Pregnancy-specific changes of antipyrine pharmacokinetics correlate inversely with changes of estradiol/progesterone plasma concentration ratios.

Antipyrine pharmacokinetics as well as estradiol and progesterone concentrations were measured in plasma of 11 healthy pregnant women during the first two trimesters and again in the same patients 6 to 20 weeks after interruption of pregnancy. During pregnancy, the clearance of antipyrine increased and its half-life decreased in all but two instances. A significant inverse relationship was found between the degree of pregnancy-specific changes of plasma clearance of antipyrine and estradiol-progesterone plasma concentration ratios: high estradiol-progesterone ratios during pregnancy corresponded to decreased plasma clearance of antipyrine; low ratios of the two hormones during pregnancy corresponded to increased plasma clearance of antipyrine.

[Breast saving cancer surgery. Results of a long-term study (Berlin study, 1963-1982)].

Between 1963 and 1982, 1,139 patients underwent surgery for unilateral mammary malignoma at the Charlottenburg Gynaecological Clinic of the Free University Berlin. Primary therapy consisted of simple mastectomy in 948 cases and tumourectomy/quadrantectomy with subsequent radiotherapy (40 Gy) in 191 cases. We performed a retrospective analysis of "matched samples" of tumourectomy/quadrantectomy and mastectomy.

[Initial results in the treatment of endometriosis with the LH-RH analog buserelin].

Twenty-six women, most of them with advanced endometriosis (Stage III according to Acosta), were treated for six months with the LH-RH agonist Buserelin. After initially increased liberation both of the gonadotropins as well as of the sexual steroids there was consecutive inhibition of gonadal function, especially after inhibition of FSH secretion. Within two to four weeks estradiol production was completely and lastingly suppressed in 21 of the 26 women.

[Daily variations in pregnancy hormones].

In a prospective study estriol, estradiol, progesterone, human placental lactogen (HPL) prolactin and SP1 (a placental glycoprotein specific for pregnancy), were performed in the second half of uncomplicated pregnancies in order to answer the question if there exist a circadian rhythm of these hormones in serum. All serum concentrations were measured by radioimmunoassay at 8.00, 10.

Pharmacokinetics and biotransformation of estradiol valerate in ovariectomized women.

Estradiol valerate is well suited for treatment of the characteristic symptoms accompanying menopause in women. The pharmacokinetics and biotransformation of estradiol valerate were studied in women following intravenous, intramuscular and oral administration. Intravenously given, estradiol valerate is split by enzymatic hydrolysis into 17 beta-estradiol and the fatty acid.

Sustained gonadal suppression in fertile women with the LHRH agonist buserelin.

Nine fertile women were treated with the luteinizing- hormone-releasing hormone agonist buserelin (seven women received 800 micrograms, two women 1200 micrograms intranasally for up to 24 weeks). Both doses produced sustained suppression of ovarian function, accompanied by hot flushes. In five women chemical castration was established within 1 to 5 weeks, whereas in the other four volunteers transient peaks of serum oestradiol occurred between the 6th and 19th weeks.

[1st clinical results of the treatment of locally advanced prostatic cancer with a powerful LH-RH analog: buserelin acetate].

From a series of 39 patients presenting with a locally advanced cancer of the prostate (Stage C), 26 were treated with an LH-RH analogue, Buserelin, for a period ranging between 7 and 22 months. After an initial period of subcutaneous injections, the treatment was administered by intranasal spray (400 mcg three times a day). This resulted in levels of testosterone similar to those of castrated men.

Treatment of prostatic cancer with LH-RH analogues.

Twenty-one of 32 patients with locally advanced prostatic cancer (stage C) were treated with the LH-RH analogue Buserelin for 7-19 months. After an initial sequence of subcutaneous injections, treatment was continued with intranasal spray application (three daily doses of 400 micrograms each) which ensured maintenance of serum testosterone within the range seen in castrated men. To evaluate the response of the primary tumor to Buserelin, cytological regression was established for all patients by fine-needle aspiration biopsy every 3 months.

Effect of metoclopramide and lisuride on hypophyseal and gonadal function in men.

The effects of chronic treatment over 7 weeks with metoclopramide and lisuride alone as well as the combination of both drugs were studied on basal and TRH/LHRH stimulated serum PRL, testosterone, LH, FSH, GH, and TSH concentrations. The study was conducted under double-blind placebo-controlled conditions and included twenty-four healthy male volunteers. In addition, repeated seminal fluid analyses were performed before, during and after treatment.

Sustained suppression of testosterone production by the luteinising-hormone releasing-hormone agonist buserelin in patients with advanced prostate carcinoma. A new therapeutic approach?

Nine patients with advanced carcinoma of the prostate were treated with the luteinising-hormone-releasing-hormone agonist buserelin (2 mg/day subcutaneously for 3 days then 0.4-1.2 mg/day intranasally for up to 24 weeks).

[The influence of long-term medication with the LH-RH analogue buserelin on the regulation of the menstrual cycle (author's transl)].

We investigated in 70 women over a period of 6 months the influence of different dose regimen of the potent LH-RH analogue Buserelin (HOE 766: 400, 200, 100 micrograms per day) on pituitary and ovarian function. The histological findings of the endometrial biopsy specimen (n = 109) were correlated with the hormonal profiles and the bleeding pattern. There was an evident dose-related inhibition of ovulation or corpus luteum integrity.

Influence of the LH-RH analogue buserelin on cyclic ovarian function and on endometrium. A new approach to fertility control?

The long-acting stimulatory luteinizing hormone - releasing hormone analogue D-Ser(TBU)6-EA10-LH-RH (buserelin) was administered intranasally once daily in a dose of 400 mcg to 24 normally ovulating women and to 4 women with pre-existing endocrine dysregulation. Ovulation was inhibited in 136 out of 156 treatment months. In 20 treatment months, progesterone values temporarily increased indicating luteinization of follicles or ovulation with defective corpus luteum function.

Cyproterone acetate, testosterone, LH, FSH, and prolactin levels in plasma after intramuscular application of cyproterone acetate in patients with prostatic cancer.

Five patients with prostatic carcinoma (stages T3N0M0) were injected intramuscularly with 300 mg of cyproterone acetate (CPA) (Androcur-Depot) at weekly intervals. The concentrations of CPA, testosterone, LH, FSH, and prolactin in plasma after the first, third, and fifth injection were measured by specific radioimmunoassays. After five injections of Androcur-Depot, CPA levels were slightly higher than in previous determinations, suggesting that a balance between active substance release from the depot and excretion could be achieved after eight to twelve injections, with only slightly higher levels of active substance attained.

Induction of abortion with sulprostone, a uteroselective prostaglandin E2 derivative: intramuscular route of application.

Sulprostone, a new prostaglandin E2-derivative, with high selectivity for the uterine muscle, was tested in 180 women (62 primigravidae) for induction of abortion in the first trimester of pregnancy by intramuscular administration. Total dosages from 500 to 1,500 mcg in single injections of 500 mcg were tested. The injections were given at intervals of 4 to 8 hours.

[The diagnosis of androgen producing tumours in women (author's transl)].

The problems of the diagnosis of an androgen producing tumour are described within the review of a case of a 37 year old woman with marked virilization. Functional endocrine tests, laparoscopy, retroperitoneal pneumography and angiography did not estabion of the ovarian and adrena veins established the pre-operative diagnostic of an androgen producing tumor of the left ovary. This permitted to limit the operative procedure to the minimum procedure necessary.

[Measurement of urethral closure pressure profiles with stress performed by CO2-infusion in stressincontinent women: sources of error in methodology and modes of clinical application (author's transl)].

The measurement of urethral closure pressure with stress is limited by the compressibility of gasiform mediums, which causes damping of intraurethral pressure spikes. In this study damping could be reduced by alterations of the catheter and the connecting tubes of an aircystometer. With this modified technique 55 incontinent women were examined.

[Sulprostone, a new prostaglandin E2 derivative (author's transl)].

Sulprostone, a new synthetic prostaglandin E2 derivative, was used for interruption of pregnancy in 479 patients with different lengths of pregnancy. Systemic forms of administration (i.v.