hemodynamic (mostly mediated through vasodilation of capacitance and conductance arteries) and non-hemodynamic effects of organic nitrate therapy, via both nitric oxide-dependent and independent mechanisms. Nitrates are rapidly absorbed from mucous membranes, the gastrointestinal tract, and the skin, and, thus, nitroglycerin is available in several preparations for delivery via several routes: oral tablets, sublingual tablets, buccal tablets, sublingual spray, transdermal ointment, and transdermal patch; it is also available in intravenous formulations. The organic nitrates are commonly used in the treatment of cardiovascular disease, but clinical data limit their use mostly to the treatment of angina. They are also used in the treatment of subsets of patients with heart failure and pulmonary hypertension. One major problem with the use of nitrates is the development of tolerance. Although several agents have been studied for use in the prevention of nitrate tolerance, none are currently recommended owing to a paucity of supportive clinical data. Only one method of preventing nitrate tolerance remains widely accepted: the use of a dosing strategy that provides an interval of no or low nitrate exposure during each 24-hour period. Nitric oxide’s important role in several cardiovascular disease mechanisms continues to drive research toward finding novel ways to affect both endogenous and exogenous sources of this key molecular mediator.

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Section: Early History Of the Use Of Nitrates In Coronary Artery Diseasementioning

confidence: 99%

“…Lauder Brunton, a Scottish physician and medical scientist, first described the clinical effectiveness of amyl nitrite (2,3,5). Brunton began caring for patients with angina pectoris as a house physician at the Edinburgh Royal Infirmary (5).…”

Section: Early History Of the Use Of Nitrates In Coronary Artery Diseasementioning

confidence: 99%

The Role of Nitroglycerin and Other Nitrogen Oxides in Cardiovascular Therapeutics

Divakaran

Loscalzo

2017

Journal of the American College of Cardiology

142

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“…12 Butyl, isobutyl, and other nitrite compounds continue to circumvent FDA regulation today and commonly are sold over the Internet, at adult bookstores, and in bars under the guise of incense or room-odorizing products. 10,13 Other pretenses for the sale of nitrites include labeling the product as video head cleaner, boot cleaner, or leather cleaner. Typically, these products are sold in small, amber glass ampoules containing 10-30 ml of the drug, at an average cost of $10-20 each.…”

Section: Historymentioning

confidence: 99%

“…Typically, these products are sold in small, amber glass ampoules containing 10-30 ml of the drug, at an average cost of $10-20 each. 10,13 Interestingly, amyl nitrite is used in emergency kits developed to treat cyanide poisoning. One report describes the theft of amyl nitrite capsules from a cyanide antidote kit, making them unavailable for an emergency situation.…”

Section: Historymentioning

confidence: 99%

Poppers: Epidemiology and Clinical Management of Inhaled Nitrite Abuse

et al. 2004

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Commonly referred to as "poppers," inhaled nitrites have a long history of abuse. Poppers are rapid-onset, short-acting potent vasodilators that produce a rush characterized by warm sensations and feelings of dizziness. Poppers sometimes are used to facilitate anal intercourse because of their actions on the anal sphincter. Epidemiologically, the frequent use of nitrites by men who have sex with men has led some experts to implicate these chemicals in the pathogenesis of Kaposi's sarcoma and acquired immunodeficiency syndrome. Controlled clinical trials to examine this potential correlation have not been conducted, and the use of nitrites simply may be a marker for other high-risk behaviors such as unprotected sex. Although regulated in the United States, many nitrite compounds and isomers are sold at various venues including bars, bookstores, and over the Internet. Adverse effects associated with these products vary from mild allergic reactions to life-threatening methemoglobinemia. The potential for drug-drug interactions and a propensity toward unsafe sex also exist. Clinicians should be familiar with the populations most likely to abuse these agents and with the clinical effects and management guidelines for acute ingestions.

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“…In general, pellet forms for sustained-release tablets are prepared using the spray method [ 11 -14 ] , which requires simple modifi cations to the manufacturing process and results in dispersion and constant absorption. Various brands of isosorbide 5-mononitrate have been marketed, and bioequivalence tests have been requested by the Korea Food and Drug Introduction ▼ Isosorbide dinitrate (CAS 87-33-2) and nitroglycerin are the most commonly prescribed nitrates for the prophylactic treatment of patients with angina pectoris [ 1 ] . Despite the usefulness of these compounds, their therapeutic potential is somewhat limited owing to a high fi rst-pass metabolism, active metabolites, and short elimination half-lives, which lead to frequent dosing, widely variable inter-subject response, and the development of tolerance [ 2 , 3 ] .…”

Section: In Vitro Dissolution and In Vivo Bioequivalence Evaluation Omentioning

confidence: 99%

In vitro Dissolution and in vivo Bioequivalence Evaluation of Two Brands of Isosorbide 5-mononitrate Sustained Release Tablets

Kim

Choi

Kam

et al. 2012

Arzneimittelforschung

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The purpose of the present study was to test a sustained release-tablet newly formulated with synthetic paraffin and compare its bioequivalence to that of the Imdur® Long-Acting tablet, based on the guidelines of the Korean Food and Drug Administration.Dissolution test was performed in 4 different dissolution media. A LC/MS/MS method of isosorbide 5-mononitrate in human plasma was validated. In vivo bioequivalence tests of the 2 isosorbide 5-mononitrate tablets were performed in both preprandial and postprandial states.A comparative dissolution test gave similar results for both tablets in all dissolution media tested: 40% dissolution in pH 1.2 at 2 h and 80% dissolution in pH 4.0, pH 6.8, or water at 10 h. In a bioequivalence study to compare 2 tablets, the mean total area under the curve (AUCt) and peak concentration (Cmax) in the fasted state were 8 476.0 ng · h/mL and 540.4 ng/mL, respectively, for the Imdur® Long Acting Tablet 60 mg, and 8 701.4 ng · h/mL and 564.2 ng/mL, respectively, for the test tablet. The mean AUCt and Cmax in the fed state were 8 793.5 ng · h/mL and 559.9 ng/mL, respectively, for the Imdur® Long-Acting tablet 60 mg, and 8 639.8 ng · h/mL and 617.9 ng/mL, respectively, for the test tablet. The 90% confidence intervals using log transformed data were within the acceptable range of 0.8 - 1.25.Based on these statistical analyses, we conclude that the test tablet is bioequivalent to the Imdur® Long-Acting tablet 60 mg in both the preprandial and postprandial states.

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Historical Aspects of Nitrate Therapy

Cited by 20 publications

References 5 publications

The Role of Nitroglycerin and Other Nitrogen Oxides in Cardiovascular Therapeutics

The Role of Nitroglycerin and Other Nitrogen Oxides in Cardiovascular Therapeutics

Poppers: Epidemiology and Clinical Management of Inhaled Nitrite Abuse

In vitro Dissolution and in vivo Bioequivalence Evaluation of Two Brands of Isosorbide 5-mononitrate Sustained Release Tablets

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