Methylnaltrexone Mechanisms of Action and Effects on Opioid Bowel Dysfunction and Other Opioid Adverse Effects

2007 ◽  
Vol 41 (6) ◽  
pp. 984-993 ◽  
Author(s):  
Chun-Su Yuan

OBJECTIVE: To review the mechanisms of action of methylnaltrexone and its effects on opioid bowel dysfunction, as well as its effects on other opioid-induced adverse effects (ADEs), and its potential roles in clinical practice. DATA SOURCES: A literature search using the MEDLINE and Cochrane Collaboration databases for articles published between 1966 and March 2007 was performed. Additional data sources were obtained from manual searches of recent journal articles, book chapters, and monographs. An updated literature search showed no additional publications. STUDY SELECTION AND DATA EXTRACTION: Abstracts and original preclinical and clinical research reports published in the English language were identified for review. Review articles, commentaries, and news reports of this compound were excluded. Literature related to opioids, opioid receptors, opioid antagonists, methylnaltrexone, opioid-induced bowel dysfunction, constipation, nausea, and vomiting was evaluated and selected based on consideration of the support shown for the proof of concept, mechanistic findings, and timeliness. Fifty-eight original articles from preclinical studies and clinical trials using methylnaltrexone were identified. Pharmacologic action, benefits, and ADEs of methylnaltrexone were reviewed, with a focus on its effects on bowel dysfunction after opioids. Emphases were placed on its receptor binding activities and therapeutically relevant sites of action (peripheral vs central), in which peripheral opioid receptors in the body contribute to physiological and drug-induced effects. DATA SYNTHESIS: Morphine and related opioids are associated with a number of limiting ADEs, including opioid-induced bowel dysfunction. Methylnaltrexone, a quaternary derivative of naltrexone, blocks peripheral effects of opioids while sparing central analgesic effects. It is currently under late-stage clinical investigation for the treatment of opioid-induced constipation in patients with advanced illness. Reported results showed the drug to be generally well-tolerated. The rapid reversal of constipation is very encouraging. Hastening postoperative discharge may also be possible. CONCLUSIONS: Methylnaltrexone has the potential to prevent or treat opioid-induced peripherally mediated ADEs on bowel dysfunction without interfering with central analgesia. The study of methylnaltrexone leads to a greater understanding of the mechanisms of action of opioid pharmacology.

Author(s):  
Ganesh Kumar Y ◽  
Pranitha D ◽  
Phaneendra D ◽  
Madhava Reddy Ch

Various types of conditions exist in the body that causes fever and pain. Drugs that are used to treat fever are called antipyretics, and those are usually prescribed to treat elevated body temperature. But those drugs result in many other side effects like ulcers, perforations, bleedings and obstructions, which make their use questionable and limiting. Medicinal plants are used in the treatment of diseases from the starting of the human race and the process; they had been subjected to rigorous investigations and tests to establish a scientific proof and validation of the various pharmacological activities and their respective mechanisms of action in treating the herbs. Considering the anti-inflammatory properties of the plant, Xylocarpus mekongesis was investigated for its antipyretic activity in yeast method and 3doses out of which 00mg/kg body weight showed a better activity compared to the standard drug and other extracts too. The mechanism of action was similar to the paracetamol action that is inhibition of prostaglandin synthesis.


2018 ◽  
Vol 24 (14) ◽  
pp. 1533-1550 ◽  
Author(s):  
Jong-Eun Kim ◽  
Ki Won Lee

Skin is a protective organ and the largest of the human body. Due to its pivotal role in aesthetic appearance, skin health has a significant impact on quality of life. Chronic inflammation of the skin often marks the beginning of various skin diseases. Immune-mediated responses serve to protect the body from external insults and require succinct control, and can lead to ongoing cellular damage and various skin conditions if left unchecked. Studies have shown that phytochemicals can alter processes involved in skin inflammation and alleviate the effects of aging, cancer, atopic dermatitis, psoriasis, and vitiligo. Direct molecular targets of some phytochemicals have been identified and their precise mechanisms of action investigated. In this review, we summarize recent findings on the effects of phytochemicals on skin inflammation and the mechanisms of action involved.


2019 ◽  
Vol 16 (3) ◽  
pp. 251-258 ◽  
Author(s):  
Javad Behravan ◽  
Atefeh Razazan ◽  
Ghazal Behravan

Breast cancer is the second leading cause of cancer death among women. National cancer institute of the US estimates that one in eight women will be diagnosed with breast cancer during their lifetime. Considering the devastating effects of the disease and the alarming numbers many scientists and research groups have devoted their research to fight breast cancer. Several recommendations are to be considered as preventing measures which include living a healthy lifestyle, regular physical activity, weight control and smoking cessation. Early detection of the disease by annual and regular mammography after the age of 40 is recommended by many healthcare institutions. This would help the diagnosis of the disease at an earlier stage and the start of the treatment before it is spread to other parts of the body. Current therapy for breast cancer includes surgical ablation, radiotherapy and chemotherapy which is often associated with adverse effects and even may lead to a relapse of the disease at a later stage. In order to achieve a long-lasting anticancer response with minimal adverse effects, development of breast cancer vaccines is under investigation by many laboratories. The immune system can be stimulated by a vaccine against breast cancer. This approach has attracted a great enthusiasm in recent years. No breast cancer vaccines have been approved for clinical use today. One breast cancer vaccine (NeuVax) has now completed clinical trial phase III and a few preventive and therapeutic breast cancer vaccines are at different steps of development. We think that with the recent advancements in immunotherapy, a breast cancer vaccine is not far from reach.


2019 ◽  
Vol 15 (2) ◽  
pp. 102-108 ◽  
Author(s):  
Rashmi Saxena Pal ◽  
Yogendra Pal ◽  
Pranay Wal

Background: Postpartum is an important phase of life after childbirth. It needs to be highly important as in terms of health in future life. This time brings lots of complications with it. Lots of aspects need to be looked after as the care of the new mom is essential to bring back her stamina and strength. Objective: The objective of this review article is to explore the heeding power hidden in nature for returning back to the mothers to the pre-pregnancy state. There are various areas of concern after postpartum to heal up the body overall, such as to heal up the uterus, providing galactagogues, nutritives, maintenance of hormones and restoring back the strength and tone of the abdomen. Materials and Methods: A literature search has been done on the various herbs, which fulfill the various desired aspects to be looked after post pregnancy. Results: There are various herbs present in nature, regarding their hidden potential still the awareness is not up to the mark. This review highlights the various plants which have been proven to be useful in dealing the post-pregnancy issues. They deal with all the aspects of complications and issues occurring post pregnancy. They heal the uterus which has undergone so many types of changes, maintains the balance of hormones back, besides providing nutrition and increasing the production of milk, they also restore back the tone and strength of the walls of the abdomen. Conclusion: These herbs are full-fledged with the phytoconstituents that heal the whole system after delivery. The need of present time is to take patiently these as the source of medicines regularly under medical supervision to overcome the various concerned problems of post pregnancy.


2020 ◽  
Vol 26 (1) ◽  
Author(s):  
Vivek Sharma ◽  
Avinash P. S. Thakur ◽  
Vasantharaja Ramasamy ◽  
Pushpendra Kumar Shukla ◽  
Fanindra Singh Solanki ◽  
...  

Abstract Background Urothelial bladder carcinoma accounts for around 3.9% cases of all the male cancers in India. Non-muscle-invasive bladder carcinoma (NMIBC) is predominant group which constitute approximately three fourth of the urothelial bladder cancer. Intravesical BCG immunotherapy is the corner stone of today’s NMIBC management. However, as with any other therapy it has its own complications and its interruption due to these adverse effects is a major cause of suboptimal efficacy. The aim of this study was to assess the complications of intravesical BCG therapy and their management in NMIBC patients. Methods This was a retrospective descriptive study conducted between October 2016 and November 2019; a backward review of 149 patients with diagnosis of NMIBC that undergone intravesicle BCG therapy was performed. Patient’s demographical, clinical, diagnostic and procedural data regarding bladder tumour, BCG therapy, its complications and management were collected and analysed. Results Total 149 patients were analysed, comprising 116 males and 33 females. The mean age was of 57.2 ± 6.7 years. Total 85.23% were primary and 14.76% were recurrent tumours. Total 96 patients (64.42%) completed the planned course, while 53 (35.57%) interrupted. The reasons for BCG interruption includes adverse effects (15.4%), progression of disease (6.7%), disease refractory to BCG (4.6%) and disease recurrence during BCG (3.3%). Most of the adverse events occurred in first 6 months and most interruptions occurred after the induction period. Cystitis was the most common observed adverse effect seen in 39.6% patients. Frequency, urgency, haematuria were common presentation. Radical cystectomy was the most common (16.10%) further treatment with patients whose treatment was interrupted. Conclusion BCG is an indispensable therapy available for NMIBC, but it is associated with array of adverse effects and complications, which are the main reasons for poor compliance to BCG therapy. Although BCG-related complications can affect any organ in the body, potentially life-threatening systemic BCG-related infections are encountered in only < 5% of patients. There are some difficulties in diagnosis of the BCG complications because acid-fast staining, culture and PCR test are not always positive; tissue biopsies should be indicated sometimes to evaluate histopathology and presence of M. bovis. A persistently monitored multidisciplinary approach with high index of suspicion and prompt anti-TB therapy can help to derive the maximum benefits while keeping the complications at check.


2003 ◽  
Vol 37 (2) ◽  
pp. 268-273 ◽  
Author(s):  
Robert J Cersosimo

OBJECTIVE: To review data on the use of tamoxifen for primary prevention of breast cancer. DATA SOURCES: A literature search was performed through MEDLINE (1992–May 2002) using the key words tamoxifen, breast cancer, and prevention. DATA SYNTHESIS: Breast cancer is the most common malignancy detected in American women. Attempts to reduce morbidity and mortality include early detection programs and chemoprevention. Clinical trials of tamoxifen for reduction of breast cancer risk are reviewed. CONCLUSIONS: Tamoxifen may reduce the risk of primary breast cancer in women at increased risk. The benefit of tamoxifen in women who are not at risk is uncertain. The risks of developing thromboembolic disorders or endometrial cancer must be considered before tamoxifen is prescribed. Women should be given all of the information about the benefits and risks of tamoxifen use so that they can make an informed decision based on the best data available.


Author(s):  
L. L. Zakharova ◽  
◽  
G. A. Zhorov ◽  
V. N. Obryvin ◽  
◽  
...  

The article presents the results of laboratory studies of the effect of sorption-detoxifying means on the accumulation of 90Sr in the body of white rats. The efficiency of a number of selective and polyfunctional sorbents, detoxicants and other biologically active substances and the developed on their basis sorption-detoxifying complexes as means of efferent therapy and detoxification of the animal body at the combined intake of xenobiotics of radiation and chemical nature was evaluated. It was found that 90Sr cumulation in bones (at the level of 53,3–60,8%) was reduced to the greatest extent with the combined use of substances of different mechanisms of action and origin. The effectiveness of separate use of detoxifying drugs did not exceed 29,1%.


2015 ◽  
Vol 12 (1) ◽  
pp. 54-59
Author(s):  
L V Luss

In the pathogenesis of various diseases histamine performs an important role relating to one of the most important mediators involved in the regulation of vital functions in the body. Histamine plays a key role in the development of allergic diseases and pseudoallergic reactions. Therefore, in clinical practice, of particular interest are drugs that block the effects of histamine - antihistamines. The lecture highlights mechanisms of action of histamine and indications for antihistamines. Particular attention is given to parenteral forms of antihistamines and benefits of a new form of antihistamines for parenteral use without sedation - fenkarol one of quinuclidine derivatives. Features and advantages of antihistamines - quinuclidine derivatives, first developed in Laboratory of academician M.D. Mashkovsky are presented.


2020 ◽  
Vol 1 (1) ◽  
pp. 44-50
Author(s):  
Anak Agung Ngurah Adhi Wibisana ◽  
I Made Sepud ◽  
I Made Minggu Widyantara

Indonesia has a law on education, namely Law No. 14 of 2005 on Teachers and Lecturers. In its implementation, there is a case that causes pros and cons to the statement of every article of the Teacher and Lecturer Law, especially in relation to the right to defend oneself in criminal acts of persecution. The purpose of this research is to know the arrangement of teaching methods for students during the learning process and to know the criminal sanctions against teachers who abuse students during the learning process. This study uses a normative method with the main data sources namely laws and regulations. The results showed that the element of an act, and / or the result of an act, pain in the body, and injuries to the body contained in Article 351 paragraph (1) of the Criminal Code refers to the Teacher and Lecturer Law, namely in Article 77 paragraph (6). This article defines the basis of persecution, namely actions that cause pain to a person. The criminal act of persecution in the world of education, at least, must be considered with the intention of disciplining and educating the nation's life.


2021 ◽  
Vol 11 ◽  
Author(s):  
Andi Zhang ◽  
Tianyuan Zou ◽  
Dongye Guo ◽  
Quan Wang ◽  
Yilin Shen ◽  
...  

As a stressor widely existing in daily life, noise can cause great alterations to the immune system and result in many physical and mental disorders, including noise-induced deafness, sleep disorders, cardiovascular diseases, endocrine diseases and other problems. The immune system plays a major role in maintaining homeostasis by recognizing and removing harmful substances in the body. Many studies have shown that noise may play vital roles in the occurrence and development of some immune diseases. In humans, both innate immunity and specific immunity can be influenced by noise, and different exposure durations and intensities of noise may exert various effects on the immune system. Short-term or low-intensity noise can enhance immune function, while long-term or high-intensity noise suppresses it. Noise can lead to the occurrence of noise-induced hearing loss (NIHL) through the production of autoantibodies such as anti-Hsp70 and anti-Hsp60 and exert adverse effects related to other immune-related diseases such as some autoimmune diseases and non-Hodgkin lymphoma. The neuroendocrine system, mainly including the hypothalamic-pituitary-adrenal (HPA) axis and the sympathetic-adrenal-medullary (SAM) system, is involved in the mechanisms of immune-related diseases induced by noise and gut microbiota dysfunction. In addition, noise exposure during pregnancy may be harmful to the immune system of the fetus. On the other hand, some studies have shown that music can improve immune function and alleviate the adverse effects caused by noise.


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