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1.
Eur J Contracept Reprod Health Care ; 26(1): 73-78, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33155847

RESUMO

AIM: Combined hormonal contraceptives, despite their high efficacy, are associated with an increased relative risk of cardiovascular events. The contraceptive mechanism of action of combined pills depends fundamentally on their progestin component. METHODS: A narrative review was performed. RESULTS: The drospirenone-only pill, including this synthetic progestogen with antimineralocorticoid and antiandrogenic activity, has high contraceptive efficacy that has been demonstrated with a 24-day schedule of 4-day administration of hormone-free pills. Due to its safety profile, the drospirenone-only pill is suitable even in high-risk populations, such as women with high blood pressure, thromboembolism, smoking or dyslipidemia. CONCLUSION: Considering the increasing prevalence of these comorbidities in Latin America, the 4 mg drospirenone-only pill is suggested as one of the strategies of choice in the region for those women who choose oral contraceptives.


Assuntos
Androstenos , Anticoncepcionais Orais Sintéticos , Antagonistas de Receptores de Mineralocorticoides , Androstenos/uso terapêutico , Anticoncepção , Anticoncepcionais Orais Combinados/efeitos adversos , Anticoncepcionais Orais Sintéticos/uso terapêutico , Estrogênios , Feminino , Humanos , América Latina/epidemiologia , Antagonistas de Receptores de Mineralocorticoides/uso terapêutico
2.
Revista Digital de Postgrado ; 9(2): 227, ago. 2020. tab
Artigo em Espanhol | LILACS, LIVECS | ID: biblio-1103383

RESUMO

Evaluar los efectos de la terapia hormonal (TH) con Drospírenona (DRSP)/17 ß -estradiol (E2), sobre los parámetros del Síndrome Metabólico (SM) en pacientes postmenopáusicas. Métodos: Investigación comparativa y aplicada, con diseño cuasi experimental, de casos y controles a simple ciego, prospectivo y de campo; realizada en la Consulta de Ginecología. Hospital "Dr. Manuel Noriega Trigo". San Francisco, Estado Zulia. Venezuela. Participaron 120 mujeres separadas al azar para recibir la combinación DRSP/E2 (Grupo A) o un placebo (Grupo B). Se evaluaron los componentes del SM antes y posterior a 6 meses de haber recibido la TH. Resultados: Se encontró una alta prevalencia de SM en ambos grupos antes de recibir el tratamiento (53,3% y 48%; grupo A y B respectivamente). Posterior al tratamiento, DRSP/E2 al compararse con un placebo, redujo significativamente tanto la prevalencia del SM como el riesgo de padecerlo (21,7% versus 48,3%, OR [IC95%]= 0,29 [0,13-0,65]; p < 0.001), con reducción significativa (p< 0.001) de la hipertensión arterial, glicemia basal alterada, hipertrigliceridemia y obesidad central; además de una reducción significativa de los síntomas vasomotores, síntomas psicológicos e incontinencia urinaria (p< 0.001). En el grupo B la prevalencia del SM se mantuvo sin cambios, salvo para la glicemia basal alterada y los síntomas vasomotores y psicológicos que mostraron una reducción significativa (p< 0.001). Conclusión: DRSP/E2 (2mg/1 mg) demostró ser eficaz luego de 6 meses de tratamiento tanto para el control de los parámetros que definen al SM; con pocos y leves efectos indeseados(AU)


To assess the effects of hormone therapy (HT) with drospirenone (DRSP)/17 ß -estradiol (E2) on the parameters of the metabolic syndrome (MS) in postmenopausal patients. Methods: We performed a comparative and applied research, with quasiexperimental, case-control, single-blind, prospective and field design. The study was realized in the Gynecology consultation. Hospital "Dr. Manuel Noriega Trigo". San Francisco, Estado Zulia. Venezuela. 120 women were included, they were separated to receive either the combination DRSP/E2 (Group A) or placebo (Group B). We assess MS components before and ather 6 months of receiving HT. Results: We found a high prevalence in both groups before receiving treatment (53.3% and 48%, group A and B respectively). A ther treatment, DRSP/E2 when compared to placebo, significantly reduced both the prevalence of MS as the risk of setting it (21.7% versus 48.3%, OR [95%] = 0.29 [0.13-0.65] p <0.001), with a significant reduction (p <0.001) of hypertension, impaired fasting glucose, hypertriglyceridemia, central obesity; and a significant reduction in vasomotor symptoms, psychological symptoms and urinary incontinence (p <0.001). In group B the prevalence of MS was unchanged, except for impaired fasting glycemia and vasomotor and psychological symptoms showed a significant reduction (p <0.001). Conclusion: DRSP/E2 (2mg /1mg), proved to be effective a ther 6 months of treatment both for the control of the parameters that define the SM, with few and mild side effects(AU)


Assuntos
Humanos , Feminino , Progestinas/uso terapêutico , Terapia de Reposição Hormonal , Síndrome Metabólica/fisiopatologia , Estradiol/uso terapêutico , Pós-Menopausa , Endocrinologia , Ginecologia
3.
Int J Womens Health ; 12: 235-242, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32280282

RESUMO

OBJECTIVE: To compare the bleeding pattern in women using ethinylestradiol 20 mcg/drospirenone 3 mg (EE 20 mcg/DRSP 3 mg) in a 24/4-day cyclic regimen with an extended regimen. Unexpected bleeding/spotting in the extended regimen group was managed by allowing a 4-day hormone-free interval (HFI). METHODS: This was a randomized, prospective, open-label, multicenter study. Participants (N = 348) were randomized to receive EE 20 mcg/DRSP 3 mg in either an extended regimen (EE/DRSPes group) or a 24/4-day cyclic regimen (EE/DRSP24/4 group) and followed for 168 days. In the EE/DRSPes group, a 4-day HFI was allowed whenever unexpected bleeding/spotting persisted for ≥7 consecutive days. The participants assessed their bleeding daily as "no bleeding," "spotting," or "light," "moderate," or "heavy" bleeding according to a predefined scale. RESULTS: EE/DRSPes group experienced fewer days of bleeding than those using a 24/4 cyclic regimen (P < 0.001). After 168 days, 57.5% of women in the EE/DRSPes group achieved complete amenorrhea (i.e., neither bleeding nor spotting) and 73.9% achieved "no bleeding" (i.e., no bleeding with or without spotting) during the final 28-day interval of the study period. Women in the extended group who instituted the 4-day HFI experienced a 94.1% rate of successful management of unexpected bleeding/spotting. CONCLUSION: The use of EE 20 mcg/DRSP 3 mg in an extended regimen resulted in high rates of amenorrhea and "no bleeding". Unexpected bleeding/spotting in the EE/DRSPes group could be managed effectively with a 4-day HFI. CLINICAL TRIAL REGISTRATION: International Standard Randomised Controlled Trial Number (ISRCTN57661673): http://www.controlled-trials.com/isrctn/pf/57661673.

4.
J Steroid Biochem Mol Biol ; 190: 54-63, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-30923014

RESUMO

Oral contraception is the most commonly used interventional method in the world. However, several women employ the continuous use of these hormones to avoid pre- and menstruation discomforts. Some studies indicate that oral contraceptives are associated with disturbances in glycemia and the effects of the use of a continuous regime are poorly elucidated. Herein, we evaluated the effects of the continuous administration of a combined oral contraceptive (COC) composed by ethinyl estradiol (EE) and drospirenone (DRSP) on glucose homeostasis in female mice. Adult Swiss mice received 0.6 µg EE and 60 µg DRSP (COC group) or vehicle [control (CTL)] daily by gavage for 35 days. COC treatment had no effect on body weight or adiposity, but increased uterus weight and induced hepatomegaly. Importantly, COC females displayed normal glycemia and glucose tolerance, but hyperinsulinemia and lower plasma C-peptide/insulin ratio, indicating reduced insulin clearance. Furthermore, COC mice displayed reduced protein content of the ß subunit of the insulin receptor (IRß) in the liver. Additionally, pancreatic islets isolated from COC mice secreted more insulin in response to increasing glucose concentrations. This effect was associated with the activity of steroid hormones, since INS-1E cells incubated with EE plus DRSP also secreted more insulin. Therefore, we provide the first evidence that the continuous administration of EE and DRSP lead to hyperinsulinemia, due to enhancement of insulin secretion and the reduction of insulin degradation, which possibly lead to the down-regulation of hepatic IRß. These findings suggest that the continuous administration of COC could cause insulin resistance with the prolongation of treatment.


Assuntos
Androstenos/efeitos adversos , Anticoncepcionais Orais Combinados/efeitos adversos , Etinilestradiol/efeitos adversos , Hiperinsulinismo/induzido quimicamente , Células Secretoras de Insulina/efeitos dos fármacos , Insulina/metabolismo , Animais , Feminino , Glucose/metabolismo , Hiperinsulinismo/metabolismo , Resistência à Insulina , Células Secretoras de Insulina/metabolismo , Camundongos
5.
Rev. obstet. ginecol. Venezuela ; 77(1): 51-57, mar. 2017. tab
Artigo em Espanhol | LILACS | ID: biblio-902640

RESUMO

Objetivo: Calcular el índice de Pearl de Genesa® en mujeres venezolanas. Métodos: Estudio fase IV, prospectivo y abierto. Las pacientes recibieron etinilestradiol 30 mcg / drospirenona 3 mg (Genesa®): un comprimido diario desde el primer día de la menstruación por 21 días; descanso de siete días y reinicio el día ocho. Resultados: Se ingresaron al estudio 115 pacientes, se obtuvo un índice de Pearl de 0,98. Los efectos adversos fueron: un embarazo, incremento de peso, retención de líquidos, náuseas, manchas en la piel. Conclusiones: Etinilestradiol 30 mcg/drospirenona 3 mg (Genesa®) presenta un adecuado índice de Pearl en mujeres venezolanas.


Objective: To calculate the Pearl index of Genesa® in Venezuelan women. Methods: Phase IV prospective and open study. Patients received ethinylestradiol 30 mcg / drospirenone 3 mg (Genesa®): one tablet daily from the first day of menstruation for 21 days; seven-day break and restart the eighth day. Results: 115 patients were admitted to the study, a Pearl index of 0.98 was obtained. Most common side effects: one pregnancy, weight gain, fluid retention, nausea, skin blemishes. One patient discontinued treatment for adverse effects (vomiting and nausea). Conclusions: Genesa® presents an adequate Pearl Index in Venezuelan woman.

6.
Eur J Contracept Reprod Health Care ; 22(1): 11-16, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27684740

RESUMO

OBJECTIVES: The aim of the study was to assess the efficacy for menstrual-related symptoms of an extended flexible regimen of an oral contraceptive pill containing 20 µg ethinylestradiol and 3 mg drospirenone in comparison with a 24/4 d cyclical regimen of the same formulation. METHODS: This randomised, non-inferiority, open-label, multicentre study was conducted in women aged 18-39 years. Their menstrual-related symptoms were assessed using the Penn Daily Symptom Rating (DSR17). Participants were randomised to use an extended flexible regimen of 20 µg ethinylestradiol and 3 mg drospirenone (EE/DRSPe.flex), comprising 168 consecutive days with a 4-d hormone-free interval (HFI, allowing for management of unexpected bleeding) or a conventional 24/4 cyclical regimen of the same pill (EE/DRSP24/4). The primary measure of efficacy was the percentage change in DSR17 total score from baseline to cycle 6. The secondary measures of efficacy were the percentage changes in DSR17 total score from baseline after each 28-d interval throughout the entire study and in the scores for individual DSR17 symptoms. RESULTS: The primary analysis demonstrated that EE/DRSPe.flex was not inferior to EE/DRSP24/4 (Mean DSR17 score 9.1; 95% confidence interval (CI) - 2.5, 20.6; p = 0.123). Analysis at intervals throughout the entire evaluation period showed greater reduction in DSR17 total score for EE/DRSPe.flex than for the 24/4 regimen (p < 0.001). The decreases in individual scores for the symptoms 'poor coordination' and 'depression/feeling sad/down or blue' were greater for the extended flexible regimen than for the cyclical regimen (p < 0.05). CONCLUSION: The extended flexible regimen was not inferior to the 24/4 cyclical regimen in terms of the primary endpoint. It significantly improved symptoms in the interval analysis, and the effects on specific DSR17 symptoms, compared with the cyclical regimen.


Assuntos
Androstenos/administração & dosagem , Anticoncepcionais Orais Combinados/administração & dosagem , Estrogênios/administração & dosagem , Etinilestradiol/administração & dosagem , Ciclo Menstrual/efeitos dos fármacos , Distúrbios Menstruais/tratamento farmacológico , Antagonistas de Receptores de Mineralocorticoides/administração & dosagem , Adolescente , Adulto , Esquema de Medicação , Feminino , Humanos , Adulto Jovem
7.
Rev. bras. pesqui. méd. biol ; Braz. j. med. biol. res;49(1): 00601, 2016. tab, graf
Artigo em Inglês | LILACS | ID: lil-765006

RESUMO

Drospirenone (DRSP) is a progestin with anti-aldosterone properties and it reduces blood pressure in hypertensive women. However, the effects of DRSP on endothelium-dependent coronary vasodilation have not been evaluated. This study investigated the effects of combined therapy with estrogen (E2) and DRSP on endothelium-dependent vasodilation of the coronary bed of ovariectomized (OVX) spontaneously hypertensive rats. Female spontaneously hypertensive rats (n=87) at 12 weeks of age were randomly divided into sham operated (Sham), OVX, OVX treated with E2 (E2), and OVX treated with E2 and DRSP (E2+DRSP) groups. Hemodynamic parameters were directly evaluated by catheter insertion into the femoral artery. Endothelium-dependent vasodilation in response to bradykinin in the coronary arterial bed was assessed using isolated hearts according to a modified Langendorff method. Coronary protein expression of endothelial nitric oxide synthase and estrogen receptor alpha (ER-α) was assessed by Western blotting. Histological slices of coronary arteries were stained with hematoxylin and eosin, and morphometric parameters were analyzed. Oxidative stress was assessed in situ by dihydroethidium fluorescence. Ovariectomy increased systolic blood pressure, which was only prevented by E2+DRSP treatment. Estrogen deficiency caused endothelial dysfunction, which was prevented by both treatments. However, the vasodilator response in the E2+DRSP group was significantly higher at the three highest concentrations compared with the OVX group. Reduced ER-α expression in OVX rats was restored by both treatments. Morphometric parameters and oxidative stress were augmented by OVX and reduced by E2 and E2+DRSP treatments. Hormonal therapy with E2 and DRSP may be an important therapeutic option in the prevention of coronary heart disease in hypertensive post-menopausal women.


Assuntos
Animais , Feminino , Ratos , Androstenos/administração & dosagem , Vasos Coronários/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Estradiol/administração & dosagem , Terapia de Reposição Hormonal/métodos , Hipertensão/tratamento farmacológico , Vasodilatação/efeitos dos fármacos , Western Blotting , Bradicinina/farmacologia , Terapia Combinada , Vasos Coronários/patologia , Receptor alfa de Estrogênio/efeitos dos fármacos , Estrogênios/administração & dosagem , Etídio/análogos & derivados , Artéria Femoral , Hemodinâmica , Antagonistas de Receptores de Mineralocorticoides/administração & dosagem , Óxido Nítrico Sintase Tipo III/efeitos dos fármacos , Ovariectomia , Estresse Oxidativo/efeitos dos fármacos , Distribuição Aleatória , Ratos Endogâmicos SHR , Vasodilatadores/farmacologia
8.
Arch Dermatol Res ; 307(10): 905-15, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26472098

RESUMO

Several studies have reported an increase in the prevalence of adult female acne. This subtype of acne presents particular characteristics, and can be triggered by several factors such as smoking, stress, the use of oily cosmetics and even by poor sleep. Sleep quality is related to well-being and the maintenance of body homeostasis. In addition, several skin diseases present a bidirectional relationship with sleep, demonstrating an important connection between skin and the central nervous system. With this in mind, we aimed to compare the effect of two types of treatment for adult female acne (azelaic acid or a combined oral contraceptive) on sleep quality and on concentrations of stress hormones. Also, we proposed to assess the correlation of sleep and hormonal parameters with acne severity. In order to do this, 32 women underwent a clinical evaluation, completed the Pittsburgh Sleep Quality Index (PSQI) questionnaire and had their blood collected for hormone assays. These procedures were performed at baseline and after 6 months of treatment. At baseline there were no differences between the groups in terms of body mass index, age, acne severity and hormone concentrations. Results showed that both treatments demonstrated effectiveness but that women treated with azelaic acid presented a better sleep quality after the treatment compared to baseline and to the group treated with the combined oral contraceptive. The combined oral contraceptive group presented an increase in cortisol and a decrease in free testosterone concentration in relation to baseline. These data suggest that both azelaic acid and combined oral contraceptive are effective in the treatment of adult female acne but, azelaic acid seems to be a more suitable option for those women who may benefit from a better subjective sleep quality.


Assuntos
Acne Vulgar/tratamento farmacológico , Anticoncepcionais Orais Combinados/uso terapêutico , Anticoncepcionais Orais Hormonais/uso terapêutico , Ácidos Dicarboxílicos/uso terapêutico , Medicamentos Indutores do Sono/uso terapêutico , Sono/efeitos dos fármacos , Hormônio Adrenocorticotrópico/sangue , Adulto , Sistema Nervoso Central/fisiologia , Feminino , Humanos , Hidrocortisona/sangue , Fenômenos Fisiológicos da Pele , Inquéritos e Questionários , Testosterona/sangue
9.
Rev. obstet. ginecol. Venezuela ; 73(4): 225-233, dic. 2013. tab
Artigo em Espanhol | LILACS-Express | LILACS | ID: lil-710645

RESUMO

Objetivo: Comparar los efectos de la terapia hormonal combinada (drospirenona /17 β-estradiol) versus un placebo sobre el peso corporal u otras variables antropométricas en pacientes posmenopáusicas asistidas en la consulta ginecológica del Hospital “Dr. Manuel Noriega Trigo”, Estado Zulia, Venezuela. Métodos: Estudio cuasi-experimental, de casos y controles, aleatorio, a simple ciego, en el cual participaron 120 mujeres posmenopáusicas, divididas en dos grupos para recibir una dosis diaria durante 6 meses de una terapia hormonal combinada (grupo A; drospirenona 2 mg/ 17 β-estradiol 1 mg) o un placebo (grupo B). Se evaluaron tanto el peso corporal como el índice de masa corporal, circunferencia abdominal e índice de cintura cadera, antes y al final del tratamiento. Resultados: Se evidenció que en el grupo que recibió la terapia hormonal hubo una reducción de alrededor de 3 kg en la media del peso corporal luego de 6 meses de tratamiento (79,80±9,35 vs. 76,33±8,36; P< 0,001); asimismo, una reducción significativa en el índice de masa corporal (30,12±2,02 vs. 28,72±1,79; P< 0,001), circunferencia abdominal (120,10±14,73 vs. 110,10±14,00; P< 0,001) y en el índice cintura cadera (0,87±0,04 vs. 0,84±0,07; P< 0,05). En el grupo que recibió un placebo no hubo modificaciones significativas en estas variables. Conclusiones: La terapia hormonal con drospirenona /17 β-estradiol se asoció con una reducción significativa del peso corporal, índice de masa corporal, circunferencia abdominal e índice cintura cadera luego de 6 meses de tratamiento en posmenopáusicas; con pocos o leves efectos adversos.


Objective: To compare the effects of combined hormonal therapy (drospirenone/17 β-estradiol) versus a placebo on body weight and other anthropometric variables in postmenopausal women assisted in the gynecology consultation at the Hospital “Dr. Manuel Noriega Trigo”, in Zulia state, Venezuela. Methods: A quasi-experimental, case control, randomized, single blind study, which involved 120 postmenopausal women, divided into two groups to receive a daily dose for 6 months of combined hormone therapy (group A; drospirenone 2 mg/ 17 β-estradiol) or placebo (group B). We evaluated body weight, body mass index, waist circumference and waist-hip ratio, before and at the end of treatment. Results: We showed that in the group receiving hormonal therapy with drospirenone / 17 β-estradiol was a reduction of about 3 kg in mean body weight after 6 months of treatment (79,80 ± 9,35 vs. 76,33 ± 8,36; P <0,001); and a significant reduction in body mass index (30,12 ± 02,02 vs. 28,72 ± 1,79; P <0,001), abdominal circumference (120,10 ± 14,73 vs. 110,10 ± 14,00; P <0,001) and waist hip (0,87 ± 0,04 vs. 0,84 ± 0,07; P <0;05). In the group receiving a placebo had no significant changes in these variables. Conclusions: Hormonal therapy with drospirenone / 17 β-estradiol was associated with a significant reduction in body weight, body mass index, waist circumference and waist-hip ratio after 6 months of treatment in postmenopausal women, with few or mild side effects.

10.
Rev. bras. saúde mater. infant ; 13(3): 259-266, jul.-set. 2013. graf, tab
Artigo em Inglês | LILACS, BVSAM | ID: lil-688728

RESUMO

To compare the endometrial effects and uterine bleeding patterns associated with treatment using (1) levonorgestrel-releasing intrauterine system (LNG-IUS) and estradiol (1 mg/day, p.o.) or (2) orally administered drospirenone (2 mg/day) andestradiol (1 mg/day). METHODS: thirty-four patients (aged 52.53 ± 4.44 in the LNG-IUS group and 53.15 ± 4.018 in the DRSP group) were randomized. The severity of menopausal symptoms was evaluated using the Kupperman index every three months. Transvaginal ultrasound, hysteroscopy and histological evaluation were repeated after 12 months. During this period, patients kept menstrual calendars. All categorical variables were described as percentages. Variables were tested for normal distribution and Student's t test was applied for independent samples and ANOVA forrepeated measures when appropriate. Data were considered to be significant when p<0.05. RESULTS: slight vaginal bleeding was reported in the first month of treatment by 53.3 percent of patients from the LNG-IUS/estradiol group compared with 7.7 percent of patients from the drospirenone/estradiol group. There were no differences in endometrial thickness between the two groups throughout the study period. End-of-study histological findings showed atrophic endometrium in 53.3 percent of patients in the LNG-IUS/estradiol group compared with 76.9 percent of patients in the drospirenone/estradiol group. CONCLUSIONS: our results suggest good endometrial protection with both HT regimens...


Comparar os efeitos endometriais e no padrão de sangramento uterino de tratamento com (1) sistema intrauterine com levonorgestrel (SIU-LNG) e estradiol (1 mg/dia, v.o.) ou (2) associação oral de drospirenona (DRSP) (2 mg/dia) e estradiol (1 mg/dia). MÉTODOS: trinta e quatro pacientes (idade 52,53 ± 4,44 grupo SIU-LNG e 53,15 ± 4,018 grupo DRSP)foram randomizadas. A gravidade dos sintomas menopausais foi avaliado pelo índice de Kupperman a cada três meses. Ultrassom transvaginal, histeroscopia e avaliação histológica foram repetidos após 12 meses. Durante este período, as pacientes fizeram registros em calendários menstruais. Todas as variáveis categóricas foram descritas como porcentagens. Variáveis foram testadas para distribuição normal e teste t de Student para amostras independents e ANOVA para medidas repetidas foram utilizados quando apropriado. Significância estatística foi considerada para p<0.05. RESULTADOS: leve sangramento vaginal foi relatado no primeiro mês de tratamento por 53,3 por cento das pacientes do grupo SIU-LNG/estradiol vs. 7,7 por cento das pacientes do grupo drospirenona/estradiol. Não houve diferença na espessura endometrial entre os grupos durante o periodo do estudo. Os achados histológicos ao final do estudo motraram endométrio atrófico em 53,3 por cento das pacientes no grupo SIU-LNG/estradiol vs. 76,9 por cento das pacientes no grupo drospirenona/estradiol. CONCLUSÕES: nossos resultados sugerem boa proteção endometrial com ambos os tratamentos de terapia hormonal...


Assuntos
Humanos , Feminino , Pessoa de Meia-Idade , Endométrio , Estradiol/uso terapêutico , Levanogestrel/uso terapêutico , Pós-Menopausa , Terapia de Reposição de Estrogênios
11.
Braz. j. pharm. sci ; 49(3): 521-528, July-Sept. 2013. ilus, tab
Artigo em Inglês | LILACS | ID: lil-689905

RESUMO

A simple, rapid, economical and reliable high performance liquid chromatographic method has been developed and successfully applied in simultaneous determination of ethinyl estradiol and drospirenone in coated tablets. The HPLC method was performed on a LiChroCART® 100RP column (125x4 mm i.d., 5 µm) with acetonitrile:water 50:50 (v/v) as mobile phase, pumped at a flow rate of 1.0 mL.min-1. The fluorescence detection for ethinyl estradiol was made at λex= 280 nm and λem= 310 nm and a UV detection for drospirenone was made at 200 nm. The elution time for ethinyl estradiol and drospirenone were 4.0 and 5.7 min, respectively. The method was validated in accordance to USP 34 guidelines. The proposed HPLC method presented advantages over reported methods and is suitable for quality control assays of ethinyl estradiol and drospirenone in coated tablets.


Um método simples, rápido, econômico e confiável foi desenvolvido empregando a cromatografia líquida de alta eficiência para a determinação simultânea de etinilestradiol e drospirenona em comprimidos revestidos. O método foi realizado utilizando coluna LiChroCART® 100RP (125 x 4 mm d.i., 5 µm), a fase móvel constituída de acetonitrila:água, 50:50 (v/v) com vazão de 1,0 mL.min-1. A detecção foi realizada empregando fluorescência em λex= 280 nm e λem= 310 nm para o etinilestradiol e na região de UV em 200 nm para a drospirenona. O etinilestradiol e a drospirenona tiveram tempo de retenção de 4,0 e 5,7 min, respectivamente. O método foi validado de acordo com as diretrizes da USP 34. O método proposto apresentou vantagens sobre os relatados na literatura e pode ser considerado adequado para o controle de qualidade do etinilestradiol e da drospirenona em comprimidos revestidos.


Assuntos
Cromatografia Líquida de Alta Pressão , Anticoncepcionais Orais/análise , Etinilestradiol/farmacocinética , Comprimidos com Revestimento Entérico , Fluorescência
12.
Int J Womens Health ; 4: 543-9, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23091400

RESUMO

BACKGROUND: The effect of resveratrol on the management of endometriosis-related pain was investigated in 12 patients who failed to obtain pain relief during use of an oral contraceptive containing drospirenone + ethinylestradiol. METHODS AND RESULTS: The addition of 30 mg of resveratrol to the contraceptive regimen resulted in a significant reduction in pain scores, with 82% of patients reporting complete resolution of dysmenorrhea and pelvic pain after 2 months of use. In a separate experiment, aromatase and cyclo-oxygenase-2 expression were investigated in the endometrial tissue of 42 patients submitted to laparoscopy and hysteroscopy for the management of endometriosis. Sixteen of these patients were using oral contraceptives alone prior to hospital admission, while the remaining 26 were using them in combination with resveratrol. Inhibition of both aromatase and cyclo-oxygenase-2 expression was significantly greater in the eutopic endometrium of patients using combined drospirenone + resveratrol therapy compared with the endometrium of patients using oral contraceptives alone. CONCLUSION: These results suggest that resveratrol potentiates the effect of oral contraceptives in the management of endometriosis-associated dysmenorrhea by further decreasing aromatase and cyclo-oxygenase-2 expression in the endometrium.

13.
Rev. Fac. Med. (Caracas) ; 34(1): 60-63, 2011. tab
Artigo em Espanhol | LILACS | ID: lil-637406

RESUMO

El síndrome de ovario poliquístico es un desorden heterogéneo de etiología incierta, que cual afecta entre el 6% y 10% de las mujeres en edad reproductiva. Una de las opciones terapéuticas especificas es el uso de los anticonceptivos orales, con la progestina, drospirerona, la cual, es un análogo de la espironolactona que posee actividad antimineralcorticoides y antiandrogénica. El objetivo de este estudio fue determinar el efecto del anticonceptivo oral combinado (EE: 30 MG y DRP: 3 mg) en el perfil bioquímico y clínico en una población de mujeres venezolanas con síndrome de ovario poliquístico. De las 20 pacientes incluidas en el estudio, 18 completaron satisfactoriamente el estudio, con una buena tolerancia al tratamiento. Se observó una disminución del IMC de 23,94 en condición basal a 23,73 kg/m². Los niveles de andrógenos se encontraron disminuidos significativamente en comparación a la basal; testosterona total cayó de 1,4 ng/mL a 0,67 ng/mL; Testosterona libre bajo de 3 pg/mL a 1,38 pg/mL; DHEAS disminuyó de 1,65 µg/mL a 1,08 µg/mL y androstenediona de 2,50 ng/mL a 1,55 ng/mL. En conclusión nuestros resultados reportan que el uso de un anticonceptivo oral que contiene 30 mg de EE y 3 mg de progestina, drospirerona en una población de mujeres venezolanas con síndrome de ovario poliquístico condujo a una disminución de los niveles de andrógenos al mismo tiempo que se evidenció un incremento de la SHBG, así como una reducción no significativa del peso corporal de este grupo de pacientes y una mejoría clínica del hirsutismo.


Policystic ovarian syndrome is a heterogeneous disorder wich etiology remained uncertain and affects 6%-10% of reproductive age women. Most recommended therapy is oral contraceptives with progestins. Drospirenone is an espironolactone analogue exhibits a partial antiandrogenic action and has predominant anti-mineralocorticoid properties. This is a prospective trial to determine efficacy of a drospirenone-containing combined oral contraceptives in venezuelan women with polycystic ovary-syndrome. Twenty women were conducted into this trial, although 18 were treated. With treatment, BMI fell by 0,21 kg/m(2) in the study group. During therapy, the levels of testosterone, free testosterone, Delta (4)-androstenedione, and androstenedione decreased significantly, whereas sex hormone-binding globulin increased significantly. Treatment of women with polycystic ovary-syndrome with drospironene containing combined oral contraceptives formulations is effective in decreasing hirsutism, androgen levels and BMI.


Assuntos
Adolescente , Adulto , Anticoncepcionais Orais/uso terapêutico , Etinilestradiol/uso terapêutico , Hiperandrogenismo/patologia , Hiperandrogenismo/tratamento farmacológico , Síndrome do Ovário Policístico/tratamento farmacológico , Síndrome do Ovário Policístico/terapia , Ginecologia
14.
Rev. chil. obstet. ginecol ; 76(2): 94-101, 2011. tab
Artigo em Espanhol | LILACS | ID: lil-592084

RESUMO

Objetivo: Evaluar en una experiencia piloto la aceptabilidad y bienestar de la usuaria, después de un periodo de 12 meses de un anticonceptivo hormonal combinado oral de baja dosis estrogénica, con modalidad de uso extendido de 84 píldoras activas consecutivas, seguidas de 7 días de placebo. Método: Se incorporan 25 mujeres voluntarias que usan una combinación de 20 ug de etinilestradiol + 3 mg de drospirenona, con un tiempo de uso de 12 meses. En calendario de registro diario se consignan los días de sangrado o goteo genital así como todo tipo de fármaco ingerido. Al término de los 12 meses se efectúa una encuesta respecto al grado de satisfacción con la posología recibida. Resultados: 13 usuarias (52 por ciento) cumplen los 12 meses de uso. Todas ellas manifiestan un alto grado de conformidad, destacando las ventajas de presentar periodos menstruales ocasionales, mejoría marcada en la sintomatología compatible con el síndrome de tensión premenstrual con el consiguiente incremento del bienestar general. Siete usuarias (28 por ciento) no terminan el estudio por razones médicas, siendo 6 de estas por alteraciones de los flujos rojos y en 5 casos (20 por ciento) se producen retiros no médicos. Conclusión: Esta experiencia, que es la primera con la formulación descrita, confirma en un porcentaje de usuarias las bondades adicionales reportadas en las experiencias previas con otros productos similares, respecto al uso extendido de anticoncepción hormonal oral en un grupo de mujeres que deseaban espaciar sus periodos menstruales.


Objetives: A pilot study designed in order to know about the acceptability of an oral combined contraceptive pill, with low estrogen dose used in an extended way of 84 consecutive days, followed by 7 days of no pills ingestion during a scheduled follow up of 1 year. Methods: 25 volunteers women were recruited among those which wants to use oral combined contraceptive pills and who accepted this extended way of use. Combined contraceptive pills contains each 20 ug of ethinylestradiol plus 3 mg of drosperinone. At admission women were provided with menstrual diary cards in order to check all bleeding days plus any extra pharmaceutical compound received. At the end of the 12 months follow up an interview was done in order to know women experiences and acceptability of this extended way of use. Results: 52 percent of women end the study at the scheduled 12 months use. All of them feel that the main advantages of these extended way of use were to have few menstrual periods and improving premenstrual symtomatology with better quality of life. 7 women (28 percent) did not finish the study because of medical reasons being due in 6 of these for bleeding disturbances. Conclusions: This report is pioneer with the use this hormone combination in this extended type way of use. Results confirm previous positive reports experiences using another similar hormonal compounds with this extended way of use in women who want to reduce the interval of their menstrual periods.


Assuntos
Humanos , Adolescente , Adulto , Feminino , Pessoa de Meia-Idade , Androstenos/administração & dosagem , Anticoncepcionais Orais Combinados/administração & dosagem , Ciclo Menstrual , Etinilestradiol/administração & dosagem , Menstruação , Cooperação do Paciente , Satisfação do Paciente , Projetos Piloto , Inquéritos e Questionários , Substâncias para o Controle da Reprodução/administração & dosagem
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