Ethinyl Estradiol and Norgestimate (oral)

Overview

Ethinyl estradiol and norgestimate is a combination contraceptive used for pregnancy prevention. Produced under the brand name Estarylla, this birth control pill contains two hormones, norgestimate and ethinyl estradiol. The combination is also used for acne treatment in females (at least 14 years of age) who are already having menstrual periods and also wish to take this medicine for birth control purposes.

Ethinyl estradiol and norgestimate is available in tablet form. It is administered orally and works by preventing ovulation during the woman's menstrual cycle. It also makes the vaginal secretion thicker to prevent fertilization by stopping sperm from getting into contact with the egg. Should fertilization occur, the drug causes changes in the uterine lining to prevent the fertilized egg from attaching onto the womb.

Besides preventing fertilization, this birth control pill can also make a woman's periods more regular and reduce both painful periods and excessive blood loss. It also reduces the woman's risk of contracting ovarian cysts.

Conditions Treated

  • Birth control
  • Acne

Type Of Medication

  • Hormonal contraceptive

Side Effects

Even though it may be rare, some women may experience severe side effects when taking this contraceptive. Talk to your healthcare provider or seek help when you experience any of the following side effects after taking this contraceptive:

  • Signs of allergic reactions, including rashes, blisters on the skin, hives, wheezing, tightness of the throat and chest, breathing and speaking difficulties or swelling on the limbs, face, mouth and throat
  • Signs of liver disorders, including dark urine, fatigue, stomach pains, yellowing skin and eyes and light-colored stool
  • Coughing up blood
  • Dizziness and passing out
  • Numbness or weakness on one side of the body, imbalance, speaking difficulty and blurred vision
  • Depression and mood changes
  • Severe migraine and headache
  • Difficulty passing urine or change in how much urine is passed
  • Itching and vaginal discharge
  • Bulging eyes
  • Spotting or vaginal discharge
  • A lump in the breast, soreness and nipple discharge
  • Vaginal bleeding

There are some other ethinyl estradiol and norgestimate side effects, too. Call your healthcare provider if any of these side effects bother you:

  • Headache
  • Weight gain
  • Stomach upsets, nausea and vomiting
  • Gas
  • Enlarged, tender breast
  • Belly pain
  • Nervous feeling
  • Irregular periods

This contraceptive may cause dark patches on your skin. Avoid exposure to direct sunlight or UV radiation and use sunscreen and protective clothing when outdoors during sunny days.

Not all these side effects may occur. Call your healthcare provider if you have questions about these side effects. You may also report the side effect to the FDA at 1-800-FDA-1088.

Dosage

Read and understand the Patient Information Leaflet provided by your pharmacist before you start using this contraceptive and each time you go for a refill. The leaflet contains vital information on when to take your contraceptive and what you should do in an event of a missed dose. Ask your healthcare or pharmacist any questions you might be having.

Take Estarylla orally as directed by your healthcare provider, usually once per day. It helps to pick a time of the day that is easy for you to remember, and take your contraceptive at the same time of the day.

It is imperative that you continue taking this pill exactly as directed by your healthcare provider. As with most brands of birth control pills, the levels of progestin and estrogen hormones in each active pill varies based on the time of the cycle. Thus, it is crucial that you follow your package's instructions to identify and start with the first pill in the pack, and take them in the right order. Avoid skipping doses. Pregnancy is more likely if you skip a dose, start your new pack late in the cycle or take your contraceptive at irregular times of the day.

Diarrhea and vomiting can prevent your contraceptive from working well. If you are prone to vomiting or diarrhea, especially after taking your pill, you should consider using a back-up birth control method, such as condoms. Check with your healthcare provider or follow the information in your pack's Patient Information Leaflet for more details.

Taking your contraceptive after dinner or just before bedtime may help if your nausea or stomach upset are associated with the medication. That said, you are free to schedule your contraceptive at a time of day that is convenient for you. No matter what your dosing schedule is, be sure to take your contraceptive at the same time each day, 24 hours apart. Consult your healthcare provider if you have any questions.

Your Estarylla pack contains 21 active pills. It may also come with seven non-medication reminder pills. Take one active pill (with hormones) once daily in a row for 21 days. If you are using a pack with 28 pills, take the inactive pill once per day for seven consecutive days after taking the last active pill, unless directed otherwise by your healthcare provider. If you are using the pack with 21 pills, do not take any pill for seven days, unless otherwise directed by your healthcare provider. You should have your menses during the fourth week of your cycle. After taking the last inactive pill in your pack or when you've gone seven days without taking an active pill, start a new pack the following day, whether or not you get your period. It is important that you consult your healthcare provider in an event of a missed period.

If you are using this contraceptive for the first time and you are not making the switch from another hormone-based birth control method, such as a patch, take the first pill in the pack on the first Sunday after the onset of your menses or on day one of your cycle. If your first day of the period falls on a Sunday, start taking your contraceptive on that day. For your first cycle of use, it is important that you use a back-up form of non-hormonal birth control, such as a condom or spermicide, for the first seven days, to prevent conception and give Estarylla enough time to work. However, you do not need to use back-up birth control method if you are starting your medication on the first day of your period.

If you are switching from other forms of hormonal birth control, like a patch or other oral contraceptives, to Estarylla, be sure to ask your healthcare provider for direction on how to best make the switch.

How to best take ethinyl estradiol norgestimate

As already mentioned, use this contraceptive as directed by your healthcare provider. Read the information provided in the pack's Patient Information Leaflet and follow the instructions therein to the letter.

  • Take Estarylla orally at the same time of day
  • You may take your contraceptive with food if it triggers stomach upsets
  • If you are combining Estarylla with colesevelam, take Estarylla at least four hours after colesevelam
  • Avoid skipping doses, even if you do not have sex regularly
  • If you diarrhea or vomit after taking Estarylla, the contraceptive may not be effective in preventing a pregnancy. If you throw up or have diarrhea within three to four hours after taking your pill, take another one. If the diarrhea or vomiting goes on for more than one day, use other forms of birth control and inform your healthcare provider.
  • If you miss two consecutive periods, take a pregnancy test before starting another pack

In case of a missed dose

Skipping a day without taking your medication can increase your chances of conceiving. If you skip one active tablet, take two tablets on the day that you remember before resuming your regular daily tablet for the remaining days of the cycle.

If you skip two active tablets consecutively in the first or second week, take two tablets daily for two consecutive days. Then resume your regular dosage for the rest of the pack. Consider using a non-hormonal back-up birth control for at least seven days following the missed tablets.

If you missed two active tablets in a row in week three, dispose of the rest of the pack and start a new pack the same way you would if you are a Day 1 starter. If you are a Sunday starter, keep taking a tablet daily until Sunday, before discarding the rest of the pack to open a new pack that Sunday.

You may miss your period if you skip two or more pills in a row. If you miss your period for two consecutive months, contact your healthcare provider for a pregnancy test.

If you skip a reminder pill, dispose of it and keep taking one reminder pill daily until you empty the pack.

Call the Poison Control center or get medical care immediately if you overdose this contraceptive.

Starting Estarylla after a miscarriage or abortion

First trimester miscarriage or abortion

You may start Estarylla immediately after the first-trimester miscarriage or abortion. You do not need an additional birth-control method if you start Estarylla immediately. If you do not start Estarylla within five days after termination of the pregnancy, you should use additional non-hormonal birth-control, such as condoms, for the first seven days of your first cycle pack.

Second-trimester miscarriage or abortion

Wait for up to four weeks before starting Estarylla following a second-trimester abortion or miscarriage. Starting this contraceptive immediately can increase your risk of thromboembolic disease. Start Estarylla in table for Day 1 or Sunday start, as you please. If you are starting on Sunday, be sure to use a back-up birth control method (e.g spermicide or condom) for the first seven days of the first cycle pack.

Starting Estarylla after childbirth

Wait for up to four weeks after delivery before starting Estarylla, to avoid the risk of contracting thromboembolic disease. Start using the contraceptive by following instructions given above.

Estarylla is not recommended for use by breastfeeding mothers

If you are yet to have a period postpartum, consider the possibility of ovulating and conceiving prior to using the contraceptive.

Three ways to remember the order in which you should take Estarylla

  • Always follow the sticker with the days of the week
  • Always take your pills from left to right
  • Always finish all the pills in your pack

Interactions

Effects of other medications on combined oral contraceptives (COCs)

Substances that lower the plasma levels in combined oral contraceptives

Drugs, vitamins or herbal supplements that affect activities of certain enzymes, like cytochrome P450 3A4, may lower the plasma levels of the contraceptive and significantly reduce its efficacy, while increasing breakthrough bleeding. Such medications and herbal products include barbiturates, phenytoin, carbamazepine, oxcarbazepine, bosentan, griseofulvin, drugs that contain St. John's wort, and rifabutin.

Interactions between COCs and these drugs may trigger breakthrough bleeding or failure of the contraceptive to prevent conception. It is thus advisable that back-up birth control methods are used when enzyme inducers are used alongside COCs. Such back-up birth control methods should be used for 28 days after discontinuing the enzyme inducer, to give the contraceptive adequate time to be effective.

Colesevelam and Estarylla

This is a bile acid sequestrant that is administered together with a COC. It is known to lower the contraceptive's efficiency if they are administered within three hours of each other.

Substances that increase the plasma concentration of COCs.

Administering atorvastatin or rosuvastatin together with Estarylla may increase the AUC for ethinyl estradiol (EE) by up to 25%. Acetaminophen and ascorbic acid are also known to increase plasma EE concentrations by inhibiting conjugations. Additionally, cytochrome P450 3A4 inhibitors like voriconazole, itraconazole, grapefruit juice, ketoconazole and fluconazole may increase plasma hormone concentrations.

How Estarylla affects other medications

  • The ethinyl estradiol present in Estarylla may inhibit metabolism of other compounds like theophylline, prednisolone, cyclosporine, voriconazole and tizanidine, and significantly affect their plasma concentrations.
  • Estarylla has been shown to lower plasma concentrations of clofibric acid, acetaminophen, morphine, lamotrigine, salicylic acid and temazepam. This reduces seizure control, hence the need for adjustment in dosage of these medications. Women who are on thyroid hormone replacement treatment may require an increase in thyroid hormone dosage, because the serum concentration of thyroid-binding globulin increases with the use of Estarylla.

Inteference with laboratory test results

The use of Estarylla may influence the outcome of certain laboratory tests, such as lipids, coagulation factors, binding proteins and glucose tolerance.

Ethinyl estradiol norgestimate

warnings

It is important that you inform your doctor of whether or not you have any of the following conditions before taking this medication:

  • If you are allergic to ethinyl estradiol, norgestimate or any ingredient used in the manufacture of this medication
  • If you are allergic to any medication, be sure to tell your doctor about the allergies, as well as the signs you have experienced before, such as hives, rashes, itching, breathing difficulty, coughs, wheezing, swelling of the limbs or any other signs
  • If you have had any of these health complications before: breast and cervical cancer, blood clotting, diseased brain or arteries, heart valve problems, high cholesterol, high blood pressure, pancreatitis as a result of high blood triglycerides, liver tumor or disease, severe headache or migraine, diabetes or a tumor that is triggered by estrogen
  • If you have suffered from any of the following: cancer of the cervix or vagina, endometrial cancer, vaginal bleeding from unknown cause
  • If you have ever suffered from cancer whose growth was accelerated by hormones
  • If you turned yellow after taking a hormone based contraceptive or during pregnancy
  • If you are pregnant
  • If you are breastfeeding or planning to breastfeed
  • If you are taking ritonavir, paritaprevir and ombitasvir

Thromboembolic disorders and other vascular problems associated with Estarylla:

  • Stop taking Estarylla if you experience venous thromboembolic event (VTE) or an arteriole thrombotic event
  • Stop taking Estarylla if you experience unexplained loss of vision, diplopia, proptosis, retinal vascular lesions or papilledema. Go for retinal vein thrombosis checkup immediately
  • Subject to your doctor's advice, stop taking Estarylla at least four weeks before and two weeks after a major surgery or procedures that are likely to increase your risk of VTE. This contraceptive should also be avoided during, and after, a prolonged immobilization.
  • Start taking Estarylla no earlier than four weeks after giving birth if you are not breastfeeding. Your risk of postpartum VTE decreases after the 3rd postpartum week, while your chances of ovulating and conceiving increase
  • Use of Estarylla increases your risk of arteriole thrombosis, such as myocardial infarctions and strokes, especially if you have other risk factors for these events. This risk increases with age, especially in women over 35 years old who smoke
  • Estarylla should be used with caution if have a risk factor for cardiovascular disease

Impaired liver function

Do not use Estarylla if you have a liver disease, such as severe cirrhosis of liver or acute viral hepatitis. Discontinue this contraceptive if you develop jaundice. Estarylla is contraindicated in patients with a tumor in the liver. Hepatic adenomas have been linked to combined oral contraceptives like Estarylla. Studies have shown that long term use of this and other COCs increases the risk of developing hepatocellular carcinoma.

High blood pressure

Estarylla is contraindicated in women with vascular disease or uncontrolled hypertension. Women with controlled hypertension should be closely monitored while on this contraceptive and its use should be terminated if blood pressure rises significantly.

Hypertension has been reported in women taking this contraceptive and this is more likely in older women who use Estarylla for extended periods. Incidence of hypertension increases with rising levels of progestin.

Gallbladder disease

Studies suggest an increased risk for gallbladder disease among women on COCs. Use of these contraceptives may worsen existing gallbladder conditions.

Carbohydrate and lipid metabolic effects

Diabetic and prediabetic women who take Estarylla should be closely monitored, as Estarylla is known to decrease glucose tolerance. Alternative contraceptive should be considered for women with uncontrolled dyslipidemia. Women with hypertriglyceridemia, or a family history of the condition, may be at an increased risk of pancreatitis when on Estarylla.

Headache and migraine

Estarylla should be discontinued if the woman develops persistent, severe or recurrent headache. The contraceptive should also be discontinued in the case of severe or frequent migraine.

Bleeding irregularities and amenorrhea

  • Breakthrough or intracyclic bleeding and spotting may occur especially during the first three months of using Estarylla. Persistent bleeding should be checked for other causes, such as malignancy or pregnancy.
  • Some women may experience amenorrhea or oligomenorrhea while using Estarylla.

Depression

Women with a history of depression should be closely monitored and Estarylla discontinued if the depression is persistent or becomes severe.

Carcinoma of the cervix and breast

  • Estarylla is contraindicated in women who are currently suffering from, or have a history of, breast cancer, because breast cancer is sensitive to hormones.
  • Some studies have associated use of combined oral contraceptives with increased risk of intraepithelial neoplasia or cervical cancer.

Hereditary angioedema

Exogenous estrogen found in Estarylla may induce or exacerbate symptoms of angioedema in women with hereditary angioedema.

Chloasma

Chloasma may occur in women with a history of chloasma gravidarum during Estarylla. Women with tendency towards chloasma should avoid exposure to UV radiation or the sun while taking Estarylla.

Storage

Estarylla should be stored at room temperature (20 degrees C to 25 degrees C). The drug should be stored in a dry place, away from moisture and direct sunlight. All medications should be safely kept out of reach of pets and children. Check with your healthcare provider or pharmacist on how to get rid of unused medication. Do not flush down the toilet or kitchen sink.

Summary

Ethinyl estradiol and norgestimate is a combination oral contraceptive (COC) medication that contains synthetic versions of ethinyl estradiol and norgestimate hormones. It is taken orally to prevent ovulation and pregnancy. The contraceptive works by causing changes to the cervical mucus, as well as the uterine lining. These changes make it impossible for the sperm get into contact with and fertilize the egg released in the uterus. Should fertilization occur, it makes it difficult for the fertilized egg to attach to the uterus to complete conception.

Ethinyl estradiol and norgestimate can also be used for treating acne in women who are at least 14 years old and have already started menstruating.

This contraceptive should not be used by pregnant women or those who are breastfeeding. In addition, you should not use Estarylla if you have an uncontrolled hypertension, coronary artery disease, heart disease, circulatory problems (especially due to diabetes), undiagnosed bleeding through the vagina, liver cancer or liver disease, if you are taking certain hepatitis C medications, experience severe headache and migraine, if you smoke and are over 35 years of age, if you have major surgery, or if you have a history of stroke, heart attack, jaundice caused by birth control medication or pregnancy, blood clots, or cancer of the cervix, vagina, uterus or breast.

Smoking while on this contraceptive can greatly increase a woman's risk of stroke, blood clots and heart attacks. The risk increases when the woman is 35 years or older.

Like with other birth control pills, taking Estarylla can increase your risk of stroke and heart attack if you are overweight, have high blood pressure, high cholesterol, diabetes, or if you are obese or overweight. The risk of stroke is highest during the first year of using this contraceptive. Your risk of stroke and blood clot is also high when you resume taking this contraceptive after a break of four weeks or longer.

Before using this contraceptive, tell your healthcare of your provider if you:

  • Are pregnant or suspect that you may be pregnant
  • Are depressed or have a history of depression
  • Had yellowing of the eyes and skin as a result of pregnancy
  • Are breastfeeding or planning to breastfeed, as Estarylla may reduce the production of breastmilk. Additionally, traces of hormones in Estarylla may pass onto the infant via breastmilk. Talk to your healthcare provider about the best birth control method while breastfeeding.

Inform your healthcare provider about all the medications you are taking, including over the counter medications, herbal medications, supplements and vitamins. Estarylla may affect the efficiency of other medications, and other medications may also affect how well this contraceptive works.

Women using Estarylla and other hormonal birth control medications should be counselled about the following information:

  • Cigarette smoking greatly increases the risk of severe cardiovascular conditions when combined with oral contraceptive use, and women who are 35 years and older should not smoke while using COCs like Estarylla.
  • Increased risk of VTE is higher when starting or restarting a COC after a four week break.
  • Estarylla does not protect against, or treat, HIV, AIDS and other sexually transmitted diseases.
  • Estarylla should not be used during pregnancy. If pregnancy occurs during the use of this contraceptive, the patient should be advised to stop further use with immediate effect.
  • Take one pill orally on a daily basis. The medicine should be taken at the same time to ensure its efficiency.
  • Use alternative or back-up birth control methods, like condoms and spermicide, when enzyme inducers are co-administered with Estarylla.
  • Estarylla, like other combined oral contraceptives, may reduce production of breastmilk.
  • Women who are starting Estarylla postpartum, and who are yet to have their periods, should use an alternative, non-hormonal birth control method until they have taken an active Estarylla pill for seven consecutive days.
  • Some women may experience amenorrhea. A pregnancy test should be considered in the event of amenorrhea at the time of the first missed menses. Seek a pregnancy test should you miss your period for two consecutive months while on Estarylla.