浙江大学医学院：《药理学》课程教学资源（PPT课件）影响生殖系统的药物 Drugs Affecting Reproductive System

Drugs Affecting Reproductive System Ling Ding, Ph. D, Associate Professor College of Pharmaceutical Sciences Zhejiang University China 310058 Email:Id362@zju.edu.cn

Drugs Affecting Reproductive System Ling Ding, Ph. D., Associate Professor College of Pharmaceutical Sciences Zhejiang University China 310058 Email: ld362@zju.edu.cn

GnRH FSH Female antenor pitutary :242 and LH Pituitary Hormones ollicular phase Ovarian Cycle 下 progesterone systemIc effects PL⊥LLLL utenne Ovarian Hormones endometrium 1315 secretory phase

Female systemic effects

hypothalamus GnRH Male ante pituitary FSH testis seminiferous systemIc interstitial tubules y sperm effects produce produce sperm testosterone plus inhibin

Male systemic sperm effects

Sex hormones and related drugs Estrogens and antiestrogens Progestogens and antiprogestogens ● Contraceptive drugs Drugs acting on uterus smooth muscle

• Estrogens and antiestrogens • Contraceptive drugs • Drugs acting on uterus smooth muscle • Progestogens and antiprogestogens Sex hormones and related drugs

Estrogens and antiestrogens Three maior naturally occurring oestrogens in women Estradiol (e2) the predominant form in nonpregnant females Estrone(el)produced during menopause Estriol(e3) the primary oestrogen of pregnancy

Three major naturally occurring oestrogens in women • Estradiol (E2) the predominant form in nonpregnant females • Estrone (E1) produced during menopause • Estriol (E3) the primary oestrogen of pregnancy Estrogens and antiestrogens

④A心B R1 Derivative RI R2 estradio雌〓醇 H 戊酸雌二醇 Estradiol valerate C(CH2)3CH3 雌二醇环戊丙酸脂 Estradiol cypionate C(CH2)2 乙炔雌二醇 Ethinyl estradiol C≡CH 氢甲睾丸素 Mestranol -CH3 C≡CH 炔雌醚 Quinestrol C≡CH 雌酮 Estrone Estrone sulfate -SO3H - 马烯雌酮 Equilint O " Designates C 17 ketone Also contains 7.8 double bond

雌二醇 戊酸雌二醇 雌二醇环戊丙酸脂 乙炔雌二醇 氢甲睾丸素 炔雌醚 雌酮 马烯雌酮

Estrogens and antiestrogens H3C OH OH HOr HOr Estradiol雌二醇 Diethylstibestrol己烯雌酚 H5 C2 NCH2 ch20 C=C Clomiphene氯米酚

H5C2 H5C2 NCH2CH2O C Cl C H3C OH HO OH HO Estradiol 雌二醇 Diethylstibestrol 己烯雌酚 Clomiphene 氯米酚 Estrogens and antiestrogens

Estrogens Pharmacological effects Development of the female genital tract and of the female secondary sex characteristics Maintenance of both proliferative and secretory phases of the uterine endometrium Ovulation T(small doses)or\(larger doses) Development of the breast and lactescence (small doses)or v(larger doses)

Pharmacological effects • Development of the female genital tract and of the female secondary sex characeteristics. • Maintenance of both proliferative and secretory phases of the uterine endometrium • Ovulation:  (small doses) or  (larger doses) • Development of the breast and lactescence •  (small doses) or  (larger doses) Estrogens

Estrogens Pharmacological effects Other actions: decreasing postmenopausal disturbances in sleep inhibiting the reabsorption of bone increasing aldosterone and causing water and nat retention decreasing Ldl and increasing hDl levels in plasma increasing factor Il, VIl, IX, X and coagulation

Other actions: • decreasing postmenopausal disturbances in sleep • inhibiting the reabsorption of bone • increasing aldosterone and causing water and Na+ retention • decreasing LDL and increasing HDL levels in plasma • increasing factor II, VII, IX, X and coagulation Pharmacological effects Estrogens

Estrogens 88 SLEEP 0 Estrogen decreases post- OSTEOPOROSIS menopausal disturbances in sleel Estrogen decreases the resorption of bone but has no effect on bone formation Estrogen decreases frequency of hip CARDIOVASCULAR fracture.[Note: Dietary calcium(1,000 to 1, 500 mg daily)and weight-bearing exercise o In postmenopausal women also slow loss of bone. ]J estrogen provides a protective effect against cardiovascular disease causing a decrease Treatment with estrogens must begin in LDL and an increase in HDL within 2 or 3 years of menopause, earlier levels in plasma. if possible UROGENITAL TRACT VASOMOTOR Estrogen treatment re-establishes Estrogen treatment reverses feed-back on hypothalamic control of postmenopausal atrophy norepinephrine secretion, leading to of vulva, vagina, urethra, and decreased frequency of" hot flashes trigone of the bladder. Pharmacological effects of estrogens

Pharmacological effects of estrogens Estrogens