Unprotected intercourse does not always lead to pregnancy. But in order not to push your luck, modern pharmaceuticals offer hormonal drugs for postcoital contraception. One of the oldest representatives of the group is Postinor. It continues to be sold in pharmacies, although safer analogues have now been developed. But if used correctly, you can use this tool.
What is post-natal contraception
The effectiveness of trying to prevent pregnancy depends on the day of your menstrual cycle and when you start treatment. In women with a normal cycle, conception has a short period of 12 hours - the time when the egg leaves the follicle and moves through the fallopian tubes. If during this time there is no meeting with a sperm, then an embryo will not form.
For this it is necessary to adhere to a clear time frame. The age of the embryo should not exceed 3-5 days. Only at this time does the endometrium have the properties necessary for implantation. Therefore, under natural conditions, the number of pregnancies that successfully progress after conception is only 30%.
High risk of pregnancy during sexual intercourse that occurred three days or less before ovulation. Sex one day after the release of the egg cannot lead to pregnancy.
Therefore, before deciding to take hormonal medications, it is necessary to assess the risk of becoming pregnant. If a woman knows exactly the time of ovulation (), the duration of her cycle, then this is as simple as possible. A day or two after the follicle bursts, unprotected sex will not lead to pregnancy. Therefore, there is no need to take hormones that can disrupt the menstrual cycle.
Emergency contraception is used within 1-3 days after sexual intercourse. The sooner this is done, the higher the effectiveness of Postinor and other drugs.
Composition and mechanism of action
The drug contains levonorgestrel. This is a synthetic progestogen that is part of. It also has an antiestrogenic effect.
How does Postinor work?
It inhibits the gonadotropic function of the pituitary gland. Under its influence, the concentration of gonadotropins - luteinizing and follicle-stimulating hormones - decreases. Therefore, if ovulation has not yet occurred, it will slow down.
Levonorgestrel affects the endometrium, changes its properties, which prevents the implantation of an already fertilized egg. It also increases the viscosity of cervical mucus, which makes it difficult for sperm to penetrate the fallopian tubes.
The active substance is rapidly absorbed when taken orally, its bioavailability is almost 100%. Maximum serum concentration is reached after 1.6 hours. The half-life is 26 hours. Levonorgestrel is excreted in equal proportions by the kidneys and through the intestines.
Indications and contraindications
Women take birth control pills Postinor after sexual intercourse without using a means of birth control. It can also be used if there is no complete confidence in the effectiveness of the main product:
- condom slipping into the genital tract;
- violation of the integrity of the condom, the female diaphragm;
- missing one or more oral contraceptive pills;
- loss or spontaneous removal of the intrauterine device;
- incorrect calculation of ovulation days when using the calendar method;
- unsuccessful interrupted sexual intercourse.
The drug acts on the implantation mechanism, so taking Postinor to terminate pregnancy in the early stages does not make sense.
Contraindications include the following conditions:
- Individual intolerance or hypersensitivity to the components of the drug. If once after taking the pills there were signs of an allergic reaction, repeated use will be accompanied by a similar reaction or even more pronounced.
- Age up to 18 years. begins on average at 12-14 years of age and continues for 4-5 years. Any intervention can lead to serious cycle disruptions, which may take several years to recover.
- Severe liver failure is accompanied by metabolic disorders. Most hormones, including levonorgestrel, pass through the liver. If organ function is insufficient, excessive accumulation and increased side effects may occur.
- Pregnancy is also a contraindication. Postinor will not cause miscarriage, but its effects on the developing fetus have not been well studied. There is always a risk of disruption of the formation of internal organs.
- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption may worsen when using Postinor, since it contains lactose monohydrate and corn and potato starch.
You should drink Postinor with caution if you have Crohn's disease, inflammatory diseases of the liver and biliary tract, or cholelithiasis.
In women over 35 years of age, the chance of developing thrombosis increases. The risk increases with blood clotting disorders and smoking a large number of cigarettes per day. The presence of migraine indicates a tendency to thrombosis. Therefore, in this case, you should also take the drug with caution.
Combination with other drugs and alcohol
Due to their metabolic characteristics, it is not recommended to combine some medications with Postinor. These include:
- proton pump inhibitors: Lansoprozole, Omeprazole;
- reverse transcriptase inhibitor: Nevirapine;
- antiretroviral: Ritonavir;
- antiepileptic drugs: Oxcarbazepine, Carbamazepine, Primidone, Phenytoin;
- immunosuppressants: Tacrolimus;
- antibiotics: Rifampicin, Ampicillin, Tetracycline, Rifabutin, Griseofulvin;
- retinoids: Tretinoin.
Levonorgestrel reduces the effectiveness of hypoglycemic drugs and worsens the use of anticoagulants of coumarin derivatives, Phenindione. Plasma concentrations of glucocorticosteroids may increase.
The simultaneous use of Levonorgestrel and Cyclosporine suppresses the mechanism of metabolism of the latter. It is an immunosuppressant prescribed for internal organ and bone marrow transplants. Failure to neutralize the drug leads to its accumulation in the liver and the appearance or intensification of adverse reactions.
Treatment with drugs based on St. John's wort, including those prepared at home, is also a contraindication.
The compatibility of Postinor and alcohol is controversial. Ethanol is metabolized through the liver. There are several ways of oxidizing and removing ethyl alcohol from the body. In some cases, they coincide with those for hormonal agents. Competition for transport proteins can lead to impaired metabolism of either alcohol or drugs.
Undesirable effects
Side effects from Postinor vary from person to person. The most common adverse events are:
- Damage to the digestive tract: pain in the lower abdomen, nausea, vomiting, digestive disorders, and in some cases diarrhea.
- Pathology of the mammary glands: pain appears on palpation of the breast.
- Reproductive system: menstrual irregularities, bleeding after administration that is not associated with the normal menstrual cycle. The delay after Postinor can be up to 7 days or more. The duration of the menstrual cycle disruption varies. Menstruation can start earlier or later than due.
- Damage to the nervous system manifests itself in the form of increased fatigue, frequent headaches, and dizziness. The appearance of this side effect is associated with the effect of Postinor on the coagulation system and an increase in blood viscosity.
Most side effects go away on their own within a few days. If they are delayed for a longer period, it is necessary to consult a doctor and also exclude pregnancy.
Menstruation after Postinor must be calculated based on previous data on the duration of the cycle and the time of onset of menstrual bleeding. If there is a delay of more than 5-7 days, you must consult a doctor. In this case, there is a high probability that the drug did not work and the pregnancy continued.
The appearance of brown discharge may be an indicator of the onset of normal menstruation or a side effect in the form of cycle disruption.
If after taking the drug there are no periods, but the pregnancy test is negative, in this case it can be assumed that the luteal phase of the cycle is insufficient. Under the influence of a large dose of levonorgestrel, profound depression of pituitary function could occur. Therefore, the lack of luteinizing and follicle-stimulating hormones affects ovulation: it is delayed indefinitely. To confirm the diagnosis, a hormonal profile examination is used: blood is donated for the main sex hormones. It is recommended for such women to be carried out to determine the onset or impossibility of ovulation.
A positive test after taking the medicine indicates pregnancy. This means that Postinor was taken incorrectly or untimely.
The consequences of contraception with Postinor may be long-term. Some women complain of missing periods or irregular cycles for several years.
Combination with pregnancy and lactation
Postinor is not designed to terminate pregnancy; it is not a medication for medical abortion. But it is impossible to call it completely safe for pregnant women: it is impossible to evaluate the effect on the developing fetus experimentally. There is also no data on such experiments on animals.
It is not known whether Postinor is harmful to the developing fetus. But in cases of pregnancy occurring while taking the drug, the preservation of the fetus did not result in the detection of severe vascular pathology or the occurrence of deformities incompatible with life.
The active substance is found unchanged in the blood and can pass into breast milk. A newborn does not need the action of hormones that affect the immature pituitary gland. Therefore, if there is a need for emergency contraception while breastfeeding, after taking the pills you must refrain from feeding for at least 1 day.
How to take Postinor
The first condition for successful use of the pills is no more than 72 hours after sexual intercourse, which occurred without contraception. The package contains two tablets. The first is taken as early as possible, and the second 12 hours after it. The maximum gap between taking two tablets is 16 hours.
An adverse reaction in the form of vomiting that appears within 3 hours after taking 1 or 2 tablets becomes the basis for taking an additional tablet.
Use Postinor on any day of the menstrual cycle. If menstruation occurs regularly, then there is no possibility of a short-term pregnancy. If it is necessary to exclude the existence of pregnancy using a rapid test.
The drug cannot be taken again during one menstrual cycle. This leads to the appearance of spotting and acyclic uterine bleeding.
How often can Postinor be used?
Peculiarities
The effectiveness of contraception with levonorgestrel depends on the time when the first pill was taken. The sooner after sexual intercourse this is done, the higher the likelihood of a successful outcome. For example, if you use it during the first day after unprotected sex, in 95% of cases or more the promised effect occurs. When using the first tablet during the second day, the effectiveness decreases to 85%, and on the third day it is only 58%.
After using the drug, it is necessary to mark the date of unprotected sex and the day of administration in the women's calendar. From this time, a countdown is taken for the appearance of possible signs of pregnancy or its successful prevention.
How to understand that Postinor has worked?
Menstruation should begin on time according to the calendar. Its duration and volume of blood loss should not differ significantly from normal days.
You should consult a doctor in the following cases:
- heavy periods;
- scanty discharge;
- delay more than 7 days;
- combination of discharge with pain in the lower abdomen.
Painful sensations can be cramping, but more often aching in nature. Sometimes this condition is accompanied by weakness and dizziness. If acute abdominal pain occurs, urgent hospitalization is necessary. This is how it usually manifests itself. An interrupted pregnancy due to a ruptured tube is characterized by the appearance of acute abdominal pain and signs of internal bleeding (low blood pressure, tachycardia).
The effectiveness of a drug can be affected not only by other drugs, but also by pathological conditions. When Crohn's disease spreads to the upper intestines, it leads to impaired absorption of nutrients. Therefore, with this pathology, as well as other inflammatory diseases of the digestive tract, absorption may be impaired and, as a result, contraception may not be effective enough.
It should also be remembered that hormonal drugs do not protect against sexually transmitted diseases. To protect yourself from infection, you must use a condom correctly. If sexual intercourse carries the risk of not only an unwanted pregnancy, but also the development of an infection, emergency protective measures should be used. To do this, the woman must urinate and treat the urethral opening with an antiseptic solution: Chlorhexidine, Miramistin. In some cases, preventive antibiotics are effective.
Postinor, and its analogues Escapel, Microlut, Eskinor F, are a means of contraception only in emergency cases, that is, for life-threatening reasons, such as rape, rupture of a condom during sexual intercourse.
Why can't it be used on an ongoing basis? This drug in developed countries can only be purchased with a prescription, unlike in Russia, since Postinor has serious side effects.
However, some women use these drugs quite often, without consulting a gynecologist and not knowing about the consequences, complications, side effects of Postinor and its analogues. To understand what effect these drugs have on the body, you should know the mechanism of their action.
Mechanism of action of Postinor
Postinor causes a lot of side effects and its use is possible only in extreme cases. During puberty and for women planning to have children in the future, its use is not advisable, since this can lead to hormonal imbalance in a woman and cause infertility in the future.
Postinor and its analogues are intended only for emergency prevention of pregnancy. The active ingredient of the drug is levonorgestrel, of which there is 0.75 mg in one tablet, which is considered a lethal dose. In low-dose oral contraceptives, for example, this dose of levonorgestrel is contained in 20 tablets. The Postinor package contains 2 tablets, which are taken 12 hours apart for 72 hours after unprotected sexual intercourse. The mechanism of action of levonorgestrel is as follows:
- a drug blocks ovulation- prevents a mature egg from leaving the ovary
- when ovulation has already occurred, Postinor prevents implantation of the fertilized egg in the uterine cavity - in this case it essentially has an abortifacient effect
- leads to a change in cervical mucus, it becomes thicker, which interferes with the penetration of sperm into the uterine cavity.
When the implantation of a fertilized egg into the wall of the uterus has already occurred, the drug becomes ineffective, since all gestagens have the property of suppressing the motor activity of the uterine muscles.
Contraindications
The use of Postinor is contraindicated for use in the following cases:
- liver dysfunction, severe liver disease
- teenage girls under 16 years old
- During lactation, the drug passes into breast milk, so it is contraindicated during breastfeeding.
- with uterine bleeding of unknown origin
- for individual intolerance
- for herpetic infections and other infectious diseases of the genitourinary system
- in diseases associated with enzymatic deficiency - impaired absorption of glucose, galactose (lactase deficiency)
- for malignant neoplasms of any location
- with a genetic predisposition to thrombosis
Use with caution for ulcerative lesions of the gastrointestinal tract, diseases of the biliary tract.
Side effects of Postinor
Any medications have side effects, and Postinor is a powerful hormonal drug, which in some cases can become a trigger for the development of serious health problems in a woman. Therefore, in developed countries this drug is available only by prescription and is considered an unsafe method of contraception. Side effects of Postinor are as follows:
- Intestinal dysfunction - diarrhea
- Digestive disorders - vomiting, diarrhea
- Headache, dizziness
- Intermenstrual bleeding
- Breast tension
- Flu-like symptoms
- Weakness, lethargy
If you experience any side effects from taking Postinor or other unusual signs of illness, you should consult a doctor.
Side effects from the reproductive system, impact on the woman’s reproductive function in the future
Considering that 1 tablet contains a huge amount of active substance, a real hormonal imbalance occurs in a woman’s body after taking Postinor. The instructions for the drug say that it is not recommended to use it more than 4 times a year. But some women often neglect these recommendations and take it uncontrollably, sometimes even several times per menstrual cycle, which is very dangerous and prohibited.
Since Postinor should be taken when there is a high probability of pregnancy (ovulation period) - at this time the mucous membrane of the uterus has not yet matured, which leads to dysfunction of the ovaries, and then they produce either less or more hormones. And even with a one-time use of the drug, a certain time is required (in each case individually) to restore ovarian function.
Therefore, if a woman with existing menstrual irregularities:
- irregular menstruation
- teenagers under 16 years old
If you take the drug even once, such disruptions can be permanent and cause infertility in the future.
The influence of this hormonal drug, especially on an ongoing basis, leads to the fact that the function of the ovaries begins to fade, become depleted, and the production of hormones gradually becomes less and less. This causes irregularities in the menstrual cycle and can affect a woman's reproductive ability. In some cases, taking the drug leads to amenorrhea (lack of menstruation) and, as a result, persistent infertility. Even a timely visit to a gynecologist in such cases cannot guarantee the successful restoration of the normal menstrual cycle and the likelihood of pregnancy.
If a woman has periodic uterine bleeding, taking Postinor and its analogues can intensify it and lead to the need for emergency medical care, so in such cases taking the drug is unacceptable. Also, one of the side effects of Postinor is engorgement and soreness of the mammary glands, and the appearance of discharge from the nipples.
Other side effects of Postinor
In addition to disorders associated with hormonal shock, the effects of Postinor and Escapel, if taken incorrectly, can have other consequences, such as, for example, the formation of blood clots in blood vessels. This side effect can mainly occur in women with bleeding disorders, but even a seemingly healthy woman has this risk (see video - documentary).
After repeated use of maximum doses of hormones, blood clotting ability increases and the risk of blood clots in blood vessels increases. When the lumens of blood vessels are partially blocked, there is a reduction in blood flow to organs and tissues and, as the most extreme pathology, blockage of blood vessels (the occurrence of pulmonary thromboembolism). When blood vessels in the heart and brain become blocked, a stroke or instant death may occur.
If a woman does not have any problems with the menstrual cycle, side effects of Postinor occur quite rarely. But other ailments may appear - pain in the lower abdomen, nausea, diarrhea, headaches, swelling. Due to frequent use of Postinor, disturbances in fat and carbohydrate metabolism may occur, causing a decrease or increase in body weight, and suppression can lead to changes in male-type hair growth or changes in the contours of the figure.
Every woman who cares about her health should watch this video before deciding to take any oral contraceptives (even low-dose ones). This is especially true for young girls who want to have children in the future.
Registration number: P N011850/01
Tradename: Postinor
International nonproprietary name:
levonorgestrel
Dosage form: pills
Compound
Each tablet contains:
Active substance: levonorgestrel 0.75 mg.
Excipients: colloidal silicon dioxide, potato starch: magnesium stearate: talc; corn starch; lactose monohydrate.
Description
Flat tablets of white or almost white color, disc-shaped with a chamfer and with a circular engraving "I N O R ●" on one side.
F armacotherapy group: gestagen.
ATX code: G03A POP
Farmacological properties
Pharmacodynamics
Levonorgestrel is a synthetic gestagen with a contraceptive effect, pronounced gestagenic and antiestrogenic properties. With the recommended dosage regimen, levonorgestrel suppresses ovulation and fertilization if sexual intercourse occurs in the preovulatory phase, when the possibility of fertilization is greatest. It may also cause changes in the endometrium that prevent implantation. The drug is not effective if implantation has already occurred.
Efficacy: with the help of Postinor tablets, pregnancy can be prevented in approximately 85% of cases. The more time passed between sexual intercourse and taking the drug, the lower its effectiveness (95% during the first 24 hours, 85% from 24 to 48 hours and 58% from 48 to 72 hours). Thus, it is recommended to start taking Postinor tablets as soon as possible (but no later than 72 hours) after sexual intercourse, if no protective measures have been taken. At the recommended dose, levonorgestrel does not have a significant effect on blood clotting factors, fat and carbohydrate metabolism.
Pharmacokinetics
When taken orally, levonorgestrel is rapidly and almost completely absorbed.
After taking 0.75 mg of levonorgestrel, the maximum concentration of the drug in serum equal to 14.1 ng/ml is achieved after 1.6 hours. After reaching the maximum level of concentration, the content of levonorgestrel decreases, and the half-life is about 26 hours.
Levonorgestrel is excreted approximately equally by the kidneys and through the intestines exclusively in the form of metabolites. The biotransformation of levonorgestrel corresponds to the metabolism of steroids. Levonorgestrel is hydroxylated in the liver and metabolites are excreted in the form of conjugated glucuronides. Pharmacologically active metabolites of levonorgestrel are unknown. Levonorgestrel binds to serum albumin and sex hormone binding globulin (SHBG). Only 1.5% of the total dose is in free form, and 65% is associated with SHBG. Absolute bioavailability is almost 100% of the dose taken.
Indications for use
Emergency (postcoital) contraception (after unprotected sexual intercourse or unreliability of the contraceptive method used).
Contraindications
Hypersensitivity to any component of the drug, use in adolescents under 16 years of age, severe liver failure, pregnancy.
Patients with rare hereditary diseases such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Carefully
Diseases of the liver or biliary tract, jaundice (including a history), Crohn's disease, lactation.
Pregnancy and lactation
Postinor should not be used during pregnancy. If pregnancy occurs while using an emergency method of contraception, then based on the available data, no adverse effect of the drug on the fetus has been identified.
Levonorgestrel passes into breast milk. After taking the drug, breastfeeding should be stopped for 24 hours.
Directions for use and doses
The drug is administered orally. You must take 2 tablets in the first 72 hours after unprotected intercourse. The second tablet should be taken 12 hours (but not later than 16 hours) after taking the first tablet.
To achieve a more reliable effect, both tablets should be taken as quickly as possible after unprotected intercourse (no later than 72 hours).
If vomiting occurs within three hours after taking 1 or 2 Postinor tablets, then you should take another Postinor tablet.
Postinor can be used at any time of the menstrual cycle. In case of irregular menstrual cycle, pregnancy must first be excluded.
After taking emergency contraception, a local barrier method (eg, condom, cervical cap) should be used until the next menstrual period. The use of the drug during repeated unprotected sexual intercourse during one menstrual cycle is not recommended due to an increase in the frequency of acyclic spotting/bleeding.
Side effect
Allergic reactions are possible: hives, rash, itching, swelling of the face.
Transient side effects occurring with varying frequency (common: ≥1/100,<1/10, очень часто: ≥1/10) и не требующие медикаментозной терапии: часто: рвота, диарея, головокружение, головная боль, болезненность молочных желез, задержка менструации (не более 5-7 дней), если менструация задерживается на более длительный срок, необходимо исключить беременность.
Very common: nausea, fatigue, lower abdominal pain, acyclic spotting (bleeding).
Frelease form
Tablets 0.75 mg. 2 tablets in an AL/PVC blister. 1 blister in a cardboard box with attached instructions for use.
Ustorage conditions
List B. At a temperature of 15 °C to 25 °C, out of the reach of children.
WITHrock expiration date
5 years.
Do not use the drug after the expiration date.
Uterms of dispensing from pharmacies
On prescription.
Manufacturer
JSC "Gedeon Richter"
1103 Budapest, st. Demrei 19-21, Hungary
Consumer complaints should be sent to:
Moscow Representative Office of JSC Gedeon Richter
119049 Moscow. 4th Dobryninsky lane d.8.
Compound
Each tablet contains:
Active substance:
levonorgestrel – 0.75 mg
Excipients:
colloidal silicon dioxide, potato starch, magnesium stearate, talc, corn starch, lactose monohydrate (71.25 mg).
Description
Round, flat, almost white tablets with a bevel, marked “ INOR●"on one side.
Pharmacotherapeutic group
Sex hormones and modulators of the reproductive system. Emergency contraception.
ATX code: G03AD01
Pharmacological properties
Pharmacodynamics
The exact mechanism of action of the drug POSTINOR is unknown.
When used in recommended doses, the effect of levonorgestrel is presumably due to the prevention of ovulation and fertilization if sexual intercourse occurs in the preovulatory phase, when the likelihood of fertilization is greatest. In addition, it can cause changes in the endometrium that prevent the implantation of a fertilized egg. The drug is ineffective if the implantation process has already begun.
Efficiency: According to the results of an earlier clinical study, 750 mcg of levonorgestrel (given as two 750 mcg doses taken 12 hours apart) prevented 85% of expected pregnancies. The effectiveness of the drug appears to decrease over time after sexual intercourse (95% within 24 hours, 85% when used between 24 and 48 hours, 58% when used between 48 and 72 hours).
According to the results of an earlier clinical study, two 750 mcg levonorgestrel tablets taken simultaneously (within 72 hours after unprotected intercourse) prevented 84% of expected pregnancies. There are no differences in the incidence of pregnancy in women who took the drug on the third or fourth day after unprotected intercourse (p > 0.2).
There are limited data that require further confirmation on the impact of excess body weight/high body mass index (BMI) on contraceptive effectiveness. Three World Health Organization (WHO) studies observed no trend toward decreased efficacy with increasing body weight/BMI (see Table 1), while 2 other studies (Creinin et al., 2006 and Glasier et al., 2010 ) there was a decrease in effectiveness with increasing body weight/BMI (see Table 2). Both meta-analyses were conducted excluding cases of drug use later than 72 hours after unprotected sexual intercourse (off-label use) and women who had unprotected sexual intercourse after taking the drug.
Table 1. Meta-analysis of three WHO studies (Von Hertzen et al., 1998 and 2002; Dada et al., 2010)
| BMI (kg/m2) | Overweight women 25-30 | Women with obesity ≥ 30 | ||
|---|---|---|---|---|
| Total | 600 | 3952 | 1051 | 256 |
| Number of pregnancies | 11 | 39 | 6 | 3 |
| Pregnancy rate | 1,83% | 0,99% | 0,57% | 1,17% |
| Confidence interval | 0,92 - 3,26 | 0,70-1,35 | 0,21 - 1,24 | 0,24 - 3,39 |
Table 2. Meta-analysis of studies Creinin et al., 2006, and Glasier et al., 2010
| BMI (kg/m2) | Low weight women 0-18.5 | Women with normal weight 18.5-25 | Women overweight 25-30 | Women with obesity ≥ 30 |
|---|---|---|---|---|
| Total | 64 | 933 | 339 | 212 |
| Number of pregnancies | 1 | 9 | 8 | 11 |
| Pregnancy rate | 1,56% | 0,96% | 2,36% | 5,19% |
| Confidence interval | 0,04 - 8,40 | 0,44-1,82 | 1,02-4,60 | 2,62 - 9,09 |
Pediatric population
A prospective observational study showed that of 305 cases of levonorgestrel tablets used as emergency contraception, seven women became pregnant. Thus, the overall failure rate was 2.3%. The failure rate in women younger than 18 years (2.6% or 4/153) was comparable to the failure rate in women 18 years and older (2.0% or 3/152).
Pharmacokinetics
After oral administration, levonorgestrel is rapidly and almost completely absorbed. After taking 1.5 mg of levonorgestrel, the maximum serum concentration is 18.5 ng/ml and is achieved after 2 hours.
After reaching the maximum, the concentration of levonorgestrel decreases, and the average half-life is about 26 hours.
Levonorgestrel is excreted in the form of metabolites and is not excreted unchanged. Levonorgestrel metabolites are excreted in urine and feces in approximately equal proportions. Biotransformation occurs in accordance with the known mechanisms of steroid metabolism: levonorgestrel is hydroxylated in the liver, and its metabolites are excreted in the form of glucuronide conjugates.
Pharmacologically active metabolites of the drug are unknown.
Levonorgestrel binds to serum albumin and sex hormone binding globulin (SHBG). Only about 1.5% of the total serum concentration is present as a free steroid, 65% is specifically bound to SHBG. The absolute bioavailability of levonorgestrel is almost 100% of the administered dose.
About 0.1% of the dose administered to the mother can be passed into the baby's breast milk.
Indications for use
Emergency contraception within 72 hours after unprotected sexual intercourse or if the contraceptive method used was unreliable.
Contraindications
Hypersensitivity to the active substance (levonorgestrel) or any of the auxiliary ingredients listed in the “Composition” section.
Use during pregnancy and breastfeeding
Pregnancy
Pregnant women should not use POSTINOR. It will not cause abortion.
According to limited epidemiological data, in the case of developing pregnancy, the drug does not have any undesirable effects on the fetus. At the same time, there is no clinical data on the possible consequences of taking levonorgestrel in doses above 1.5 mg.
Breast-feeding
Levonorgestrel is excreted in breast milk. The potential exposure of a nursing infant to levonorgestrel can be reduced if a nursing woman takes the tablets immediately after feeding, avoiding feeding after each dose of POSTINOR.
Fertility
Levonorgestrel increases the possibility of menstrual irregularities, which in some cases leads to earlier or later ovulation. These changes may influence fertile dates, but long-term fertility data are not available.
Directions for use and doses
Dosing
You need to take two tablets.
Both tablets should be taken as soon as possible, preferably within the first 12 hours and no later than 72 hours after unprotected sexual intercourse (see section "Pharmacodynamics").
If vomiting occurs within three hours after taking any of the tablets, you should immediately take the other 2 tablets.
For women who have taken drugs that are inducers of liver microsomal enzymes in the past 4 weeks and require emergency contraception, the use of a non-hormonal emergency contraceptive, such as a copper-containing intrauterine device (IUD) or taking a double dose of levonorgestrel (for example, 4 tablets once) is recommended. women who are unable or unwilling to use a copper-containing IUD (see section Interactions with other medicinal products).
POSTINOR can be used in any phase of the menstrual cycle, provided there is no delay in menstrual bleeding.
After using emergency contraception, it is recommended to use a local barrier method (condoms, cervical cap) until the next menstruation. The use of POSTINOR is not a contraindication for continuing regular hormonal contraception.
Use in children
Levonorgestrel is not recommended for use in children.
There are very limited data for use in young women under 16 years of age. The drug POSTINOR is not intended for use in adolescent children for the indication of emergency contraception.
Mode of application
For oral administration.
Side effect
The most common adverse reaction was nausea.
| Organ system class according to MedDRA 16.0 | Frequency of adverse reactions | |
|
Very frequent (≥ 10%) |
Frequent (from ≥ 1% to< 10%) |
|
| Nervous system disorders | Headache | Dizziness |
| Nausea Pain in the lower abdomen |
Diarrhea Vomit |
|
| Bleeding not associated with menstruation | Delay of menstruation by more than 7 days Irregular menstruation Breast engorgement |
|
| Increased fatigue | ||
If the onset of the next menstruation is delayed by more than 5 days, pregnancy should be excluded.
During post-marketing surveillance, the following adverse reactions were recorded:
Digestive system disorders
Very rare (<1/10000): боль в животе.
Skin and subcutaneous tissue disorders
Very rare (<1/10000): кожная сыпь, крапивница.
Reproductive system and breast disorders
Very rare (<1/10000): боль в области таза, дисменорея.
Systemic disorders and complications at the injection site
Very rare (<1/10000): отёк лица.
Overdose
No serious adverse effects have been reported following acute overdose of large doses of oral contraceptives. In case of overdose, nausea and breakthrough bleeding may occur. There are no specific antidotes; treatment should be symptomatic.
Interaction with other drugs
The metabolism of levonorgestrel is activated by the simultaneous use of drugs that are inducers of liver enzymes, mainly inducers of the CYP3A4 enzyme system. When coadministered with efavirenz, a decrease in levonorgestrel plasma levels (AUC) of approximately 50% was found.
Drugs that are thought to have a similar ability to reduce plasma levels of levonorgestrel include barbiturates (including primidone), phenytoin, carbamazepine, herbal preparations containing St. John's wort (Hypericum perforatum), rifampicin, ritonavir, rifabutin, and griseofulvin. Women receiving these drugs should seek advice from their doctor.
Women who have taken liver microsomal enzyme inducing drugs in the past 4 weeks and require emergency contraception should consider the use of a non-hormonal emergency contraceptive (eg, a copper IUD). Taking double-dose levonorgestrel (eg, 3,000 mcg levonorgestrel within 72 hours of unprotected intercourse) is an option for those women who are unable or unwilling to use a copper IUD, although this specific combination (double-dose levonorgestrel while using microsomal inducers) liver enzymes) has not been studied.
Medicines containing levonorgestrel may cause increased toxicity of cyclosporine due to possible inhibition of cyclosporine metabolism.
Precautionary measures
Emergency contraception is a method that can be used occasionally. It should not replace a regular contraceptive method.
Emergency contraception does not prevent pregnancy in all cases.
If there is doubt about the timing of unprotected intercourse, or if unprotected intercourse occurred earlier than 72 hours earlier during the same menstrual cycle, there is a possibility that conception has already occurred. In this regard, the use of the drug POSTINOR during the second sexual intercourse may be ineffective in preventing pregnancy. If the menstrual cycle is delayed by more than 5 days, or if unusual bleeding occurs on the day of the expected menstruation, or if there is other reason to suspect pregnancy, pregnancy must be excluded.
If pregnancy occurs after using the drug POSTINOR, the possibility of ectopic pregnancy must be taken into account. The absolute risk of ectopic pregnancy appears to be low because levonorgestrel prevents ovulation and fertilization. Ectopic pregnancy can develop despite the appearance of uterine bleeding. In this regard, levonorgestrel should be used with increased caution in the presence of risk factors for ectopic pregnancy (salpingitis or a history of ectopic pregnancy).
The use of POSTINOR is not recommended in patients with severe liver dysfunction.
The effectiveness of POSTINOR may be negatively affected by severe malabsorption syndromes, such as Crohn's disease. Women suffering from such diseases should consult a doctor if they need emergency contraception.
After taking the drug POSTINOR, menstruation usually occurs normally and occurs on time. Sometimes menstruation may start a few days earlier or later. Women should be advised to visit their doctor to select and begin using a method of regular contraception. If withdrawal bleeding does not occur in the next period without pills after using the drug POSTINOR and after using regular hormonal contraception, pregnancy should be excluded.
Repeated use of the drug during one menstrual cycle is not recommended due to the possibility of cycle disruption.
There is limited data that requires further confirmation that the contraceptive effectiveness of POSTINOR may decrease with increasing body weight or body mass index (BMI) (see section "Pharmacodynamics"). All women, regardless of their weight and BMI, should take emergency contraception as soon as possible after unprotected intercourse.
POSTINOR is not effective as a standard, regular method of contraception and should only be used as an emergency measure. Women seeking repeated courses of emergency contraception should be advised to use long-term methods of contraception.
The use of emergency contraception does not replace necessary precautions related to protection against sexually transmitted diseases.
The drug contains lactose monohydrate. Patients with congenital galactose or lactose intolerance or glucose-galactose malabsorption syndrome are not recommended to take the drug.
"Postinor" is currently one of the most popular drugs for preventing unwanted pregnancy. Among the female half of the population, due to its properties and characteristics of use, it received the name of a remedy that terminates pregnancy “the next morning.” In developed countries, Postinor is not used as a contraceptive; this drug is prescribed only after consultation with a specialist and is sold in pharmacies strictly according to a prescription due to the unsafety of its use. In our country, the drug can be bought freely at any pharmacy if it is available in the range, and if it is not available, you can place an order, and in the shortest possible time it will appear on the pharmacy counter. The drug is used as an emergency prevention of unwanted pregnancy; it is not used for continuous use. But some women have found Postinor to be used on an ongoing basis as a method of contraception.
The drug "Postinor" - pharmacological properties
The medicine has progestogenic, antiestrogenic and contraceptive properties, therefore, it works in three directions:
- blocks the release of an already mature egg from the ovary into the fallopian tubes, as a result of which fertilization by sperm does not occur;
- in the case of ovulation and fertilization, it prevents the fertilized egg from implanting into the walls of the uterus by changing the composition of the endometrium, as a result it becomes loose and the egg cannot attach to it;
- changes the composition of cervical mucus, as a result of which it becomes viscous, the speed of sperm decreases, they cannot penetrate the uterine cavity, therefore the process of fertilization does not occur.
If the fertilized egg does attach to the walls of the uterus, the drug becomes ineffective.
In what forms is the medicine available?
This drug is available in a single form - tablets. White or milky oval tablets. One tablet contains 0.75 mg of the active substance - levonorgestrel - an artificial hormone and other additional substances (silicon dioxide, magnesium stearate, talc, corn lactose monohydrate). One cardboard package contains one blister containing two tablets.
Indications for use of the drug
Accepted only in cases where sexual intercourse was forced and unprotected or when the condom was mechanically damaged in order to prevent unwanted pregnancy. It is not recommended to constantly take this drug, since its negative effect on the body leads to hormonal changes in the future and threatens infertility, which is difficult to treat.
The effectiveness of "Postinor"
The effectiveness of the drug is on average about 85% and depends on several factors, such as the correct use of the medicine and the time that has passed since sexual intercourse. If no more than 24 hours have passed since sexual intercourse, the effectiveness of the drug reaches 95%, if no more than 48 hours - 85%, if more than 48 hours and up to 72 hours - less than 58%.
How dangerous is the drug?
Like all hormonal drugs, Postinor has a number of side effects. The most common:
- allergic reactions - rash, itching, Quincke's edema;
- general symptoms - chills, sweating, feeling hot, weakness, lethargy, pain in the lower abdomen;
- from the digestive system - nausea, vomiting, stool disorders (diarrhea);
- from the central nervous system - headache, dizziness, irritability;
- on the part of the reproductive system - intermenstrual bleeding, its pain, the appearance of discharge when pressing on the nipples, in girls who took Postinor, the delay of menstruation may be 5-7 days, there may also be amenorrhea - absence of menstruation, which in the future can lead to infertility ;
- hormonal disorders - male pattern hair growth (appearance of facial hair);
- violation of carbohydrate and fat metabolism (body weight can either decrease or increase);
- increasing the likelihood of developing an ectopic pregnancy.
Assessing the consequences of Postinor, many women leave negative reviews, because the drug must be taken very carefully.
How to take it?
Postinor is taken as soon as possible after unprotected sexual intercourse has occurred. During the first 48 hours, you should take one tablet of the drug orally, without chewing, with a small amount of water. 12 - 16 hours after taking the first tablet, you must take the second, but no later than 72 hours. If vomiting occurs, another tablet is taken within 2 - 3 hours after taking the medicine. "Postinor" can be used on any day of the menstrual cycle. If there is irregularity of the menstrual cycle, then before taking the drug it is necessary to exclude the presence of pregnancy. It is not advisable to take the drug more than once during one menstrual cycle. After taking Postinor, until the onset of menstruation, during sexual intercourse you should use barrier methods of contraception, such as a cervical cap or a condom.
What could be the threatening consequences of taking Postinor?
As a result of taking the drug, heavy uterine bleeding may develop as a result of an increase in the gestagen hormone in the blood and a change in the thickness of the endometrium. The occurrence of bleeding should serve as a signal to seek qualified medical help.
Another very dangerous side effect of the drug is increased blood clotting, which can result in thrombosis of blood vessels. The blockage can be partial - when the lumen of the vessels is not completely blocked, or complete. In this case, there is a high probability of developing ischemic stroke with various types of paralysis and paresis.
In some cases, the resulting blood clots can break off and result in a brain hemorrhage, sometimes fatal. The consequences of "Postinor", reviews from women indicate this, are very dangerous, so you should not take this drug lightly.
To whom is the drug contraindicated?
Termination of pregnancy with Postinor is contraindicated in a number of diseases and conditions of the body. The main ones:
- diseases of the liver and biliary tract with impaired functions (liver failure) due to the fact that hormone metabolism occurs in the liver;
- the age of girls under 16 years old - due to the negative impact on the development of the female hormonal system;
- pregnancy - due to a negative effect on the fetus;
- lactation period - due to the high probability of passage into breast milk and effects on the child;
- individual sensitivity to active and excipients;
- uterine bleeding of unknown origin - due to an increase in their duration;
- any infectious diseases of the genitourinary system (in particular, we are talking about genital herpes);
- disruption of the enzymatic activity of the gastrointestinal tract, when the process of absorption of glucose and galactose is disrupted;
- cancer of any organ - due to the likelihood of accelerated tumor growth and the appearance of metastases;
- disruption of the circulatory system, when there is a tendency to increased thrombus formation;
- Crohn's disease - due to a decrease in absorption and assimilation of the drug and, as a result, a decrease in the effectiveness of the drug;
- peptic ulcer of the stomach and duodenum - due to the high likelihood of gastric bleeding.
Features of the course of menstruation after "Postinor"
The course of menstruation, its very appearance, says a lot. With their appearance, we can conclude that there is a pregnancy. But this may also indicate some violations in this area. There are two possible options for menstrual irregularities after using the drug:
- Menstruation after Postinor may be delayed for up to one week (in cases where more than two weeks have passed and menstruation has not started, you should immediately contact a gynecologist, as this may indicate pregnancy or be a consequence of the negative effect of the drug itself on the female body) , sometimes amenorrhea occurs - absence of menstruation, which leads to infertility;
- Severe uterine bleeding, which is a signal to contact a medical facility.
For what menstrual cycle disorders should Postinor not be used?
There are a number of menstrual cycle disorders for which the drug is strictly not allowed to be used:
- heavy and prolonged periods;
- brown discharge instead of menstruation;
- bleeding from the uterine cavity;
- pain during menstruation;
- Irregular menstrual cycle.
"Postinor" price
The cost of the drug depends on which pharmacy or pharmacy chain it is sold at. For those wishing to purchase Postinor, the price ranges from 228 to 281 rubles per package with two 0.75 mg tablets. The cost of the drug may vary depending on the region where you purchase it. Also, the price differs among pharmacy chains. In general, the drug is one of the available medical products for different segments of the population.
Consequences of "Postinor" - reviews
Many women, despite the consequences of this drug, used it and continue to use it. There are different views on the use and consequences of Postinor. Reviews about this medication are mixed. Some claim that the artificial hormone really helps, others are not so sure. According to women's testimonies, Postinor, whose price is relatively low, is not always effective in preventing unwanted pregnancy. On the contrary, in some cases it can only strengthen it.
There is evidence that the drug can postpone menstruation. But this is not scientific information, so it is very unsafe to use it for these purposes. The consequences of "Postinor", reviews from women indicate this, may worsen as a result of failure to follow the instructions. Sometimes women, having a great fear of pregnancy, can take pills, forgetting about the rules of use. It’s worth “pulling yourself together,” focusing on your condition and trying to protect your health. They may appear after Postinor. This is not an indicator that pregnancy has occurred; such a phenomenon may indicate the occurrence of side effects from the drug.
"Postinor", the use of which is not a panacea for pregnancy, affects the woman's health. To prevent pregnancy, you can use other methods of protection, such as a condom, then there will be no risk of side effects from the drug.
