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Cholinergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Vishal S. Gulecha, Manoj S. Mahajan, Aman Upaganlawar, Abdulla Sherikar, Chandrashekhar Upasani
Urinary urgency induced by minor inflammatory bladder disorders can be treated by atropine and other muscarinic antagonists. Urinary bladder predominantly consists of M2 and M3 receptors mediating direct activation of contraction of detrusor muscles, especially by M3 receptors subtype. Dicyclomine and oxybutynin are indicated in renal colic and urethral smooth muscle spasm (Sharma and Sharma, 2017; Barar, 2004). Trospium, a nonselective antagonist, is an alternative to oxybutynin. Trospium has better efficacy and reduced side effects than oxybutynin. Darifenacin and solifenacin are other approved agents with enhanced selectivity toward M3 receptors. A directly acting smooth muscle relaxant, flavoxate, possesses anticholinergic and antispasmodic activities and is useful in urinary urge incontinence and for subrapubic pain in cystitis and urethritis (Srivastava, 2017; Sharma and Sharma, 2017).
Commonly prescribed drugs
Published in Alistair Burns, Michael A Horan, John E Clague, Gillian McLean, Geriatric Medicine for Old-Age Psychiatrists, 2005
Alistair Burns, Michael A Horan, John E Clague, Gillian McLean
This usually arises from detrusor instability, and a combination of drug treatment with non-drug approaches such as pelvic floor exercises and bladder draining is the treatment of choice. Antimuscarinic drugs (oxybutynin, tolterodine, flavoxate, propiverine, trospium) increase the capacity of the bladder and reduce contractions.
Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Jianan Sun, Jiahui Mu, Shenglin Wang, Cai Jia, Dahong Li, Huiming Hua, Hao Cao
From late 1930s to 2014, 77% of anti-tumour drugs approved worldwide are closely related to natural products, and the utilisation of natural products and/or their novel structures is still alive and well18,19. Chromones are a type of compounds with a benzo-γ-pyrone skeleton, which are widely distributed in nature20,21. It has been proved that chromones have various kinds of biological activities, including antitumor22, antimicrobial23,24, anti-HIV25, anti-inflammatory26, antioxidant27, wound healing28, and so on. In addition, chromones and its derivatives are also the most important heterocyclic compounds, playing an important role in the design and discovery of new physiologically/pharmacologically active compounds20,29, such as apigenin (4′,5,7-trihydroxyflavone, A, Figure 1), flavoxate (2-(1-piperidyl)ethyl 3-methyl-4-oxo-2-phenylchromene-8-carboxylate, B, Figure 1), etc.30–32. More importantly, chromone derivatives possess low mammalian toxicity and are present in large amounts in the diet of humans due to their origin in plants21. In terms of antitumor activity, chromones show activity against many kinds of tumour cells, and the antiproliferative mechanisms involve cytotoxicity, anti-metastasis, anti-angiogenesis, chemoprevention, immunomodulation, etc.33–39. To date, there are some chromone derivatives showing potent cytotoxic effect on breast cancer cells, such as C and D (Figure 1)40,41.
Long-term effectiveness of an intervention to enhance mirabegron use revision and its deprescribing: 36-month follow-up of a quasi-experimental trial in primary care
Published in Current Medical Research and Opinion, 2021
Eladio Fernández-Liz, Pere Vivó-Tristante, Antonio Aranzana-Martínez, Maria Estrella Barceló-Colomer, Maria Larrosa-Garcia, José Luís del Val García, Elisabeth Martín-Gracia
Drugs for urinary frequency and incontinence are recommended as second-line therapies for OAB symptoms after behavioural therapy. Currently, there are two main groups of drugs used in OAB according to their mechanisms of action: antimuscarinics (fesoterodine, oxybutynin, tolterodine, propiverine, solifenacin, trospium chloride and flavoxate), and β3 adrenergic receptor agonists (mirabegron). These drugs can cause adverse effects: antimuscarinics can led to anticholinergic effects (including dry mouth, constipation and blurred vision), and mirabegron can cause urinary tract infection, headache, dizziness, tachycardia, nausea, constipation and diarrhoea3–8.
The cognitive safety of antimuscarinics in the treatment of overactive bladder
Published in Expert Opinion on Drug Safety, 2020
George Araklitis, Dudley Robinson
A 12-year cohort study from Taiwan recruited 16,412 patients over the age of 50 years using antimuscarinics for lower urinary tract symptoms [44]. Drugs used include; flavoxate, oxybutynin, propiverine, tolterodine, solifenacin, and trospium chloride. They looked at cumulative defined daily doses of the drug, which reflected the total-exposed dosage per day of antimuscarinics. Those with cumulative defined daily doses of 85–336 had a Hazard Ratio (HR) 1.15 (95% CI = 0.97–1.37, p = 0.107) and doses of greater than 337 had a HR 1.40 (95% CI = 1.12–1.75, p = 0.004), in the development of dementia.