![conference banner](/images/conference-banner.jpeg)
Abstract
Inhibition of carbonic anhydrase (CA, EC 4.2.1.1) isoforms present in the eyes (CA I, II, IV and XII), with sulfonamides such as acetazolamide, methazolamide, ethoxzolamide and dichlorophenamide, is still widely used for the systemic treatment of glaucoma. The mechanism of action of these drugs consists in inhibition of CA isozymes present in ciliary processes of the eye, with the consequent reduction of bicarbonate and aqueous humour secretion, and of elevated intraocular pressure (IOP) characteristic of this disease. As isoforms CA II/IV/XII are present in many other tissues/organs, generally, systemic CAIs possess undesired side effects such as numbness and tingling of extremities; metallic taste; depression; fatigue; malaise; weight loss; decreased libido; gastrointestinal irritation; metabolic acidosis; renal calculi and transient myopia. For avoiding these side effects, recently, topically effective CAIs have been developed in the last 10 years, with two drugs available clinically: dorzolamide and brinzolamide. Both these drugs are applied topically as water solutions/ suspensions, alone or in combination with other agents (β-blockers, prostaglandin derivatives, etc) and produce a consistent and prolonged reduction of IOP. Furthermore, recent reports show both the systemically as well as topically acting sulfonamide CAIs to be effective in the treatment of macular edema, macular degeneration disease, or diabetic retinopathy, for which pharmacological treatment is unavailable up to now. Much research is in act in the search of more effective topically acting CAIs, free of the inconveniences and side effects of the presently available drugs. For achieving this goal, two recently reported strategy, the tail approach and its variant, the sugar-tail approach, were extensively applied for the synthesis of large numbers of derivatives possessing desired physico-chemical properties. Many such new sulfonamides showed promising antiglaucoma activity in animal models of the disease.
Current Pharmaceutical Design
Title: The Development of Topically Acting Carbonic Anhydrase Inhibitors as Antiglaucoma Agents
Volume: 14 Issue: 7
Author(s): Claudiu T. Supuran, Andrea Scozzafava and Francesco Mincione
Affiliation:
Abstract: Inhibition of carbonic anhydrase (CA, EC 4.2.1.1) isoforms present in the eyes (CA I, II, IV and XII), with sulfonamides such as acetazolamide, methazolamide, ethoxzolamide and dichlorophenamide, is still widely used for the systemic treatment of glaucoma. The mechanism of action of these drugs consists in inhibition of CA isozymes present in ciliary processes of the eye, with the consequent reduction of bicarbonate and aqueous humour secretion, and of elevated intraocular pressure (IOP) characteristic of this disease. As isoforms CA II/IV/XII are present in many other tissues/organs, generally, systemic CAIs possess undesired side effects such as numbness and tingling of extremities; metallic taste; depression; fatigue; malaise; weight loss; decreased libido; gastrointestinal irritation; metabolic acidosis; renal calculi and transient myopia. For avoiding these side effects, recently, topically effective CAIs have been developed in the last 10 years, with two drugs available clinically: dorzolamide and brinzolamide. Both these drugs are applied topically as water solutions/ suspensions, alone or in combination with other agents (β-blockers, prostaglandin derivatives, etc) and produce a consistent and prolonged reduction of IOP. Furthermore, recent reports show both the systemically as well as topically acting sulfonamide CAIs to be effective in the treatment of macular edema, macular degeneration disease, or diabetic retinopathy, for which pharmacological treatment is unavailable up to now. Much research is in act in the search of more effective topically acting CAIs, free of the inconveniences and side effects of the presently available drugs. For achieving this goal, two recently reported strategy, the tail approach and its variant, the sugar-tail approach, were extensively applied for the synthesis of large numbers of derivatives possessing desired physico-chemical properties. Many such new sulfonamides showed promising antiglaucoma activity in animal models of the disease.
Export Options
About this article
Cite this article as:
Supuran T. Claudiu, Scozzafava Andrea and Mincione Francesco, The Development of Topically Acting Carbonic Anhydrase Inhibitors as Antiglaucoma Agents, Current Pharmaceutical Design 2008; 14 (7) . https://dx.doi.org/10.2174/138161208783877866
DOI https://dx.doi.org/10.2174/138161208783877866 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
Blood-based biomarkers in large-scale screening for neurodegenerative diseases
Disease biomarkers are necessary tools that can be employ in several clinical context of use (COU), ranging from the (early) diagnosis, prognosis, prediction, to monitor of disease state and/or drug efficacy. Regarding neurodegenerative diseases, in particular Alzheimer’s disease (AD), a battery of well-validated biomarkers are available, such as cerebrospinal fluid ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Diabetes mellitus: advances in diagnosis and treatment driving by precision medicine
Diabetes mellitus (DM) is a chronic degenerative metabolic disease with ever increasing prevalence worldwide which is now an epidemic disease affecting 500 million people worldwide. Insufficient insulin secretion from pancreatic β cells unable to maintain blood glucose homeostasis is the main feature of this disease. Multifactorial and complex nature of ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Vascular Dementia: Atherosclerosis, Cognition and Alzheimers Disease
Current Alzheimer Research Pharmacological Treatments for Cocaine Dependence: Is There Something New?
Current Pharmaceutical Design Hypertension in Pregnancy: Pathophysiology & Management Strategies
Current Pharmaceutical Design Editorial:Polypharmacology of Natural Products
Mini-Reviews in Organic Chemistry Use of Medication in Coronary Imaging by CT
Current Medical Imaging The Complexity of Aging: Cancer Risk Among Elderly People and Infectious Risk Among Those with Cancer
Anti-Cancer Agents in Medicinal Chemistry Targeting Microtubules to Inhibit Angiogenesis and Disrupt Tumour Vasculature:Implications for Cancer Treatment
Current Cancer Drug Targets Neurotensin NTS1-Dopamine D2 Receptor-Receptor Interactions in Putative Receptor Heteromers: Relevance for Parkinson`s Disease and Schizophrenia
Current Protein & Peptide Science Combination of Therapeutic Hypothermia and Other Neuroprotective Strategies after An Ischemic Cerebral Insult
Current Neuropharmacology Effects of <i>Nigella Sativa</i> (Black seeds) Supplementation on Plasma Lipid Profile in Human Subjects - A Review
Current Nutraceuticals Medication-Induced Nephrotoxicity in Older Patients
Current Drug Metabolism New Pharmacological Approaches in Infants with Hypoxic-Ischemic Encephalopathy
Current Pharmaceutical Design Noradrenergic Regulation of Glial Activation: Molecular Mechanisms and Therapeutic Implications
Current Neuropharmacology Lymphocytic Interstitial Pneumonia Associated with Sjögren Syndrome: Case-Based Review
Current Rheumatology Reviews Interleukin 2 in Cancer Therapy
Current Medicinal Chemistry Blood Pressure Lowering and Outcomes in type 2 Diabetes: Implications of the Blood Pressure-Lowering Arm of the Advance Trial
Current Hypertension Reviews New Agents to Treat Life-Threatening Fungal Infections
Current Topics in Medicinal Chemistry Is Mania the Hypertension of the Mood? Discussion of A Hypothesis
Current Neuropharmacology Torasemide in Hypertension and Heart Failure: Re-inventing Loop Diuretic Therapy?
Current Pharmaceutical Design Loop Diuretics Strategies in Acute Heart Failure: From Clinical Trials to Practical Application
Current Drug Targets