Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0027497 (
nausea
)
23,468
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
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
Ethinyl estradiol
(EE), at a dosage of 5 mg/day for 5 consecutive days (5 mg EE) has generally been used for interception. A combination of 200 mcg EE and 2 mg dl--norgestrel (EE+NG) was porposed as an effective alternative. Efficacy and tolerance of these methods were compared in a randomized, double-blind study. A group of 465 women was studied with a follow-up rate of 94.3%. In the 5 mg EE group, a pregnancy rate of 0.9% was observed, and in the EE+NG group, a rate of 0.4% was found. These rates differ significantly from the expected rates (P0.0005, in both series).
Nausea
was noted in 59.1% of the 5 mg EE group in and 54.0% of the EE+NG group. Nausea and vomiting occurred in 20.8% and 15.8% respectively. The efficacy of both methods as alternative to morning-after medication was confirmed. The new method is preferable since treatment is limited to only 1 day.
...
PMID:A comparison of high-dose estrogens versus low-dose ethinylestradiol and norgestrel combination in postcoital interception: a study in 493 women. 388 Dec 94
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
Five study centers enrolled 1,311 women seeking postcoital contraception methods.
Ethinyl estradiol
was administered at 5 mg/day and conjugated estrogens at 30 mg/day for five consecutive days starting within 72 hours of unprotected coitus. Eleven pregnancies occurred in the 976 women who had a single unprotected coitus at midcycle. Based on published information, 69 pregnancies would have been expected if no contraceptives were used. Although both treatments were effective in preventing pregnancy, ethinyl estradiol seemed to be more effective. At the two centers alternately prescribing both drugs, none of 137 women treated with ethinyl estradiol became pregnant, while six of the 132 given conjugated estrogens became pregnant. Women whose treatment commenced on the first postcoital day seemed to have lower pregnancy rates than those whose medication was delayed to the second or third postcoital day regardless of which drug was used. Side effects were mainly limited to
nausea
that occurred in 70% and vomiting that was experienced by 33% of all women treated.
...
PMID:Ethinyl estradiol and conjugated estrogens as postcoital contraceptives. 625 Dec 88
Low dose estrogen tablets, containing less than 50 mcg of ethinyl estradiol, were formulated because of the recognized dose response relationship with the steroid content of the tablet and side effects. These new oral contraceptives (OCs) are as effective as the older high-dose OCs, and available evidence reports fewer side effects. This discussion reviews pharmacology of these new OCs, the mechanism of action, contraindications, side effects, and problems with the low-dose estrogen OC.
Ethinyl estradiol
is the only estrogen used in the low-dose combination OC. There are several synthetic progestins: norethindrone, norethindrone acetate, norgestrel, levonorgestrel, and ethynodiol diacetate. These progestins have different potencies so the pharmacologic activity cannot be accurately predicted based on the amount present in the tablet. The synthetic steroids in OCs are absorbed in the small intestine, metabolized in the liver, excreted in the bile and feces with a half-life of 24 hours. The low-dose estrogen combination preparation is taken 3 out of every 4 weeks. Its contraceptive effect is primarily a result of hypothalamic mediated gonadotropin suppression with subsequent inhibition of ovulation. Contraindications to taking the low-dose OC are the same as for the higher dose OC: thromboembolic or cardiovascular disease, estrogen dependent neoplasia, markedly impaired liver function, undiagnosed genital bleeding, congenital hyperlipidemia, pregnancy, and women over age 30 who smoke. Relative contraindications include hypertension, diabetes mellitus, migraine headaches, uterine myomas, and epilepsy. The often quoted 2-5-fold increased incidence of thromboembolic disease, myocardial infarction, and stroke is based on large epidemiologic studies involving patients taking the older higher dose OCs. Current data from patients taking the newer low-dose medication demonstrate minimal if any increased incidence of these problems in young women who do not smoke. The low-dose estrogen OCs have minimal effect on lipid levels. Early reports of patients using the low-dose OC have shown little if any increased incidence of hypertension. The low-dose contraceptives have little effect on glucose tolerance, and there is no evidence to show an increased incidence of overt diabetes in OC users. There is no evidence that use of the combination OC causes an increase in cancer of the cervix, uterus, or ovaries. Clinical complaints of
nausea
, breast discomfort, chloasma, weight changes, and depression are reduced with the low-dose estrogen preparation. Hypomenorrhea while taking the OC occasionally occurs because the lower dose of estrogen is insufficient to stimulate the endometrial growth in face of the predominant progestin-atrophy effect.
...
PMID:Oral contraceptives in 1984. 649 Mar 38
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