Basic clinical Pharmacology Drugs affecting reproductive system
Drugs affecting reproductive system Basic & Clinical Pharmacology
Drugs affecting male reproductive system Classification A Androgens and antiandrogens 1. testosterone(睾酮) 2. methyltestosterone(甲睾酮) orally effective 3. testosterone propionate(丙酸睾丸素) most commonly used 4. mesterolone(甲二氢睾酮,美睾酮) 5 fluoxymesterone(氟甲睾酮 6 testosterone phenyl- acetate(苯乙酸睾丸素) 7.tristeronum compositum testosterone propionate 25mg estradiol benzoate(苯甲酸雌二醇)1.25mg progesterone 12.5mg,im B Antiandrogens cyproterone(环丙孕酮,环甲氯地孕酮 C. Drugs used to treat erectile dysfunction sidenafil(西地那非)
Classification A. Androgens and antiandrogens 1. testosterone(睾酮 ) 2. methyltestosterone(甲睾酮) orally effective 3. testosterone propionate (丙酸睾丸素) most commonly used 4. mesterolone (甲二氢睾酮，美睾酮) 5.fluoxymesterone(氟甲睾酮) 6.testosterone phenyl-acetate(苯乙酸睾丸素) 7.tristeronum compositum testosterone propionate 25mg estradiol benzoate(苯甲酸雌二醇) 1.25mg progesterone 12.5mg，i.m B. Antiandrogens • cyproterone(环丙孕酮，环甲氯地孕酮) C. Drugs used to treat erectile dysfunction • sidenafil(西地那非) Drugs affecting male reproductive system
A. Androgens and antiandrogens Androgens OH 0-C-( CH2)9-CH3 Testosterone睾酮 Testosterone undecanoate十一酸睾酮 OC—CH2CH: 一一“ Nandrolone phenylpropionate 苯丙酸诺龙
A. Androgens and antiandrogens Androgens Testosterone 睾酮 Testosterone undecanoate 十一酸睾酮 O O H CH2CH2 O C Nandrolone phenylpropionate 苯丙酸诺龙
26 Mineralo cortic oids (21 carbons) 27 Cholesterol Aldosterone Cholesterol side-chain Aldosterone lavage enzyme synthas Deoxy- Progesterone corticosterone Corticosterone Pregnenolone 17a-hydroxyla n 17a-hycroxy 1a-hydroxy e pregnene progesterone OH 0 11-deoxycartisol Cortisol 1.20ba5g Glucocorticoids (21 carbons) Dehycoepi- Andtoste-3 strone androsterone redone 17阝-HsD Estriol Adrostenedd Testosterone Estrada 5a-reductase Cellular location of enzymes Mitochondria Dihydrotestosterone Smooth endoplasmic reticulum
A. Androgens and antiandrogens Pharmacological effects (1)Development of the male sexual apparatus and secondary sex characteristics (2) Necessary for normal spermatogenesis(精子发生) (3)Increasing protein anabolism (4) Promoting growth of blood cells in bone marrow, especially for red blood cells(EPO D) (other effects: immune regulation, antinflammation effects, cvs effects
Pharmacological effects (1) Development of the male sexual apparatus and secondary sex characteristics (2) Necessary for normal spermatogenesis (精子发生) (3) Increasing protein anabolism (4) Promoting growth of blood cells in bone marrow, especially for red blood cells (EPO ) (5)Other effects: immune regulation, antiinflammation effects,CVS effects A. Androgens and antiandrogens
A. Androgens and antiandrogens Clinical uses (1) Replacement therapy in men hypogonadism (2)Female disorders: dysfunctional uterine bleeding endometriosis(子宫内膜异位症), advanced breast and ovarian cancers (3 Anemia: aplastic or other anemia ( largely replaced by recombinant erythropoietin (4) Infirmity(体质虚弱): anabolic steroids(同化激素) (oThers: male contraception, osteoporosis(either alone or in conjunction with estrogens. Replaced by bisphosphonates)etc
Clinical uses (1) Replacement therapy in men: hypogonadism (2)Female disorders: dysfunctional uterine bleeding, endometriosis (子宫内膜异位症), advanced breast and ovarian cancers (3) Anemia: aplastic or other anemia (largely replaced by recombinant erythropoietin ) (4) Infirmity (体质虚弱): anabolic steroids (同化激素) (5) Others: male contraception, osteoporosis(either alone or in conjunction with estrogens. Replaced by bisphosphonates) etc. A. Androgens and antiandrogens
A. Androgens and antiandrogens Adverse effects due largely to their masculinizing actions and are most noticeable in women and prepubertal children (1) Sex dysfunction: virilisation in female (hirsutism acne amenorrhea, clitoral enlargement, and deepening of the voice, testosterone> 200-300 mg of per month) o increased libido in male (2) Hepatic toxicity occurs early in the course of treatment, the degree is proportionate to the dose bilirubin levels t
Adverse effects - due largely to their masculinizing actions and are most noticeable in women and prepubertal children. (1) Sex dysfunction: • virilisation in female(hirsutism, acne, amenorrhea, clitoral enlargement, and deepening of the voice, testosterone> 200–300 mg of per month) • increased libido in male (2) Hepatic toxicity • occurs early in the course of treatment, the degree is proportionate to the dose. bilirubin levels ↑ A. Androgens and antiandrogens
A. Androgens and antiandrogens Contraindications 1. pregnant women, infants and young children (somatotropin is more appropriate to produce a growth spurt) 2. male patients with carcinoma of the prostate or breast. 3. renal or cardiac disease predisposed to edema Caution: Several cases of hepatocellular carcinoma have been reported in patients with aplastic anemia treated with androgen anabolic therapy. Erythropoietin and colony- stimulating factors should be used instead
A. Androgens and antiandrogens Contraindications 1. pregnant women, infants and young children (somatotropin is more appropriate to produce a growth spurt). 2. male patients with carcinoma of the prostate or breast. 3. renal or cardiac disease predisposed to edema Caution: Several cases of hepatocellular carcinoma have been reported in patients with aplastic anemia treated with androgen anabolic therapy. Erythropoietin and colonystimulating factors should be used instead
A. Androgens and antiandrogens Classic anabolic hormones 1. Growth hormone 2. IGF1 and other insulin-like growth factors 3. Insulin 4. Testosterone and analogs 5. Estradiol
A. Androgens and antiandrogens Classic anabolic hormones 1. Growth hormone 2. IGF1 and other insulin-like growth factors 3. Insulin 4. Testosterone and analogs 5. Estradiol
A. Androgens and antiandrogens Anabolic-androgen steroids(AAS) Drugs which mimic the effects of the male sex hormones testosterone and dihydrotestosterone They increase protein synthesis within cells, which results in the buildup of cellular tissue(anabolism), especially in muscles. Anabolic steroids also have androgenic and virilizing properties, including the development and maintenance of masculine characteristics such as the growth of the vocal cords, testicles, and body hair(secondary sexual characteristics)
Anabolic-androgen steroids (AAS) • Drugs which mimic the effects of the male sex hormones testosterone and dihydrotestosterone. • They increase protein synthesis within cells, which results in the buildup of cellular tissue (anabolism), especially in muscles. • Anabolic steroids also have androgenic and virilizing properties, including the development and maintenance of masculine characteristics such as the growth of the vocal cords, testicles, and body hair (secondary sexual characteristics). A. Androgens and antiandrogens