Search results for "bisphosphonates."
showing 10 items of 66 documents
Mevolonate Pathway:role of bisphosphonates and statins
2006
Cardiovascular diseases, i.e. high blood pressure, coronary heart disease, and stroke, and osteoporosis are public health problems, with several epidemiological links, and they might be related to each other in terms of pathogenesis and therapeutic agents. Bisphosphonates inhibit bone resorption and are used in the treatment of osteoporosis, whereas statins inhibit cholesterol biosynthesis and are used for the treatment of atherosclerosis and lipid metabolic disorders. Some late clinical studies suggested bisphosphonates may have beneficial effect in vivo on atherosclerotic progression, lipid profiles, and cardiovascular morbidity and mortality, whereas statins might increase bone density, …
Mode of action of herbicidal derivatives of aminomethylenebisphosphonic acid. I. Physiologic activity and inhibition of anthocyanin biosynthesis
1996
N-Pyridylaminomethylenebisphosphonic acids constitute a class of promising herbicides. Since their mode of action at the cellular level is still poorly understood, we studied the influence of N-pyridylaminomethylenebisphosphonic acids on plant growth, at the whole plant and undifferentiated tissue levels, using seedlings and cell suspension cultures of mono- and dicotyledonous species. These compounds exhibited strong herbicidal properties, being equipotent with the popular herbicide glyphosate. Since they also depressed buckweed anthocyanin biosynthesis, the shikimate pathway could represent a site of action of N-pyridylaminomethylenebisphosphonic acids.
Bone targeting compounds for radiotherapy and imaging: *Me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid
2016
Background Bisphosphonates have a high adsorption on calcified tissues and are commonly used in the treatment of bone disorder diseases. Conjugates of bisphosphonates with macrocyclic chelators open new possibilities in bone targeted radionuclide imaging and therapy. Subsequent to positron emission tomography (PET) examinations utilizing 68Ga-labelled analogues, endoradiotheraphy with 177Lu-labelled macrocyclic bisphosphonates may have a great potential in the treatment of painful skeletal metastases. Methods Based on the established pharmaceuticals pamidronate and zoledronate two new DOTA-α-OH-bisphosphonates, DOTAPAM and DOTAZOL(MM1.MZ) were successfully synthesized. The ligands were labe…
CYP2C8 gene polymorphism and bisphosphonate-related osteonecrosis of the jaw in patients with multiple myeloma
2011
Osteonecrosis of the jaw is an uncommon but potentially serious complication of bisphosphonate therapy in multiple myeloma. Previous studies showed that the presence of one or two minor alleles of the cytochrome P450, subfamily 2C polypeptide 8 gene (CYP2C8) polymorphism rs1934951 was an independent prognostic marker associated with development of osteonecrosis of the jaw in multiple myeloma patients treated with bisphosphonates. The aim of this study was to validate the frequency of SNP rs193451 in 79 patients with multiple myeloma. In 9 (22%) patients developing osteonecrosis of the jaw, a heterozygous genotype was found, in contrast with those who did not develop osteonecrosis of the jaw…
Bisphosphonate prodrugs utilizing endogenous carriers
2016
Targeting of therapeutic agents to a specific site, as well as controlling the rate and time of release, has been intensively investigated and established over the last decades. These studies concerning drug delivery systems led to the formulation of several products that can improve the diffusion across the barriers after drug administration. For this purpose, the development of strategies of novel drug delivery systems for bisphosphonates had taken hold to improve both the bioavailability and safety. Firstly, they have been used for over a century in the branch of industry and later, in the 1960s, in medicine. Bisphosphonates are synthetic compound analogs to the naturally occurring pyrop…
Adverse drug reactions in the oral cavity
2012
Several drugs may have a number of adverse reactions (ADRs) involving the oro-facial region. The dose of the drug and the time required for the reaction to take place are relevant parameters; nonetheless, ADRs mechanisms are not always known and ADRs are not always predictable since aspects other than drug pharmacodynamics and/or pharmacokinetics, as well as various interacting variables contribute to the final outcome. All tissues and many functions of the oral cavity can be affected. In particular, salivary function is fre- quently involved and hypo-salivation is the main manifestation; several mucosal lesions with different morphology (ulcerations, vesiculo- bullous lesions, white lesion…
Osteonecrosis of the jaw after long-term oral bisphosphonates, followed by short-term denosumab treatment for osteoporosis: a case report
2014
Bisphosphonates and denosumab are antiresoptive agents and are mainly used for management of metastatic bone cancer, osteoporosis and other diseases. Bisphosphonates (BP) can reduce skeletal related events (SRE) by 30–50%1; denosumab (D) has been found even more effective than BP2. BP and D have been both associated to osteonecrosis of the jaw (ONJ). We report a case of an osteoporotic woman (62 yrs), complaining maxillary intense pain after a recent tooth molar extraction, observed in July 2013 at our centre. She mentioned previous treatments with monthly ibandronate (Bonviva ® 150 mg) per os (from January 2003 to April 2010), risedronate (35 mg weekly, from May 2010 to May 2012) and two a…
Osteonecrosis of the jaws by intravenous bisphosphonates and osteoradionecrosis : a comparative study
2009
Aims: We analyze the possible clinical differences between bone jaw exposed areas in ONJ (osteonecrosis of the jaws) and ORN (osteoradionecrosis). Patients and method: Group 1 was composed with 53 ONJ cases and group 2 with 20 ORN cases. In both groups we analyzed, the major size of the exposed bone areas, the number of exposed areas, the location on the jaws and the presence of others associated and severe complications, such as skin fistulas and jaw fractures. We also investigated the possible local aetiology or trigger factor of the lesions. Results: The major size of the bone exposed areas was 2.29±2.02(mean ± std.dev) in group 1 and 2.7±2.9 (mean ± std.dev) in group 2 (p>0.05). The num…
Criteria for the prescription of oral bisphosphonates for the treatment of osteoporosis in a series of women referred for tooth extraction
2012
Objective: To evaluate the criteria for the prescription of oral bisphosphonates (OB) in a series of women with osteoporosis referred for tooth extraction. Study design: The study included 38 postmenopausal women on treatment with OBs. The following variables were analysed: age, weight, height, type of OB and duration of treatment, bone densitometry and risk factors for osteoporosis. In addition, the osteoporosis self-assessment tool (OST) was administered and collagen type I C-telopeptide (CTX) levels were measured. Results: Bone densitometry had only been performed in six patients (15.7%) before starting OB treatment. Based on the results of the OST, nine (23.6%) of the participants prese…
Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocyte…
2008
A small series of aminobisphosphonates (N-BPs) structurally related to zoledronic acid was synthesized with the aim of improving activity toward activation of human gammadelta T cells and in turn their in vivo antitumor activity. The absence of the 1-OH moiety, together with the position and the different basicity of the nitrogen, appears crucial for antitumor activity. In comparison to zoledronic acid, compound 6a shows a greater ability to activate gammadelta T cells expression (100 times more) and a proapoptotic effect that is better than zoledronic acid. The potent activation of gammadelta T cells, in addition to evidence of the in vivo antitumor activity of 6a, suggests it may be a new…