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Dexmedetomidine and ST-91 analgesia in the formalin model is mediated by alpha2A-adrenoceptors: a mechanism of action distinct from morphine.

BACKGROUND AND PURPOSE: Intrathecal administration of alpha(2)-adrenoceptor agonists produces potent analgesia. This study addressed the subtype of spinal alpha(2)-adrenoceptor responsible for the analgesic effects of i.t. dexmedetomidine and ST-91 in the formalin behavioural model and their effects on primary afferent substance P (SP) release and spinal Fos activation. EXPERIMENTAL APPROACH: The analgesic effects of i.t. dexmedetomidine and ST-91 (alpha(2) agonists) were tested on the formalin behavioural model. To determine the subtype of alpha(2)-adrenoceptor involved in the analgesia, i.t

Methylphenidate versus placebo for fatigue in patients with advanced cancer: the MePFAC randomised controlled trial.

BACKGROUND: Previous meta-analyses suggested methylphenidate may be effective for cancer-related fatigue. TRIAL DESIGN: Phase III, parallel … disorders; anaemia; thrombocytopenia; leucopenia; infection; renal or liver impairment; concomitant clonidine, warfarin, monoamine oxidase inhibitors or modafinil; alcohol or drug dependency; epilepsy. INTERVENTIONS: Methylphenidate 5 mg tablets or matching placebo. Starting at 1 tablet twice daily, titrated over 6 weeks to a maximum of 12 tablets/day. OB …

Налтрексон для острого управления навязчивыми сексуальными и одержимыми симптомами у пациента с неевроразвитым расстройством.

Навязчивое сексуальное расстройство (CSBD) характеризуется постоянной сложностью контроля за сексуальными желаниями и поведением, связанным с явными расстройствами или расстройствами. Данные, основанные на населении, свидетельствуют о том, что ~8.6% , взрослых американцев испытывают трудности, связанные с борьбой с сексуальными желаниями, чувствами и поведением, в то время как крупные международные исследования в области скрининга показывают, что ~5% ОСББ может подвергаться высокому риску, однако лишь меньшинство обращается за лечением. Диагностическая классификация по-прежнему сопряжена с тру

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… Score (1 = not at all like me; 2 = slightly like me; 3 = mainly like me; and 4 = very much like me) At home, the patient was maintained on fluoxetine, clonidine, guanfacine, trazodone, and olanzapine. … Upon admission, an effort was made to simplify the patient’s alpha‐2 adrenergic agonist regimen by consolidating guanfacine and clonidine to clonidine alone, which was subsequently titrated and optimized during the hospital stay. …

Involvement of Opioid Receptors and α2-Adrenoceptors in Inhibitory Pain Modulation Processes: A Double-Blind Placebo-Controlled Crossover Study.

UNLABELLED: In healthy humans, high-frequency electrical stimulation (HFS) of the forearm not only evokes local signs of central sensitization but also triggers broader ipsilateral inhibitory influences on pain akin to a lateralized form of conditioned pain modulation. Paradoxically, some of these inhibitory influences are augmented by α2-adrenoceptor blockade. To determine whether opioid peptides mediate inhibitory effects after HFS, the opioid receptor antagonist naltrexone was coadministered orally with the α2-adrenoceptor antagonist yohimbine in 16 healthy women in a double-blind placebo-c

Recurrent postoperative CRPS I in patients with abnormal preoperative sympathetic function.

PURPOSE: A complex regional pain syndrome of an extremity that has previously resolved can recur after repeat surgery at the same anatomic site. Complex regional pain syndrome is described as a disease of the autonomic nervous system. The purpose of this study was to evaluate preoperative and postoperative sympathetic function and the recurrence of complex regional pain syndrome type I (CRPS I) in patients after repeat carpal tunnel surgery. METHODS: Thirty-four patients who developed CRPS I after initial carpal tunnel releases and required repeat open carpal tunnel surgeries were studied. La

alpha2B-adrenoceptor agonist ST-91 antagonizes beta2-adrenoceptor-mediated relaxation in rat mesenteric artery rings.

We sought an isolated vascular preparation and experimental setting where the function of alpha2B-adrenoceptors could be demonstrated by non-recombinant technique. ST-91 (2-[2,6-diethylphenylamino]-2-imidazoline), an alpha 2B-adrenoceptor agonist with a mixed alpha adrenergic receptor type/subtype selection profile antagonized the relaxant effect of isoproterenol in endothelium-denuded rat mesenteric artery rings precontracted with phenylephrine. At 10(-7) M of ST-91, the antagonism was characterized by a rightward shift of isoproterenol dose-response curve (A50=6.81+/-1.40 e-7 (n=4) vs the co

Analgesia, Opioids, and Other Drug Use During Pregnancy and Neonatal Abstinence Syndrome.

When opioid misuse rises in the United States, pregnant women and their neonates are affected. This article summarizes the use of Food and Drug Administration-approved products, including methadone, buprenorphine, and the combination formulation of buprenorphine and naloxone to treat adult opioid use disorder during the perinatal period. All labels include pregnancy, neonatal, and lactation information and note the accepted use of these medications during the perinatal period if the benefits outweigh the risks. A summary of the neonatal abstinence syndrome definition, its assessment tools, tre

A G protein gamma subunit-specific peptide inhibits muscarinic receptor signaling.

Muscarinic acetylcholine receptors modulate the function of a variety of effectors through heterotrimeric G proteins. A prenylated peptide specific to the G protein gamma5 subunit type inhibits G protein activation by the M2 muscarinic receptor in a reconstitution assay. Scrambling the amino acid sequence of the peptide significantly reduces the efficacy of the peptide. The peptide does not disrupt the G protein heterotrimer. In cultured sympathetic neurons, the gamma5 peptide inhibits modulation of Ca(2+) current by the M4 receptor. Peptide activity is specific, the scrambled peptide and pept

[Nuclear medicine diagnosis of pheochromocytoma with metaiodobenzylguanidine].

Excess secretion of any of the adrenal cortical or medullary hormones contributes to a number of well-known clinical syndromes.. They may re … high levels of free catecholamines and their metabolites (metanephrines and Vanillylmandelic acid). Clonidine test may be important in some cases. The purpose of this study is to point that metaiodobenzylguanidine (mlBG) has proved to be a safe, sensitive and highly specific agent for the location of phaeochromocytoma. The first successful schinigraphic dem …

Endogenous opioid peptides acting at mu-opioid receptors in the dorsal horn contribute to midbrain modulation of spinal nociceptive neurons.

Activation of neurons in the midbrain periaqueductal gray (PAG) inhibits spinal dorsal horn neurons and produces behavioral antinociception in animals and analgesia in humans. Although dorsal horn regions modulated by PAG activation contain all three opioid receptor classes (mu, delta, and kappa), as well as enkephalinergic interneurons and terminal fields, descending opioid-mediated inhibition of dorsal horn neurons has not been demonstrated. We examined the contribution of dorsal horn mu-opioid receptors to the PAG-elicited descending modulation of nociceptive transmission. Single-unit extra

Melittin, a honeybee venom derived peptide for the treatment of chemotherapy-induced peripheral neuropathy.

Chemotherapy-induced peripheral neuropathy (CIPN) is the most prevalent neurological complication of cancer treatment which involves sensory and motor nerve dysfunction. Severe CIPN has been reported in around 5% of patients treated with single and up to 38% of patients treated with multiple chemotherapeutic agents. Present medications available for CIPN are the use of opioids, nonsteroidal anti-inflammatory agents, and tricyclic antidepressants, which are only marginally effective in treating neuropathic symptoms. In reality, symptom reappears after these drugs are discontinued. The pathogene

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… Similarly, it has shown that BVA could enhance the analgesic effect of clonidine injection in the persistent constriction-caused neuropathic pain model [ 41 ]. Whole honeybee venom attributes to allergic reaction whereas melittin is free from such action. … Yoon SY Roh DH Kwon YB Kim HW Seo HS Han HJ Lee HJ Beitz AJ Lee JH Acupoint stimulation with diluted bee venom (apipuncture) potentiates the analgesic effect of intrathecal clonidine in the rodent formalin test and in a neuropathic pain model J Pain 2009 10 3 253 263 19010737 10.1016/j.jpain.2008.09.002 …

Alpha 2-adrenergic stimulation promotes preadipocyte proliferation. Involvement of mitogen-activated protein kinases.

Primary cultures of rat preadipocytes were shown to express alpha 2- and beta-adrenoreceptors when maintained in serum-deprived medium. alpha 2-Adrenoreceptor stimulation led to an increase in cell number, whereas beta-adrenoreceptor stimulation was without effect. On 3T3-F442A clones stably transfected with the human alpha 2-C10 gene and expressing a physiologically related number of alpha 2-adrenoreceptors to overexpression, the proliferative effect of alpha 2-adrenoreceptor agonist UK14304 was proportional to the level of alpha 2-adrenoreceptor expressed in individual clones and required al

Treatments for hyperemesis gravidarum and nausea and vomiting in pregnancy: a systematic review and economic assessment.

BACKGROUND: Nausea and vomiting in pregnancy (NVP) affects up to 85% of all women during pregnancy, but for the majority self-management suf … symptoms. Dextrose saline may be more effective at reducing nausea than normal saline. Transdermal clonidine patches may be effective for severe HG. Enteral feeding is effective but extreme method treatment for very severe symptoms. Day case management for moderate/severe symptoms is feasible, acceptable and as effective as inpatient care. For all other in …

Pharmacological interventions for the management of pain and discomfort during lumbar puncture in newborn infants.

BACKGROUND: Lumbar puncture (LP) is a common invasive procedure, most frequently performed to diagnose infection. Physicians perform LP in n … f local anesthetics [EMLA], lidocaine) • Opioids (e.g. morphine, fentanyl) • Alpha-2 agonists (e.g. clonidine, dexmedetomidine) • N-Methyl-D-aspartate (NMDA) receptor antagonists (e.g. ketamine) • Other analgesics (e.g. paracetamol) • Sedatives (e.g. benzodiazepines such as midazolam) DATA COLLECTION AND ANALYSIS: We used standard Cochrane methods. We used …

Metaplasticity of hypothalamic synapses following in vivo challenge.

Neural networks that regulate an organism's internal environment must sense perturbations, respond appropriately, and then reset. These adaptations should be reflected as changes in the efficacy of the synapses that drive the final output of these homeostatic networks. Here we show that hemorrhage, an in vivo challenge to fluid homeostasis, induces LTD at glutamate synapses onto hypothalamic magnocellular neurosecretory cells (MNCs). LTD requires the activation of postsynaptic alpha2-adrenoceptors and the production of endocannabinoids that act in a retrograde fashion to inhibit glutamate rele

Drug therapy for obstructive sleep apnoea in adults.

BACKGROUND: The treatment of choice for moderate to severe obstructive sleep apnoea (OSA) is continuous positive airways pressure (CPAP) via … sleep time favoured placebo. No significant beneficial effects were found for medroxy progesterone, clonidine, mibefradil, cilazapril, buspirone, aminophylline, theophylline doxapram, ondansetron or sabeluzole. AUTHORS' CONCLUSIONS: There is insufficient evidence to recommend the use of drug therapy in the treatment of OSA. Small studies have reported posi …

Plasmacytoid Urothelial Carcinoma of Ureter with Retroperitoneal Metastasis: A Case Report.

BACKGROUND Plasmacytoid is a rare histological variant of urothelial carcinoma (UC). Since the first reported case of plasmacytoid urothelial carcinoma (PUC), in 1991, only about 100 cases have since been reported, with most cases involving the bladder. Urothelial carcinomas of the upper urinary tract represent only 5% of urothelial cancers. To the best of our knowledge, there has only been 1 reported case of PUC of the ureter. PUC is a highly aggressive disease, with a poor prognosis. We present a rare biopsy-proven case of PUC of the ureter with retroperitoneal metastasis. CASE REPORT A 60-y

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… The list of related medication are as follows: clonidine patch 0.2 mg, metoprolol 5 mg IV q6h, sodium chloride 1 gm tab PO BID, Ativan 0.5 mg IV push q8, Morphine 1 mg/ml PCA interval 8 min 4 h limit dose 30 mg IV, Robaxin 1000 mg PO q6 PRN, and hyperalimentation-ADULT 2160 mL IV over 24 h. …

Comparative cardiovascular safety of medications for attention-deficit hyperactivity disorder in children, adolescents, and adults: a systematic review and network meta-analysis.

BACKGROUND: Concerns about the cardiovascular safety of medications used for the treatment of attention-deficit hyperactivity disorder (ADHD … lished and unpublished randomised controlled trials comparing amphetamines, atomoxetine, bupropion, clonidine, guanfacine, lisdexamfetamine, methylphenidate, modafinil, or viloxazine against each other or placebo. Primary outcomes were change in systolic blood pressure (SBP) and diastolic blood pressure (DBP), measured in mm Hg, and pulse, measured in beats …

Midazolam for sedation before procedures.

BACKGROUND: Midazolam is used for sedation before diagnostic and therapeutic medical procedures. It is an imidazole benzodiazepine that has … tanyl (1), flunitrazepam (1) and propofol (1); oral chloral hydrate (4), diazepam (2), diazepam and clonidine (1); ketamine (1) and placebo (3); and intranasal placebo (2). There was a high risk of bias due to inadequate reporting about randomization (75% of trials). Effect estimates were imprecise due to small sample sizes. None of the trials reported on a …

Cardiotoxicity after cancer treatment: a process map of the patient treatment journey.

Background/aimCardiotoxicity is a potential complication of anticancer therapy. While guidelines have been developed to assist practitioners, an effective, evidence based clinical pathway for the treatment of cardiotoxicity has not yet been developed. The aim of this study was to describe the journey of patients who developed cardiotoxicity through the healthcare system in order to establish baseline data to inform the development and implementation of a patient-centred, evidence-based clinical pathway.MethodsMixed-methods design with quantitative and qualitative components using process mappi

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… Radiation therapy 28 (61) a Dose not recorded b Each patient’s regimen comprised individualised composites and doses of the above cytotoxic agents c Other drugs taken include: amiloride, amiodarone, amlodipine, atenolol, atorvastatin, bisoprolol, candesartan, carvedilol, cephalexin, cholecalciferol, clonidine … Record Review cohort only) a Dose not recorded b Each patient’s regimen comprised individualised composites and doses of the above cytotoxic agents c Other drugs taken include: amiloride, amiodarone, amlodipine, atenolol, atorvastatin, bisoprolol, candesartan, carvedilol, cephalexin, cholecalciferol, clonidine …