Gene/Protein
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Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
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Drug
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Target Concepts:
Gene/Protein
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Enzyme
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Query: UMLS:C0018681 (
headache
)
56,091
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
History of development, composition, effectiveness, and side effects of first and second generation steroid contraceptive agents are briefly reviewed with special emphasis on advantages of third generation contraceptives, including triphasic hormonal contraceptives. Mechanism of action of triphasic contraceptives is based on the physiological biorhythm in the formation, secretion and blood levels of estrogens and gestagens during the menstrual cycle. The first phase (5 to 7 tablets) is characterized by high levels of estrogens and relatively low levels of gestagens. The second phase (5 to 10 tablets) is characterized by relatively high levels of estrogens and gestagens. And the third phase (7 to 10 tablets) is characterized by decreased levels of estrogens and significantly increased levels of gestagens. The most commonly used gestagens are levonorgestrel, norethindrone, and norethisterone.
Ethinyl estradiol
is the most commonly used estrogen. During various phases of the cycle the dosage of gestagens ranges from 0.03 to 1.00 mg and dosage of estrogen ranges from 0.3 to 0.4 mg. A single package of triphasic contraceptives contains 21 tablets. Duration of a cycle is 23-25 days with 7-day interval between the cycles. Hemorrhage during the first half of the cycle can be successfully treated with additional estrogens, while hemorrhage during the second half can be treated with gestagens. Side-effects of triphasic contraceptives include
headache
, dizziness, and irregular menstrual cycle. Triphasic contraceptives are specifically indicated to women older than 35 years of age, to smoking women, and to women with changes in lipid metabolism.
...
PMID:[Triphasic hormonal contraceptives]. 267 94
At this time 3 triphasics are widely used in the US: Ortho-Novum 7/7/7, Tri-Norinyl, and Triphasil.
Ethinyl estradiol
is the preferred estrogenic agent for the triphasic products. Torethindrone and levonorgestrel were chosen as the progestins for the triphasic products. It is the combined effects of estrogen and progestin in the triphasics that provide their contraceptive action. Triphasil increases both the estrogen and the progestin at midcycle; Tri-Norinyl and Ortho-Novum 7/7/7 elevate the progestin only. The midcycle surges of estrogen and luteinizing hormone are dampened, and ovulation is inhibited. The triphasics represent a 98.7% reduction in total steroid content since oral contraceptives (OCs) were introduced. An estrogen dose of 30-50 mcg will inhibit ovulation, and side effects with such a dose are considered tolerable. The triphasic OCs are in this range. An estrogen dose of 20 mcg has been tested but is slightly less effective and is not recommended. Contraceptive failures have occurred with the triphasic products. In 1486 women studied, 6 pregnancies have occurred. Of these failures, one may have been because of a drug interaction with a barbituate. 1 pregnancy was due to patient failure; 3 consecutive pills were missed. Only 2 pregnancies were certain drug failures. Because of the gentle suppression of ovarian function, it has been observed that the menstrual flow is less affected than by standard OCs. Due to the fact that less total steroid is delivered and more endometrial shedding occurs, it is hoped that the triphasic preparations will have less of a "lingering" effect on the return to functional fertility. Most of the published data on side effects is available from the UK, North America, and Europe on the formulation known in the US as Triphasil. Nausea, vomiting, breakthrough bleeding, weight gain, and breast tenderness appear to be the most common side effects. The major medical reasons for triphasic discontinuation include breast tenderness, weight gain, breakthrough bleeding, nausea and vomiting,
headache
, and increased bleeding during the 1 week of withdrawal. Rifampin and phenobarbital are examples of drugs found to decrease pill efficiency, including triphasics. Also, a triphasic may interfere with the action of another drug. The new triphasics are appropriate when starting new patients on OCs. Patient counseling is essential. Due to the low margin of error as a consequence of lesser suppression of ovarian function, the patient needs to be well instructed in how to take the pill and advised of the consequences of missed tables.
...
PMID:The triphasics: insights for effective clinical use. 382 67
203 women 19-40 years of age were administered the gestagen preparations
Volidan
, Cyclofarlutal, Ovulen, Ciba AC-101, and Stediril as a contraceptive. 49 other women were administered these preparations as therapeutic and/or diagnostic measures in different gynecological complications. Side effects such as spotting, acylic bleeding, nausea,
headaches
and breast swelling were more frequent with the high-dose preparations such as
Volidan
and Cyclofarlutal. Intolerance to the preparation and subsequent discontinuation occurred only in a small percentage of the users. All of the preparations achieved 100% effectiveness as contraceptives. It is noted that these preparations were used with some success in treating dysmenorrhea, menometrorrhagia because of hyperplasia of the endometrium, and in severe climacteric syndromes. It has also been used as a pregnancy test. Constant medical control of the administration of these preparations is necessary both when they are used as contraceptives and as therapeutic measures, particularly in the case of young women.
...
PMID:[Clinical aspects of the administration of gestagen preparations (Volidan, Cyclofarlutal, Ovulen, Ciba AC-101 and Steridil)]. 545 44
The sequential method of contraception with megestrol acetate with ethinyl estradiol was offered to 61 women for 549 cycles in this study. No pregnancies occurred. Flow was less in 7 women and greater in 3; duration of flow was longer in 5 women and shorter in 3. There were 2 instances of breakthrough bleeding. Persistant postnatal amenorrhea occurred in 1 woman and menorrhagia in another. Random endometrial biopsies showed proliferative activity in the majority of cases. Side effects observed were: nausea, vomiting, giddiness, leucorrhea,
headache
, weakness and abdominal pain. Most of these symptoms occurred in the first 2 cycles. 29 women dropped out after the first year, and 8 of these women conceived.
Ethinyl estradiol
was used in .1mg dose, megestrol acetate in 1 mg.
...
PMID:Evaluation of sequential method of contraception with megestrol acetate and ethinyl oestradiol. 1215 52