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Anabolic and related sports supplements

Anabolic and related sports supplements
Agent Alternative name(s) listed on supplement label Proposed mechanism of activity Potential adverse effects
Anabolic steroids Often described using chemical terms such as "androstra-3,5-diene-7,17-idone" Agonists of endogenous androgens, including testosterone

Acne vulgaris, gynecomastia, neuropsychiatric symptoms (mood disorders, aggressive behavior)[1-3]

With oral 17-alpha-alkylated androgens: LFT abnormalities, cholestatic jaundice, and peliosis hepatis[1-3]

Hypogonadism (in males) can occur following discontinuation[2]
Aromatase inhibitors Testolactone, letrozole, anastrozole, exemestane Inhibits aromatase (which converts androstenedione to estrone, and testosterone to estradiol) Reduced bone mineral density, cardiovascular disease, diabetes, hypercholesterolemia, myalgias
SARMs Andarine (GTX-007, S-4 cpd), ostarinestarine, LGD-4033 SARMs which bind better to androgen receptors in certain tissues (eg, muscle and bone) than to those in genital tissues[4,5] Unknown
SERMs (eg, tamoxifen, raloxifene, others) * When used by males taking exogenous testosterone, they prevent gynecomastia that develops due to testosterone conversion to estradiol Flushing, hypertension, depression, menstrual irregularities
IGF-1 Deer antler velvet, deer velvet (deer antler velvet supplements have been adulterated with pharmaceutical IGF-1 [mecasermin])[6] Stimulates growth of many tissues Irreversible enlargement of tissues, including joints, heart, and liver[6,7]
Testing of dietary supplements often reveals drugs not declared on labeling, labeled drugs/herbs not detected in the product, inaccurate quantities, and adulteration with prescription and experimental drugs. In addition, doses contained in supplements may far exceed pharmaceutical quantities, increasing the risks of adverse effects. For review of health risks and an approach to patient counseling, refer to UpToDate topic reviews of high-risk dietary supplements and performance-enhancing drugs and hormones in sport.

LFT: liver function test; SARMs: selective androgen receptor modulators; SERMs: selective estrogen receptor modulator; IGF-1: insulin-like growth factor 1.

* Typically not declared/listed on supplement label.
References:
  1. Timcheh-Hariri A, Balali-Mood M, Aryan E, et al. Toxic hepatitis in a group of 20 male body-builders taking dietary supplements. Food Chem Toxicol 2012; 50:3826.
  2. Maravelias C, Dona A, Stefanidou M, Spiliopoulou C. Adverse effects of anabolic steroids in athletes. A constant threat. Toxicol Lett 2005; 158:167.
  3. Krishnan PV, Feng ZZ, Gordon SC. Prolonged intrahepatic cholestasis and renal failure secondary to anabolic androgenic steroid-enriched dietary supplements. J Clin Gastroenterol 2009; 43:672.
  4. Van Wagoner RM, Eichner A, Bhasin S, et al. Chemical composition and labeling of substances marketed as selective androgen receptor modulators and sold via the internet. JAMA 2017; 318:2004.
  5. US Food and Drug Administration. Dietary supplement ingredient advisory list. Available at: https://www.fda.gov/food/dietary-supplement-products-ingredients/dietary-supplement-ingredient-advisory-list (Accessed on July 17, 2022).
  6. Cox HD, Eichner D. Detection of human insulin-like growth factor-1 in deer antler velvet supplements. Rapid Commun Mass Spectrom 2013; 27:2170.
  7. Adams GR. Insulin-like growth factor in muscle growth and its potential abuse by athletes. Br J Sports Med 2000; 34:412.
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