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Ethinylestradiol

AEMPS

Estrogens. Natural and semisynthetic estrogens, plain

ATC code: G03CA01

Brand names: Yasmin (combination), Loestrin (combination), Ortho Tri-Cyclen (combination), Yaz (combination)

Updated · Methodology

Indications

A

Combined oral contraception

First line

Ethinylestradiol is the main estrogen component of most combined hormonal contraceptives. The dose ranges from 15 to 35 mcg depending on the product. With perfect use, the Pearl Index is less than 1. Modern formulations with 20–30 mcg ethinylestradiol balance efficacy and safety. Alternatives include COCs with natural estradiol or estradiol valerate for patients with thromboembolism risk factors.

Before prescribing, assess the CDC USMEC 2016 category: age, smoking, blood pressure, migraine with aura, history of thromboembolism, BMI and comorbidities.

Sources

  1. CDC: U.S. Medical Eligibility Criteria for Contraceptive Use, 2016 (2016)
  2. ГРЛС: Этинилэстрадиол – Государственный реестр лекарственных средств (2024)

ICD-10: Z30.0 · ICD-11: QA21.1

B

Acne and PCOS with hyperandrogenism

Second line

Selected COCs with ethinylestradiol (combined with drospirenone, norgestimate, cyproterone) are -approved for moderate acne in women of reproductive age who also need contraception. The effect develops over 3–6 months. Prescribed only when contraindications to combined hormonal contraception are absent and after discussion of risk-benefit balance with the patient (thromboembolism risk versus added benefit over standard anti-acne therapy).

Sources

  1. CDC: U.S. Medical Eligibility Criteria for Contraceptive Use, 2016 (2016)

ICD-10: L70.0 · ICD-11: ED80

B

Menopausal hormone therapy

Second line

As a component of menopausal hormone therapy, ethinylestradiol is rarely used – current international guidelines ( NG23, NAMS 2022) prefer transdermal natural estradiol due to a better safety profile. Ethinylestradiol has stronger effects on hepatic coagulation factor synthesis and raises venous thromboembolism risk. Used only in selected clinical situations when modern MHT preparations are unavailable.

Sources

  1. CDC: U.S. Medical Eligibility Criteria for Contraceptive Use, 2016 (2016)

ICD-10: N95.1 · ICD-11: GA30.00

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

F

COCs in women over 35 who smoke

Not recommended

In women over 35 who smoke more than 15 cigarettes per day, combined hormonal contraception with ethinylestradiol is contraindicated (CDC USMEC 2016 category 4). The combination of nicotine toxicity and estrogen effects on coagulation raises risks of myocardial infarction, stroke and venous thromboembolism to unacceptable levels. Alternatives: progestin-only methods (levonorgestrel IUD, progestin-only pill, implant), barrier methods.

Sources

  1. CDC: U.S. Medical Eligibility Criteria for Contraceptive Use, 2016 (2016)
F

Migraine with aura

Not recommended

In women with migraine with aura, combined hormonal contraception with ethinylestradiol is contraindicated (CDC USMEC 2016 category 4) due to increased ischemic stroke risk. Alternatives: progestin-only methods, barrier methods, copper IUD. In migraine without aura, the decision is individualized based on age and other risk factors (USMEC categories 2–3).

Sources

  1. CDC: U.S. Medical Eligibility Criteria for Contraceptive Use, 2016 (2016)

ICD-10: G43.1 · ICD-11: 8A80.1

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

A synthetic estrogen, the primary estrogen component of most combined oral contraceptives. Binds estrogen receptors in the hypothalamus and pituitary, suppressing FSH and LH secretion. This prevents ovulation and maintains a stable hormonal background when combined with a progestin. Additional effects: increased hepatic synthesis of transport proteins (including sex hormone–binding globulin), favorable lipid effects, mineralocorticoid effects at some doses.

Safety

Boxed warning

FDA boxed warning: smoking significantly increases the risk of serious cardiovascular events on combined hormonal contraception. Risk increases with age, particularly after 35, and with smoking intensity. Combined ethinylestradiol-containing contraceptives are contraindicated in women over 35 who smoke.

Contraindications

  • Active venous thromboembolism, history of VTE
  • Active ischemic heart disease, history of stroke
  • More than 15 cigarettes per day in women over 35
  • Migraine with aura
  • Uncontrolled hypertension (BP ≥ 160/100)
  • Inherited thrombophilias
  • History or current breast cancer
  • Severe liver disease, active hepatitis
  • Hormone-dependent tumors
  • Pregnancy
  • Within 6 weeks postpartum
  • Diabetes with vascular complications
  • Systemic lupus erythematosus with antiphospholipid syndrome

Serious adverse effects

  • Venous thromboembolism (deep vein thrombosis, PE) – 3–9 cases per 10 000 woman-years
  • Arterial thromboembolism (MI, ischemic stroke)
  • Hepatocellular adenoma
  • Cholestatic jaundice
  • Anaphylactic reactions

Common adverse effects

  • Nausea, especially in early cycles
  • Breast tenderness
  • Breakthrough bleeding
  • Headache
  • Decreased libido
  • Mood changes

Uncommon adverse effects

  • Chloasma
  • Vaginal dryness
  • Reduced contact lens tolerance
  • Depression

Pregnancy: can you take Ethinylestradiol?

FDA category X. If pregnancy occurs on COC, the drug is discontinued immediately. Accumulated data do not show increased congenital malformation risk, but pregnancy is not routinely continued on hormonal contraception.

Breastfeeding: can you take Ethinylestradiol?

Within 6 weeks postpartum, ethinylestradiol-containing COCs are contraindicated (USMEC category 4) due to thromboembolism risk. After 6 weeks with stable lactation – USMEC category 2. Ethinylestradiol may reduce milk supply, especially in the early months. Progestin-only methods are preferred in breastfeeding mothers.

Maternal peak time
3 h
Calculate RIDSafe feeding windowFull profile on NIH LactMed ↗

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Timing and administration

Taken daily at the same time. Most ethinylestradiol-containing COCs are 21+7 (21 days of active pills, 7 days of placebo or break), some are 24+4. A delay over 12 hours reduces efficacy; additional contraceptive measures and missed-pill rules are detailed in the product label.

Monitoring

Monitor blood pressure before start, at 3 months and annually thereafter. STI screening and gynecological exam – at standard intervals. Calculate 10-year cardiovascular risk before prescribing to women over 35. In patients with thromboembolism risk factors, assess D-dimer and, if needed, perform genetic thrombophilia testing (factor V Leiden, prothrombin 20210A).

Special situations

Before elective surgery with prolonged immobilization, COC withdrawal is discussed 4 weeks beforehand with a switch to barrier or progestin-only methods; resumption 2 weeks after full mobilization. With prolonged immobilization, severe infection or trauma – immediate withdrawal.

Common myths

Myth: «COCs cause significant weight gain». Fact: systematic reviews show no clinically significant weight gain with modern low-dose COCs. Individual variation exists.

Myth: «after long-term COC use, you cannot conceive for years». Fact: ovulation usually resumes within 1–3 months of withdrawal; fertility is not affected.

Myth: «COCs increase cancer risk». Fact: they increase venous thromboembolism risk and slightly raise breast and cervical cancer risk. They simultaneously reduce ovarian and endometrial cancer risk by 30–50% with long-term use.

Myth: «you need breaks every 2 years». Fact: routine breaks are not needed and do not improve safety; they raise risk of unplanned pregnancy.

Drug–nutrient interactions

Folate

Long-term combined oral contraceptive use moderately lowers erythrocyte folate. Women planning pregnancy immediately after COC withdrawal are advised to take 400 mcg folic acid daily starting at least 1 month before conception. Some COCs (Yaz Plus, Yasmin Plus) include metafolin as an additional component.

Vitamin B6

COCs moderately reduce plasma pyridoxine. Clinical significance for most patients is limited; with pronounced mood symptoms and insufficient dietary intake, dietary adjustment or 25 mg pyridoxine daily is discussed.

Drug–drug interactions

10 pairs found. Sorted from critical to minor.

MajorCarbamazepineAntiepileptics. Carboxamide derivatives

Mechanism

Carbamazepine induces CYP3A4 and accelerates ethinylestradiol metabolism. Combined oral contraceptive efficacy drops; pregnancies during regular use have been reported.

Symptoms

Breakthrough bleeding, missed periods, unplanned pregnancy. The patient feels no symptoms at the moment of dosing.

Management

Switch hormonal contraception to non-hormonal methods (copper IUD or barrier methods) for the duration of carbamazepine therapy. Alternatives: depot progesterone or a levonorgestrel IUD.

Sources

Pair details →Carbamazepine →

MajorHypericum perforatumAntidepressants. Other antidepressants of herbal origin

Mechanism

St. John's wort is a potent inducer of the CYP3A4 enzyme (and of CYP2C9 and P-glycoprotein). After 1–2 weeks it speeds up the breakdown of Ethinylestradiol and lowers its blood level, weakening its effect.

Symptoms

Faster breakdown of estrogen and progestin, breakthrough bleeding, reduced contraceptive protection and risk of unintended pregnancy.

Management

Do not combine with oral contraceptives. While taking St. John's wort use a barrier method or another reliable form of contraception.

Sources

Pair details →Hypericum perforatum →

MajorRifampicinAntituberculous antibiotic

Mechanism

Rifampicin is the most potent CYP3A4 inducer in clinical practice. Ethinylestradiol plasma levels fall by 40–60% within the first week. Combined oral contraceptive efficacy drops to chance.

Symptoms

Breakthrough bleeding, missed periods, unplanned pregnancy. The patient feels no symptoms at the moment of dosing – the problem becomes apparent only later.

Management

Switch hormonal contraception to non-hormonal methods (copper IUD or barrier methods) for the duration of rifampicin and an additional 4 weeks after stopping. Alternatives: depot progesterone or a levonorgestrel IUD (minimal CYP3A4 effect).

Sources

Pair details →Rifampicin →

ModerateBudesonideInhaled corticosteroids (ICS)

Mechanism

Oestrogens raise corticosteroid-binding globulin, increasing the bound budesonide fraction, but the effective free fraction changes minimally. The interaction is clinically minor.

Symptoms

No specific clinical manifestations. On systemic long-term therapy, both drugs' side effects may appear.

Management

No dose adjustment needed. In women on combined oral contraceptives and oral budesonide, check BP and weight every 3 months. With significant systemic budesonide side effects, consider switching to inhaled glucocorticoids or mesalazine.

Sources

Pair details →Budesonide →

MinorAmoxicillinPenicillins with extended spectrum

Mechanism

Historical theory of reduced combined oral contraceptive efficacy via gut flora suppression. Cochrane meta-analysis (2017) did not confirm clinically significant reductions in ethinylestradiol levels with broad-spectrum antibiotics other than CYP3A4 inducers (rifampicin, rifabutin).

Symptoms

The combination usually causes no specific symptoms. Each drug's individual side effects remain.

Management

Additional contraception during short amoxicillin courses is not needed (updated Medical Eligibility Criteria 2015). The old "use a barrier method for the whole cycle" practice is outdated and applies only to rifampicin, rifabutin, CYP3A4-inducing anticonvulsants (carbamazepine, phenytoin), and most HIV antivirals.

Sources

Pair details →Amoxicillin →

MinorAzithromycinMacrolides

Mechanism

Azithromycin has minimal effect on CYP3A4 (unlike clarithromycin and erythromycin). No clinically significant reduction in ethinylestradiol levels has been reported.

Symptoms

The combination usually causes no specific symptoms. Each drug's individual side effects remain.

Management

Additional contraception during short azithromycin courses (3–5 days) is not needed. In women on combined oral contraceptives with respiratory or urogenital infections, azithromycin remains an antibiotic of choice.

Sources

Pair details →Azithromycin →

MinorCiprofloxacinFluoroquinolone antibacterials

Mechanism

The historical theory of reduced combined oral contraceptive efficacy via gut flora suppression is rejected by meta-analyses. Ciprofloxacin does not induce CYP3A4 and does not affect ethinylestradiol metabolism.

Symptoms

The combination usually causes no specific symptoms. Each drug's individual side effects remain.

Management

Additional contraception during short ciprofloxacin courses is not needed. The old "use a barrier method for the whole cycle" advice is outdated.

Sources

Pair details →Ciprofloxacin →

MinorDoxycyclineTetracyclines

Mechanism

Doxycycline does not affect hepatic ethinylestradiol metabolism. The historical theory of reduced COC efficacy via suppression of enterohepatic recirculation is rejected by meta-analyses.

Symptoms

The combination usually causes no specific symptoms. Each drug's individual side effects remain.

Management

Additional contraception during short doxycycline courses is not needed. For long-term therapy (e.g. acne, Lyme disease), no adjustment either.

Sources

Pair details →Doxycycline →

MinorMetronidazoleImidazole derivatives (antiprotozoal / antibacterial)

Mechanism

Metronidazole does not induce CYP3A4 and does not affect hepatic ethinylestradiol metabolism. The historical theory of reduced COC efficacy is rejected by meta-analyses.

Symptoms

The combination usually causes no specific symptoms. Each drug's individual side effects remain.

Management

Additional contraception during short metronidazole courses is not needed. Exclude alcohol throughout the course and for 48 hours after due to a disulfiram-like reaction.

Sources

Pair details →Metronidazole →

MinorNorfloxacinSecond-generation fluoroquinolone

Mechanism

Norfloxacin does not induce CYP3A4 and does not affect ethinylestradiol metabolism. The historical theory of reduced COC efficacy is rejected by meta-analyses.

Symptoms

The combination usually causes no specific symptoms. Each drug's individual side effects remain.

Management

Additional contraception during short norfloxacin courses (3–7 days) is not needed.

Sources

Pair details →Norfloxacin →

Label mentions47 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • Majorbarbitúricosclass named in the label
    «Tratamiento de larga duración: Barbitúricos, bosentán, carbamazepina, fenitoína, primidona, rifampicina y los medicamentos para el VIH ritonavir, nevirapina y efavirenz y, también posiblemente…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorCarbamazepine
    «Tratamiento de larga duración: Barbitúricos, bosentán, carbamazepina, fenitoína, primidona, rifampicina y los medicamentos para el VIH ritonavir, nevirapina y efavirenz y, también posiblemente…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorEfavirenz
    «Tratamiento de larga duración: Barbitúricos, bosentán, carbamazepina, fenitoína, primidona, rifampicina y los medicamentos para el VIH ritonavir, nevirapina y efavirenz y, también posiblemente…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorPhenytoin
    «Tratamiento de larga duración: Barbitúricos, bosentán, carbamazepina, fenitoína, primidona, rifampicina y los medicamentos para el VIH ritonavir, nevirapina y efavirenz y, también posiblemente…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorRifampicin
    «Tratamiento de larga duración: Barbitúricos, bosentán, carbamazepina, fenitoína, primidona, rifampicina y los medicamentos para el VIH ritonavir, nevirapina y efavirenz y, también posiblemente…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorRitonavir
    «Drospirenona/etinilestradiol está contraindicado en el uso concomitante con medicamentos que contengan ombitasvir / paritaprevir / ritonavir y dasabuvir, medicamentos que contengan…»

    AEMPS, section 4.3 · Open on CIMA

  • MajorTopiramate
    «Tratamiento de larga duración: Barbitúricos, bosentán, carbamazepina, fenitoína, primidona, rifampicina y los medicamentos para el VIH ritonavir, nevirapina y efavirenz y, también posiblemente…»

    AEMPS, section 4.5 · Open on CIMA

  • MinorTheophylline
    «Los datos clínicos sugieren que el etinilestradiol inhibe el aclaramiento plasmático de los sustratos del CYP1A2, conduciendo a un aumento débil (p.ej., teofilina) o moderado (p.ej., tizanidina) en…»

    AEMPS, section 4.5 · Open on CIMA

  • Ciclosporin
    «Los anticonceptivos orales (AOCs) pueden influir en el metabolismo de otros principios activos. En consecuencia, los niveles plasmáticos o tisulares pueden aumentar (p. ej. ciclosporina) o disminuir…»

    AEMPS, section 4.5 · Open on CIMA

  • Etoricoxib
    «Sustancias que disminuyen el aclaramiento de los AOCS (inhibidores enzimáticos): Se ha demostrado que dosis de etoricoxib de 60 a 120 mg/día aumentan las concentraciones plasmáticas de…»

    AEMPS, section 4.5 · Open on CIMA

  • Ketoconazole
    «Sustancias que disminuyen el aclaramiento de los AOCS (inhibidores enzimáticos): En un estudio a dosis múltiples con una combinación de drospirenona (3 mg/día) / etinilestradiol (0,02 mg/día), la…»

    AEMPS, section 4.5 · Open on CIMA

  • Lamotrigine
    «Los anticonceptivos orales (AOCs) pueden influir en el metabolismo de otros principios activos. En consecuencia, los niveles plasmáticos o tisulares pueden aumentar (p. ej. ciclosporina) o disminuir…»

    AEMPS, section 4.5 · Open on CIMA

From other drugs’ labels

  • MajorDarunavir
    «ANTICONCEPTIVOS ESTROGÉNICOS: Drospirenona etinilestradiol (3 mg/0,02 mg una vez al día) Etinilestradiol Noretindrona 35 mcg/1 mg una vez al día»

    AEMPS, section 4.5 · Open on CIMA

  • MajorTirzepatide
    «Anticonceptivos orales: La administración de un anticonceptivo oral combinado (0,035 mg de etinilestradiol más 0,25 mg de norgestimato, un profármaco de la norelgestromina) junto con una dosis única…»

    AEMPS, section 4.5 · Open on CIMA

  • ModerateEtoricoxib
    «Etoricoxib es un inhibidor de la actividad de la sulfotransferasa humana, particularmente la SULT1E1, y se ha demostrado que aumenta las concentraciones séricas de etinilestradiol. Mientras que el…»

    AEMPS, section 4.5 · Open on CIMA

  • ModerateLamotrigine
    «Empeoramiento clínico y riesgo de suicidio: La administración de una combinación de etinilestradiol/levonorgestrel (30 µg/150 µg) aumenta hasta aproximadamente el doble el aclaramiento de lamotrigina…»

    AEMPS, section 4.4 · Open on CIMA

  • ModerateLeflunomide
    «DRUG INTERACTIONS: Teriflunomide may increase the systemic exposures of ethinylestradiol and levonorgestrel. Consideration should be given to the type or dose of contraceptives used in combination…»

    FDA, section 7 · Open on DailyMed

  • MinorRoflumilast
    «Estudios clínicos de interacción con los inhibidores de CYP 3A4 eritromicina y ketoconazol han mostrado un aumento del 9% en la actividad inhibidora total del PDE4. La coadministración con teofilina…»

    AEMPS, section 4.5 · Open on CIMA

  • Candesartan
    «hidroclorotiazida, warfarina, digoxina, anticonceptivos orales, (etinilestradiol/levonorgestrel), glibenclamida, nifedipino y enalapril. No se han identificado interacciones farmacocinéticas…»

    AEMPS, section 4.5 · Open on CIMA

  • Celecoxib
    «Anticonceptivos orales: farmacocinética de los anticonceptivos orales (1 mg de noretisterona/35 μg de etinilestradiol).»

    AEMPS, section 4.5 · Open on CIMA

  • Dronedarone
    «Interacción con medicamentos que son metabolizados por el CYP 3A4: No se observaron descensos de etinilestradiol y levonorgestrel en sujetos sanos que recibieron dronedarona (800 mg dos veces al día)…»

    AEMPS, section 4.5 · Open on CIMA

  • Eslicarbazepine acetate
    «Anticonceptivos orales: La administración de 1.200 mg de acetato de eslicarbazepina una vez al día a mujeres que usaban un anticonceptivo oral combinado mostró una disminución promedio del 37% y 42%…»

    AEMPS, section 4.5 · Open on CIMA

  • Eslicarbazepine acetate
    «Oral Contraceptives: Because concomitant use of eslicarbazepine acetate and ethinylestradiol and levonorgestrel is associated with lower plasma levels of these hormones, females of reproductive…»

    FDA, section 7 · Open on DailyMed

  • Ezetimibe
    «En estudios de interacción clínica, ezetimiba no tuvo efecto sobre la farmacocinética de dapsona, dextrometorfano, digoxina, anticonceptivos orales (etinilestradiol y levonorgestrel), glipizida…»

    AEMPS, section 4.5 · Open on CIMA

  • Fesoterodine
    «Anticonceptivos orales: La fesoterodina no afecta a la supresión de la ovulación producida por los anticonceptivos hormonales orales. En presencia de fesoterodina, no hay ningún cambio en la…»

    AEMPS, section 4.5 · Open on CIMA

  • Gabapentin
    «La coadministración de gabapentina con anticonceptivos orales que contengan noretindrona y/o etinilestradiol no influye en la farmacocinética en estado estacionario de ambos componentes.»

    AEMPS, section 4.5 · Open on CIMA

  • Lacosamide
    «Anticonceptivos orales: En un estudio de interacción no hubo interacción clínicamente relevante entre lacosamida y los anticonceptivos orales etinilestradiol y levonorgestrel. Las concentraciones de…»

    AEMPS, section 4.5 · Open on CIMA

  • Lamotrigine
    «DRUG INTERACTIONS: preparations containing 30 mcg ethinylestradiol and 150 mcg levonorgestrel ↓ levonorgestrel Decrease in levonorgestrel component by 19%.»

    FDA, section 7 · Open on DailyMed

  • Leflunomide
    «Anticonceptivos orales: En un estudio con voluntarias sanas en el que se administró leflunomida junto con un anticonceptivo oral trifásico que contenía 30 μ g de etinilestradiol, no se produjo…»

    AEMPS, section 4.5 · Open on CIMA

  • Levetiracetam
    «Anticonceptivos orales y otras interacciones farmacocinéticas: Dosis diarias de 1.000 mg de levetiracetam no influenciaron la farmacocinética de los anticonceptivos orales (etinilestradiol y…»

    AEMPS, section 4.5 · Open on CIMA

  • Liraglutide
    «Anticonceptivos orales: Tras la administración de una única dosis de un medicamento anticonceptivo oral, liraglutida disminuyó la C max de etinilestradiol y levonorgestrel un 12% y un 13%…»

    AEMPS, section 4.5 · Open on CIMA

  • Mycophenolate mofetil
    «Effect of Mycophenolate Mofetil on Other Drugs: Clinical Impact Concomitant use with mycophenolate mofetil decreased the systemic exposure to levonorgestrel, but did not affect the systemic exposure…»

    FDA, section 7 · Open on DailyMed

  • Pantoprazole
    «Otros estudios de interacciones: Los estudios de interacción con medicamentos que se metabolizan igualmente mediante estas rutas metabólicas, como carbamazepina, diazepam, glibenclamida, nifedipino y…»

    AEMPS, section 4.5 · Open on CIMA

  • Pregabalin
    «Anticonceptivos orales, noretisterona y/o etinilestradiol: La administración de pregabalina junto con anticonceptivos orales como noretisterona y/o etinilestradiol, no influye en la farmacocinética…»

    AEMPS, section 4.5 · Open on CIMA

  • Rifabutin
    «Effect of Other Drugs on Rifabutin Pharmacokinetics: Ethinylestradiol (EE)/ Norethindrone (NE) 35 mg EE / 1 mg NE for 21 days 300 mg once a day for 10 days Healthy female subjects (22) ND EE: ↓ AUC…»

    FDA, section 7 · Open on DailyMed

  • Rosuvastatin
    «Anticonceptivos orales/terapia hormonal sustitutiva (THS): la administración conjunta de rosuvastatina y un anticonceptivo oral originó un incremento del AUC de etinilestradiol y norgestrel del 26% y…»

    AEMPS, section 4.5 · Open on CIMA

  • Semaglutide
    «Anticonceptivos orales: No se prevé que semaglutida disminuya el efecto de los anticonceptivos orales, ya que semaglutida no modificó de una forma clínicamente significativa la exposición general de…»

    AEMPS, section 4.5 · Open on CIMA

  • Sirolimus
    «Anticonceptivos orales: No se observó ninguna interacción farmacocinética clínicamente significativa entre Rapamune solución oral y 0,3 mg de norgestrel/0,03 mg de etinilestradiol. Aunque los…»

    AEMPS, section 4.5 · Open on CIMA

  • Solifenacin
    «Anticonceptivos orales: La administración de solifenacina no mostró interacción farmacocinética de solifenacina con los anticonceptivos orales de combinación (etinilestradiol/levonorgestrel).»

    AEMPS, section 4.5 · Open on CIMA

  • Tacrolimus
    «Recomendaciones relativas a la a dministración simultánea: Inhibidores del CYP3A4 moderados o débiles: agentes antifúngicos (p. ej., fluconazol, isavuconazol, clotrimazol, miconazol), antibióticos…»

    AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Ethinylestradiol used for?

Ethinylestradiol is evaluated for the following indications with varying evidence strength: Combined oral contraception (evidence tier A), Menopausal hormone therapy (evidence tier B), Acne and PCOS with hyperandrogenism (evidence tier B). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Ethinylestradiol?

Common side effects of Ethinylestradiol (≥ 1 in 100): Nausea, especially in early cycles, Breast tenderness, Breakthrough bleeding, Headache, Decreased libido, Mood changes. See the Safety section for uncommon and serious reactions.

Is Ethinylestradiol safe during pregnancy?

FDA category X. If pregnancy occurs on COC, the drug is discontinued immediately. Accumulated data do not show increased congenital malformation risk, but pregnancy is not routinely continued on hormonal contraception.

Is Ethinylestradiol compatible with breastfeeding?

Within 6 weeks postpartum, ethinylestradiol-containing COCs are contraindicated (USMEC category 4) due to thromboembolism risk. After 6 weeks with stable lactation – USMEC category 2. Ethinylestradiol may reduce milk supply, especially in the early months. Progestin-only methods are preferred in breastfeeding mothers.

Who should not take Ethinylestradiol?

Ethinylestradiol is contraindicated in: Active venous thromboembolism, history of VTE; Active ischemic heart disease, history of stroke; More than 15 cigarettes per day in women over 35; Migraine with aura; Uncontrolled hypertension (BP ≥ 160/100). Full list in the Safety section.

Does Ethinylestradiol carry an FDA boxed warning?

FDA boxed warning: smoking significantly increases the risk of serious cardiovascular events on combined hormonal contraception. Risk increases with age, particularly after 35, and with smoking intensity. Combined ethinylestradiol-containing contraceptives are contraindicated in women over 35 who smoke.

COCs cause significant weight gain

systematic reviews show no clinically significant weight gain with modern low-dose COCs. Individual variation exists.

after long-term COC use, you cannot conceive for years

ovulation usually resumes within 1–3 months of withdrawal; fertility is not affected.

COCs increase cancer risk

they increase venous thromboembolism risk and slightly raise breast and cervical cancer risk. They simultaneously reduce ovarian and endometrial cancer risk by 30–50% with long-term use.

you need breaks every 2 years

routine breaks are not needed and do not improve safety; they raise risk of unplanned pregnancy.

Official sources

Direct links to regulator labels. Open in a new tab.

Other drugs in this group

Ethinylestradiol + Desogestrel, Ethinylestradiol + Gestodene, Ethinylestradiol + Levonorgestrel, Ethinylestradiol + Norgestimate, Etonogestrel (implant), Norelgestromin + Ethinylestradiol (transdermal patch), Tongkat ali (Eurycoma longifolia), Drospirenone + ethinylestradiol