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Androstenedione/Drug Interactions:
5 alpha reductase inhibitors5 alpha reductase inhibitors: In human studies of patients taking finasteride, a synthetic antiandrogen that inhibits type II 5-alpha reductase, levels of serum androstenedione were not observed to change; however, a significant decrease in the 5 alpha-androstane-3 alpha,17 beta-diol glucuronide/androstenedione ratio was noted, indicating a possible interaction of 5-alpha reductase inhibitors with androstenedione (20; 23; 42). AlcoholAlcohol: Evidence from a study in premenopausal women using oral contraceptives indicates that alcohol consumption altered the metabolism of androstenedione (18). AndrogensAndrogens: In clinical research oral androstenedione increased circulating testosterone and estradiol in men (1). Concurrent administration of androgens and exogenous androstenedione may cause excessive testosterone levels and increase the risk of adverse effects. Anti-androgensAnti-androgens: In humans, androgen receptor blockers, including flutamide and biclutamide, antagonized the effects of androstenedione (7; 8). Anticoagulants and antiplateletsAnticoagulants and antiplatelets: In humans, androstenedione caused platelet aggregation, blood clots, and erythrocytosis (3; 4). AntidiabeticsAntidiabetics: Human evidence has been conflicting regarding whether metformin or troglitazone use altered the metabolism of androstenedione (9; 10; 11). AntifungalsAntifungals: In humans, ketoconazole inhibited steroid synthesis primarily by inhibition of 17-20 desmolase and 17-hydroxylase (12; 13). In humans, higher levels of androstenedione correlated to a higher likelihood of response to ketoconazole (12). AntilipemicsAntilipemics: A number of clinical trials indicate that androstenedione decreased high density lipoprotein cholesterol (HDL-C) levels (5; 4; 15; 3) and increased the low-density lipoprotein cholesterol (LDL-C/HDL-C)/(apolipoprotein A/apolipoprotein B) lipid ratio (3). Aromatase inhibitorsAromatase inhibitors: Androstenedione may be converted to estrone and estradiol by aromatization (4). Based on clinical evidence, administration of fadrozole (an aromatase inhibitor) to postmenopausal patients with advanced breast cancer altered androstenedione metabolism (16). CabergolineCabergoline: In humans, cabergoline altered metabolism of androstenedione (14). ContraceptivesContraceptives: Androstenedione is a precursor to estrogen and may increase estrogen levels in humans (17). Other human study has shown reduced endogenous androstenedione levels were in woman taking hormonal contraceptive agents (43; 44; 45). Evidence from a study in premenopausal women using oral contraceptives indicates that alcohol consumption altered the metabolism of androstenedione (18). CorticosteroidsCorticosteroids: In a study of healthy men that took dexamethasone, a decrease in plasma concentrations of androstenedione was observed (19).EstrogensEstrogens: Androstenedione is a precursor to estrogen increased estrogen levels in humans (17). Androstenedione may be converted to estrone and estradiol by aromatization (4). In clinical study, serum levels of estradiol and estrone were raised following androstenedione administration (4). In a study of postmenopausal women with cardiovascular disease receiving oral conjugated estrogens or transdermal estradiol-17-beta, an inverse relation between the change in androstenedione levels was observed (46). Gonadotropin-releasing hormone (GnRH) agonistsGonadotropin-releasing hormone (GnRH) agonists: A decrease in serum androstenedione levels has been observed in several studies of women taking a GnRH agonist (20; 8; 21). HepatotoxinsHepatotoxins: Based on secondary sources, androstenedione may cause liver damage.OctreotideOctreotide: In a human trial of infertile women given octreotide concurrently with human menopausal gonadotrophin, octreotide therapy lowered androstenedione concentrations (22). PhotosensitizersPhotosensitizers: Based on anecdotal reports, androstenedione may cause photosensitivity.SpironolactoneSpironolactone: Spironolactone may inhibit ovarian and adrenal biosynthesis of androgens, and directly inhibit 5-alpha-reductase activity. However, in human study, spironolactone treatment has a lack of an effect on serum androstenedione levels (23). Androstenedione/Herb/Supplement Interactions:
GeneralGeneral: Some individuals combine androstenedione with other supplements such as dehydroepiandrosterone (DHEA), puncture vine, saw palmetto, indole-3-carbinol, and chrusin (DION) in the hopes of lessening the adverse effects of androstenedione such as increased levels of estradiol and dihydrotestosterone (DHT), which are associated with increased prostate cancer risk(6). Data pertaining to the effectiveness of these combinations in preventing androgenic effects in humans, however, are lacking. AndrogensAndrogens: In clinical research oral androstenedione has been shown to increase circulating testosterone and estradiol in men (1). Concurrent administration of androgens and exogenous androstenedione may cause excessive testosterone levels and increase the risk of adverse effects. Anti-androgensAnti-androgens: In humans, androgen receptor blockers, including flutamide and biclutamide, may antagonize the effects of androstenedione (7; 8). Anticoagulants and antiplateletsAnticoagulants and antiplatelets: In humans, androstenedione caused platelet aggregation, blood clots, and erythrocytosis (3; 4). AntilipemicsAntilipemics: A number of clinical trials indicate that androstenedione decreased HDL-C levels (5; 4; 15; 3) and increased the LDL-C/HDL-C/(apolipoprotein A/apolipoprotein B) lipid ratio (5.2% increase with androstenediol;10.5% increase with androstenedione) (3). ContraceptivesContraceptives: Androstenedione is a precursor to estrogen and may increase estrogen levels in humans (17). Other human study has shown reduced endogenous androstenedione levels were in women taking hormonal contraceptive agents (43; 44; 45). Evidence from a study in premenopausal women using oral contraceptives indicated that alcohol consumption altered the metabolism of androstenedione (18). Dehydroepiandrosterone (DHEA)Dehydroepiandrosterone (DHEA): In human study, androstenedione supplementation increased DHEA concentrations (3). HepatotoxinsHepatotoxins: Based on secondary sources, androstenedione may cause liver damage.HypoglycemicsHypoglycemics: Human evidence has been conflicting regarding whether metformin or troglitazone use alters the metabolism of androstenedione (9; 10; 11). PhotosensitizersPhotosensitizers: Based on anecdotal reports, androstenedione may cause photosensitivity.PhytoestrogensPhytoestrogens: Androstenedione is a precursor to estrogen and may increase estrogen levels in humans (17). Androstenedione may be converted to estrone and estradiol by aromatization (4). In clinical study, serum levels of estradiol and estrone were raised following androstenedione therapy (4). In a study of postmenopausal women with cardiovascular disease receiving oral conjugated estrogens or transdermal estradiol-17-beta, a significant inverse relation between the change in androstenedione levels was observed (46). Saw palmettoSaw palmetto: Some manufacturers suggest that saw palmetto be taken in conjunction with androstenedione to reduce androgenic side effects including hair loss and prostate enlargement. In a study of male subjects that took a nutritional supplement (AND-HB) containing saw palmetto, basal serum androstenedione concentrations were observed to increase (47). Administration of a supplement containing DHEA, androstenedione, Tribulus terrestris, chrysin, indole-3-carbinol, and saw palmetto caused alterations in serum levels of sex hormones and interleukins (15). The protective mechanism of saw palmetto may involve interference with androgen receptors (24). SteroidsSteroids: Androstenedione is a steroid hormone produced in the adrenal glands and the gonads, and the biochemical precursor to the sex hormones testosterone, estrone, and estradiol. In a study of healthy men that took dexamethasone, a decrease in plasma concentrations of androstenedione was observed (19).Androstenedione/Food Interactions:
AlcoholAlcohol: Evidence from a study in premenopausal women using oral contraceptives indicates that alcohol consumption altered the metabolism of androstenedione (18). Androstenedione/Lab Interactions:
Body massBody mass: In human study, a small increase in lean body mass was observed, but these findings were lacking statistical significance (26). Dehydroepiandrosterone (DHEA) levelsDehydroepiandrosterone (DHEA) levels: In human study, androstenedione supplementation increased DHEA concentrations (3). Estrogen levelsEstrogen levels: In a study of healthy males enrolled in an eight-week resistance training program, serum levels of estradiol and estrone were raised by ~50% following two weeks of therapy with 300mg androstenedione daily (4). Androstenedione is a precursor to estrone and might alter results of estrone assays (17; 3). In a study of healthy men, serum estradiol levels were elevated 42% with 100mg androstenedione and 128% with 300mg daily (1). In women administered single oral doses of androstenedione, serum levels of estrone were elevated up to ~115% over 12 hours at the 100mg dose, while estradiol levels were unaffected (48). Hemoglobin/hematocritHemoglobin/hematocrit: In human study, androstenedione supplementation did not significantly affect hemoglobin/hematocrit (4). InterleukinsInterleukins: Administration of a supplement containing DHEA, androstenedione, Tribulus terrestris, chrysin, indole-3-carbinol, and saw palmetto did not change LPS-induced production of interleukin (IL)-1-beta, and phytohemagglutinin (PHA)-induced IL-2, IL-4, IL-10, or interferon (IFN)-( production in vitro, but did increase IL-4 levels (15). Iron levelsIron levels: In human study, androstenedione supplementation did not significantly affect total iron (4). Lipid profileLipid profile: Further clinical research has indicated a decrease in HDL-C levels and an increase in respective LDL-C/HDL-C/(apolipoprotein A/apolipoprotein B) lipid ratio (5.2% increase with androstenediol;10.5% increase with androstenedione) (3). Several other clinical studies have also shown that serum HDL cholesterol was reduced following androstenedione supplementation (5; 4; 15). Liver function testsLiver function tests: Based on secondary sources, androstenedione may cause liver damage. While anabolic steroid intake has been associated with an increase in serum levels of liver enzymes, research has found liver enzymes in serum after androstenedione intake and found that serum liver enzyme levels were unaffected by an eight-week period of androstenedione administration (4). Luteinizing hormone (LH)/follicle stimulating hormone (FSH)Luteinizing hormone (LH)/follicle stimulating hormone (FSH): Alterations in androstenedione metabolism have been noted in studies of women taking follicle stimulating hormone (FSH) (49; 50). Androstenedione supplementation elevated plasma luteinizing hormone (LH) approximately 70% but did not alter testosterone concentration in human study (51). In other human study however, serum concentrations of LH and FSH were unaffected by androstenedione supplementation (4). Nandrolone urine testNandrolone urine test: Trace contamination of androstenedione with 19-norandrostenedione may result in positive urine test results for nandrolonenondrolone use in humans (52). PSA levelsPSA levels: A lack of significant changes in prostate-specific antigen (PSA) levels was observed following androstenedione supplementation in human study (26). Testosterone levelsTestosterone levels: Androstenedione is a precursor to testosterone and may alter results of total and free testosterone assays during the first month of androstenedione use in humans. It has been observed that levels of testosterone in the blood begin to rise approximately 15 minutes after administration of androstenedione and remain elevated for about three hours, with testosterone levels peaking at 1-1.5 hours. However, testosterone levels tend to normalize when androstenedione is used for longer than one month (17; 3). According to a German patent (DE 42 14953 A1. 1995) for androstenedione, 50mg given orally raised plasma testosterone levels 140%-183% above normal, whereas 100mg of androstenedione raised levels 211%-337% above normal. Some studies indicate that, when taken orally, androstenedione produces significantly more testosterone than either a placebo or DHEA (32; 33; 34; 35; 36; 37; 38). Women taking 100mg oral doses of androstenedione have also shown significant increases in serum testosterone, with a 450% increase observed over 12 hours (48) and a 16-fold increase observed over 24 hours (53). The results with men have been variable, with no changes in serum testosterone levels observed following a single 100mg androstenedione dose or extended administration (4; 54; 26; 51), although one study reported a mean ~35% increase in testosterone in the serum at the 300mg daily dose in men (1). Administration of a supplement containing DHEA, androstenedione, Tribulus terrestris, chrysin, indole-3-carbinol, and saw palmetto caused increases in serum levels of free testosterone, estradiol, and DHT (15).