Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Estradiol valerate 2mg/dienogest 2mg is an oral estrogen/ progestogen formulation that has been approved throughout the European Union for the treatment of climacteric symptoms in postmenopausal women. Dienogest is a progestogen that combines the properties of both progesterone and 19-nortestosterone derivatives. It has moderate affinity for the progesterone receptor, significant antiproliferative and antiandrogenic activity, and produces secretory transformation of the endometrium. Estradiol valerate is an esterified form of natural 17beta-estradiol, the most potent endogenous human ovarian estrogen, and is hydrolysed to estradiol soon after oral administration. Results from a randomised, double-blind, multicentre trial showed that oral estradiol valerate 2mg/dienogest 2mg and estradiol valerate 2mg/dienogest 3mg once daily for 1 year were each as effective as estradiol 2mg/estriol 1mg/norethisterone acetate 1mg in the treatment of climacteric symptoms in 581 postmenopausal women; reductions from baseline in Kupperman Index scores were 78.5, 74.5 and 75.0%, respectively. The number of days without any type of bleeding was lowest in patients treated with estradiol valerate 2mg/dienogest 2mg (8.7 days), and highest in the estradiol valerate 2mg/ dienogest 3mg group (12.1 days). During the twelfth month of treatment with estradiol valerate 2mg/dienogest 2mg, the percentage of patients who reported bleeding was 14.5%. Endometrial biopsy results were similar in patients treated with estradiol valerate 2mg/dienogest 2mg, estradiol valerate 2mg/dienogest 3mg or estradiol 2mg/estriol 1mg/norethisterone acetate 1mg once daily for 1 year; 90.8, 87.4 and 87.5% of samples, respectively, contained atrophic material. Proliferative material was found in 4.2, 2.5 and 4.4% of the biopsies, respectively; there was no incidence of hyperplasia in any of the treatment groups. A noncomparative multicentre study in 1501 postmenopausal women demonstrated that adverse events associated with estradiol valerate 2mg/dienogest 2mg once daily for 48 weeks included breakthrough bleeding, mastalgia, headache, abdominal pain, hypertension, thrush, migraine, weight gain, increase in endometrial thickness and metrorrhagia.
 ...
PMID:Estradiol valerate/dienogest. 1182 62

The low-dose combined oral contraceptive of ethinylestradiol 30 microg and dienogest 2 mg was launched in Germany in 1995, and is now the most commonly prescribed oral contraceptive in this country. Dienogest is a novel 19-nortestosterone-derived progestin with a unique pharmacokinetic and pharmacological profile, including antiandrogenic properties. Clinical studies have demonstrated that ethinylestradiol/dienogest is a reliable ovulation inhibitor with high contraceptive efficacy that is comparable with other combined oral contraceptives. It also provides effective cycle control, with reduced intensity and duration of menstrual bleeding, and improves dysmenorrhoea. The combination of ethinylestradiol and dienogest reduces serum androgen levels, and increases the levels of thyroid hormones; however, although thyroid hormone levels increase, there is no increased activity due to increases in transporter protein. Like other low-dose oral contraceptives, ethinylestradiol/dienogest has only minor influences on lipid and carbohydrate metabolism, adrenal hormones and blood pressure parameters, and appears to have a balanced effect on the haemostatic system. Ethinylestradiol/dienogest also has beneficial effects on hair and skin; a number of studies have reported decreased hair and skin greasiness, and improvements in acne vulgaris following treatment with ethinylestradiol/dienogest. After discontinuation of ethinylestradiol/dienogest, there may be a small delay in conception during the first three cycles, but there is no subsequent impairment of fertility. Furthermore, the duration of use of ethinylestradiol/dienogest does not seem to influence the rate of conception or time to conception. Ethinylestradiol/dienogest is well tolerated; adverse reactions associated with treatment include breast pain, headache and nausea/vomiting. These adverse reactions are rare and decrease in incidence over time.
 ...
PMID:Ethinylestradiol/dienogest in oral contraception. 2039 55