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Medicamentos atuantes no sistema reprodutivo feminino - Anticoncepcionais Gilberto De Nucci

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Apresentação em tema: "Medicamentos atuantes no sistema reprodutivo feminino - Anticoncepcionais Gilberto De Nucci"— Transcrição da apresentação:

1 Medicamentos atuantes no sistema reprodutivo feminino - Anticoncepcionais Gilberto De Nucci

2 Dúvidas Arquivo Medicamentos atuantes no sistema reprodutivo feminino - Anticoncepcionais Link Dúvidas Arquivo Medicamentos atuantes no sistema reprodutivo feminino - Anticoncepcionais Link

3 In the United States according to a study published in 2011 In 2006, 49% of pregnancies were unintendeda slight increase from 48% in Among women aged 19 years and younger, more than 4 out of 5 pregnancies were unintended. The proportion of pregnancies that were unintended was highest among teens younger than age 15 years, at 98%.

4 Walter F. Boron/ Emile L. Boulpaep – Medical Physiology – Fig 54-1 The anatomy of the female internal genitalia and accessory sex organs

5 Walter F. Boron/ Emile L. Boulpaep – Medical Physiology – Fig 54-1 The anatomy of the female internal genitalia and accessory sex organs

6 Ovarian cycle Rupture of mature follice and release of ovum (ovulatory phase) Corpus luteum formation (luteal phase) Growth and development of the follice (follicular phase) Corpus luteum degeneration Foyes Principles of Medicinal Chemistry – Fig. 29.2

7 In this illustration, the menstrual cycle is divided into four stages. (1)an egg matures inside the ovary, (2)which then releases the egg, (3) allowing it to travel through the fallopian tube, where it rests awaiting fertilization (4)If the egg is not fertilized, it is flushed out with the menstrual flow

8 Estradiol (pg/ml) FSH and LH (ng/ml) Days of female sexual cycle FSH LH Estradiol Ovulation Progesterone Progesterone (ng/ml) Menstruation Approximate plasma concentrations of the gonadotropins and ovarian hormones during the normal female sexual cycle Guyton & Hall – Textbook of Medical Physiology – fig 81.3

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15 Mechanism of Action of Estrogen/Progestin Contraceptives Inhibition of ovulation by suppression of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) Alteration of cervical mucus to inhibit sperm transport Interference with ovum transport Inhibition of implantation by suppression of normal endometrial development Essential of Reproductive Medicine – Tab. 26.1

16 Fertilization process

17 Puberty Menopause Age (yr) Estrogens excreted in urine (µg/24 hr) Estrogen secretion throughout the sexual life of the female human being Guyton & Hall – Textbook of Medical Physiology – fig 81.10

18 MÉTODOS ANTICONCEPCIONAIS Tabela – Natural Barreira – impede o encontro - Diafragma - Preservativo - DIU normal Medicamentoso -DIU – cobre ou progestogênico -Skin patch -Anel vaginal -Implante -Pílula

19 A clinical guide for contraception – fifth Ed – pg 191

20 CONTRACEPTIVOS HORMONAIS Forma eficaz, segura e reversível. - Puros: somente progestágeno - Combinados: associação de estrogênio e progestágeno

21 Historical Landmarks Animal experiments in the late 1930s demonstrated that high- dose progesterone could arrest ovulation Carl Djerassi synthetized progestin from an extract of Mexican wild yam root in late 1940 First pill marketed for cycle control (1960) - Enovid 10 – 9.85 mg norethynodrel microg mestranol Not legal to discuss contraception or prescribe the pill for the indication of contraception until 1969 Pope Paul VI Humanae Vitae (1968) – pill sinful Essential of Reproductive Medicine – Tab. 26.1

22 ESTROGÊNIO Década de 60 - Pró-Hormônio – Mestranol 150 mcg Etinil Estradiol - Alta dose (> ou = 50 mcg) - Baixa dose (35, 30, 20, 15 mcg) - Tendência – Ultrabaixa (sem consenso)

23 Mestranol (pró-droga) A clinical Guide For Contraception - Fifth edition - pag 36

24 Ethinyl estradiol A clinical Guide For Contraception - Fifth edition - pag 36

25 Estradiol Valerate a

26 Low – Dose Oral Contraceptives Products containing less than 50 mcg of ethinylestradiol

27 Classification of oral contraceptives Into generation according to the type of progestogens associated with estrogen Combined (estrogen + progestin) or progesting only

28 First-Generation Oral Contraceptives Products containing either norethisterone acetate, lynestrenol, ethynodiol acetate or norethynodrel.

29 Testosterone A clinical Guide For Contraception - Fifth edition - pag 37 Ethisterone

30 Norethindrone A clinical Guide For Contraception - Fifth edition - pag 37 Ethisterone Progestagional derivatives of testosterone

31 A clinical Guide For Contraception - Fifth edition - pag 38

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33 Second-Generation Oral Contraceptives Products containing levonorgestrel or norgestimate

34 A clinical Guide For Contraception - Fifth edition - pag 38

35 A clinical Guide For Contraception - Fifth edition - pag 41

36 Dienogest A clinical Guide For Contraception - Fifth edition - pag 42

37 Third-generation Oral Contraceptives Products containing desogestrel, norgestimate or gestodene

38 A clinical Guide For Contraception - Fifth edition - pag 39

39 Fourth-Generation Oral Contraceptives Products containing drospirenone, dienogest or nomegestrol acetate

40 Drospirenone A clinical Guide For Contraception - Fifth edition - pag 42

41 s Nomegestrel

42 s Dienogest

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45 Change in adjusted mean number of lesions (papules, pustules, open and closed comedones) from baseline to end point (full analysis set). Hormonal Contraceptives for Acne Management – CUTANEOUS MEDICINE FOR THE PRACTITIONER - VOL. 81 NO. 1S JANUARY 2008 DRSP, drospirenone; EE, ethinyl estradiol; COC, indicates combined oral contraceptive;

46 Oral Contraceptives With Acne Benefits Pharmacology of Hormonal Contraceptives and Acne – CUTANEOUS MEDICINE FOR THE PRACTITIONER - VOL. 81 NO. 1S JANUARY 2008

47 Progestin only Low daily doses of progestin (norethindrone, levonorgestrel or desogestrel) Injectable 3-month contraceptives (depot medroxyprogesterone acetate) IM Levenorgestrel implant or etonogestrel single-rod implant – 3 years Intrauterine device containing levonorgestrel – 5 years

48 Contraceptive use in the United States, Essential of Reproductive Medicine – Fig % 24% 19% 7% 6% 3% 1% Percentage of Women Ages PillSterilizationCondomWithdrawa/ Rhythm Hysterectomy/ Menopause InjectableSpermicideIUDImplants Method

49 A clinical Guide For Contraception - Fifth edition - pag 63

50 A clinical Guide For Contraception - Fifth edition - pag 66

51 Age group (years) Deaths / 100,000 women nonuser, nonsmoker user, nonsmoker nonuser, heavy smoker user, heavy smoker Number of deaths from cardiovascular diseases per 100,000 women by smoking status or nonuse of oral contraceptives. Essential of Reproductive Medicine – Fig. 26.4

52 Relative Risk and Actual Incidence of Venous Thromboembolism Population Relative RiskIncidence Young women-general population14-5 per 100,000 per year Pregnant women High-dose oral contraceptives Low dose oral contraceptives Leiden mutation carrier Leiden carrier and oral contraceptives Leiden mutation – homozygous A Clinical Guide for Contraception – tab. Pag 53

53 Noncontraceptive Health Benefits of Oral Contraceptives Percent Reduction/ Protection (%) Minium Use Required Duration of Effect OCP Formulation Comments Definitive evidence Ovarian cancer months At least 15 >20 µg EE Also protective against years hereditary ovarian cancer Endometrial cancer months 15 years All monophasic No data on multiphasic or progestin-only forms Benign breast disease months 1 year >20 µg EE Effect consistent across all age groups Pelvic inflamatory months Current use >20 µg EE ? Effect on outpatient disease cases of PID Ectopic pregnancy 90 Current use Current use >20 µg EE No increased risk for ectopic pregnancy in women who become pregnant with OCP use Essential of Reproductive Medicine – Tab. 26.2

54 Noncontraceptive Health Benefits of Oral Contraceptives Percent Reduction/ Protection (%) Minium Use Required Duration of Effect OCP Formulation Comments Conflicting evidence, favor beneficial effect Bone mineral density 60 Unknown Unknown >35 µg EE Decreased incidence of hip fractures with higher doses Colorectal cancer months Unknown >50 µg EE Increasing protection with increased duration Uterine leiomyomas 30, years; Unknown Unclear If used in setting of fibroids no 7 years clinically significant uterine growth Toxic shock syndrome 50 Current use Current use Unclear May be influenced by change in tampon composition/absorbency Essential of Reproductive Medicine – Tab. 26.2

55 Noncontraceptive Health Benefits of Oral Contraceptives Percent Reduction/ Protection (%) Minium Use Required Duration of Effect OCP Formulation Comments Conflicting evidence, favor no effect Functional ovarian cysts 80, 48, 8 Current use Current use Monophasic No statistically significant effect >35 µg EE; Monophasic <35 mcg EE triphasic all types Rheumatoid arthritis 40 Current use Current use Unclear May alter severity and clinical course rather development Essential of Reproductive Medicine – Tab. 26.2

56 Benefícios dos AOC Menor risco de câncer endometrial e ovariano. Menor risco de prenhez ectópica Menstruaçãoo mais regular (menor fluxo, menor dismenorréia, menor anemia) Menor incidência de salpingite Aumento da densidade óssea

57 AOC e câncer Redução de 50% do risco de câncer de endométrico Redução de 40% do risco de câncer de ovário Sem efeito no câncer de cérvix uterina ou no câncer de mama.

58 Possible Contradications to Use of Combined Oral Contraceptive Pills Absolute Contraindications 1. Thrombophlebitis or Thromboembolic disorders 2. Past history of deep vein thrombophlebitis or thromboembolic disorders 3. Cerebrovascular or coronary artery disease 4. Known or suspected breast carcinoma 5. Known or suspected estrogen-dependent neoplasia 6. Pregnancy 7. Benign or malignant liver tumor 8. Known impaired liver function 9. Previous cholestasis during pregnancy or with prior pill use Essential of Reproductive Medicine – Tab. 26.6

59 Possible Contradications to Used of Combined Oral Contraceptive Pills (cont) Strong Relative Contraindications 10. Severe headaches, particularly vascular or migraine headaches, that start after initiation of oral contraceptives 11. Hypertension with resting diastolic BP of 140 mmHg or greater on three or more separate visits or an accurate measurement of 110 mmHg diastolic or more on single visit 12. Mononucleosis, acute phase 13. Elective major surgery or major surgery requiring immobilization planned in next 4 week 14. Long-leg cast or major injury to lower leg 15. Over 40 years old, accompanied by a second risk factor for the development of cardiovascular disease (such as diabetes or hypertension) 16. Over 35 years old and currently a heavy smoker (15 or more cigarettes/day) 17. Abnormal genital bleeding Essential of Reproductive Medicine – Tab. 26.6

60 AOC e Fígado Transporte ativo de componentes biliares é inibido por estrógenos e progestágenos. Contraindicado formalmente em doença colestática aguda ou crônica

61 Importante Não há evidências de aumento de incidência de doença hepática séria causado por uso de ACO

62 Contraceptivo Oral e Trombose Estrógenos, mas não progestágenos, aumentam a produção de fatores de coagulação. Tabagismo e uso de estrógenos apresentam efeito aditivo no risco de trombose arterial. Contraceptivos de dose baixa de estrógeno (< 50 microg EE) não aumentam o risco de IM ou AVC em mulheres saudáveis, não fumantes, independente da idade. IM e AVC podem ocorrer em mulheres que usam contraceptivos de alta dose, ou que apresentam fatores de risco cardiovascular acima da idade de 35 anos.

63 Anticonvulsants Anti-infective agents Barbiturates Carbamazepine Phenytoin Rifampin Topiramate Vigabatrin Medications That Decrease Serum Concentrations of Hormonal Contraception Oral Contraceptives: Mechanism of Action, Dosing, Safety, and Efficacy – CUTANEOUS MEDICINE FOR THE PRACTITIONER - VOL. 81 NO. 1S JANUARY 2008

64 Monophasic pill Contains a fixed combination of a estrogen (generally ethinyl estradiol) and a progestogen

65 Biphasic Pill - Kariva 21 white tablets contains 0.15 mg desogestrel and 0.02 mg ethinyl estradiol. 2 light-green tablets contains inert ingredients 5 light-blue tablet contains 0.01 mg ethinyl estradiol.

66 Triphasic pill - Ortho Tri-Cyclen 28 7 tablet contains mg of norgestimate and mg of ethinyl estradiol 7 light blue tablet contains mg of norgestimate and mg of ethinyl estradiol 7 dark blue tablet contains mg of norgestimate and mg of ethinyl estradiol 7 green tablet contains only inert ingredients

67 Quadraphasic pill - Natazia 2 dark yellow tablets containing 3 mg estradiol valerate 5 red tablets containing 2 mg estradiol valerate and 2 mg dienogest 17 light yellow tablets containing 2 mg estradiol valerate and 3 mg dienogest 2 dark red tablets each containing 1 mg estradiol valerate 2 white tablets (inert)

68 Return of fertility after stopping contraception (Doll et al., 2001) (with permission). Intrauterine devices and intrauterine systems - Human Reproduction Update, Vol.14, No.3 pp. 197–208, 2008

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71 Pressione o anel Retire do Sachê Escolha uma posição confortável para inserir o anel

72 Coloque o anel na vagina com uma das mãos (fig. A). Se necessário o lábio pode ser afastado com a outra mão. Empurre o anel para dentro da vagina até senti-lo confortável (fig. B) Deixe o anel no lugar durante 3 semanas (fig. C) Figura AFigura B Figura C

73 40 mm 2 mm Rate-controlling membrane: (.06 mm) 100% EVA Core: 40% Ethylene vinyl acetate (EVA) 60% Etogestrel (68 mg)

74 Required Equipment for Implanon Insertion

75 Implantation technique

76 Contraindication for Implanon Known or suspected pregnancy Current or past history of thrombotic disease Hepatic tumors or active liver disease Undiagnosed abnormal genital bleeding Known, suspected or history of breast cancer Hypersensitivity to any of the components in Implanon A New Implantable Contraceptive - Nursing for Womens Health - Volume 11 - Issue 6

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78 Technique for the Tcu-380A

79 Níveis de levonorgestrel A Clinical Guide for Contraception - Pag. 169

80 Serum levels of LNG according to delivery. Author Route of delivery Serum levels (ng/ml) Raudaskoski et al. IUS 0.1–0.2 (1995) (PMW) Lahteenmaki et al mg oral ~ 1.7 (1995) Kives et al. (2005) 1.5 mg oral mg vaginal 5.4 Sivin et al. (1997) Implant 1.4–1.0 Rod 0.77 Intrauterine devices and intrauterine systems - Human Reproduction Update, Vol.14, No.3 pp. 197–208, 2008

81 HORMONIOS EM TRATAMENTOS Correção de ciclos irregulares Reposição em caso de perdas de orgão produtores Complementos (Climatério)


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