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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A phase I study of NK 622 (toremifene citrate), a novel antiestrogen, was conducted in female patients with cancer. Patients received a single oral dosing or daily once oral dosing for five consecutive days. Any adverse effects were not experienced in the single dosing of 40 or 60 mg of NK 622. In the daily administration of 10, 20, 40, 60, 120, 240 and 480 mg/day, one of three patients who received 20 mg/day experienced grade 1 anorexia, three of four patients received 240 mg/day experienced adverse effects: Grade 1 leukopenia in one patient, Grade 1 general hot flush in one patient, and Grade 1 nausea, hot flush in the face and vertigo, Grade 2 anorexia, fatigue, dull headache and general hot flush in another one patient. These symptoms recovered to normal levels after treatment. Serum hormone levels were examined in postmenopausal patients, and a significant increase of the sex hormone binding globulin level was observed in the patients received 120 and 240 mg/day doses. Serum levels of NK 622 determined as free base (TOR) reached the peak levels in 2 to 4 hours after administration on the 1st and 5th day in daily treatment, while a metabolite N-demethyltoremifene (TOR-1) reached the peak level in 4 to 170 hours. Maximum serum levels and area under the concentration versus time curves of TOR and TOR-1 increased dose-dependently. These values also increased by repetition of the treatment. Half-lives of TOR and TOR-1 in serum ranged in 74.5 to 148.9 hours and 154.1 to 653.1 hours, respectively. From these results, it was concluded that safety and efficacy of NK 622 should be assessed by using 240 mg or less doses in clinical phase II studies where breast cancer patients received long term treatment with NK 622.
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PMID:[Phase I study of NK 622 (toremifene citrate)]. 146 43

A comparison of the triphasic Triphasil and the combined oral contraceptive Diane 50 for treatment of acne for 6 cycles showed significant improvement in both groups. Triphasil (Wyeth-Ayerst) contains 50 mcg levonorgestrel and 30 mcg ethinyl estradiol, 75 mcg levonorgestrel and 40 mcg ethinyl estradiol for 5 days and 125 mcg levonorgestrel and 30 mcg ethinyl estradiol for 10 days. Diane 50 (Schering Ag) contains 2 mg cyproterone acetate and 50 mcg ethinyl estradiol for 21 days per cycle. 10 women in each group had physical, pelvic, ophthalmologic and neurologic exams, hematologic and biochemical screens, assays of free testosterone, sex hormone binding globulin (SHBG), androstenedione, dehydroepiandrosterone SO4 (DHEAS), progesterone, and computations of acne and hirsutism scores. Subjects had used tetracyclines, isotretinoin, erythromycin, topical clindamycin and benzoyl peroxide previously, but were withdrawn from medication in the cycle before the intervention. The mean acne scores, derived from grading and counting lesions and comedones, fell from 63.3 to 6 in the Diane 50 and from 64.2 to 4.5 in the Triphasil group. Subjective results were excellent for 6, good for 2 and unsatisfactory for 2 in the Diane 50 group, and excellent for 8 and good for 2 in the Triphasil group. In both groups mean free testosterone, androgen index, androstenedione and DHEAS, and an increase in SHBG were documented. 5 Triphasil and 5 Diane 50 subjects had increased cholesterol levels during the trial, the only abnormality detected. Side effects reported were recurrence of varicose veins and hemorrhoids in 1 women who withdrew, and complaints of mastalgia, nausea, dysmenorrhea, migraine, headache, backache and vaginal discharge.
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PMID:An open study of Triphasil and Diane 50 in the treatment of acne. 183 45

The effects of ketoconazole, a synthetic imidazole derivate, were evaluated in 42 women affected by acne (17 cases) and/or hirsutism (36 cases) treated with 400 mg/day for 3-6 months. Androstenedione, total and free testosterone, 5 alpha dihydrotestosterone and dehydroepiandrosterone levels progressively dropped during treatment while 17 alpha hydroxyprogesterone, estradiol, ACTH, cortisol, LH and FSH levels increased. Dehydroepiandrosterone sulfate decreased only towards the end of treatment, while estrone, sex hormone binding globulin, and PRL remained unchanged. Daily mean +/- SD rate of hair growth, measured by a special image analysis processor, decreased within 3 months of therapy from 0.258 +/- 0.058 to 0.184 +/- 0.039 mm/day (P less than 0.02) and mean +/- SD hair diameter from 0.123 +/- 0.015 to 0.110 +/- 0.013 mm (P less than 0.05) together with decreasing hormone levels. The therapeutic effects of ketoconazole on hirsutism was evident at 6 months in only 14 subjects, while no significant change in hirsutism score was recorded in 22 women who failed to complete the therapy. Acne improved in all cases. Several side effects and complications arose during treatment, such as headache, nausea, loss of scalp hair, hepatitis, and biochemical changes. Even though ketoconazole improves hyperandrogenism, only selected patients are eligible for treatment as scrupulous monitoring is required.
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PMID:Ketoconazole therapy for women with acne and/or hirsutism. 216 69

Serum testosterone, dihydrotestosterone, delta 4-androstendione and 17 beta-estradiol, sex hormone binding globulin (SHBG) and gonadotropic response to luteinizing hormone releasing hormone (LHRH) were studied in 34 male subjects with episodic or chronic cluster headache (CH). The sex steroid free fractions and those bound to SHBG and albumin were determined by a simulatory computerized method based on the mass action law. Individual steroid values were dispersed over a wide range in CH patients. Total, free and carrier protein-bound testosterone levels were significantly diminished only in chronic CH, where luteinizing hormone (LH) peak values after intravenous administration of LHRH were also decreased. Basal and peak follicle stimulating hormone (FSH) levels were significantly increased in episodic and in chronic CH groups, in comparison to healthy controls.
Cephalalgia 1989 Jun
PMID:Cluster headache in the male: sex steroid pattern and gonadotropic response to luteinizing hormone releasing hormone. 266 74

28 patients with polycystic ovary syndrome were treated for 12 months with the new preparation SH B 209 AE, consisting of 0.035 mg of ethinyl estradiol and 2 mg of cyproterone acetate. This was the first clinical trial of estroprogestational therapy on a homogeneous sample of women with polycystic ovary syndrome. Endocrine findings indicated a significant decrease in all hormonal parameters, the invariableness of prolactinemia, a considerable increase in sex hormone binding globulin (SHBG) at the 6th treatment cycle examination, a continuous significant decrease in 17 beta E2 and androstenedione from the 6th to the 12th treatment cycles. In terms of clinical findings, there was a significant decline in the severity of acne, seborrhea, and hirsutism during drug administration. The menstrual cycle in the 28 study subjects remained under control during treatment, and there were no pregnancies. Side effects such as weight gain, nausea, headache, and changes in libido were not reported. Overall, the findings of this study suggest that administration of the new monophasic contraceptive association SH B 209 AE can normalize endocrine patterns in polycystic ovary syndrome and improve its androgenic symptomatology. The low content of estrogen, the changes in clinical and hormonal parameters, the low incidence of side effects, and the good control of the menstrual cycle provided by this treatment make SH B 209 AE deserving of more widespread application.
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PMID:A new association of ethinylestradiol (0.035 mg) cyproterone acetate (2 mg) in the therapy of polycystic ovary syndrome. 294 60

8 women, aged 17-25, with polycystic ovary syndrome (PCO) were treated with Practil 21 (Organon) containing 30 mcg of ethinyl estradiol and 150 mcg of desogestrel, or with Planum (Menarini). Checkups were conducted 3 and 6 months later to measure hormone levels. The average level of testosterone dropped significantly from 121.5 (+ or - 50.9) ng/dl to 23.1 (+ or - 10.6) ng/dl after 3 months. The level of androstenedione also decreased significantly from 265.2 (+ or - 101.4) ng.dl to 96.7 (+ or - 22.5) ng/dl. Similarly, the level of 17-hydroxyprogesterone declined from 120.5 (+ or - 69.8) ng/dl to 24.5 (+ or - 10.7) ng/dl . On the other hand, the level of sex hormone binding globulin rose from 1.3 (+ or - .6) mcg/100 ml to 3.9 (+ or - 1.8) mcg/100 ml. Cortisone level increased significantly from 15 (+ or - 3.2) mcg/100 ml to 30.6 (+ or - 10.4) mcg/100 ml after 3 months, but the normal range (5-20 mcg/100 ml) was attained at the end. Ecographic evaluation of the size of the ovaries indicated a 18.2-66.5% reduction after 3 months. In 3 cases, the number and dimension of follicles also diminished conspicuously. Acne, hirsutism, and other symptoms of hyperandrogenism also declined. Side effects were minor and included slight weight gain, spotting and headache; treatment was suspended in only 1 case because of a grand mal seizure. The administration of this new monophasic OC proved to be a valid alternative therapy for PCO.
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PMID:[Changes in plasma levels of androgens and SHBG in patients with polycystic ovary syndrome (PCOs) treated with oral contraceptives containing desogestrel]. 297 29

A trial of a triphasic oral contraceptive in 13 women with polycystic- ovary syndrome is presented, backed up with data on levels of sex hormone binding globulin (SHBG), testosterone, androstenedione, 17-OH-progesterone and other hormones. This illness is really a hyperandrogenic response of the ovary secondary to high gonadotropin levels and unopposed estrogens with low SHBG. Only mediocre results have been reported with low-dose oral contraceptive treatment, compared to earlier high-dose pills. The pills used here contained 50 mcg levonorgestrel (LNG) with 30 mcg ethinyl estradiol (EE) for 6 days, 75 mcg LNG and 40 mcg EE for 5 days, and 125 mcg LNG with 30 mcg EE for 10 days. After 3 months of treatment LH levels fell from 29.7 to 3.6 mIU/m1; FSH fell from 12.3 to 2.6 mIU/m1, and the LH/FSH ratio decreased from 2.34 to 1.38. All androgens declined significantly (p0.01), into the normal range. Serum cortisol rose significantly from 16.9-36.7 mcg/100 ml. SHBG rose from 1.67-3.0 mcg/100 ml, the high limit of normal. Hirsutism and acne improved in all but 1 patient. 1 woman dropped out because of weight gain, and another because of nausea and headache. These results suggest that triphasic oral contraceptives may be safe and effective for chronic anovulatory syndrome.
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PMID:SHBG, testosterone, androstenedione, 17-OH-Progesterone plasma levels in PCO affected women treated with a triphasic oral contraceptive. 345 1

New progestin molecules have been synthesized for the purpose of maintaining the antiovulatory and antiestrogenic effects of existing progestins while suppressing their undesirable androgenic effects. Desogestrel, gestodene, and norgestimate are 3 third generation progestins now available in Europe in combined oral contraceptives (OCs) containing ethinyl estradiol. The 3 gonane molecules all result from modifications in the structure of levonorgestrel which neutralize its androgenic activity. The 3 molecules maintain their affinity for the androgen receptors. A review of the literature suggests that the third generation OCs have no major disadvantages compared to other low dose preparations now being marketed. Among the fundamental differences between levonorgestrel and the 3 new gonanes, the absence of the androgenic effect reveals the predominant estrogenic effect on HDL cholesterol and sex hormone binding globulin (SHBG). It appears however that the absence of androgenic effect does not affect the antiestrogenic power of the molecule at the level of the target cells such as the endometrium, or at the level of the pituitary cells. As with all low-dose formulations, a nonnegligible percentage of patients conserves ovarian activity with follicular maturation and estrogen secretion. It remains to be demonstrated whether the 2-10% of users reporting undesirable effects such as breast tenderness, swelling, headaches, and irritability are those in whom ovarian activity is not completely suppressed. The percentage of women using the third generation gonanes who conserve ovarian activity seems to be lower than that of users of the older low-dose formulations. Carbohydrate tolerance differs little from that observed with levonorgestrel. Modifications of coagulation factors reflect the estrogen content and do not differ in the third generation gonanes and older low-dose formulations. It is difficult to identify major clinical advantages of any 1 of the new preparations because of the minor differences between them. Prospective, longterm epidemiologic studies will be needed to confirm possible cardiovascular benefits and the absence of increased mammary pathology.
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PMID:[Disadvantages of third generation progestins]. 1231 28

Oral contraceptives have been available for a little over 40 years and, during that time, many different formulations have been introduced. There have been dramatic dosage reductions of both the estrogen and progestogen components and various progestogens have been introduced over time. The properties of most progestogens used in oral contraceptives are very similar, differing mainly in potency. Oral contraceptives with progestogens having new and unique properties are needed. World-wide, around 20-30% of women of childbearing age use oral contraceptives and their use declines after the age of 35 years, with an accompanying increase in the rates of unintended pregnancy and elective termination. Incorrect use likewise gives rise to high unintended pregnancy rates. Use in Europe is higher than in other regions. Discontinuation because of unwanted effects and misperceptions is very common. Common misperceptions that prevent women from initiating oral contraceptive use are weight gain, cancer risks and that bleeding indicates a significant problem. Unwanted effects that commonly give rise to discontinuation are bleeding, nausea, weight gain, mood changes, breast tenderness and headaches. Discontinuation rates are high, particularly in the first year, and adolescents have the highest rates of discontinuation. Correct consistent use must be encouraged by taking pills at a regular time each day and by reinforcing that bleeding and other unwanted effects are not medically serious. Reinforcement of the non-contraceptive health benefits is very important and it needs to be emphasized that long-term use enhances these non-contraceptive benefits. Most non-contraceptive benefits are due to the progestogen component and its inhibition of ovulation. The new drospirenone-containing oral contraceptive (Yasmin, Schering AG, Berlin, Germany) offers the traditional non-contraceptive benefits; however, due to its unique antimineralocorticoid and antiandrogenic properties, new and unique benefits have been observed. Acne is well controlled, as would be expected from its inhibition of ovulation, antiandrogenic activity and lack of attenuation of the estrogen-mediated increase in sex hormone binding globulin. Its antimineralocorticoid activity gives rise to a reduction in fluid-related symptoms. The oral contraceptive containing 3 mg drospirenone with 30 microg ethinylestradiol DRSP/EE) has excellent efficacy since drospirenone is a potent progestogen, the corrected Pearl index being 0.09. This index is lower than those of many other oral contraceptives. Cycle control is excellent and comparable to that experienced with other oral contraceptives. A significant and consistent weight loss was seen with DRSP/EE compared to a reference preparation containing desogestrel. Day-to-day compliance and the duration of intake of an oral contraceptive are dependent on the woman's satisfaction with the pill she is taking. DRSP/EE meets these expectations and, with its new and unique non-contraceptive benefits, offers a real new choice to women.
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PMID:Yasmin: the reason why. 1265 2

A 69-year-old man was referred for elevated thyroid hormone levels. He had no symptoms apart from mild hyperhidrosis and heat intolerance with occasional headaches. Past medical history included a right hemithyroidectomy for a multinodular goiter and Hashimoto's disease. At presentation the patient had a firm, slightly enlarged left thyroid lobe. There were no visual abnormalities, and the rest of the physical findings were unremarkable. Laboratory findings included elevated values of free T4, free T3, total T3, thyrotropin-secreting hormone (TSH), antithyroglobulin, and antimicrosomal antibodies. Normal values were found for cortisol, prolactin, testosterone, follicle-stimulating hormone, luteinizing hormone, alpha-subunit, and thyroid-stimulating immunoglobulin. Thyroid 123I scan showed an increased 5-hour uptake of 23% and a 24-hour uptake of 53% with a diffuse uniform enlargement of the left side. TSH level did not increase after a thyrotropin-releasing hormone stimulation test. Serum sex hormone binding globulin was elevated. Magnetic resonance imaging of the pituitary revealed a pituitary macroadenoma with suprasellar extension to the optic chiasm. Histologic examination of the adenoma after transsphenoidal hypophysectomy showed cells that stained positive for TSH. TSH-secreting pituitary adenomas account for 1% of functioning pituitary tumors and are an exceedingly rare cause of hyperthyroidism. To our knowledge, this is the first report of pituitary tumor inducing hyperthyroidism in the setting of Hashimoto's disease. There is a possibility that TSH elevation related to Hashimoto's disease might have contributed to the development of a TSH-secreting pituitary adenoma.
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PMID:Thyrotropin-secreting pituitary tumor and Hashimoto's disease: a novel association. 1451 96


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