Levonorgestrel-Ethinyl Estradiol Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

This combination hormone medication is used to prevent pregnancy. It contains 2 hormones: a progestin (levonorgestrel) and an estrogen (ethinyl estradiol).Besides preventing pregnancy, birth control pills may make your periods more regular, decrease blood loss and painful periods, decrease your risk of ovarian cysts, and also treat acne.Using this medication does not protect you or your partner against sexually transmitted diseases (such as HIV, gonorrhea, chlamydia).

How to use levonorgestrel-ethinyl estradiol oral

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.

It is very important to continue taking this medication exactly as prescribed by your doctor. Follow the package instructions to find the first tablet, start with the first tablet in the pack, and take them in the correct order. Do not skip any doses. 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.

Vomiting or diarrhea can prevent your birth control pills from working well. If you have vomiting or diarrhea, you may need to use a back-up birth control method (such as condoms, spermicide). Follow the directions in the Patient Information Leaflet and check with your doctor or pharmacist for more details.

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. Ask your doctor or pharmacist if you have any questions.

Begin taking this medication on the first Sunday following the beginning of your menstrual period. If your period begins on a Sunday, begin taking this medication on that day. Your pill pack contains 84 active pills (with hormones) and 7 inactive pills (without hormones). Take one active pill daily for 84 days in a row. The day after you finish all the active pills, start taking one inactive pill daily for 7 days in a row. You should have your period during the week you are taking the inactive pills. The day after you take the last inactive tablet in the pack, start a new pack whether or not you have your period. If you do not get your period, consult your doctor.

If this is the first time you are using this medication, use an additional form of non-hormonal birth control (such as condoms, spermicide) for the first 7 days to prevent pregnancy until the medication has enough time to work. If you start on the first day of your period, you do not need to use back-up birth control the first week.

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, swelling of the ankles/feet (fluid retention), or weight change may occur. Vaginal bleeding between periods (spotting) may occur, especially during the first few months of use. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

You should not have your period during the 3 months that you are taking the active pills. Instead, you will have your period once every 3 months, during the week that you are taking the inactive pills. This effect is normal with this product. However, if you do not have your period while taking the inactive pills, 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

See also Warning section.

Before using this medication, tell your doctor or pharmacist if you are allergic to ethinyl estradiol or levonorgestrel; or to other estrogens or 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), high cholesterol or triglyceride (blood fat) levels, depression, diabetes, family or personal history of a certain swelling disorder (angioedema), gallbladder problems, 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), kidney disease, liver disease (including tumors), stroke, swelling (edema), thyroid problems, unexplained vaginal bleeding.

If you have diabetes, this medication may affect your blood sugar. Check your blood sugar regularly as directed and share the results with your doctor. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. Your doctor may need to adjust your diabetes medication, exercise program, or diet.

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.

If you are nearsighted or wear contact lenses, you may develop vision problems or trouble wearing your contact lenses. Contact your eye doctor if these problems occur.

It may take longer for you to become pregnant after you stop taking birth control pills. Consult your doctor.

This medication should not be used during pregnancy. If you become pregnant or think you may be pregnant, tell your doctor right away. If you have just given birth or had a pregnancy loss/abortion after the first 3 months, talk with your doctor about reliable forms of birth control, and find out when it is safe to start using birth control that contains a form of estrogen, such as this medication.

This medication may decrease breast milk production. A small amount passes into breast milk and may have undesirable effects on a nursing infant. 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 products that may interact with this drug include: aromatase inhibitors (such as anastrozole, exemestane), fezolinetant, ospemifene, tamoxifen, tizanidine, tranexamic acid, certain combination products used to treat chronic hepatitis C (ombitasvir/paritaprevir/ritonavir with or without dasabuvir).

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 lab tests (such as blood clotting factors, thyroid), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.

Does levonorgestrel-ethinyl estradiol oral 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 and 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

levonorgestrel 0.15 mg-ethinyl estradiol 30 mcg tablets,3 mos pack(91)

Color: multi-color (2)Shape: roundImprint: E1 or E2

This medicine is a multi-color (2), round, dose pack imprinted with “E1 or E2”.

levonorgestrel 0.15 mg-ethinyl estradiol 30 mcg tablets,3 mos pack(91)

Color: multi-color (2)Shape: roundImprint: LU U21 or U22

This medicine is a multi-color (2), round, dose pack imprinted with “E1 or E2”.

levonorgestrel 0.15 mg-ethinyl estradiol 30 mcg tablets,3 mos pack(91)

Color: multi-color (2)Shape: roundImprint: E1 or E2

This medicine is a multi-color (2), round, dose pack imprinted with “E1 or E2”.

levonorgestrel 0.15 mg-ethinyl estradiol 30 mcg tablets,3 mos pack(91)

Color: multi-color (2)Shape: roundImprint: LU U21 or U22

This medicine is a multi-color (2), round, dose pack imprinted with “E1 or E2”.

levonorgestrel 0.15 mg-ethinyl estradiol 30 mcg tablets,3 mos pack(91)

Color: multi-color (2)Shape: roundImprint: 212 or 279

This medicine is a multi-color (2), round, dose pack imprinted with “E1 or E2”.

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.

Ethinyl Estradiol/Desogestrel, Oral – Tufts Medical Center Community Care

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ETH-in-iI es-tra-DY-ole des-oh-JES-trel

What are other names for this medicine?

Type of medicine: contraceptive (birth control)

Generic and brand names: ethinyl estradiol and desogestrel, oral; Apri; Azurette; Caziant; Cyclessa; Desogen; Kariva; Mircette; Ortho-Cept 28; Reclipsen; Velivet; Viorele

What is this medicine used for?

This medicine (commonly called birth control pills) is used to prevent pregnancy.

This medicine may be used to treat other conditions as determined by your healthcare provider.

What should my healthcare provider know before I take this medicine?

Before taking this medicine, tell your healthcare provider if you have ever had:

• An allergic reaction to any medicine
• A bleeding disorder
• Angioedema (swelling)
• Asthma
• Blood clots or a blood clotting disorder
• Breast cancer or cancer of the lining of the uterus, cervix, or vagina
• Breast lumps, breast cysts, or abnormal mammograms
• Chest pain (angina)
• Depression
• Diabetes
• Heart valve or heart rhythm problems
• Gallbladder or kidney disease
• Headaches along with symptoms such as vomiting, double vision, unsteadiness, weakness, or personality changes
• Heart attack, heart disease, or stroke
• Hereditary angioedema
• High blood pressure
• High cholesterol or high triglycerides
• Irregular periods
• Liver disease or liver tumor
• Porphyria (nerve pain or sensitivity to sunlight)
• Seizures
• Thyroid disease
• Unexplained vaginal bleeding, uterine fibroids, or abnormal Pap smears
• Yellowing of the eyes or skin (jaundice) during pregnancy or during past use of birth control pills

Tell your healthcare provider if you have recently had a long period of bed rest after a major surgery or illness, or a broken bone in a cast, or you have recently delivered a baby. You may be at a risk of developing blood clots. Also, tell your healthcare provider if you are scheduled for surgery.

Tell your provider if you have a family history of heart disease, heart attack, high cholesterol, blood clots, strokes, breast cancer, or other conditions.

Tell your healthcare provider if you smoke. Smoking while you are using this medicine increases the risk of serious side effects such as heart attack, stroke, and blood clots. The risk increases with age and the number of cigarettes smoked a day. Talk to your healthcare provider about ways to quit smoking.

Females of childbearing age: DO NOT use this product if you are pregnant or breast-feeding because it may harm the baby. Stop taking this medicine at the first sign you may be pregnant and contact your healthcare provider right away.

How do I take it?

Check the label on the medicine for directions about your specific dose. Take this medicine exactly as prescribed by your healthcare provider on the schedule prescribed. Take it with a full glass (8 ounces) of water. Take it at the same time each day. Use the special packaging to keep track of doses. Read the information sheet that comes in the medicine package for more information.

Check with your healthcare provider before using this medicine in children who have not reached puberty.

What if I miss a dose?

If you miss a dose at your normal time, take it as soon as you remember. If you do not remember until the next day, take 2 tablets that day. If you miss 2 or more doses in a row, see the information sheet that comes in the medicine package or ask your healthcare provider what to do. You may need to use another method of birth control (such as a condom or spermicide) as a back-up method for 7 days.

What if I overdose?

If you or anyone else has intentionally taken too much of this medicine, call 911 or go to the emergency room right away. If you pass out, have seizures, weakness or confusion, or have trouble breathing, call 911. If you think that you or anyone else may have taken too much of this medicine, call the poison control center. Do this even if there are no signs of discomfort or poisoning. The poison control center number is 800-222-1222.

Symptoms of an acute overdose may include: nausea, vomiting, vaginal bleeding.

What should I watch out for?

You need to see your provider at least once a year for checkups while you are taking this medicine. Do not take this medicine for longer than 1 year without a complete physical exam.

Depending on the type of pill prescribed for you, your healthcare provider may recommend that you use a second method of birth control when you first start taking this medicine.

This medicine only prevents pregnancy. It does not prevent sexually transmitted diseases (STDs) such as HIV or herpes.

If you need emergency care, surgery, or dental work, tell the healthcare provider or dentist you are using this medicine. If you need any lab tests, tell your healthcare provider you are using this medicine. Birth control hormones may change some blood test results.

If you have spotting or light bleeding or feel sick to your stomach, do not stop taking the pill. The symptoms will usually go away. If symptoms continue, check with your healthcare provider.

Severe vomiting or diarrhea and certain other medicines may make this medicine less effective. Tell all healthcare providers who treat you that you are taking this medicine. You may need to use another method of birth control if the healthcare provider prescribes a medicine that might reduce the effectiveness of the birth control pills.

If you notice a change in your vision or wear contacts and it becomes difficult to wear your lenses, contact your healthcare provider.

If you have diabetes: If you are taking insulin or another medicine for diabetes, talk to your healthcare provider because your dosage of diabetes medicine may need to be changed.

What are the possible side effects?

Along with its needed effects, your medicine may cause some unwanted side effects. Some side effects may be very serious. Some side effects may go away as your body adjusts to the medicine. Tell your healthcare provider if you have any side effects that continue or get worse.

Life-threatening (Report these to your healthcare provider right away. If you are unable to reach your healthcare provider right away, get emergency medical care or call 911 for help):

• Allergic reaction (hives, itching, rash, tightness in your chest, trouble breathing)
• Severe chest pain or pressure, coughing blood, or sudden shortness of breath
• Sudden severe headache or vomiting, dizziness or fainting, problems with vision or speech, weakness, or numbness in an arm or leg
• Sudden partial or complete loss of vision

Serious (report these to your healthcare provider right away):

• Yellowing of the skin or eyes, especially with fever, tiredness, loss of appetite, dark urine, or light-colored bowel movements
• Pain, redness, or swelling in the calf
• Severe pain, swelling, or tenderness in the abdomen
• Breast lumps or tenderness
• Irregular vaginal bleeding or spotting that happens in more than 1 menstrual cycle or lasts for more than 7 days
• Swelling of your hands or ankles
• Discomfort from contact lenses or vision changes
• Trouble sleeping, weakness, lack of energy, fatigue, or depression

Other: Vaginal or urinary infection, vaginal discharge, weight changes, nausea, vomiting, dizziness, nervousness, bloating, darkening of skin on the face, headache, hair loss, change in sexual desire.

What products might interact with this medicine?

When you take this medicine with other medicines, it can change the way this or any of the other medicines work. Nonprescription medicines, vitamins, natural remedies, and certain foods may also interact. Using these products together might cause harmful side effects. Talk to your healthcare provider if you are taking:

• Acne medicines such as acitretin (Soriatane) and isotretinoin (Amnesteem, Claravis, Sotret)
• Aminophylline and theophylline
• Antianxiety medicines such as alprazolam (Xanax), clonazepam (Klonopin), clorazepate (Tranxene), diazepam (Valium), flurazepam, and triazolam (Halcion)
• Antibiotics such as amoxicillin (Augmentin, Moxatag), ampicillin, clarithromycin (Biaxin), demeclocycline, dicloxacillin, doxycycline (Adoxa, Doryx, Monodox, Vibramycin), erythromycin (Ery-tabs, E.E.S.), isoniazid, minocycline (Minocin), oxacillin, penicillin, rifampin (Rifadin), rifabutin (Mycobutin), rifapentine (Priftin), and tetracycline
• Antidepressants such as amitriptyline, desipramine (Norpramin), doxepin, imipramine (Tofranil), nefazodone, and nortriptyline (Pamelor)
• Anti-HIV medicines such as atazanavir (Reyataz), delavirdine (Rescriptor), elvitegravir/cobicistat/emtricitabine/tenofovir (Stribild), efavirenz (Sustiva), etravirine (Intelence), indinavir (Crixivan), nevirapine (Viramune), nelfinavir (Viracept), and ritonavir (Norvir, Kaletra)
• Antiseizure medicines such as carbamazepine (Tegretol), ethotoin (Peganone), felbamate (Felbatol), fosphenytoin (Cerebyx), gabapentin (Neurontin), lamotrigine (Lamictal), levetiracetam (Keppra), oxcarbazepine (Trileptal), phenytoin (Dilantin), primidone (Mysoline), tiagabine (Gabitril), topiramate (Topamax), and valproic acid (Depacon, Depakene, Depakote)
• Antifungals such as fluconazole (Diflucan), griseofulvin (Grifulvin V, Gris-Peg), itraconazole (Sporanox), ketoconazole (Nizoral), posaconazole (Noxafil), and voriconazole (VFEND)
• Antiviral medicines such as boceprevir (Victrelis) and telaprevir (Incivek)
• Aprepitant (Emend)
• Artemether/lumefantrine (Coartem)
• Barbiturates such as butabarbital (Butisol), pentobarbital (Nembutal), and phenobarbital
• Beta blockers such as acebutolol (Sectral), atenolol (Tenormin), carvedilol (Coreg), labetalol (Trandate), metoprolol (Lopressor, Toprol XL), nadolol (Corgard), nebivolol (Bystolic), pindolol, propranolol (Inderal LA), and sotalol (Betapace)
• Bexarotene (Targretin)
• Bosentan (Tracleer)
• Cholesterol-lowering medicines (statins) such as atorvastatin (Lipitor), lovastatin (Mevacor), rosuvastatin (Crestor), and simvastatin (Zocor) or cholesterol-lowering medicines such as cholestyramine (Questran), colesevelam (WelChol), and colestipol (Colestid) (separate by at least 4 hours)
• Conivaptan (Vaprisol) or tolvaptan (Samsca)
• Corticosteroids such as betamethasone (Celestone), cortisone, dexamethasone, hydrocortisone (Hydrocortone, Cortef), methylprednisolone (Medrol), prednisone (Liquid Pred, Prednisone Intensol), prednisolone (Pediapred, Prelone), and triamcinolone (Aristospan, Kenalog)
• Dantrolene (Dantrium)
• Diabetes medicines such as insulin, exenatide (Byetta, Bydureon), glipizide (Glucotrol), glyburide (DiaBeta, Glynase PresTab), metformin (Glucophage), pioglitazone (Actos), repaglinide (Prandin), and rosiglitazone (Avandia)
• Enzalutamide (Xtandi)
• Heart medicines such as diltiazem (Cardizem) and verapamil (Calan, Verelan)
• Immunosuppressants such as cyclosporine (Sandimmune, Neoral, Gengraf), tacrolimus (Prograf), and mycophenolate (CellCept)
• MAO inhibitors such as isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl, Emsam), and tranylcypromine (Parnate) (Do not take this medicine and an MAO inhibitor within 14 days of each other. )
• Morphine (MS Contin, Oramorph, Kadian)
• Natural remedies such as alfalfa, chasteberry, bloodroot, hops, yucca, licorice, St. John’s wort, dong quai, black cohosh, red clover, ginseng, and saw palmetto
• Stimulant medicines such as armodafinil (Nuvigil) and modafinil (Provigil)
• Selegiline (Eldepryl, Emsam)
• Thyroid medicine such as levothyroxine (Levoxyl, Synthroid, Unithroid), liothyronine (Cytomel, Triostat), liotrix (Thyrolar), and thyroid (Armour Thyroid)
• Tizanidine (Zanaflex)
• Vitamins A, B, and C, and minerals such as zinc, iron, and magnesium
• Warfarin (Coumadin)

Do not eat grapefruit or drink grapefruit juice while taking this medicine. Grapefruit affects the way this medicine works and may increase the risk of side effects.

If you are not sure if your medicines might interact, ask your pharmacist or healthcare provider. Keep a list of all your medicines with you. List all the prescription medicines, nonprescription medicines, supplements, natural remedies, and vitamins that you take. Be sure that you tell all healthcare providers who treat you about all the products you are taking.

How should I store this medicine?

Store this medicine at room temperature. Keep the container tightly closed. Protect it from heat, high humidity, and bright light.

This advisory includes selected information only and may not include all side effects of this medicine or interactions with other medicines. Ask your healthcare provider or pharmacist for more information or if you have any questions.

Ask your pharmacist for the best way to dispose of outdated medicine or medicine you have not used. Do not throw medicine in the trash.

Keep all medicines out of the reach of children.

Do not share medicines with other people.

Developed by RelayHealth.

Medication Advisor 2015.1 published by RelayHealth.
Last modified: 2014-08-11
Last reviewed: 2013-11-27

This content is reviewed periodically and is subject to change as new health information becomes available. The information is intended to inform and educate and is not a replacement for medical evaluation, advice, diagnosis or treatment by a healthcare professional.

Copyright ©1986-2015 McKesson Corporation and/or one of its subsidiaries. All rights reserved.

Description of ETHINYLESTRADIOL indications, dosages, contraindications of the active substance ETHINYLESTRADIOL

Rec.INN WHO registered drug interaction Included in preparations: list Pharmacological action Synthetic estrogen. Just like endogenous estrogens, it stimulates the development of the uterus, fallopian tubes, secondary sexual characteristics, causes proliferative changes in the endometrium, and increases the excitability of the uterus. Regulates nitrogen metabolism, reduces the level of lipids and cholesterol in the blood, has a weak anabolic effect. Increases the absorption of calcium and the formation of calcium depots in the bones. In high doses, it causes sodium and water retention. Pharmacokinetics Binds predominantly to plasma albumin. Metabolized in the liver to form hydroxylated and methylated metabolites. Excreted as metabolites by the kidneys – 40% and through the intestines – 60%. Indications of the active substance ETINILESTRADIOL Contraception (mainly in combined preparations). Manifestations of climacteric syndrome associated with estrogen deficiency; female hypogonadism, dysmenorrhea. Palliative treatment of malignant tumors of the mammary gland in the postmenopausal period. Palliative treatment of malignant tumors of the prostate. Open list of ICD-10 codes C50 Malignant neoplasm of the mammary gland C61 Malignant neoplasm of the prostate E23. 0 Hypopituitarism N94.4 Primary dysmenorrhea N94.5 Secondary dysmenorrhea N95.1 Menopause and climacteric conditions in women N95.3 Conditions associated with induced menopause Z30.0 General advice and advice on contraception Z51.5 Palliative care Dosing regimen Set individually, depending on the indication. The daily dose for oral administration varies from 10 mcg to 3 mg. Side effects On the part of the digestive system: nausea, vomiting, gastrointestinal dysfunction, liver dysfunction, jaundice, formation of gallstones are possible. From the endocrine system: possible soreness and enlargement of the mammary glands, changes in libido, menstrual irregularities and bleeding after withdrawal, decreased glucose tolerance. From the side of metabolism: possible swelling, weight gain. From the nervous system: possible depression, headache, migraine, dizziness. Dermatological reactions: possible skin hyperpigmentation. On the part of the blood coagulation system: may increase the tendency to thrombosis and increase the risk of thromboembolism. Contraindications for use Breast cancer and other estrogen-dependent neoplasms, vaginal bleeding of unknown origin, endometriosis, thrombosis and thromboembolism (including in history), severe cardiovascular disease, liver failure, sickle cell anemia, herpes of pregnant women in history; pregnancy, lactation (breastfeeding). Use in pregnancy and lactation Contraindicated in pregnancy and lactation (breastfeeding). Use in hepatic impairment Contraindicated in hepatic impairment. Use in impaired renal function Use with caution in kidney disease. Special instructions Use with caution in bronchial asthma, epilepsy, migraine, heart and kidney diseases, as well as arterial hypertension, hypercalcemia, multiple sclerosis, systemic lupus erythematosus, otosclerosis. Can be used in combination with gestagens (including gestodene, dienogest, drospirenone, desogestrel, levonorgestrel) and cyproterone. Drug interactions Estrogens may reduce the effects of anticoagulants, antihypertensives and hypoglycemic agents. With the simultaneous use of ethinylestradiol and drugs that induce hepatic enzymes (barbiturates, carbamazepine, griseofulvin and rifampicin), a decrease in the level of ethinylestradiol in blood plasma is possible.

Ethinylestradiol – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English name

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Ethinylestradiol

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• Application of the substance Ethinylestradiol

• Contraindications

• Use during pregnancy and lactation

• side effects of ethinylestradiol

• Interaction

• Dosage and administration

• Trade names with the active substance Ethinylestradiol

Structural formula

Russian name

Ethinylestradiol

English name

Ethinylestradiol

Latin name

Aethinyloestradiolum ( genus Aethinyloestradioli)

Chemical name

(17 alpha)-19-Norpregna-1,3 ,5(10)-triene-20-yn-3,17-diol

Gross formula

C ₂₀ H ₂₄ O ₂

Pharmacological group of the substance Ethinylestradiol

Estrogens, gestagens; their homologues and antagonists

Anticancer hormonal agents and hormone antagonists

Nosological classification

ICD-10 code list

CAS code

57-63-6

Pharmacological action

Pharmacological action –

anabolic , hypolipidemic , estrogenic .

Characteristics

White or off-white fine crystalline powder. Practically insoluble in water, soluble in alcohols and vegetable oils.

Pharmacology

Interacts with specialized estrogen receptors in target cells. Rapidly absorbed through mucous membranes and skin. It undergoes hepatoenteric recirculation, accompanied by the effect of “first pass” through the liver, where it undergoes oxidation with the formation of 2-OH-ethinylestradiol and 2-methoxyethinylestradiol and subsequent glucuronidation and sulfonation. Metabolites are inactive, excreted in the urine and bile. Depending on the physiological state (pregnancy, individual phases of the ovarian-menstrual cycle, age, and other conditions), the excretion rate varies greatly. In the fallopian tubes, cervix, vagina, external genital organs, excretory ducts of the mammary glands, it increases the proliferation of the epithelium. Increases the sensitivity of the muscles of the uterus and tubes to substances that excite their motility. It has a hypocholesterolemic effect, increases blood levels of beta-lipoproteins, insulin sensitivity, improves glucose utilization. In high doses, it retains water and sodium in the body, inhibits erythropoiesis. In large doses, it reduces, and in small doses, it activates the secretion of FSH from the pituitary gland. In men, it inhibits spermatogenesis (atrophic changes may develop in the testicles) and suppresses the secretion of androgens. It has a weak anabolic effect. Under certain conditions, it exhibits contraceptive properties (it is an integral part of a number of oral contraceptives).

Use of the substance Ethinylestradiol

Some forms of endocrine infertility, severe pathological menopause, dysfunctional uterine bleeding, androgen-dependent prostate cancer, some forms of breast cancer.

Contraindications

Hypersensitivity, thrombophlebitis, active hepatitis, liver cirrhosis, arterial hypertension, breast and endometrial cancer, porphyria, pregnancy.

Pregnancy and lactation

Category of effect on the fetus according to FDA – X.

Side effects of the substance Ethinylestradiol

Violation of calcium metabolism, edematous syndrome, nausea, headache, thromboembolic syndrome, arterial hypertension; men have gynecomastia.

Interactions

Efficiency is reduced by barbiturates (accelerate oxidation).

Method of administration and doses

IM, for amenorrhea and oligomenorrhea — 0.02–0.1 mg/day for 20 days, then progesterone is administered intramuscularly for 5 days — 5 mg/day . With dysmenorrhea, treatment begins on the 4-5th day of the menstrual cycle – 0.01-0.03 mg / day (in 3 doses) for 20 days, the course of treatment is repeated every 2-3 months. To stop lactation, it is prescribed in the first three days after childbirth, 0.02 mg 3 times a day, then in the next three days – 0.01 mg 3 times a day, then – 0.01 mg / day once for 3 days . In the treatment of acne vulgaris – 0.