Hormonal Contraceptives part III

II.5. Estrogen-Gestagen preparations

Combination preparations (monophasic)

Dosage combination is the most widely used preparations.  g ethinylestradiol and gestagen with a certain dose. Each tablet mengadung 20-100  In the selection of different types of oral contraceptives (the pill) are the most important is to choose the type that has the least efficacy of contraceptive failure. In addition to the rapid return of fertility after use dihentikanb, other keuntukngan pill is this: to prevent an ectopic pregnancy, pelvic infection protection against the occurrence of cervical mucosa because guess who works as a barrier to bacteria, reduce period pain, reduces symptoms of premenstrual syndrome, lowers risk of ovarian cancer. (Hormonal contraception, hormonal contraception) Although I have to choose the type that has the fewest side effects, it is not a priority in the selection of the contraceptive pill.

All types of combinations have similar efficacy, but not necessarily every individual has the same comfort. Most side effects are caused by the content of estrogen in the contraceptive  g)mpill preparation is so divided into pills with low estrogen (20-35   g) and high-dose estrogen pills (50  basically choose stocks with a low dose of estrogen. The use of high doses is only justified in cases of bleeding in the use of low estrogen dose preparations.

Determine the dose of estrogen in a contraceptive pill is much easier when compared to determine the dose gestagen because almost all of gestagen has a chemical structure and metabolic processes are nearly equal. Based on the chemical structure and metabolism, the type of gestagen is in the pill is divided into 3 groups, namely nortestesteron derivatives, derivatives and estrane progesterone (13-methyl-gonane) and "gonane" (13-ethyl gonane). Which include or gestagen norethisterone estrane is that the body is converted to norethisterone (etinodiol diacetate, linestrenol, norethisterone acetate, noretister onantat, and noretinodrel). Which includes a derivative of progesterone is klormadinon acetate, cyproterone acetate, and medroxyprogesterone acetate, while the included "gonanen" is levonorgestrel, Desogestrel, norgestimat, and gestoden.

If seen so many types of gestagen are available, the question arises which type of gestagen that has a strong effect on suppression of ovulation. This question is difficult to find the answer because there is an effect on endometrial gestagen so strong, but the effects of gonadotropin suppression is not so strong even though the bond receptors in endometrium and pituitary are equally strong (100%). The difference in the work of each gestagen, although equally strong receptor binding, is still not known with certainty.

In order not to burden the body and also in order not to give too many side effects, almost all oral contraceptives available today contain low doses of estrogen and gestagen, who once thought impossible. For example, the contraceptive pill was Enovid was first produced at a dose  g ethinylestradiol and 9.85 mg noretinodre.mof 150  Arise during the use of a lot of side effects so that the pill is no longer manufactured kontrapsepsi. It turned out that the dose of estrogen and gestagen low has also been able to obtain sufficient ovulation suppression effects.

Combination preparations Terraced

In order not to use high-dose gestagen, began looking for ways to reduce the dose gestagen oral contraceptives, for example by making the type of preparation "two" or "three" levels (Figure 6). In the preparation of two levels, first level gestagen dose is much lower when compared with conventional dosage combination, which is only 0.05 mg, and at both dose levels of 0.124 mg dose of estrogen while on the multilevel system is not undergoing any change.
Two-level system to be modified again in the form of three-level system, such as Triquilar. In this system gestagen dose is increased after 6 days, 5 days and then increased again, while the dose of estrogen is never fixed, but on the  g.msecond level is raised from 30 to 40  should be emphasized here that the two-and three-level system is a combination of stocks, but not the biphasic combination.

How it Works The combination preparations

To get the type of contraceptive pill which has a high effectiveness of the most important is the extent to which the ability of these pills can suppress gonadotropin secretion and affects the functions of genetalia. In the monophasic combination preparations, estrogen and progesterone have been since the beginning of pressing gonadopropin secretion. This suppression occurs not only on the basal secretion of FSH and LH, but also to the suppression of LH preovulasi. Due to the influence of progesterone from the beginning, the implantation process will be disrupted, not physiological cervical mucus formation, and impaired tubal motility, so that transport the egg by itself would also disrupted. (Figure 7) how to work two and three storey stock equal to the workings of monophasic combination preparations.

Sequential preparations (biphasic)

Making preparations biphasic based on the notion that a woman's normal menstrual cycle is the follicular phase and a biphasic secretory phase (phase-phase estrogen and progesterone). Thus, the provision of similar cycles of sequential preparations are similar to normal menstrual cycle, because after administration of progesterone at the beginning of the menstrual cycle as in the administration of monophasic combined pill is not physiological. In terms of side effects no difference between biphasic with monophasic.

In the monophasic combination preparations, estrogen and progesterone simultaneously suppress gonadotropin secretion that is not needed dose of estrogen and progesterone are high, whereas on a sequential estrogen alone preparations which suppress gonadotropin secretion, so that in itself required a high dose of estrogen. Estrogen kdua phase serves only to cause bleeding lucut. Possibility of pregnancy in sequential use of preparations is greater when compared with use of monophasic combined pill. Because the first phase of the sequential preparation containing only progesterone, found no effect of pressure on the cervical mucus and endometrium, whereas the monophasic combination preparations from the very beginning there has been an emphasis on cervical mucus production by estrogen and progesterone. Anyway to get a good contraceptive efficacy, the dose of estrogen in sequential preparation should be high and this can cause vaginal discharge and spotting the onset of bleeding, which in turn will create discomfort for the wearer. In addition, high doses of estrogen is a risk of thromboembolism and malignancy of the endometrium. In the monophasic combination preparations as early effects of estrogen have been influenced by the gestagen, the possibility of side effects due to estrogen is much smaller. On the basis of this is ultimately the most widely used is a monophasic combination pills and sequential pills andaikatapun want to use, choose the type of gestagen component of pills containing the 15-day duration.

How it Works Sequential preparations

Suppression of gonadotropin secretion is not as strong when compared with monophasic combination preparations, because the first phase of the work only estrogen suppress gonadotropin secretion, whereas the monophasic combination preparations of estrogen and progesterone has been since the beginning of both working suppress gonadotropin secretion. Effect on cervical mucus is also not so good at sequential use of preparations, so it still can happen sperm penetration.

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