Anabolic steroids

MBBS Sem IV theory class

1. Anabolic Steroids Dr. Pravin Prasad M.B.B.S., MD Clinical Pharmacology Lecturer, Lumbini Medical College 1 July, 2018 (17 Ashad , 2075), Sunday

2. By the endo of the class, MBBS Sem IV students will be able to: List the anabolic steroids Explain the pharmacological basis of use of anabolic steroids List the side effects of anabolic steroids List the contraindication of anabolic steroids

3. Pre-test Which of the following is the male sex hormone: A. Testosterone B. Estrogen C. Both A and B D. None

4. Pre-test Which of the following is not an effect of testosterone: Development of sexual characters in male Pubertal growth spurt in males Increasing the erythropoiesis in females Fusion of epiphyses in males (Androgenic effect) (Anabolic effect)

5. Anabolic steroids: Introduction Synthetic androgens Higher anabolic activity Anabolic: androgenic activity = 1 to 3 Lesser selectivity in human Are indicated in scenarios requiring only the anabolic effects of testosterone

6. Anabolic steroids: Classification 17 α -alkyl substituted compounds: Oxymetholone Stanozolol Others: Methandienone Nandrolone Testosterone Stanozolol

7. Anabolic steroids: Mechanism of Action Similar to testosterone

8. Anabolic steroids: Mechanism of Action MOA: Binds to androgen receptors (AR) Interacts with the androgen response elements Modifies gene transcription in presence of co-activators and co-repressors

9. Anabolic steroids: Preparations available Methandienone: Oral tablets- 2mg, 5mg Oral drops- 2mg/mL Intramuscular injection- 25mg/mL Nandrolone: Intramuscular injection- 10mg/mL, 25mg/mL, 100mg/mL

10. Anabolic steroids: Preparations available Oxymetholone: Oral tablets- 5mg, 50mg Stanozolol: Oral tablet- 2mg Intramuscular injection- 50mg/ampoule

11. Anabolic steroids: Uses Catabolic states Acute illness, cancer cachexia, major surgery Acts by reducing N 2 loss Transient response only seen Indicated for short term therapy 1 2 3

12. Anabolic steroids: Uses Indication Basis of use of anabolic steroids Other/preferred drugs Osteoporosis In elderly males due to prolonged immobilization Alendronate, Zolendronate Suboptimal growth in boys Brief spurts in linear growth seen Useful in hypogonadism Somatropin Anaemia (hypoplastic, malignancy associated, haemolytic) Increases RBC count and Hb% Erythropoietin

13. Anabolic steroids: Misuse Enhance physical abilities in athletes Steroids+ exercise = increased strength of muscle Short-lived effects Uncertain improvement in performance Considered illegal Included in dope-test

14. Anabolic steroids: Side effects Cholestatic jaundice Lowering of HDL and rise in LDL levels Virilization, excess body hair and menstrual irregularities in females Salt retention, edema

15. Anabolic steroids: Contraindications Carcinoma of prostate Carcinoma of male breast Liver and kidney disease During pregnancy

16. Future Prospects Selective Androgen Receptor Modulators Ostarine , Andarine Higher anabolic:androgenic ratio Completed phase II clinical trials: Decreased HDL levels Increased AST/ALT Not approved by US-FDA till date Available as dietary supplements: illegal

17. Conclusion Anabolic steroids are synthetic androgens with higher selectivity for anabolic effects They are used for brief duration during catabolic states Their use to boost athletic performance is illegal SARMs are more selective for anabolic effects of androgens

18. Questions?? Thank you!