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PubMed1998

Pharmacokinetics of medroxyprogesterone acetate after single and multiple injection of Cyclofem in Chinese women.

To provide pharmacokinetic data for safety evaluation on prolonged treatment with Cyclofem, which contains 25 mg medroxyprogesterone acetate (MPA) and 5 mg estradiol cypionate in 0.5 mL microcrystalline aqueous suspension, the pharmacokinetic profiles of MPA after single and multiple administration of this monthly injectable contraceptive were investigated in Chinese women. Nine healthy fertile women received Cyclofem based on a once-a-month regiment for up to 1 year. Blood samples were collected immediately prior to drug administration and on days 1, 3, 5, 7, 14, 21, and 28 after injection. After the 1st, 6th, and 12th injection, the maximum serum concentrations (Cmax) of MPA were observed on days 3.4 +/- 0.9, 4.3 +/- 2.2, and 3.7 +/- 2.6, respectively. Cmax of serum MPA during the 1st, 6th, and 12th treatment cycles were 3.75 +/- 1.27, 5.54 +/- 1.79, and 5.55 +/- 1.80 nmol/L, whereas the areas under the curve (AUC0-28 days) were 55.84 +/- 28.15, 95.45 +/- 26.56, and 98.81 +/- 21.84 nmol/L.day, respectively. There was significant interindividual variation in the pharmacokinetics of MPA after intramuscular injection of Cyclofem. No significant change was demonstrated in mean residence time (MRT) of MPA after single and multiple injection. There was a tendency of increase in Cmax and AUC0-28 days of MPA during the first 6 months of treatment, whereas no further enhancement was found between the 6th and 12th injection (p > 0.05). Peak levels of estradiol (E2) observed in Cyclofem users were within the normal range of the preovulatory phase. Results of this long-term study suggest that no drug accumulation occurred after repeated administration of Cyclofem in the Chinese women.

Adult↗

PubMed1998

Bone density among long-term users of medroxyprogesterone acetate as a contraceptive.

The bone density (BD) of 72 women using depot-medroxyprogesterone acetate (DMPA) for at least 1 year was compared with that of 64 women who were not users of hormonal contraceptives. The BD of lumbar spine, femoral neck, Ward's triangle, and trochanter was measured by dual energy X-ray absorptiometry (DEXA-LUNAR DPX). Estradiol (E2) concentrations were measured by radioimmunoassay (RIA). The mean age of DMPA users and nonusers was 31.8 and 31.1 years, respectively. Mean E, was 55.7 pg/mL for users and 149.9 pg/mL for controls (p < 0.001). The BD was significantly lower for DMPA users than for controls in all sites (p < 0.01). In addition, young adult T-scores in the lumbar spine were significantly lower among DMPA users than in controls (p < 0.01). Differences were maintained in a subsample of 47 women per group paired by age and body mass index (BMI). Multiple regression analysis showed that older age, lower BMI, and longer amenorrhea were associated with lower BD in the femoral neck, whereas lower BMI and use of DMPA were associated with lower BD in the lumbar spine.

Absorptiometry, Photon↗

PubMed1999

Long-term depot-medroxyprogesterone acetate and bone mineral density.

The association between long-term use of depot-medroxyprogesterone acetate (DMPA) and bone mineral density (BMD) has been controversial, as seen in three case-control studies in New Zealand, Thailand, and the United Kingdom. In the present case-controlled study of BMD, a group of 67 Chinese women who had used DMPA from 5-15 years was compared with 218 women of the same age range who had not used any steroidal hormones. DMPA users were found to have a significantly lower BMD at lumbar vertebra (L2-4) (0.93 g/cm2), neck of femur (0.69 g/cm2), trochanter (0.59 g/cm2), and Ward's triangle (0.58 g/cm2), as compared with the control group, whose corresponding BMD values were 1.03 g/cm2, 0.83 g/cm2, 0.71 g/cm2, and 0.78 g/cm2, respectively (p < 0.001). The average percentage of bone loss per year was estimated to be 1.1% in L2-4, 2.3% in neck of femur, 2.4% in trochanter, and 3.5% in Ward's triangle. The percentage of bone loss in L2-4 was found to be more pronounced with age. This study provided information that the use of DMPA in a Chinese group for > 5 years in associated with bone loss, and a prospective study is needed to confirm these data, which are different from two case-control studies.

Absorptiometry, Photon↗

PubMed1999

Lunelle monthly contraceptive injection (medroxyprogesterone acetate and estradiol cypionate injectable suspension): effects of body weight and injection sites on pharmacokinetics.

A new contraceptive option, medroxyprogesterone acetate (MPA) and estradiol cypionate (E2C) (MPA/E2C, Lunelle Monthly Contraceptive Injection), will soon be available for women in the US. This article reports the results of a US trial that assessed the effects of body weight and injection site on the pharmacokinetics of MPA, the progestin mediating contraceptive efficacy. This assessment was part of a nonrandomized, open-label, multicenter US study in healthy women receiving a monthly injection of MPA/E2C for 60 weeks. A total of 77 women (aged 18-47 years) at four centers participated in the pharmacokinetics assessment during the sixth or the seventh injection. For determination of serum MPA concentration-time profiles, blood samples were collected before the sixth and seventh injections (day 0) and on days 3, 7, 14, 21, and 28 after the sixth and seventh monthly administrations. For effects of injection site, MPA pharmacokinetics were compared at injection sites of the arm, hip, and leg. The pharmacokinetics of MPA, determined at the sixth and seventh injection, were not significantly affected by injection sites. The mean area under the curve (AUC0-28), however, was different between the arm and the leg injection sites; the difference was < 20%. More important, the average MPA trough concentrations (Cmin) at the fifth and sixth monthly injections were similar (range 0.42-0.51 ng/mL) for the three injection sites and well above the threshold levels of 0.10-0.20 ng/mL required to suppress ovulation. For effects of body mass index (BMI) on pharmacokinetics, women were stratified into three groups: thin/normal (BMI 18-28, n = 48), obese (BMI 29-38, n = 23), and highly obese (BMI > 38, n = 6). There were no significant differences in the pharmacokinetics of MPA among the three BMI categories. The only significant difference (p = 0.0387) was the AUC0-28 between BMI 18-28 and BMI 29-38. Because of the small sample size in the highly obese group, a reanalysis was performed by pooling subjects of the obese and highly obese groups. Results of the pooled statistical analysis remained the same. In summary, these results suggest that minor differences observed in the MPA pharmacokinetics--whether due to injection site or body weight or both--have no impact on the contraceptive efficacy of MPA/E2C, as trough concentrations (Cmin) are well above the threshold levels required to suppress ovulation. No dose adjustment is necessary based on body weight or injection site.

Adult↗

PubMed1999

Lunelle monthly contraceptive injection (medroxyprogesterone acetate and estradiol cypionate injectable suspension): steady-state pharmacokinetics of MPA and E2 in surgically sterile women.

The steady-state pharmacokinetics and pharmacodynamics of medroxyprogesterone acetate (MPA) and estradiol (E2, released from E2C by esterase enzymes) were characterized after administration to surgically sterile women. This report describes the pharmacokinetics of this multiple-dose and open-labeled study (pharmacodynamics are reported in a subsequent article in this issue). Women with regular menstrual cycles were studied for one control cycle, 3 consecutive treatment months, and 3-5 months of follow-up. Blood samples were drawn before each monthly dose and at specified time points after the third monthly injection. A total of 16 women were enrolled, 14 of whom completed the study. These 14 women (13 white, one black) ranged in age from 28 to 43.4 years, in body weight from 47.6 to 68.9 kg, and in height from 150 to 175 cm. Mean serum MPA concentrations peaked in the first week after administration of MPA/E2C (Lunelle Monthly Contraceptive Injection). The mean MPA Cmax and AUC0-t(last) were 1.25 ng/mL and 32.13 ng.day/mL, respectively. Serum MPA concentrations declined with a mean terminal half-life of 14.7 days, indicating that absorption from the injection site is prolonged after administration of MPA/E2C. The time for MPA concentrations to fall below the lower limit of quantitation (i.e., < 10 pg/mL) after the third injection ranged from 63 to 84 days. The average MPA trough (Cmin' day 28) concentrations for the three consecutive monthly injections ranged from 0.44 to 0.47 pg/mL, indicating that steady-state conditions were achieved after the first injection. The MPA Cmin values were well above threshold levels required to suppress ovulation throughout the injection interval. Absorption of E2 from the injection site was also prolonged after injection of MPA/E2C. Mean concentrations of E2 peaked at approximately 2 days after the third injection, and the average Cmax was 247 pg/mL. Serum E2 levels declined with a terminal half-life of approximately 8 days; E2 levels returned to baseline (typically, approximately 100 pg/mL) by 14 days after each injection. The average trough (Cmin' day 28) levels for E2 ranged from 40 to 55 pg/mL. The results of this study demonstrate that steady-state conditions are achieved after the first injection of MPA/E2C; no further MPA or E2 accumulation occurs beyond the first injection. Furthermore, the E2 peak observed after injection of MPA/E2C is similar to the nontreated preovulatory E2 range and returns to baseline levels by approximately 14 days after injection.

Absorption↗

PubMed1983

Teratogenic effects of Silastic intrauterine devices in the rat with or without added medroxyprogesterone acetate.

The teratogenicity of intrauterine devices (IUDs) made of silicone rubber (Silastic, Dow Corning Corporation, Midland, MI) with or without added medroxyprogesterone acetate (MPA) has been investigated in the rat. Small rod-shaped IUDs were inserted into the uterus, one between each embryo, on day 9 of pregnancy and left in place until the rats were killed just before term for examination of the fetuses. MPA exposure caused masculinization of the external genitalia of female fetuses and feminization of the external genitalia of male fetuses. There was no increase in other, nongenital malformations in MPA-exposed fetuses, compared with fetuses exposed to Silastic alone, but both Silastic-exposed groups had significantly more malformations than untreated control rats. In a second experiment, a significant increase in malformations in fetuses exposed to Silastic alone, compared with untreated control fetuses, was confirmed. The malformation rate in control rats that underwent sham operations was not significantly increased, compared with untreated control rats.

Abnormalities, Drug-Induced↗

PubMed1988

Placebo-controlled study on serum concentrations of CA-125 before and after treatment of endometriosis with danazol or high-dose medroxyprogesterone acetate alone or after surgery.

Serum concentrations of CA-125 were determined in association with 6-month medical (n = 48) or surgical and medical therapy (n = 40) of endometriosis. The concentration of CA-125 was significantly higher in stages III + IV (66.6 +/- 22.0 [standard deviation] U/ml) than in stage I (20.9 +/- 2.3 U/ml) or II (28.4 +/- 2.8 U/ml); in stage II, the concentration was higher than in stage I. Surgical elimination of endometriosis significantly decreased the level of CA-125, as did danazol, but not medroxyprogesterone acetate (MPA), although these drugs were equal in clinical efficacy. The CA-125 changes during hormonal treatment did not correlate with the clinical response. Postoperatively, CA-125 responses to danazol, MPA, or placebo did not differ significantly from each other. During the 6-month follow-up after medication, the CA-125 concentrations tended to increase, especially in danazol-treated women. The determination of CA-125 is useful in estimating the extent of the disease, but it is less valuable in monitoring the treatment effect. The ability of danazol to suppress CA-125 expression emphasizes the specific properties of this drug.

Antigens, Neoplasm↗

PubMed1988

A randomized, double-blind trial of a gonadotropin releasing-hormone agonist (leuprolide) with or without medroxyprogesterone acetate in the treatment of leiomyomata uteri.

A randomized, double-blind study was performed on 16 women to compare the efficacy of daily subcutaneous (SC) injections of leuprolide acetate (LA; TAP Pharmaceuticals, North Chicago, IL) plus oral placebo tablets (group A, n = 7) with SC LA plus oral medroxyprogesterone acetate (The Upjohn Company, Kalamazoo, MI; group B, n = 9) in the treatment of leiomyomata uteri. Patients in group A had a significant reduction in uterine size from a pretreatment volume of 601 +/- 62 cm3 (mean +/- standard error) to a mean uterine volume of 294 +/- 46 cm3 at 24 weeks of therapy (P less than 0.01). Group B patients had a reduction in uterine volume from 811 +/- 174 cm3 to 688 +/- 154 cm3, which was not statistically significant. However, only one patient in group B experienced hot flashes, whereas six patients in group A had this symptom (P less than 0.01). Both groups demonstrated significant increases in mean hemoglobin concentrations, hematocrits, and serum iron levels at 24 weeks of therapy compared with pretreatment levels.

Adult↗

PubMed1988

Danazol and medroxyprogesterone acetate inefficacious in the treatment of infertility in endometriosis.

Danazol (200 mg three times a day) and medroxyprogesterone acetate (MPA, 100 mg a day) were compared with placebo in the treatment of infertility of patients with endometriosis. Twenty-seven patients had medical therapy alone for 6 months, and 22 patients received it after conservative surgery. The clinical characteristics of the patients in the danazol group (n = 18), the MPA group (n = 17), and the placebo group (n = 14) were comparable to each other. The follow-up time was 30 months. The cumulative pregnancy rates, 33% in the danazol group (n = 6), 42% in the MPA group (n = 7), and 46% in the placebo group (n = 6), did not differ significantly from each other. The time to pregnancy after the start of therapy was 17.7 +/- 8.4 (standard deviation [SD]) months in the danazol group, 18.0 +/- 9.0 months in the MPA group and 10.0 +/- 5.8 months in the placebo group with no significant difference between the groups. The abortion rate was 26%, and there was no significant difference among the groups. Cox multivariant analysis did reveal ovarian endometriosis a prognostically significant negative indicator as regards fecundation in endometriosis (P less than 0.05). In summary, correction of infertility alone does not appear to be an indication for the use of danazol or MPA in the treatment of endometriosis, and ovarian endometriotic lesions but not peritoneal ones do make a worse prognosis as regards fecundation in endometriosis.

Adult↗

PubMed1989

Suppression of sperm function by depot medroxyprogesterone acetate and testosterone enanthate in steroid male contraception.

Ten normal men were given three monthly intramuscular injections of 200 mg of depot medroxyprogesterone acetate (MPA) and 250 mg of testosterone (T) enanthate. Six men became azoospermic, while four remained oligozoospermic, with a mean sperm density of 1.5 +/- 0.3 standard error of the mean million/ml. Zona-free hamster oocyte penetration was abolished in all oligozoospermic samples at the end of treatment. Twenty of the 21 oligozoospermic samples yielding at least 0.6 to 5.0 million motile spermatozoa showed a complete absence of oocyte penetration. Semen parameters returned to normal, although some took up to 12 months. These findings demonstrated an antifertility action of MPA and T enanthate on the functional capacity of residual spermatozoa and support the view that extreme oligozoospermia may be a tenable target for reversible steroid male contraception.

Adult↗

PubMed1989

Circulating lipid and lipoprotein concentrations during danazol and high-dose medroxyprogesterone acetate therapy of endometriosis.

In a study on endometriosis, ten patients were treated with danazol (200 mg three times a day) and ten patients with high-dose medroxyprogesterone acetate (MPA) (100 mg a day) for 6 months. The circulating high-density lipoprotein-cholesterol concentration decreased significantly in the danazol (53%) and in the MPA groups (26%); the change in the danazol group was significantly higher than that in the MPA group. Danazol also significantly increased the low-density lipoprotein-cholesterol levels (37%), whereas MPA had no significant effect. Danazol (29%) and MPA (12%) decreased the apolipoprotein A-1 levels significantly. The decrease caused by danazol was significantly greater. Danazol also significantly decreased the apolipoprotein A-2 levels (12%) and significantly increased the apolipoprotein B levels (17%), whereas MPA had no significant effects on them. Three months after the end of medication, all values were at the pretreatment levels. The circulating cholesterol, triglyceride, and very low-density lipoprotein concentrations remained unchanged during both treatments. Danazol and high-dose MPA induced a similar significant regression of peritoneal endometriotic implants in relation to placebo. Our present results, showing that danazol, to a greater extent than high-dose MPA, is associated with changes in lipoprotein metabolism that expose the individual to an increased risk of cardiovascular diseases, suggest that high-dose MPA is preferable to danazol in the long-term treatment of endometriosis.

Adult↗

PubMed1983

The anabolic effect of high dose medroxyprogesterone acetate in oncology.

Ten advanced cancer patients not amendable to conventional therapy were treated with high dose (greater than 500 mg/day, for 30 days) Medroxyprogesterone Acetate (MAP) both orally and intramuscularly, in order to evaluate a possible anabolic effect of this hormone. During the treatment, mean protein intake increased from 37.2 gr/day to 58.8 gr/day (p less than 0.01), nitrogen intake from 5.8 to 9.4 gr/day (p less than 0.01) and caloric intake from 1407.9 to 2075 Kcal/day (p less than 0.01). Nitrogen balance also showed a significant increase (p less than 0.05), as well as elementary strength (p less than 0.02). Lean body mass and body weight did not show significant variations. The above data confirms what was already been documented by us in animals and proposed in man-that MAP has an anabolic effect.

Anabolic Agents↗

PubMedDate not supplied

Depot medroxyprogesterone. Management of side-effects commonly associated with its contraceptive use.

Depot medroxyprogesterone acetate is one of the most popular, effective methods of contraception used in the United States. Many women experience unpleasant side effects from this method, including episodic vaginal bleeding, hair loss, depression, and weight gain. This Clinical Practice Exchange describes the treatment strategies for these side-effects used by nurse-midwives from a variety of settings and locales. Contraceptive use can be more acceptable for many women if they are better able to cope with unpleasant side effects of the method. This Clinical Practice Exchange provides knowledge to enhance client coping.

Adaptation, Psychological↗

PubMed1980

Return of fertility after discontinuation of depot medroxyprogesterone acetate and intra-uterine devices in Northern Thailand.

796 Thai women who stopped using the long-acting injectable contraceptive 'Depo-Provera' (medroxyprogesterone acetate) and 125 women who had an intra-uterine device removed to have a planned pregnancy were followed-up to ascertain the delay between conception and the end of contraception, and to determine the proportion of women who did not conceive in the 2 years after discontinuation. The median delay before conception was 5.5 months plus the estimated duration of the effect of the last injection of depo-provera and 4.5 months after discontinuing the IUD. Since depo-provera acts for approximately 15 weeks, women can except a median delay to conception of around 9 months after their last injection. The proportions of women who did not conceive within 1 year and within 2 years of stopping contraception by the two methods were similar. There was no evidence to suggest that prolonged use of depo-provera increases the delay before conception, and the return of fertility among never pregnant ex-users resembled that of ever pregnant ex-users.

Delayed-Action Preparations↗

PubMed1988

Adjuvant therapy for operable breast cancer with medroxyprogesterone acetate alone in postmenopausal patients or in combination with CMF in premenopausal patients.

The present paper concerns two multicenter studies on adjuvant therapy with medroxyprogesterone acetate (MAP) for operable N+ breast cancer. The patients entered the study between April 1979 and March 1986. One hundred and fifty-one premenopausal patients were randomly assigned to receive either polychemotherapy (CMF) or CMF + MAP. One hundred and thirty-eight postmenopausal patients were randomized to receive either MAP h.d. or no treatment. CMF was administered according the following schedule: cyclophosphamide mg 100/ms p.o. 1-4 days; methotrexate mg 40/ms i.v. and fluorouracil mg 600/ms i.v. 1st and 8th days. The cycle was repeated six times every 28 days. MAP was administered at 1000 mg X 2/daily p.o. for 30 days and afterwards 500 mg X 2/daily for 5 months. In the premenopausal study after a median follow-up of 36 months no difference was observed in the incidence of recurrence, site of recurrence, actuarial 5-year disease-free survival (DFS) or overall survival (OS). In the postmenopausal study a statistically significant lower number of recurrences was observed in MAP-treatment patients after a median follow-up of 37 months. The effect of MAP was limited to patients with less than or equal to 3 metastatic axillary lymph nodes. In addition, there are suggestions that only patients with ER+ tumors draw some advantage from the treatment. On the other hand, no difference exists in the OS. The treatments were substantially well tolerated. The MAP + CMF regimen induces lower vomiting compared to the CMF alone. The most frequent MAP side-effects were vaginal spotting (16%) and tremors (12%). We conclude that MAP h.d., like tamoxifen and aminoglutethimide, can improve the DFS of operable N+ breast cancer in postmenopausal patients.

Adult↗

PubMed1983

Medroxyprogesterone induced changes in rat liver. A light and electron microscopic study.

Medroxyprogesterone acetate (MPA) induced morphological alterations in the normal female rat liver and after carbon tetrachloride exposure were assessed by light and electron microscopy and morphometry. Administration of MPA increased the smooth endoplasmic reticulum (SER) in normal rat. Carbon tetrachloride, injected intraperitoneally for four weeks, caused fatty accumulation, enlargement of the cell nucleus and decrease of the rough endoplasmic reticulum (RER) and increase of the SER. After one week of recovery, without treatment, the fatty infiltration and the SER membranes decreased and the RER increased. MPA, following injury, induced a decrease in the fatty accumulation and mitochondrial volume density and the hepatocyte nuclear and cytoplasm size normalized. The SER membrane volume density increased and the surface density decreased, the RER membrane volume density increased while the surface density did not alter significantly. The volume densities of the mitochondria and the peroxisomes decreased in the MPA treated CCl4 exposed groups. The results demonstrate that MPA induces a proliferation of the SER in normal rat liver and after hepatic injury the compound has a beneficial effect on the regeneration.

Animals↗

PubMed1990

Treatment of carcinoma of the breast with high dose oral medroxyprogesterone acetate: does increased bioavailability improve the therapeutic ratio?

Medroxyprogesterone acetate (MPA) is regarded as a valuable hormonal therapy for metastatic breast cancer. The drug is manufactured by more than one pharmaceutical company, and one particular brand of oral MPA (Provera Tablets, Upjohn) has been reformulated to incorporate micronized particles, providing significantly enhanced bioavailability. The response rate and side-effect data from a pilot study, which used the old formulation Provera Tablets 100 mg at a dosage of 800 mg/day in 28 patients with recurrent breast cancer after treatment with tamoxifen, are compared with those from another study in which 59 similar patients received 800 mg/day of new formulation Provera Tablets 200 mg. Neither of these studies, conducted in the United Kingdom, has previously been published. The response rates were similar in both studies, but there were higher incidences of significant weight gain and increased blood pressure in those patients treated with the new formulation. These side effects have been noticed by other workers employing new formulation MPA at a dosage of 800 mg per day, while it has been reported that reducing the dosage to 400 mg perday is accompanied by a lower incidence of side effects, without affecting the response rate. It is concluded that the increased serum levels of MPA, made possible by the micronized product, do not favourably influence the response of metastatic breast cancer to therapy, but may be associated with a higher incidence of side effects. Reducing the dosage of the new formulation MPA to 400 mg/day may allow a more acceptable side-effect profile, without loss of therapeutic efficacy. Such a dose reduction would make this brand of MPA more cost effective.

Administration, Oral↗

PubMed1992

Chemotherapy with or without high-dose medroxyprogesterone acetate in oestrogen-receptor-negative advanced breast cancer. Norwegian Breast Cancer Group.

In a randomised study 142 patients with advanced oestrogen-receptor-negative breast cancer in the tumour tissue received chemotherapy alone or chemotherapy combined with high doses (1000 mg daily) of oral medroxyprogesterone acetate (HD-MPA). Of the 126 fully evaluable for response, the response rates were 46% for chemotherapy alone and 73% for chemotherapy with HD-MPA (P = 0.005). There was no significant difference with regard to duration of response. Of the 138 patients evaluable for survival and toxicity, survival was shorter in the combined treatment group; median survival of 9 versus 13 months (P less than 0.05). Considerable toxicity was seen from HD-MPA, especially weight gain and fluid retention. The present study provides evidence that in concordance with preclinical studies an interaction between chemotherapy and HD-MPA may exist in breast cancer normally resistant to hormone therapy. The side-effects from MPA were substantial, however, and the survival data are of great concern.

Antineoplastic Agents↗