Pharmacodynamic effects of once-a-month combined injectable contraceptives.


:The pharmacology and clinical assessment of existing first generation once-a-month combined injectable contraceptives, mainly Deladroxate and Chinese Injectable No. 1, are reviewed. Although these two types of monthly injectables have been used in some million women in China and Latin America, Deladroxate needs indepth re-evaluation of its long-term toxicity and possible accumulation. For injectable No. 1, its disadvantage of being administered on an erratic schedule will cause significant confusion in family planning practice. When used in a strict once-a-month schedule, it is not sufficiently effective for contraception. In order to attain predictable menstrual cycle control as well as high efficacy with a 30-day injection schedule, two improved once-a-month injectable formulations, Cyclofem and Mesigyna, were developed. Pharmacokinetic/pharmacodynamic study on estrogenic components suggested that estradiol valerate and cypionate were suitable estrogen esters to give elevated plasma estrogen levels for 7 to 11 days. After a single injection of Cyclofem and Mesigyna, both formulations showed equal contraceptive effect with inhibition of follicle maturation for some 30 days and ovulation, corpus luteum formation for some 60 days. Multicentre studies on the optimization of dosages of progestogens and estrogens in once-a-month injectables confirmed that the full doses of Cyclofem (DMPA 25 mg/estradiol cypionate 5 mg) and Mesigyna (NET-EN 50 mg/estradiol valerate 5 mg) are suitable for large scale clinical trials. Pharmacodynamics and progestogen/estrogen ratio study indicated the importance of not only the absolute amounts of the progestogen and estrogen but also of their ratio. Reduction of estrogen dose resulted in breakthrough ovulation with both Cyclofem and Mesigyna. Also, it is important to note that the second part of the injection cycle is dominated by the progestogen component of both monthly formulations. A longitudinal study indicated that there is no accumulation of norethisterone after 12 months of treatment with NET-EN 50 mg and estradiol valerate 5 mg. :About 1 million women in Latin America and China have used the 1st generation once-a-month combined injectable contraceptives Deladroxate and Chinese Injectable No. 1. Animal toxicity studies of Deladroxate found pituitary hyperplasia in rats, breast tumors in beagles, and accumulation of estradiol enanthate in the body. Thus, long-term toxicity and accumulation of Deladroxate need to be reevaluated. The erratic schedule of the Injectable No. 1 (initially administered on day 5 with 2 ampoules or 1 dose on day 5 and 1 dose on day 12; subsequent administration on the 10-12th day of the cycles) will confuse acceptors and family planning providers. Yet, a strict once-a-month cycle of Injectable No. 1 does not adequately protect against conception. Researchers have developed 2 improved once-a-month injectable formulations, Cyclofem and Mesigyna, to achieve good menstrual cycle control and high efficacy. The estrogen components of both formulations (estradiol valerate and cypionate) sufficiently elevate plasma estrogen levels for 7-11 days. One injection of both formulations inhibits follicle maturation for about 30 days and ovulation and corpus luteum formation for about 60 days. The doses of Cyclofem (25 mg depot-medroxyprogesterone acetate + 5 mg estradiol cypionate) and Mesigyna (50 mg norethindrone acetate + estradiol valerate) have been found to be optimal for use in large scale clinical trials. Not only are the absolute amounts of the progestogen and estrogen important, but also the progestogen/estrogen ratio. A lower estrogen dose in both Cyclofem and Mesigyna effects breakthrough ovulation. The progestogen component predominates the 2nd part of the injection cycle in both formulations. Norethindrone does not accumulate in the body after 12 months of treatment with Mesigyna.






Sang GW




Has Abstract


1994-04-01 00:00:00














  • Implications of dispensing self-administered hormonal contraceptives in a 1-year supply: a California case study.

    abstract::On September 23, 2016, California became the sixth state to pass legislation requiring health plans and insurers to cover a 12-month supply of FDA-approved self-administered hormonal contraceptives such as contraceptive pills, patches and vaginal rings. This legislation is estimated to result in 38% of current contrac...


    pub_type: 杂志文章


    authors: McMenamin SB,Charles SA,Tabatabaeepour N,Shigekawa E,Corbett G

    更新日期:2017-05-01 00:00:00

  • A new experimental three-dimensional, reticular intrauterine device (3-DRIUD) composed of nitinol and silicone rubber.

    abstract:BACKGROUND:The aim of this study was to explore a new three-dimensional, reticular intrauterine device (3-DRIUD) composed of nitinol and silicone rubber and to observe the contraceptive effect of the device in rats. STUDY DESIGN:Two contraceptive experiments were performed. In the first, female rats underwent bilatera...


    pub_type: 杂志文章


    authors: Qiu Y,Wang LG,Zhang MH,Zhang YP,Zhang AD,Yang DT

    更新日期:2013-07-01 00:00:00

  • The probability of side effects with ovral, norinyl 1/50 and norlestrin.

    abstract::This report provides specific information on the prevalence rates of the most common side effects during the first 3 cycles of use of 3 combination oral contraceptives (OCs) containing 50 mcg estrogen. The probabilities of a symptom occurring for the first time, or persisting once present, during the initial cycles of...


    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Berger GS,Edelman DA,Talwar PP

    更新日期:1979-11-01 00:00:00

  • Over-the-internet availability of hormonal contraceptives regardless of risk factors.

    abstract:OBJECTIVE:The purpose of this study is to measure the accessibility to purchase oral and transdermal contraceptives over the Internet for low- and high-risk individuals. METHODS:The Internet was used to search for and order both oral and transdermal contraceptives. Using the "Google" search engine to locate online pha...


    pub_type: 杂志文章


    authors: Memmel LM,Miller L,Gardner J

    更新日期:2006-04-01 00:00:00

  • Prospective study on the cytological aspects of the nasal respiratory epithelium in premenopausal women taking 30 mcg ethinylestradiol and 3 mg drospirenone oral contraceptive.

    abstract:BACKGROUND:This study was conducted to determine the effects of the monophasic oral contraceptive (OC) containing 30 mcg ethinylestradiol (EE) and 3 mg drospirenone (DRSP) on the nasal respiratory epithelium in premenopausal women. STUDY DESIGN:Fifty premenopausal women participated in the prospective study. Baseline ...


    pub_type: 临床试验,杂志文章


    authors: Caruso S,Serra A,Grillo C,Agnello C,Di Mari L,Cianci A

    更新日期:2008-05-01 00:00:00

  • The intensive and extensive margins of contraceptive use: comparing the effects of method choice and method initiation.

    abstract:OBJECTIVES:The risk of pregnancy is estimated to be 20 times as high among women who use oral contraception, and 90 times as high among condom users, as among women who use certain long-acting contraceptive methods. We explored the population-level implications of this variation in contraceptive efficacy. STUDY DESIGN...


    pub_type: 杂志文章


    authors: Thomas A,Karpilow Q

    更新日期:2016-08-01 00:00:00

  • Ultrastructural changes in the spermatozoa of langur monkeys Presbytis entellus entellus after vas occlusion with styrene maleic anhydride.

    abstract::Changes in the physical characteristics of semen and ultrastructure of the spermatozoa of langur monkeys after vas occlusion with styrene maleic anhydride (SMA), a polymer with pH-lowering action, are reported. Vas occlusion resulted in severe reversible hypospermia. Severe oligospermia was observed in the majority of...


    pub_type: 杂志文章


    authors: Lohiya NK,Manivannan B,Mishra PK

    更新日期:1998-02-01 00:00:00

  • A comparison of contraceptive procurement pre- and post-benefit change.

    abstract:BACKGROUND:In 2002, the Kaiser Foundation Health Plan in California changed its coverage policy to include 100% universal coverage for the most effective forms of contraception and for emergency contraceptive pills (ECPs). This study sought to evaluate whether removing the cost of contraception as a potential barrier t...


    pub_type: 杂志文章


    authors: Postlethwaite D,Trussell J,Zoolakis A,Shabear R,Petitti D

    更新日期:2007-11-01 00:00:00

  • Comparison of outcomes at 6 weeks following postpartum intrauterine contraceptive device insertions by doctors and nurses in India: a case-control study.

    abstract:OBJECTIVE:As part of a strategy to revitalize postpartum family planning services, Government of India revised its policy in 2013 to permit trained nurses and midwives to insert postpartum intrauterine contraceptive devices (PPIUCDs). This study compares two key outcomes of PPIUCD insertions--expulsion and infection--f...


    pub_type: 杂志文章


    authors: Yadav V,Balasubramaniam S,Das S,Srivastava A,Srivastava A,Kumar S,Sood B

    更新日期:2016-04-01 00:00:00

  • Maintaining physiological testosterone levels by adding dehydroepiandrosterone to combined oral contraceptives: I. Endocrine effects.

    abstract:OBJECTIVE:To determine whether adding dehydroepiandrosterone to combined oral contraceptives (COCs) maintains physiological levels of free testosterone. STUDY DESIGN:A randomized, double-blind, placebo-controlled, two-way crossover study conducted in 81 healthy women (age range: 20-35 years; Body mass index (BMI) rang...


    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Coelingh Bennink HJT,Zimmerman Y,Laan E,Termeer HMM,Appels N,Albert A,Fauser BCJM,Thijssen JHH,van Lunsen RHW

    更新日期:2017-11-01 00:00:00

  • Can mifepristone medical abortion be simplified? A review of the evidence and questions for future research.

    abstract::Mifepristone medical abortion has been a valuable addition to the reproductive health options of women. Aspects of its provision have however sometimes limited its accessibility and use. This article summarizes existing evidence for simplifying the provision of medical abortion and thus increasing its availability. We...


    pub_type: 杂志文章,评审


    authors: Clark WH,Gold M,Grossman D,Winikoff B

    更新日期:2007-04-01 00:00:00

  • Medicaid and fulfillment of desired postpartum sterilization.

    abstract:OBJECTIVE:We sought to assess fulfillment of sterilization requests while accounting for the complex interplay between insurance, clinical and social factors in a contemporary context that included both inpatient and outpatient postpartum sterilization procedures. STUDY DESIGN:This is a retrospective single-center coh...


    pub_type: 杂志文章


    authors: Arora KS,Wilkinson B,Verbus E,Montague M,Morris J,Ascha M,Mercer BM

    更新日期:2018-06-01 00:00:00

  • Effect of steroid hormones on the metabolism of human spermatozoa.

    abstract::Information relating to the effect of steroids on the metabolism and motility of human spermatozoa is limited despite the increasing interest in the use of these hormones for the purpose of contraception. In the present study it was shown that progesterone, testosterone, and 11-beta-OH-progesterone significantly inhib...


    pub_type: 杂志文章


    authors: Trifunac NP,Bernstein GS

    更新日期:1981-05-01 00:00:00

  • Use effectiveness of a spermicidal suppository containing benzalkonium chloride.

    abstract::A multicentric trial in 9 Spanish Clinics of Family Planning was conducted to evaluate the effectiveness of a vaginal contraceptive Ovule (suppository), containing 18.9 mg of benzalkonium chloride. Gynaecological and cytobacteriological examinations were made to evaluate any possible side-effect. Six-hundred-fifty-thr...


    pub_type: 临床试验,杂志文章


    authors: Méndez F,Castro A,Ortega A

    更新日期:1986-10-01 00:00:00

  • Acceptability of Norplant implants for fertility regulation in Singapore.

    abstract::The continuation rate at the end of this five-year clinical study was 60% with no accidental pregnancy occurring throughout the five years. The post-removal conception rate in women desiring pregnancy was 92% at the end of two years. The majority of acceptors described the overall experience with the implants as favou...


    pub_type: 杂志文章


    authors: Singh K,Viegas OA,Fong YF,Ratnam SS

    更新日期:1992-01-01 00:00:00

  • Did increasing use of highly effective contraception contribute to declining abortions in Iowa?

    abstract:BACKGROUND:Between 2006 and 2008, Iowa increased access to family planning services through a Medicaid expansion and a privately funded initiative. During this same time, Iowa expanded access to abortion through telemedicine provision of medical abortion. Despite increased access to abortion services, abortions in Iowa...


    pub_type: 杂志文章


    authors: Biggs MA,Rocca CH,Brindis CD,Hirsch H,Grossman D

    更新日期:2015-02-01 00:00:00

  • Do as we say, not as we do: experiences of unprotected intercourse reported by members of the Society of Family Planning.

    abstract:OBJECTIVES:We examine the lifetime and past-year prevalence and circumstances of unprotected intercourse among members of the Society of Family Planning (SFP), a professional reproductive health organization in the United States. STUDY DESIGN:We invited the membership of SFP (n=477) via email to participate in an anon...


    pub_type: 杂志文章


    authors: Aiken AR,Trussell J

    更新日期:2015-07-01 00:00:00

  • Estimating systemic exposure to levonorgestrel from an oral contraceptive.

    abstract:OBJECTIVE:The gold standard for measuring oral contraceptive (OC) pharmacokinetics is the 24-h steady-state area under the curve (AUC). We conducted this study to assess whether limited sampling at steady state or measurements following use of one or two OCs could provide an adequate proxy in epidemiological studies fo...


    pub_type: 杂志文章


    authors: Basaraba CN,Westhoff CL,Pike MC,Nandakumar R,Cremers S

    更新日期:2017-04-01 00:00:00

  • Serum lipids in Chinese patients using oral contraceptive pills.

    abstract::Eighty-four Chinese patients attending the Family Planning Association of Hong Kong for contraception with oral contraceptive pills were randomized into 2 groups. The first group received pills containing 0.15 mg levonorgestrel and 0.03 mg ethinyl oestradiol. The second group received pills containing 0.15 mg desogest...


    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Ho PC,Liu WT,Kwan MS

    更新日期:1990-01-01 00:00:00

  • Misoprostol as an adjunct to overnight osmotic dilators prior to second trimester dilation and evacuation: A systematic review and meta-analysis.

    abstract:OBJECTIVE:To understand effect of adjunct misoprostol on cervical preparation with overnight osmotic dilators for dilation and evacuation after 16 weeks gestation. METHODS:We searched on-line reference databases using search terms for second trimester, abortion, misoprostol, and dilators. Randomized controlled trials ...


    pub_type: 杂志文章


    authors: Cahill EP,Henkel A,Shaw JG,Shaw KA

    更新日期:2020-02-01 00:00:00

  • A prospective, non-randomized study of home use of mifepristone for medical abortion in the U.S.

    abstract:OBJECTIVE:To determine the acceptability of taking mifepristone at home for early medical abortion in the United States. STUDY DESIGN:This prospective, non-randomized, open-label study at six Planned Parenthood centers gave women with pregnancies up to 63 days' gestation seeking medical abortion the choice of taking m...


    pub_type: 临床试验,杂志文章,多中心研究


    authors: Chong E,Frye LJ,Castle J,Dean G,Kuehl L,Winikoff B

    更新日期:2015-09-01 00:00:00

  • Factors associated with contraceptive nonuse among US women ages 35-44 years at risk of unwanted pregnancy.

    abstract:BACKGROUND:Women ages 35 years and older have the greatest proportion of contraceptive nonuse and unintended pregnancies ending in abortion. STUDY DESIGN:We conducted a population-based case-control study among women ages 35-44 years at risk of unwanted pregnancy using the National Survey of Family Growth (NSFG) data ...


    pub_type: 杂志文章


    authors: Upson K,Reed SD,Prager SW,Schiff MA

    更新日期:2010-05-01 00:00:00

  • Doing more for less: identifying opportunities to expand public sector access to safe abortion in South Africa through budget impact analysis.

    abstract:OBJECTIVE(S):To estimate the costs of public-sector abortion provision in South Africa and to explore the potential for expanding access at reduced cost by changing the mix of technologies used. STUDY DESIGN:We conducted a budget impact analysis using public sector abortion statistics and published cost data. We estim...


    pub_type: 杂志文章


    authors: Lince-Deroche N,Harries J,Constant D,Morroni C,Pleaner M,Fetters T,Grossman D,Blanchard K,Sinanovic E

    更新日期:2018-02-01 00:00:00

  • An initial pharmacokinetic study with a Metered Dose Transdermal Systemfor delivery of the progestogen Nestorone as a possible future contraceptive.

    abstract:BACKGROUND:Transdermal delivery of steroids is gaining popularity for contraception and hormone replacement therapy. This study aimed to test metered spray delivery of a precise dosage of Nestorone (NES) progestogen as a possible transdermal progestogen-only contraceptive. STUDY DESIGN:Six healthy postmenopausal volun...


    pub_type: 杂志文章


    authors: Fraser IS,Weisberg E,Kumar N,Kumar S,Humberstone AJ,McCrossin L,Shaw D,Tsong YY,Sitruk-Ware R

    更新日期:2007-12-01 00:00:00

  • A multicenter efficacy and safety study of an oral contraceptive containing 150 micrograms desogestrel and 30 micrograms ethinyl estradiol.

    abstract::The study reported herein is the primary efficacy and safety study conducted to support U.S. registration of an oral contraceptive containing 150 micrograms desogestrel and 30 micrograms ethinyl estradiol. A large multicenter study enrolled 1,221 women at 50 centers in the United Kingdom. A total of 11,656 cycles of e...


    pub_type: 临床试验,杂志文章,多中心研究


    authors: Walling M

    更新日期:1992-10-01 00:00:00

  • Latin american experience with two low-dose oral contraceptives containing 30 microg ethinylestradiol/75 microg gestodene and 20 microg ethinylestradiol/150 microg desogestrel.

    abstract::The objective of this study was to compare cycle control, efficacy and tolerance of an oral contraceptive containing 20 microg ethinylestradiol and 150 microg desogestrel with a preparation containing 30 microg ethinylestradiol combined with 75 microg gestodene. This study involved 342 women and 4104 cycles use in Arg...


    pub_type: 临床试验,杂志文章,多中心研究,随机对照试验


    authors: Bassol S,Alvarado A,Celis C,Cravioto MC,Peralta O,Montaño R,Novelli J,Albornoz H,Kesseru E,Soares A,Petracco A,Isaia B,Mendes J,Bahamondes L,de Melo NR,Reyes-Marquez R,Albrecht G

    更新日期:2000-09-01 00:00:00

  • The lack of effect of sodium valproate on the pharmacokinetics of oral contraceptive steroids.

    abstract::Patients taking anticonvulsants such as phenobarbitone, phenytoin and carbamazepine together with their oral contraceptive steroid may suffer contraceptive failure because of the enzyme-inducing properties of these anticonvulsants. We have examined, in six women, the effect of sodium valproate, an effective broad spec...


    pub_type: 杂志文章


    authors: Crawford P,Chadwick D,Cleland P,Tjia J,Cowie A,Back DJ,Orme ML

    更新日期:1986-01-01 00:00:00

  • An assessment of the quality of information available on the internet about the IUD and the potential impact on contraceptive choices.

    abstract::This study analyzed data gathered from a survey of online information on the intrauterine device (IUD) to determine the content and quality of information available to consumers and providers, as evidenced by the presence or absence of a series of attributes measuring the accuracy and objectiveness of information prov...


    pub_type: 杂志文章


    authors: Weiss E,Moore K

    更新日期:2003-11-01 00:00:00

  • Safety and efficacy of Implanon, a single-rod implantable contraceptive containing etonogestrel.

    abstract:OBJECTIVES:The safety and efficacy of a single-rod implantable contraceptive containing etonogestrel (Implanontrade mark) were investigated in a multicenter clinical trial. STUDY DESIGN:Sexually active American women (N=330) with apparently normal menstrual cycles used the implant for up to 2 years. All subjects recor...


    pub_type: 临床试验,杂志文章,多中心研究


    authors: Funk S,Miller MM,Mishell DR Jr,Archer DF,Poindexter A,Schmidt J,Zampaglione E,Implanon US Study Group.

    更新日期:2005-05-01 00:00:00

  • "And Isn't that the point?": pleasure and contraceptive decisions.

    abstract:OBJECTIVE:Previous survey research indicates that women and men experience reduced sexual pleasure when using condoms, especially compared to nonbarrier family planning methods. This study seeks to explore those experiences of reduced pleasure in-depth and how they affect contraceptive method decisions and use. STUDY ...


    pub_type: 杂志文章


    authors: Fennell J

    更新日期:2014-04-01 00:00:00