Exemestane a new steroidal aromatase inhibitor of clinical relevance

If an etiology is identified, a targeted therapy can be provided; however, delays in evaluation may require empiric treatment for patient comfort. 1 It is reasonable to begin with a trial of a phenothiazine, such as prochlorperazine, because these medications are effective in a range of clinical situations. A trial of a prokinetic agent (., metoclopramide [Reglan]) may then be beneficial. Serotonin antagonists (., ondansetron [Zofran]) are effective and are better tolerated than phenothiazines and prokinetics, but their high cost (approximately $20 per dose, even for the recently approved generic ondansetron) makes long-term use impractical. Trials determining the specific effectiveness of medications for nausea and vomiting are limited; therefore, a trial of any medication may be reasonable on an individual basis. 1   Antiemetic agents commonly used for nausea and vomiting are listed in Table 4 1 , 2 , 6  ; therapies for known etiologies of nausea and vomiting are listed in Table 5 2 , 20 – 26  ; and alternative therapies are listed in Table 6 . 22 , 27 – 29

Other Endocrine Effects
Exemestane does not bind significantly to steroidal receptors, except for a slight affinity for the androgen receptor (% relative to dihydrotestosterone). The binding affinity of its 17-dihydrometabolite for the androgen receptor, however, is 100 times that of the parent compound. Daily doses of exemestane up to 25 mg had no significant effect on circulating levels of androstenedione, dehydroepiandrosterone sulfate, or 17-hydroxyprogesterone, and were associated with small decreases in circulating levels of testosterone. Increases in testosterone and androstenedione levels have been observed at daily doses of 200 mg or more. A dose-dependent decrease in sex hormone binding globulin (SHBG) has been observed with daily exemestane doses of mg or higher. Slight, nondose-dependent increases in serum luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels have been observed even at low doses as a consequence of feedback at the pituitary level. Exemestane 25 mg daily had no significant effect on thyroid function [free triiodothyronine (FT3), free thyroxine (FT4), and thyroid stimulating hormone (TSH)].

Exemestane a new steroidal aromatase inhibitor of clinical relevance

exemestane a new steroidal aromatase inhibitor of clinical relevance

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