New Opioids

2014 ◽  
Vol 32 (16) ◽  
pp. 1671-1676 ◽  
Author(s):  
Sebastiano Mercadante ◽  
Giampiero Porzio ◽  
Vittorio Gebbia

Despite the skilled use of opioid analgesics, which is crucial to the relief of cancer pain, there is a lack of evidence to support many aspects of current clinical practice. Therefore, there is a significant need for more effective treatment options. New opioids have been marketed in the past years, including hydrocodone and oxymorphone. Moreover, mixed opioids with combined mechanisms of action have been developed; one such agent, tapentadol, is a centrally acting oral analgesic that possesses a combined mechanism of action: μ-opioid receptor activation with norepinephrine reuptake inhibition. Drug development strategies involving naloxone have been initiated to reduce peripheral opioid-related adverse effects. The rationale is based on the local antagonist activity of naloxone in intestinal opioid receptors and the negligible oral bioavailability of naloxone, particularly in a prolonged-release formulation. New delivery systems have been developed to provide rapid analgesia with potent opioid drugs such as fentanyl. Despite the upcoming availability of these new drugs and technologies that will add to existing types of opioid medication, their benefits and liabilities will ultimately need to be determined by the individual physician and individual patient experiencing pain.

Ból ◽  
2017 ◽  
Vol 17 (4) ◽  
pp. 26-40
Author(s):  
Magdalena Kocot-Kępska ◽  
Renata Zajączkowska ◽  
Anna Przeklasa-Muszyńska ◽  
Jan Dobrogowski

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.


2021 ◽  
Vol 13 (1) ◽  
pp. 101-106
Author(s):  
M. V. Zamergrad ◽  
S. V. Morozova

In recent years, some progress has been achieved in elaborating the algorithms and standards for the treatment of many conditions accompanied by vertigo. The current possibilities of treating vestibular vertigo consist of a gradually expanding arsenal of symptomatic and pathogenetic drugs. Among the drugs used for the symptomatic treatment of vestibular vertigo, there are vestibular suppressants (antihistamines, benzodiazepines, and calcium antagonists) and antiemetics (dopamine antagonists and serotonin 5-HT3 receptor antagonists). The paper discusses the possibilities of using betahistine and vitamin D as pathogenetic agents for recurrent benign paroxysmal positional vertigo; diuretics, betahistine (including the new prolonged release formulation Betaserc® Long), glucocorticoids, and gentamicin for Meniere's disease; triptans, beta-blockers, tricyclic antidepressants, and anticonvulsants for vestibular migraine; glucocorticoids, antiviral agents, and drugs that accelerate vestibular compensation for acute unilateral peripheral vestibulopathy (vestibular neuritis and Ramsey Hunt syndrome).The emergence of new drugs, as well as the design of new dosage forms that enhance patient adherence to the prescribed treatment, can improve quality of life in patients suffering from diseases that have recently led to long-term disability or even incapacitation.


Cancers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 909
Author(s):  
Krzysztof Kotowski ◽  
Jakub Rosik ◽  
Filip Machaj ◽  
Stanisław Supplitt ◽  
Daniel Wiczew ◽  
...  

Glycolysis is a crucial metabolic process in rapidly proliferating cells such as cancer cells. Phosphofructokinase-1 (PFK-1) is a key rate-limiting enzyme of glycolysis. Its efficiency is allosterically regulated by numerous substances occurring in the cytoplasm. However, the most potent regulator of PFK-1 is fructose-2,6-bisphosphate (F-2,6-BP), the level of which is strongly associated with 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase activity (PFK-2/FBPase-2, PFKFB). PFK-2/FBPase-2 is a bifunctional enzyme responsible for F-2,6-BP synthesis and degradation. Four isozymes of PFKFB (PFKFB1, PFKFB2, PFKFB3, and PFKFB4) have been identified. Alterations in the levels of all PFK-2/FBPase-2 isozymes have been reported in different diseases. However, most recent studies have focused on an increased expression of PFKFB3 and PFKFB4 in cancer tissues and their role in carcinogenesis. In this review, we summarize our current knowledge on all PFKFB genes and protein structures, and emphasize important differences between the isoenzymes, which likely affect their kinase/phosphatase activities. The main focus is on the latest reports in this field of cancer research, and in particular the impact of PFKFB3 and PFKFB4 on tumor progression, metastasis, angiogenesis, and autophagy. We also present the most recent achievements in the development of new drugs targeting these isozymes. Finally, we discuss potential combination therapies using PFKFB3 inhibitors, which may represent important future cancer treatment options.


Breast Care ◽  
2015 ◽  
Vol 10 (5) ◽  
pp. 312-315 ◽  
Author(s):  
Lorenzo Rossi ◽  
Olivia Pagani

The optimal endocrine therapy for premenopausal women with early and advanced breast cancer still remains an important and controversial issue. For over 30 years, tamoxifen has been the gold standard in the adjuvant setting. New therapeutic options, such as the addition of ovarian function suppression to oral endocrine therapy (either tamoxifen or aromatase inhibitors), can improve outcomes over tamoxifen alone in well-selected patients. Treatment duration has also been revisited, and extended therapy is becoming a new standard of care, especially in high-risk patients. Endocrine therapy for advanced disease still represents a challenge and a research priority. New drugs and combinations able to overcome endocrine resistance are at the horizon, and their role in premenopausal women should be better elucidated. Side effects and quality of life (including family planning considerations) play an important role in treatment selection and in the patients' treatment adherence and should always be discussed before start of treatment. The paper will specifically focus on how to integrate all new treatment options in the current armamentarium of endocrine therapy of premenopausal women, with the aim of best fine-tuning treatment selections according to the individual risk/benefit evaluation.


2005 ◽  
Vol 20 (2-3) ◽  
pp. 120-132 ◽  
Author(s):  
Henry Brodaty ◽  
Jody Corey-Bloom ◽  
Felix C.V. Potocnik ◽  
Luc Truyen ◽  
Michael Gold ◽  
...  

2018 ◽  
Vol 2018 ◽  
pp. 1-9
Author(s):  
D. Banaszek ◽  
D. Spence ◽  
P. O’Brien ◽  
K. Lefaivre

Nonunion is a relatively rare, yet challenging problem after fracture of the femoral neck. Risk factors include verticality of the fracture line and presence of comminution of the posteromedial calcar, as well as quality of reduction. Treatment options consist of valgus intertrochanteric osteotomy versus arthroplasty. Treatment should be tailored to the individual patient, taking into account patient age and activity demands. This review outlines the principles and technical considerations for valgus osteotomy of the proximal femur in the setting of femoral neck nonunion.


2021 ◽  
Vol 23 (11) ◽  
Author(s):  
Laura D’Erasmo ◽  
Simone Bini ◽  
Marcello Arca

Abstract Purpose of Review This review aims to summarize the most recent published literature concerning lomitapide and volanesorsen that are approved for the use in HoFH and FCS patients, respectively. Moreover, it will briefly revise the published evidence on novel, non-approved treatments that are under evaluation for the management of these rare forms of dyslipidemias Recent Findings The definition of rare dyslipidemias identifies a large number of severe disorders of lipid metabolism of genetic origin. Among them were homozygous familial hypercholesterolemia (HoFH) (OMIM #143890) and familial chylomicronemia syndrome (FCS) (OMIM #238600), which are characterized by a markedly impaired cholesterol- and triglyceride-containing lipoproteins metabolism. They are being particularly associated with poor health outcomes and quality of life. Considering the severity of these diseases, common lipid-lowering drugs are often ineffective or do not allow to achieve the recommended lipid targets to prevent the development of complications. Nowadays, several new drugs have been found to effectively treat HoFH and FCS with an acceptable safety profile. Summary Treating patients with HoFH and FCS remains very challenging. However, novel treatment options are emerging and might be considered in addition to conventional therapy for managing these diseases. These novel drugs will possibly change the natural history of these two rare and life-threatening diseases.


Sign in / Sign up

Export Citation Format

Share Document