Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Exemestane is an orally active steroidal aromatase inhibitor that has demonstrated efficacy in the treatment of postmenopausal patients with advanced breast cancer. This compound exhibits a good tolerability and safety profile, which may result from its highly selective mechanism of action. Exemestane binds irreversibly to the aromatase enzyme causing inactivation of the enzyme. This irreversible loss of enzyme may contribute to the sustained inhibition of estrogen synthesis noted following exemestane administration. Exemestane is a potent inhibitor of aromatization reducing estrogen synthesis in vivo by greater than 97%. The recommended dose of exemestane is 25 mg once daily. Although dosages up to 600 mg/day have been tested, the maximum tolerated dose of exemestane has not been reached in clinical study. The most frequently reported drug-related adverse events are hot flushes, nausea and fatigue, which are consistent with the estrogen-suppressive effects of the drug. Discontinuation due to adverse events is rare. Exemestane is a safe and well-tolerated alternative for the treatment of postmenopausal patients with advanced breast cancer.
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PMID:Exemestane in advanced breast cancer. 1108 51

The authors are sharing their experience in using a new medicine Livial (Organon) for the treatment of climacteric complaints. Twenty women have been included in the study. They have received one tablet of 2.5 mg Livial daily throughout four cycles of 28 days. All women report decrease of climacteric symptoms, especially hot flushes and night sweats. Only one of them had genital bleeding while using the drug. Twenty percent of the women reported adverse effects (breast tenderness and nausea), which turned out to be transitional. Conclusions concerning the usage of Livial in the treatment of climacteric complaints have been made.
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PMID:[Our experience in the treatment of climacteric complaints with Livial (Organon)]. 1180 63

Idoxifene is a novel selective oestrogen receptor modulator (SERM) which had greater binding affinity for the oestrogen receptor (ER) and reduced agonist activity compared with tamoxifen in preclinical studies. In a randomized phase II trial in 56 postmenopausal patients with progressive locally advanced/metastatic breast cancer we assessed whether idoxifene showed evidence of activity compared with an increased 40 mg/day dose of tamoxifen in patients who had previously demonstrated resistance to the standard 20 mg/day dose of tamoxifen. Of 47 patients eligible for response (25 idoxifene, 22 tamoxifen), two partial responses and two disease stabilizations (SD) for >6 months were seen with idoxifene (overall clinical benefit rate 16%, 95% CI 4.5-36.1%). The median duration of clinical benefit was 9.8 months. In contrast, no objective responses were seen with the increased 40 mg/day dose of tamoxifen, although two patients had SD for 7 and 14 months (clinical benefit rate 9%, 95% CI 1.1-29.2%). Idoxifene was well tolerated and the reported possible drug-related toxicities were similar in frequency to those with tamoxifen (hot flushes 13% vs 15%, mild nausea 20% vs 15%). Endocrine and lipid analysis in both groups showed a similar significant fall in serum follicle-stimulating hormone and luteinizing hormone after 4 weeks, together with a significant rise in sex hormone binding globulin levels and 11% reduction in serum cholesterol levels. In conclusion, while idoxifene was associated with only modest evidence of clinical activity in patients with tamoxifen-resistant breast cancer, its toxicity profile and effects on endocrine/lipid parameters were similar to those of tamoxifen.
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PMID:A cancer research (UK) randomized phase II study of idoxifene in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. 1472 33

In this pilot study, 22 women with breast cancer on tamoxifen therapy with at least two hot flashes a day took oral gabapentin at 300 mg three times a day for 4 weeks. The 16 women who completed the study had a mean decrease in hot flash duration of 73.6% (P = 0.027), frequency of 44.2% (P < 0.001), and severity of 52.6% (P < 0.001), with a complete response in 8/16 women. Side effects reported by four women who did not complete 4 weeks of the study were nausea (1/4), rash (1/4) and excessive sleepiness (3/4). Two additional patients did not provide complete data. Gabapentin is a promising new agent in the treatment of tamoxifen induced hot flashes, and should be studied further.
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PMID:Pilot study using gabapentin for tamoxifen-induced hot flashes in women with breast cancer. 1499 58

Letrozole (Femara), a nonsteroidal, third-generation aromatase inhibitor administered orally once daily, has shown efficacy in the treatment of postmenopausal women with early-stage or advanced, hormone-sensitive breast cancer. In early-stage disease, extending adjuvant endocrine therapy with letrozole (beyond the standard 5-year period of tamoxifen) improved disease-free survival; compared with placebo there was a 43% relative reduction in disease recurrences or new contralateral breast tumours at a median follow-up of 2.4 years. The results of 4 months' neoadjuvant treatment with letrozole or tamoxifen in postmenopausal women with untreated primary disease favour letrozole. In advanced breast cancer, letrozole was superior to tamoxifen as first-line treatment; time to disease progression was significantly longer (9.4 vs 6.0 months, p < 0.0001) and objective response rate was significantly greater with letrozole, but median overall survival was similar between groups. For second-line therapy of advanced breast cancer that had progressed on antiestrogen therapy, letrozole showed efficacy equivalent to that of anastrozole and similar to or better than that of megestrol acetate. Letrozole is generally well tolerated and has a similar tolerability profile to tamoxifen; the most common treatment-related adverse events were hot flushes, nausea and hair thinning. In patients with tumours that had progressed on antiestrogen therapy, letrozole was tolerated as least as well as, or better than, anastrozole or megestrol acetate. In the trial of extended adjuvant therapy, adverse events reported more frequently with letrozole than placebo were hot flushes, arthralgia, myalgia and arthritis. The long-term effects of letrozole on bone mineral density or lipid profile have not been determined and these parameters may require monitoring. In several pharmacoeconomic modelling studies from various public healthcare system perspectives, letrozole was considered a cost effective choice for first-line (vs tamoxifen) or second-line (vs megestrol acetate) treatment for advanced breast cancer in postmenopausal women. In conclusion, letrozole 2.5 mg/day is effective in the treatment of postmenopausal women with early-stage or advanced breast cancer. The efficacy, cost effectiveness and favourable tolerability profile of letrozole are reflected in current treatment guidelines recommending the drug as first-line therapy for advanced breast cancer. Letrozole is superior to tamoxifen for first-line treatment and is at least as effective as standard second-line treatments in disease that has progressed on antiestrogen therapy. For early-stage disease, letrozole is superior to tamoxifen in the neoadjuvant setting, and prolongs disease-free survival when administered after the standard 5-year period of adjuvant tamoxifen therapy.
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PMID:Letrozole: a review of its use in postmenopausal women with breast cancer. 1516 28

4-Hydroxyandrost-4-ene-3,17-dione (formestane) is a selective aromatase inhibitor. It is indicated for postmenopausal patients with advanced breast cancer. The aim of the present study was to investigate the effect of 4-hydroxyandrost-4-ene-3,17-dione on the bile secretion and metabolism of 4-(14)C-cholesterol to bile acid. The experiments were carried out in the ovariectomized and sham-operated female Wistar rats. Formestane (20 mg/kg, i.m., daily) was administered to animals for 2 weeks. Twenty four hours after the last drug administration, rats were anesthetized with ethyl urethane. 4-(14)C-cholesterol (740 kBq/kg, s.a. 2.28 GBq/mmol) was infused for 1 min by catheter inserted into the jugular vein. Bile samples were assayed for total 14C radioactivity 14C-bile acids were determined in bile (after thin-layer chromatographic separation) by the use of isotopic technique with liquid scintillator. Previous studies showed that systemic adverse effects occurred in about 12% of patients following intramuscular drug administration. Many of them such as hot flushes, vaginal spotting and emotional lability were related to the mechanism of action of formestane i.e. estrogen suppression. Lethargy, rash, nausea, dizziness, indigestion, ataxia, cramps and facial swelling have also been reported. The results of the present study have shown that formestane administered to the female ovariectomized rats decreased the bile secretion and diminished conversion of 4-(14)C-cholesterol to trihydroxy bile acids. The decreased synthesis of trihydroxy bile acids and increased concentrations of cholesterol and litocholic acid in bile may be associated with increased risk of gallstone formation.
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PMID:Effect of 4-hydroxyandrost-4-ene-3,17-dione (formestane) on the bile secretion and metabolism of 4-(14)C-cholesterol to bile acids. 1638 15

To evaluate the safety and efficacy of vardenafil in primary care, we undertook a post-marketing surveillance study in 384 men with erectile dysfunction (ED), enrolled by 22 family physicians in Korea, from July 2004 to August 2005. Of the 384 patients enrolled, 343 (89.3%) returned for efficacy assessment and safety evaluation. Among the latter, 279 patients (81.3%) reported that their erectile function improved, 292 (92.1%) showed enhanced IIEF (International Index of Erectile Function)-5 scores and 265 (77.9%) responded that they were 'very satisfied' or 'satisfied' with vardenafil treatment. The most frequent reason for patient satisfaction with vardenafil was erectile potency (62.4%), followed by safety (42.4%), rapid onset (35.3%), adequate duration of efficacy (28.5%) and easy administration (25.9%). A total of 23 adverse events were observed in 18 patients, with the most frequent being hot flushes (3.2%), followed by headache (1.2%), nasal congestion (0.6%), color vision disturbance (0.3%), dizziness (0.3%), dry mouth (0.3%), dyspepsia (0.3%), nausea (0.3%) and diarrhea (0.3%). Only one patient discontinued vardenafil as a direct result of an adverse event. These results suggest that vardenafil prescribed by primary care physicians improved erectile function and was well tolerated by patients with ED.
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PMID:Post-marketing surveillance study of the efficacy and safety of vardenafil among patients with erectile dysfunction in primary care. 1728 34

To summarise the advances in the hormonal treatment of post-menopausal metastatic breast cancer, this paper reviews the published literature regarding the randomised trials comparing aromatase inhibitors (AIs) versus tamoxifen as a first-line therapeutic choice, or AIs versus megestrole acetate (MEG) as a second-line option. The pooled analysis of these authors on AI versus MEG as a second-line option for post-menopausal metastatic breast cancer suggested that AIs do not add any significant benefit over MEG in terms of overall response rate (ORR) and time to progression. According to the Cochrane Database, use of an AI as a second-line therapy versus any other endocrine therapy (mostly MEG) has shown a significant benefit in terms of overall survival, but not for progression-free survival, clinical benefit (CB) or ORR. Concerning the authors' comparisons between AIs versus tamoxifen as a first-line endocrine option in post-menopausal women with metastatic breast carcinoma, AIs seem to be superior to tamoxifen, with a significant benefit in terms of ORR, CB and time to progression being observed in favour of AIs over tamoxifen with fixed effects estimates. According to the Cochrane Database, there was an advantage to the use of AIs over tamoxifen in terms of progression-free survival and CB, but not for overall survival or ORR. With regards to toxicity, AIs show similar levels of hot flushes and arthralgia, increased risks of nausea, diarrhoea and vomiting, but a decreased risk of vaginal bleeding and thromboembolic events compared with other endocrine therapies. Weight gain, dyspnoea and peripheral oedema seem to be more frequent with MEG. At present, there is no proved overall survival difference in patients who are treated first with an AI and then with tamoxifen compared with the opposite sequence. In the metastatic setting, results are limited and are based on retrospective analyses.
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PMID:Aromatase inhibitors in post-menopausal metastatic breast carcinoma. 1759 87

We investigated the clinical efficacy of milnacipran (Serotonin-Noradrenalin Reuptake Inhibitor: SNRI) in prostate cancer patients who suffer from hot flushes. Our study included 12 patients who had taken hormone therapy for at least 3 months prior to the trial entry. All patients had severe hot flushes at least 3 times daily. Among 12 patients, 7 subjects received milnacipran 25 mg orally once a day and 5 subjects received 50mg once a day. The questionnaire was used to measure the frequency and severity of hot flushes at baseline, and at 6 and 12 weeks. At 12 weeks, 9 patients were available for the evaluation. Four patients received 50 mg per day and 5 patients received 25 mg per day. The patients with > or =50% decrease in baseline hot flash score were observed in 3 out of 4 who received 50 mg and 2 out of 5 who received 25 mg per day. The frequency of hot flushes had significantly decreased at the 12 weeks period than the baseline in the milnacipran 50 mg per day treatment group (p < 0.05, paired t-test). Adverse events were observed in 3 patients: 2 cases of nausea and 1 case of constipation. However, all of them were mild to moderate. These results indicated that milnacipran 50 mg per day therapy is effective in the treatment of hot flushes, which is the side effect of hormone therapy for prostate cancer.
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PMID:[The clinical efficacy of SNRI milnacipran in the treatment of hot flushes with prostate cancer hormonally treated]. 1762 34

Medical treatments including chemotherapy, endocrine therapy, and antibody therapy effectively reduce the risk of recurrence after breast cancer and are also used against metastatic disease. This article reviews patients' experience of these treatments. Common side effects of chemotherapy include hair loss, nausea, hot flushes, mucositis, fatigue, and cognitive side effects. Overall quality of life, social relations, and sexuality may also be affected. Endocrine therapies are characterised by hot flushes, vaginal dryness, arthralgias, and reduced libido.
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PMID:[Patients' experience of breast cancer treatment]. 1787 63


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