Do we need sex-oriented clinical practice guidelines for the treatment of schizophrenia?
Purpose of review Clinical practice guidelines (CPGs) do not usually offer a sex-specific approach for the management of schizophrenia. With this narrative review, we aim to give an integrated and synthesized overview of the current state of knowledge regarding sex-specific aspects in schizophrenia and how this topic may be adapted in the development of CPGs. Recent findings Recent studies further suggest sex-specific differences in epidemiologic features, the course of illness, underlying pathomechanisms, response likelihood to antipsychotic medication and differences in tolerability. Beyond this, selective estrogen ...
Source: Current Opinion in Psychiatry - April 7, 2020 Category: Psychiatry Tags: SCHIZOPHRENIA AND RELATED DISORDERS: Edited by Lynn E. DeLisi and Iris E.C. Sommer Source Type: research

“if i had known, i wouldn’t have come”: implications and challenges of qualitative interview
This article aimed to discuss the challenges for the researcher in the use of the qualitative interview and possible implications for the interviewed. Our analysis, based on excerpts from interviews drawn from different research projects, focused on two aspects: 1. The relationship between researcher and participant, and 2. Possible implications for the interviewee. We argue that the researcher-participant intersubjective field constitutes the interview, with contextual variability and influences that preclude the possibility of complete control of the process by the investigator, conferring an active role to both interact...
Source: Psicologia em Estudo - March 17, 2020 Category: Psychiatry & Psychology Source Type: research

In-situ forming chitosan implant-loaded with raloxifene hydrochloride and bioactive glass nanoparticles for treatment of bone injuries: Formulation and biological evaluation in animal model
Publication date: Available online 9 March 2020Source: International Journal of PharmaceuticsAuthor(s): Fatma S. Abdel-Salam, Seham A. Elkheshen, Azza A. Mahmoud, Emad B. Basalious, Mohammed S. Amer, Amany A. Mostafa, Nermeen A. Elkasabgy (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 11, 2020 Category: Drugs & Pharmacology Source Type: research

Effect of Raloxifene on Bone Formation Around Implants in the Osteoporotic Rat Maxilla: Histomorphometric and Microcomputed Tomographic Analysis.
CONCLUSION: The results show that raloxifene administration demonstrated enhanced new peri-implant bone formation in the osteoporotic rat maxilla. Further research is needed to reveal the effect of raloxifene on the clinical outcome of patients with poor bone quality who undergo dental implant treatment. PMID: 32142560 [PubMed - as supplied by publisher] (Source: International Journal of Oral and Maxillofacial Implants)
Source: International Journal of Oral and Maxillofacial Implants - March 7, 2020 Category: ENT & OMF Tags: Int J Oral Maxillofac Implants Source Type: research

A matrix dispersion based on phospholipid complex system: preparation, lymphatic transport, and pharmacokinetics.
Authors: Li H, Lu S, Luo M, Li X, Liu S, Zhang T Abstract Raloxifene hydrochloride (RH) suffers from low oral bioavailability due to its low water-solubility and first-pass metabolism. Therefore, a novel phospholipid complex of RH (RHPC) and a matrix dispersion based on phospholipid complex (RHPC-MD) were successfully prepared and optimized. Several methods were used to validate the formation of RHPC and RHPC-MD, such as differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, transmission electron microscopy, infrared spectroscopy, particle size, and zeta potential, meanwhile, their octa...
Source: Drug Development and Industrial Pharmacy - March 6, 2020 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Raloxifene administration enhances retention in an orthodontic relapse model.
Abstract BACKGROUND AND OBJECTIVES: Orthodontic relapse is a physiologic process that involves remodelling of the alveolar bone and principle periodontal ligament fibres. Raloxifene is an Food and Drug Administration (FDA)-approved selective oestrogen receptor modulator that inhibits systemic bone loss. In our study, we examined the effects of Raloxifene on alveolar bone modelling and orthodontic relapse in a rodent model. MATERIALS AND METHODS: The efficacy of raloxifene was evaluated in 15-week-old male Wistar rats, 8 in each group (Control, Raloxifene, Raloxifene + 7-day relapse, Raloxifene + 14-day relaps...
Source: European Journal of Orthodontics - February 17, 2020 Category: Dentistry Authors: Azami N, Chen PJ, Mehta S, Kalajzic Z, Dutra EH, Nanda R, Yadav S Tags: Eur J Orthod Source Type: research

Raloxifene Potentiates The Effect Of Fluoxetine Against Maximal Electroshock Induced Seizures In Mice.
Abstract The evidence to guide clinicians regarding rationale polytherapy with current antiepileptic drugs (AEDs) is lacking, and current practice recommendations are largely empirical.  The excessive drug loading with combinatorial therapies of existing AEDs are associated with escalated neurotoxicity, and that emergence of pharmacoresistant seizures couldn't be averted. In pursuit of judicious selection of novel AEDs in combinatorial therapies with mechanism based evidences, standardized dose of raloxifene, fluoxetine, bromocriptine and their low dose combinations, were experimentally tested for their impac...
Source: European Journal of Pharmaceutical Sciences - February 12, 2020 Category: Drugs & Pharmacology Authors: Pottoo FH, Tabassum N, Javed MN, Nigar S, Sharma S, Barkat MA, Harshita, Alam MS, Ansari MA, Barreto GE, Ashraf GM Tags: Eur J Pharm Sci Source Type: research

Proton pump inhibitors enhance chemosensitivity, promote apoptosis, and suppress migration of breast cancer cells.
In conclusion, the addition of PPIs to the treatment regimen of breast cancer appears to be a promising strategy to potentiate the efficacy of chemotherapy and may suppress cancer metastasis. PMID: 31955147 [PubMed - in process] (Source: Acta Pharmaceutica)
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Ihraiz WG, Ahram M, Bardaweel SK Tags: Acta Pharm Source Type: research

Antiviral activity of sertindole, raloxifene and ibutamoren against transcription and replication-competent Ebola virus-like particles.
Abstract A chemical library comprising 2,354 drug-like compounds was screened using a transcription and replication-competent virus-like particle (trVLP) system that implements the whole Ebola virus (EBOV) life cycle. Dose-dependent inhibition of Ebola trVLP replication was induced by 15 hit compounds, which target different kinds of G protein-coupled receptors (GPCRs) mainly. Based on the chemical structures, they were divided into three groups, diphenylmethane derivatives, promazine derivatives or without any core skeletons. Within the third group, sertindole, raloxifene, and ibutamoren showed prominent antivira...
Source: BMB Reports - January 21, 2020 Category: Biochemistry Authors: Yoon YS, Jang Y, Hoenen T, Shin H, Lee Y, Kim M Tags: BMB Rep Source Type: research

Sequential Treatment of Estrogen Deficient, Osteopenic Rats with Alendronate, Parathyroid Hormone (1 –34), or Raloxifene Alters Cortical Bone Mineral and Matrix Composition
AbstractAnti-resorptive and anabolic treatments can be used sequentially to treat osteoporosis, but their effects on bone composition are incompletely understood. Osteocytes may influence bone tissue composition with sequential therapies because bisphosphonates diffuse into the canalicular network and anabolic treatments increase osteocyte lacunar size. Cortical bone composition of osteopenic, ovariectomized (OVX) rats was compared to that of Sham-operated rats and OVX rats given monotherapy or sequential regimens of single approved anti-osteoporosis medications. Adult female Sprague –Dawley rats were OVX (N =...
Source: Calcified Tissue International - November 29, 2019 Category: Orthopaedics Source Type: research

NewsCAP: The USPSTF recommends tamoxifen, raloxifene, or aromatase inhibitors for women at high breast cancer risk.
Authors: PMID: 31764039 [PubMed - in process] (Source: The American Journal of Nursing)
Source: The American Journal of Nursing - November 27, 2019 Category: Nursing Tags: Am J Nurs Source Type: research

NewsCAP: The USPSTF recommends tamoxifen, raloxifene, or aromatase inhibitors for women at high breast cancer risk.
No abstract available (Source: AJN)
Source: AJN - November 25, 2019 Category: Nursing Tags: In the News Source Type: research

Effects of raloxifene on cognition in postmenopausal women with schizophrenia: a 24-week double-blind, randomized, parallel, placebo-controlled trial.
Authors: Huerta-Ramos E, Labad J, Cobo J, Núñez C, Creus M, García-Parés G, Cuadras D, Franco J, Miquel E, Reyes JC, Marcó-García S, RALOPSYCAT Group, Usall J Abstract We assessed the utility of raloxifene (60 mg/day) as an adjuvant treatment for cognitive symptoms in postmenopausal women with schizophrenia in a 24-week, double-blind, randomized, placebo-controlled study. Patients were recruited from the inpatient and outpatient services of Parc Sanitari Sant Joan de Déu, Hospital Universitari Institut Pere Mata, and Corporació Sanitària Parc Taul&...
Source: European Archives of Psychiatry and Clinical Neuroscience - November 16, 2019 Category: Psychiatry Tags: Eur Arch Psychiatry Clin Neurosci Source Type: research

Pulmonary delivery alters the disposition of raloxifene in rats
ConclusionsPulmonary administration improved the bioavailability of raloxifene and further increased the distribution on the target organ (bone), with no obvious impact on its excretory pattern. (Source: Journal of Pharmacy and Pharmacology)
Source: Journal of Pharmacy and Pharmacology - November 15, 2019 Category: Drugs & Pharmacology Authors: Ying Kong, Hui Cai, Han Xing, Chang Ren, Dexuan Kong, Chen Ning, Ning Li, Di Zhao, Xijing Chen, Yang Lu Tags: Research Paper Source Type: research

Effects of raloxifene on cognition in postmenopausal women with schizophrenia: a 24-week double-blind, randomized, parallel, placebo-controlled trial
AbstractWe assessed the utility of raloxifene (60  mg/day) as an adjuvant treatment for cognitive symptoms in postmenopausal women with schizophrenia in a 24-week, double-blind, randomized, placebo-controlled study. Patients were recruited from the inpatient and outpatient services of Parc Sanitari Sant Joan de Déu, Hospital Universitari Institut Pere Mata, and Corporació Sanitària Parc Taulí. Seventy eight postmenopausal women with schizophrenia were randomized to either adjunctive raloxifene or placebo. Sixty-eight began the clinical trial (37 women on raloxifene adjunct) and 31 on p...
Source: European Archives of Psychiatry and Clinical Neuroscience - November 14, 2019 Category: Neuroscience Source Type: research

[Osteoporosis: long-term treatment versus drug holiday-what is the evidence?]
Abstract The occurrence of multiple vertebral fractures after discontinuation of denosumab in the treatment of osteoporosis has reopened the debate on the optimal treatment duration and drug holidays.In principle, there is a difference in this regard between the discontinuation of medications such as bisphosphonates and substances without bone retention such as selective estrogen receptor modulators (SERMs), denosumab or teriparatide. Even after the end of application bisphosphonates have a very long half-life in the bones. After cessation of drug intake there is a slow, slight increase of bone turnover marke...
Source: Zeitschrift fur Rheumatologie - October 25, 2019 Category: Rheumatology Authors: Farahmand P, Cassens J Tags: Z Rheumatol Source Type: research

Benefits and harms of selective oestrogen receptor modulators (SERMs) to reduce breast cancer risk: a cross-sectional study of methods to communicate risk in primary care.
CONCLUSION: Specific risk formats may lead to more women considering taking SERMs to reduce breast cancer risk, especially if they are at high risk of the condition. Raloxifene may be a more acceptable SERM to patients. PMID: 31636127 [PubMed - as supplied by publisher] (Source: The British Journal of General Practice)
Source: The British Journal of General Practice - October 21, 2019 Category: Primary Care Authors: McIntosh JG, Minshall J, Saya S, Bickerstaffe A, Hewabandu N, Qama A, Emery JD Tags: Br J Gen Pract Source Type: research

Bisphosphonates for Postmenopausal Osteoporosis
This JAMA Women ’s Health summarizes evidence-based use of bisphosphonates for fracture prevention in women with postmenopausal osteoporosis, and reviews potential harms of the drugs and alternative agents (denosumab, raloxifene) for patients with contraindications or intolerance to alendronate, risedronate, or z oledronate. (Source: JAMA - Journal of the American Medical Association)
Source: JAMA - Journal of the American Medical Association - October 17, 2019 Category: General Medicine Source Type: research

Fibromyalgia, sleep disturbance and menopause: Is there a relationship? A literature review
ConclusionFurther studies are needed to elucidate the nature of the association between menopause, sleep and persistent pain syndromes, such as FM, showing the role of hormone therapy in prospective placebo ‐controlled trials. (Source: International Journal of Rheumatic Diseases)
Source: International Journal of Rheumatic Diseases - October 14, 2019 Category: Rheumatology Authors: Rejane Camila Alvarenga Dias, Jaime Kulak Junior, Eloise Hayde ê Ferreira da Costa, Renato Mitsunori Nisihara Tags: REVIEW Source Type: research

Tissue Distribution and Systemic Toxicity Evaluation of Raloxifene Targeted Polymeric Micelles of Poly (Styrene-Maleic Acid)-Poly (Amide-Ether-Ester-Imide)-Poly (Ethylene Glycol) Loaded With Docetaxel in Breast Cancer Bearing Mice.
CONCLUSION: The results indicate that RA-conjugated polymeric micelles may be a strong and effective drug delivery system for DTX therapy and uptake of drug into tumor cells, and overcome the disadvantages and side effects of conventional DTX. PMID: 31538904 [PubMed - as supplied by publisher] (Source: Recent Patents on Anti-Cancer Drug Discovery)
Source: Recent Patents on Anti-Cancer Drug Discovery - September 22, 2019 Category: Cancer & Oncology Tags: Recent Pat Anticancer Drug Discov Source Type: research

Phospholipid-based complex of raloxifene with enhanced biopharmaceutical potential: Synthesis, characterization and preclinical assessment
Publication date: Available online 17 September 2019Source: International Journal of PharmaceuticsAuthor(s): Atul Jain, Sumant Saini, Rajendra Kumar, Teenu Sharma, Rajan Swami, Om Prakash Katare, Bhupinder SinghGraphical Abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

Long lasting in-situ forming implant loaded with raloxifene HCl: An injectable delivery system for treatment of bone injuries
This study aimed to prepare novel liquid lipid-based PLGA-IFI loaded with raloxifene hydrochloride for prolonged non-surgical treatment of bone injuries by applying solvent-induced phase inversion technique. Labrasol® and Maisine® were added to the selected IFI forming long lasting lipid-based IFI (LLL-IFI). The formulations were characterized by analysing their in-vitro drug release, solidification time, injectability, rheological properties, and DSC in addition to their morphological properties. Results revealed that the LLL-IFI composed of 10%w/v PLGA with a lactide to glycolide ratio of 75:25 with ester termina...
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

Amelioration of visual deficits and visual system pathology after mild TBI via the cannabinoid Type-2 receptor inverse agonism of raloxifene.
Abstract Visual deficits after traumatic brain injury (TBI) are common, but interventions that limit the post-trauma impairments have not been identified. We have found that treatment with the cannabinoid type-2 receptor (CB2) inverse agonist SMM-189 for 2 weeks after closed-head blast TBI greatly attenuates the visual deficits and retinal pathology this otherwise produces in mice, by modulating the deleterious role of microglia in the injury process after trauma. SMM-189, however, has not yet been approved for human use. Raloxifene is an FDA-approved estrogen receptor drug that is used to treat osteoporosis, bu...
Source: Experimental Neurology - September 10, 2019 Category: Neurology Authors: Honig MG, Del Mar NA, Henderson DL, Ragsdale TD, Doty JB, Driver JH, Li C, Fortugno AP, Mitchell WM, Perry AM, Moore BM, Reiner A Tags: Exp Neurol Source Type: research

Breast cancer chemoprevention: An update on current practice and opportunities for primary care physicians
Publication date: Available online 5 September 2019Source: Preventive MedicineAuthor(s): Somedeb Ball, Meily Arevalo, Edna Juarez, J. Drew Payne, Catherine JonesAbstractSeveral risk assessment models have been validated for the estimation of risk of breast cancer in women. Chemoprevention through hormonal therapy is an effective way to reduce the incidence of breast cancer in women with high risk. Selective estrogen receptor modulators, tamoxifen and raloxifene, are approved for this indication by the United States Food and Drug Administration, and aromatase inhibitors have also shown promise in recent studies. These medic...
Source: Preventive Medicine - September 7, 2019 Category: International Medicine & Public Health Source Type: research

USPSTF Recommendation: Medications to Reduce Risk of Breast Cancer
This 2019 Recommendation Statement from the US Preventive Services Task Force recommends that clinicians offer tamoxifen, raloxifene, or aromatase inhibitors to women at increased risk for breast cancer and at low risk for adverse medication effects (B recommendation) and recommends against routine use of such medications in women not at increased risk for breast cancer (D recommendation). (Source: JAMA)
Source: JAMA - September 3, 2019 Category: General Medicine Source Type: research

USPSTF Evidence Report: Medications for Risk Reduction of Primary Breast Cancer in Women
This systematic review to support the 2019 US Preventive Services Task Force Recommendation Statement on medication use for breast cancer risk reduction summarizes published evidence on the benefits and harms of tamoxifen, raloxifene, and aromatase inhibitors used to reduce risk of primary invasive breast cancer in women. (Source: JAMA)
Source: JAMA - September 3, 2019 Category: General Medicine Source Type: research

Medications to Reduce Breast Cancer Risk
Breast cancer is diagnosed among more than a quarter of a million women in the United States each year. Tamoxifen, raloxifene, and aromatase inhibitors can reduce women ’s risk of developing breast cancer. With so many women at risk for breast cancer, these drugs have the potential to substantially affect public health. In this issue of JAMA, the US Preventive Services Task Force (USPSTF) reports updated recommendations regarding use of these medications. The tas k force recommends that clinicians “offer to prescribe risk-reducing medications, such as tamoxifen, raloxifene, or aromatase inhibitors, to women who...
Source: JAMA - September 3, 2019 Category: General Medicine Source Type: research

Use of Endocrine Therapy for Breast Cancer Risk Reduction: ASCO Clinical Practice Guideline Update.
Abstract PURPOSE: To update the ASCO guideline on pharmacologic interventions for breast cancer risk reduction and provide guidance on clinical issues that arise when deciding to use endocrine therapy for breast cancer risk reduction. METHODS: An Expert Panel conducted targeted systematic literature reviews to identify new studies. RESULTS: A randomized clinical trial that evaluated the use of anastrozole for reduction of estrogen receptor-positive breast cancers in postmenopausal women at increased risk of developing breast cancer provided the predominant basis for the update. UPDATED RECOMMENDATIO...
Source: Clinical Genitourinary Cancer - September 3, 2019 Category: Cancer & Oncology Authors: Visvanathan K, Fabian CJ, Bantug E, Brewster AM, Davidson NE, DeCensi A, Floyd JD, Garber JE, Hofstatter EW, Khan SA, Katapodi MC, Pruthi S, Raab R, Runowicz CD, Somerfield MR Tags: J Clin Oncol Source Type: research

Raloxifene inhibits adipose tissue inflammation and adipogenesis through Wnt regulation in ovariectomized rats and 3  T3-L1 cells
Loss of ovarian function, as in menopause or after ovariectomy (OVX), is closely associated with obesity and white adipose tissue (WAT) inflammation. Estrogen replacement protects against postmenopausal obesit... (Source: Journal of Biomedical Science)
Source: Journal of Biomedical Science - August 31, 2019 Category: Biomedical Science Authors: Hsin-Hsueh Shen, Chien-Yi Yang, Ching-Wen Kung, Shu-Ying Chen, Hong-Min Wu, Pao-Yun Cheng, Kwok-Keung Lam and Yen-Mei Lee Tags: Research Source Type: research

The Impact of Hormonal Replacement Treatment in Postmenopausal Women with Uterine Fibroids: A State-of-the-Art Review of the Literature.
Conclusions: For women with uterine fibroids, the choice of the most appropriate HRT regimen is crucial to avoid leiomyomas growth and the symptoms possibly related to it. Available data are conflicting, but suggest that uterine fibroids might be influenced by HRT, without representing an absolute contraindication to hormonal replacement therapy. Women with uterine fibroids subjected to HRT should be periodically examined and hormonal treatment should be discontinued if leiomyomas appear to increase in size. Moreover, the minimal effective dose of progestin should be employed. PMID: 31480288 [PubMed - in process] (Sou...
Source: Medicina (Kaunas) - August 30, 2019 Category: Universities & Medical Training Authors: Moro E, Degli Esposti E, Borghese G, Manzara F, Zanello M, Raimondo D, Gava G, Arena A, Casadio P, Meriggiola MC, Seracchioli R Tags: Medicina (Kaunas) Source Type: research

A rational search for discovering potential neutraligands of human complement fragment 5a (hC5a).
Abstract The human complement fragment 5a (hC5a) is an extremely potent proinflammatory glycoprotein, which upon binding to C5aR triggers a plethora of immune and non-immunological responses in humans. Dysregulation of complement system is associated with the upregulation of hC5a, leading to the surge of proinflammatory cytokines, which further exacerbate the chronic inflammation induced pathological conditions. Thus, hC5a is considered as a major pharmacological target for developing complement therapeutics that can directly or indirectly modulate the function of hC5a. However, the idea of small molecules, direct...
Source: Bioorganic and Medicinal Chemistry - August 19, 2019 Category: Chemistry Authors: Mishra R, Rana S Tags: Bioorg Med Chem Source Type: research

Laboratory evaluation of secondary causes of bone loss in Veterans with spinal cord injury and disorders
ConclusionsScreening for secondary causes of osteoporosis, particularly for hypogonadism and hypovitaminosis D, should be considered in patients with a SCI/D. (Source: Osteoporosis International)
Source: Osteoporosis International - August 13, 2019 Category: Orthopaedics Source Type: research

Cost-effectiveness of antiosteoporosis strategies for postmenopausal women with osteoporosis in China
Conclusion: From the perspective of the Chinese medical system, zoledronate is more cost-effective than the calcium/vitamin D strategy, alendronate, raloxifene, and teriparatide for the treatment of osteoporosis in elderly postmenopausal women. Not factoring the parameters of adherence and persistence in, and consequent variability in treatment effectiveness relative risks, seems like a major limitation, but it can be speculated that it would not change the conclusion that zoledronate is the most economical strategy. (Source: Menopause)
Source: Menopause - August 1, 2019 Category: OBGYN Tags: Original Articles Source Type: research

Comparative efficacy and safety of pharmacological interventions for osteoporosis in postmenopausal women: a network meta-analysis (Chongqing, China)
Conclusions: Abaloparatide and teriparatide are most efficacious in preventing new vertebral and nonvertebral fractures in postmenopausal women with osteoporosis, whereas zoledronic acid and romosozumab are in preventing clinical fractures. Meanwhile, there is no statistical difference between abaloparatide, teriparatide or romosozumab, and placebo in terms of safety. Furthermore, in terms of adverse events, zoledronic acid is statistically worse than placebo, and two of the best interventions are denosumab and romosozumab, of which denosumab also reduces the risk of different kinds of fractures. (Source: Menopause)
Source: Menopause - August 1, 2019 Category: OBGYN Tags: Review Articles Source Type: research

New promising avenue for the simvastatin combination with residronate, strontium ranelate and raloxifene in experimentally-induced osteoporosis
Publication date: Available online 24 July 2019Source: The Egyptian RheumatologistAuthor(s): Amira K. Khalifa, Sohier A. Diab, Ghada M. Hashem, Essam F. Alalkamy, Mira F. YacoubAbstractAim of the workThis is the first experimental study to assess the possible synergistic effects of simvastatin combination with residronate, strontium ranelate and raloxifene on glucocorticoid induced osteoporosis (GIO) in female albino rats.Materials and methods48 mature healthy female albino rats were randomly allocated into 6 main groups (8 rats /group) and received all drugs daily orally for 6 weeks. (G1) negative control group; (G2) os...
Source: The Egyptian Rheumatologist - July 25, 2019 Category: Rheumatology Source Type: research

Raloxifene Retards Cartilage Degradation and Improves Subchondral Bone Micro-architecture in Ovariectomized Rats with Patella Baja-Induced- Patellofemoral Joint Osteoarthritis
This study was performed to evaluate the efficacy of RAL on patella baja-induced patellofemoral joint OA (PFJOA) in an ovariectomized rat model. (Source: Osteoarthritis and Cartilage)
Source: Osteoarthritis and Cartilage - July 18, 2019 Category: Rheumatology Authors: M.-J. Bei, F.-M. Tian, Y.-P. Xiao, X.-H. Cao, N. Liu, Z.-Y. Zheng, M.-W. Dai, W.-Y. Wang, H.-P. Song, L. Zhang Source Type: research

BIND, a novel analytical approach for monitoring powder adhesion at the die wall with use of the surface replication method
Publication date: Available online 27 June 2019Source: International Journal of PharmaceuticsAuthor(s): Shinichi Saito, Takashi Osamura, Hiroaki Kikuoka, Tadatsugu Tanino, Satomi OnoueAbstractTableting failure due to binding is often caused by powder adhesion to the die wall. The present study was undertaken to develop a novel approach for analyzing the binding characteristics of various formulations and manufacturing methods, named “Binding Identification for Net Detriment” (BIND). Binding characteristics with raloxifene hydrochloride as a model preparation were evaluated by visual observation, ejection force ...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

The selective estrogen receptor modulator raloxifene mitigates the effect of all-trans-retinal toxicity in photoreceptor degeneration [Signal Transduction]
The retinoid cycle is a metabolic process in the vertebrate retina that continuously regenerates 11-cis-retinal (11-cisRAL) from the all-trans-retinal (atRAL) isomer. atRAL accumulation can cause photoreceptor degeneration and irreversible visual dysfunction associated with incurable blinding retinal diseases, such as Stargardt disease, retinitis pigmentosa (RP), and atrophic age-related macular degeneration (AMD). The underlying cellular mechanisms leading to retinal degeneration remain uncertain, although previous studies have shown that atRAL promotes calcium influx associated with cell apoptosis. To identify compounds ...
Source: Journal of Biological Chemistry - June 14, 2019 Category: Chemistry Authors: Tamar Getter, Susie Suh, Thanh Hoang, James T. Handa, Zhiqian Dong, Xiuli Ma, Yuanyuan Chen, Seth Blackshaw, Krzysztof Palczewski Tags: Molecular Bases of Disease Source Type: research

Production of a new platform based on fumed and mesoporous silica nanoparticles for enhanced solubility and oral bioavailability of raloxifene HCl
The purpose of the present study was to compare mesoporous and fumed silica nanoparticles (NPs) to enhance the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RH). Mesoporous silica NPs (MSNs) and fumed silica NPs were used by freeze-drying or spray-drying methods. MSNs were obtained with different ratios of cetyltrimethylammonium bromide. Saturation solubility of the NPs was compared with the pure drug. The optimised formulation was characterised by scanning electron microscopy (SEM), X-ray diffraction (XRD) and differential scanning calorimetry. The pharmacokinetic studies were done by oral admin...
Source: IET Nanobiotechnology - June 11, 2019 Category: Nanotechnology Source Type: research

Effect of Raloxifene Administration on Bone Response Around Implant in the Maxilla of Osteoporotic Rats
Conclusion: Raloxifene showed increased bone formation around implant. This might have clinical implications in prosthetic restoration by dental implants for patients with poor bone quality. (Source: Implant Dentistry)
Source: Implant Dentistry - May 30, 2019 Category: Dentistry Tags: Basic and Clinical Research Source Type: research

SERMs: past and present
SERMs are selective estrogen receptor modulators. Actually, clomiphene citrate was the first SERM, although for all practical purposes, tamoxifen, introduced in the late 1970's, is thought of as the first SERM. It results in increased survival and disease-free survival in women with breast cancer. It is the most widely prescribed anti-neoplastic drug worldwide. It has some untoward effects in the uterus and venous system. It is approved for breast cancer prevention as well. Raloxifene is approved for prevention and treatment of osteoporosis as well as breast cancer prevention. (Source: Maturitas)
Source: Maturitas - May 14, 2019 Category: Primary Care Authors: Steven Goldstein Tags: INV50 Source Type: research

Incidence of venous thromboembolism (VTE) among postmenopausal women prescribed ospemifene, selective oestrogen receptor modulators (SERM), or untreated vulvar and vaginal atrophy
Ospemifene is a non-steroidal selective oestrogen receptor modulator (SERM) for moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy (VVA) due to menopause. An ongoing EU post-authorization safety study estimated the incidence of venous thromboembolism (VTE) in a cohort of postmenopausal women prescribed ospemifene, other SERM (raloxifene, bazedoxifene, or tamoxifen, for non-cancer indications), or untreated VVA. (Source: Maturitas)
Source: Maturitas - May 14, 2019 Category: Primary Care Authors: Bin Cai, Beth Nordstrom, Yuki Yoshida, Nafeesa Dhalwani, Fabio De Gregorio, Trevor Gibbs Tags: P36 Source Type: research

Romosozumab (Evenity) for Postmenopausal Osteoporosis
Date: June 3, 2019 Issue #:  1573Summary:  The FDA has approved romosozumab-aqqg (Evenity– Amgen), a sclerostin inhibitor, for once-monthly subcutaneous (SC) treatment of osteoporosis in postmenopausal women who are at high risk for fracture (history of osteoporotic fracture or multiple risk factors for fracture) or who have failed or cannot tolerate other drugs for this indication. R omosozumab is the first sclerostin inhibitor to be approved in the US and the third drug for treatment of postmenopausal osteoporosis that stimulates bone formation; the parathyroid hormone (PTH) receptor ag...
Source: The Medical Letter - May 1, 2019 Category: Drugs & Pharmacology Authors: admin Tags: abaloparatide Aclasta Actonel Alendronate Atelvia Binosto Bisphosphonates Boniva Denosumab Evenity Evista Forteo Fosamax Fosavance Ibandronate Osteoporosis Postmenopausal osteoporosis Prolia Raloxifene Reclast rised Source Type: research

Estrogen Modulates Cartilage and Subchondral Bone Remodeling in an Ovariectomized Rat Model of Postmenopausal Osteoarthritis.
CONCLUSIONS In an ovariectomized rat model of postmenopausal OA, estrogen deficiency resulted in resorption of subchondral bone and degeneration of articular cartilage. PMID: 31031401 [PubMed - in process] (Source: Medical Science Monitor)
Source: Medical Science Monitor - May 1, 2019 Category: Research Tags: Med Sci Monit Source Type: research

Risk-reducing medications for primary breast cancer: a network meta-analysis.
CONCLUSIONS: For women with an above-average risk of developing breast cancer, CPAs can reduce the incidence of this disease. AIs appear to be more effective than SERMs (tamoxifen) in reducing the risk of developing breast cancer. AIs are not associated with an increased risk of endometrial cancer and thromboembolic events. However, long-term data on toxicities from tamoxifen are available while the follow-up toxicity data on unaffected women taking AIs is relatively short. Additional data from direct comparisons are needed to fully address the issues of breast cancer prevention by risk-reducing medications, with special r...
Source: Cochrane Database of Systematic Reviews - April 29, 2019 Category: General Medicine Authors: Mocellin S, Goodwin A, Pasquali S Tags: Cochrane Database Syst Rev Source Type: research

In Vitro Metabolism by Aldehyde Oxidase Leads to Poor Pharmacokinetic Profile in Rats for c-Met Inhibitor MET401
ConclusionsThese results indicate that the main metabolic pathway of MET401 is AO-mediated metabolism, which leads to poor in vivo pharmacokinetic profiles in rodents. The deuterium substitution strategy could be used to reduce AO-mediated metabolism liability. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - April 27, 2019 Category: Drugs & Pharmacology Source Type: research

Long-Term Drug Therapy and Drug Discontinuations and Holidays for Osteoporosis Fracture Prevention: A Systematic Review.
Conclusion: Long-term alendronate and zoledronic acid therapies reduce fracture risk in women with osteoporosis. Long-term bisphosphonate treatment may increase risk for rare adverse events, and continuing treatment beyond 3 to 5 years may reduce risk for vertebral fractures. Long-term hormone therapy reduces hip fracture risks but has serious harms. Primary Funding Source: National Institutes of Health and Agency for Healthcare Research and Quality. (PROSPERO: CRD42018087006). PMID: 31009947 [PubMed - as supplied by publisher] (Source: Annals of Internal Medicine)
Source: Annals of Internal Medicine - April 23, 2019 Category: Internal Medicine Authors: Fink HA, MacDonald R, Forte ML, Rosebush CE, Ensrud KE, Schousboe JT, Nelson VA, Ullman K, Butler M, Olson CM, Taylor BC, Brasure M, Wilt TJ Tags: Ann Intern Med Source Type: research

Impacts of Psychological Stress on Osteoporosis: Clinical Implications and Treatment Interactions
Ryan R. Kelly1,2†, Lindsay T. McDonald1,2†, Nathaniel R. Jensen1,2, Sara J. Sidles1,2 and Amanda C. LaRue1,2* 1Research Services, Ralph H. Johnson VA Medical Center, Charleston, SC, United States 2Department of Pathology and Laboratory Medicine, Medical University of South Carolina, Charleston, SC, United States The significant biochemical and physiological effects of psychological stress are beginning to be recognized as exacerbating common diseases, including osteoporosis. This review discusses the current evidence for psychological stress-associated mental health disorders as risk factors for os...
Source: Frontiers in Psychiatry - April 9, 2019 Category: Psychiatry Source Type: research

Raloxifene decreases cell viability and migratory potential in prostate cancer cells (LNCaP) with GPR30/GPER1 involvement
ConclusionsRaloxifene was able to modulate GPER1 in LNCaP prostate tumour cells, decreasing cell viability and their migratory potential. (Source: Journal of Pharmacy and Pharmacology)
Source: Journal of Pharmacy and Pharmacology - March 28, 2019 Category: Drugs & Pharmacology Authors: Giovanna Cassone Salata, Cristiane Figueiredo Pinho, Andr é T. A. G. Freitas, Ariana Musa Aquino, Luis Antonio Justulin, Leonardo Oliveira Mendes, Bianca F. Gonçalves, Flávia Karina Delella, Wellerson Rodrigo Scarano Tags: Research Paper Source Type: research