RESUMO
Determinar el efecto sobre la sintomatología clínica, perfil lipídico y niveles plasmáticos de estradiol y estrona frente a la administración de estrógenos conjugados equinos y estrógenos conjugados genéricos formulados localmente. Estudio prospectivo, controlado y randomizado, comparando cuatro grupos de 20 pacientes cada uno con formulaciones diferentes de estrógenos conjugados (EC) contra placebo por un período de 6 meses. No hubo diferencias significativas en la respuesta clínica ni en los niveles plasmático de estradiol y estrona entre los grupos con EC. Todos los grupos mostraron mejorías en el perfil lipídico al compararse contra placebo, se encontró significación sólo en dos de ellos. La respuesta a la sintomatología clínica así como los niveles plasmáticos de estradiol son comparables entre los grupos de EC. Las diferencias significativas entre estrógenos conjugados equinos y los genéricos sobre algunas fracciones de perfil lipídico deber ser precisadas con estudios complementarios para precisar su real significado
Assuntos
Feminino , Estrogênios Conjugados (USP)/farmacocinética , Pré-Menopausa/efeitos dos fármacos , Terapia de Reposição de Estrogênios/métodos , Congêneres do Estradiol/farmacocinética , Estradiol/sangue , Estrona/sangue , Lipídeos/sangue , Placebos/farmacocinéticaRESUMO
The possible hypertensive effect of oral contraceptives is a controversial issue. We studied 371 women, admitted to the family planning program of a atate funded outpatient clinic, that were followed during 12 months. These women were divided in 4 groups. Group 1 was constituted by 98 women that used intrauterine devices. Group 2 by 98 women taking 30 µg of estrogen and 300 µg of progestogen. Group 3 by 83 women taking 35 µg of estrogen and 500 µg of progestogen and Group 4 by 92 puerperal women taking 30 µg of levonorgestrel, that after six month started to use an intrauterine device (n=35) or the contraceptives of group 2 (n=38) or group 3 (n=19). Age, initial blood pressure and weight were similar in the 4 groups. There was no significant change in blood pressure after 6 or 12 centrations up to 35 µg and progestogen concentrations between 300 and 500 µg do not induced changes in blood pressure
Assuntos
Humanos , Feminino , Adulto , Anticoncepcionais Orais/farmacocinética , Pressão Sanguínea , Peso Corporal/efeitos dos fármacos , Ensaios Clínicos Controlados Aleatórios como Assunto , Congêneres do Estradiol/farmacocinéticaRESUMO
Some details about the function of natural and synthetical hormonas are reviewed, particularly estrogens as ethynyl estradiol and its 3, Methyl ether (mestranol); its peripheral concentration vs tissular hormonal contents, a relationship of biological importance as the first step in its hormonal action and the cummulative local effects that could explain some intra and extracellular phenomena.
PIP: Some studies of the peripheral concentration and concentration in reproductive tissues of ethinyl estradiol (EE) and mestranol are reviewed. Orally administered EE is observable in the peripheral circulation within 30-60 minutes. A 1970 study of radioactive EE demonstrated that the endometrium and ovaries captured most of the EE, with levels in the uterus and serum much lower. Adipose tissue was found to be important in storing the hormones. Other studies of radioactive mestranol and EE demonstrated that the compounds were deposited in other organs in significant quantities and that the deposits were perhaps irreversible or of very slow release. The ability of estrogens to remain concentrated at the systemic level and not just in reproductive organs may be related to some adverse effects reported in women using oral contraceptives (OCs). Advances in radiochemistry and immunology in the 1960s made it possible to measure steroid hormone levels in different tissues. The capacity of the endometrium to concentrate natural steroids such as 17-beta estradiol and progesterone during the ovulatory menstrual cycle was demonstrated in 1978. A subsequent study showed that the endometrium captured and stored the synthetic estrogen EE in even greater concentrations than the natural estrogen estradiol. A study of the pharmacodynamics of EE in hysterectomized women showed that 24 hours after the 1st dose of 30 mcg the EE was not detected in the peripheral circulation. But the peripheral concentration increased with continuous daily administration of 30 mcg of EE. 27 days after suppression of treatment it was still detectable in the peripheral circulation. Another experiment was designed to measure simultaneously the concentrations of EE in the peripheral circulation and in the endometrial tissue of 36 women terminating use of OCs containing norgestrel and EE after 2-36 months of treatment. The study showed that synthetic estrogen was still observable in the endometrial tissue 1 month after discontinuing OC use. Inexplicably, levels of EE were higher in the circulation in the cycle after treatment than in the final treatment cycle. 5 of the women participated in the study for 3 posttreatment cycles. EE was observed in the circulation 1 month after termination of OC use in 5 women, 2 months after termination in 4 women, and 3 months after termination in 3 women. The persistence of EE in the tissue months after termination of treatment suggests the need for further research and assessment of possible resulting risks.
Assuntos
Anticoncepcionais Orais Sintéticos/farmacocinética , Congêneres do Estradiol/farmacocinética , Tecido Adiposo/metabolismo , Adulto , Etinilestradiol/farmacocinética , Feminino , Genitália Feminina/metabolismo , Humanos , Distribuição TecidualRESUMO
Some details about the function of natural and synthetical hormonas are reviewed, particularly estrogens as ethynyl estradiol and its 3, Methyl ether (mestranol); its peripheral concentration vs tissular hormonal contents, a relationship of biological importance as the first step in its hormonal action and the cumulative local effects that could explain some intra and extracellular phenomena.