Megestrol acetate drug

Other drugs with glucocorticoid activity (e.g., megestrol acetate, medroxyprogesterone)... 

Farinha, A., Bica, A., and Tavares, P., Improved bioavailability of a micronized megestrol acetate tablet,Drug Dev. Ind. Pharm., 26, 567, 2000. 

A 35-year old Caucasian man with AIDS and multiple opportunistic infections, including Mycobacterium kansasii and Mycobacterium avium complex (MAC) disease developed moderate to severe primary sensorineural hearing loss after 4—5 months of therapy with oral azithromycin 500 mg/day. Other medications included ethambutol, isoniazid, rifabutin, ciprofloxacin, co-trimoxazole, fluconazole, zidovudine (later switched to stavudine), lamivudine, indinavir, methadone, mod-ified-release oral morphine, pseudoephedrine, diphenhydramine, megestrol acetate, trazodone, sorbitol, salbutamol by metered-dose inhaler and nebulizer, ipratropium, and oral morphine solution as needed. Significant improvement of the hearing impairment was documented 3 weeks after drug withdrawal. 

Some drugs are metabolized at particular positions in their skeleton. For example, the oral contraceptive megestrol acetate is oxidized at position 6 to give a hydroxyl group at that position. The introduction of a polar group such as this usually allows the formation of polar conjugates which can be quickly eliminated from the system. 

Wood L, Palmer M, Hewitt J, Urtasun R, Bruera E, Rapp E, Thaell JF. Results of a phase III, double-blind, placebo-controlled trial of megestrol acetate modulation of P-glycoprotein-me-diated drug resistance in the first-line management of small-cell lung carcinoma. BrJ Cancer (1998) 77,627-31. 

Pu Y-S, Cheng A-L, Chen J, Guan J-Y, Lu S-H, Lai M-K, Hsieh C-Y. Megestrol acetate antagonizes cisplatin cytotoxicity. Anticancer Drugs ( 99Z) 9, 733-8. 

The data indicate that the oral bioavailability of nanoparticulate megestrol acetate was 54.8% higher in the fed state when dosed at 450mg and 43.3% higher when dosed at 675 mg in the fed state than the respective values in the fasted state. However, the 800-mg dose of drug in the micronized form was more than 100% more bioavadable in the fed state than in the fasted state. The reduced variability... 

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