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The purpose of prescribing combined oral contraceptives (OCs) is achievement of good cycle control and effective contraception with the least side effects, using an OC with the lowest possible dose of estrogen. Triphasil, Triquilar, Nordette, Microgynon 30, and Brevinor are good 1st choices because of the low estrogen dose (30-35 mcg). Women who probably cannot tolerate breakthrough bleeding and who need simple packaging should use a monophasic, more progestogenic OC, e.g., Nordette or Microgynon 30. Physicians should suggest a low dose estrogen and low dose antiandrogenic progestogen (OC) (e.g., Diane-35 ED) for women who have acne. They should advise patients that when they take OCs, their menstrual periods usually become shorter, regular, and lighter. Women need not take a break from OC usage. Vitamin C, antibiotics, griseofulvin, rifampicin, and anticonvulsants (except sodium valproate) interact with OCs. Women using warfarin and oral hypoglycemics and wanting to start using OCs need to consult their physician about changing requirements for warfarin and oral hypoglycemics. The effectiveness of OCs can be diminished by diarrhea and vomiting. Absolute contraindications to OCs include pregnancy, use during the first 2 weeks postpartum, history of thromboembolism, undiagnosed abnormal vaginal bleeding, focal migraine, coronary heart disease, steroid-dependent tumors, recent impaired liver function, and cardiovascular accidents. Some relative contraindications are older than 35 years old and smoking, breast feeding, and hypertension. This article provides a section on how to manage common side effects. For example, if the side effect is acne, the physician should prescribe an OC with increased estrogen and reduced progestogen (e.g., Triphasil/Triquilar to Biphasil/Sequilar). This article lists trade names of various OCs and their estrogen and progestogen doses, e.g., Nordette has 30 mcg ethinyl estradiol and 150 mcg levonorgestrel.
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PMID:Combined oral contraception. 147 9

Oral contraceptives (OCs, long-acting progestins (LAPs), and IUDS are reviewed in terms of new information on safety and efficacy. OC formulations are described and their mechanism of action and efficacy indicated. Reports are provided for thromboembolism, hemorrhagic and thrombotic stroke, ischemic heart diseases, alterations in lipid and hypoprotein and carbohydrate metabolism, hypertension, coagulation changes, breast and cervical cancers, and such minor side effects as menstrual irregularities, nausea, headaches, weight gain, premenstrual syndrome effects, and mood and libido changes. Noncontraceptive health benefits and clinical considerations are discussed. Norplant, as the only long acting progestin available in the US is described in terms of its formulations, mechanism of action, sequelae and metabolic effects, menstrual irregularities, metabolic effects, nuisance side effects, candidates for insertion, method of insertion and removal, and continuation rates. 2 IUD types are identified as the only ones available in the US, Progestasert T and T-Cu-380A (Paragard). Mechanism of action, efficacy, candidates, major sequelae such as salpingitis, infertility, and uterine perforation, minor sequelae such as metrorrhagia and dysmenorrhea, and other considerations are indicated. OCs in the US contain an average of 35 mg of ethinyl estradiol and assorted progestins e.g.s, ethynodiol diacetate, norethindrone acetate, nortestosterone derivatives with a complex mechanism of action. The failure rate for use effectiveness is 6 pregnancies/100 woman years. Modern formulations have combined rates of no more than 50 to 100 adverse events/100,000 users. Some of the effects are indicated as follows: Thromboembolism accounts for 60% of adverse effects and appears to be declining along with hemorrhagic and thrombotic stroke, however, modern use studies are only partially available. Myocardial infarction related to OC use may be embolic, and has a low risk at 7/100,000 users. Low-dose contraceptives substantially reduce the associated risks. Those with risk factors need close monitoring. Norplant is useful for those not wanting to take a daily regimen and is commonly accompanied by menstrual irregularity and sometimes headaches. Continuation is 80% after the 1st year and 40% after 5 years. Candidates for IUDs are parous women in monogamous relationships, who are not at risk for salpingitis, which is related to IUD use, or sexually transmitted diseases. Continuation is 70% after 1 year compared with 50% of OC users.
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PMID:Modern trends in contraception. 212 11

The effect of oral contraceptives (OCs) on changes in arterial pressure (AP) was studied in 160 healthy women, 22-35 years of age, with ovulatory menstrual cycles. They took Ovidan and Non-ovlon for 12 months to prevent unwanted pregnancy. These steroidal preparations contain equal doses (.05 mg) of ethinyl estradiol and different doses of gestagenic components: .25 mg of levonorgestrel in Ovidan and 1 mg of norethisterone acetate in Non-ovlon. Measurements of AP parameters were taken with a mercury sphygmomanometer, and complications caused by OCs were recorded. Results were processed by the usual methods of variational statistics. With Ovidan, a significant increase (p .05) in systolic and diastolic AP was recorded after 3 and 6 months. Systolic and diastolic APs exceeded the initial levels by 7 and 6 mm Hg, respectively. Non-ovlon caused a less pronounced effect; a significant increase (p .05) of systolic and diastolic AP was recorded during the 12th month of contraception only. Thus, the results indicate that OCs can cause an increase in AP, and the gestagenic component increases the risk of hypertension. Levonorgestrel causes a more marked effect than norethisterone. Periodic AP measurements (every 3 months) are recommended for women using OCs. In cases of a steady increase in AP, use of this contraceptive method should be terminated.
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PMID:[Indicators of arterial blood pressure during hormonal contraception]. 241 29

This guide to choice of oral contraceptives, for U.S. clinicians, includes a review of the available types of pills, the pharmacology of the steroids in pills, safety issues regarding thrombosis, arterial disease and hypertension related to estrogens and progestins in pills, common side effects, and therapeutic uses of orals. Choice of an oral contraceptive narrows down to which of the 5 available progestins and their formulation, since all contain ethinyl estradiol as the estrogen. While Briggs' theory espoused picking a pill with the minimal metabolic effect, recent evidence suggests that some estrogenic activity may be preferable to the unopposed progestagen, actually an anti-estrogenic receptor effect, to prevent adverse lipid and blood pressure effects in users. Current pills with low doses of estrogens probably are not significant risks for women as regards thrombosis, particularly if predisposed women and smokers are excluded. Pills containing 0.35 mg ethinyl estradiol and 0.5 mg norethindrone, based on large population trials, are probably the minimal effective dose yet even these are more effective than most other contraceptive methods. Breakthrough bleeding and spotting have been further minimized, however, with multiphasic pills. It is best to start with a 0.30-0.35 mg estrogen oral contraceptive, such as Loestrin, Demulin, Orthonovum 1.35, Orthonovum 7/7/7 or Nordette, encouraging the patient to accept early side effects for 3 months before switching to others. Disorders that can be managed with oral contraceptives include recurring and pre-existing ovarian cysts, endometriosis, dysfunctional uterine bleeding and dysmenorrhea. Brief guidelines for handling normal side effects and treatment of the above disorders are included.
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PMID:Choosing the best oral contraceptive. 274 45

2 cases reports are described of patients with renal artery stenosis who presented with hypertensive encephalopathy, normal blood pressures having been recorded within the previous 6 months while taking oral contraceptives (OCs). A 27-year-old woman, admitted to the hospital following 2 grand mal fits, had suffered from increasing headaches, nausea, and vomiting over the previous month. Her blood pressure had been elevated at 160/110 mmHg 1 week prior to admission but had been normal over previous 11 years while taking OCs (various formulations of combined estrogen and progestogen) which she had stopped taking 2 months previously. She was a nonsmoker. Her blood pressure was controlled with atenolol, nifedipine, and bendrofluazide, and her conscious level returned to normal with no further fits. An intravenous urogram revealed a small left kidney with a delayed nephrogram, and subsequent arteriography showed bilateral medial fibromuscular dysplasia with a narrow stenosis of the left renal artery. Attempted balloon angioplasty was unsuccessful due to arterial spasm. 4 months after presentation she became pregnant. Blood pressure was controlled with methyl dopa during pregnancy which progressed uneventfully to full term. In the 2nd case, a 19-year old girl became confused and suffered a grand mal convulsion. She had complained of headaches over the previous 3 days. Her blood pressure had been normal over the previous 6 months while taking Logynon (phased formulation of ethinylestradiol and levonorgestrel). She was a nonsmoker. On admission to the hospital, she suffered further generalized convulsions. Despite control of her convulsions with intravenous chlormethiazole, her blood pressure rose to 220/140 mmHg, and this was controlled with intravenous hydralazine and propranolol. The following day she was conscious and was changed to oral therapy. A renogram and DMSA scan showed normal sized kidneys, but there was evidence of decreased blood flow to the left kidney with an increased transit time. Renal arteriography showed a stenosis of the left renal artery, typical of intimal fibromuscular dysplasia, which was dilated by balloon angioplasty. Anti-hypertensive medication was withdrawn postoperatively, and her blood pressure has remained well controlled. In both of the cases the onset of hypertension was rapid with encephalopathy being the presenting feature. Hypertensive encephalopathy is well recognized as a presenting feature of renal transplant artery stenosis but not in cases of native renal artery stenosis. 1 of the patients had stopped using OCs 2 months before presentation, suggesting that although there may have been an association between OC use and the development of fibromuscular dysplasia, it could not be implicated in the mode of presentation.
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PMID:Encephalopathy in renovascular hypertension associated with the use of oral contraceptives. 311 27

This report describes the long-term follow-up of 376 women who received NORPLANT implants in the period October 1974 through May 1979. One-hundred-and-ten subjects received replacement implants after variable lengths of use of the first set. The average levonorgestrel plasma levels declined steadily through eight years of use of NORPLANT capsules (r = -.937). Values were 0.35 ng/ml, 0.29 ng/ml and 0.22 ng/ml at treatment years 1, 5 and 8, respectively. Levonorgestrel plasma levels after replacement with a second set of implants were similar to those observed after the first insertion, either when placed in the same site as the first set or in a different area. Nineteen pregnancies occurred during 18,530 woman-months of use of the first set of implants, eleven of them during years 6 through 8 of treatment. The Pearl Index for the first 5 years of NORPLANT implants use was 0.63. No pregnancy has occurred in 4194 woman-months observed during treatment with a second set of capsules. Fifty-six women (14.9%) out of 376 acceptors of the first implant and 10 (9.1%) out of 110 acceptors of the replacement implants were terminated for other medical reasons, mainly bleeding problems and side effects commonly associated with hormonal contraception. Two women died while using NORPLANT implants, one of a cardiac arrest after surgery for a gallbladder disease and one because of endocranial hypertension originating from the rupture of an aneurism of the median cerebral artery. The bleeding pattern observed in the three months after NORPLANT capsules replacement was similar to that observed in the 90 days before replacement and different from that experienced by the same women in the first 90 days of implant use. This finding can be interpreted as an indicator of adaptive changes experienced by the target organs during long-term continuous administration of levonorgestrel. The prompt recovery of fertility after removal of NORPLANT implants suggests that these changes are reversible.
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PMID:Long-term follow-up of women treated with Norplant implants. 311 90

The history of the development of oral contraceptives (OCs) has been a progressive reduction in dosage to what is now probably the lowest does that is compatible with the desired therapeutic effect -- to inhibit ovluation. Yet, controversy and argument continue. A table lists the OCs that are available in Australia. Many of these preparations, although having different trade names, have an identical composition. Since the withdrawal of sequential OCs from the Australian market, there are only 2 generic types. These are the progestogen only (mini) OCs, which consist of either 30 mcg of levonorgestrel or 350 mcg of norethisterone given at the same time every day; and the combined OCs, which contain an estrogen and a progestogen. In the last 12 months, some of the older high-dose OCs have been withdrawn, and it seems likely that further withdrawals will follow. Only 2 estrogens are used in the formulation of the OC, but there is a greater variety of progestogens. Ethinyl estradiol is used in most preparations. A small minority of OCs contain mestranol, the 3-methyl ether of ethinyl estradiol. Currently, there are only 4 OC agents that are available in Australia that contain mestranol and 2 of these contain the high doses of 100 mcg. Fundamentally, there are 2 types of progestogens -- those that contain, or are metabolized to, norethisterone and those that contain norgestrel or its close relative, desogestrel. With the exception of the norgestrel group and desogestrel, all other progestins, including norethisterone itself, are effective in vivo after they have been metablized to norethisterone. Mestranol is effective in humans after demethylation to ethinyl estradiol. In the norgesterel group, since d-norgestrel is inert endocrinologically, 250 mcg of levonorgestrel and 500 mcg of dl-norgestrel are equivalent. Levonorgestrel and desogestrel are of approximately equal potency. With the combined OC agents, the overwhelming mechanism of action is by the inhibition of the midcycle peak of luteinizing hormone (LH) secretion and, hence, the inhibition of ovulation. Progestogen-only OCs have additional actions such as effects on cervical and fallopian tube mucin. Minor side-effects include disturbance of the menstrual cycle, changes in weight, and changes in mood. Major side-effects relate to 4 areas -- subsequent reproduction, the cardiovascular system, other metabolic effects, and the risk of malignancy. A table presents the absolute contraindication contraindications. There is not the slightest doubt that a woman who is over 35, who smokes, and who, in addition, may be obese and has hypertension should not use OCs. Progestogen (mini) OCs have a slightly higher failure rate and a greater incidence of irregular bleeding than have combined OCs. The mini OC has little place in women who need effective hormonal contraception and good cycle control. The mini OC may have a place in a patient who finds other contraception unacceptable and in whom estrogens are contraindicated specifically.
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PMID:Oral contraceptive agents. 394 19

Drug companies have been at work throughout the 1960s, 1970s, and 1980s trying to reduce the steroid content of their oral contraceptives (OCs). Researchers have been successful in reducing steroid content while maintaining effectiveness, thereby making OCs safer. In the 1st half of the natural menstrual cycle, a woman secretes estrogen as the dominant steroid product. In the 2nd half, estrogen is the principal reproductive hormone. Estrogens inhibit ovulation, possibly by inhibiting implantation, altering ovum transplant, or in some way preventing corpus luteum function, which is necessary to maintain early pregnancies and the endometrium. There are still only 2 estrogens and 6 progestins on the market today. They are probably the most thoroughly studied chemical ever seen in the history of pharmacy or medicine. 1 of the estrogens, mestranol, is really a drug of the past. In the body, mestranol is converted to ethinyl estradiol, the other estrogen on the market. Consequently, there is no reason to use mestranol itself. Within the dose range of 50-100 mcg, there's little difference in contraceptive effect. Progestins are the other active ingredient in the combination OC. Their principal action is the thickening of the cervical mucus, which prevents sperm penetration. Also, with sufficient progesterone, ovulation is inhibited, but this happens in only 40% of those patients taking, for instance, the "mini-pill" (which consists of progesterone only). The progestins and the estrogens work in concert to make OCs a highly effective contraceptive method. Recent surveys conducted by the Centers for Disease Control and National Cancer Institute looked into the relative effectiveness of OCs. Nordette had a use effectiveness failure rate of 3.5; Ovral, 3.6. Loestrin 1/20 -- norethindrone acetate, 1 mg, and estinyl estradiol, 20 mcg -- shows a failure rate of 4.5. This indicates that the threshold for an effective dose of estinyl estradiol in OCs is 30 mcg. For 1 mini-pill, Ovrette, the failure rate is 9.5 -- much higher. Depo-Provera has a failure rate of 0.7. The primary complaint from women taking OCs is spotting and breakthrough bleeding during the cycle. 30-50% of women given OCs stop taking them within a year. OC side effects include nausea, fluid retention, breast tenderness, leukorrhea, hypomenorrhea, headaches, spotting around the face, hypertension, and visual changes. 1 of the risks of birth control pills may be cervical dysplasia -- changes in the cells of the cervix. The relative risk of cervical cancer with OCs after 5-9 years is approximately 1.8. Clinical cases of deep vein thrombosis number 1/1000 per year among nonusers of OCs. Among users, the rate is 3 times as high: 3/1000. The most serious potential adverse effect is myocardial infarction. Of the excess deaths attributed to OCs (23.3 total per 100,000 users), 22.7 are due to myocardial infarctions and hemorrhage. The discussion also briefly reviews other methods of contraception -- Depo-Provera, male contraceptives, implants, the diapragm, and IUDs.
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PMID:Prescription contraceptives: countering the risks. 405 Jun 70

490 women who used Stediril (.5 mg norgestrel and .05 mg ethinyl estradiol, combined) for a total of 5600 cycles or 466 woman-years over a 3 year period are presented. They all took the pills primairly for contraception; most were 20-30 years old, and took Stediril 3-6 months. Some other indications were 119 cases of menstrual irregularity, 15 of spaniomenorrhea, 14 of premenstrual syndrome and 3 of acne, all relieved. 46 of 50 cases of menorrhagia, 83 of 89 of dysmenorrhea and 32 of 34 with pelvic pain were relieved. Withdrawal bleeding was usually less than before and tended to diminish with time. There were 46 women with nausea, 3 of whom stopped Stediril. Migraines sometimes a ppeared, sometimes disappeared, but often occurred regularly on the first day between pill cycles. 52 women complained of breast congestion for the first time. Weight rose in 2301, fell in 98 and stayed constant in 134 after 3 months: weight was easily controlled with diet and appetite supressant drugs. No hypertension was observed. There were 19 single cycles of amenorrhea, several cases of persistant amenorrhea and 4 cases of amenorrhea after stopping. 2-3% of cycles were marked by metrorrhagia; 63 women had spotting, 8 had significant metrorrhagia; 7 had metrorrhagia followed by withdrawal bleeding in that cycle. 1 woman had a thromboembolism of the left leg after 2 pill cycles during which she gained 3 kg. There was 1 pregnancy due to irregular pill use.
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PMID:[Clinical study of an estro-progestative association in low doses. Experience of 3 years (490 patients-5600 cycles)]. 426 90

The oral contraceptive (OC) Stediril acts by inhibiting ovulation, rendering the endometrium inhospitable to implantation, and rendering the cervical mucus impermeable to sperm. The effectiveness of Stediril may be compromised by failure to follow the dosage schedule: 1 pill daily for 21 days followed by a pill-free interval of 7 days when withdrawal bleeding occurs. Stediril should be taken at a regular time each day. If pills are missed for more than 48 hours, efficacy cannot be guaranteed. If vomiting occurs within 4 hours of pill ingestion, the pill should be replaced. Certain drugs, such as Rifadine, may affect the action of Stediril. Stediril should only be prescribed after a complete medical history and examination, including responding to any questions the patient may have. At a 3-month follow-up visit the patient's tolerance to the drug should be assessed by absence of various symptoms: psychological problems such as nervousness and irritibality that resemble those of pregnancy; skin problems such as acne or changes of pigmentation; periods of nausea that diminish in frequency after a few weeks; weight gain; bleeding problems; or signs of thromboembolic risk, such as headaches, unusual visual disturbances, or hypertension, which require immediate cessation of OC use. Because Stediril constitutes a risk to the fetus in case of unplanned pregnancy, the preliminary gynecological examination is mandatory and the pill should only be prescribed to women able to comply with dosage requirements. The pill should be stopped 6 weeks-3 months before pregnancy to allow the endometrium to regenerate. The carcinogenic role of the pill is frequently discussed but not conclusively proven. Follow-up visits should occur 3 and 6 months after beginning use and every year thereafter.
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PMID:[Stediril]. 656 44


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