Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0016382 (flushing)
 6,387 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Leuprorelin (leuprolide acetate) is a synthetic analogue of gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH)] which initially stimulates luteinising hormone (LH) and hence testicular androgen release; continuous administration then results in profound suppression of these hormones. Testosterone levels associated with castration are attained within 3 to 4 weeks. A biodegradable subcutaneous or intramuscular depot formulation of leuprorelin 3.75 or 7.5 mg, which releases the drug at a constant rate over 28 days, is available and may be preferred over daily subcutaneous injections. The progression of previously untreated advanced prostatic cancer is delayed in 70 to 90% of men receiving leuprorelin, with median survival of approximately 2 years. The efficacy of leuprorelin is equivalent to that of estrogen therapy, but the tolerability of the GnRH analogue is far better. In contrast to most other studies of GnRH agonists, a slight survival advantage has been reported for combined treatment with leuprorelin and the antiandrogen flutamide. Small noncomparative trials reveal that leuprorelin also causes regression of benign hyperplastic prostate tissue with corresponding relief of obstructive, but not irritative, symptoms although continuous treatment is necessary to maintain remission. Impotence and flushing occur in most leuprorelin recipients but, unlike diethylstilbestrol (stilboestrol), cardiovascular toxicity and gynaecomastia are not significant problems. Symptom flare, usually manifested as bone pain in prostate cancer patients and exacerbation of obstructive symptoms in those with benign prostatic hypertrophy, can occur in 4 to 29% at the beginning of treatment. Leuprorelin treatment is therefore an established effective palliative measure in men with previously untreated advanced prostatic cancer, and may have a role in those with benign hypertrophy who are unfit for surgery.
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PMID:Leuprorelin. A review of its pharmacology and therapeutic use in prostatic disorders. 179 35

(1) The reference treatment for uterine leiomyoma with major symptoms is surgery. (2) Leuprorelin and triptorelin, two Gn-RH analogues, are the first drugs to be licensed in France for preoperative treatment of uterine leiomyoma associated with anaemia, when a reduction in the size of the leiomyoma is necessary to facilitate or modify the surgical technique. (3) A double-blind placebo-controlled trial of leuprorelin in nearly 300 anaemic women showed no advantage in terms of the need for non autologous transfusion. (4) Three double-blind placebo-controlled trials have shown that leuprorelin reduces the volume of uterine leiomyomas, but whether or not this facilitates or modifies the surgical technique is not known. An unblinded trial versus lynestrenol in non anaemic women showed a superior effect of leuprorelin on the size of the leiomyoma, but again there were no data on a possible effect on the choice of surgical technique. (5) In the absence of comparative double-blind trials, the observed effects of triptorelin on the choice of surgical technique are uninterpretable. (6) The adverse effects of leuprorelin are mainly linked to its hormone effect, i.e. flushing, headache, vaginitis and vaginal dryness. There are no recent reviews of the adverse effects of triptorelin in this setting. (7) In practice, for anaemic women with leiomyomas requiring surgery, there is no proof that leuprorelin and triptorelin have any tangible clinical advantages.
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PMID:Leuprorelin and triptorelin: new indication. Preoperative treatment of uterine leiomyoma: no proven value. 1171 67