Chemistry, Analysis, Pharmacokinetics and Pharmacodynamics Aspects of Lorcaserin, a Selective Serotonin 5-HT2C Receptor Agonist: An Update

2020 ◽  
Vol 20 (9) ◽  
pp. 768-778
Author(s):  
Sanjay Sharma ◽  
Komal S. Aware ◽  
Ketan Hatware ◽  
Kiran Patil
Keyword(s):  
Side Effects ◽  
Receptor Agonist ◽  
Scale Up ◽  
Mass Spectrometric ◽  
Selective Serotonin ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Step Method ◽  
Comprehensive Information ◽  
Tissue Matrix ◽  
Liquid Chromatographic

This review refers to the all-inclusive details of Lorcaserin Hydrochloride on comprehensive information about the synthesis, analytical methods, pharmacodynamics, pharmacokinetics, drug interactions and adverse effects. Lorcaserin Hydrochloride is chemically (R)-8-Chloro-1-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine hydrochloride. Lorcaserin HCl is a novel, synthetic, centrally-acting selective serotonin C (5-HT2c) receptor, l agonist, which results in increased satiety and decreased food consumption in patients. Headache, dizziness and nausea are the most common side effects associated with this drug. Lorcaserin HCl has two major metabolites, one conjugated with glucuronide called N-carbamoyl glucuronide which is excreted in urine and the second Lorcaserin N-sulfamate, which is circulated in the blood. Lorcaserin HCl is synthesized using four different schemes of which a six-step method that resulted in 92.3% yield with 99.8% of purity is employed for scale-up production. It is analyzed quantitatively in the plasma and brain tissue matrix of rats by Ultra Performance Liquid chromatographic (UPLC) method using MS-MS (Mass Spectrometric) detection.

scholarly journals Are side effects of cannabidiol (CBD) products caused by tetrahydrocannabinol (THC) contamination?

F1000Research ◽  
2020 ◽  
Vol 8 ◽  
pp. 1394 ◽  
Author(s):  
Dirk W. Lachenmeier ◽  
Stephanie Habel ◽  
Berit Fischer ◽  
Frauke Herbi ◽  
Yvonne Zerbe ◽  
...  
Keyword(s):  
Side Effects ◽  
Adverse Effects ◽  
Mass Spectrometric ◽  
Health Claims ◽  
Dose Effect ◽  
Full Spectrum ◽  
German Market ◽  
Food Ingredients ◽  
Tandem Mass Spectrometric ◽  
Liquid Chromatographic

Cannabidiol (CBD)-containing products are widely marketed as over the counter products, mostly as food supplements, to avoid the strict rules of medicinal products. Side-effects reported in anecdotal consumer reports or during clinical studies were first assumed to be due to hydrolytic conversion of CBD to psychotropic Δ9-tetrahydrocannabinol (THC) in the stomach after oral consumption. However, research of pure CBD solutions stored in simulated gastric juice or subjected to various storage conditions such as heat and light with specific liquid chromatographic/tandem mass spectrometric (LC/MS/MS) and ultra-high pressure liquid chromatographic/quadrupole time-of-flight mass spectrometric (UPLC-QTOF) analyses was unable to confirm THC formation. Another hypothesis for the side-effects of CBD products may be residual THC concentrations in the products as contamination, because most of them are based on crude hemp extracts containing the full spectrum of cannabinoids besides CBD. Analyses of 67 food products of the German market (mostly CBD oils) confirmed this hypothesis: 17 products (25%) contained THC above the lowest observed adverse effects level (2.5 mg/day). Inversely, CBD was present in the products below the no observed adverse effect level. Hence, it may be assumed that the adverse effects of some commercial CBD products are based on a low-dose effect of THC and not due to effects of CBD itself. The safety, efficacy and purity of commercial CBD products is highly questionable, and all of the products in our sample collection showed various non-conformities to European food law such as unsafe THC levels, full-spectrum hemp extracts as non-approved novel food ingredients, non-approved health claims, and deficits in mandatory food labelling requirements. In view of the growing market for such lifestyle products, the effectiveness of the instrument of food business operators' own responsibility for product safety must obviously be challenged.

scholarly journals Are side effects of cannabidiol (CBD) products caused by tetrahydrocannabinol (THC) contamination?

F1000Research ◽  
2020 ◽  
Vol 8 ◽  
pp. 1394 ◽  
Author(s):  
Dirk W. Lachenmeier ◽  
Stephanie Habel ◽  
Berit Fischer ◽  
Frauke Herbi ◽  
Yvonne Zerbe ◽  
...  
Keyword(s):  
Side Effects ◽  
Adverse Effects ◽  
Mass Spectrometric ◽  
Health Claims ◽  
Dose Effect ◽  
Full Spectrum ◽  
German Market ◽  
Food Ingredients ◽  
Tandem Mass Spectrometric ◽  
Liquid Chromatographic

Cannabidiol (CBD)-containing products are widely marketed as over the counter products, mostly as food supplements, to avoid the strict rules of medicinal products. Side-effects reported in anecdotal consumer reports or during clinical studies were first assumed to be due to hydrolytic conversion of CBD to psychotropic Δ9-tetrahydrocannabinol (Δ9-THC) in the stomach after oral consumption. However, research of pure CBD solutions stored in simulated gastric juice or subjected to various storage conditions such as heat and light with specific liquid chromatographic/tandem mass spectrometric (LC/MS/MS) and ultra-high pressure liquid chromatographic/quadrupole time-of-flight mass spectrometric (UPLC-QTOF) analyses was unable to confirm THC formation. Another hypothesis for the side-effects of CBD products may be residual Δ9-THC concentrations in the products as contamination, because most of them are based on crude hemp extracts containing the full spectrum of cannabinoids besides CBD. Analyses of 67 food products of the German market (mostly CBD oils) confirmed this hypothesis: 17 products (25%) contained Δ9-THC above the lowest observed adverse effects level (2.5 mg/day). Inversely, CBD was present in the products below the no observed adverse effect level. Hence, it may be assumed that the adverse effects of some commercial CBD products are based on a low-dose effect of Δ9-THC and not due to effects of CBD itself. The safety, efficacy and purity of commercial CBD products is highly questionable, and all of the products in our sample collection showed various non-conformities to European food law such as unsafe Δ9-THC levels, full-spectrum hemp extracts as non-approved novel food ingredients, non-approved health claims, and deficits in mandatory food labelling requirements. In view of the growing market for such lifestyle products, the effectiveness of the instrument of food business operators' own responsibility for product safety must obviously be challenged.

scholarly journals Are side effects of cannabidiol (CBD) products caused by tetrahydrocannabinol (THC) contamination?

F1000Research ◽  
2019 ◽  
Vol 8 ◽  
pp. 1394 ◽  
Author(s):  
Dirk W. Lachenmeier ◽  
Stephanie Habel ◽  
Berit Fischer ◽  
Frauke Herbi ◽  
Yvonne Zerbe ◽  
...  
Keyword(s):  
Side Effects ◽  
Adverse Effects ◽  
Mass Spectrometric ◽  
Health Claims ◽  
Dose Effect ◽  
Full Spectrum ◽  
German Market ◽  
Food Ingredients ◽  
Tandem Mass Spectrometric ◽  
Liquid Chromatographic

Cannabidiol (CBD)-containing products are widely marketed as over the counter products, mostly as food supplements, to avoid the strict rules of medicinal products. Side-effects reported in anecdotal consumer reports or during clinical studies were first assumed to be due to hydrolytic conversion of CBD to psychoactive Δ9-tetrahydrocannainol (THC). However, research of pure CBD solutions stored in simulated gastric juice or subjected to various storage conditions such as heat and light with specific liquid chromatographic/tandem mass spectrometric (LC/MS/MS) and ultra-high pressure liquid chromatographic/quadrupole time-of-flight mass spectrometric (UPLC-QTOF) analyses was unable to confirm THC formation. Another hypothesis for the side-effects of CBD products may be residual THC concentrations in the products as contamination, because most of them are based on crude hemp extracts containing the full spectrum of cannabinoids besides CBD. Analyses of 28 food products of the German market containing hemp extract as an ingredient (mostly CBD oils) confirmed this hypothesis: 10 products (36%) contained THC above the lowest observed adverse effects level (2.5 mg/day). Inversely, CBD was present in the products below the no observed adverse effect level. Hence, it may be assumed that the adverse effects of some commercial CBD products are based on a low-dose effect of THC and not due to effects of CBD itself. The safety, efficacy and purity of commercial CBD products is highly questionable, and all of the products in our sample collection showed various non-conformities to European food law such as unsafe THC levels, full-spectrum hemp extracts as non-approved novel food ingredients, non-approved health claims, and deficits in mandatory food labelling requirements. In view of the growing market for such lifestyle products, the effectiveness of the instrument of food business operators' own responsibility for product safety must obviously be challenged.

Liquid chromatographic-electrospray mass spectrometric analysis of Coptidis Rhizoma

1996 ◽  
Vol 755 (1) ◽  
pp. 19-26 ◽  
Author(s):  
Wu-Chang Chuang ◽  
Dun-Shyurng Young ◽  
Lilian Kao Liu ◽  
Shuenn-Jyi Sheu
Keyword(s):  
Mass Spectrometric ◽  
Mass Spectrometric Analysis ◽  
Spectrometric Analysis ◽  
Coptidis Rhizoma ◽  
Liquid Chromatographic

scholarly journals Polypharmacy and Malnutrition Management of Elderly Perioperative Patients with Cancer: A Systematic Review

Nutrients ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 1961
Author(s):  
Eiji Kose ◽  
Hidetaka Wakabayashi ◽  
Nobuhiro Yasuno
Keyword(s):  
Side Effects ◽  
Cancer Cachexia ◽  
Drug Effects ◽  
Drug Efficacy ◽  
Nutritional Management ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Drug Induced ◽  
Anabolic Resistance ◽  
Patients With Cancer ◽  
The Impact

Malnutrition, which commonly occurs in perioperative patients with cancer, leads to decreased muscle mass, hypoalbuminemia, and edema, thereby increasing the patient’s risk of various complications. Thus, the nutritional management of perioperative patients with cancer should be focused on to ensure that surgical treatment is safe and effective, postoperative complications are prevented, and mortality is reduced. Pathophysiological and drug-induced factors in elderly patients with cancer are associated with the risk of developing malnutrition. Pathophysiological factors include the effects of tumors, cachexia, and anorexia of aging. Metabolic changes, such as inflammation, excess catabolism, and anabolic resistance in patients with tumor-induced cancer alter the body’s ability to use essential nutrients. Drug-induced factors include the side effects of anticancer drugs and polypharmacy. Drug–drug, drug–disease, drug–nutrient, and drug–food interactions can significantly affect the patient’s nutritional status. Furthermore, malnutrition may affect pharmacokinetics and pharmacodynamics, potentiate drug effects, and cause side effects. This review outlines polypharmacy and malnutrition, the impact of malnutrition on drug efficacy, drug–nutrient and drug–food interactions, and intervention effects on polypharmacy or cancer cachexia in elderly perioperative patients with cancer.

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