To review the management of Idiopathic Intracranial Hypertension (IIH) with co-existing conditions affecting therapy: obesity, sulfa allergy, nephrolithiasis, and pregnancy.

RECENT FINDINGS:

The IIH-WT trial showed that bariatric surgery is currently the most effective method for obese patients with IIH to lose weight, leading to normalization of CSF pressure in many cases. Allergy to sulfonamide antibiotics does not preclude the use of acetazolamide; rather, penicillin allergy or multiple drug allergies are the strongest predictor of a hypersensitivity reaction. Carbonic anhydrase inhibitors should be avoided in individuals with a personal history of nephrolithiasis; the risk of renal stones increases with concomitant use of other medications with the potential for nephrolithiasis. Glucagon-like peptide-1 receptor antagonists (GLP-1RA) are promising non-surgical weight loss options although preliminary studies have not demonstrated considerable impact on papilledema, headache or vision. Women with IIH have high rates of pregnancy complications partly related to obesity. Recommendations for weight gain or loss during gestation are controversial. Recent studies show better outcomes in obese women who maintain or lose weight while pregnant including gestational diabetes, pre-eclampsia and emergency caesarian section. Progress continues in the search for the cause and best treatments for IIH. Larger multicenter trials of GLP-1RA are needed to determine their efficacy.

2025-08-01·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of isatin-functionalized benzenesulfonamides as novel carbonic anhydrase II and VII inhibitors with antiepileptic potential

Article

作者: Elnaggar, Yosra S R ; Eldehna, Wagdy M ; Giovannuzzi, Simone ; Abo-Ashour, Mahmoud F ; El-Hamaky, Anwar A ; Elsayed, Zainab M ; Al-Sanea, Mohammad M ; Alkabbani, Mahmoud Abdelrahman ; Tawfik, Haytham O ; Supuran, Claudiu T ; Nocentini, Alessio ; Khaleel, Eman F

Epilepsy continues to be a challenging neurological disorder with a partially understood etiology that necessitates novel therapeutic strategies. This study introduces isatin-functionalized benzenesulfonamides (5a-f and 7a-e) targeting carbonic anhydrase (CA) isoforms II and VII implicated in seizure mechanisms. The design exploits a one-tail approach, integrating a sulfonamide warhead for zinc coordination in the CA active site, a triazole linker (inspired by FDA-approved antiepileptic rufinamide), and an isatin-based tail. In vitro evaluation revealed potent inhibition of hCA II and VII, with sulfonamides 5c, 5e, 5f, 7a, and 7d showing notable activity. The anticonvulsant activity of five carbonic anhydrase inhibitors (5c, 5e, 5f, 7a, and 7d) was assessed using PTZ and pilocarpine-induced convulsions in mice. These compounds were selected based on their superior in vitro inhibitory potency against hCA II and VII isoforms, as reflected by their low nanomolar K_I values. Among them, 5e and 7a exhibited the highest efficacy, achieving 100 % protection in the PTZ model and significantly delaying seizure onset in the pilocarpine model. These compounds also reduced seizure severity and improved survival rates, surpassing valproic acid's effectiveness. Additionally, biochemical evaluation revealed that both compounds restored hippocampal KCC2 and mTOR levels, suggesting their role in modulating neuronal excitability and ionic balance. Safety assessments, including Rotarod and biochemical toxicity tests, confirmed their favorable safety profile, supporting their potential as promising anticonvulsant candidates.

2025-07-01·AMERICAN JOURNAL OF OTOLARYNGOLOGY

Acetazolamide use in postoperative CSF leak prevention: A literature review

Review

作者: Patel, Evan A ; Saad, Anthony M ; Filimonov, Andrey ; Filip, Peter

BACKGROUND:

Acetazolamide, a carbonic anhydrase inhibitor and commonly utilized diuretic, has been found to decrease cerebrospinal fluid (CSF) production, leading to its use in the prevention of postoperative CSF leaks. Despite its widespread use, the efficacy and optimal protocols for acetazolamide in this context remain poorly defined. This systematic review aims to elucidate the role of acetazolamide in preventing postoperative and traumatic CSF leaks.

METHODS:

A systematic review was performed in Covidence adhering to PRISMA Guidelines. A search of PubMed, SCOPUS, and CINAHL for literature published through July 2023 identified 215 unique publications related to acetazolamide use in preventing postoperative CSF leaks. Full texts were independently screened by two authors, with discrepancies resolved by third reviewer. 15 publications were selected and categorized into themes including postoperative CSF leak prevention, trauma management, dosage optimization, and adverse effects.

RESULTS:

Of the fifteen articles, twelve focused on the role of acetazolamide in preventing postoperative CSF leaks, highlighting its effectiveness in reducing leak rates following neurosurgical and otolaryngological procedures. Themes discussed in the remaining six articles included acetazolamide's role in managing intracranial hypertension in trauma patients, optimal dosing strategies, and the spectrum of side effects ranging from mild to severe.

CONCLUSION:

Acetazolamide shows promise in the prevention of postoperative CSF leaks and in certain trauma contexts. However, further studies should establish standardized protocols and optimize dosing regimens. Future research should also focus on long-term outcomes and the management of adverse effects to fully elucidate the benefits and limitations of acetazolamide in these clinical settings.

项与 Carbonic anhydrase inhibitors(CSIRO) 相关的新闻（医药）

2024-07-06

·ETPharma

Drugs body flags side effects of heart, Glaucoma medications

New Delhi: Drug standards body Indian Pharmacopoeia Commission (IPC) has issued a drug safety alert on commonly used drugs amlodipine and acetazolamide , saying both these medicines cause adverse reactions. Amlodipine - used for treatment of fatal coronary heart disease and non-fatal myocardial infarction and to reduce the risk of stroke - causes lichenoid keratosis, an inflammatory reaction, IPC said. According to IPC, amlodipine is also used to reduce the risk of coronary revascularisation procedures and need for hospitalisation due to angina in patients with coronary artery disease. The medicine is used alone or in combination with other medications. The lesions generally appear on the forearms, hands, chests of middle-aged women, or areas exposed to the sun, it said. Acetazolamide - a carbonic anhydrase inhibitor used to treat glaucoma - may lead to choroidal effusion or choroidal detachment, which is fluid buildup in the choroid layer of the eye. IPC, which comes under the health and family welfare ministry, has cautioned healthcare professionals to "diligently monitor" the potential occurrence of adverse drug reactions (ADRs) when administering these drugs. It has also advised patients and consumers to closely monitor the possibility of the above ADRs when using the suspected drugs. "Companies manufacturing these drugs may be asked to insert warnings in their package so that patients and doctors know about the adverse event," a government official said on the condition of anonymity. The IPC warning is based on preliminary analysis of adverse drug reactions (ADRs) from the Pharmacovigilance Programme of India (PvPI) database. By Teena Thacker ,