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ESTROGENS AND ANDROGENS

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Presentation on theme: "ESTROGENS AND ANDROGENS"— Presentation transcript:

1 ESTROGENS AND ANDROGENS

2 Estrogens Natural: Estradiol, estrone & estriol
Conjugated: premarin (estrone and equillin) Steroidal synthetic: Mestranol & Ethinyl estradiol Non-steroidal synthetic: Diethylstilbesterol Rationale for synthetic: to ↑ oral-bioavailability, half-life and ↑ feedback inhibition on FSH & LH

3 Estradiol – Transdermal patch, IM
Oral – Premarin ( Estrone + Equilin) , Estinyl estradiol , Mestranol Excretion - Renal

4 Estrogens: Clinical Uses
Contraception: ↓ feedback release of gonadotropins Female Hypogonadism (estrogen + progestin) or ovarian failure Estrogens for hormone replacement therapy in menopausal women to ↓ bone resorption Uterine bleeding Dysmenorrhea Men with androgen dependent prostate cancer to slow the growth of the cancer cell.

5 Endometrial hyperplasia Increased skin pigmentation
SIDE EFFECT: Nausea Breast tenderness Endometrial hyperplasia Increased skin pigmentation Increased blood coagulation at high doses Increased risk of endometrial cancer unless progestin is added Breakthrough bleeding DES clear cell adenocarcinoma of vagina in females exposed to DES in utero. Estrogen increases melanin Increase factor 2, 7, 9 & 10 as well as decrease antithrombin III

6 Contraindicated Patients:
With estrogen-dependent neoplasm (e.g. endometrial carcinoma) At higher risk for or with breast carcinoma that are estrogen dependent Predisposed to thromboembolic disease

7 SELECTIVE ESTROGEN RECEPTOR MODULATOR (SERMS)
Are non-steroidal compounds that bind to estrogen receptors. They can act as either agonist, partial agonists and antagonists depending on the tissue

8 Tamoxifene: Has various actions depending on the tissue Bone: agonist to prevent bone resorption Breast: antagonist Endometrium: a partial agonist with the risk of increasing endometrial cancer USES: estrogen dependent breast cancer SE: Hot flushes, nausea and vomiting

9 Raloxifene Bone: agonist Uterus and breast: antagonist
USES: prophylaxis of postmenopausal osteoporosis. SE: increased risk of DVT, pulmonary embolism

10 Clomiphene MOA: ↓ feedback inhibition→ ↑FSH and LH
USE: for infertility caused by anovulatory cycle such as those seen in patients with PCOS Side effect: multiple pregnancies, ovarian enlargement

11 ANTI ESTROGENS Anastrozole:
MOA: is an aromatase inhibitor, resulting in decreased estrogen synthesis USE: estrogen-dependent postmenopausal breast cancer.

12 Progestin's Progestins can be androgenic and antiestrogenic in action
Progesterone: major natural progesterone Medroxyprogesterone Norethindrone 17α-Hydroxyprogesterone Norgestrel Desogestrel: devoid of androgenic and antiestrogenic actions

13 Clinical Uses: Progestins
Major uses: hormone contraception : ↑ feedback inhibition esp LH → no ovulation hormone replacement treatment along with estrogen to decrease endometrial cancer dysmenorrhea

14 Adverse Effects: Progestins
reduce plasma HDL ↑LDL Breakthrough bleeding Acne, weight gain and hirsutism (androgenic effect)

15 ANTIPROGESTIN Mifepristone (RU-486):
Used as an abortifacient, administered with misoprostol (PGE₁) Also an antiglucocorticoid SIDE EFFECT: bleeding, GI effects(nausea, vomiting) and abdominal pain

16 Hormonal Contraception
Progestins (Mini pill) only (norethindrone or norgestrel) Estrogens and progestins (combination pills) Progestin implants Post-coital contraception uses estrogen (mestranol or etinyl estradiol) Mechanism of Action: contraception ovulation-inhibition by suppressing gonadotropins change in cervical mucus(progesterone)

17 Drug interaction: p450 inducers ↓ contraceptive effectiveness
Can result in unwanted pregnancies

18 Combined oral contraceptive pill
ADVANTAGE DISADVANTAGE Reliable (<1% failure) Taken daily ↓ risk of endometrial and ovarian cancer No protection against STDs ↓ pelvic infections ↑ triglycerides ↓ risk of osteoporosis Depression, weight gain, nausea, hypertension No dysmenorrhea Hypercoagulable state

19 SIDE EFFECTS ESTROGENS: Nausea Bloating Headache Mastalgia
Increase skin pigmentation Weight gain Breakthrough bleeding Withdrawal bleeding

20 PROGESTIN: Weight gain Hirsutism Acne Increase LDL

21 Adverse Effects of combined ocps
Venous Thromboembolic Disease breakthrough bleeding Withdrawal bleeding RISK FACTORS: Smoking, Increased age

22 ANDROGENS Testosterone - Cypionate, Enanthate,Propionate
dihydrotestosterone Fluoxymesterone Danazol androstenedione Nandrolone

23 USES: Male hypogonadism For anabolic actions to increase muscle mass Illicit use in athletes

24 Replacement therapy in men
Acne excessive libido & erections, increased muscle & bone mass, aggravation of pre existing prostate cancer.   Reduce plasma HDL and increase LDL

25 Gynecological Disorders: Androgens
Danazol used in the treatment of endometriosis which is the growth of endometrial tissue outside the uterus, especially in the pelvis.

26 SIDE EFFECTS OF ANDROGENS
SE: Excessive masculinization Premature closure of epiphysis Aggression Dependence and abuse Depression of menses and hirsutism in women

27

28 Contraindications: Androgenic Steroids
Pregnant women: its teratogenic Children Androgens - Not used in children Men with prostatic carcinoma

29 Anti-Androgen Cyproterone acetate Flutamide Finasteride

30 Androgen Suppression & Antiandrogens
Symptomatic Management of prostatic carcinoma Management of BPH

31 Antiandrogens Finasteride: Inhibits 5 alpha reductase
Conversion Inhibitors Finasteride: Inhibits 5 alpha reductase decreases dihydrotestosterone levels in the prostate Uses – BPH to reduce the size of the prostate and male pattern baldness Has been replaced by α1 blockers in the symptomatic treatment of BPH DHT causes hair loss and prostate enlargement

32 Antiandrogens Competitive androgenic Receptor Inhibitors:
Cyproterone & Cyproterone acetate Clinical use: Women - hirsutism Men - reduction of sexual drive

33 Antiandrogens Flutamide Competitive inhibitor of androgens
Used in androgen receptor positive Prostatic Carcinoma Testosterone causes the cancer cell to grow more rapidly

34 Bicalutamide Effective orally for the treatment of metastatic prostatic cancer.


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