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Alendronate

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https://www.readbyqxmd.com/read/28817072/efficient-transdermal-delivery-of-alendronate-a-nitrogen-containing-bisphosphonate-using-tip-loaded-self-dissolving-microneedle-arrays-for-the-treatment-of-osteoporosis
#1
Hidemasa Katsumi, Yutaro Tanaka, Kaori Hitomi, Shu Liu, Ying-Shu Quan, Fumio Kamiyama, Toshiyasu Sakane, Akira Yamamoto
To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogen-containing bisphosphonate, we developed self-dissolving microneedle arrays (MNs), in which ALN is loaded only at the tip portion of micron-scale needles by a dip-coating method (ALN(TIP)-MN). We observed micron-scale pores in rat skin just after application of ALN(TIP)-MN, indicating that transdermal pathways for ALN were created by MN. ALN was rapidly released from the tip of MNs as observed in an in vitro release study...
August 17, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28811200/globular-adiponectin-reverses-osteo-sarcopenia-and-altered-body-composition-in-ovariectomized-rats
#2
Shyamsundar Pal China, Subhashis Pal, Sourav Chattopadhyay, Konica Porwal, Sapana Kushwaha, Sharmishtha Bhattacharyya, Monika Mittal, Anagha A Gurjar, Tarun Barbhuyan, Abhishek K Singh, Arun K Trivedi, Jiaur R Gayen, Sabyasachi Sanyal, Naibedya Chattopadhyay
Adiponectin regulates various metabolic processes including glucose flux, lipid breakdown and insulin response. We recently reported that adiponectin receptor1 (adipoR1) activation by a small molecule reverses osteopenia in leptin receptor deficient db/db (diabetic) mice. However, the role of adiponectin in bone metabolism under the setting of post-menopausal (estrogen-deficiency) osteopenia and associated metabolic derangements has not been studied. Here, we studied the therapeutic effect of the globular form of adiponectin (gAd), which is predominantly an adipoR1 agonist, in aged ovariectomized (OVX) rats and compared it with standard-of-care anti-osteoporosis drugs...
August 12, 2017: Bone
https://www.readbyqxmd.com/read/28810648/combination-of-alendronate-and-genistein-synergistically-suppresses-osteoclastic-differentiation-of-raw267-4-cells-in-vitro
#3
Masayoshi Yamaguchi, Robert M Levy
Bone is a dynamic tissue that undergoes constant remodeling, with removal by osteoclastic bone resorption and replacement via osteoblastic bone formation and mineralization. Deterioration of bone mass with aging leads to osteoporosis. Bisphosphonates are potent inhibitors of osteoclastic bone resorption. Genistein, an isoflavone, exerts a bone anabolic effect by suppressing osteoclastic bone resorption and stimulating osteoblastic bone formation. The present study was undertaken to investigate the anabolic effects of a combination of alendronate and genistein on osteoclastic differentiation...
August 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28793342/risk-of-long-term-infection-related-death-in-clinical-osteoporotic-vertebral-fractures-a-hospital-based-analysis
#4
Ying-Chou Chen, Wei-Che Lin
BACKGROUND: Osteoporotic vertebral fractures adversely impact quality of life and also increase the risk of infection and mortality. Alendronate treatment increases bone mass and reduces the risk of fractures in patients with osteoporosis by suppressing bone resorption. We investigated the relationship between alendronate treatment and infection-related death in patients with osteoporotic vertebral fractures. METHODS: We retrospectively reviewed patients with osteoporosis and vertebral fractures from January 2001 to December 2007...
2017: PloS One
https://www.readbyqxmd.com/read/28793321/effects-of-combination-treatment-with-alendronate-and-raloxifene-on-skeletal-properties-in-a-beagle-dog-model
#5
Matthew R Allen, Erin McNerny, Mohammad Aref, Jason M Organ, Christopher L Newman, Brian McGowan, Tim Jang, David B Burr, Drew M Brown, Max Hammond, Paul R Territo, Chen Lin, Scott Persohn, Lei Jiang, Amanda A Riley, Brian P McCarthy, Gary D Hutchins, Joseph M Wallace
A growing number of studies have investigated combination treatment as an approach to treat bone disease. The goal of this study was to investigate the combination of alendronate and raloxifene with a particular focus on mechanical properties. To achieve this goal we utilized a large animal model, the beagle dog, used previously by our laboratory to study both alendronate and raloxifene monotherapies. Forty-eight skeletally mature female beagles (1-2 years old) received daily oral treatment: saline vehicle (VEH), alendronate (ALN), raloxifene (RAL) or both ALN and RAL...
2017: PloS One
https://www.readbyqxmd.com/read/28774501/synaptic-vesicle-2c-and-its-synaptic-related-function
#6
REVIEW
Yan-Wei Hu, Lei Xiao, Lei Zheng, Qian Wang
Synaptic vesicle 2 C (SV2C) is a novel isoform belonging to the synaptic vesicle 2 (SV2) protein superfamily; a family of proteins known to have roles in vesicle trafficking, exocytosis and neurotransmission. In humans, SV2C is expressed in evolutionarily older brain regions, and is a known receptor for botulinum neurotoxin/A (BoNT/A), controlling glucose-evoked granule recruitment and regulating dopamine release, thus serving as a potential target molecule in the treatment of psychosis. In addition, recent researches have shown that SV2C regulates hypertension and accelerates venous thromboembolism (VTE) and coagulation pathways and may play roles in several non-nervous system diseases...
July 31, 2017: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/28768046/carbon-monoxide-released-from-its-pharmacological-donor-tricarbonyldichlororuthenium-ii-dimer-corm-2-accelerates-the-healing-of-pre-existing-gastric-ulcers
#7
Magierowski Marcin, Magierowska Katarzyna, Hubalewska-Mazgaj Magdalena, Sliwowski Zbigniew, Ginter Grzegorz, Pajdo Robert, Chmura Anna, Kwiecien Slawomir, Brzozowski Tomasz
BACKGROUND AND PURPOSE: Carbon monoxide (CO), gaseous mediator produced by heme oxygenases (HO), has been shown to prevent stress-, ethanol-, aspirin- or alendronate-induced gastric damage, however, its role in the gastric ulcer healing has not been fully explained. We investigated whether CO released from tricarbonyldichlororuthenium (II) dimer (CORM-2) can affect gastric ulcer healing and determined mechanisms involved in healing action of this compound. EXPERIMENTAL APPROACH: Gastric ulcers were induced in Wistar rats by serosal application of acetic acid...
August 2, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28765912/disorder-of-the-mevalonate-pathway-inhibits-calcium-induced-differentiation-of-keratinocytes
#8
Rui Jin, Xin Luo, Kang Luan, Li Liu, Liang-Dan Sun, Sen Yang, Sheng-Quan Zhang, Xue-Jun Zhang
Mutation of genes encoding the enzymes of the mevalonate pathway cause a variety of diseases, including skin disorders. Mutation of four genes in this pathway, including mevalonate kinase, phosphomevalonate kinase, mevalonate diphosphate decarboxylase and farnesyl diphosphate synthase, have demonstrated to be responsible for porokeratosis (PK). However, the pathogenesis of PK remains unclear. In the present study, specific enzyme inhibitors of the mevalonate pathway, including pravastatin (PRA), alendronate (ALD), farnesyl transferase inhibitor (FTI‑277) and geranylgeranyl transferase inhibitor (GGTI‑298), were used to investigate the effect on differentiation of keratinocytes (KCs)...
August 1, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28755782/romosozumab-sclerostin-monoclonal-antibody-versus-teriparatide-in-postmenopausal-women-with-osteoporosis-transitioning-from-oral-bisphosphonate-therapy-a-randomised-open-label-phase-3-trial
#9
Bente L Langdahl, Cesar Libanati, Daria B Crittenden, Michael A Bolognese, Jacques P Brown, Nadia S Daizadeh, Eva Dokoupilova, Klaus Engelke, Joel S Finkelstein, Harry K Genant, Stefan Goemaere, Lars Hyldstrup, Esteban Jodar-Gimeno, Tony M Keaveny, David Kendler, Peter Lakatos, Judy Maddox, Jorge Malouf, Fabio E Massari, Jose Fernando Molina, Maria Rosa Ulla, Andreas Grauer
BACKGROUND: Previous bisphosphonate treatment attenuates the bone-forming effect of teriparatide. We compared the effects of 12 months of romosozumab (AMG 785), a sclerostin monoclonal antibody, versus teriparatide on bone mineral density (BMD) in women with postmenopausal osteoporosis transitioning from bisphosphonate therapy. METHODS: This randomised, phase 3, open-label, active-controlled study was done at 46 sites in North America, Latin America, and Europe...
July 26, 2017: Lancet
https://www.readbyqxmd.com/read/28744112/strontium-ranelate-treatment-in-a-postmenopausal-woman-with-osteonecrosis-of-the-jaw-after-long-term-oral-bisphosphonate-administration-a-case-report
#10
Whei-Lin Pan, Pi-Lun Chen, Cho-Ying Lin, Yi-Chun Pan, Yuh-Ren Ju, Chiu-Po Chan, Robert Ww Hsu
Bisphosphonates (BPs) suppress bone resorption and increase bone strength, thus reducing the risk of fracture. Oral BPs are widely used for the prevention and treatment of osteoporosis and osteopenia. Here, we describe the case of a postmenopausal woman who took oral alendronate for >3 years for osteoporosis. The patient presented at the clinic with sharp jaw pain and swelling on the left mandible 4 months after extraction of the third molar. Clinical examinations identified an inflamed mucosal opening with pus over an area of necrotic bone...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/28744102/bioequivalence-of-generic-alendronate-sodium-tablets-70-mg-to-fosamax-%C3%A2-tablets-70-mg-in-fasting-healthy-volunteers-a-randomized-open-label-three-way-reference-replicated-crossover-study
#11
Yifan Zhang, Xiaoyan Chen, Yunbiao Tang, Youming Lu, Lixia Guo, Dafang Zhong
PURPOSE: The aim of this study was to evaluate the bioequivalence of a generic product 70 mg alendronate sodium tablets with the reference product Fosamax(®) 70 mg tablet. MATERIALS AND METHODS: A single-center, open-label, randomized, three-period, three-sequence, reference-replicated crossover study was performed in 36 healthy Chinese male volunteers under fasting conditions. In each study period, the volunteers received a single oral dose of the generic or reference product (70 mg)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28743325/low-doses-of-simvastatin-potentiate-the-effect-of-sodium-alendronate-in-inhibiting-bone-resorption-and-restore-microstructural-and-mechanical-bone-properties-in-glucocorticoid-induced-osteoporosis
#12
Priscila L Sequetto, Reggiani V Gonçalves, Aloísio S Pinto, Maria G A Oliveira, Izabel R S C Maldonado, Tânia T Oliveira, Rômulo D Novaes
By using an experimental model of dexamethasone-induced osteoporosis we investigated the effects of different therapeutic schemes combining sodium alendronate (SA) and simvastatin on bone mineral and protein composition, microstructural and mechanical remodeling. Wistar rats were randomized into eight groups: G1: non-osteoporotic; G2: osteoporotic; G3, G4, and G5: osteoporotic+SA (0.2, 0.4, and 0.8 mg/kg, respectively); G6, G7, and G8: osteoporotic+SA (0.2, 0.4, and 0.8 mg/kg, respectively)+simvastatin (0.4, 0...
July 26, 2017: Microscopy and Microanalysis
https://www.readbyqxmd.com/read/28727345/-denosumab-in-clinical-practice-beware-before-during-and-after
#13
Olivier Lamy, Elena Gonzalez-Rodriguez, Delphine Stoll, Bérengère Aubry-Rozier
Denosumab is a very effective treatment of osteoporosis, easy to use and very well tolerated. Due to some associated risks, a close clinical follow-up is necessary. Before the first injection, it is necessary to correct hypocalcaemia or vitamin D deficiency when present. Calcemia has to be followed in case of renal insufficiency. Injections of denosumab should be done scrupulously every 6 months (± 3 weeks). Discontinuation of denosumab is associated with a severe rebound effect characterized by increased markers of bone remodeling, a rapid decrease of bone density values, and a risk of multiple spontaneous vertebral fractures...
April 19, 2017: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28725994/evaluation-of-the-effects-of-photobiomodulation-on-vertebras-in-two-rat-models-of-experimental-osteoporosis
#14
Mohammadjavad Fredoni, Mahdi Ghatrehsamani, Mohammad-Amin Abdollahifar, Sahar Bayat, Mohammad Bayat
The aim of this study was to evaluate the effects of photobiomodulation (PBM) on cancellous bone in rat models of ovariectomized induced osteoporosis (OVX-D) and glucocorticoid-induced osteoporosis (GIOP). The experiment comprised of nine groups. A group of healthy rats was used for baseline evaluations. The OVX-D rats were further divided into groups as follows: control rats with osteoporosis, OVX-D rats that received alendronate (1 mg/kg 60 days), OVX-D rats treated with pulsed wave laser (890 nm, 80 Hz, 900 s, 0...
July 19, 2017: Lasers in Medical Science
https://www.readbyqxmd.com/read/28719844/phosphate-functionalized-4-4-armchair-cnts-as-novel-drug-delivery-systems-for-alendronate-and-etidronate-anti-osteoporosis-drugs
#15
Zahra Nikfar, Zahra Shariatinia
The ability of (4,4)-armchair CNT and its three phosphate functionalized forms (CNT-nH2PO4, n=1-3) were evaluated as novel drug delivery systems (DDSs) for the two commercially well-known anti-osteoporosis drugs namely alendronate (AL) and etidronate (ET). For this purpose, the DFT calculations were accomplished at both B3LYP and B3PW91 levels using 6-31g(d) basis set. The binding energy was increased by increasing number of H2PO4 moieties attached on the CNT with the most negative binding energy was measured for the carrier containing three phosphate groups...
July 8, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28715470/impairment-of-cold-injury-induced-muscle-regeneration-in-mice-receiving-a-combination-of-bone-fracture-and-alendronate-treatment
#16
Shigeo Kawada, Atsushi Harada, Naohiro Hashimoto
Alendronate, a nitrogen-containing bisphosphonate, is well established as a treatment for osteoporosis through regulation of osteoclast activity. Previously, the pharmacological effects of bisphosphonates on cells outside the bone environment have been considered irrelevant because bisphosphonates target bone. Here we show that administration of alendronate impairs muscle regeneration in mice after bone fracture. A series of injections of alendronate alone or bone fracture alone did not affect muscle regeneration induced by cold injury...
2017: PloS One
https://www.readbyqxmd.com/read/28715463/potassium-citrate-prevents-increased-osteoclastogenesis-resulting-from-acidic-conditions-implication-for-the-treatment-of-postmenopausal-bone-loss
#17
Donatella Granchi, Elena Torreggiani, Annamaria Massa, Renata Caudarella, Gemma Di Pompo, Nicola Baldini
The extracellular acidic milieu in bones results in activation of osteoclasts (OC) and inhibition of osteoblasts (OB) causing a net loss of calcium from the skeleton and the deterioration of bone microarchitecture. Alkalinization through supplementation with potassium citrate (K citrate) has been proposed to limit the osteopenia progression, even though its pharmacological activity in bone microenvironment is not well defined. We evaluated if K citrate was able to prevent the adverse effects that acidic milieu induces on bone cells...
2017: PloS One
https://www.readbyqxmd.com/read/28714038/one-and-two-year-persistence-with-different-anti-osteoporosis-medications-a-retrospective-cohort-study
#18
C Reyes, C Tebe, D Martinez-Laguna, M S Ali, A Soria-Castro, C Carbonell, D Prieto-Alhambra
Adherence to anti-osteoporosis medications is poor. We carried out a cohort study using a real-world population database to estimate the persistence of anti-osteoporosis drugs. Unadjusted 2-year persistence ranged from 10.3 to 45.4%. Denosumab users had a 40% lower risk of discontinuation at 2 years compared to alendronate users. PURPOSE: The purpose of this study was to estimate real-world persistence amongst incident users of anti-osteoporosis medications. METHODS: This is a retrospective cohort using data from anonymised records and dispensation data ( www...
July 16, 2017: Osteoporosis International
https://www.readbyqxmd.com/read/28704906/the-therapeutic-effects-of-combination-therapy-with-curcumin-and-alendronate-on-spine-fusion-surgery-in-the-ovariectomized-rats
#19
Dae-Chul Cho, Kyoungsu Ryu, Kyoung-Tae Kim, Joo-Kyung Sung
OBJECTIVE: The purpose of this study was to evaluate the therapeutic effects of combination therapy with curcumin and alendronate on spine fusion surgery in ovariectomized rats. METHODS: Thirty-two female Sprague-Dawley rats (12 weeks old) underwent bilateral ovariectomy (OVX). Eight weeks after surgery, animals underwent intertransverse spine fusion at L4-5. The rats were randomly distributed amongst 4 groups; untreated OVX group, curcumin administered group, alendronate administered group, and the combination therapy group...
June 2017: Korean Journal of Spine
https://www.readbyqxmd.com/read/28699744/design-synthesis-and-pharmacokinetics-of-a-bone-targeting-dual-action-prodrug-for-treatment-of-osteoporosis
#20
Haibo Xie, Gang Chen, Robert N Young
A dual-action bone-targeting prodrug has been designed, synthesized and evaluated for in vitro and in vivo metabolic stability and in vivo tissue distribution, and rates of release of the active constituents after binding to bones through the use of differentially double labelled derivatives. The conjugate (general structure 7) embodies the merger of a very potent and proven anabolic selective agonist of the prostaglandin EP4 receptor, compound 5, and alendronic acid, a potent inhibitor of bone resorption, optimally linked through a differentially hydrolyzable linker unit, N-4-carboxymethylphenyl-methyloxycarbonyl-leucinyl-argininyl-para-aminophenylmethylalcohol (Leu-Arg-PABA)...
July 12, 2017: Journal of Medicinal Chemistry
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