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Androgens & Anabolic
Steroids
Dr. Indrajit Banerjee
MBBS, MD
Department of Pharmacology
Learning Objectives
Androgens
 Synthesis, secretion & Regulation
 Pharmacological actions
 Pharmacokinetics
 Preparati...
Androgens
 Testes – 3-12mg testosterone from cholesterol
 5 alpha reductase – dihydrotestosterone in
extraglandular tiss...
Secretion & Regulation of testosterone
Pharmacological Actions
1) Androgenic – dev. of sex organs & secondary
sexual characters
Thickening of skin
Loss of subcut...
Anabolic Actions
(3) Skeleton & skeletal muscles- growth spurt
Bone growth – thickness & length
After puberty – epiphyses ...
Mechanism of Action
 Testosterone – dihydrotestosterone- cytoplasmic
receptor- combine with DNA
 DNA transcription- prot...
Pharmacokinetics
 High first pass metabolism
 Inactive orally (IM injection / synthetic esters
used)
 Methyltestosteron...
Preparations
Testosterone Preparations Dose
Testosterone suspension 50-100mg / 2 weeks
Testosterone esters:
 Testo. propi...
Side Effects
 In women – virilization, menstrual irregularities,
hirsuitism, acne
 In male –acne, oligozoospermia, preco...
Clinical Uses
 Replacement therapy in Testicular failure –
primary / secondary
 Hypopituitarism- added at the time of pu...
Anabolic Steroids
 Synthetic androgens High anabolic action, low
androgenic action
 Methandienone- 2-5 mg OD, oral, 25 m...
Uses
 Catabolic states – severe trauma, acute illness,
major surgery, elderly, under nourished, debilitated
–sense of wel...
Abuse…….
 To enhance
physical ability
in athletes- Increase the
strength of exercised
muscles- mostly
short lived
list of...
Adverse effects
 Anabolic steroids were developed with the
idea of avoiding the virilizing side effects of
androgens whil...
Contraindications
 Same as testosterone
 carcinoma of prostate and male breast, liver
and kidney disease and during preg...
Impeded androgens &
Antiandrogens
Danazol (Impeded Androgens)
 Orally active mild androgenic, anabolic & progestational
activity
 Suppression of Gn secret...
Side Effects
 Complete amenorrhoea
 Androgenic – acne, hirsuitism, deepening of
voice, edema, weight gain
 Hot flashes ...
Antiandrogens
 Synthetic GnRH agonists
 Estrogens
 Ketoconazole
 Spironolactone
 Cimetidine
 Cyproterone acetate
 F...
Flutamide
 Non-Steroidal, Specific antiandrogenic drug
 Blocks androgen action on sex organ, pituitary –blocks
feed back...
Finasteride
 5 alpha reductase inhibitor
 Selective for type-II isoenzyme in male urogenital
tract
 Lowers dihydrotesto...
Androgens& Anabolic steroids_MBBS_ENDOCRINOLOGY_PHARMACOLOGY
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Androgens& Anabolic steroids_MBBS_ENDOCRINOLOGY_PHARMACOLOGY

  1. 1. Androgens & Anabolic Steroids Dr. Indrajit Banerjee MBBS, MD Department of Pharmacology
  2. 2. Learning Objectives Androgens  Synthesis, secretion & Regulation  Pharmacological actions  Pharmacokinetics  Preparations & Therapeutic uses  Adverse effects Anabolic steroids  Differ from androgens?  Preparations & Therapeutic uses  Adverse effects Impeded Androgens & Anti-androgens
  3. 3. Androgens  Testes – 3-12mg testosterone from cholesterol  5 alpha reductase – dihydrotestosterone in extraglandular tissue  Adrenal cortex- dehydroepiandrosterone, androstenedione (weak androgens)  Ovary –small amount testosterone
  4. 4. Secretion & Regulation of testosterone
  5. 5. Pharmacological Actions 1) Androgenic – dev. of sex organs & secondary sexual characters Thickening of skin Loss of subcutaneous fat Voice deepens Behavioural effects 2) Testes –Normal spermatogenesis Maturation of spermatozoa
  6. 6. Anabolic Actions (3) Skeleton & skeletal muscles- growth spurt Bone growth – thickness & length After puberty – epiphyses fuse Muscle building aided by exercise Nitrogen retaining effect (4) Erythropoiesis – increased renal erythropoietin secretion
  7. 7. Mechanism of Action  Testosterone – dihydrotestosterone- cytoplasmic receptor- combine with DNA  DNA transcription- protein synthesis
  8. 8. Pharmacokinetics  High first pass metabolism  Inactive orally (IM injection / synthetic esters used)  Methyltestosterone & fluoxymesterone - orally  Highly protein bound (98% to SHBG & albumin)  Estradiol – in extraglandular tissue
  9. 9. Preparations Testosterone Preparations Dose Testosterone suspension 50-100mg / 2 weeks Testosterone esters:  Testo. propionate  Testo. phenylpropionate  Testo. cypionate  Testo. enanthate 25-50 mg / 3 times a week 40-60mg / 1 or 2 week 100 – 200mg / 2 weeks 250 mg / 2 weeks Orally active  Methyl testosterone tab.  Fluoxymesterone  Mesterolone 25-50 mg/d oral; 5-10 mg/d sublingual 2-10 mg/d oral Gel 5-10 g applied OD Implants wall of abdomen/thigh Transdermal Patches One patch OD on back, abdomen, upper arms, or thighs
  10. 10. Side Effects  In women – virilization, menstrual irregularities, hirsuitism, acne  In male –acne, oligozoospermia, precocious puberty, short stature, gynaecomastia (estradiol)  Edema- heart, kidney disease  Cholestatic jaundice- not with esters  Hepatic carcinoma  Low HDL, high LDL - Atherosclerosis
  11. 11. Clinical Uses  Replacement therapy in Testicular failure – primary / secondary  Hypopituitarism- added at the time of puberty along with other hormones  AIDS related muscle wasting  Hereditary angioneurotic edema- Methytestosterone / Danazol prevent attacks
  12. 12. Anabolic Steroids  Synthetic androgens High anabolic action, low androgenic action  Methandienone- 2-5 mg OD, oral, 25 mg IM, weekly  Nandrolone phenylpropionate –10-50mg wkly IM Nandrolone decanoate- 25-100mg IM every 3 wky  Oxymetholone-5-10 mg oral  Stanozolol - 2-6 mg oral
  13. 13. Uses  Catabolic states – severe trauma, acute illness, major surgery, elderly, under nourished, debilitated –sense of well being, appetite  Osteoporosis- senile, postmenopausal, GC induced ( Bisphosphonates are preferred)  Suboptimal growth in children  Hypoplastic, haemolytic, malignancy associated anaemia  Renal Failure- urea production & frequency of dialysis
  14. 14. Abuse…….  To enhance physical ability in athletes- Increase the strength of exercised muscles- mostly short lived list of ‘dope test’
  15. 15. Adverse effects  Anabolic steroids were developed with the idea of avoiding the virilizing side effects of androgens while retaining the anabolic eftect  Oxymetholone and Stanozolol -Jaundice, worsen lipid profile.
  16. 16. Contraindications  Same as testosterone  carcinoma of prostate and male breast, liver and kidney disease and during pregnancy (masculinization of female foetus)  They should be used cautiously in patients who may be adversely affected by fluid retention-such as CHF  It can worsen epilepsy, migraine
  17. 17. Impeded androgens & Antiandrogens
  18. 18. Danazol (Impeded Androgens)  Orally active mild androgenic, anabolic & progestational activity  Suppression of Gn secretion from pituitary in both sexes  Inhibition of testicular / ovarian function  Uses - Endometriosis – 200-800 mg/d relieves pain, dyspareunia, dysmenorrhoea, excessive bleeding - Menorrhagia- 200 mg/d - Fibrocystic breast disease: pain, nodularity & engorgement - Precocious puberty in boys - Infertility
  19. 19. Side Effects  Complete amenorrhoea  Androgenic – acne, hirsuitism, deepening of voice, edema, weight gain  Hot flashes in women, night sweats, muscle cramps, GI upset, increased hepatic enzymes
  20. 20. Antiandrogens  Synthetic GnRH agonists  Estrogens  Ketoconazole  Spironolactone  Cimetidine  Cyproterone acetate  Flutamide, Bicalutamide, Nilutamide  Finasteride, Dutasteride
  21. 21. Flutamide  Non-Steroidal, Specific antiandrogenic drug  Blocks androgen action on sex organ, pituitary –blocks feed back inhibition- increase LH  Used in - Prostatic carcinoma with GnRH agonist - Female hirsuitism alongwith oral contraceptive  ADR – gynaecomastia, liver damage Bicalutamide & Nilutamide: more potent, longer acting- given OD less hepatotoxic
  22. 22. Finasteride  5 alpha reductase inhibitor  Selective for type-II isoenzyme in male urogenital tract  Lowers dihydrotestosterone levels  Uses- BHP (5mg/d)-symptom relief, retard disease progression – combined with α1 blocker - Male pattern baldness (1mg/d)  ADR- loss of libido, impotence, skin rash Dutasteride: inhibits both type I & II isoenzymes Clinical responses faster without α1 blockade
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