madman
Super Moderator
ABSTRACT
Yohimbine is an indole alkaloid from the leaves and bark of the Pausinystalia johimbe tree that has acquired an enviable reputation in treating erectile dysfunction. This report presents four simultaneous severe poisoning/death cases caused by yohimbine. The test samples comprised the venous blood of four middle-aged men (aged 47–65) who were suspected of poisoning; one of the men died due to ineffective rescue. Ethanol concentration determination and toxicological routine screening were performed using gas chromatography with flame ionization detection (GC-FID) and liquid chromatography-tandem mass spectrometry (LC-MS/MS). A specific LC-MS/MS method was developed to quantify yohimbine, which showed concentrations of 459, 249, and 301 ng/mL in three poisoned blood samples and concentrations as high as 5631 ng/mL in the deceased. Moreover, the deceased’s autopsy ruled out death from trauma and previous illness, and no other common toxic components were detected in his blood. Therefore, yohimbine poisoning appears to be the most likely cause of death. As a type of alkaloid that can be employed in the treatment of clinical diseases and additives for supplements, the danger of yohimbine should be of widespread concern in society.
1. Introduction
Yohimbine is a natural indole alkaloid that is extracted from the leaves and bark of the yohimbine tree Pausinystalia johimbe, which belongs to Rubiaceae, mainly grows in West Africa, Cameroon, and Congo, and has a long history of use as an aphrodisiac in African countries [1,2]. Pharmacological studies have confirmed that yohimbine is a highly potent antagonist of presynaptic and postsynaptic α2-adrenoreceptors within smooth muscles and blood vessels [3]. It is generally believed that by selectively blocking α2-adrenoceptors in the locus ceruleus in the brain, sympathetic nerves are excited to increase the release of norepinephrine and dopamine, which can relax vascular smooth muscle, increase peripheral parasympathetic tension, and reduce sympathetic tension [4,5].
Studies have shown that yohimbine has a significant effect on the treatment of male erectile dysfunction and is considered an effective drug for improving impotence [3,6]. Alkaloids also dilate peripheral blood vessels, lower blood pressure, have anti-inflammatory effects and can be utilized for the clinical treatment of atherosclerosis and rheumatism [7]. Yohimbine has also gained popularity in the bodybuilding community due to its lipolytic and sympathomimetic effects for fast weight loss and bodybuilding supplementation [8].
Currently, yohimbine is clinically utilized as a prescription drug with its main dosage forms in powder and tablets, and is also available for purchase on the Internet as an herbal supplement and oral liquid [9]. With increased research, dose-related side effects in clinical applications have been reported. The adverse effects of yohimbine include gastrointestinal distress, hypertension, tachycardia, manic reactions, bronchospasm, palpitations, insomnia/ anxiety, chills/cold/shivering, sweating, flushing, and headaches, which can be attributed to its central adrenergic activity [3,9]. Previous studies have reported several adverse cases caused by taking yohimbine [10]. According to the FDA Center for Food Safety and Nutrition (CFSAN), 275 cases of poisoning caused by dietary supplements were monitored in San Francisco within a year (2006), and yohimbine products accounted for 18% of supplement related symptomatic cases [11]. Since the drug has not yet been subjected to scientifically rigorous human clinical trials and safety assessments, a few death cases related to yohimbine have been published.
This study reports four simultaneous cases of poisoning/death caused after yohimbine consumption.
Yohimbine is an indole alkaloid from the leaves and bark of the Pausinystalia johimbe tree that has acquired an enviable reputation in treating erectile dysfunction. This report presents four simultaneous severe poisoning/death cases caused by yohimbine. The test samples comprised the venous blood of four middle-aged men (aged 47–65) who were suspected of poisoning; one of the men died due to ineffective rescue. Ethanol concentration determination and toxicological routine screening were performed using gas chromatography with flame ionization detection (GC-FID) and liquid chromatography-tandem mass spectrometry (LC-MS/MS). A specific LC-MS/MS method was developed to quantify yohimbine, which showed concentrations of 459, 249, and 301 ng/mL in three poisoned blood samples and concentrations as high as 5631 ng/mL in the deceased. Moreover, the deceased’s autopsy ruled out death from trauma and previous illness, and no other common toxic components were detected in his blood. Therefore, yohimbine poisoning appears to be the most likely cause of death. As a type of alkaloid that can be employed in the treatment of clinical diseases and additives for supplements, the danger of yohimbine should be of widespread concern in society.
1. Introduction
Yohimbine is a natural indole alkaloid that is extracted from the leaves and bark of the yohimbine tree Pausinystalia johimbe, which belongs to Rubiaceae, mainly grows in West Africa, Cameroon, and Congo, and has a long history of use as an aphrodisiac in African countries [1,2]. Pharmacological studies have confirmed that yohimbine is a highly potent antagonist of presynaptic and postsynaptic α2-adrenoreceptors within smooth muscles and blood vessels [3]. It is generally believed that by selectively blocking α2-adrenoceptors in the locus ceruleus in the brain, sympathetic nerves are excited to increase the release of norepinephrine and dopamine, which can relax vascular smooth muscle, increase peripheral parasympathetic tension, and reduce sympathetic tension [4,5].
Studies have shown that yohimbine has a significant effect on the treatment of male erectile dysfunction and is considered an effective drug for improving impotence [3,6]. Alkaloids also dilate peripheral blood vessels, lower blood pressure, have anti-inflammatory effects and can be utilized for the clinical treatment of atherosclerosis and rheumatism [7]. Yohimbine has also gained popularity in the bodybuilding community due to its lipolytic and sympathomimetic effects for fast weight loss and bodybuilding supplementation [8].
Currently, yohimbine is clinically utilized as a prescription drug with its main dosage forms in powder and tablets, and is also available for purchase on the Internet as an herbal supplement and oral liquid [9]. With increased research, dose-related side effects in clinical applications have been reported. The adverse effects of yohimbine include gastrointestinal distress, hypertension, tachycardia, manic reactions, bronchospasm, palpitations, insomnia/ anxiety, chills/cold/shivering, sweating, flushing, and headaches, which can be attributed to its central adrenergic activity [3,9]. Previous studies have reported several adverse cases caused by taking yohimbine [10]. According to the FDA Center for Food Safety and Nutrition (CFSAN), 275 cases of poisoning caused by dietary supplements were monitored in San Francisco within a year (2006), and yohimbine products accounted for 18% of supplement related symptomatic cases [11]. Since the drug has not yet been subjected to scientifically rigorous human clinical trials and safety assessments, a few death cases related to yohimbine have been published.
This study reports four simultaneous cases of poisoning/death caused after yohimbine consumption.
