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General Pharmacology Sex hormone (estrogen, progestin and androgen مادة اﻻدوية –المرحلة الثالثة: د. عماد نعمان شريف • • Objective :- • - Know the drug used as sex hormone agonist and antagonist.- • - Know the pharmacokinetic, pharmacodynamic , indication, side effect, contraindication for drug used as estrogen, profgesterone and androgen agonists and antagonists. • - How treatment of erectile dysfunction. SEX HORMONES: (estrogen, progestin and androgen). • Sex hormones are steroids (fat soluble compounds) that control sexual maturity and reproduction. These hormones are produced mainly by the endocrine glands. The endocrine glands in females are ovaries and those in males are testes. While both males and females have all types of hormones present in their bodies, females produce the majority of two types of hormones, estrogens and progesterone, while males produce mainly androgens such as testosterone. Most androgens produced by females are converted to estrogens and some androgens in males are also converted to estrogens. Sex hormones are synthesized from cholesterol (a fatty acid) and other compounds and secreted throughout a person's lifetime at different levels. Their production increases at puberty and normally decreases in old age. • Hormone Production; • The production of hormones are a complex process. At puberty, the brain's hypothalamus gland produces increased amounts of gonadotropin-releasing hormone. This hormone stimulates the nearby pituitary gland to release two other hormones: follicle-stimulating hormone (FSH) and luteinizing hormone (LH). Finally, these two hormones signal the sex glands (gonads) to produce the sex hormones. • Female Reproductive cycle: • Females produce three estrogens: estradiol, estriol, and estrone. These estrogens stimulate growth of the ovaries and begin preparing the uterus for pregnancy. Estrogens also control the body's secondary sex characteristics, including breast and pelvic development and the distribution of fat and muscle. Progesterone maintains uterine conditions during pregnancy. It also acts on the central nervous system in a way that isn't yet understood. During the monthly reproductive cycle, FSH stimulates growth of an ovarian body called the graafian follicle. The follicle encloses the egg. LH aids in the rupture of the follicle, sending the egg to the fallopian tubes. LH also promotes growth of the corpus luteum (a yellow, progesterone- secreting mass of cells that forms from an ovarian follicle after the release of a mature egg) as the ovary prepares to release the egg into the uterus. • If no pregnancy occurs within 10-12 days, the corpus luteum withers and the uterus shed the blood supply that was formed to nourish a fetus. This shedding of the uterine lining and blood supply is called menstruation (the period). The production of estrogens and progesterone drops dramatically, and the cycle begins again. • Male Reproduction • In males, LH stimulates the development of the testes. The testes produce the androgens testosterone and androsterone. When FSH activates the testes' sperm-forming cells, testosterone maintains the process of forming sperm. This is the ten-week process results in sperm constantly ready for release by ejaculation from the penis. The androgens also promote the secondary sex characteristics of muscle growth, lowered voice range, the Adam's apple, and increased body hair. Estrogen:- • Action:- • 1- increase growth, development of uterus, fallopian tube, and oviduct. • 2- Increase growth, development of myometherium during puberty and pregnancy. • 3- Increase endothelial lining of endometherium (proliferative phase). • 4- Increase epithelial layer, secretion of vagina. • 5- Increase duct formation of breast (prepare for lactation). • 6- Decrease bone resorption, but has not effect on bone formation. • 7- Increase HDL, decrease LDL and TG. • = Estrogen therapy:- • Indication: • 1- Hormonal replacement therapy. • 2- Reduces or eliminates several symptoms of menopause such as hot flushes, disturbed sleep resulting from hot flashes and vaginal dryness. • 3- Oral contraceptive in combination with progesterone. • 4- Delayed puberty. • 5- Primary dysmenorrheal. • 6- Acne and hirsutism. • 7- Carcinoma prostate: It is androgen dependent tumors and estrogens acts by suppressing the androgen production. • Adverse effect: • 1- Nausea, headache and breast tenderness. • 2- Postmenopausal uterine bleeding. • 3- The risk of thromboembolic events, peripheral edema, hypertension, myocardial infarction, breast and endometrial cancer. • Estrogen formulations and route of administration: Oral, transdermal, subcutaneous implants, vaginal (ring, cream, tablet or pessary), skin patch, gel, nasal spray which is delivers 300 micrograms of estradiol daily. • Preparations of estrogens: • = Estrogen. • - Ethinyl estradiol • - Estradiol, estrone and estriol. • - Estrasorb. • - Conjugated estrogens (premarin). • - Estropipate (piperazine estrone sulphate). • - Diethylstilbestrol (stilbestrol). • = Selective estrogen receptor modulators (SERMS): Combine estrogenic and antiestrogenic properties (raloxifene, clomiphene, tamoxifene, toremifene and tibolone). They readily absorbed after oral absorption. • - Clomiphene: Is structurally related to diethylstilbestrol; it is a weak estrogen agonist less activity than natural estrogens, • Mode of action: It act as a partial estrogen agonist and interferes with the negative feedback of estrogen on the hypothalamus. This effect thereby increases the secretion of gonadotropin-releasing hormone and gonadotropins leading to stimulating ovulation. • Clomiphene is administered during the early follicular phase of the menstrual cycle (50mg daily on days 2-6) and is successful in inducing ovulation in about 85% of women. • Uses: • - Treat infertility associated with anovulatory cycles , but not effective in women with ovulatory dysfunction due to pituitary or ovarian failure. • Side effect: Are dose related. • 1- Headache, nausea, vasomotor flushes, visual disturbance, and ovarian enlargement. • 2- Multiple ovulation with multiple pregnancy may occur 3-5%. • 3- There have been reports of an increased incidence of ovarian carcinoma following multiple exposure, and the number of consecutive cycles for which clomiphene may be used to stimulate ovulation should be limited to 12. • - Cyclofenil: Acts similarly to clomiphene. • Tamoxifene: Is a non-steroidal competitive estrogen antagonist on target organs as breast tissue. Although available for anovulatory infertility (20 mg daily on days 2,3,4, and 5 of the cycle). • Uses: • 1- Its main use in the treatment of estrogen-dependent breast cancer. • 2- Is currently used in the palliative treatment of metastatic breast cancer in postmenopausal women. • 3- It may also be used as adjuvant therapy following mastectomy or radiation in breast cancer and as a prophylactic therapy to reduce the risk of breast cancer in high risk patients. • adverse effects:- • 1- Hot flashes and nausea. • 2- Menstrual irregularities and vaginal bleeding • Raloxifene: Has antiestrogenic effects on breast and endometerium, but estrogenic effects on bone and is used for prevention and treatment of osteoporosis. It is approve for the prophylaxis of breast cancer in high risk women, but increases risk of deep-vein thrombosis, pulmonary embolism and retinal vein thrombosis, in addition raloxifene should be avoided in women who are or may become pregnant. • Tibolone: Is licensed for short-term treatment of osteoporosis. • Progesterone:- • Progesterone:- • Action: • 1- Maintain uterine condition during pregnancy. • 2- Decrease uterine motility and contraction. • 3- Increase mammary gland action. • 4- Negative feedback on LH which decrease ovulation. • 5- Thick, viscous secretion in cervix. • 6- Decrease aldosterone effect. • 7- Decrease plasma levels of many amino acids. • Indication of Progestational Agents (therapy)in clinical practice: • 1- Hormonal deficiency. • 2- Dysfunctional uterine bleeding. • 3- A part from contraceptive, they are generally used with estrogen, either in combination or in a sequential manner. • 4- Dysmenorrheal and endometriosis. • 5- Infertility. • Adverse effect: • - Headache, depression, weight gain and change in lipido. • - Some type can increase the ratio of LDL to HDL cholesterol and cause acne and hirsutism. • - Injectable medroxyprogesterone acetate has been associated with an increased risk of osteoporosis. • Preparation: • 1- Natural. The most side effect are fatigue and sedation. • 2- Synthetic • - Oral: Norethindrone, norethindrone acetate, norgestrel, levonorgestrel, desogestrel, norgestimate, drospirenone. • - Suppositories or pessaries: Progesterone. • - Injectable: Progesterone, hydroxyprogesterone, medroxyprogesterone. ANTIPROGESTOGENS:- • Antiprogestogen, also called an antiprogesterone agent, is a type of hormone antagonist which antagonizes or suppresses the action of progesterone in the body. • Menstruation (in its luteal phase) is dependent on progesterone, and uterine bleeding follows antagonism of progesterone. Pregnancy is dependent on progesterone (for implantation, endometrial stimulation, suppression of uterine contraction and placanta formation), and abortion follows progesterone antagonism in early pregnancy. • Mifepristone: Is a progesterone antagonist with partial agonist activity and has potent antiglucocorticoid activity. Is orally active. • Adverse effect: Nausea and vomiting, dizziness, asthenia, abdominal pain, uterine bleeding may be heavy. It also offers the opportunity for mid-trimester
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