RESUMO
La anticoncepción de emergencia se refiere al uso de medicación o a la inserción de un dispositivo intrauterino de cobre para prevenir el embarazo luego de una relación sexual no protegida o del fallo de un método anticonceptivo, en una mujer que no desea el embarazo. De entre las alternativas farmacológicas del método, se estima que el uso de levonorgestrel prevendría el 50% de los embarazos. A partir de una viñeta clínica, en la cual se describe el caso de una paciente obesa que resultó embarazada luego de utilizar anticoncepción hormonal de emergencia tras una relación sexual no protegida, se realizó una búsqueda bibliográfica para establecer la efectividad del método en pacientes con esta característica (obesidad). La búsqueda identificó un metaanálisis que relacionó al triple la probabilidad de embarazo en pacientes con índice de masa corporal superior a 30 kg/m2 que utilizaron anticoncepción de emergencia hormonal. (AU)
Emergency contraception refers to the use of medication or the insertion of a copper intrauterine device to prevent pregnancy after the occurance of unprotected sex intercourse or failure of a contraceptive method in a woman who does not desire pregnancy. Among the pharmacological alternatives of the method it is estimated that the use of levonorgestrel prevents 50% of pregnancies. From a clinical vignette, in which the case of an obese patient who became pregnant using hormonal emergency contraception after unprotected sex intercourse is described, a literature search was conducted to establish the effectiveness of the method in patients with this feature (obesity). The search identified a metaanalysis that shows an incresed probability (threetimes) of pregnancy in patients with body mass index greater than 30 kg/m2 that used hormonal emergency contraception. Emergency contraception is less effective in women with obesity. (AU)
Assuntos
Humanos , Feminino , Gravidez , Adulto , Anticoncepcionais Hormonais Pós-Coito , Anticoncepcionais Sintéticos Pós-Coito , Obesidade/complicações , Gravidez/estatística & dados numéricos , Índice de Massa Corporal , Metanálise como Assunto , Fatores de Risco , Levanogestrel/administração & dosagem , Anticoncepcionais Pós-Coito , Dispositivos Intrauterinos de Cobre/estatística & dados numéricos , NorpregnadienosRESUMO
BACKGROUND: The days just prior to ovulation are the most crucial for emergency contraception (EC) efficacy. Ulipristal acetate (UPA) and levonorgestrel's (LNG) capacity to inhibit follicular rupture have never been compared directly at this time of the cycle. STUDY DESIGN: Raw data from three pharmacodynamics studies with similar methodology were pooled to allow direct comparison of UPA, LNG and LNG + meloxicam's ability to prevent ovulation when administered orally in the advanced follicular phase, with a leading follicle of ≥ 18 mm. RESULTS: Forty eight LNG-treated (1.5 mg) cycles, 31 LNG (1.5 mg) + meloxicam (15 mg), 34 UPA (30 mg) cycles and 50 placebo cycles were compared. Follicle rupture was delayed for at least 5 days in 14.6%, 38.7%, 58.8% and 4% of the LNG-, LNG + meloxicam-, UPA- and placebo-treated cycles, respectively. UPA was more effective than LNG and placebo in inhibiting follicular rupture (p = .0001), while LNG, when administered at this time of the cycle, was not different than placebo. The addition of meloxicam improved the efficacy of LNG in preventing follicular rupture (p = .0292 vs. LNG; p = .0001 vs. placebo; non-significant vs. UPA). UPA was effective in preventing rupture in the 5 days following treatment, even when administered at the time of the luteinizing hormone (LH) surge (UPA 79%, LNG 14% and placebo 10%). None of the treatments were effective when administered on the day of the LH peak. The median time from treatment to rupture was 6 days during the ulipristal cycles and 2 days in the placebo and LNG/LNG + meloxicam cycles (p = .0015). CONCLUSION: Although no EC treatment is 100% effective in inhibiting follicular rupture when administered in the late follicular phase, UPA is the most effective treatment, delaying ovulation for at least 5 days in 59% of the cycles. LNG is not different from placebo in inhibiting follicular rupture at this advanced phase of the cycle. No treatment was effective in postponing rupture when administered on the day of LH peak.
Assuntos
Anticoncepcionais Hormonais Pós-Coito/farmacologia , Anticoncepcionais Sintéticos Pós-Coito/farmacologia , Levanogestrel/farmacologia , Norpregnadienos/farmacologia , Folículo Ovariano/efeitos dos fármacos , Ovulação/efeitos dos fármacos , Adolescente , Adulto , Chile , Estudos Cross-Over , Inibidores de Ciclo-Oxigenase/farmacologia , República Dominicana , Método Duplo-Cego , Combinação de Medicamentos , Feminino , Humanos , Estimativa de Kaplan-Meier , Luteinização/efeitos dos fármacos , Hormônio Luteinizante/sangue , Meloxicam , Tiazinas/farmacologia , Tiazóis/farmacologia , Adulto JovemRESUMO
OBJECTIVE: Ulipristal acetate (UPA) acts as an emergency contraceptive by inhibiting ovulation. This study explores possible additional effects on the fragmentation of sperm DNA during in vitro incubation. METHODS: Motile spermatozoa from healthy donors were selected by swim-up and incubated under capacitating conditions in control medium or with UPA (1, 10, 100, 1,000 or 10,000 ng/ml). In some experiments, 200 µM of H2O2 were added to induce oxidative stress. The sperm chromatin dispersion test was performed to analyse DNA integrity (400 cells; 1000×). Lipid peroxidation (thiobarbituric acid assay), induced-acrosome reaction (AR) and sperm vitality (Eosin Y) were also evaluated in spermatozoa exposed to UPA and/or H2O2. RESULTS: During sperm incubation, the percentage of fragmented DNA increased significantly, from 15.0 ± 1.3 to 41.0 ± 4.5% (p < 0.001). In the presence of UPA, DNA fragmentation decreased significantly (p < 0.05), in a dose-dependent manner. At 100 and 1000 ng/ml, UPA also counteracted the effect of H2O2 and prevented DNA fragmentation. No effect on sperm vitality, lipid peroxidation or induced-AR was found with any treatment. CONCLUSIONS: During in vitro sperm capacitation DNA fragmentation increased but the latter was counteracted in the presence of UPA, which possibly acted as a scavenger of reactive oxygen species produced by spermatozoa.
Assuntos
Anticoncepcionais Sintéticos Pós-Coito/farmacologia , Fragmentação do DNA/efeitos dos fármacos , Norpregnadienos/farmacologia , Espermatozoides/efeitos dos fármacos , Reação Acrossômica/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Peróxido de Hidrogênio/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Oxidantes/farmacologia , Estresse Oxidativo , Espermatozoides/fisiologiaRESUMO
OBJECTIVE: A pill containing ulipristal acetate (UPA) is used for emergency contraception (EC). Considering that, following its intake, spermatozoa may be exposed to UPA in the female genital tract we intended to evaluate sperm functions after incubation with this compound. METHODS: Motile spermatozoa were selected by swim-up and were incubated under capacitating conditions with UPA (at concentrations of 1, 10, 100, 1,000, and 10,000 ng/ml) or control medium. The main outcome measures were sperm vitality, sperm protein tyrosine phosphorylation (TyrP), spontaneous acrosomal reaction (AR), and human follicular fluid (hFF)-induced AR. RESULTS: Sperm vitality and TyrP pattern were similar between spermatozoa exposed to UPA or control. In addition, spontaneous AR ranged from 14.0 ±1.5% to 18.0 ±1.9% after exposure to UPA or control medium without significant differences, and UPA did not prevent hFF-induced AR. CONCLUSIONS: Incubation of sperm with UPA at concentrations around the expected plasma levels after ingestion of this EC pill (Ë100-200 ng/ml) did not modify the signal transduction of TyrP involved in sperm capacitation. Moreover, UPA showed no agonist effect on progesterone receptors because it did not induce AR. Considering that progesterone in hFF is essential for AR induction, and UPA did not prevent the hFF-induced AR, an antagonist action of UPA on the AR is unlikely.
Assuntos
Reação Acrossômica/efeitos dos fármacos , Anticoncepcionais Sintéticos Pós-Coito/farmacologia , Norpregnadienos/farmacologia , Espermatozoides/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Feminino , Líquido Folicular/fisiologia , Humanos , Técnicas In Vitro , Masculino , Fosforilação/efeitos dos fármacos , Capacitação Espermática/efeitos dos fármacos , Motilidade dos Espermatozoides/efeitos dos fármacos , Espermatozoides/fisiologiaRESUMO
Estrous female domestic rabbits (Oryctolagus cuniculus) display scent marking ("chinning") and sexual receptivity. Mating induces ovulation, which occurs approximately 12h later, and also decreases chinning and receptivity. In the present study, we explored the participation of mating-associated stimuli, ovulation, and the progesterone receptor (PR) in mediating such behavioral effects. We found that copulatory stimuli were not necessary, and that ovulation alone was sufficient, as these behavioral changes were replicated in unmated females by intravenous administration of human chorionic gonadotropin (hCG). The post-mating administration (s.c.) of 5µg/day estradiol benzoate (EB), prevented the decline in chinning and receptivity. A lower dose of EB (1µg/day) had no effect, nor did the antiprogestin RU486 (20mg, s.c., administered 3h before mating). However, the combination of a single pre-mating administration of RU486 plus the post-mating administration of 1µg/day EB completely blocked the decline in estrous behavior. We propose that PR activation around the time of mating and a post-mating decline in ovarian estradiol secretion and/or estradiol responsiveness act in parallel to terminate estrus in this species.
Assuntos
Copulação/fisiologia , Ciclo Estral/fisiologia , Inibição Psicológica , Ovulação/fisiologia , Receptores de Progesterona/fisiologia , Comportamento Sexual Animal/fisiologia , Animais , Anticoncepcionais Sintéticos Pós-Coito/farmacologia , Copulação/efeitos dos fármacos , Estradiol/análogos & derivados , Estradiol/metabolismo , Estradiol/farmacologia , Ciclo Estral/efeitos dos fármacos , Feminino , Masculino , Mifepristona/farmacologia , Ovulação/efeitos dos fármacos , Estimulação Física , Coelhos , Receptores de Progesterona/metabolismo , Caracteres Sexuais , Comportamento Sexual Animal/efeitos dos fármacosRESUMO
BACKGROUND: Current methods of hormonal emergency contraception (EC) are ineffective in preventing follicular rupture when administered in the advanced pre-ovulatory phase. This study was designed to determine the capacity of ulipristal acetate (UPA), a selective progesterone receptor modulator developed for EC, to block follicular rupture when administered with a follicle of >or=18 mm. METHODS: This was a double-blind, crossover, randomized, placebo-controlled study. Thirty-five women contributed with UPA (30 mg. oral) and a placebo cycle. Serial blood sampling for luteinizing hormone (LH), estradiol and progesterone measurements and follicular monitoring by ultrasound were performed before and for 5 days following treatment. Follicular rupture inhibition was assessed in the overall study population and in subgroups of women stratified by when treatment was administered in relation to LH levels (before the onset of the LH surge, after the onset of the surge but before the LH peak or after the LH peak). RESULTS: Follicular rupture failed to occur for at least 5 days following UPA administration in 20/34 cycles [59%; 95% confidence interval (CI) (40.7-75.4%)], whereas rupture took place in all cycles within 5 days of placebo intake. When UPA was administered before the onset of the LH surge, or after the onset but before the LH peak, follicle rupture had not occurred within 5 days in 8/8 (100%) and 11/14 [78.6%; 95% CI (49.2-95.3)] cycles, respectively. In contrast, when UPA was given after the LH peak, follicle rupture inhibition was only observed in 1/12 [8.3%; 95% CI (0.2-38.5)] cycles. CONCLUSIONS: This study demonstrates that UPA can significantly delay follicular rupture when given immediately before ovulation. This new generation EC compound could possibly prevent pregnancy when administered in the advanced follicular phase, even if LH levels have already begun to rise, a time when levonorgestrel EC is no longer effective in inhibiting ovulation.
Assuntos
Anticoncepção Pós-Coito/métodos , Anticoncepcionais Sintéticos Pós-Coito/uso terapêutico , Fase Folicular/efeitos dos fármacos , Norpregnadienos/administração & dosagem , Norpregnadienos/uso terapêutico , Folículo Ovariano/efeitos dos fármacos , Inibição da Ovulação/efeitos dos fármacos , Adulto , Anticoncepção Pós-Coito/efeitos adversos , Anticoncepcionais Sintéticos Pós-Coito/administração & dosagem , Anticoncepcionais Sintéticos Pós-Coito/efeitos adversos , Estudos Cross-Over , Método Duplo-Cego , Estradiol/sangue , Feminino , Fase Folicular/sangue , Humanos , Hormônio Luteinizante/sangue , Norpregnadienos/efeitos adversos , Tamanho do Órgão , Folículo Ovariano/anatomia & histologia , Folículo Ovariano/diagnóstico por imagem , Progesterona/sangue , Receptores de Progesterona/antagonistas & inibidores , Estatística como Assunto , Fatores de Tempo , Ultrassonografia , Adulto JovemRESUMO
INTRODUCCIÓN: cuando se revisa la literatura médica referente al embarazo no deseado, es usual encontrar reportes que informan la existencia de cifras elevadas de muertes maternas producidas por abortos en condiciones de riesgo, de los cuales una cuarta parte corresponde a las adolescentes. Para evitar estas gestaciones no deseadas una variante eficaz es la anticoncepción de emergencia. OBJETIVO: aportar un conocimiento actualizado sobre la anticoncepción de emergencia y sus beneficios para los médicos de la atención primaria de salud. MÉTODOS: se realizó una revisión bibliográfica actualizada sobre la anticoncepción de emergencia, y sus beneficios como alternativa para disminuir el número de embarazos no deseados y de abortos provocados en la atención primaria de salud. CONCLUSIONES: la anticoncepción de emergencia ha demostrado ser una opción eficaz y practicamente inocua para la prevención de gestaciones no deseadas. A pesar de esto, es una técnica aún poco conocida y empleada en nuestro país entre los médicos de la atención primaria de salud.
INTRODUCTION: when medical literature related to non-desired pregnancy is reviewed, it is common to find reports on existence of high figures of mother death provoked by miscarriages in risk situations, from which a quarter of them to correspond to adolescents. To avoid these non-desired pregnancies an effective variant is the emergence contraception. OBJECTIVE: to provide update knowledge on emergences, and its benefits for physicians of health primary care. METHODS: we made an updated bibliographic review on emergence contraception, and its benefits like alternatives to decrease the non-desired pregnancies figures, and the miscarriages provoked in health primary care. CONCLUSIONS: emergence contraception has shown to be an efficient option and practically safe to the non-desired pregnancies. Despite it, is a not yet known technique, and used in our country among physicians of health primary care.
Assuntos
Humanos , Feminino , Anticoncepcionais Sintéticos Pós-Coito , Conhecimentos, Atitudes e Prática em Saúde , Médicos de Família , Atenção Primária à SaúdeRESUMO
El término anticoncepción hormonal de emergencia (AHE) se usa para descibir un método que cuando se toma durante los primeros días después de una relación sexual no protegida, puede prevenir un embarazo no buscado. Es sabido que sobre anticoncepción de emergencia mucho se dice y poco realmente se conoce. El desconocimiento del mecanismo de acción por parte de los médicos y la información errónea que reciben los pacientes, ya sea de ámbitos científicos, como de los medios de comunicación, han generado creencias y mitos en torno a los mismos, que no permiten que se utilicen correctamente. Se ha dicho sobre la AHE: que es abortiva; que trae importantes efectos adversos; que las pacientes van a dejar de utilizar otros métodos anticonceptivos; que aumenta el contagio de infecciones de transmisión sexual, etc. Hemos revisado la bibliografía existente hasta el momento sobre AHE, y podemos decir y justificar que ninguno de estos mitos son correctos y que aumentando los conocimientos acerca de la misma, y transmitiendo información correcta a nuestras pacientes, podremos brindar mejores opciones anticonceptivas para aquellas personas que no han utilizado correctamente un método, ha fracasado el mismo o ha sido víctima de una violación. (AU)
Assuntos
Anticoncepcionais Hormonais Pós-Coito , Anticoncepcionais Sintéticos Pós-Coito , Anticoncepcionais FemininosRESUMO
A pesar de lo extendido del uso de la anticoncepción de emergencia (AE) con levonorgestrel (LNG) en el mundo, el mecanismo de acción continúa siendo discutido, lo que ha sido aprovechado para que grupos confesionales aaquen su uso, argumentando que la misma es abortiva. Actualmente, dos comprimido de LNG de 0,75 mg hasta 5 días posteriores al coito no protegido, ha sido recomendada y mostrada como eficaz para AE. El mecanismo de acción probablemente depende del momento de la toma en relación al día del ciclo menstrual. Cuando el LNG para AE es administrado antes del período ovulatorio, el mismo inhibe la ovulación en algunas mujeres y afecta el endometrio. Sin embargo la administración de LNG antes de la ruptura folicular no mostró tener influencia sobre la expresión de glicodelina-A en biopsias de endometrio tomadas 24 o 48 horas después de la toma de las píldoras de LNG. Los resultados de los estudios no apoyan la idea de que el LNG como AE causaría un efecto anti-implantatorio. Fue especulado que el LNG podría actuar sobre los espermatozoides. En estudios muy antiguos de la Argentina fue observado que la administración de 0,4 mg de LNG dado 3-10 horas post coito reducía el número de espermatozoides recuperados de la cavidad uterina, causaba alcalinización del fluido intrauterino, inmovilizaba los espermatozoides y aumentaba la viscosidad del moco cervical. Esto llevó a sugerir que la migración espermática a los lugares de fertilización podría esar comprometida después de la ingesta de LNG como AE. Sin embargo, nosotros hemos trabajado sobre esta hipótesis, pero no observamos efectos sobre reacción acrosomal después de la exposición in vitro al LNG de espermatozoides capacitados...(AU)
Assuntos
Humanos , Feminino , Levanogestrel/administração & dosagem , Levanogestrel/farmacologia , Levanogestrel/uso terapêutico , Anticoncepcionais Hormonais Pós-Coito/administração & dosagem , Anticoncepcionais Hormonais Pós-Coito/farmacocinética , Anticoncepcionais Hormonais Pós-Coito/uso terapêutico , Anticoncepcionais Sintéticos Pós-Coito/administração & dosagem , Anticoncepcionais Sintéticos Pós-Coito/farmacocinética , Anticoncepcionais Sintéticos Pós-Coito/uso terapêutico , Anticoncepcionais Femininos/administração & dosagem , Anticoncepcionais Femininos/farmacocinética , Anticoncepcionais Femininos/uso terapêuticoRESUMO
A pesar de lo extendido del uso de la anticoncepción de emergencia (AE) con levonorgestrel (LNG) en el mundo, el mecanismo de acción continúa siendo discutido, lo que ha sido aprovechado para que grupos confesionales aaquen su uso, argumentando que la misma es abortiva. Actualmente, dos comprimido de LNG de 0,75 mg hasta 5 días posteriores al coito no protegido, ha sido recomendada y mostrada como eficaz para AE. El mecanismo de acción probablemente depende del momento de la toma en relación al día del ciclo menstrual. Cuando el LNG para AE es administrado antes del período ovulatorio, el mismo inhibe la ovulación en algunas mujeres y afecta el endometrio. Sin embargo la administración de LNG antes de la ruptura folicular no mostró tener influencia sobre la expresión de glicodelina-A en biopsias de endometrio tomadas 24 o 48 horas después de la toma de las píldoras de LNG. Los resultados de los estudios no apoyan la idea de que el LNG como AE causaría un efecto anti-implantatorio. Fue especulado que el LNG podría actuar sobre los espermatozoides. En estudios muy antiguos de la Argentina fue observado que la administración de 0,4 mg de LNG dado 3-10 horas post coito reducía el número de espermatozoides recuperados de la cavidad uterina, causaba alcalinización del fluido intrauterino, inmovilizaba los espermatozoides y aumentaba la viscosidad del moco cervical. Esto llevó a sugerir que la migración espermática a los lugares de fertilización podría esar comprometida después de la ingesta de LNG como AE. Sin embargo, nosotros hemos trabajado sobre esta hipótesis, pero no observamos efectos sobre reacción acrosomal después de la exposición in vitro al LNG de espermatozoides capacitados...
Although emergency contraception (EC) with levonorgestrel (LNG) is widely extended worldwide, the mechanism of action is still under discussion, which may be used by religious groups to argue that it is an abortifacient drug. Actually, two pills of LNG with 0.75 mg every 12 hours or the administration of a single doses of 1.5 mg up to 5 days after unprotected coitus, has been recommended and with a good efficacy to EC. The mechanism of action probably depends of the time of ingestion in relationship to the day of the menstrual cycle. When the LNG as EC is taken before of the ovulatory period, it's inhibited ovulation in some women and affects the endometrium. However, the intake of LNG before the follicular rupture did not show any influence upon the expression of glycodelin-A in endometrial biopsies taken 24 or 48 hours after the intake of the pills of LNG. The results of the studies did not support the idea that LNG as EC caused an anti-implantation effect. It was speculated that LNG could acted upon the spermatozoa. In older studies conducted in Argentina it was observed that the administration of 0.4 mg of LNG taken 3-10 hours post coitus reduced the number of spermatozoa recovery from the uterine cavity, cause alkalinization of uterine fluid, immobilized spermatozoa and increase the viscosity of cervical mucus. This suggests that sperm migration to the fertilization local could be impaired after taken a LNG as EC. Nevertheless, we have been working in this hypothesis but we did not observed effects upon acrosomal reaction (AR) after exposition in vitro to LNG of capacitated spermatozoa. In the aggregate, the in vivo exposition of spermatozoa to LNG as EC showed that the intake of 1.5 mg of LNG as EC alter different times post coitus and the recovery of spermatozoa from the uterine cavity alter different times of the pill intake (12, 24 or 36 hours), did not affect the quality of cervical mucus, or the sperm penetration, neither the fertilizing capacity showed through the AR rate, which was similar to observed after the intake of placebo
Assuntos
Humanos , Feminino , Levanogestrel/administração & dosagem , Levanogestrel/farmacologia , Levanogestrel/uso terapêutico , Anticoncepcionais Femininos/administração & dosagem , Anticoncepcionais Femininos/farmacocinética , Anticoncepcionais Femininos/uso terapêutico , Anticoncepcionais Hormonais Pós-Coito/administração & dosagem , Anticoncepcionais Hormonais Pós-Coito/farmacocinética , Anticoncepcionais Hormonais Pós-Coito/uso terapêutico , Anticoncepcionais Sintéticos Pós-Coito/administração & dosagem , Anticoncepcionais Sintéticos Pós-Coito/farmacocinética , Anticoncepcionais Sintéticos Pós-Coito/uso terapêuticoRESUMO
El término anticoncepción hormonal de emergencia (AHE) se usa para descibir un método que cuando se toma durante los primeros días después de una relación sexual no protegida, puede prevenir un embarazo no buscado. Es sabido que sobre anticoncepción de emergencia mucho se dice y poco realmente se conoce. El desconocimiento del mecanismo de acción por parte de los médicos y la información errónea que reciben los pacientes, ya sea de ámbitos científicos, como de los medios de comunicación, han generado creencias y mitos en torno a los mismos, que no permiten que se utilicen correctamente. Se ha dicho sobre la AHE: que es abortiva; que trae importantes efectos adversos; que las pacientes van a dejar de utilizar otros métodos anticonceptivos; que aumenta el contagio de infecciones de transmisión sexual, etc. Hemos revisado la bibliografía existente hasta el momento sobre AHE, y podemos decir y justificar que ninguno de estos mitos son correctos y que aumentando los conocimientos acerca de la misma, y transmitiendo información correcta a nuestras pacientes, podremos brindar mejores opciones anticonceptivas para aquellas personas que no han utilizado correctamente un método, ha fracasado el mismo o ha sido víctima de una violación.
The word emergency hormonal contraception (EHC) is used to describe a method that, when during the first days after an unprotected sexual relationship can prevent a non wanted pregnancy. It is known that about emergency contraception much is said and very little is known. Doctors´unawareness on the mechanism of action and the wrong information received by the patients, both coming from scientific environments as well as means of communication have created beliefs and miths around them which do not permit their correct use. The following has been said about EHC: it is abortive; it brings important side effects; the patients have the tendency to quit other contraception methods; it increases the transmission of sexual diseases, etc. We have revised the existing bibliography about EHC and we can affirm and justify that neither of these miths is correct and that by increasing the knowldege on it and by transmitting correct information about it to our patients, we will be able to provide better contraception options for those who have not used a method properly or have failed using it; or for those who have been rape victims
Assuntos
Anticoncepcionais Hormonais Pós-Coito , Anticoncepcionais Sintéticos Pós-Coito , Anticoncepcionais FemininosRESUMO
El riesgo de embarazo ectópico después de anticoncepción de emergencia es un hecho conocido y con el aumento de la demanda por este método, es esperable un mayor número de casos en el futuro. Se presenta un caso de embarazo ectópico después del fracaso de la anticoncepción de emergencia con levonorgestrel.
The risk of ectopic pregnancy after emergency contraception is known and with the increased use of this treatment, we might expect more cases in the future. One case of ectopic pregnancy after failure of emergency contraception with levonorgestrel is presented.
Assuntos
Humanos , Feminino , Gravidez , Adulto , Anticoncepcionais Sintéticos Pós-Coito/efeitos adversos , Gravidez Ectópica/induzido quimicamente , Levanogestrel/efeitos adversos , RiscoRESUMO
Brief vaginocervical stimulation using a glass rod (VCS) combined with manual flank-perineal stimulation (FS) rapidly (within 5 min) induced both receptive and proceptive behavioural responses to males in ovariectomised, oestrogen-primed rats. This receptive-proceptive response to males, resulting from a single brief (5-s duration) instance of manual VCS + FS, declined markedly within 4 h. However, the decline was prevented if the females were mounted by males immediately after the manual VCS + FS and 2 h later. We tested the participation of the cAMP-dependent protein kinase A system and the mitogen-activated protein kinase (MAPK) system in the response to VCS + FS by infusing either 100 ng of Rp-adenosine 3',5'-cyclic monophosphorothiate triethylamonium salt (a protein kinase A blocker) or 3.3 microg of PD98059 (a MAPK blocker) i.c.v. 15 min prior to VCS + FS. Both inhibitors blocked the ability of VCS + FS to induce the proceptive-receptive responses to males at all testing intervals. In experiment 2, systemic administration of 5 mg of RU486 1 h before VCS + FS also blocked the ability of VCS + FS to induce the proceptive-receptive responses to males. The present findings suggest that both VCS + FS and mating stimuli provided by males release neurotransmitters and neuromodulators that trigger the protein kinase A and the MAPK signalling systems, which interact with the progestin receptor to rapidly (within 5 min) induce proceptive-receptive behaviour in females.
Assuntos
Proteínas Quinases Dependentes de AMP Cíclico/antagonistas & inibidores , Proteínas Quinases Ativadas por Mitógeno/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Receptores de Progesterona/antagonistas & inibidores , Comportamento Sexual Animal/efeitos dos fármacos , Animais , Colo do Útero/fisiologia , Anticoncepcionais Sintéticos Pós-Coito/farmacologia , AMP Cíclico/análogos & derivados , AMP Cíclico/farmacologia , Proteínas Quinases Dependentes de AMP Cíclico/metabolismo , Estradiol/análogos & derivados , Estradiol/metabolismo , Feminino , Flavonoides/farmacologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Sistema de Sinalização das MAP Quinases/fisiologia , Masculino , Mifepristona/farmacologia , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Ovariectomia , Períneo/fisiologia , Postura , Ratos , Ratos Sprague-Dawley , Receptores de Progesterona/metabolismo , Comportamento Sexual Animal/fisiologia , Tionucleotídeos/farmacologia , Vagina/fisiologiaRESUMO
BACKGROUND: The objectives were firstly to assess acrosome reaction (AR) status of spermatozoa following uterine flushing, secondly to measure levonorgestrel (LNG) levels in serum and in uterine flushing fluid and finally to measure endometrial glycodelin-A expression after administration of LNG as a form of emergency contraception (EC). METHODS: Forty-eight experiments were conducted on 15 regularly menstruating women. Four groups were formed based on different intercourse to treatment interval and treatment to recovery of spermatozoa and the biopsies. RESULTS: Twenty-four and forty-eight hours after treatment, there were 14.5 +/- 3.9 x 10(6) and 17.3 +/- 6.8 x 10(6) sperm recovered from the uterus, respectively. There were no differences between the AR rate and the endometrial glycodelin-A staining intensity in an LNG or placebo treated cycles. The LNG in uterine flushing medium represented 1.38% of the values observed in serum 24 h after the LNG intake. CONCLUSIONS: Twenty-four and forty-eight hours after administration of EC, neither the proportion of AR sperm, nor the glycodelin-A level was influenced by 1.5 mg of LNG. LNG did not impair the cervical mucus either because viable spermatozoa were found in the genital tract 36-60 h after coitus and 24-48 h after LNG intake. The mechanism of action of LNG as EC remains unknown.
Assuntos
Reação Acrossômica/fisiologia , Anticoncepção Pós-Coito , Anticoncepcionais Sintéticos Pós-Coito/administração & dosagem , Endométrio/metabolismo , Glicoproteínas/biossíntese , Levanogestrel/administração & dosagem , Proteínas da Gravidez/biossíntese , Adulto , Método Duplo-Cego , Endométrio/efeitos dos fármacos , Feminino , Glicodelina , Humanos , Levanogestrel/sangue , MasculinoRESUMO
OBJECTIVE: The study was conducted to assess levonorgestrel (LNG) serum levels achieved after a single administration of two different doses of Carraguard vaginal gel containing LNG (CARRA/LNG), designed for use as microbicide and contraceptive for potential dual protection. MATERIALS AND METHODS: This was a randomized double-blind pharmacokinetic study conducted in 12 subjects enrolled at two centers. Each subject received a single vaginal administration of CARRA/LNG containing either 0.75 or 1.5 mg LNG per 4 mL of gel on Days 10-12 of the menstrual cycle. LNG serum levels were measured at 0, 1, 2, 4, 8 and 12 h after administration and for the following 7 days. LH and progesterone (for a preliminary evaluation of effect on the ovarian function) as well as SHBG were measured in the daily samples. RESULTS: Serum LNG maximum concentrations (Cmax) were 14.1+/-2.1 and 11.7+/-2.7 nmol/L and Tmax was 12.0 and 6.0 h for the low and high dose, respectively, with large intersubject variability within the first 48 h. Mean levels at 96 h were 10% of Cmax. Differences in AUC between both doses were not statistically significant. SHBG levels decreased approximately 25% by Day 4 after administration. Luteal activity was observed in 3/6 and 5/6 of the subjects in the low- and high-dose group, respectively. CONCLUSION: This study demonstrates that the CARRA/LNG gel can sustain elevated serum levels of the contraceptive steroid for up to 96 h after a single application. The serum levels attained with the 0.75-mg formulation are in the range expected to perturb the ovulatory process as observed in some subjects. The lack of correlation between the administered dose and serum concentrations of the steroid may be related to a rate-limiting absorption of LNG from the vaginal mucosa. The results reported here suggest that the CARRA/LNG formulation has good potential to become a dual-protection method, possibly preventing conception and sexually transmitted infections.
Assuntos
Anti-Infecciosos/farmacocinética , Levanogestrel/farmacocinética , Administração Intravaginal , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/sangue , Área Sob a Curva , Química Farmacêutica , Chile , Anticoncepcionais Sintéticos Pós-Coito/administração & dosagem , Anticoncepcionais Sintéticos Pós-Coito/sangue , Anticoncepcionais Sintéticos Pós-Coito/farmacocinética , República Dominicana , Método Duplo-Cego , Feminino , Humanos , Absorção Intestinal , Levanogestrel/administração & dosagem , Levanogestrel/sangue , Cremes, Espumas e Géis VaginaisRESUMO
BACKGROUND: Levonorgestrel (LNG) consistently prevents follicular rupture only when it is given before the onset of the ovulatory stimulus. As locally synthesized prostaglandin (PG) plays a crucial role in follicular rupture and cyclooxygenase-2 (cox-2) catalyses the final step of PG synthesis, we reasoned that adding a cox-2 inhibitor to LNG would prevent follicular rupture even after the ovulatory process had been triggered by the gonadotrophin surge. METHODS: Forty-one women were divided into two groups. One was treated when the size of the leading follicle was 15-17 mm (n=10) and the other when it was >or=18 mm (n=31). Each woman contributed with one cycle treated with LNG 1.5 mg single dose plus placebo and another treated with LNG + meloxicam (Melox) 15 mg, in a randomized order. Serial blood sampling for the assay of LH and follicular monitoring by transvaginal ultrasound were performed before and after treatment. RESULTS: Follicular rupture failed to occur within the 5-day period that followed treatment in 50 and 70% of cycles treated with LNG + Placebo and LNG + Melox, respectively, in the 15-17 mm group (P=0.15) and in 16 and 39% of cycles treated with LNG + Placebo and LNG + Melox, respectively, in the >or=18 mm group (P < 0.052). The overall proportion of cycles with no follicular rupture or ovulatory dysfunction increased significantly by the addition of Melox to LNG (66 versus 88%, P < 0.012; n=41-matched pairs). CONCLUSIONS: The trend towards increased incidence of no follicular rupture when Melox was combined with LNG suggests that the addition of a cox-2 inhibitor has the potential to improve the contraceptive efficacy of LNG by a pre-fertilization effect.