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PubMed1996

Tissue distribution and pharmacokinetics of centchroman. A new nonsteroidal postcoital contraceptive agent and its 7-desmethyl metabolite in female rats after a single oral dose.

This study reports assay methodology, tissue distribution, and the basic pharmacokinetic behavior of centchroman and its 7-desmethyl metabolite [7-desmethyl centchroman (DMC)] after a single 12.5 mg/kg po dose in young female rats. Plasma, liver, lung, spleen, uterus, and adipose tissue were collected at various time intervals up to 14 days after dose. Reversed-phase HPLC, coupled with fluorescence detector, was used for simultaneous determination of centchroman and DMC in biosamples. The drug and metabolite were quantitated up to 2 and 5 ng/ml in plasma and 10 and 20 ng/g in tissues, respectively. The assay method was validated in terms of accuracy, precision, interassay, and intraassay variability, and was found to be reliable and reproducible. Peak centchroman levels in all of the tissues were found between 8-12 hr, whereas DMC peaks appeared between 8 and 24 hr, except that in liver the first peak of 1.2 micrograms/g appeared in the 1-hr sample. Tissue-to-plasma concentration ratios of centchroman were > 200 times in the lung; > 100 times in the spleen, liver, and adipose tissue; and > 40 times in the uterus at maxima in each tissue. Similarly, tissue concentrations of DMC were > 350 times in the lung, > 100 times in the liver and spleen, and > 25 times in the uterus and adipose tissue than in the plasma. High tissue-to-plasma concentration ratios of metabolites than the parent drug are indicative of its greater affinity for tissues. Terminal half-life of the centchroman and DMC in plasma were 24.1 and 36.6 hr, respectively. The mean residence time of centchroman was highest in the liver (78.4 hr), followed by the uterus (72.7 hr), adipose tissue (47.5 hr), lung (46 hr), spleen (44.1 hr), and plasma (37.7 hr). The mean residence time of DMC was also highest in the liver (133.7 hr), followed by the uterus (122 hr), adipose tissue (85.2 hr), lung (62.6 hr), spleen (62.6 hr), and plasma (48.2 hr).

Administration, Oral↗
PubMed1997

[The use and effects of postcoital contraception].

OBJECTIVES: To find those people seeking post-coital contraception (PCC), its efficacy and effects. DESIGN: A crossover study using a structured questionnaire, filled in both at the moment of demand and after using PCC. SETTING: The "Nóvoa Santos" Family Planning Centre in Ourense. PARTICIPANTS: All those requesting PCC between January 1995 and June 1996 (220 in all). INTERVENTIONS: The PCC norm was 8 pills, two taken every 12 hours, of 0.05 mg of Ethinyloestradiol (EE) plus 0.5 mg of Norgestrel. MEASURES AND MAIN RESULTS: We analysed social and demographic variables, sexual behaviour and PCC use with the SPSS programme for Windows. 96.4% attending were women, average age 21.98. They began coitus at 18.58 years old. 191 (86.8%) had a stable partner and 0 to 3 coitus per week. The condom was the commonest method (90.6%). CONCLUSIONS: Young women requesting PCC immediately after the risk coitus are students and residents in the city. It is a method used when there are problems with the condom and the frequency of failure is low. Sexually active people should be informed of the existence and use of PCC, as should the health professionals who could be asked for it.

Adult↗
PubMed1997

[Postcoital contraception. Dates based on a 5-year use in a private consultation service].

BACKGROUND: The aim of this 5-year retrospective study is to define the efficacy of oestro-progestinic interception. METHODS: An oestro-progestinic mixture (0.05 mg ethinyl estradiol and 0.250 mg dlnorgestrel) was prescribed to 6003 women attending the gynaecological outpatients clinic of AIED (Associazione Italiana per l'Educazione Demografica) in Genoa, Italy, without evidence of any previous contra-indications. The prescription was of two pills at once and two pills 12 hours after. Before examination, the doctor asked for personal and medical history (age, date of onset of menses, unprotected intercourse date and anticonceptional failure); patients were also asked to report the data of the following menses to the clinic. The largest age range was between 20 and 24 years, probably because of their inadequate knowledge of contraceptives. The reasons for post-coital contraception were: sexual intercourse without contraceptive, failure of coitus interruptus and of the condom. RESULTS: Post-coital interception efficacy (monthly oestro-progestinic contraception was 99.5%) according to retrospective statistical analysis, was according to Pearl index 92.9% vs 50% without any contraceptive. CONCLUSIONS: Finally, the efficacy of this method, together with its easy management and low frequency of severe contra-indications, allows us to indicate the "morning after pill" as one of the most useful outpatient strategies to avoid unwanted pregnancies.

Adult↗
PubMed1987

Postcoital contraception with dl-norgestrel/ethinyl estradiol combination: six years experience in a student medical clinic.

Postcoital contraception with ethinyl estradiol/dl-norgestrel in combination has been available to women students attending the University of British Columbia since 1974. This paper reports on the side effects, cycle control and efficacy, for a six-year period (1979-1985). In this sample of women 50% reported side effects of nausea alone or nausea with vomiting. Length of the menstrual cycle was shortened in women who took the medication prior to the expected day of ovulation. The number of pregnancies reported was significantly (p less than 0.002) less than the number expected had the medication not been taken. Some women took the medication even though there was a possibility of conception earlier in the cycle and this might account for four of the failures. The mode of action of the postcoital medication remains unsolved making it difficult to understand possible reasons for the other 14 failures.

Adult↗
PubMed1980

Ethinyl estradiol and conjugated estrogens as postcoital contraceptives.

Five study centers enrolled 1,311 women seeking postcoital contraception methods. Ethinyl estradiol was administered at 5 mg/day and conjugated estrogens at 30 mg/day for five consecutive days starting within 72 hours of unprotected coitus. Eleven pregnancies occurred in the 976 women who had a single unprotected coitus at midcycle. Based on published information, 69 pregnancies would have been expected if no contraceptives were used. Although both treatments were effective in preventing pregnancy, ethinyl estradiol seemed to be more effective. At the two centers alternately prescribing both drugs, none of 137 women treated with ethinyl estradiol became pregnant, while six of the 132 given conjugated estrogens became pregnant. Women whose treatment commenced on the first postcoital day seemed to have lower pregnancy rates than those whose medication was delayed to the second or third postcoital day regardless of which drug was used. Side effects were mainly limited to nausea that occurred in 70% and vomiting that was experienced by 33% of all women treated.

Adolescent↗
PubMed1998

Emergency postcoital contraception.

Of the estimated 3.5 million unintended pregnancies that occur each year in the United States, some 1.7 million are thought to be the result of contraceptive failure. The extremely high numbers of unintended pregnancies not only in the United States but also worldwide indicates that emergency contraception remains an important but underused method of pregnancy prevention. Emergency postcoital contraception via mechanical or pharmacological means inhibits fertilization and/or implantation from unprotected sexual intercourse. Although emergency contraception has been used primarily in victims of sexual assault, it offers a low-cost, highly effective method to reduce the incidence of unintended pregnancy. Emergency contraception decreases the costs and emotional and physical risks to women who have had unprotected intercourse. Emergency contraception also increases the latitude women have to make reproductive decisions by offering an alternative to abortion and childbearing. The heart of the problem with emergency contraception is not the failure rate or side effects of specific methods but the fact that so few women and adolescents who have had unprotected intercourse know the option exists, and their providers may be reluctant to prescribe the method.

Adolescent↗
PubMed2005

Ectopic pregnancy with postcoital contraception--a case report.

The incidence of ectopic pregnancies is increasing. Common risk factors are tubal pathology, previous tubal surgery, previous ectopic pregnancy, intrauterine device use and embryo transfer. Levonelle-2, a progesterone-only postcoital contraceptive works by a combination of mechanisms including ovulation inhibition, prevention of fertilization, and inhibition of implantation. It is 85% effective and there have been 12 reported cases of ectopic pregnancy in the UK with its use. It is believed that progesterone slows the intratubal migration of the fertilized ovum. In the case reported here, a woman presented with an ectopic pregnancy after use of Levonelle-2 as postcoital contraception; there were no clinical predisposing risk factors. In the absence of any histological evidence of tubal damage, we suspect that the levonorgestrel from Levonelle-2 could have been responsible for delayed embryo transfer which resulted in the ectopic pregnancy.

Adult↗
PubMed1997

[Postcoital contraception. An emergency option].

In recent years, there has been a marked increase in the demand for postcoital contraception in both primary care centers and hospital emergency wards. This article proposes to assure professional nurses acquire adequate basic knowledge regarding this emergency contraceptive method. Due to the fact that nurses play a major role in providing women who seek this method a health education, we believe it is of importance to deal with this aspect carefully while discussing this topic.

Contraceptives, Postcoital↗
PubMed1987

[Postcoital contraception with dienogest].

Fifty eight fertile female volunteers between 20 to 45 years were enrolled in a clinical trial to evaluate the efficacy and tolerance of the progestin dienogest (17 alpha-cyanomethyl-17 beta-hydroxyestra-4,9-dien-3-one, VEB Jenapharm Jena GDR) as a postcoital contraceptive. An oral dose of 2 mg dienogest was administered immediately after each coitus. The 58 women reported 872 intercourses during 302 cycles. Frequency of ingestion was on average 3 times per cycle. Pregnancy occurred in 14 women corresponding to a Pearl-index of 55.6. The observed pregnancy rate referring to all intercourses was 1.6 per cent. The incidence of expected pregnancies in relation to the coital exposures was 4.04 per cent. As a result the risk of pregnancy was reduced 2.5 times by dienogest. Menstrual disorders occurred in 18.9 per cent in regard of the total numbers of cycles. The results and an overview of literature suggest that neither dienogest nor other progestins are suitable as a sole contraceptive method when used as a postcoital agent. They are only indicated as a risk-reducing method after so-called "contraceptive emergencies".

Adult↗