opiate rotation

Although diarrhea is a common complaint, its evaluation and treatment can be challenging. Appropriately defining and classifying diarrhea provide the framework for approaching diagnostic and therapeutic options. Diarrhea can be defined based on frequency, consistency, and/or weight, and classified as acute or chronic with specific clinical characteristics and stool appearance. Colonoscopy is the most common diagnostic tool used in the evaluation of patients with chronic diarrhea. Other evaluation strategies include timed stool collections, evaluation of inflammatory markers, and hydrogen breath tests...

AIMS: Stress hormones might be involved in motion sickness. The influence of loperamide on kinetosis-induced nausea and stress hormone release was investigated in a placebo-controlled, cross-over study. METHODS: Standardized rotation around the vertical axis combined with head movements was used to induce nausea 3 h after 16 mg loperamide or placebo (n = 8). Plasma antidiuretic hormone (ADH), adrenocorticotropic hormone (ACTH) and nausea ratings were investigated...

Opioids are widely used as effective analgesic therapy for cancer pain. Despite years of controversy, their use has been also accepted in chronic non-cancer pain. Oxycodone alone and in combination has been used for over 80 years in the treatment of a variety of pain syndromes. As single agent, the controlled release (CR) oxycodone's market in the USA grew from 10% in 1996 to 53% in 2000 and it has become a leading opioid in the United States. Recent data showed that the fixed-combination oxycodone/acetaminophen (5 mg/325 mg) is the most often prescribed opioid across all the different chronic pain diagnoses...

Experiments were performed on mongrel male rats to study the effects of blockade of delta, mu, and kappa opiate receptors on antibody formation, delayed-type hypersensitivity (DTH), and changes in the numbers of antibody-forming cells (AFC) and nucleated cells in the lymph nodes and spleen in a local form of immune response in a model of rotation stress. These studies showed that rotation stress led to mild suppression of immune inflammation in DTH, significant increases in the numbers of AFC and nucleated cells in regional lymph nodes, but no change in the peripheral blood antibody titer...

Disease-directed treatment of lung cancer reduces the morbidity and extends life for patients. However, as providers we must recognize that treating the symptoms of the disease may be as important as the treatment of the disease itself. This is particularly true in advanced disease and after disease-directed therapies have been exhausted. Aggressive assessment of symptoms and use of palliative therapies can significantly reduce the symptomatology of advanced lung cancer. Though the impact of these symptoms (ie, pain, dyspnea, and cachexia) are well known, they tend to be under-treated...

The gastrointestinal (GI) effects of morphine and other opioids may result in opioid-induced bowel dysfunction (OBD) and the need for treatment. Although OBD is very common in morphine-treated patients, it is usually under-diagnosed. Opioids deliver their GI effect through central and peripheral mechanisms. Laxatives are the pharmaceuticals prescribed most in this area. Prokinetics as well as cholinergic agonists have been used satisfactorily. One-third of patients with OBD have to be treated rectally. The use of opioid antagonists has been favored, but the bioavailability of oral forms is poor...

RATIONALE: Medications combining hydrocodone bitartrate and non-steroidal anti-inflammatory agents appear more beneficial than anti-inflammatory medications alone in treating pain and inflammation from acute soft tissue trauma, but opiate side effects may include sedation and impaired cognitive and motor performance. OBJECTIVE: Performance on complex cognitive and motor tasks was evaluated in healthy subjects with exercise-induced muscle damage who were treated with a hydrocodone-ibuprofen combination, ibuprofen alone, or placebo...

A field study was performed at two police agencies to evaluate the utility and accuracy of five on-site urine analysis drug-testing devices when used to test driving under the influence (DUI) arrestees. The devices evaluated were AccuSign, Rapid Drug Screen, TesTcup-5, TesTstik, and Triage. Standard workplace screening cut-off concentrations were used and samples were tested for marijuana, cocaine and metabolites, amphetamine(s), opiates, and PCP (except opiates 300 ng/mL). Four-hundred arrestees were recruited at each site, informed consent was obtained, and urine specimens were collected from each subject for analysis...

The chakragati (ckr) mouse is a transgenic insertional mutant that displays lateralized circling behavior, locomotor hyperactivity, hyperexcitability as well as body weight deficits. The mutation is autosomal and recessive. We have previously found that ckr mice have bilateral asymmetric elevations in striatal dopamine (DA) D2-like (D2, D3 and/or D4), but not D1-like (D1 and/or D5) receptors. Predictably, these mice increase turning in response to the D2-like agonist quinpirole and spontaneously rotate contralateral to the striatal side with the higher D2-like receptors...

A topochemical model to explain the bioactivity of morphiceptin (Tyr1-Pro2-Phe3-Pro4-NH2) was developed by taking account of accessible conformations around rotatable bonds which define relative spatial arrangements of opioid pharmacophores, the amine and phenolic groups of tyrosine and the aromatic ring of phenylalanine, necessary for receptor recognition. For this purpose, 1H-NMR measurements and computer simulations were extensively carried out on 10 stereoisomeric analogs related to morphiceptin: Tyr-Pro-(L and D)-Phe- (L and D)-Pro-NH2; Tyr-Pro-(L and D)-(NMe)Phe-(L and D)-Pro-NH2; Tyr-(NMe)Ala-Phe-D-Pro-NH2; and Tyr-Ala-Phe-D-Pro-NH2...

Three novel benzomorphans, (+)-N-benzylnormetazocine, (-)-deoxy-N-benzylnormetazocine, and (-)-deoxypentazocine were tested for their ability to produce circling behavior in rats following intranigral microinjections. Dose studies revealed the following rank order of potency: (-)-deoxypentazocine > (-)-deoxy-N-benzylnormetazocine > (+)-N-benzylnormetazocine. This rank order approximates that for affinities for sigma 2 receptors but not sigma 1 receptors. It is very unlikely that the effects of the (-)-deoxybenzomorphans were mediated by opiate receptors for the following reasons: (1) consistent with the known requirement for the phenolic hydroxyl group for opiate activity, both (-)-deoxy compounds showed very low affinity for opiate receptors; (2) naloxone (4 micrograms) co-administered with (-)-deoxy-N-benzylnormetazocine failed to reduce its efficacy; (3) both (-)-deoxy compounds failed to produce marked analgesic effects in the tail flick test following systemic injections of 20 mg/kg s...

One hundred and six HIV-positive drug users were tested with a two-tone auditory evoked potential (AEP) task and a small battery of neuropsychological tests, to examine the relationship between the latency of the P300 component (P3) of the AEP, intellectual function, mood and drug use. Principal components analysis revealed a significant correlation between P3 latency and the first principal component (r = -0.43, P < 0.001). Varimax rotation generated three orthogonal components which we interpreted as intellectual performance, memory, and mood...

Brain-derived neurotrophic factor (BDNF) and neurotrophin-4/5 (NT-4/5) have both been identified as ligands for the TrkB receptor, yet differences have emerged in terms of their in vitro potencies for neuronal survival and differentiation. This has prompted the in vivo study of their effects on behavior and neuro-chemical parameters associated with dopamine, serotonin, and GABAergic neurons in the basal ganglia. Two-week supranigral infusions of NT-4/5 and BDNF were similar in their ability to augment levels of the dopamine metabolite homovanilic acid (HVA) (63 and 78%, respectively) and the ratios of dihydroxphenylacetic acid/dopamine (DOPAC/DA) (39, 48%) and HVA/DA (85, 77%) in the caudate-putamen of the hemisphere ipsilateral to the nigral infusion...

A fraction consisting of low-molecular components (LMCs) was isolated from the brain of rats with unilateral destruction of the Deuters lateral vestibular nucleus (LVN) or with the generator of excitation (GE) created in the LVN with tetanus toxin. Intracranial administration of the preparation to normal rats produced the tension of body muscles, bending and opposite changes in the muscle tone of the hind limbs - the delay in the pulling up of the paw passively set aside and enhancement of the flexor tone of the opposite hind limb...

The conformational preferences of phenylmorphan have been determined by the MM2 (Molecular Mechanics II) program using full energy minimization. Chair-chair conformations of the cyclohexane and piperidine rings were preferred by 2.6 kcal/mol or more. With the preferred chair-chair conformation, three stable orientations of the phenyl ring were found with relative energies of 0.0, 1.0, and 1.2 kcal/mol. The barrier to rotation of the phenyl ring was computed to be 4 kcal/mol. The preferred phenyl orientation for the (+)-antipode was similar to that of morphine using a previously postulated molecular model for opiate substrates...

The effects of morphine and naloxone on nigrostriatal function were evaluated by their influence on rotational behavior in rats with unilateral lesions of the substantial nigra. Two different rotational syndromes which result from different lesion placements, were examined. Rats with the contraversive syndrome, when given apomorphine, rotate away from the lesioned side, while rats with the ipsiversive syndrome rotate toward the lesioned side. In both syndromes, rats rotate toward the lesioned side when given amphetamine...

A major component of opiate reward is derived from a drug action in the ventral tegmental area: (a) rats quickly learn to self-administer morphine directly into the ventral tegmentum, (b) intracranial self-administration into other brain sites is not quickly learned, and (c) narcotic antagonist microinjections into the ventral tegmentum attenuate reward from intravenous heroin infusions. At least one component of opiate reward is dependent on a dopaminergic system: (a) electrophysiological and neurochemical indices suggest that opiates activate ventral tegmental dopaminergic neurons, (b) ventral tegmental opiate infusions are behaviorally activating producing contralateral rotation that is blocked by neuroleptics, (c) reward from heroin is blocked by neuroleptics, and (d) reward from heroin is attenuated by dopamine-depleting lesions of the ventral tegmental system...

The effects of mu and kappa-opiate receptor agonists were studied in a variety of tests in the mouse designed to correspond to clinical side-effects in man. These included sedation, decrease in pupil diameter, Straub tail, decrease in body temperature, decrease in respiratory rate and inhibition of gut propulsion. The mu-receptor agonists tested produced opiate side-effects in the mouse at doses between 2.4 and 34 times higher than their antinociceptive doses in the abdominal constriction test. Their ranked orders of potency in producing these effects were very similar to their order of antinociceptive potency...

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Exposure to rotating and elevated magnetic fields significantly reduced over three hours the ingestive effects of the opiate agonist, morphine (10 mg/kg), in free-feeding slugs, Limax maximus. Magnetic field exposure also inhibited the opioid-mediated increased ingestive responses of slugs that had been food-deprived for 24 hr. These results suggest that magnetic stimuli inhibit opiate-mediated behavioral and physiological functions in invertebrates in a similar manner as observed in vertebrates.