Norethindrone (Contraceptive) Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

This medication is used to prevent pregnancy. It is often referred to as the “mini-pill” because it does not contain any estrogen. Norethindrone (a form of progestin) is a hormone that prevents pregnancy.While the “mini-pill” is more effective than certain other methods of birth control (such as condoms, cervical cap, diaphragm), it is less effective than combination hormone (estrogen and progestin) birth control because it does not consistently prevent ovulation. It is usually used by women who cannot take estrogen. To reduce the risk of pregnancy, it is very important to take this medication exactly as prescribed.Using this medication does not protect you or your partner against sexually transmitted diseases (such as HIV, gonorrhea, chlamydia).

How to use Norethindrone

Read the Patient Information Leaflet provided by your pharmacist before you start using this product and each time you get a refill. The leaflet contains very important information on when to take your pills and what to do if you miss a dose. If you have any questions, ask your doctor or pharmacist.

Take this medication by mouth as directed by your doctor, usually once daily. Pick a time of day that is easy for you to remember, and take your pill at the same time each day.

Taking this medication after your evening meal or at bedtime may help if you have stomach upset or nausea with the medication. You may choose to take this medication at another time of day that is easier for you to remember. No matter what dosing schedule you use, it is very important that you take this medication at the same time each day, 24 hours apart.

It is best to begin taking this medication on the first day of your menstrual period. If you begin taking it on any other day, use an additional form of non-hormonal birth control (such as condoms, spermicide) for the first 48 hours to prevent pregnancy until the medication has enough time to work.

Continue taking one tablet every day. After taking the last tablet in a pack, start a new pack the next day. There is no break between packs, and you do not take any “reminder” tablets (tablets without medication). Your periods may be irregular, or heavier/lighter than usual. You may also have vaginal bleeding (spotting) between periods. Do not stop taking your pills if this happens.

Pregnancy is more likely if you miss pills, start a new pack late, or take your pill at a different time of the day than usual. If you miss a pill, or take it 3 or more hours later than usual, or have diarrhea, or vomit soon after taking a pill, use a back-up method of birth control (such as condoms, spermicide) every time you have sex for the next 48 hours.

Ask your doctor or pharmacist about how to switch from other forms of hormonal birth control (such as patch, other birth control pills) to this product. If any information is unclear, consult the Patient Information Leaflet or your doctor or pharmacist.

Side Effects

Nausea, vomiting, headache, bloating, breast tenderness, or weight gain may occur. Vaginal bleeding between periods (spotting) or missed/irregular periods may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly. If you miss 2 periods in a row (or 1 period if the pill has not been used properly), contact your doctor for a pregnancy test.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high.

Tell your doctor right away if you have any serious side effects, including: lumps in the breast, mental/mood changes (such as new/worsening depression), severe stomach/abdominal pain, unusual changes in vaginal bleeding (such as continuous spotting, sudden heavy bleeding, missed periods), dark urine, yellowing eyes/skin.

This medication may rarely cause serious (sometimes fatal) problems from blood clots (such as deep vein thrombosis, heart attack, pulmonary embolism, stroke). Get medical help right away if any of these side effects occur: chest/jaw/left arm pain, confusion, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, trouble speaking, sudden shortness of breath/rapid breathing, unusual headaches (including headaches with vision changes/lack of coordination, worsening of migraines, sudden/very severe headaches), unusual sweating, weakness on one side of the body, vision problems/changes (such as double vision, partial/complete blindness).

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before using this medication, tell your doctor or pharmacist if you are allergic to norethindrone; or to other progestins; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood clots (for example, in the legs, eyes, lungs), blood clotting disorders (such as protein C or protein S deficiency), high blood pressure, abnormal breast exam, cancer (especially endometrial or breast cancer), low levels of “good” cholesterol (HDL), depression, diabetes, severe headaches/migraines, heart problems (such as heart valve disease, irregular heartbeat, previous heart attack), history of yellowing eyes/skin (jaundice) during pregnancy or while using hormonal birth control (such as pills, patch), liver disease (including tumors), unexplained vaginal bleeding.

Smoking raises your risk of stroke, heart attack, blood clots, and high blood pressure from hormonal birth control (such as the pill, patch, ring). The risk of these serious problems increases with age and with the number of cigarettes you smoke. Do not smoke or use tobacco.

Tell your doctor if you just had or will be having surgery or if you will be confined to a bed or chair for a long time (such as a long plane flight). These conditions increase your risk of getting blood clots, especially if you are using hormonal birth control. You may need to stop this medication for a time or take special precautions.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

This medication may cause blotchy, dark areas on your face and skin (melasma). Sunlight may worsen this effect. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors.

This medication should not be used during pregnancy. If you become pregnant or think you may be pregnant, tell your doctor right away.

This medication passes into breast milk. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some drugs may cause hormonal birth control to work less well by decreasing the amount of birth control hormones in your body. This effect can result in pregnancy. Examples include griseofulvin, modafinil, rifamycins (such as rifampin, rifabutin), ritonavir, St. John’s wort, drugs used to treat seizures (such as barbiturates, carbamazepine, felbamate, phenytoin, primidone, topiramate), HIV drugs (such as nelfinavir, nevirapine), among others.

Tell your doctor when you start any new drug, and discuss if you should use additional reliable birth control. Also tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your birth control is not working well.

This medication may interfere with certain laboratory tests (such as sex hormone-binding globulin, thyroid), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this medication.

Does Norethindrone interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include severe nausea, vomiting, sudden/unusual vaginal bleeding.

Do not share this medication with others.

Regular complete physical exams which include lab and/or medical tests (such as blood pressure, breast exam, pelvic exam, Pap smear) should be done while you are taking this medication. Follow your doctor’s instructions for examining your breasts, and report any lumps right away. Keep all medical and lab appointments. Consult your doctor for more details.

Refer to the product package information for advice on missed doses. You may need to use back-up birth control (such as condoms, spermicide) to prevent pregnancy. Ask your doctor or pharmacist if you have any questions.

If you often forget to take your pills as directed, contact your doctor to discuss switching to another form of birth control.

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

norethindrone (contraceptive) 0.35 mg tablet

Color: light yellowShape: roundImprint: G 305

This medicine is a light yellow, round, tablet imprinted with “G” and “305”.

norethindrone (contraceptive) 0.35 mg tablet

Color: yellowShape: roundImprint: LU J22

This medicine is a light yellow, round, tablet imprinted with “G” and “305”.

norethindrone (contraceptive) 0.35 mg tablet

Color: yellowShape: roundImprint: LU J22

This medicine is a light yellow, round, tablet imprinted with “G” and “305”.

norethindrone (contraceptive) 0.35 mg tablet

Color: peachShape: roundImprint: 213

This medicine is a light yellow, round, tablet imprinted with “G” and “305”.

norethindrone (contraceptive) 0.35 mg tablet

Color: light yellowShape: roundImprint: G 305

This medicine is a light yellow, round, tablet imprinted with “G” and “305”.

norethindrone (contraceptive) 0.35 mg tablet

Color: yellowShape: roundImprint: 220

This medicine is a light yellow, round, tablet imprinted with “G” and “305”.

norethindrone (contraceptive) 0.35 mg tablet

Color: yellowShape: roundImprint: 220

This medicine is a light yellow, round, tablet imprinted with “G” and “305”.

Next

Save up to 80% on your prescriptions.

Available coupons

Save up to 80% on your prescription with WebMDRx

Drug Survey

Are you currently using Norethindrone?

This survey is being conducted by the WebMD marketing sciences department.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Norethindrone for painful or heavy menstrual periods (Aygestin) | Medicine

Norethindrone for painful or heavy menstrual periods

Aygestin

In this article

• What is norethindrone?
• What to know before taking norethindrone
• How to take norethindrone tablets
• Getting the most from your treatment
• Norethindrone side effects and problems
• How to store norethindrone tablets
• Important information about all medicines

What is norethindrone?

Norethindrone (also known as norethisterone) is a man-made form of progesterone, a naturally occurring female sex hormone. It is referred to as a progestin and it has a number of uses. Low doses are used to prevent pregnancy, or as hormone replacement therapy (HRT). Medium-strength tablets (5 mg) such as Aygestin® are used to treat heavy and painful menstrual periods particularly if they are associated with a condition called endometriosis. Aygestin® tablets are also used to treat endometriosis itself. Higher doses are used in the treatment of some female cancers, such as breast cancer.

Endometriosis is a condition where tissue which is normally only found inside the womb (uterus), becomes ‘trapped’ in other parts of the body, often in the pelvic area or lower abdomen. This causes symptoms such as painful and heavy periods. Treatment aims to reduce the pain and amount of blood loss. Norethindrone can also be considered for heavy periods not associated with endometriosis.

This leaflet discusses norethindrone when it is used to treat endometriosis or painful or heavy periods. There are a number of other medicine leaflets which will give you more information about norethindrone if you are taking it for birth control or as HRT. These are: Progestin-only contraceptive tablets, Combination oral contraceptives and Estrogen and progestin for HRT.

What to know before taking norethindrone

Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking norethindrone it is important that your physician knows:

• If you are pregnant or breastfeeding.
• If you have any problems with the way your liver works, or any kidney problems.
• If you have heart or blood vessel problems, or if you have ever had a blood clot in an artery or vein.
• If you have any of the following: diabetes, epilepsy, migraine, high blood pressure (hypertension), or asthma.
• If you smoke, are overweight or have high cholesterol levels.
• If you have ever had cancer.
• If you have ever had a depressive illness.
• If you have ever had yellowing of your skin or the whites of your eyes (jaundice), severe itching, or a skin condition called pemphigoid gestationis during a pregnancy.
• If you have a rare inherited blood disorder called porphyria.
• If you are taking any other medicines. This includes any medicines you are taking which are available to buy without a prescription, as well as herbal and complementary medicines.
• If you have ever had an allergic reaction to a medicine.

How to take norethindrone tablets

• Before you start this treatment, read the manufacturer’s printed information leaflet from inside your pack. The manufacturer’s leaflet will give you more information about norethindrone and a full list of side-effects which you may experience from taking it.
• Take norethindrone exactly as your physician tells you to. You may be asked to take the tablets regularly each day, or to take them just on certain days of your monthly cycle. This information will be printed on the label of your pack of tablets to remind you, but if you are still unsure ask your pharmacist for further advice.
• For treatment of endometriosis it is usual to start with a low dose of half to one tablet (2. 5 mg-5 mg) each day. Your physician will ask you to increase your dose slightly every two weeks until you are taking three tablets (15 mg) each day.
• If you are taking norethindrone for painful or heavy menstrual periods, the usual dose is between half and two tablets each day (2.5 mg-10 mg) for five to ten days in each menstrual cycle.
• Swallow the tablets with a drink of water. You can take norethindrone tablets either before or after meals.
• Try to take your doses at the same times of day, as this will help you to remember to take them.
• If you do forget to take a dose at your usual time, take it as soon as you remember, unless it is nearly time for your next dose in which case leave out the forgotten dose. Remember to take your next dose when it is due but do not take two doses together to make up for a forgotten dose.

Getting the most from your treatment

• Try to keep all your regular appointments with your physician. This is so your physician can check on your progress.
• You should avoid getting pregnant as norethindrone can affect a developing baby. Use barrier methods of birth control (such as a condom) if you have sex whilst taking norethindrone. If you need further birth control (contraception) advice, speak with your physician.
• If you have diabetes you may need to check your blood sugar (glucose) more frequently, as norethindrone can affect the levels of sugar in your blood. Your physician will be able to advise you about this.
• If you are due to have surgery or any medical treatment, tell the person carrying out the treatment that you are taking norethindrone.

Norethindrone side effects and problems

Along with their useful effects, most medicines can cause unwanted side-effects although not everyone experiences them. The table below contains some of the most common ones associated with norethindrone. You will find a full list in the manufacturer’s information leaflet supplied with your medicine. The unwanted effects often improve as your body adjusts to the new medicine, but speak with your physician or pharmacist if any of the following continue or become troublesome.

Important: norethindrone can also have some serious side-effects, although these occur only rarely. If you experience any of the following symptoms, stop taking the tablets and contact your physician for advice straightaway:

• Any feeling of pain or tightness in your chest.
• Any disturbances of your vision or hearing.
• Any unusually severe headaches.
• Any yellowing of your skin or the whites of your eyes (jaundice).

If you experience any other symptoms which you think may be due to this medicine, speak with your physician or pharmacist.

How to store norethindrone tablets

• Keep all medicines out of the reach and sight of children.
• Store in a cool, dry place, away from direct heat and light.

Important information about all medicines

• FDA Drug Label, Aygestin® 5 mg tablets – norethindrone acetate; Teva Women’s Health Inc, DailyMed, National Institutes of Health, US National Library of Medicine. Dated August 2019.

• FDA Drug Label, Norethindrone acetate 5 mg tablets; Amneal Pharmaceuticals of New York LLC, DailyMed, National Institutes of Health, US National Library of Medicine. Dated December 2022.

Norethisterone (NET)

Did you win a grant? We guarantee you an excellent price for reagents and fast delivery.

+7 (495) 798-02-48

sales@immunotex. ru

+7 (865) 228-34-60

sales.imm

Search product
by ANTIGEN

Kits
ELISA

Kits
ELISA

Search
ANTIBODIES

Small molecules
and PROTEINS

Additional
materials

ELISA toxins
MEDICINES

Make
SPECIAL ORDER

Norethisterone is a drug that is used in combination with estrogen or alone in hormonal contraceptives, hormone replacement therapy, and in the treatment of gynecological diseases. It is a synthetic progestogen (or progestin) from the 19-nortestosterone group and has similar properties to natural progesterone, including suppression of gonadotropic hormones, inhibition of ovulation, and endometrial transformation. In addition to its progestogenic activity, norethisterone also has weak androgenic and estrogenic effects at high doses.
Norethisterone is used as a hormonal contraceptive in combination with an estrogen – usually ethinyl estradiol – in combined oral contraceptives and alone as tablets. In addition to its use as a contraceptive, norethisterone can be used to treat premenstrual syndrome, dysmenorrhea, menorrhagia, irregular menstruation, menopausal symptoms (in combination with estrogens), or delayed menstruation. It is also widely used to prevent uterine bleeding in complex non-surgical or non-surgical gynecological conditions and in the treatment of cyclic mastalgia.

Organism

Article

Name

Available

Sandwich ELISA for Norethisterone (NET)

Organism:

For all

Code:

SEV755Ge

Sandwich ELISA for Norethisterone (NET)

In stock :

Clarify

Organism

Article

Name

In the presence of

Sandwich Clia For Norethisterone (NET)

Organism:

For all

SKU:

SCV755Ge

Sandwich CLIA for Norethisterone (NET)

In stock:

Specify

that it is available for customization.

Call back

Chat with a specialist

Write to us

Moscow State University

Almazov Research Center

Scientific Center of Virology and Biotechnology “Vector”

Institute of Biomedical Problems RAS

Institute of Cytology and Genetics SB RAS

Institute of Physiology. Pavlova

Sechenov University

IRTC of Eye Microsurgery named after Fedorov

MIPT

Institute of Experimental Medicine

Research Center named after. Dmitry Rogachev

NRC Kurchatov Institute

St. Petersburg Institute of Nuclear Physics. B.P. Konstantinova

Research Institute of Eye Diseases. Helmholtz

Kulakov Research Center for Obstetrics, Gynecology and Perinatology

Sechenov IEPhB RAS

Lobachevsky National Research University

Tomsk Scientific Research Medical Center

Kazan Federal University

Mechnikov North-Western State Medical University

Baltic Federal University

Scientific center of neurology

North Caucasian Federal University

Far Eastern Federal University

Federal Scientific and Research Center for Physical and Chemical Medicine

Federal Scientific and Practical Center for Resuscitation and Rehabilitology

Siberian Federal University

Institute of Gene Biology RAS

Federal Research Center for Nutrition and Biotechnology

Siberian Medical University

Institute of Cell Biophysics RAS

NIPI im. Bekhterev

Institute of Fundamental Problems of Biology RAS

Institute of Toxicology FMBA of Russia

Research Institute of Obstetrics and Gynecology. Otta

Research Institute of Mental Health

Russian Medical Academy of Postgraduate Education

Krasnoyarsk Medical University. Voino-Yasenetsky

Altai Medical University

Nearmedic

Volgograd Medical University

Novosibirsk Medical University

RNIOI

acad. Shemyakina and Ovchinnikova

Petrovax Pharm

South Ural State University

PIMU

Gorbatov Federal Scientific Center for Food Systems RAS

The evolution of hormonal contraception » Medvestnik

V.V. YAGLOV, obstetrician-gynecologist, Polyclinic No. 78, Moscow, Ph.D. gg.). However, the real prerequisites for the use of hormones to prevent unwanted pregnancies were formed by the 1950s.

At the same time, the need to take large doses of progesterone up to 200-300 mg to suppress ovulation when administered orally and its rapid inactivation in the gastrointestinal tract, a short contraceptive effect, pronounced adverse reactions, manifested in the form of acyclic bleeding from the vagina, depression, dyspeptic disorders and, finally, direct dependence on sources of obtaining biological material required different approaches to solving the problem.

The discovery of a method for obtaining progesterone from plants (Russel Marker, 1930s) was an important step in expanding the scope of hormonal drugs, but did not fundamentally affect the evolution of hormonal contraception. Additional research and development was required, which ultimately led to the emergence of today’s numerous synthetic analogues of progesterone (synonyms: progestogens, gestagens, progestins), which fully meet modern criteria for the effectiveness and safety of drugs used for contraception.

Nobel Laureate Grigory Pinkus

In general, research was carried out in two main areas.

On the one hand, in the early 60s of the twentieth century, progestogens were synthesized, similar in structure to progesterone, while having significantly more acceptable pharmacokinetic parameters and called pregnanes or, more precisely, acetylated pregnane derivatives. The related cyproterone acetate, chlormadinone acetate and medroxyprogesterone acetate have been successfully used as part of combined oral contraceptives for four decades up to the present day and, in addition to contraception itself, can be used to correct androgen-dependent skin disorders (acne, seborrhea) of mild and moderate severity in women who need contraception.

On the other hand, even earlier (Carl Djerassi, 1951), synthetic progestogens were first obtained, similar in structure to testosterone and related to its estran derivatives: norethindrone (norethisterone), norethinodrel, linesstrinol, norethindrone acetate, etinodiol diacetate and et al.

The earlier synthesis of estrans compared to pregnanes was due to the simpler and more convenient structure of the testosterone molecule for research compared to that of progesterone. It was norethindrone (norethisterone) that became the first progestogen included in the first, registered in 1960, FDA (Food and Drug Administration, USA), a combined oral contraceptive (COC) called Enovid, after the first clinical study in 1956 by an American scientist of Russian origin Gregory Pincus, who later received the Nobel Prize for research in the field of hormonal contraception.

Progestogens with extremely low androgenic activity

It should be noted that the progestogenic activity of the synthesized estrans significantly exceeded that of progesterone. However, their concentration, necessary to suppress ovulation, still remained high and was measured in milligrams (up to 10 mg), which was reflected in the side effects of their use: a greater likelihood of androgenization symptoms, impaired carbohydrate and fat metabolism, mood changes, etc. At the same time, the pronounced progestogenic properties of estrans, combined with moderate androgenic and antiestrogen effects, have contributed to their use for the treatment of endometrial hyperplastic processes for several decades.

Both original and generic drugs are registered in Russia. According to their pharmacological characteristics, acceptability and effectiveness, they do not differ. The effect of COCs is realized due to the blocking effect of the progestogen and estrogenic components that make up the drug on the hypothalamic-pituitary-ovarian system that regulates the normal menstrual cycle, inhibition of the synthesis of follicle-stimulating and luteinizing hormones of the pituitary gland and prevention of ovulation.

The search and development of even more active analogues of progesterone led to the production in 1963 of levonorgestrel, the first fully synthetic oral progestogen, already related to gonan derivatives of testosterone (gonans). The advent of levonorgestrel made it possible to reduce the daily dosage of progestogen to 150 mcg, and then to 100 mcg.

More than 20 years passed before clinical practice in the 80s. of the last century, new synthetic ethynylated gonan derivatives of testosterone were introduced – gestagens with extremely low androgenic activity. Desogestrel, gestodene and norgestimate have found the greatest use. At the same time, the dosage of the progestogen in some modern oral contraceptives was reduced to 75 mcg, which made it possible to use ethynylated gonans, incl. and for the correction of skin manifestations of androgenization of mild and moderate severity in women who need contraception.

Fundamentally new progestogens

Finally, at the turn of the century, two fundamentally new progestogens appeared: dienogest (1990s) and drospirenone (2000s).

The characteristic property of the so-called hybrid progestogen dienogest, a non-ethynylated derivative of testosterone, was its high acceptability due to a combination of pronounced selectivity for progesterone receptors – like natural progesterone and metabolic stability inherent in synthetic 19-norgestagenam (gonans).

Dienogest does not accumulate in the body when taken daily and does not affect the main types of metabolism – protein, lipid and carbohydrate. In addition, it has pronounced antiandrogenic properties, neutralizing the effects of increased concentrations of male sex hormones produced in the body of a woman, preventing the formation of acne, oily skin and excessive hair growth.

The new progestogen drospirenone is a derivative of spironolactone and therefore endowed with a number of new pharmacological properties. Possessing a pronounced antimineralocorticoid activity, it helps to neutralize the negative effects of aldosterone and prevents the accumulation of excess fluid in the body, while the pharmacological profile of drospirenone binding to receptors is very similar to that of endogenous progesterone, but drospirenone practically does not show glucocorticoid, antiglucocorticoid and estrogenic activity.

Subsequent generations have fewer similar effects

Thus, over a half-century period of oral hormonal contraceptive use, several generations of progestogens that are part of them have been synthesized. Each new generation had fewer side effects than the previous one, retaining or even enhancing contraceptive and other related therapeutic properties. In the arsenal of a modern doctor there are various progestogens: derivatives of progesterone, testosterone, spironolactone.

It is customary to isolate 3 generations of gestagens, testosterone derivatives:

• first – norethinodrel, norethisterone, ethinadiol acetate, linestrinol
• second – norgestrel, levonorgestrel
• third – gestodene, desogestrel, norgestimate.

Some authors distinguish the fourth generation, which includes the so-called hybrid gestagen dienogest.

The biological effects of progestogens are determined by their interaction with both progesterone receptors (gestagenic effect) and androgenic (residual androgenic or, conversely, antiandrogenic effect), glucocorticoid, mineralocorticoid, sometimes estrogen and other receptors. In general, all synthetic progestogens are more active and less selective (selective) compared to natural progesterone.

Synthetic ethinylestradiol is the most effective

In order to increase the acceptability of hormonal contraception, along with the so-called pure gestagenic contraceptives containing only a progesterone or testosterone derivative as an active substance (in Russia, in particular, hormonal contraceptives containing levonorgestrel as the only active substance are registered , linestrinol, desogestrel, medroxyprogesterone), an estrogen component has been added to the composition of hormonal preparations for progestogen. The most effective oral estrogen was synthetic ethinylestradiol, which today is part of the vast majority of combined oral hormonal contraceptives (COCs).

With virtually no effect on the effectiveness of contraception, ethinyl estradiol (EE) helps prevent acyclic bleeding by maintaining adequate endometrial trophism. At the same time, it is well known that high concentrations of estrogen increase blood clotting and contribute to thrombophilia. When analyzing the results of clinical studies, it was found that with a decrease in the dose of ethinylestradiol in combined oral contraceptives (COCs), the incidence of complications decreases, while acceptability remains quite high. Based on the content of EE, combined hormonal contraceptives are classified as high-dose (more than 35 µg EE), low-dose (more than 20 µg EE, but less than 35 µg EE), microdosed (20 µg EE), ultra-microdosed (15 µg EE).

Mono-, bi- and triphasic contraceptives

In addition to significantly reducing the likelihood of acyclic bleeding, estrogens increase the secretion of the apocrine and paraurethral glands, preventing discomfort in the vagina; participate in reducing the secretion of the sebaceous glands, thereby contributing to a positive cosmetic effect; contribute to the utilization of calcium by bone tissue, eliminating osteoporosis and activating the function of osteogenesis.

In addition, estrogens reduce the level of atherogenic lipid fractions in the blood, have a beneficial effect on the function of the brain and subcortical structures, relieving vegetative-vascular and psycho-emotional disorders.

Currently, a COC is registered, which instead of ethinylestradiol contains estradiol valeriate, the main metabolite of which is estradiol, similar to natural estrogen, which, on the one hand, reduces the risk of estrogen-dependent side effects, on the other hand, requires combination with a highly selective progestogen in order to reduce the likelihood of acyclic spotting/bleeding.

Based on the ratio of the concentration of active substances (progestagen and estrogen) in each tablet / dragee, COCs are divided into mono-, two-, three-phase. A greater combination of combinations of estrogen and progestogen in one COC is also possible – a number of researchers believe that such a combination is more physiological for the female body, however, other scientists give priority to monophasic hormonal contraceptives, when each active tablet contains the same ratio of estrogen and progestogen.

Modern drugs have become safer

Thus, with almost 100% effectiveness of modern contraceptives when used correctly, their choice is primarily determined by acceptability and safety, which largely depends on the composition of progestogen and estrogen and their concentration.

It becomes clear why monophasic hormonal drugs, in addition to reliable contraception, are recommended for women with menstrual disorders (oligo-, poly-, dysmenorrhea, premenstrual syndrome), endometrial hyperplastic processes, fibrocystic mastopathy, as well as in various maladaptation and stress situations contributing to an overstrain of the neuroendocrine system, including after an abortion and childbirth, when, due to various circumstances, a woman cannot breastfeed.

Due to the reduction in the dose of estrogens (up to 5-7 times) and progestogens (up to 100-120 times!) in comparison with their predecessors of the 60-70s of the last century, modern combined oral contraceptives have become safer: they can be used both in young nulliparous women who begin sexual activity and in women of older reproductive age. Of course, in any case, one should also remember about possible contraindications to the use of hormonal contraception, so the choice of method, duration and mode of its use must be discussed with an obstetrician-gynecologist. It is appropriate to recall that oral hormonal contraceptives are prescription drugs.

Maximum concentration – within two hours

Along with the indicated mechanism, the contraceptive effect is also due to an increase in the viscosity of cervical mucus, which prevents the advancement of spermatozoa.

Concerning some fundamental features of modern gestagens, it is important to note that the antiandrogenic effect of COCs (reduction of skin and hair oiliness, reduction of acne vulgaris) is due to the fact that gestagens suppress the production of luteinizing hormone, which stimulates the synthesis of androgens in the ovaries, while EE stimulates the synthesis in the liver of sex steroid-binding globulins (SHBG). This leads to a decrease in the free fraction of androgens in the blood.

According to various sources, COCs containing 20-30 µg of EE cause an increase in the content of SHBG in the blood by about 1.5-3 times. A certain selection of concentrations of estrogen and progestogen components allows either a minimal effect on metabolic processes, or, on the contrary, in addition to providing a contraceptive effect, to compensate for existing metabolic disorders in a woman’s body. The vast majority of clinical trials have shown the high acceptability of modern COCs, which is also characterized by a low frequency of “spotting” and “breakthrough” acyclic bleeding during their use.

When taken orally, COC components are absorbed in the upper small intestine. The maximum concentration in blood plasma, as a rule, is observed during the first 2 hours. In the future, there is a 2-phase decrease with a half-life of 0.5-1 hour and 18-24 hours for progestogen and 1-3 and 24 hours for EE. Daily use of the drug is not accompanied by a noticeable cumulation of active substances and their metabolites. After entering the blood, the main part of progestogen and EE binds to plasma albumin and globulin, which determines their long-term effect. Subsequently, the progestogen is completely metabolized in the liver with the formation of practically inactive metabolites, which are excreted mainly by the kidneys and to a small extent through the intestines. EE is excreted through the kidneys and through the intestines in a ratio of 2/3.

How to take contraceptives

There are different ways to take monophasic COCs – the standard 28-day regimen (21 active tablets + 7 placebo tablets or 7 drug-free days during which menstrual bleeding occurs) and prolonged (extended) regimen, when menstrual-like bleeding occurs once every 2-3 months (63 active tablets + 7 placebo tablets or 7 drug-free days during which menstrual-like bleeding occurs).

The drug is started on the first day of the cycle (1st day of menstruation), using tablets from the cell marked with the corresponding day of the week. Tablets are taken without chewing and washed down with a small amount of water. The time of admission does not play a role, but the subsequent intake should be made at the same selected hour. For 21 (63) days, take 1 tablet daily, then take a break for 7 days, during which menstrual bleeding occurs. The next package of the drug is started on the 8th day.

The search for new routes of administration continues

In order to increase the acceptability of hormonal contraceptives, the search for new routes of administration continues.