Oral Contraceptives Estrogen and Progestin

2 Hormonal contraceptives Hormonal contraceptives contain either a combination of an estrogen and a progestin or a progestin alone. Hormonal contraceptives are available in a variety of preparations, including oral pills, long-acting injections, transdermal patches, vaginal rings, and intrauterine devices

3 types of oral contraceptives Three types of oral contraceptives for women are available: 1.combination estrogen-progestin tablets that are taken in constant dosage throughout the menstrual cycle (monophasic preparations); 2.combination preparations (biphasic and triphasic) in which the progestin or estrogen dosage, or both, changes during the month (to more closely mimic hormonal changes in a menstrual cycle) 3.progestin-only preparations.

4 The postcoital contraceptives The postcoital contraceptives (also known as "emergency contraception") prevent pregnancy if administered within 72 h after unprotected intercourse. Oral preparations containing a progestin (L-norgestrel) alone, estrogen alone, or the combination of an estrogen and a progestin are effective.

5 Combined mode of action of estrogen and progestin Prevents ovulation Thickens mucous in cervix Thins endometrium

6 Adverse Effects Adverse Effects MILD ADVERSE EFFECTS 1. Nausea, mastalgia and oedema 2. Headache is mild and often transient. 3. Withdrawal bleeding sometimes fails to occur

7 Adverse Effects Adverse Effects B. MODERATE ADVERSE EFFECTS 1. Breakthrough bleeding 2. Weight gain is more common with the combination agents 3. Increased skin pigmentation may occur 4. Acne may be exacerbated by agents containing androgen-like progestins 5. Hirsutism 6. Vaginal infections are more common and more difficult to treat in patients who are receiving oral contraceptives. 7. Amenorrhea occurs in some patients

8 Adverse Effects Adverse Effects C. SEVERE ADVERSE EFFECTS 1.Thromboembolism: There is a well- documented increase in the risk of thromboembolic events (myocardial infarction, stroke, deep vein thrombosis, pulmonary embolism) in older women, smokers, and women with a personal or family history of such problems 2.Depression

9 Contraindications & Cautions A.Absolute contraindication 1.patients with thrombophlebitis, thromboembolic phenomena, and cardiovascular and cerebrovascular disorders 2.patients with known or suspected tumors of the breast or other estrogen-dependent neoplasms. 3.Since these preparations have caused aggravation of preexisting disorders, they should be avoided in patients with infective hepatitis and migraine.

10 Contraindications & Cautions B. Relative contraindication 1.patients with past history of thrombophlebitis, thromboembolic phenomena, and cardiovascular and cerebrovascular. 2.DM 3.Hypertension 4.Smoking > 40 cigarettes per day 5.Age over 35 year 6.Obesity 7.Long term immobility 8.Breast feeding

11 Women using oral contraceptives must be made aware of an important interaction that occurs with antimicrobial drugs. Because the normal gastrointestinal flora increases the enterohepatic cycling (and bioavailability) of estrogens, antimicrobial drugs that interfere with these organisms may reduce the efficacy of oral contraceptives. Additionally, coadministration with potent inducers of the hepatic microsomal metabolizing enzymes, such as rifampin, may increase liver catabolism of estrogens or progestins and diminish the efficacy of oral contraceptives

12 ANDROGENS ANDROGENS 1.Testosterone and related androgens are produced in the testis, the adrenal, and, to a small extent, the ovary. 2.The hormone is converted in several organs (eg, prostate) to dihydrotestosterone (DHT), which is the active hormone in those tissues. 3. Because of rapid hepatic metabolism, testosterone given orally has little effect. It may be given by injection in the form of long-acting esters or transdermal patch. Orally active variants are also available ( mesterolon)

13 ANDROGENS ANDROGENS 4.Many androgens have been synthesized in an effort to increase the anabolic effect without increasing androgenic action. (Oxandrolone and stanozolol ) However, all the so-called anabolic steroids have full androgenic agonist effects when used in humans

14 Therapeutic uses 1.Androgenic effects: Androgenic steroids are used in males with inadequate androgen secretion. 2.Anabolic effects: Anabolic steroids can be used to treat senile osteoporosis and severe burns, to speed recovery from surgery or from chronic debilitating diseases. 3.Endometriosis: Danazol, a mild androgen, is used in the treatment of endometriosis and fibrocystic mastitis

15 Adverse effects 1.In females: Androgens can cause masculinization with acne, growth of facial hair, deepening of the voice and Menstrual irregularities. 2.In males: Excess androgens can cause priapism, impotence, decreased spermatogenesis, and gynecomastia. 3.In children: Androgens can cause growth disturbances resulting from premature closing of the epiphyseal plates and abnormal sexual maturation. 4.General effects: Androgens increase serum LDL and lower serum HDL level. Androgens can also cause fluid retention leading to edema.

16 Antiandrogens Reduction of androgen effects is an important mode of therapy for 1. both benign and malignant prostate disease. 2. precocious puberty. 3.hair loss. 4. hirsutism.

17 Antiandrogens Receptor Inhibitors Cyproterone and cyproterone acetate are effective antiandrogens that inhibit the action of androgens at the target organ. These compounds have been used in women to treat hirsutism and in men to decrease excessive sexual drive Flutamide and related drugs (Bicalutamide and nilutamide) are nonsteroidal competitive antagonists of androgen receptors. These drugs are used to decrease the action of endogenous androgens in patients with prostate carcinoma.

18 Antiandrogens Receptor Inhibitors Spironolactone, a drug used principally as a potassium-sparing diuretic also inhibits androgen receptors and is used in the treatment of hirsutism in women.

19 Antiandrogens 5-αReductase Inhibitors Testosterone is converted to DHT by the enzyme 5-α reductase. Some tissues, most notably prostate cells and hair follicles, depend on DHT rather than testosterone for androgenic stimulation. This enzyme is inhibited by finasteride, a drug used to treat benign prostatic hyperplasia and, at a lower dose, to prevent hair loss in men. Because the drug does not interfere with the action of testosterone, it is less likely than other antiandrogens to cause impotence, infertility, and loss of libido. Dutasteride is a newer 5-reductase inhibitor with a much longer half-life than that of finasteride.

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