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CONTRACEPTIVE AND PRO-FERTILITY AGENTS

CONTRACEPTIVE AND PRO-FERTILITY AGENTS. Yulia Komarova , Ph.D. ykomarov@uic.edu. Oral Contraceptives. Combined – contain both estrogenic and progestogenic agents Monophasic Multiphasic Biphasic Triphasic Continuous use of progestin only “ minipill ” – Progesterone only

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CONTRACEPTIVE AND PRO-FERTILITY AGENTS

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  1. CONTRACEPTIVE AND PRO-FERTILITY AGENTS YuliaKomarova, Ph.D. ykomarov@uic.edu

  2. Oral Contraceptives Combined – contain both estrogenic and progestogenic agents • Monophasic • Multiphasic • Biphasic • Triphasic Continuous use of progestin only “minipill” – Progesterone only New Generation • Yasmin – oral - new progestin component • Ortho Evra – transdermal • Etonogestrel - implantable • Nuvaring – hormone-releasing vaginal ring

  3. Oral and Implantable Contraceptive Agents

  4. Oral and Implantable Contraceptive Agents

  5. Benefits of Oral Contraceptives • Reduction of Pregnancies • Reductions of menstrual disorders • Reduction of premenopausal/menopausal symptoms • Reduction of reproductive organ neoplasms • Reduction of reproductive disorders (Pelvic Inflammatory Disease & endometriosis • Reduced incidence of ectopic pregnancies • Other: reduction of acne, anemia, ulcers, rheumatoid arthritis

  6. Pharmacologic effect of Contraceptive Agents

  7. Severe Adverse Effects

  8. Clotting disorders Known cancer Hepatic disorders Diabetes - insulin Pregnancy Age older than 35 years and smoker Migraine Hypertension Varicose veins Cardiac/renal dysfunction Diabetes w/o insulin Hepatitis Hypercholesterolemia Contraindications Relative Contraindications

  9. Postcoital Contraceptives

  10. Pro-fertility agents:Estrogen Inhibitors and Antagonists • tamoxifen, a competitive partial agonist inhibitor of estradiol at the estrogen receptor, • is used in the palliative treatment of breast cancer in postmenopausal women and for chemoprevention of breast cancer in high-risk women; • may increase the risk of endometrial cancer • raloxifene ,estrogen agonist-antagonist, is approved for the prevention of postmenopausal osteoporosis and prophylaxis of breast cancer in women with risk factors. • clomiphene, partial agonist, is used as an ovulation-inducing agent cyclophenanthrene structure triphenylethylene structure benzothiophene structure triphenylethylene structure

  11. Multiple Outcomes of Raloxifene Evaluation (MORE) Double Blind Placebo-Controlled Trial 7705 PMP women aged 31 to 80 Raloxifene 60 mg/d or 120 mg/d or placebo Follow-up for 36 months for efficacy and 40 months for adverse events Increased bone mineral density (BMD) in femoral neck by 2.1% (60 mg) and by 2.4% (120 mg) Increased BMD in spine by 2.6% (60 mg) and by 2.7% (120 mg) Increased risk of venous thromboembolism Conclusions:Raloxifene increases BMD in spine and femoral neck and reduces risk of vertebral fracture – but increases risk of venous thromboembolism

  12. Clomiphene • Clomiphene is used in the treatment of ovulation disorders in patients who wish to become pregnant. It stimulates ovulation in 70% of women. The compound is of no value in patients with ovarian or pituitary failure. • Clomiphene is also used in men to stimulate gonadotropin release and enhance spermatogenesis • Clomiphene increases the amplitude of LH and FSH pulses, without a change in pulse frequency, acting largely at the pituitary level to block inhibitory actions of estrofene on gonadotropin release from the gland • Adverse Effects • hot flushes, occasionally, headache, constipation, allergic skin reactions, and reversible hair loss have been reported • multiple pregnancy is approximately 10%. • Contraindications • special precautions should be observed in patients with enlarged ovaries. • treatment with clomiphene for more than a year may be associated with an increased risk of low-grade ovarian cancer

  13. Selective Estrogen Receptor Modulators (SERMs)

  14. Other Therapies for Induction of Ovulation • Gonadotropins: • Follicle-stimulating hormone analog: follitropin-α • Human chorionic gonadotropin (hCG) • Synthetic GnRH Agonists • Gonadorelin (short-acting GnRH)

  15. Side effects of synthetic fertility drugs • headache • flushing • abdominal discomfort • hot flashes, osteoporosis • vaginal dryness • altered lipid metabolism • multiple births • emotional lability • acne • weight gain • hirsituism

  16. Progesterone Inhibitors and Antagonists • Mifepristone, a "19-norsteroid“, that binds strongly to the progesterone receptor and inhibits the activity of progesterone • is used as postcoital contraceptive • limited clinical studies suggest that mifepristonemay be useful in the treatment of endometriosis, Cushing's syndrome, breast cancer • Danazol, an isoxazole derivative of ethisterone (17 -ethinyltestosterone) with weak progestational, androgenic, and glucocorticoidactivities • binds to androgen, progesterone, and glucocorticoid receptors, and to sex hormone-binding and corticosteroid-binding globulins • is use in the treatment of endometriosis; it can be given in a dosage of 600 mg/d. The dosage is reduced to 400 mg/d after 1 month and to 200 mg/d in 2 months. About 85% of patients show marked improvement in 3–12 months. • is used in the treatment of fibrocystic disease of the breast and hematologic or allergic disorders

  17. Literature: Bertram G. Katzung, Susan B. Masters, Anthony J. Trevor Basic & Clinical Pharmacology, 11e,

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