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Edward E. Smissman-Bristol-Myers Squibb Award Address. The role of concepts in structure-activity relationship studies of opioid ligands.

Various concepts have served as the basis for the development of models to explore the relationship between molecular structure and biologic … ese highly selective antagonists have advantages over the universal opioid antagonists naloxone and naltrexone because they are of value in probing the interaction of endogenous opioid peptides with opioid receptor types. Additionally, they are useful in evaluating the selectivity of new opioid agonists. Also, selective opioid antagonists have potential clin …

Psychoneuroimmunological approach to gastrointestinal related pain.

BACKGROUND AND PURPOSE (AIMS): Psychoneuroimmunology is both a theoretical and practical field of medicine in which human biology and psycho … ebiotics, probiotics, nutritional advice, and off-label drugs. An example of the latter is low-dose naltrexone, a compound which opens the perspective of targeting glial cells to reduce neuroinflammation and ultimately pain. IMPLICATIONS (OUR OPINION ON WHAT OUR FINDINGS MEAN): Current findings from basic science provide sound mechanistic evidence and once …

Long-term stability of abused drugs and antiabuse chemotherapeutical agents stored at -20 degrees C.

Stability is an important consideration in the use of specimens for accurate determination of analyte concentrations. To determine the long- … s reached 15% at 158-216 days. The 700-ng/mL controls reached 15% at 784-1340 days. In plasma, only naltrexone and buprenorphine displayed negative slopes at all three concentrations, reaching the 15% mark as early as 576 and 272 days, respectively. LAAM, norLAAM, dinorLAAM, ibogaine, 6-beta-naltrexone, risperidone, and 9-OH-risperidone did not exceed a 15% …

Оценка и лечение агрессивного сексуального поведения: нынешние ограничения и потенциальные стратегии.

Несмотря на то, что в МКБ-11 была введена соответствующая классификация и симптоматика расстройства сексуального поведения (CSBD) по-прежнему противоречива. В этом обзоре мы изучили историю, эпидемиологический статус-кво, коморбиды, теории нейрофизики, текущие диагнозы и рекомендации по лечению для CSBD. Кроме того, мы подчеркнули недостатки текущих исследований и перспективы будущей работы. Селективные ингибиторы серотонина и налтрексон обычно используются в качестве "немаркированных" наркотиков. Диагностика и лечение пациентов, проходящих курс лечения, должны включать в себя биологические, п

Совпадение в аннотации оригинала
AimDespite having been introduced into ICD-11, the appropriate classification and symptomatology of compulsive sexual behavior disorder (CSB … l therapy are the preferred treatment methods for CSBD. Selective serotonin reuptake inhibitors and naltrexone are commonly used as "off-label" drugs. The diagnosis and treatment of patients with CSBD should integrate biological, psychological, and social factors with expertise in sexual medicine by employing a comprehensive and holistic therapeutic approach …

Current Understanding of Compulsive Sexual Behavior Disorder and Co-occurring Conditions: What Clinicians Should Know about Pharmacological Options.

Compulsive sexual behavior disorder (CSBD) has recently been recognized as a psychiatric disorder. Pharmacological treatments for CSBD have received little study and thus have limited empirical support. The main objective of the present work is to review existing literature on the efficacy of different drugs on the symptomatology of CSBD, including the subtype of problematic pornography use (PPU). The main pharmacological approaches to treating CSBD have included opioid antagonists (naltrexone and nalmefene), selective serotonin reuptake inhibitors (paroxetine, citalopram, fluoxetine, and sert…

Non-Atopic Chronic Nodular Prurigo (Prurigo Nodularis Hyde): A Systematic Review of Best-Evidenced Treatment Options.

BACKGROUND: Chronic nodular prurigo (CNPG) is a chronic, inflammatory skin disease, characterized by intense and debilitating pruritus. The … opical therapy with hydrocortisone and pimecrolimus, thalidomide, UVA phototherapy, pregabalin, and naltrexone. Included RCTs and case studies all had a heterogeneous methodology making direct comparison almost impossible. KEY MESSAGES: There is sparse evidence for the currently used therapies for non-atopic CNPG. Several RCTs on new therapies are running o …

Comorbid chronic pain and opioid use disorder: literature review and potential treatment innovations.

Chronic pain (CP) and opioid use disorder (OUD) remain challenging complex public health concerns. This is an updated review on the relationship between CP and OUD and the use of stepped care models for assessment and management of this vulnerable population. A literature search was conducted from 2008 to the present in PubMed, Embase, and PsycInfo using the terms pain or chronic pain and opioid-related disorders, opiate, methadone, buprenorphine, naltrexone, opioid abuse, opioid misuse, opioid dependen*, heroin addict, heroin abuse, heroin misuse, heroin dependen*, or analgesic opioids, and s…

Treatment of obesity in 2015.

Obesity is a major health priority in the United States, as well as globally. It is associated with multiple comorbidities and reduced life … phentermine/topiramate extended release, and lorcaserin, and there are 2 on the horizon, bupropion/naltrexone and liraglutide. Bariatric surgery is an effective strategy recognized to produce durable weight loss with amelioration of obesity-related comorbidities and should be considered a treatment option in eligible patients.

Sodium oxybate: a review of its use in alcohol withdrawal syndrome and in the maintenance of abstinence in alcohol dependence.

A liquid formulation of sodium oxybate (Alcover(®)), the sodium salt of γ-hydroxybutyric acid (GHB), is approved in Italy and Austria for us … ts with alcohol withdrawal syndrome, rapidly alleviating symptoms, and was at least as effective as naltrexone or disulfiram in the maintenance of abstinence in alcohol-dependent patients. Sodium oxybate was generally well tolerated. The risk of sodium oxybate abuse is generally low when it is administered to alcohol-dependent patients at its approved dosage …

New therapeutic approaches in the treatment of diabetic keratopathy: a review.

The cornea is densely innervated, and the integrity of these nerve fibres is critical in maintaining the refractive and protective functions … and consequently accelerate wound healing. More recently, local/topical administration of insulin, naltrexone (opioid antagonist) and nicergoline (ergoline derivatives) were found to improve, and significantly increase, the corneal wound healing rate. This report reviews the major attributes of these growth factors and therapeutic agents that may be used in …

Mu opioid receptor antagonists: recent developments.

For thousands of years mu opioid agonists such as morphine have been utilized for their analgesic properties. Today, morphine and related compounds are still used as a first line therapy in the treatment of moderate to severe pain. However, despite the clear benefits of mu agonists in pain management, severe side effects such as dependence and respiratory depression are associated with use of these drugs. To date, there are only two approved mu opioid antagonists for use in the treatment of these adverse effects, that is, naloxone and naltrexone. However, many other clinical and therapeutic ar…

Bipolar disorder and comorbid alcoholism: prevalence rate and treatment considerations.

Classic Kraepelian observations and contemporary epidemiological studies have noted a high prevalence rate between bipolar disorder and alco … t of bipolar disorder with comorbid alcoholism. A number of add-on, adjunctive medications, such as naltrexone, acamprosate, topiramate, and the atypical antipsychotics quetiapine and clozapine, may be candidates for further testing.

Hyperalgesic response to noxious stimulation in genetically polydipsic mice.

Inbred mice, STR/N, are known to exhibit extreme polydipsia and polyuria but no abnormality in the response to exogenous vasopressin (AVP) a … y to show morphine analgesia after up-regulation of the opioid system by repeated administration of naltrexone (s.c., 5 mg/kg) for 3 consecutive days. The results suggest that the anti-nociceptive function of the opioid system is down-regulated in STR/N mice as is observed in chronic morphine-treated animals.

Morphine modulation of thioglycollate-elicited peritoneal inflammation in the goldfish, Carassius auratus.

Intraperitoneal (i.p.) injection of adult goldfish with 3% thioglycollate (TG) induces an acute peritoneal inflammation connected with a massive influx of inflammatory leukocytes mainly of the head kidney origin. The number of peritoneal exudate cells retrieved on day 2 of the inflammatory response is significantly lower in fish injected with TG and morphine (20 mg/kg b.w.) than in animals injected with TG only. The morphine effect was totally antagonized in fish injected 20 min earlier with naltrexone (1 mg/kg), a well-known blocker of opioid receptors. Light microscopy of the head kidney Epo…

Recent developments in the pharmacotherapy of alcohol dependence.

The effectiveness of a treatment for alcohol dependence can be appropriately determined only after controlling for the usual clinical course … cations are quite promising regarding their potential future impact in the alcohol field, including naltrexone, the medication with the most available data in the United States. There are additional data regarding buspirone and acamprosate. Intriguing results have also been generated regarding medications that affect serotonin and dopamine brain activity and …

Opioid peptides and testicular activity in the lizard Podarcis s. sicula Raf.

In mammals endorphinergic systems have been shown to modulate reproductive processes and beta-endorphin (beta-EP) has been found to influenc … ring April, when the highest testicular activity occurred. Using in vivo studies, it was found that naltrexone treatment, blocking pituitary opioid receptor, increased androgen levels in the plasma and in the testis. It was also found with in vitro studies that the endogenous opioid system inhibits gonadotrophin release and therefore androgen production by t …

The kappa-opioid receptor agonist, U50,488H, exerts antidystonic activity in a mutant hamster model of generalized dystonia.

The kappa-opioid receptor agonist, U50,488H (trans-(+-)-3,4-dichloro-N-methyl-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide), has recently been reported to induce dystonia after s.c. administration of 5-10 mg/kg in guinea pigs. The dystonic movements observed in response to U50,488H resembled those previously reported to occur spontaneously or in response to mild environmental stimuli in a mutant hamster model of paroxysmal generalized dystonia. This prompted us to study the effects of opioid receptor antagonists and of U50,488H in the mutant hamster model. Naloxone and naltrexone, 1 and 1…

Beta-endorphin blunts phosphatidylinositol formation during in vitro activation of isolated human lymphocytes: preliminary report.

We have previously described the regulatory effect of beta-endorphin on three human cytotoxic cell populations. We confirmed the variable na … l the donors tested. This effect is dose-dependent and is blocked in part by the opioid antagonist, naltrexone, suggesting involvement of the opioid receptor.

Role of the pineal gland in immunity: II. Melatonin enhances the antibody response via an opiatergic mechanism.

The pineal gland constitutes a major neuroendocrine organ in the brain. It transduces exogenous signals such as circadian and seasonal varia … globulins) in vivo according to a dose-response behaviour and that (c) the opioid receptors blocker naltrexone antagonizes the immunostimulatory effect of melatonin. These findings point to a fundamental immunoregulatory role of circadian melatonin and to an activity of the neurohormone via opioid peptides.

Modulation of mu-opioid pathway for the treatment of pruritus: a systematic review of 1,146 patients.

BACKGROUND: Pruritus is a debilitating symptom and conventional therapies often provide incomplete relief. The μ-opioid receptor (MOR) pathw … systemic pruritus, predominantly cholestatic and uremic pruritus. RCTs investigated oral or topical naltrexone, intravenous naloxone, nalmefene, and extended-release nalbuphine, with most demonstrating clinically meaningful reductions in pruritus intensity using validated itch scales. Non-randomized studies reported improvement across a wide range of dermato …