Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The aim of the regional administration of opioids is to provide an efficient and prolonged analgesia. Then, opiates can be useful for postoperative analgesia and for the treatment of chronic pain of malignant origin. Analgesia is correlated with several adverse effects of which the most frequent are nausea and itching and the most severe is respiratory depression. Beside the adverse effects, other properties of opiates could be responsible of favourable effects which can be taken in advantage in specific indications. In the postoperative period, epidurally administered opioid can attenuate the neuroendocrine and metabolic responses to surgery and pain. This effect is responsible of a reduction of the resistance to insulin and of a better nutritional balance, especially after major abdominal surgical procedures. Opioids also act by a reduction of the motor functions of the bowel, which perhaps could reduce the incidence of anastomotic breakdowns. Finally, other effects have been reported, as anecdotes, such as the treatment of spasm after bilateral replantation of the ureters, neurologic bladder dysfunctions and enuresis. Spinal administration of opioids has also been used as a treatment of premature ejaculation.
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PMID:[Non-analgesic effects of opioids]. 167 72

Dapoxetine [LY 210448], a selective serotonin reuptake inhibitor (SSRI), is structurally related to fluoxetine with antidepressant activity. Dapoxetine is the D-enantiomer of LY 243917 and is 3.5 times more potent as a serotonin reuptake inhibitor than the L-enantiomer. Dapoxetine was in phase I clinical trials in the US with Eli Lilly as an antidepressant, but no recent development has been reported for this indication. However, development is underway for the treatment of premature ejaculation, with phase III trials for this indication being completed in the US. The phase II trial for the treatment of premature ejaculation was conducted by PPD GenuPro, a subsidiary of PPD, which was established from a collaboration between Eli Lilly and PPD for the development of drugs to treat genitourinary disorders. Both Lilly and PPD had an option to re-license dapoxetine upon completion of phase II trials, but neither company exercised its option, and the rights remained with PPD GenuPro. In December 2003, PPD Inc. acquired from Eli Lilly and Co. the patents for dapoxetine for development in the field of genitourinary disorders. As part of the transaction, PPD and Lilly terminated their existing license agreement for dapoxetine. In December 2000, PPD GenuPro granted an exclusive, worldwide license for dapoxetine to ALZA Corporation, a wholly owned subsidiary of Johnson & Johnson. ALZA will be responsible for development, manufacturing and commercialisation of dapoxetine for urological indications, including premature ejaculation. It will make initial, milestone and royalty payments to PPD GenuPro, a portion of which will be paid to originator Eli Lilly. PPD Inc. received a milestone payment relating to the ongoing development of dapoxetine for premature ejaculation in July 2003. In December 2003, PPD and ALZA amended the dapoxetine license to allow PPD to receive a fixed-sum cash payment apon NDA approval. In return for this, ALZA will not have to make sales-based payments for a period of time following the approval of dapoxetine. If dapoxetine is approved by the US FDA for premature ejaculation, the drug will be marketed in the US by Ortho-McNeil Pharmaceutical, Inc. In December 2004, ALZA Corporation submitted a new drug application to the FDA for dapoxetine hydrochloride in the treatment of premature ejaculation. If approved by the FDA, dapoxetine hydrochloride will be marketed in the US by Ortho-McNeil Pharmaceutical, Inc. Johnson & Johnson plans to support the launch of dapoxetine for premature ejaculation with a 'responsible' direct-to-consumer advertising campaign. In May 2005, Johnson & Johnson presented data from two phase III trials involving dapoxetine for the treatment of premature ejaculation, during the 100th Annual Scientific Meeting of the American Urological Association (AUA-2005). Results on drug interactions and pharmacodynamics of dapoxetine were also presented during this meeting. Dapoxetine also appears to be a useful adjunct to morphine, lowering the threshold for analgesia, although the compound itself has negligible analgesic activity. In December 2003, PPD, Inc. acquired from Eli Lilly and Company the patents for dapoxetine for development in the field of genitourinary disorders. Under the terms of the agreement with Lilly, PPD will pay Lilly 65 million US dollars in cash. PPD will also pay Lilly a royalty on net sales of dapoxetine in excess of a certain threshold of annual net sales. As part of the transaction, PPD and Lilly terminated their existing license agreement for dapoxetine.
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PMID:Dapoxetine: LY 210448. 1612 1

To date, there is no FDA-approved therapy for premature ejaculation (PE). Recently, phosphodiesterase 5 inhibitors (PDE5-Is) have been demonstrated to have encouraging results in the treatment of PE by a few studies. The aim of this review was to assess the updated manuscripts and thereafter present the practical recommendations and possible mechanisms concerning PDE5-Is for treating PE. Using MEDLINE, we searched and assessed the peer manuscripts published from 1 January 1996 to 1 September 2005 about PDE5-Is for treating PE. The results show that the number of patients in all the reports is very few and most of the studies do not employ double-blinded and placebo-controlled tests, though they are prospective and randomized. Therefore, the results and conclusions might be biased. PDE5-Is are suggested to be used in PE with old age or associated with erectile dysfunction (ED), or to be employed alone or in combination with selective-serotonin reuptake inhibitors (SSRIs) when SSRIs fail to treat PE; behavioural therapy is proposed to be used for preventing the recurrence of PE following withdrawal of PDE5-Is. In addition, for the PE patient with a definite aetiological cause, the aetiology should be cured first, if PE still exists, followed by PDE-Is prescription. Possible mechanisms that are involved include relaxing the smooth muscles of vas deferens, seminal vesicle, prostate and urethra; decreasing the central sympathetic output; inducing peripheral analgesia; prolonging the duration of erection; and increasing confidence, the perception of ejaculatory control, overall sexual satisfaction, and decreasing the post-orgasmic refractory time to achieve a second erection after ejaculation. Well-designed multicentre studies are urgently warranted to further elucidate the efficacies and safety as well as mechanisms of PDE5-Is in the treatment of PE.
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PMID:Phosphodiesterase 5 inhibitors in the treatment of premature ejaculation. 1657 7

Premature ejaculation (PE) is a common male sexual disorder with an incidence rate of 20-30%. Recent clinical trials have demonstrated that phosphodiesterase type 5 inhibitors (PDE5i), as the first-line drug for erectile dysfunction (ED), can improve ejaculatory function probably by acting on the peripheral and central adrenergic nerves. The possible action mechanisms of PDE5i may involve lessening of the central sympathetic output, modulation of the contractile responses from the vas deferens, seminal vesicles, prostate and urethra, induction of peripheral analgesia, and prolonging of the total erectile duration, increasing the confidence of ejaculation control, and reducing the post-ejaculation refractory time. This review discusses the possible mechanisms and clinical application of PDE5i in the treatment of PE.
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PMID:[Phosphodiesterase type 5 inhibitors for premature ejaculation: advances in studies]. 2624 50

Fluoxetine is one of the top ten prescribed antidepressants. Other therapeutic applications were approved for fluoxetine including, anxiety disorders, bulimia nervosa, and premature ejaculation. However, the role of fluoxetine in nociceptive pain management is still unclear. In this review, we discuss an overview of five possible roles of fluoxetine in pain management: intrinsic antinociceptive effect, enhancement of acute opioid analgesia, attenuation of tolerance development to opioid analgesia, attenuation of dependence development and abstinence syndrome, and attenuation of opioid induced hyperalgesia. Conflicting data were reported about fluoxetine intrinsic anti-nociceptive effect in preclinical and clinical studies except for inflammatory pain. Similar controversy was described in preclinical and clinical studies which explored the possible enhancement of opioid analgesia by fluoxetine co-administration. However, fluoxetine was found to have a promising effect on opioid tolerance and dependence in animal and human studies. Regarding opioid induced hyperalgesia, no studies examined fluoxetine effects in this regard. Our literature review revealed that, the most likely beneficial use of fluoxetine in nociceptive pain management is for alleviation of inflammatory pain and attenuation of opioid tolerance and dependence. Non-steroidal anti-inflammatory and corticosteroids carry many adverse effects and toxicities. Effective alleviation of opioid tolerance and dependence represents a huge health burden and growing unmet medical need. Moreover, most agents used to attenuate these phenomena are either experimental or poorly tolerable drugs which limit their transitional value. Fluoxetine offers an effective, safe, and tolerable alternative for management of both inflammatory pain and opioid tolerance and dependence presently available to clinicians.
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PMID:Uses of fluoxetine in nociceptive pain management: A literature overview. 2960 97

Zha-xun is widely used in Tibetan medicine and is also an international traditional medicine. This article would summarize the use status and research progress of Zha-xun by various ethnic groups all over the world, and the results show that it has various synonyms but most of them imply its most characteristic feature-outflow from the rock; Zha-xun resources are distributed in various places of the world, and its bearing spots are closely related to the geological structure; there are sharp arguments on the origins of Zha-xun, mainly including the minerals origin, biological fossils origin, biological origin, etc. Zha-xun has multiple functions and is mainly used to treat stomach disease, liver disease and rheumatoid arthritis in China, and premature ejaculation, impotence, vaginitis embolism in foreign countries. "Iron" Zha-xun is used into medicines both at home and abroad. According to ancient materia medica texts, it was mainly classified into five types, including gold Zha-xun, silver Zha-xun, copper Zha-xun, iron Zha-xun and lead Zha-xun mainly based on the predominance of color rather than the minerals contained. It is commonly believed by the domestic and foreign scholars that humic acid is the main medicinal part of Zha-xun, and their studies have found that it has a variety of pharmacological activities such as anti-ulcer, anti-inflammatory, liver protection, analgesia, immune regulation, increasing sexual desire and fertility, antioxidation, antibacterial, antidiabetic, antiepileptic, antipsychotic, etc. This paper provides a scientific basis for the rational utilization of Zha-xun resources.
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PMID:[Research progress of Tibetan medicine "Zha-xun"]. 2975