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Biosensors Jul 2022The illegal use of β-adrenergic agonists during livestock growth poses a threat to public health; the long-term intake of this medication can cause serious... (Review)
Review
The illegal use of β-adrenergic agonists during livestock growth poses a threat to public health; the long-term intake of this medication can cause serious physiological side effects and even death. Therefore, rapid detection methods for β-adrenergic agonist residues on-site are required. Traditional detection methods such as liquid chromatography have limitations in terms of expensive instruments and complex operations. In contrast, paper methods are low cost, ubiquitous, and portable, which has led to them becoming the preferred detection method in recent years. Various paper-based fluidic devices have been developed to detect β-adrenergic agonist residues, including lateral flow immunoassays (LFAs) and microfluidic paper-based analytical devices (μPADs). In this review, the application of LFAs for the detection of β-agonists is summarized comprehensively, focusing on the latest advances in novel labeling and detection strategies. The use of μPADs as an analytical platform has attracted interest over the past decade due to their unique advantages and application for detecting β-adrenergic agonists, which are introduced here. Vertical flow immunoassays are also discussed for their shorter assay time and stronger multiplexing capabilities compared with LFAs. Furthermore, the development direction and prospects for the commercialization of paper-based devices are considered, shedding light on the development of point-of-care testing devices for β-adrenergic agonist residue detection.
Topics: Adrenergic beta-Agonists; Immunoassay; Lab-On-A-Chip Devices; Microfluidic Analytical Techniques; Paper; Point-of-Care Systems; Point-of-Care Testing
PubMed: 35884321
DOI: 10.3390/bios12070518 -
Medicina (Kaunas, Lithuania) 2006Epinephrine is an adrenergic agonist used to treat bronchospasm, anaphylactic reactions, bradycardia, cardiac arrest, and hypotension. Its toxicity is usually caused by... (Review)
Review
Epinephrine is an adrenergic agonist used to treat bronchospasm, anaphylactic reactions, bradycardia, cardiac arrest, and hypotension. Its toxicity is usually caused by iatrogenic errors. In overdose there is a typical rapid onset of agitation, hypertension, tachycardia, and dysrhythmias. This review article focuses on the causes of overdose, signs and symptoms, treatment and expected course, and prognosis of this iatrogenic pathology.
Topics: Adrenergic Agonists; Anaphylaxis; Arrhythmias, Cardiac; Bradycardia; Bronchial Spasm; Drug Overdose; Epinephrine; Heart Arrest; Humans; Hypertension; Hypotension; Iatrogenic Disease; Prognosis; Pulmonary Edema; Shock, Cardiogenic; Tachycardia
PubMed: 16861845
DOI: No ID Found -
Clinical Pharmacy 1985The beta 2-adrenergic agonists are reviewed in terms of their dose-response characteristics, and two newer agents, fenoterol hydrobromide and bitolterol mesylate... (Comparative Study)
Comparative Study Review
The beta 2-adrenergic agonists are reviewed in terms of their dose-response characteristics, and two newer agents, fenoterol hydrobromide and bitolterol mesylate aerosols, are reviewed in relation to older agents. The fenoterol aerosol contains a more potent beta 2-adrenergic agonist dose per puff than the other aerosols but, when given in equipotent doses, offers no advantage over available agents. Bitolterol mesylate is a prodrug that is hydrolyzed to the active beta 2-adrenergic agonist colterol by lung esterases. Bitolterol demonstrates an improved bronchoselectivity in animals, but there are insufficient comparative data in humans. Tachycardia is the dose-limiting toxicity for all beta 2-adrenergic agonists. Currently available data do not suggest an important improvement in duration of action for the newer agents over terbutaline or albuterol. Aerosol administration improves bronchoselectivity of all the agents. Optimal use of beta 2-adrenergic agonist aerosols requires understanding of the variable dose-response characteristics. The type of delivery system and patient technique are important variables in determining the dose delivered. Tube-spacer devices attached to aerosol canisters can significantly improve delivery of the beta 2-adrenergic agonists to the lungs in patients unable to synchronize actuation and inspiration. They provide minimal to no improvement in patients who can perform the appropriate technique. Aerosol administration is the route of choice for beta 2-adrenergic agonists for prophylaxis of exercise-induced bronchospasm; albuterol and terbutaline provide a prolonged duration of action with excellent beta 2-adrenergic selectivity. Patients should be carefully instructed in the optimal use of metered-dose inhalers, and some patients may benefit from use of tube-spacers.
Topics: Adrenergic beta-Agonists; Aerosols; Animals; Asthma; Biological Availability; Bronchi; Bronchodilator Agents; Chemical Phenomena; Chemistry; Dose-Response Relationship, Drug; Ethanolamines; Fenoterol; Forced Expiratory Volume; Humans; Kinetics; Respiratory Therapy; Tachycardia
PubMed: 2864159
DOI: No ID Found -
Clinical Toxicology (Philadelphia, Pa.) Aug 2022Xylazine is an alpha-2-adrenergic agonist used for its sedative and analgesic properties in veterinary medicine. While not approved by the Food and Drug Administration...
PURPOSE
Xylazine is an alpha-2-adrenergic agonist used for its sedative and analgesic properties in veterinary medicine. While not approved by the Food and Drug Administration for use in humans, anecdotal evidence suggests that exposures in humans is on the rise. We sought to systematically review and synthesize the evidence on xylazine exposure in humans focusing on the clinical presentation, management, and outcomes.
METHODS
We conducted a systematic review of the literature including PubMed, Embase, and Scopus from their inception to September 9, 2021. We searched abstracts from selected emergency medicine and toxicology conferences from 2011 through 2021. We included clinical reports of xylazine exposure in humans. We excluded animal studies, studies, laboratory studies, or articles in a language other than English. From each included article, we extracted subjective and objective data that focused on clinical presentation, management, and outcomes of patients exposed to xylazine.
RESULTS
We evaluated a total of 1409 records, rendering a final set of 17 articles and 2 abstracts meeting inclusion criteria. We identified a total of 98 patients amongst reports ranging from 1979 to 2020 and across nine countries. The most common types of xylazine exposures reported were unintentional exposure and intentional misuse/abuse. Common symptoms on presentation included hypotension, bradycardia, drowsiness, lethargy, while apnea with intubation and death were less frequently reported.
CONCLUSION
Human exposure to xylazine appears to be a rising concern within the prehospital and emergency medicine setting. Although a standardized treatment algorithm cannot be recommended at this time, further research is needed to improve the care of patients exposed to xylazine.
Topics: Adrenergic Agonists; Bradycardia; Humans; Hypnotics and Sedatives; Hypotension; United States; Xylazine
PubMed: 35442125
DOI: 10.1080/15563650.2022.2063135 -
The Annals of Pharmacotherapy 2013To review the place in therapy of mirabegron, a new oral β3-adrenergic receptor agonist, for the treatment of overactive bladder (OAB). (Review)
Review
OBJECTIVE
To review the place in therapy of mirabegron, a new oral β3-adrenergic receptor agonist, for the treatment of overactive bladder (OAB).
DATA SOURCES
A literature search of MEDLINE and MEDLINE In-Process & Other Non-Indexed Citations Databases (1996-April 2013) was conducted using the key words mirabegron, receptor, adrenergic, beta-3; adrenergic beta-3 receptor; beta-3 receptor, and overactive bladder; urinary bladder; overactive. All published articles regarding mirabegron were included. References of selected articles, data from poster presentations, and abstract publications were additionally reviewed.
STUDY SELECTION AND DATA EXTRACTION
Available English-language data from reviews, abstracts, presentations, and clinical trials of mirabegron in humans were reviewed; relevant clinical data were selected and included.
DATA SYNTHESIS
Mirabegron is the newest option for treatment of OAB with symptoms of urge incontinence. As a β3-receptor agonist, it reduces bladder muscle contractions. In two 12-week, randomized, double-blind, placebo-controlled Phase 3 studies, mirabegron significantly reduced the number of incontinence episodes per 24 hours from baseline (-1.47, -1.63, and -1.13; p < 0.05; and -1.57, -1.46, and -1.17; p < 0.05; all values for mirabegron 50 mg, 100 mg, and placebo). Micturitions per 24 hours were also reduced from baseline (-1.66, -1.75, and -1.05; p < 0.05; and -1.93, -1.77, and -1.34; p < 0.05; all values for mirabegron 50 mg, 100 mg, and placebo). A 12-month trial found mirabegron to have a safety and efficacy profile similar to that of tolterodine.
CONCLUSIONS
Treatment of OAB initially includes lifestyle and nonpharmacologic intervention; for patients with persistent symptoms despite these treatments, drug therapy represents a next-step approach for symptom control. Mirabegron alleviates symptoms of OAB while having a mechanism of action that provides an alternative for patients who are intolerant of or who have contraindications to anticholinergic agents. The place in therapy of mirabegron relative to anticholinergics in the treatment of urge incontinence has not yet been established.
Topics: Acetanilides; Administration, Oral; Adrenergic Agonists; Animals; Clinical Trials as Topic; Humans; Receptors, Adrenergic, beta-3; Thiazoles; Treatment Outcome; Urinary Bladder, Overactive
PubMed: 23757386
DOI: 10.1345/aph.1S054 -
European Journal of Heart Failure Mar 2023Pulmonary hypertension (PH) associated with left heart disease is an increasingly prevalent problem, orphan of targeted therapies, and related to a poor prognosis,... (Randomized Controlled Trial)
Randomized Controlled Trial
β3 adrenergic agonist treatment in chronic pulmonary hypertension associated with heart failure (SPHERE-HF): a double blind, placebo-controlled, randomized clinical trial.
AIMS
Pulmonary hypertension (PH) associated with left heart disease is an increasingly prevalent problem, orphan of targeted therapies, and related to a poor prognosis, particularly when pre- and post-capillary PH combine. The current study aimed to determine whether treatment with the selective β3 adrenoreceptor agonist mirabegron improves outcomes in patients with combined pre- and post-capillary PH (CpcPH).
METHODS AND RESULTS
The β3 Adrenergic Agonist Treatment in Chronic Pulmonary Hypertension Secondary to Heart Failure (SPHERE-HF) trial is a multicentre, randomized, parallel, placebo-controlled clinical trial that enrolled stable patients with CpcPH associated with symptomatic heart failure. A total of 80 patients were assigned to receive mirabegron (50 mg daily, titrated till 200 mg daily, n = 39) or placebo (n = 41) for 16 weeks. Of them, 66 patients successfully completed the study protocol and were valid for the main analysis. The primary endpoint was the change in pulmonary vascular resistance (PVR) on right heart catheterization. Secondary outcomes included the change in right ventricular (RV) ejection fraction by cardiac magnetic resonance or computed tomography, other haemodynamic variables, functional class, and quality of life. The trial was negative for the primary outcome (placebo-corrected mean difference of 0.62 Wood units, 95% confidence interval [CI] -0.38, 1.61, p = 0.218). Patients receiving mirabegron presented a significant improvement in RV ejection fraction as compared to placebo (placebo-corrected mean difference of 3.0%, 95% CI 0.4, 5.7%, p = 0.026), without significant differences in other pre-specified secondary outcomes.
CONCLUSIONS
SPHERE-HF is the first clinical trial to assess the potential benefit of β3 adrenergic agonists in PH. The trial was negative since mirabegron did not reduce PVR, the primary endpoint, in patients with CpcPH. On pre-specified secondary outcomes, a significant improvement in RV ejection fraction assessed by advanced cardiac imaging was found, without differences in functional class or quality of life.
Topics: Humans; Hypertension, Pulmonary; Heart Failure; Quality of Life; Stroke Volume; Adrenergic Agonists; Double-Blind Method; Treatment Outcome
PubMed: 36404400
DOI: 10.1002/ejhf.2745 -
Journal of Addiction MedicineXylazine is an alpha-2 adrenergic agonist commonly used as a large animal anesthetic. It is used as an adulterant in illicit opioids, and it is now well established that...
BACKGROUND
Xylazine is an alpha-2 adrenergic agonist commonly used as a large animal anesthetic. It is used as an adulterant in illicit opioids, and it is now well established that its synergistic effect with opioids increases lethality. The amount of xylazine adulterating illicit opioids is growing at an alarming rate, present in almost one-third of opioid overdose deaths reported in Philadelphia in 2019. Despite this, there are no reports considering the management of patients using xylazine chronically. In particular, there are no reported cases detailing the management of xylazine withdrawal or exploring the potential for ongoing treatment for those in recovery from xylazine use.
CASE SUMMARY
We present the case of a 29 year old female with opioid use disorder and chronic xylazine use, admitted to the intensive care unit for treatment of chronic lower extremity wounds thought to be due to xylazine injection. Her xylazine withdrawal was managed with a combination of dexmedetomidine infusion, phenobarbital and tizanidine, later transitioned to clonidine. By hospital day 4 she was no longer experiencing withdrawal symptoms. She was transitioned from full-agonist opioids for pain to buprenorphine via a buprenorphine "micro-induction" and was ultimately discharged on buprenorphine, clonidine, and gabapentin on day 19 of admission.
CLINICAL SIGNIFICANCE
This case illustrates a potential treatment pathway that allows for safe and comfortable xylazine withdrawal in hospitalized patients. It also provides an introduction into several medical concerns affecting this patient population specifically, including xylazine-mediated soft tissue wounds.
Topics: Adrenergic Agonists; Analgesics, Opioid; Animals; Buprenorphine; Clonidine; Dexmedetomidine; Female; Gabapentin; Humans; Opioid-Related Disorders; Phenobarbital; Substance Withdrawal Syndrome; Xylazine
PubMed: 35020700
DOI: 10.1097/ADM.0000000000000955 -
Critical Care Medicine Sep 1993
Review
Topics: Adrenergic alpha-Agonists; Adrenergic beta-Agonists; Adult; Animals; Cardiopulmonary Resuscitation; Cerebrovascular Circulation; Child; Coronary Circulation; Dose-Response Relationship, Drug; Heart Arrest; Hemodynamics; Humans; Oxygen Consumption; Patient Discharge
PubMed: 8103444
DOI: 10.1097/00003246-199309001-00010 -
Drugs of Today (Barcelona, Spain : 1998) Aug 2021Overactive bladder (OAB) is an extremely common condition in adults of both sexes. It is characterized by an urgent need to micturate often accompanied by incontinence....
Overactive bladder (OAB) is an extremely common condition in adults of both sexes. It is characterized by an urgent need to micturate often accompanied by incontinence. The condition may also increase the number of micturitions in a 24-hour period as well as nocturia. The syndrome is not due to a urinary infection or other obvious pathology. In terms of drug treatment of OAB, there are two main approaches. One is the use of anticholinergic drugs that reduce the effect of the parasympathetic nervous system on the bladder. The other involves the use of drugs that are agonists at β-adrenergic receptors in the bladder. These drugs increase the capacity of the bladder and cause reductions in the number of daily micturitions and nocturia and also importantly reduce the frequency of urinary urgency and urinary urgency incontinence. Vibegron is the second β-adrenergic agonist to be approved for the treatment of OAB.
Topics: Acetanilides; Adrenergic Agonists; Adrenergic beta-3 Receptor Agonists; Adult; Female; Humans; Male; Pyrimidinones; Pyrrolidines; Treatment Outcome; Urinary Bladder, Overactive
PubMed: 34405208
DOI: 10.1358/dot.2021.57.8.3293588 -
Cancer Chemotherapy and Pharmacology Dec 2023Globally breast cancer accounts for 24.5% in incidence and 15.5% in cancer deaths in women. The triple-negative subtype lacks any specific therapy and is treated with...
PURPOSE
Globally breast cancer accounts for 24.5% in incidence and 15.5% in cancer deaths in women. The triple-negative subtype lacks any specific therapy and is treated with chemotherapy, resulting in significant side-effects. We aimed to investigate if the dose of chemotherapeutic drugs could be diminished by co-administering it with the β2-agonist salbutamol.
METHODS
Cell proliferation was measured by thymidine incorporation; gene expression, by real-time PCR and protein phosphorylation by WB. Apoptosis was assessed by acridine orange / ethidium bromide and TUNEL tests. Public patient databases were consulted. Cells were inoculated to nude mice and their growth assessed.
RESULTS
The β-agonist salbutamol synergizes in MDA-MB-231 cells in vitro with paclitaxel and doxorubicin on cell proliferation through ADRB2 receptors, while the β-blocker propranolol does not. The expression of this receptor was assessed in patient databases and other cell lines. Triple negative samples had the lowest expression. Salbutamol and paclitaxel decreased MDA-MB-231 cell proliferation while their combination further inhibited it. The pathways involved were analyzed. When these cells were inoculated to nude mice, paclitaxel and salbutamol inhibited tumor growth. The combined effect was significantly greater. Paclitaxel increased the expression of MDR1 while salbutamol partially reversed this increase.
CONCLUSION
While the effect of salbutamol was mainly on cell proliferation, suboptimal concentrations of paclitaxel provoked a very important enhancement of apoptosis. The latter enhanced transporter proteins as MDR1, whose expression were diminished by salbutamol. The expression of ADRB2 should be assessed in the biopsy or tumor to eventually select patients that could benefit from salbutamol repurposing.
Topics: Animals; Mice; Humans; Female; Paclitaxel; Breast Neoplasms; Triple Negative Breast Neoplasms; Mice, Nude; Albuterol; Cell Line, Tumor; Cell Proliferation; Propranolol; Adrenergic Agonists; Apoptosis
PubMed: 37725114
DOI: 10.1007/s00280-023-04586-9