Search results for "Azole"
showing 10 items of 2392 documents
Dopamine agonists in schizophrenia: a review.
1995
Although it is unlikely that the different types of course and severity of schizophrenia are caused by one neurochemical abnormality alone, indirect pharmacological evidence still suggests a relative excess of dopaminergic activity being implicated in the pathogenesis of most of the schizophrenic symptoms, e.g. positive symptomatology. Synthesis and release of dopamine as well as firing rates of dopaminergic neurons are controlled by stimulation of autoreceptors via a negative feedback regulation. Investigations on therapeutic effects of autoreceptor-nonselective dopamine agonists in schizophrenia have yielded inconsistent results. Dopamine autoreceptor agonists like pramipexole, roxindole,…
Synchronous Antithyroid Drug-Induced Agranulocytosis and Fournier Gangrene
2018
ABSTRACT: Objective: Antithyroid drugs (ATDs) such as thioimidazoles (e.g., methimazole, also called thiamazole, and carbimazole) and propylthiouracil are commonly used for the treatment of hyperthyroidism. A life-threatening reaction is agranulocytosis with an incidence of 0.1 to 0.5%. There are very few cases in the literature showing that the intake of ATDs finally led to sepsis with accompanying tissue necrosis.Methods: We present an unusual case of severe symptomatic agranulocytosis with sudden development of Fournier gangrene in a patient who was treated with ATDs for hyperthyroidism due to Graves disease.Results: A 69-year-old female was referred to our hospital with fever and a sore…
Brimonidine versus dapiprazole: Influence on pupil size at various illumination levels.
2005
To evaluate the influence of dapiprazole versus brimonidine on pupil size at various illumination levels.Department of Ophthalmology, Johannes Gutenberg-University, Mainz, Germany.In randomized prospective study, 19 healthy volunteers received 2 ophthalmic solutions, dapiprazole and brimonidine, 1 in each eye, for intraindividual comparison. Before and after application, pupil diameter was measured using an infrared binocular pupillometer at 3 illumination levels (0.03, 0.82, and 6.4 lux).Only slight pupil dilation was observed under scotopic conditions after application of both agents. After 20 minutes, the median reduction in pupil width was 1.4 mm for brimonidine and 0.9 mm for dapiprazo…
Maintenance therapy in gastro-oesophageal reflux disease.
2005
Gastro-oesophageal reflux disease (GORD) is a chronic condition. Symptom control and the maintenance of healing of erosive oesophagitis, if present, are important topics. In patients responding to a proton pump inhibitor (PPI) and showing no treatment symptoms it is appropriate to consider long-term treatment strategies, whether continuous, intermittent or on demand. Maintenance PPI therapy is well tolerated for up to 10 years of continuous use. Furthermore, tachyphylaxis does not occur during long-term maintenance PPI therapy. Previous concerns about risks of long-term PPI therapy in Heliobacter pylori-negative or H. pylori-positive patients have not materialized, while no cases of intesti…
Novel Combination of Sorafenib and Celecoxib Provides Synergistic Anti-Proliferative and Pro-Apoptotic Effects in Human Liver Cancer Cells
2013
Molecular targeted therapy has shown promise as a treatment for advanced hepatocellular carcinoma (HCC). Sorafenib, a multikinase inhibitor, recently received FDA approval for the treatment of advanced HCC. However, although sorafenib is well tolerated, concern for its safety has been expressed. Celecoxib (Celebrex®) is a selective cyclooxygenase-2 (COX-2) inhibitor which exhibits antitumor effects in human HCC cells. The present study examined the interaction between celecoxib and sorafenib in two human liver tumor cell lines HepG2 and Huh7. Our data showed that each inhibitor alone reduced cell growth and the combination of celecoxib with sorafenib synergistically inhibited cell growth an…
Dexrazoxane shows cytoprotective effects in zoledronic acid-treated human cells in vitro and in the rabbit tibia model in vivo
2012
Abstract Introduction Bisphosphonates are important and effective drugs in oncology and osteoporosis therapy. They accumulate in the bone matrix becoming released and active by bone resorption. This leads to effective inhibition of tumor cells and bone degradation. A side effect of bisphosphonates similar to other drugs like denosumab is osteonecrosis of the jaws (ONJ). This problem mostly occurs after tooth extraction. We studied the cytoprotectant dexrazoxane known from anthracycline chemotherapy for cytoprotection in nitrogen-containing bisphosphonate treated cells and in the rabbit tibia model to evaluate a possible value in ONJ management. Materials & methods Human osteoblasts (HOB) P2…
Salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole, a structural and analog of acetazolamide, show interesting carbonic anhydrase inhibitory properties…
2015
Three salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole (Hats) were prepared and characterized by physico-chemical methods. The p-toluensulfonate, the methylsulfonate, and the chlorhydrate monohydrate salts of Hats were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) and as anticonvulsants and diuretics, since many CAIs are clinically used as pharmacological agents. The three Hats salts exhibited diuretic and anticonvulsant activities with little neurotoxicity. The human (h) isoforms hCA I, II, IV, VII, IX, and XII were inhibited in their micromolar range by these salts, whereas pathogenic beta and gamma CAs showed similar, weak inhibitory profiles.
Review of Pharmacokinetics and Pharmacogenetics in Atypical Long-Acting Injectable Antipsychotics
2021
Over the last two decades, pharmacogenetics and pharmacokinetics have been increasingly used in clinical practice in Psychiatry due to the high variability regarding response and side effects of antipsychotic drugs. Specifically, long-acting injectable (LAI) antipsychotics have different pharmacokinetic profile than oral formulations due to their sustained release characteristics. In addition, most of these drugs are metabolized by CYP2D6, whose interindividual genetic variability results in different metabolizer status and, consequently, into different plasma concentrations of the drugs. In this context, there is consistent evidence which supports the use of therapeutic drug monitoring (TD…
Zn2+ and Cu2+ complexes of a fluorescent scorpiand-type oxadiazole azamacrocyclic ligand: crystal structures, solution studies and optical properties
2020
A ligand comprised of a macrocyclic pyridinophane core having a pendant arm containing a secondary amine group linked through a methylene spacer to a pyridyl–oxadiazole–phenyl (PyPD) fluorescent system has been prepared (L). The crystal structures of [ZnL](ClO4)2 and [CuL](ClO4)2 show that M2+ is coordinated to all the nitrogen atoms of the macrocyclic core, the secondary amine of the pendant arm and the nitrogen atom of the pyridine group of the fluorescent moiety, the latter bond being clearly weaker than the one with the pyridine of the macrocycle. Solution studies showed the formation of a highly stable Cu2+ complex with 1 : 1 stoichiometry, whereas with Zn2+ least stable complexes were…
COX-2 expression in chondrosarcoma: A role for celecoxib treatment?
2010
Chondrosarcomas are resistant to conventional chemo- and radiotherapy. A subset of chondrosarcomas arises secondarily in the benign tumour syndromes enchondromatosis (EC) and multiple osteochondromas (MO), and prevention of tumour development would greatly improve prognosis. We therefore investigated the effect of selective COX-2 inhibition on chondrosarcoma growth. COX-2 expression was studied in central- and peripheral cartilaginous tumours. The effect of COX-2 inhibition was assessed in four high-grade chondrosarcoma cell lines using celecoxib and NS-398 treatment. COX-2 activity (prostaglandin E-2 (PGE(2)) ELISA) and cell viability were measured. The (prophylactic) effect of celecoxib o…