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Drospirenone and Ethinyl estradiol - Uses, Dosage, and Side Effects

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A birth control pill that contains two types of hormones, Drospirenone, and Ethinyl estradiol, helps to prevent pregnancy when taken properly.

Medically reviewed by

Dr. Monica Mathur

Published At January 30, 2023
Reviewed AtMarch 28, 2024


Drospirenone and Ethinyl estradiol is a birth control pill that contains female hormones that inhibit ovulation (the release of an egg from an ovary). Changes in the uterine lining and cervical mucus are also caused by Drospirenone and Ethinyl estradiol, making it more difficult for sperm to reach the uterus and a fertilized egg to attach to the uterus.

How Do Drospirenone and Ethinyl estradiol Work?

To prevent pregnancy, Drospirenone and Ethinyl estradiol are used as contraception. This medication is also used to treat moderate acne in women over 14 who have started menstruating and want to use birth control pills.


Drospirenone and Ethinyl estradiol treat moderate acne and premenstrual dysphoric disorder (PMDD) and prevent pregnancy. Drospirenone and Ethinyl estradiol can be taken alone or in combination with other medications. Drospirenone and Ethinyl estradiol belongs to the acne agents, systemic, estrogen, progestins, and contraceptives. It is unknown whether Drospirenone and Ethinyl estradiol are safe and effective in children under 14. This medication will not protect one from sexually transmitted diseases or acquired immunodeficiency syndrome (AIDS). In addition, it is ineffective as an emergency contraception method, such as after unprotected sexual contact.


For Oral Administration (tablets):

To use for contraception (to avoid pregnancy), PMDD, or acne:

  • Drospirenone and Ethinyl estradiol for Adults and Teenagers: One yellow tablet (active) is taken every day at the same time for 21 days, followed by one white (inert) tablet every day for seven days per menstrual cycle.

  • For Children: The doctor will determine the appropriate use and dosage.


  • Do not use it if a woman is pregnant or has recently had a baby.

  • If a person has an adrenal gland disorder, kidney disease, heart disease, uncontrolled high blood pressure, coronary artery disease, undiagnosed vaginal bleeding, circulation problems, liver disease or liver cancer, or severe migraine, the medicine must be avoided.

  • If one has major surgery, if one smokes and is over 35, or if one has ever had a heart attack, stroke, blood clot. Drospirenone and Ethinyl estradiol must not be used.

  • This medication may increase the chances of developing blood clots, stroke, or heart attack.

  • Smoking increases the risk of blood clots, stroke, and heart attack. Therefore, one should not take this medication if one smokes and is over 35.

For Patients:-

What Must Be Known About Drospirenone and Ethinyl estradiol?

Drospirenone and Ethinyl Estradiol tablets prevent ovulation and pregnancy. It treats acne and premenstrual dysphoric disorder (PMDD). It is a type of medication known as an oral contraceptive. It has hormones estrogen and progestin.

Learn More about Drospirenone and Ethinyl Estradiol:-

When and How Often to Take Drospirenone and Ethinyl estradiol?

  • Read these instructions before taking the pills or when unsure what to do.

  • Take one pill every day or as directed by the physician. Take one pill after the meal in the evening or at night.

  • During the initial days, many women experience light bleeding at unexpected times or may feel sick to their stomachs. Do not stop taking the pill if symptoms like spotting, light bleeding, or nausea are noted. The issue will usually resolve itself. If it does not go away, check with the healthcare provider.

How Effective Are Drospirenone and Ethinyl estradiol?

The combination of Ethinyl estradiol 20 grams and Drospirenone 3 mg (milligrams) yields a combined oral contraceptive with a low estrogen dose of 3 mg. Its primary mechanism of action is to prevent ovulation by suppressing hormone and follicle-stimulating hormone levels.

Things to Inform the Doctor Before They Prescribe Drospirenone and Ethinyl Estradiol:

Inform the doctor about the following;

  • Abnormal vaginal bleeding.

  • Adrenal gland disease.

  • Blood vessel disease or blood clots.

  • Heart disease or recent heart attack.

  • High blood pressure.

  • High cholesterol.

  • Breast, cervical, endometrial, ovarian, liver, or uterine cancer.

  • Diabetes (a metabolic disease that causes elevated blood sugar levels).

  • Gallbladder disease.

  • Stroke.

  • Systemic lupus erythematosus (SLE) (an inflammatory autoimmune disease).

  • Tobacco use.

  • Kidney disease.

  • Liver disease.

  • Migraine headaches.

  • An unusual or allergic reaction to estrogens, progestins, other medications, foods, dyes, or preservatives.

  • Pregnant or trying to get pregnant.

  • Breast-feeding.

Starting Drospirenone and Ethinyl estradiol:-

How to Take Drospirenone and Ethinyl estradiol?

It is essential to take Drospirenone and Ethinyl Estradiol tablets simultaneously every day, preferably after the evening meal or bedtime, with some liquid as needed. Drospirenone and Ethinyl Estradiol tablets can be taken at any time of day. The Drospirenone and Ethinyl estradiol tablet pack contains 21 yellow pills (with hormones) that should be taken for three weeks, followed by seven white to off-white pills (without hormones) that should be taken for one week.

Things to Do One Starts Taking Drospirenone and Ethinyl Estradiol:

After starting, Drospirenone and Ethinyl estradiol schedule regular appointments with the doctor to conduct a physical and diagnostic test to detect abnormalities; based on the test results, the doctor will recommend dose continuation, reduction, elevation, or drug interruption.

Look Out for Side Effects:

  • Skin rash, hives, itching, and swelling of the lips, tongue, face, or throat are examples of allergic reactions.

  • Pain, warmth in the leg, swelling, shortness of breath, and chest pain are all symptoms of a blood clot.

  • Gallbladder issues include severe stomach pain, vomiting, and fever.

  • Blood pressure elevation.

  • Liver damage manifests as right upper abdominal pain, dark yellow or brown urine, nausea, light-colored stool, yellowing skin or eyes, unusual weakness, and fatigue.

  • Migraines or headaches that are new or worsening.

  • Numbness or weakness of the face, arm, or leg; difficulty speaking; confusion, difficulty walking; dizziness, loss of balance or coordination; severe headache; and vision change.

  • Vaginal discharge, odor, and itching that is unusual.

  • Depression.

Dietary Alterations:

Give the doctor a list of all the medications, herbs, non-prescription drugs, and dietary supplements one takes. Inform them about smoking, consuming alcohol, or using illegal drugs to interact with the medications.

What Should Be Done if a Dose Is Missed?

If someone misses one yellow pill, take it as soon as possible and continue with the regular schedule. If a person misses two yellow pills in week one or two, take them as soon as possible, followed by the next two pills the following day. After missing a dose, use the second form of birth control (condom, spermicide) for seven days.

For example, if a person misses two yellow pills in the third or fourth week or three or more yellow pills in the week:

Day one begins: Throw the rest of the pack away and start a new pack the next day.

Start on Sunday: Take one pill per day until Sunday, discard the rest of the pack, and begin a new one that same day. To avoid pregnancy, use the second form of birth control (such as a condom or spermicide) for seven days after missing a dose. If one misses the period for two months, consult the doctor because there can be chances of pregnancy. If a person misses any of the seven white pills in the fourth week, throw them away.

What Should Be Done to Treat Drospirenone and Ethinyl estradiol Overdose?

There are no reports of serious adverse effects from an overdose, including child ingestion. However, in females, overdosage may result in withdrawal, bleeding, and nausea. DRSP (Drospirenone) is an analog of Spironolactone with anti-mineralocorticoid properties. In cases of overdose, serum potassium and sodium concentrations and evidence of metabolic acidosis should be monitored.

How to Store Drospirenone and Ethinyl estradiol?

Store at 25 degrees Celsius (77 degrees Fahrenheit); excursions to 15 to 30 degrees Celsius (59 to 86 degrees Fahrenheit) are permitted.

Store the medication at room temperature in a tightly sealed container away from heat, moisture, and direct light. Prevent freezing. Keep out of children's reach. Do not keep expired or no longer-needed medications. Inquire with the healthcare provider about properly disposing of any medications that are no longer required.

Handling of Drospirenone and Ethinyl estradiol:

The biconvex faces of the film-coated tablets are rounded, and one side is embossed with a regular hexagon shape. There are 28 film-coated tablets in each blister pack.

How to Dispose of Drospirenone and Ethinyl estradiol?

Unwanted medications should be disposed of in a specific manner. Avoid flushing this medication down the toilet. Instead, a medicine take-back program is the best way to dispose of your medication. Learn about take-back programs by contacting the local garbage or recycling department.

Avoid Self-Medication:

Avoid taking tablets for a condition that was not prescribed. Avoid suggesting the tablet to people with the same symptoms as the medication affects each individual differently. Instead, consult the physician, discuss with them, and then take medicine.

Staying On Drospirenone and Ethinyl estradiol:-

Tips to stay on track with Drospirenone and Ethinyl estradiol:

  • Take the drug as directed by the physician.

  • Do not miss a dose or overdose to compensate for a missed dose. Inform the physician immediately.

  • Also, schedule regular appointments with the physician to monitor the disease progression and recommend dose alteration.

For Doctors:-


This medication combines two hormones, estrogen (Ethinyl estradiol) and progestin (Drospirenone). This medication is used to avoid pregnancy. It prevents pregnancy, and birth control pills may make the periods more regular. Reduces painful periods and decreases blood loss and the risk of ovarian cysts. This medication does not protect against sexually transmitted diseases such as HIV (human immunodeficiency virus), gonorrhea, or chlamydia.


Mechanism of Action:

The suppression of gonadotropin release from the hypothalamus is the mechanism of action. With gonadotropin suppression, ovarian stimulation, and follicular maturation are impossible, and estradiol levels are low due to decreased follicular production. This is because follicles primarily produce estradiol, and as follicular maturation decreases, so does estradiol production.


The oral contraceptive regimen contains 24 active film-coated tablets containing 3 mg Drospirenone and 0.02 mg Ethinyl estradiol. Betadex, as a clathrate, stabilizes these hormones in the tablet. The rest of the regimen comprises four inert film-coated tablets. The Drospirenone structure is a 17 alpha spironolactone analog.


Active Ingredient:

Ethinyl estradiol and Drospirenone.

Inactive Ingredients:

Ferric Oxide yellow, Hypromellose, Lactose Monohydrate, Magnesium Stearate, Polyethylene Glycol, Starch, Corn, Talc, Titanium dioxide.


Due to first-pass effects, Drospirenone has an absolute bioavailability of approximately 76 percent. The maximum plasma concentration of Drospirenone occurs within one to two hours after oral administration. The estimated range is between 60 and 87 ng/mL (nanograms per milliliter).


The serum concentrations of Drospirenone and Ethinyl estradiol decrease in two stages. Drospirenone has an apparent volume of distribution of about 4 L/kg (liter per kilogram), and Ethinyl estradiol has an apparent volume of distribution of about 4 to 5 L/kg. Drospirenone does not bind to sex hormone-binding globulin (SHBG) or corticosteroid-binding globulin (CBG), but it does bind to other serum proteins in about 97 percent of cases. The free fraction remained unchanged after three cycles of multiple dosing. Ethinyl estradiol is highly but non-specifically bound to serum albumin and increases serum concentrations of both SHBG and CBG.


Preclinical and clinical studies have investigated the pharmacokinetic profile of 3 mg DRSP/20 g (grams) Ethinyl estradiol-24/4. When evaluating a single tablet containing only DRSP, the absolute bioavailability of DRSP is approximately 76 percent, as measured after first pass metabolism through the liver. After the first pass, considering systemic conjugation, the absolute bioavailability of Ethinyl estradiol (without the DRSP component) is approximately 40 percent. The absolute bioavailability of a combination tablet containing 3 mg DRSP and 20 g Ethinyl estradiol, as used in the currently marketed OCP (oral contraceptive pill), has not been studied. When the DRSP or Ethinyl estradiol tablet is taken with food, the concentrations are reduced by 40 percent. Food consumption influences the rate but not the extent of absorption, which is not considered clinically significant. The liver and small bowel mucosa both metabolize Ethinyl estradiol, a synthetic hormone that is highly protein bound to albumin in the circulation. Aromatic hydroxylation is the primary mode of Ethinyl estradiol metabolism, producing a wide range of free and glucuronide or sulfate-conjugated metabolites. This synthetic estrogen metabolite is methylated and glucuronidated after two hydroxylation by cytochrome P450 (CYP) 3A4 enzymes before being excreted in the urine and feces.


Drospirenone serum concentrations have a terminal disposition phase half-life of about 30 hours after single and multiple-dose regimens. After ten days, Drospirenone excretion was nearly complete, with feces excreting slightly more than urine. Only trace amounts of unchanged DRSP were excreted in urine and feces, indicating that DRSP was extensively metabolized. In urine and feces, at least 20 different metabolites were discovered. Glucuronide and sulfate conjugates make up approximately 38 to 47 percent of the metabolites in urine. About 17 to 20 percent of the metabolites were excreted as glucuronides and sulfates in feces.


Co-exposure to Drospirenone and Ethinyl estradiol increases genotoxicity, which may pose a risk of cancer development in women who take these drugs for an extended period.

Warnings and Precautions:

  • Keep children and pets out of reach.

  • Store between 15 and 30 degrees Celsius at room temperature (59 and 86 degrees Fahrenheit). After the expiration date, throw away any unused medication.

  • Women should not use oral contraceptives over the age of 35 who smoke. Cigarette smoking raises the risk of serious cardiovascular side effects from using a combination of oral contraceptives.

Dosage and Forms:

Dosage: 3 mg/0.02 mg, 3 mg/0.03 mg.

For Contraception: One active tablet (3 mg Drospirenone/0.03 mg Ethinyl estradiol) PO every day for 21 days, later one inert tablet PO (per os or by mouth) every day for seven days.

For Moderate Acne Vulgaris: Indicated in women with moderate acne, but only if oral contraception is used as a method of birth control. One active tablet (3 mg Drospirenone/0.02 mg Ethinyl estradiol) PO every day for 24 days, later one inert tablet PO every day for four days.

For Premenstrual Dysphoric Disorder: Indicated for a premenstrual dysphoric disorder, but only if oral contraception is used as a method of birth control. One active tablet (3 mg Drospirenone/0.02 mg Ethinyl estradiol) PO every day for 24 days, later one inert tablet PO every day for four days.

Administration of the Drug:

Take one tablet orally simultaneously every day or as directed by the physician. When pills are missed or taken incorrectly, the failure rate rises.

Considerations for Administration:

  • During the first seven days of therapy, women should be advised to use additional nonhormonal contraception.

  • Administer tablets simultaneously daily in the order specified on the blister pack calendar.

  • Increased risk of venous thromboembolism (VTE) after delivery with combined hormonal contraceptives; risk decreases rapidly after 21 days but does not return to normal until 42 days after delivery.

  • In postpartum women without additional VTE risks, the CDC (Centers for Disease Control and Prevention) recommends waiting 21 to 42 days before starting therapy.

  • Postpartum women who do not breastfeed or have had an abortion in the second trimester should wait four weeks before starting the therapy.

  • Women who have given birth via cesarean section should wait for six weeks before starting therapy.


  • Hypersensitivity.

  • Breast cancer or history of breast cancer.

  • Atherosclerotic disease (stroke, MI-myocardial infarction), thrombophlebitis, DVT (deep vein thrombosis), and thrombogenic valvular disease or has a history.

  • Uncontrolled hypertension.

  • Diabetes with vascular complications.

  • Migraine.

  • Undiagnosed uterine abnormal bleeding.

  • Benign or malignant liver tumors, hepatic impairment, or development of jaundice with prior oral contraceptive use.

  • Pregnancy.

  • Renal dysfunction.

  • Adrenal insufficiency.

Clinical Studies for Drospirenone and Ethinyl estradiol:

2,629 subjects completed 33,160 cycles of use without any other contraception in clinical efficacy studies lasting up to two years. The subject's average age was 25 to 54.7 years. The ages ranged from 16 to 37. 83 percent were Caucasian, 1 percent Hispanic, 1 percent Black, 1 percent Asian, 1 percent other, 1 percent missing data, 14 percent not inquired, and 1 percent unspecified. Pregnancy rates were less than one per 100 woman-years of use in the clinical trials.

Drug Interactions:

Although certain medicines should never be used, two different medicines may be used together even if an interaction occurs. In these cases, the doctor may want to adjust the dose or take other precautions. It is not recommended to take this medication with any of the following medications. The doctor may decide not to treat with this medication or may change some of the medications a person is currently taking.

The following medications include;

  • Boceprevir.

  • Dasabuvir.

  • Paritaprevir.

  • Ritonavir.

  • Tranexamic acid.

  • Ombitasvir.

Certain medicines should not be taken while eating specific types of food because interactions may occur. Using alcohol or tobacco while taking certain medications may also result in interactions. Using this medicine in conjunction may increase the risk of certain side effects, but it may be unavoidable in some cases. If one takes these medications together, the doctor may change the dose or frequency of administration or give special instructions about food, alcohol, or tobacco use.

Other Specifications:-

Drospirenone and Ethinyl estradiol in Pregnant Women:

Women who use during early pregnancy have little to no increased risk of birth defects. Epidemiologic studies and meta-analyses have found no increased risk of genital or non-genital birth defects following prenatal or early pregnancy exposure to low-dose COCs (combined oral contraceptives). COCs to induce withdrawal bleeding should not be used as a pregnancy test. COCs should not be used to treat threatened or habitual abortions during pregnancy.

Drospirenone and Ethinyl estradiol in Lactating Women:

When possible, advise the nursing mother to use alternative contraception until the child has been weaned. COCs that contain estrogen can reduce milk production in breastfeeding mothers. This is less likely to happen once breastfeeding is established, but it can happen at any time in some women. Breast milk contains trace amounts of oral contraceptive steroids and metabolites.

Drospirenone and Ethinyl estradiol in Pediatric Group:

Drospirenone and Ethinyl estradiol tablets are safe and effective in women of reproductive age. The efficacy for postpubertal adolescents under 18 and older is expected to be the same. This product should be used after menarche (the first appearance of menstruation).

Drospirenone and Ethinyl estradiol in Geriatric Patients:

Tablets of Drospirenone and Ethinyl estradiol have not been studied in postmenopausal women and are not recommended in this population.

Drospirenone and Ethinyl estradiol in Renal Impairment Patients:

Drospirenone and Ethinyl estradiol is contraindicated in patients with renal impairment.

Drospirenone and Ethinyl estradiol in Hepatic Impairment Patients:

Drospirenone and Ethinyl estradiol is contraindicated in patients with hepatic impairment.

Frequently Asked Questions


What Are the Applications of Drospirenone and Ethinyl Estradiol?

The oral contraceptive combination of Drospirenone and Ethinyl Estradiol is used to prevent pregnancy. It is a type of birth control pill that contains two types of hormones, Drospirenone and Ethinyl Estradiol, and prevents conception when taken appropriately. Each month, it prevents a woman's egg from fully maturing.


What Are the Side Effects of Drospirenone and Ethinyl Estradiol?

The side effects of  Drospirenone and Ethinyl Estradiol are as follows:
- Nausea.
- Bloating.
- Vomiting.
- Missed or irregular periods.
- Weight change.
- Breast tenderness.
- Headache.
- Ankle or foot edema (fluid retention).
- Vaginal bleeding (spotting).


Do Ethinyl Estradiol and Drospirenone Cause Weight Gain?

According to research, it has been found that both Ethinyl Estradiol and Drospirenone do not significantly increase body weight compared to other oral contraceptives. However, they may cause weight gain in some women mainly due to changes in appetite and water retention or if the medication is discontinued.


Are Periods Stopped With Drospirenone?

Drospirenone works by stopping the development of a woman’s egg and thus prevents the egg from accepting sperm, thereby preventing fertilization or pregnancy. The bleeding normally ceases after about a week. If the bleeding lasts more than a week after taking hormonal contraceptives on schedule, it is advised to visit the doctor.


What Are the Advantages of Ethinyl Estradiol and Drospirenone?

The combination of Drospirenone and Ethinyl Estradiol is used to prevent pregnancy. Its other advantages include the following:
- Regulating periods.
- Decrease in blood loss.
- Acne treatment.
- Decreased risk of ovarian cysts.
- Decrease in painful periods.


Is Drospirenone a Hair-Growth Stimulant?

Drospirenone has high anti-androgen activity, and therefore, it reduces acne and hair development by blocking the androgen action on the oil and hair follicles. Drospirenone mainly opposes or blocks the testosterone hormone that is primarily responsible for hair fall.


When Do Periods Occur After Using Drospirenone Pills?

Drospirenone pills are available in two packings containing 21 pills and 28 pills (hormones), respectively, along with seven inactive or without hormone pills, which are to be taken as directed by the doctor. Periods usually occur after three days of taking the last active tablet in the cycle, mainly during the fourth week of the pack. However, the doctor should be consulted if the periods did not occur after taking the pill.


Can Drospirenone Help Get Rid of Acne?

Drospirenone's antiandrogenic function means that it inhibits the male sex hormones (testosterone) that cause acne. The drug is approved by the United States FDA (Food and Drug Administration) for use in combination therapy for acne treatment due to its anti-androgenic properties. Thus, it helps to get rid of acne.


Which Is Better, Taking Birth Control Pills in the Morning or at Night?

If the combination tablet that contains the hormones estrogen and progestin is taken, then pregnancy is prevented anyway as long as it is taken every day. It makes no difference whether it is taken in the morning or evening as long as it is taken at the same time every day.


How Long Do One Bleed on Drospirenone?

The bleeding normally ceases after about a week. If the bleeding lasts more than a week, it is best to consult the doctor. In some women, vaginal bleeding or spotting may occur for the first few months of using this medication. However, if the bleeding dose lasts for more than three months, they must consult the doctor immediately.


Can Drospirenone Cause Infertility?

No, Drospirenone does not cause infertility. The women who have used hormonal birth control are exactly as likely as women who have never used hormonal contraception to become pregnant. The duration and type of any contraceptive pill do not have any effects on the women’s ability to conceive after termination of pregnancy.


How Safe Is Drospirenone Ethinyl?

This medicine may occasionally cause serious and potentially fatal blood clot complications such as deep vein thrombosis (blood clots), pulmonary embolism (blockage of blood flow in lungs), stroke, and heart attack. Though this medication is more effective than other contraceptive pills, the safety of the drug is being questioned by the FDA (Food and Drug Administration).
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Dr. Monica Mathur
Dr. Monica Mathur

Obstetrics and Gynecology


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