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PubMed1983

Disposition of medroxyprogesterone acetate and drug metabolism activity.

The role of drug-metabolizing enzyme activity on the disposition of medroxyprogesterone acetate (MPA) was investigated in male rats. The metabolizing enzyme system was induced by phenobarbital (PB) or inhibited by SKF 525A. Plasma concentrations of unmetabolized MPA and the amounts of MPA-related residues in various tissues were higher in the SKF 525A and slightly lower in the PB treated animals than in the controls. The disappearance of MPA-related substances from the lung, skeletal muscle and brain was slow, and in the lung there was even an increase in the amount of radioactivity in the PB and saline treated rats at 24 hr. Almost equal amounts of radioactivity were excreted in the urine and intestine in the control rats, while the induction of drug metabolism enhanced the excretion in the urine and its reduction enhanced elimination in the intestinal tract within 24 hours. The findings demonstrate that plasma and tissue levels of MPA and its elimination route are influenced by the drug metabolism activity.

Animals↗
PubMed1983

The bioavailability of an orally administered medroxyprogesterone acetate suspension.

The relative bioavailability of an orally administered aqueous suspension of medroxyprogesterone acetate (MPA) intended for intramuscular injection (Depo-Provera) was determined in relation to orally administered tablets. Serum levels of MPA were determined by radioimmunoassay following the administration of 400-mg doses to 19 adult male volunteers in a crossover design after an overnight fast. The two treatments were judged bioequivalent based upon a comparison of the resultant MPA serum levels and the derived bioavailability parameters. Hence, the intramuscular suspension administered orally offers an alternative means of achieving optimal serum levels of MPA in patients requiring high dose therapy.

Administration, Oral↗
PubMed1982

[Oral high-dose medroxyprogesterone acetate (MPA) in the treatment of advanced and recurrent breast cancer: a dose-response evaluation].

The antitumor effect and side effects of oral high-dose Medroxyprogesterone acetate (MPA) therapy were studied in 110 patients with advanced or recurrent breast cancer. MPA in 200 mg tablets was consecutively administered at a daily dose of 600, 800, 1,000, 1,200, 1,600, 1,800 or 2,400 mg. The overall response rate was 32/110 (29.1%), and the highest response rate was obtained in the 1,200 mg group (38.2%). The response rate by the site of lesion was higher in the soft tissues and also in bone metastases. Side effects such as moon face, vaginal spotting and abnormal glucose tolerance was mild and tolerable. Accordingly, from the antitumor effect and side effects, the optimal dose was considered to be 1,200 mg a day. Furthermore, as MPA therapy increases appetite and body weight of patients without causing myelopoietic depression, this drug could be used successfully in combination with other chemotherapeutic agents.

Adult↗
PubMedDate not supplied

Effect of injection volume on the bioavailability of sterile medroxyprogesterone acetate suspension.

The influence of injection volume on the absorption and bioavailability of medroxyprogesterone acetate (MPA) was studied. A single i.m. injection of MPA 400 mg was administered to 24 healthy men; 12 of the subjects received 4 ml of a 100 mg/ml suspension of the drug, and the other 12 subjects were given 1 ml of a 400 mg/ml suspension. Blood samples for MPA determinations were collected periodically during a 202-day period after drug administration. Mean steady-state serum concentrations of MPA were simulated from single-dose data to reflect those achieved after standard dosage regimens. Values for area under the serum concentration-time curve and time required to reach peak serum concentrations were compared between subjects receiving different injection volumes of MPA. Mean peak serum concentration were significantly higher and occurred significantly sooner in subjects receiving the 4-ml injection of MPA than in those given the 1-ml injection. No significant differences in areas under the serum concentration-time curve were noted in subjects receiving different injection volumes. The rate but not the extent of absorption of injectable MPA suspension is enhanced by increasing the injection volume of equivalent doses from 1 ml to 4 ml.

Adult↗
PubMed1983

[Therapy of the surgical menopause syndrome with depot medroxyprogesterone acetate and its objective evaluation testing the reaction of the anterior pituitary gland to stimulation with gonadotropin-releasing hormone].

A randomized placebo-controlled double-blind study was conducted to evaluate the effect of 150 mg depot medroxyprogesterone acetate (DMPA) intramuscularly on the surgical menopause syndrome. The clinical material consisted of 30 hysterectomized and bilaterally salpingo-oophorectomized women between 38 and 54 years of age. Inclusion criteria were regular menstrual cycles until operation, the appearance of frequent vasomotor flushes (VMF) after operation, and serum FSH levels exceeding 20 mIU per ml. Since it has been shown that an increase in "LH pulses" and basal serum LH levels constitute objective parameters of VMF, determination of LH was chosen as biochemical criterion of therapeutic efficacy. DMPA was proven to reduce basal serum LH levels owing to its suppressive effect on the adenohypophysis. In order to clarify and quantify the suppressive potency of DMPA and obtain precise information on its mechanism of action, pituitary stimulation tests with gonadotropin releasing hormone (GnRH tests) were performed before and then at 2 and 6 weeks after initiation of therapy. Pituitary response to GnRH remained unaltered, however, at a level corresponding to the decreased basal concentrations, i.e. "LH peaks" dropped by more than 50% (p less than 0.005, Student t-test). The incidence of VMF decreased significantly and remained at a low level until 6 weeks after the administration of DMPA. Treatment with placebo resulted in a slight, but not significant decrease in VMF and did not affect the functional capacity of the adenohypophysis. A remarkable correlation was observed between the reduced size of "LH peaks" and the diminished incidence of VMF. Therefore, evaluation of pituitary response to stimulation with GnRH represents a helpful objective parameter in the assessment of the efficacy of DMPA.

Adult↗
PubMedDate not supplied

Hepatic impairment during simultaneous administration of medroxyprogesterone acetate and tamoxifen in the treatment of endometrial and ovarian carcinoma.

Simultaneous administration of medroxyprogesterone acetate (MPA) and tamoxifen markedly elevated the serum alanine and aspartate aminotransferase activities in 4 out of 30 patients with endometrial or ovarian carcinoma; and also slightly increased the activities of gamma-glutamyl transferase in 2 of the patients. These pathological changes spontaneously returned to normal in 1 patient, and after the cessation of tamoxifen or tamoxifen plus MPA treatment in 3 patients. This kind of hepatic impairment was thought to be caused by reversible damage of liver cells possibly associated with slight intrahepatic cholestasis. It is suggested that special attention be paid to liver function during simultaneous MPA and tamoxifen administration; in case of adverse liver reaction during the combined treatment, a formula of sequential administration of the drugs could be implemented.

Aged↗
PubMed1984

Alterations and reversibility of digestive and absorptive functions of rat intestine following medroxyprogesterone acetate administration.

The long term (90 days) effects of medroxyprogesterone acetate (MPA) administration on the digestive and absorptive functions of the small gut have been investigated in female albino rats. The uptake of glucose and amino acids was found to be significantly increased while Ca++ uptake decreased following MPA treatment (35 mg/kg body weight). The observed increase in glucose uptake might be due to carrier mediated transport in enterocytes and not to a change in cell number. The Michaelis constant for glucose uptake was not altered by MPA. Activities of brush border membrane disaccharidases, leucine aminopeptidase and basolateral membrane enzyme Na+, K+-ATPase were significantly increased in response to MPA treatment. It was observed that these biochemical alterations caused by MPA in intestinal digestive and absorptive functions were reversible by 5 weeks after termination of the drug treatment. The action of the drug appears to closely resemble that of known effects of glucocorticoids on intestinal mucosa.

Animals↗
PubMed1984

Effect of medroxyprogesterone acetate on the intestinal absorptive functions in protein-deficient rat.

Effect of Medroxyprogesterone acetate (MPA) at a dose level of 35mg/Kg body weight per week for four weeks on the intestinal uptake of nutrients viz glucose, amino acids, (alanine and leucine), calcium and zinc has been investigated in protein-deficient female rats. The administration of MPA was found to enhance significantly the uptake of glucose and amino acids in both the pair-fed and the protein-deficient rats. In contrast, calcium uptake was depressed as a result of treatment with the drug as well as protein-deficiency. The uptake of zinc was not affected on drug administration. This steroidal contraceptive caused elevation in sodium-dependent glucose uptake, while the sodium-independent uptake remained unaltered. The kinetic parameters of glucose and leucine uptake indicate that MPA might be inducing the transport carrier protein of these nutrients as elevation in Vmax of these nutrients transport system was observed following its administration.

Amino Acids↗
PubMed1984

A comparison of the effects of phenobarbital and medroxyprogesterone acetate on drug and glucose metabolism in rats with chemical liver injury.

The effects of medroxyprogesterone acetate (MPA) and phenobarbital (PB) on hepatic glucose and drug metabolism were investigated in male rats after liver injury, induced with dimethylnitrosamine (DMN). MPA normalized fasting blood glucose (BG) and serum immunoreactive insulin (IRI) levels and enhanced hepatic glucose-6-phosphatase (G6Pase) and NADPH cytochrome P450 reductase activities and glycogen and cytochrome P450 (cytP450) contents after liver injury. PB improved hepatic glycogen and cytP450 contents and NADPH cytP450 reductase activity in DMN pretreated rats. The increase in drug metabolism was more pronounced after PB than MPA therapy whereas MPA had more effect on glucose metabolism than had PB. This suggests that the inducing properties of these compounds diverge from each other.

Animals↗
PubMed1984

Oral route administration of medroxyprogesterone acetate (MAP) at high doses in the treatment of advanced breast cancer: clinical results.

Twenty-six patients with metastatic breast cancer were treated with high dose medroxyprogesterone acetate (MAP) p.o. according to currently available pharmacokinetic data (2000 mg/day b.i.d. for 30 days, 1000 mg/day for the following 60 days). Objective response (WHO criteria) was obtained in seven patients (CR + PR = 27%), with good results on visceral and soft tissue localizations; performance status improvement and/or pain relief was obtained in twenty-three (88%). Oral high dose MPA seems to be an effective and well tolerated palliative treatment in advanced breast cancer.

Administration, Oral↗
PubMed1984

The effect of high dose medroxyprogesterone acetate on water and salt metabolism in advanced cancer patients.

Ten advanced cancer patients (both with hormone-sensitive and non-hormone sensitive tumors) were treated with high dose medroxyprogesterone acetate (MAP, greater than 500 mg/day). We determined body weight, lean body mass, blood pressure, sodium blood level, urinary excretion, and exchangeable sodium pool by the 22Na method before and after treatment. These data seem to exclude a fluid retentive effect for high-dose MAP.

Antineoplastic Agents↗
PubMed1983

Effect of medroxyprogesterone acetate on liver collagen and drug metabolism in rats after chemical liver injury.

The effect of medroxyprogesterone acetate (MPA) on the hepatic collagen and drug metabolism was investigated in female rats following dimethylnitrosamine (DMN) induced liver injury. The increased liver collagen content and prolyl hydroxylase (PH) activity caused by DMN were associated with decreased cytochrome P-450 and benzo(a)pyrene hydroxylase activity. During the repair phase after the liver injury there was a decline in liver collagen and PH activity while the drug metabolizing capacity of the liver increased. This inverse relationship between collagen and drug metabolism was further enhanced by MPA. The findings show that MPA stimulates liver function by enhancing favorable repair processes after liver injury.

Animals↗
PubMed1984

[Metastatic breast cancer: a comparative study of the efficacy of tamoxifen and the sequential administration of tamoxifen and medroxyprogesterone acetate].

Seventy-nine patients with an histologically proven disseminated breast cancer, never treated before with additive hormonal therapy, entered into a randomized trial between june 1981 and december 1982. In the first group 44 patients were given continually a daily dose of tamoxifen (TAM) of 20 mg/m2. In the 2nd group 35 patients were given a daily dose of TAM of 20 mg/m2 for 15 days and then an oral daily dose of medroxyprogesterone acetate of 350 mg/m2 for the next 15 days. In both groups I and II, the treatment was stopped at the first manifestation of progression of the disease. The hormonal receptor status was determined in 30 patients of the group I and 23 patients of the group II. An objective response to treatment was observed in 48 per cent of the patients of the group I and 60 per cent of the group II. This difference is not significant (X2 = 1,05). However, the mean duration of therapeutic response is significantly higher in the group II (p = 0,01).

Adenocarcinoma↗
PubMed1981

Gross and histopathologic effects of medroxyprogesterone acetate and progesterone on the mammary glands of adult beagle bitches.

Adult beagle bitches received 0.2 to 75 mg/kg doses of medroxyprogesterone acetate (MPA) once every 3 months for 1 to 1.5 years. Doses greater than 2.0 mg/kg prevented the recurrence of ovarian cycles; lower doses did not. MPA (10 and 75 mg/kg) induced a dose-related development of multiple, large (greater than 5 mm diameter) mammary nodules that occurred earlier in older dogs than in younger dogs. MPA-induced mammary hyperplasia and nonnodular dysplasias were also noted. Most of the large (5 to 110 mm in diameter) MPA-induced nodules were, in nearly equal numbers, nodules of lobular hyperplasia, simple adenomas, or complex adenomas. Such benign mammopathies all appear to have histopathologic counterparts in human breast disease. However, simple adenomas are uncommon in both humans and dogs. Some of the MPA-induced nodules were benign mixed tumors with cartilaginous metaplasia. No malignant tumors were found. Induction of mammary tumors by 75 mg MPA/kg was not affected by prior ovariectomy but was reached by prior hypophysectomy, suggesting involvement of pituitary secretion in MPA-induced mammary gland disease.

Adenoma↗
PubMed1981

Effects of 17 beta-estradiol and medroxyprogesterone acetate upon MtTW15 mammosomatotropic pituitary tumor growth and hormone production in male and female rats.

The purpose of this study was to characterize the effects of two functionally diverse steroids, 17 beta-estradiol and medroxyprogesterone acetate (MPA), on MtTW15 rat mammosomatotropic pituitary tumor growth and hormone production. Steroid responsiveness, as well as the hormonally autonomous nature of the tumor, was studied by treating both male and female tumor-bearing rats for 7 weeks with weekly injections of either 17 beta-estradiol (600 ng/g body weight/week) or MPA (200 microgram/g body weight/week) and, subsequently, comparing both the tumor weights and the in vivo production of growth hormone (GH) and prolactin (PRL) among the treatment groups. Large tumors (6 to 20 gm) were obtained in all treatment groups, indicating hormonal autonomy; however, tumors were markedly smaller, on the average, in untreated males an ovariectomized females. Treatment of such rats with 17 beta-estradiol stimulated tumor growth. Radioimmunoassay of tumor and serum GH and PRL levels in all treatment groups indicated the following: (a) tumors from untreated male or female hosts did not favor the production of one hormone over the other to any great extent; (b) MPA, however, promoted significant increases (p less than 0.05) in GH production in both male and female tumor-bearing rats while having little effect on the production of PRL; and (c) 17 beta-estradiol significantly inhibited (p less than 0.05) GH production and promoted PRL production by tumors borne by either sex. Selected studies utilizing multiple doses of MPA (1 to 500 microgram per gm body weight per week) and 17 beta-estradiol (10 to 800 ng per gm body weight per week) were accomplished and demonstrated that hormone production can be influenced in a dose-related manner. These results indicated that the estrogen-induced MtTW15 rat pituitary tumor is hormonally autonomous, yet divergently responsive to two different classes of steroidal compounds, thus making this tumor line an appropriate model for the study of hormonally responsive pituitary tumor cells.

Animals↗
PubMedDate not supplied

Ethinyl estradiol and medroxyprogesterone treatment in advanced breast cancer: a pilot study.

Twenty patients with disseminated breast cancer unresponsive to conventional chemotherapy and chemohormonotherapy were treated with an alternating sequential schedule of ethinyl estradiol and medroxyprogesterone on the basis of correlations between hormones and estrogen and progestin receptors. Of 19 evaluable patients, six underwent partial or complete remission, while five others showed minor responses.

Breast Neoplasms↗
PubMed1996

Depot medroxyprogesterone acetate contraception. Metabolic parameters and mood changes.

This review summarizes the existing literature regarding metabolic parameters and mood changes in women using depot medroxyprogesterone acetate (DMPA). MEDLINE and additional bibliographic sources were searched to identify English-language articles describing clinical trials and cross-sectional studies of DMPA published during the last 20 years. DMPA has little or no effect on glucose tolerance, but insulin levels may increase. An increase in low-density lipoprotein cholesterol and a decrease in high-density lipoprotein cholesterol have been observed in cross-sectional and longitudinal studies; however, there are no data to indicate whether the observed lipid alterations lead to adverse clinical events. There is some evidence suggesting decreased bone density in long-term DMPA users. Longitudinal data regarding bone density changes are needed to assess changes both during and after use. Most cross-sectional and longitudinal studies show increased mean weight or weight gain in DMPA users. Controlled studies of weight change that evaluate subgroups and effects of confounding variables are also needed to provide constructive advice to patients. Data regarding depression or mood changes in DMPA users are scanty and do not support a causal relationship between use of this contraceptive and affective disorders. For all of these parameters, case reports indicating adverse clinical outcomes are nearly absent from the literature despite widespread long-term international use of DMPA.

Affect↗
PubMedDate not supplied

Early experience with the contraceptive use of depot medroxyprogesterone acetate in an inner-city clinic population.

There are few data on the experience of American women with the injectable depot medroxyprogesterone acetate (DMPA) since its recent approval by the Food and Drug Administration for contraceptive use in the United States. An exploratory study was conducted using chart reviews and telephone interviews of 261 women who initiated DMPA use between December 1992 and June 1994 at either a hospital-based (48%) or community-based (49%) clinic in New York City. Most DMPA users were single (70%), had had at least one birth (88%), had had at least one abortion (67%) and had ever practiced contraception (75% of those with available data). Life-table DMPA continuation rates were 63% at six months and 42% at 12 months and were not affected by the users' age, marital status, pregnancy history, clinic site or proximity of residence to the clinic. Among adults, the risk of DMPA discontinuation was highest during the three-month period following the second injection, while among adolescents, this risk increased throughout the duration of use. The most commonly reported reasons for method discontinuation were side effects, primarily menstrual irregularities (30%) and weight gain (24%).

Adolescent↗