Anticonceptivos / Contraconceptive

No disponible

Contraceptive and hormonal properties of the stem bark of Dysoxylum binectariferum in rat and docking analysis of rohitukine, the alkaloid isolated from active chloroform soluble fraction.

BACKGROUND: This study was aimed to investigate the pregnancy interceptive activity of the stem bark of Dysoxylum binectariferum Hook. f. administered during the pre- and peri-implantation periods and immediately after implantation by oral route in adult female Sprague-Dawley rats. STUDY DESIGN: Ethanolic extract and its fractions were administered to female rats on Days 1-10, Days 1-7, Days 1-5 or Day 1 postcoitum by oral route. At autopsy on Day 12, the number and status of corpora lutea and implantations were recorded. For estrogenic activity, ovariectomized immature rats received the test extract or the vehicle once daily for 3 days and at autopsy on Day 4, uterine weight and status of vaginal opening and extent of vaginal cornification were recorded. For antiestrogenic activity, the extract was administered along with ethinyl estradiol. Docking analysis of rohitukine, the alkaloid isolated from active chloroform soluble fraction, to estrogen receptor (ERalpha) was conducted using AutoDock 3.0.5 on a Linux workstation. RESULTS: The ethanolic extract intercepted pregnancy in rats at a daily dose of 500 mg/kg on Days 1-7 postcoitum. On fractionation, the activity was localized in the chloroform fraction, which inhibited pregnancy in all females at the 35-mg/kg dose on Days 1-7, at the 50-mg/kg dose on Days 1-5 or at the single 300-mg/kg dose on Day 1 postcoitum. Chromatography of this fraction yielded an alkaloid, rohitukine, which prevented pregnancy at the 10-mg/kg dose administered on Days 1-7 but was partially (45%) effective at this dose when administered during the entire preimplantation period and ineffective even at 10 times this dose when administered only on Day 1 postcoitum, except that there was a significant reduction in implantation number in pregnant females. While the active chloroform soluble fraction was devoid of any estrogen agonistic or antagonistic properties, a mild uterotropic effect without induction of premature opening of vagina or cornification of vaginal epithelium was observed in rohitukine at the 10-mg/kg dose. Rohitukine, with an almost similar molecular size (mol. wt. 305) as 17beta-estradiol, fits ideally into the hydrophobic pocket of ER. While it does not appear to simultaneously interact with GLU353, ARG394 and HIS524 as estradiol to elicit frank estrogenic response, different conformations of the ligand or its metabolite(s) might acquire geometry with phenolic groups at C-3', C-5 and C-7 positions disposed in a fashion to interact with active site(s) of ER, which might be responsible for its contraceptive and/or weak uterotropic effects. The absence of a basic side chain directed toward the antiestrogen binding site (ASP351) on the receptor appears to be responsible for the lack of any estrogen antagonistic activity. CONCLUSIONS: Findings demonstrate the antifertility activity of the ethanolic extract of D. binectariferum, its chloroform soluble fraction and rohitukine. Efforts are being made to enhance the anti-implantation activity of rohitukine by structural modifications.

Opinions of West Texas pharmacists about emergency contraception

Background: The pharmacist’s role in dispensing emergency contraception (EC) has become controversial due to the intersection of personal and professional ethics. Therefore, to examine the issue of EC availability, we surveyed a sample of West Texas pharmacists. West Texas is a religiously and politically conservative region where no methods of EC have been made available. Objective: to survey a sample of pharmacists in West Texas about their experience, beliefs, and knowledge of EC both before and after a presentation of the current literature about EC. Methods: We asked a convenience sample of 75 pharmacists about their experience, beliefs, and knowledge of EC both before and after a presentation of the current literature about EC. Results: Sixty-four (85%) pharmacists agreed to complete the study questionnaire. None carries EC in his/her pharmacy, and scientific understanding of EC was generally poor. Fourteen percent stated EC conflicts with their religious views, 17% considered it a method of abortion, 11% would not be willing to fill an EC prescription written by a doctor. 58% would be willing to offer EC over the counter. The presentation encouraged more to offer it over the counter, but in general did not significantly change their beliefs. Conclusion: Our sample of West Texas pharmacists demonstrated very little experience with, a general lack of knowledge about, and some personal and religious objections to EC (AU)

Antecedentes: El papel del farmacéutico dispensando contraceptivos de emergencias (CE) es controvertido debido a la intersección de la ética personal y profesional. Así que para examinar el problema de la disponibilidad de CE investigamos una muestra de farmacéuticos de West Texas. West Texas es una región religiosa y políticamente conservadora donde no están disponibles métodos de CE. Objetivo: Investigar una muestra de farmacéuticos de West Texas sobre sus experiencias, creencias y conocimiento de CE antes y después de una presentación sobre la literatura actual sobre CE. Métodos: Preguntamos a una muestra de conveniencia de 75 farmacéuticos sobre sus experiencias, creencias y conocimiento sobre CE antes y después de una presentación de la literatura actual sobre CE. Resultados: Sesenta y cuatro (85%) farmacéuticos aceptaron completar el cuestionario del estudio. Ninguno posee CE en su farmacia, y el conocimiento científico de la CE era realmente pobre. El catorce por ciento afirmó que la CE colisiona con sus creencias religiosas, el 17% lo consideró un método de aborto, el 11% no era capaz de dispensar una receta de CE escrita por un médico. El 58% sería capaz de ofrecer CE de libre venta. La presentación animó a ofrecerla como libre venta, pero en general no cambió sus creencias significativamente. Conclusión: Nuestra muestra de farmacéuticos de West Texas demostró muy poca experiencia, una falta general de conocimientos y algunas objeciones personales y religiosas sobre la CE (AU)

Developing a radioimmunoassay for anordrin: the synthesis of propionyl and hemisuccinyl esters of anordiol.

We describe the chemical synthesis of the 2 beta-propionate-17 beta- hemisuccinate and 2 beta-hemisuccinate-17 beta-propionate diesters of anordiol (2 alpha,17 alpha-diethynyl-A-nor-5 alpha-androstane-2 beta,17 beta-diol) and the method for coupling them to bovine serum albumin and Affi-gel 102, in order to prepare antibodies for radioimmunoassay of anordrin. In addition, we describe the chemical synthesis of the following derivatives: 2 beta-ol-17 beta-propionate, 2 beta-propionate-17 beta-ol, 2 beta-hemisuccinate-17 beta-ol, and 2 beta-ol-17 beta-hemisuccinate.