scholarly journals Opioid-induced gastrointestinal side effects, the role of naldemedine in their therapy

Ból ◽  
2020 ◽  
Vol 21 (2) ◽  
pp. 54-58
Author(s):  
Jarosław Woroń ◽  
Jerzy Wordliczek
Keyword(s):  
Gastrointestinal Tract ◽  
Side Effects ◽  
Therapeutic Option ◽  
Opioid Analgesics ◽  
Gastrointestinal Disorders ◽  
Pharmacodynamic Profile ◽  
Negative Effect ◽  
Gastrointestinal Side Effects ◽  
Effective Drugs

Although opioid analgesics are highly effective in the treatment of pain, one of the main disadvantages of their use is their negative effect on the functioning of the gastrointestinal tract. Opioid-induced side effects include a variety of symptoms known as opioid gastrointestinal disorders (OIBD). One of the effective drugs used in OIBD is naldemedine, which, due to its pharmacokinetic and pharmacodynamic profile and safety profile, is currently the optimal therapeutic option.

The increasing challenge of the possible impact of ethnicity on psychopharmacology

CNS Spectrums ◽  
2020 ◽  
pp. 1-10
Author(s):  
Donatella Marazziti ◽  
Federico Mucci ◽  
Maria T. Avella ◽  
Laura Palagini ◽  
Marly Simoncini ◽  
...  
Keyword(s):  
Side Effects ◽  
Ethnic Differences ◽  
Therapeutic Option ◽  
Side Effect Profile ◽  
Limited Data ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Cultural Stereotypes ◽  
Intrinsic Factors ◽  
Psychopharmacological Treatment

Abstract Ethnic differences may significantly influence the outcome of psychopharmacological treatment, in terms of prescription, adherence, clinical response, emergence of side effects, as well as pharmacokinetics and pharmacodynamics. The purpose of this review was to explore the available literature in order to provide general suggestions to help clinicians in choosing the best therapeutic option for patients, taking into account ethnicity. Although findings are sometimes controversial, the overall published studies suggest that ethnicities other than Caucasians tend to show a lower response to antidepressants and a reduced compliance. Africans tend to be more prescribed with antipsychotics, probably due to cultural stereotypes, except with clozapine, probably for their chronic benign neutropenia. Asians usually require less antipsychotic dosages than Caucasians. The differential response and side effect profile of antidepressants and antipsychotics have been related to individual intrinsic factors, to genetic make-up, but also to cultural and contextual variables. Interestingly, albeit limited data suggest ethnic-related genetic heterogeneity at the level of the serotonin transporters, the cytochromes and some neuroreceptors. Taken together, no conclusive findings are available about the role and impact of ethnicity in psychopharmacology. One of the main problems is that the majority of the studies in psychopharmacology have been conducted on Caucasians, so that there is an urgent need to have data in other populations. Furthermore, in the era of precision medicine, the role of ethnicity may be also supported by genetic analysis.

The role of oxycodone/naloxone in pain management

Ból ◽  
2017 ◽  
Vol 17 (4) ◽  
pp. 26-40
Author(s):  
Magdalena Kocot-Kępska ◽  
Renata Zajączkowska ◽  
Anna Przeklasa-Muszyńska ◽  
Jan Dobrogowski
Keyword(s):  
Side Effects ◽  
Pain Treatment ◽  
Treatment Options ◽  
Analgesic Efficacy ◽  
Opioid Analgesics ◽  
Bowel Dysfunction ◽  
Prolonged Release ◽  
Gastrointestinal Side Effects ◽  
Strong Opioids ◽  
Pain Patients

ABSTRACT: Strong opioid analgesics are essential for pain treatment of moderate to severe intensity, regardless of its etiology. An important factor limiting safety and efficacy of opioids are side effects, particularly gastrointestinal. Constipation as part of opioid induced bowel dysfunction is one of the most common reason for discontinuation of strong opioids. Introduction of novel oxycodone/naloxone formulation is an attempt to resolve the problem of opioid induced gastrointestinal side effects. On the basis of clinical trials from 2008-2016 the authors discuss the applicability of oxycodone/naloxone prolonged release in management of different pain syndromes in humans, in cancer patients, in neuropathic pain patients, in the elderly, in acute post-operative pain and other clinical indications for example restless leg syndrome. Presented data indicate comparable or in some cases even better analgesic efficacy of oxycodone with naloxone and lower risk of gastrointestinal side effects, especially constipation, when compared to other strong opioids. The introduction of oxycodone with naloxone significantly expands treatment options for chronic pain patients, likewise improving safety and thus the effectiveness of treatment with strong opioids.

scholarly journals Infection of Human Cells by SARS-CoV-2 and Molecular Overview of Gastrointestinal, Neurological, and Hepatic Problems in COVID-19 Patients

2021 ◽  
Vol 10 (21) ◽  
pp. 4802
Author(s):  
Mahdie Rahban ◽  
Agata Stanek ◽  
Amirreza Hooshmand ◽  
Yasaman Khamineh ◽  
Salma Ahi ◽  
...  
Keyword(s):  
Gastrointestinal Tract ◽  
Angiotensin Converting Enzyme ◽  
Intestinal Permeability ◽  
Molecular Mechanisms ◽  
External Environment ◽  
Gastrointestinal Disorders ◽  
Converting Enzyme ◽  
Angiotensin Converting Enzyme 2 ◽  
Liver Infection

The gastrointestinal tract is the body’s largest interface between the host and the external environment. People infected with SARS-CoV-2 are at higher risk of microbiome alterations and severe diseases. Recent evidence has suggested that the pathophysiological and molecular mechanisms associated with gastrointestinal complicity in SARS-CoV-2 infection could be explained by the role of angiotensin-converting enzyme-2 (ACE2) cell receptors. These receptors are overexpressed in the gut lining, leading to a high intestinal permeability to foreign pathogens. It is believed that SARS-CoV-2 has a lesser likelihood of causing liver infection because of the diminished expression of ACE2 in liver cells. Interestingly, an interconnection between the lungs, brain, and gastrointestinal tract during severe COVID-19 has been mentioned. We hope that this review on the molecular mechanisms related to the gastrointestinal disorders as well as neurological and hepatic manifestations experienced by COVID-19 patients will help scientists to find a convenient solution for this and other pandemic events.

Gastrin, Nitric Oxide Synthase and their Role in Ulceration and Distention of Stomach after Cisplatin and Taxol Treatment

1997 ◽  
Vol 3 (S2) ◽  
pp. 85-86
Author(s):  
Ying Wang ◽  
Surinder K. Aggarwal
Keyword(s):  
Side Effects ◽  
Chemotherapeutic Agent ◽  
Severe Nausea ◽  
Smooth Muscle Contractility ◽  
Anti Cancer ◽  
Gastrointestinal Side Effects ◽  
Cancer Agent ◽  
Oxide Synthase ◽  
Head Neck

Cisplatin, a potent broad spectrum anti-cancer agent, has been proven effective in the treatment of different kinds of cancer, such as bladder, lung, ovarian, head, neck, etc.. Drawbacks of this chemotherapeutic drug are its toxic side-effects, which include severe nausea, vomiting, stomach distention and peptic ulcer.Taxol is another effective chemotherapeutic agent which is usually used in conjection with cisplatin. It has demonstrated impressive activity in breast, ovarian, lung, and head and neck cancers. The toxic side-effects include nausea, vomiting, nephrotoxicity. The mechanism of these gastrointestinal side-effects are still unclear. Because of the role of NOS and gastrin on stomach smooth muscle contractility and gastroprotection, these were studied in the rats after cisplatin and taxol administration.Wistar rats(100-150 g) were injected with cisplatin(9 mg/kg) and taxol(20 mg/kg) in five divided dosages over a period of 5 days. Rats were killed one day after the last injection. Rat stomach tissues were fixed in Bouin’s solution and processed for light microscopy.

scholarly journals Non-vitamin K Antagonist Oral Anticoagulants and Drug-Food Interactions: Implications for Clinical Practice and Potential Role of Probiotics and Prebiotics

2022 ◽  
Vol 8 ◽  
Author(s):  
Ana Sánchez-Fuentes ◽  
José Miguel Rivera-Caravaca ◽  
Raquel López-Gálvez ◽  
Francisco Marín ◽  
Vanessa Roldán
Keyword(s):  
Clinical Practice ◽  
Vitamin K ◽  
Potential Role ◽  
Therapeutic Option ◽  
Vitamin K Antagonists ◽  
Oral Anticoagulants ◽  
Vitamin K Antagonist ◽  
Pharmacodynamic Profile ◽  
Potential Interactions

Non-vitamin K antagonist oral anticoagulants (NOACs) are a therapeutic option to prevent stroke in patients with atrial fibrillation (AF). In fact, NOACs have become the recommended choice by international clinical practice guidelines over vitamin K antagonists (VKA), because of their efficacy and safety profile, especially in newly initiated patients. The more predictable pharmacokinetic and pharmacodynamic profile of this family of drugs allows preventing anticoagulation drug monitoring. Furthermore, NOACs have significantly fewer drug and food interactions in comparison with VKAs. Despite this, there are no studies that compare the effects on the quality of anticoagulation of NOACs with the intake of potential interactions drugs of P-glycoprotein and cytochrome P450 (CYP). This review brings an overview of NOACs pharmacokinetics profile and their potential drug-food interactions. We also briefly discuss the potential role of prebiotics and probiotics in patients under therapy with NOACs.

scholarly journals A review on five medicinal plants considering the therapeutic potentials in the management of COVID-19

2020 ◽  
Author(s):  
Fahad Jubayer ◽  
Shahidullah Kayshar ◽  
Anisur Rahman Mazumder ◽  
Syeda Sabrina Akter
Keyword(s):  
Clinical Trials ◽  
Side Effects ◽  
Medicinal Plants ◽  
Therapeutic Option ◽  
Pharmacological Properties ◽  
Specific Effects ◽  
Control Options ◽  
Life Threatening ◽  
Working Mechanisms

The spread of pandemic coronavirus disease-2019 has become a health emergency worldwide. Since the unprecedented outbreak, attention has been raised worldwide to develop and research for control options and treatments. Although several clinical trials are ongoing, no registered drugs or vaccines are available yet. As situation warrants for the exploration of a successful antiviral, there should be a search for the remedies in nature also. Medicinal plants and their metabolites have long been used as a treatment option for various life-threatening diseases with minimal or no side effects. Thus this review aims to summarize previous outcomes concerning the role of medicinal plants in treating several life-threatening diseases. Above all, this work intends to find the constituents of five selected medicinal plants and their possible working mechanisms in the management of COVID-19. Constituents of the presented medicinal plants possess excellent pharmacological properties, including significant antiviral and antimicrobial potential. Based on the traditional uses, pharmacological properties, and previous studies, these medicinal plants mentioned in this review can be considered as a possible therapeutic option for the management and treatment of COVID-19. However, further extensive researches and trials are suggested to discover specific effects and dosage for this pathogenic outbreak.

A Reappraisal of the Role of Chlorambucil in Patients with End Stage Ovarian Cancer Who Have Previously been Treated with Platinum Regimens

2000 ◽  
Vol 45 (2) ◽  
pp. 51-53 ◽  
Author(s):  
K.S. McCully ◽  
G.V. Narayansingh ◽  
G.P. Cumming ◽  
T.K. Sarkar ◽  
D.E. Parkin
Keyword(s):  
Ovarian Cancer ◽  
Side Effects ◽  
Epithelial Ovarian Cancer ◽  
Therapeutic Option ◽  
Median Number ◽  
Younger Women ◽  
Platinum Based Chemotherapy ◽  
End Stage

The role of chlorambucil in end stage platinum resistant epithelial ovarian cancer was evaluated in women with end stage ovarian cancer. They had received platinum based chemotherapy and all other intravenous chemotherapeutic options had been exhausted. Over a 15 year period, 30 patients were identified. The median age was 64.5 years (range 45–81). The median number of chlorambucil pulses was 4 (range 1–16). The median survival following the introduction of chlorambucil was 5.5 months (range 0.72 – 38.8). The 22 patients who survived for longer than three months were significantly younger than those who did not (p= 0.03). Apart from two patients who developed transient myelosupression there were no toxic side effects. Chlorambucil should be considered as a therapeutic option in end stage ovarian cancer. It is has minimal toxicity, and can be prescribed safely for long term use. In younger women, an increase in benefit may be anticipated.

scholarly journals Impact of Gastrointestinal Side Effects on Patients’ Reported Quality of Life Trajectories after Radiotherapy for Prostate Cancer: Data from the Prospective, Observational Pros-IT CNR Study

Cancers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 1479
Author(s):  
Marianna Noale ◽  
Alessio Bruni ◽  
Luca Triggiani ◽  
Michela Buglione ◽  
Filippo Bertoni ◽  
...  
Keyword(s):  
Quality Of Life ◽  
Prostate Cancer ◽  
Side Effects ◽  
Los Angeles ◽  
Therapeutic Option ◽  
National Research Council ◽  
Bowel Function ◽  
Cancer Data ◽  
Gastrointestinal Side Effects

Radiotherapy (RT) represents an important therapeutic option for the treatment of localized prostate cancer. The aim of the current study is to examine trajectories in patients’ reported quality of life (QoL) aspects related to bowel function and bother, considering data from the PROState cancer monitoring in ITaly from the National Research Council (Pros-IT CNR) study, analyzed with growth mixture models. Data for patients who underwent RT, either associated or not associated with androgen deprivation therapy, were considered. QoL outcomes were assessed over a 2-year period from the diagnosis, using the Italian version of the University of California Los Angeles-Prostate Cancer Index (Italian-UCLA-PCI). Three trajectories were identified for the bowel function; having three or more comorbidities and the use of 3D-CRT technique for RT were associated with the worst trajectory (OR = 3.80, 95% CI 2.04–7.08; OR = 2.17, 95% CI 1.22–3.87, respectively). Two trajectories were identified for the bowel bother scores; diabetes and the non-Image guided RT method were associated with being in the worst bowel bother trajectory group (OR = 1.69, 95% CI 1.06–2.67; OR = 2.57, 95% CI 1.70–3.86, respectively). The findings from this study suggest that the absence of comorbidities and the use of intensity modulated RT techniques with image guidance are related with a better tolerance to RT in terms of bowel side effects.

scholarly journals Improved Safety and Anti-Glioblastoma Efficacy of CAT3-Encapsulated SMEDDS through Metabolism Modification

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 484
Author(s):  
Hongliang Wang ◽  
Lin Li ◽  
Jun Ye ◽  
Wujun Dong ◽  
Xing Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Side Effects ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lymphatic Transport ◽  
Pharmacokinetic Parameters ◽  
Gastrointestinal Side Effects ◽  
The Brain

13a-(S)-3-pivaloyloxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (CAT3) is a novel oral anti-glioma pro-drug with a potent anti-tumor effect against temozolomide-resistant glioma. 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (PF403) is the active in vivo lipase degradation metabolite of CAT3. Both CAT3 and PF403 can penetrate the blood–brain barrier to cause an anti-glioma effect. However, PF403, which is produced in the gastrointestinal tract and plasma, causes significant gastrointestinal side effects, limiting the clinical application of CAT3. The objective of this paper was to propose a metabolism modification for CAT3 using a self-microemulsifying drug delivery system (SMEDDS), in order to reduce the generation of PF403 in the gastrointestinal tract and plasma, as well as increase the bioavailability of CAT3 in vivo and the amount of anti-tumor substances in the brain. Thus, a CAT3-loaded self-microemulsifying drug delivery system (CAT3-SMEDDS) was prepared, and its physicochemical characterization was systematically carried out. Next, the pharmacokinetic parameters of CAT3 and its metabolite in the rats’ plasma and brain were measured. Furthermore, the in vivo anti-glioma effects and safety of CAT3-SMEDDS were evaluated. Finally, Caco-2 cell uptake, MDCK monolayer cellular transfer, and the intestinal lymphatic transport mechanisms of SMEDDS were investigated in vitro and in vivo. Results show that CAT3-SMEDDS was able to form nanoemulsion droplets in artificial gastrointestinal fluid within 1 min, displaying an ideal particle size (15–30 nm), positive charge (5–9 mV), and controlled release behavior. CAT3-SMEDDS increased the membrane permeability of CAT3 by 3.9-fold and promoted intestinal lymphatic transport. Hence, the bioavailability of CAT3 was increased 79% and the level of its metabolite, PF403, was decreased to 49%. Moreover, the concentrations of CAT3 and PF403 were increased 2–6-fold and 1.3–7.2-fold, respectively, in the brain. Therefore, the anti-glioma effect in the orthotopic models was improved with CAT3-SMEDDS compared with CAT3 in 21 days. Additionally, CAT3-SMEDDS reduced the gastrointestinal side effects of CAT3, such as severe diarrhea, necrosis, and edema, and observed less inflammatory cell infiltration in the gastrointestinal tract, compared with the bare CAT3. Our work reveals that, through the metabolism modification effect, SMEDDS can improve the bioavailability of CAT3 and reduce the generation of PF403 in the gastrointestinal tract and plasma. Therefore, it has the potential to increase the anti-glioma effect and reduce the gastrointestinal side effects of CAT3 simultaneously.

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