Endocrine Therapies
David E. Thurston, Ilona Pysz in Chemistry and Pharmacology of Anticancer Drugs, 2021
In the UK, megestrol acetate is recommended by NICE for the treatment of breast cancer. However, it is also used in other countries for the treatment of endometrial and prostate cancers, and as an appetite stimulant for a variety of medical conditions. In the case of cancer patients with cachexia (i.e., loss of appetite), it has been used to induce weight gain. The mechanism of appetite enhancement is unclear, but it is known that megestrol acetate induces a variety of downstream biochemical changes including stimulation of the release of neuropeptide Y in the hypothalamus, modulation of calcium channels in the ventromedial hypothalamus, and inhibition of the secretion of proinflammatory cytokines (e.g., TNF-α, IL-1α, IL-1β, and IL-6), all of which have been implicated in appetite enhancement. Megestrol acetate has also been used at a relatively low dose (e.g., 5 mg) in combination with an estrogen as a contraceptive.
Treatment – Chronic Illness-Related Malnutrition
Jennifer Doley, Mary J. Marian in Adult Malnutrition, 2023
Perhaps the most commonly used appetite stimulant is megestrol acetate, as it is FDA approved for the treatment of cachexia, anorexia, or unexplained weight loss in individuals with AIDS and cancer.38 In a systematic review of its effectiveness and safety, the authors concluded that megestrol acetate did result in increased appetite and slight weight gain of approximately two kilograms. However, several adverse side effects were reported, including thromboembolic events and edema. While 400–800 mg/d is most typically prescribed,38 there is insufficient evidence to suggest an ideal dosage, although weight gain appeared to be associated with higher doses more than lower doses.39 These factors should be considered when decisions are made regarding the use of this medication.
Control of symptoms other than pain
Nigel Sykes, Michael I Bennett, Chun-Su Yuan in Clinical Pain Management, 2008
The results of two systematic reviews on the use of megestrol acetate135, 136[I] demonstrated the following: Megestrol acetate is significantly superior to placebo in increasing appetite, producing weight gain, and increasing patients’ sense of well-being.Weight gain is dose related (160–1600 mg in various trials).Weight gain is mainly due to fat and fluid retention – there is no increase in muscle mass (lean body mass).Megestrol has an antinauseant effect.Quality of life improvements were generally poorly measured in the reviewed trials and there was no effect on survival.
FAACT-Anorexia Cachexia Scale: Cutoff Value for Anorexia Diagnosis in Advanced Non-Small Cell Lung Cancer Patients
Published in Nutrition and Cancer, 2019
Jenny Georgina Turcott, Luis F. Oñate-Ocaña, Giovanny Soca-Chafre, Laura-Alejandra Ramírez-Tirado, Diana Flores-Estrada, Zyanya Lucia Zatarain-Barrón, Oscar Arrieta
CACS treatment modalities include early nutritional intervention, physical activity, and pharmacological treatment (23). Currently used therapeutic drugs include megestrol acetate, which increases appetite and body weight; however, it carries the risk of potential side effect such as thrombo-embolic phenomena, edema, poor response to chemotherapy, and a tendency to lower survival compared with placebo in LC patients (25). Other agents that have proven their effectiveness in patients with NSCLC include anamorelin, which has shown a significant improvement in appetite according to A/CS, incresed body weight and fat-free mass compared with placebo (26). Anamorelin is a ghrelin receptor agonist, but is not available worldwide, including Mexico. On the other hand, cannabinoids have been proposed as a valuable treatment option for treating cancer-related anorexia, particularly nabilone has been associated with increased energy consumption and quality-of-life in LC patients (24).
Effects of crystalline state and self-nanoemulsifying drug delivery system (SNEDDS) on oral bioavailability of the novel anti-HIV compound 6-benzyl-1-benzyloxymethyl-5-iodouracil in rats
Published in Drug Development and Industrial Pharmacy, 2018
Ying-Yuan Lu, Wen-Bing Dai, Xin Wang, Xiao-Wei Wang, Jun-Yi Liu, Pu Li, Ya-Qing Lou, Chuang Lu, Qiang Zhang, Guo-Liang Zhang
Plasma concentration of W-1 was determined using a validated high-performance liquid chromatography (HPLC) method as described in previous publication [12]. Briefly, the HPLC system consisted of a model 510 pump, a model 2487 ultraviolet detector, a model Rheodyne 7725 injector and a column oven. The detection wavelength was 284 nm. The analytical column was a reversed-phase Alltima C18 (4.6 mm × 150 mm, 5.0 μm). The mobile phase was a mixture of acetonitrile and distilled water (60:40, v/v) at a flow rate of 1 ml/min. Megestrol acetate was used as the internal standard (IS). The plasma samples were extracted with ethyl acetate twice using liquid–liquid extraction. The supernatants were combined and evaporated to dryness under a light stream of nitrogen gas at 37 °C. The residue was reconstituted with 100 μL of methanol and 20 µL was injected into the HPLC system. Linearity of the calibration curve of W-1 was obtained over the concentration ranging from 0.01 to 8 μg/mL in rat plasma. The lower limit of quantification (LLOQ) of W-1 was 10 ng/mL and the extraction recoveries ranged from 97.9 to 101.6% [12].
Challenges with optimizing nutrition in cystic fibrosis
Published in Expert Review of Respiratory Medicine, 2019
Carla Colombo, Rita Maria Nobili, Gianfranco Alicandro
The use of appetite stimulants is still controversial because of doubts concerning their efficacy and also due to possible side effects. A recent meta-analysis examined the efficacy and safety of megestrol acetate and of cyproheptadine hydrochloride in a total of 47 patients [21]. In the short term (six months) in adults and children, appetite stimulants improved weight (or weight z score) and appetite, with no difference between the two drugs; side effects were insufficiently reported to fully establish safety [21]. All studies were small in size and offered only a moderate amount of evidence, making it impossible to provide evidence-based recommendations on the use of appetite stimulants for CF patients. Lastly, the beneficial effects of CFTR modulators on nutritional status have been related to several factors including improved appetite and food intake [22] (Figure 2)
Related Knowledge Centers
- Appetite Stimulant
- Birth Control
- Endometrial Cancer
- Estrogen
- Polyphagia
- Cachexia
- Breast Cancer
- Progestogen
- Oral Administration
- Side Effect