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ANTIFERTILITY/ FERTILITY DRUGS

ANTIFERTILITY/ FERTILITY DRUGS. HYPOTHALAMUS. 1) GnRH. ANTERIOR PITUITARY. 2) FSH. LH. OVARY. 3) ESTROGENS ( β -ESTRADIOL) AND PROGESTERONE. Plasma concentrations of the gonadotropins & ovarian hormones during the normal female sexual cycle.

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ANTIFERTILITY/ FERTILITY DRUGS

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  1. ANTIFERTILITY/ FERTILITY DRUGS

  2. HYPOTHALAMUS 1)GnRH ANTERIOR PITUITARY 2)FSH LH OVARY 3)ESTROGENS (β-ESTRADIOL) AND PROGESTERONE

  3. Plasma concentrations of the gonadotropins & ovarian hormones during the normal female sexual cycle

  4. Types of Progestogens1. Progesterone, i.m. (ineffective orally) 2. Hydroxyprogesterone, i.m. 3. Dydrogesterone, tablets 4. Medroxyprogesterone, i.m &tablets 5. Norethindrone, tablets Use of Progestogens 1. Contraception 2. Dysmenorrhea 3. Infertility due to inadequate luteal phase

  5. Types of estrogens a.Natural and semisynthetic estrogens1. Estradiol 2. Estrone 3. Estriol 4. Ethinylestradiol 5. Mestranol (3-methyl ether of ethinylestradiol) b. Synthetic estrogens1. Diethylstilbestrol 2. Proestrogens e.g. Chlorotrianisene

  6. Use of estrogens 1. Contraception 2. Dysmenorrhea 3. Hypogonadism(estrogen-deficient patients) 4. Menopause - hot flushes, muscle cramp, anxiety, over breathing 5. Osteoporosis-Increase ca² deposition in bones 6. Prostatic Cancer(anti-androgenic effect)

  7. ADVERSE EFFECTS A. Estrogen Related 1. Nausea and breast tenderness 2. Headache(migrain is getting worse) 3. Increase Skin Pigmentation 4. Impair glucose tolerance(hyperglycemia) 5. Increase incidence of breast, vaginal and cervical cancer?? 6. Cardiovascular — most concern a. Thromboembolism b. Hypertension 7. Increase Frequency of gall bladder disease

  8. ADVERSE EFFECTS (Cont’d)B. Progestin Related1. Nausea, vomiting 2. Headache(very common) 3. Fatigue, depression of mood 4. Menstrual irregularities 5. Prolonged menstrual bleeding(8 days or more) 5. Weight gain(fluid retention) 6. Increased facial or body hair growth(hirsutism) 7. Masculinization (Norethindrone) 8. Ectopic pregnancy

  9. Oral Contraceptives Combination of estrogen & progestin are the most common (100% effective ) The concentration of estrogen is very low to minimize its side effects Contraceptive pills are taken for 21 days starting on 5th day of cycle The tablets should be taken at approx. the same time each day Phase formulations are more closely mimic normal endogenous hormonal activity (see table)

  10. Contraceptives(Cont’d) Contraceptives containing only a progestin are also available (progestogen only pill or minipill” P.O.P). Most effective 4-5 hrs after taking it. What are the indications?

  11. Indications for contraceptives containing only a progestogen (minipill): When it is desirable to eliminate estrogen:1. During breast feeding (estrogen suppress postpartum lactation) 2. Contraindications to estrogen (e.g. hypertension or breast cancer) 3. Older users & smokers more than 35years old Disadvantages 1. Slightly higher failure rate (efficacy 97%) 2. Irregular bleeding 3. Should be taken every day, 365 days of the year 4. Risk of ectopic pregnancy

  12. Contraceptives containing only a progestin 1. Oral tabletsNameProgestin (mg) Micronor ----- Norethindrone 0.35 NOR — QD ----- Norethindrone 0.35 Ovrette ----- dl- Norgestrel 0.075 2. Intramuscular injectione.g. medroxyprogesterone acetate 150 mg, i.m every 3 months 3. Implantable progestine preparatione.g. Norplant — L- Norgestrel (6 tubes of 36 mg each) ( 5 years protection ).

  13. Emergency Postcoital Contraception ( morning-after pill ) Indications:When the desirability of avoiding pregnancy is obvious e.g.rape,unsuccessful withdrawal before ejaculation,condom torn during intercourse,exposure to teratogen e.g.,live vaccine,cytotoxic drug.

  14. MECHANISM OF CONTRACEPTION 1. Inhibition of ovulation 2. Abnormal transport time through Fallopian tube 3. Abnormal characteristics of cervical mucus 4. Abnormal contraction of the Fallopian tubes and uterine musculature.

  15. CONTRAINDICATION OF ORAL CONTRACEPTIVES 1. Thromboembolic disorders 2. Markedly impaired hepatic function 3. Suspected carcinoma of the breast 4. Undiagnosed genital bleeding.

  16. Factors Limit Effectiveness of Oral Contraceptives Vomiting and diarrhea Drugs interfere with absorption ( eg. Ampicillin ) Inducers of hepatic enzymes ( eg. Barbiturates, phenytoin )

  17. Long-acting Hormonal Methods • Vaginal ring • The patch • Injectables • Implants( Norplant) • Intrauterine device( IUD)

  18. Natural Birth Control • Fertility awareness • 2. Withdrawal • 3. Lactational amenorrhea method • 4. Sympto-thermal method • 5. Ovulation method ( Mucus method ) • 6. Fertility computers

  19. HYPOTHALAMUS GnRH ANTERIOR PITUITARY FSH LH OVARY ESTROGENS (β-ESTRADIOL) AND PROGESTERONE

  20. FERTILITY DRUGS 1. Antiestrogens eg.Clomiphene & Tamoxifen 2. Gonadotropin - Releasing Hormone (GnRH) e.g. Leuprolin, goserlin 3. Human Menopausal Gonadotropin (HMG) 4. Bromocriptine

  21. OVULATION INDUCING AGENTS1. Antiestrogens- Clomiphene - Tamoxifen Mechanism of Action: Indications: Women infertility not due to pituitary failure or ovarian failure. Success rate: - ovulation = 80% - pregnancy = 40% Dosage: 50 mg/d for 5 days from day 5th of the cycle to 10th if no response:- 100 mg/d for 5 days from day 5th to 10th

  22. HYPOTHALAMUS GnRH ANTERIOR PITUITARY FSH LH OVARY ESTROGENS (β-ESTRADIOL) AND PROGESTERONE

  23. Plasma concentrations of the gonadotropins & ovarian hormones during the normal female sexual cycle

  24. ADVERSE EFFECTS OF CLOMIPHENE 1. Hot Flushes 2. Gastric upset (nausea and vomiting) 3. Visual disturbances (reversible) 4. Skin rashes 5. Increase nervous tension 6. Depression 7. Fatigue 8. Weight gain 9. Breast tenderness 10. Hair loss (reversible) - occasional 11. Hyper stimulation of the ovaries and high incidence of multiple birth.

  25. Tamoxifen Similar & alternative to clomiphene… Difference: Not a steroidal agent Used in palliative treatment of advanced breast cancer with estrogen receptor- positive tumor(but not clomiphene..why?)

  26. 2. GONADOTROPIN RELEASING HORMONE (GnRH) Uses: Induction of ovulation in patients with hypothalmic amenorrhea (GnRH deficient) Analgoues with agonist activity: Leuprolin, goserelin GnRH and agonists, given S.C. in a pulsatile(drip) form to stimulate gonadotropin release (1 – 10 µg / 60 – 120 min) Given continuously, when gonadal suppression is desirable e.g. precocious puberty and advanced breast cancer in women and prostatic cancer in men

  27. HYPOTHALAMUS GnRH ANTERIOR PITUITARY FSH LH OVARY ESTROGENS (β-ESTRADIOL) AND PROGESTERONE

  28. HYPOTHALAMUS GnRH Agonists GnRH Continuous Pulsatile + + - GnRHR ANTERIOR PITUITARY FSH LH

  29. Side effects of GnRH agonists: - Hypo-oestrogenism (long term use) Hot flashes Decreased libido Osteoporosis

  30. 3. Human menopausal gonadotropin (HMG) Mechanism of Action Indications Women infertility due to pituitary insufficiency for 10 days followed by human chorionic gonadotropin (hCG) Adverse effects of HMG Fever Ovarian enlargement (hyper stimulation) Multiple Pregnancy (approx. 20%)

  31. HYPOTHALAMUS GnRH ANTERIOR PITUITARY FSH LH OVARY ESTROGENS (β-ESTRADIOL) AND PROGESTERONE

  32. 4. Human Chorionic Gonadotropin (hCG) Mechanism of action Similar to LH Indications Adjunct in treatment of infertility Adverse effects 1. Headache 2. Oedema

  33. Plasma concentrations of the gonadotropins & ovarian hormones during the normal female sexual cycle

  34. 5. BromocriptineIndication Infertility in women with elevated level of prolactin Mechanism of action Inhibits prolactin secretion from anterior pituitary gland Adverse effects: 1. Nausea, vomiting and dizziness 2. Orthostatic hypotension 3. Constipation 4. Dry mouth 5. Leg cramp 6. Insomnia 7. Involuntary movement 8. Nasal congestion

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