Fluctuations in biochemical parameters defining cardiovascular, liver and muscoskeletal health were analyzed to evaluate the health status of world class bodybuilders using performance enhancement drugs such as anabolic-androgenic steroids (AAS) [testosterone propionate, drostanolone propionate (Masteron), trenbolone acetate (Finajet), oxandrolone (Anavar), stanozolol (Winstrol) and boldenone undecylenate], human growth hormone (HGH) and “fat-burning drugs” [triiodothyronine (t3), clenbuterol, mesterolone (Proviron), tamoxifen citrate (Nolvadex) and 2,4-Dinitrophenol (2,4-DNP)], and a 6-month preparation period. Changes in serum levels of total cholesterol (TC), triglyceride (TG), high-density lipoprotein (HDL-C), low-density lipoprotein (LDL-C), aspartate aminotransferase (AST), alanine transaminase (ALT), and bilirubin, as well as body mass (BM) and total body fat percentage (BF%), were measured as a function of the competition preparation period. The study shows a continuous increase in BM, accompanied by a decrease in BF% to the physiologically optimal level. TC levels varied significantly within the desired concentration range (TC < 5.18 mmol / L), and TG fluctuated between the ranges of concentrations borderline high (1.69 mmol / L ≤ TG < 2.26 mmol / L) and high (2.26 mmol / L ≤ TG < 5.65 mmol / L) concentration ranges. HDL-C levels remained within the low range (TG < 1.03 mmol / L), whereas LDL-C fluctuated across all physiologically important ranges, that is, near-optimal / above optimal (2.59 mmol / L ≤ LDL-C < 3.34 mmol / L), borderline high (3.35 mmol / L ≤ LDL-C < 4.11 mmol / L), and high (4.14 mmol / L ≤ LDL-C < 4.91 mmol / L). AST and ALT concentrations remained within the high-concentration region, i.e., > 0.58 mkat / L and > 0.91 mkat / L. Bilirubin concentration fluctuated within the desirable limits (3.42 mmol / L ≤ Bilirubin < 2.53 mmol / L), and urea concentration were between desirable (3.2 mmol / L ≤ Urea < 7.9 mmol / L) and high values (Urea ≥ 7.9 mmol / L). Although most of the changes are within physiologically acceptable ranges, there are evident disturbances in LDL-C and Urea levels induced by performance-enhancing drugs. To our knowledge, this study is among the few, if not the only, that discloses the physiological changes associated with doping-assisted preparations for an international bodybuilding contest.