Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia) - Schedule

Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia) is an oral hormonal contraceptive medicine that is used in females of reproductive potential to avoid pregnancy. It is also used as off-label medicine for the treatment of abnormal vaginal bleeding and dysmenorrhea.

Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia) Uses:

  • Contraception:

    • Used for the prevention of pregnancy Limitation of use:
      • Products containing the equivalent of estrogen 50 mcg should not be used unless medically indicated.

  • Off Label Use of Ethinyl estradiol and ethynodiol diacetate in Adults:

    • Used for abnormal uterine bleeding
    • Used for  dysmenorrhea
    • Used for  hirsutism
    • Used for  menstrual bleeding (menorrhagia)
    • Used for  pain associated with endometriosis
    • Used for  polycystic ovary syndrome (PCOS) in women with menstrual irregularities and hirsutism/acne

Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia) Dosage and Schedule in Adults:

Contraception:

    • Oral: 1 tablet once in a day.

  • Schedule 1 (Sunday starter):

    • Dose begins on the first Sunday after the onset of menstruation;
    • if the menstrual period starts on Sunday, take the first tablet that very same day.
    • With a Sunday start, an additional method of contraception should be used until after the first weak of consecutive administration:

    • Schedule 2 (Day 1 starter):

      • Dose starts on the first day of the menstrual cycle taking 1 tablet every day:

  • Missed or late doses:

    • If one dose is late ( less than 24 hours since the dose should have been taken) or if one dose is missed (24 to <48 hours since the dose should have been taken):
      • Take dose as soon as possible. Continue remaining doses at the usual time (even if that means 2 doses on the same day).
    • If 2 or more than 2 consecutive doses are missed (≥48 hours since dose should have been taken):
      • Take the most recently missed dose as soon as possible, discard any other missed doses.
      • Continue remaining doses at the usual time (even if that means taking 2 doses on the same day);
      • Use back-up contraception until hormonal pills have been taken for 7 consecutive days.
      • If doses were missed during the last week of hormonal (active) tablets (eg, days 15 to 21 of a 28-day pack), omit the hormone-free interval by finishing the hormonal pills from the current pack and starting a new pack.
      • If unable to start a new pack immediately, back up contraception is needed until hormonal pills from a new pack have been taken for 7 consecutive days.
      • Consider the use of emergency contraception in some situations (refer to guidelines for details).
    • Also, refer to the package insert for product specific information.

Use in Children:

Refer to adults dosing.

Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia) Pregnancy Risk Factor: X

  • Pregnant women should not use it.
  • For women who do not breastfeed, the manufacturer advises that you wait 4 to 6 weeks before starting combination hormonal contraceptives.
  • To prevent pregnancy, combination hormonal contraceptives can be used. If pregnant, treatment should be stopped.
  • Combination hormonal contraceptives are generally not associated with any adverse effects on the fetus or mother if used inadvertently early in pregnancy.
  • Combination hormonal contraceptives should be stopped in women who have delivered less than 21 days after delivery due to increased risk of venous embolism (VTE).
  • Postpartum day 42 sees a decrease in the risk to baseline.
  • Combination hormonal contraceptives should be used in women 21 to 42 days after delivery.
  • Women who use combination hormonal contraceptives must take into account the woman's risk factors (eg., age >=35, transfusion at birth, thrombophilia or immobility), BMI >=30kg/m2, postpartum bleeding, smoking, and preeclampsia.

Use of ethynodiol diacetate and etherinol estradiol during breastfeeding

  • Breast milk may contain contraceptive steroids.
  • Breastfeeding mothers who use combination hormonal contraceptives have not reported any adverse health effects or persistent effects on infant growth and illness.
  • The manufacturer suggests that contraceptives containing estrogen be used until the child is weaned. This will reduce milk production.
  • Breastfeeding women should not start combination hormonal contraceptives less than 21 days after delivery due to an increased risk of venous embolism (VTE).
  • Postpartum day 42 sees a decrease in the risk to baseline.
  • Combination hormonal contraceptives should be used in women 21 to 42 days after birth.
  • Women who use combination hormonal contraceptives must take into account the woman's risk factors (eg., age >=35, previous VTEs, transfusion at delivery or cesarean delivery), immobility and preeclampsia.
  • When starting treatment for breastfeeding women, it is important to consider the risks and benefits of combination hormonal contraception.

Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia) Dose in Kidney Disease:

Manufacturer's labeling doesn't provide any dosage adjustments (has not been studied); use with caution and monitor blood pressure closely.

Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia) Dose in Liver disease:

Its use is contraindicated.

Side effects of Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia):

  • Cardiovascular:

    • Myocardial Infarction
    • Pulmonary Thromboembolism
    • Retinal Thrombosis
    • Arterial Thromboembolism
    • Budd-Chiari Syndrome
    • Cerebral Thrombosis
    • Cerebrovascular Accident
    • Edema
    • Hypertension
    • Local Thrombophlebitis
    • Mesenteric Thrombosis

  • Central Nervous System:

    • Dizziness
    • Headache
    • Migraine
    • Nervousness
    • Cerebral Hemorrhage
    • Depression

  • Dermatologic:

    • Acne Vulgaris
    • Chloasma (May Persist)
    • Erythema Multiforme
    • Erythema Nodosum
    • Allergic Skin Rash
    • Loss Of Scalp Hair

  • Endocrine & Metabolic:

    • Amenorrhea
    • Weight Gain
    • Weight Loss
    • Change In Libido
    • Change In Menstrual Flow
    • Decreased Glucose Tolerance
    • Decreased Serum Folate Level
    • Hirsutism
    • Increased Serum Triglycerides
    • Increased Sex Hormone Binding Globulins
    • Increased Thyroxine Binding Globulin
    • Porphyria
    • Premenstrual Syndrome

  • Gastrointestinal:

    • Colitis
    • Gallbladder Disease
    • Nausea
    • Vomiting
    • Abdominal Cramps
    • Bloating
    • Carbohydrate Intolerance
    • Change In Appetite
    • Cholestasis

  • Genitourinary:

    • Breakthrough Bleeding
    • Change In Cervical Secretions
    • Cystitis-Like Syndrome
    • Decreased Lactation (Postpartum)
    • Spotting
    • Transient Infertility (Following Discontinuation)
    • Vaginitis
    • Breast Hypertrophy
    • Breast Secretion
    • Breast Tenderness
    • Change In Cervical Erosion
    • Vulvovaginal Candidiasis

  • Hematologic & Oncologic:

    • Increased Clotting Factor VII
    • Increased Clotting Factor VIII
    • Increased Clotting Factor IX
    • Increased Clotting Factor X
    • Increased Norepinephrine-Induced Platelet Aggregation
    • Prolonged Prothrombin Time
    • Decreased Antithrombin III Plasma Level
    • Hemolytic-Uremic Syndrome
    • Hemorrhagic Eruption

  • Hepatic:

    • Cholestatic Jaundice
    • Hepatic Neoplasm (Benign)
    • Jaundice
    • Hepatic Adenoma

  • Ophthalmic:

    • Cataract
    • Change In Corneal Curvature (Steepening)
    • Contact Lens Intolerance
    • Optic Neuritis

  • Renal:

    • Renal Insufficiency

Contraindications to Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia):

  • Breast cancer and other estrogen-, progestin-dependent Neoplasms (currently or in the past).
  • Hepatic tumors (benign and malignant), hepatic disease, jaundice, or previous combination hormonal contraceptive treatment.
  • pregnancy,
  • Cholestatic jaundice during pregnancy
  • Undiagnosed abnormal uterine bleeding
  • coadministration with hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir.

Women at high risk for arterial or vein thrombotic disease, such as women with:

  • Cerebrovascular Disease
  • Deep vein thrombosis
  • Coronary artery disease
  • Myocardial Infarction, thrombophlebitis, or thromboembolic Disorders (current or historical)

Canadian labeling: Additional contraindications

  • Hypersensitivity to any ingredient of the formulation
  • Ocular lesions caused by ophthalmic vessels disease, including partial or total loss of vision and defect in the visual fields.
  • Pancreatitis in association with severe hypertriglyceridemia (current and/or history of);
  • Thrombophilias (inherited, acquired);
  • severe dyslipoproteinemia;
  • Women over 35 who smoke more than 15 cigarettes per days are considered to be older than the average woman.
  • Major surgery can increase the risk of postoperative bleeding.
  • Long-term immobilization
  • Thrombogenic valvular rhythm or heart disease;
  • Headaches with focal neurological symptoms (eg aura)
  • Diabetes mellitus and vascular disease
  • Hypertension uncontrolled

Warnings and precautions

  • Breast cancer

    • Breast cancer is a hormone sensitive tumor. Women with a history of breast cancer or a recent diagnosis may have a worse prognosis if they use combination hormonal contraceptives.
    • Combination hormonal contraceptives have not been proven to reduce breast cancer risk in women who are at high risk due to their family history or susceptibility genes (BRCA1, BRCA2)
    • Women with breast cancer history or who have had it are advised to not use this product.

  • Cervical cancer:

    • Theoretically, it may influence the prognosis for an existing disease.
    • Combination hormonal contraceptives may be used by women who are awaiting treatment for cervical carcinoma.
    • Combination hormonal contraceptives have been linked to a slight increase in cervical cancer risk. However, the evidence is inconsistent and could be due to other risk factors.

  • Chloasma

    • Treatment should be avoided for women who are susceptible to chloasma and other risk factors.
    • Combination hormonal contraceptives as well as sun exposure, pregnancy and sun exposure are all triggers for chloasma.

  • Cholestasis:

    • Contraindicated in combination with hormonal contraceptive or cholestatic jaundice prior to pregnancy.
    • Cholesteasis risk may increase if there has been a history of cholestasis in pregnancy, or with prior oral contraceptive use.

  • The Lipid Effects

    • Combination hormonal contraceptives can adversely affect lipid levels, especially serum triglycerides.
    • Combination hormonal contraceptives can increase the risk of pancreatitis in women with hypertriglyceridemia and a family history.

  • Retinal vascular embolism:

    • If you experience an undiagnosed loss of vision, diplopia or papilledema, or retinal vessels lesions, discontinue use immediately and get checked for retinal vein embolism.

  • Thromboembolic disorders

    • The risk of venous embolism may be increased by oral contraceptives. This risk is greater in the first year and lower than that associated with pregnancy. Some studies have suggested that the risk may be higher for preparations containing third- or fourth-generation progestins, and/or high dose Ethinyl Estradiol.
    • Women who have inherited thrombophilias, such as protein C or S deficiencies, factor V Leiden mutations, antithrombin deficiency and prothrombin mutations, may be at greater risk for venous thromboembolism.
    • Women who use combined hormonal contraceptives for longer periods of time, such as 35 and older, are more likely to experience thrombotic events.
    • Combination hormonal contraceptives can also increase the risk for arterial thrombosis (eg MI, stroke). Women with a history or ischemic heart disease should not use them.
    • Women with thromboembolic conditions should not use it.

  • Vaginal bleeding

    • Unresolved vaginal bleeding is a sign of malignancy and pregnancy.
    • In the initial 3 months of therapy, it is possible to experience breakthrough or intr-acyclic bleeding.
    • There may be occasional missed periods.
    • Combination hormonal contraceptives may cause amenorrhea and oligomenorrhea, particularly if the condition was not present previously.

  • Cardiovascular disease

    • Patients with cardiovascular risk factors (e.g. diabetes, hypertension, low HDL, high cholesterol, high LDL, older women, smoking) should be cautious.
    • Combination hormonal contraceptives can increase your risk of developing cardiovascular disease.

  • Depression

    • Patients with a history or depression should be cautious; discontinue use if severe depression recurs.

  • Diabetes:

    • This may impair glucose tolerance. Women with diabetes and prediabetes should be cautious.
    • Contraceptive use should not be used in women who have concomitant neuropathy or retinopathy, nephropathy or other vascular diseases.
    • Combination oral contraceptives have a limited effect on insulin requirements and do not have long-term effects on diabetes control for women with nonvascular diseases.

  • Fluid retention can lead to more severe diseases

    • Patients with fluid retention-related diseases should be cautious.

  • Endometrial and ovarian cancers:

    • Combination hormonal contraceptives reduce the risk of ovarian or endometrial cancer.
    • Combination hormonal contraceptives may be used by women awaiting treatment for ovarian or endometrial cancer.
    • Women with BRCA1 or BRCA2 mutations may have to use oral contraceptives to lower their risk of developing ovarian cancer.

  • Gallbladder disease

    • Combining hormonal contraceptives can increase the risk of gallbladder diseases or make existing gallbladder diseases worse.

  • Hepatic adenomas and carcinomas

    • Combination hormonal contraceptives can cause hepatic tumors (rare), and rupture could lead to fatal intra-abdominal bleeding.
    • Preexisting hepatic cancers are not recommended.
    • A rare form of hepatocellular carcinoma is the risk associated with long-term, prolonged use.

  • Hepatic impairment

    • Women with impaired liver function may not be able to process hormonal contraceptives in combination.
    • Preexisting hepatic diseases are contraindicated.
    • Combination hormonal contraceptives can be used for women with mild (compensated), but not severe (decompensated), cirrhosis.
    • If jaundice occurs during treatment or if the liver function is abnormal, discontinue use.

  • Hepatitis

    • Combination hormonal contraceptives are not recommended for women suffering from acute viral hepatitis, flares, or other severe conditions.
    • Women with chronic hepatitis have not been shown to experience an increase in the severity or rate of cirrhotic fibrisis.
    • It has been proven that continued use of a drug by women who are carriers does not cause liver disease or severe hepatic dysfunction.

  • Hereditary angioedema:

    • Women with hereditary angioedema may be affected by estrogens.

  • Hypertension:

    • Women with hypertension or vascular disease or persistent blood pressure levels >=160mm Hg Systolic or >=100mm Hg Diastolic should not use combination hormonal contraceptives.
    • Women with mild hypertension (140-159 mmHg systolic, 90-99 mmHg diastolic) and women with moderate hypertension (140-159 mmHg systolic; or hypertension controlled to an acceptable level) may not be at risk.
    • When prescribing contraceptives, it is important to consider other risk factors such as smoking, diabetes, and older age.
    • Manufacturer recommends that hypertension be monitored in women; stop taking medication if blood pressure increases significantly.

  • Migraine

    • Headaches that are persistent, severe, and persistent.
    • Women with migraines without aura, including menstrual migraines, may consider using combination hormonal contraceptives.

  • Renal impairment

    • Women suffering from renal disease should be encouraged not to use hormonal contraception.

  • Transplantation of solid-organs:

    • Although the data is not complete, serious medical complications were reported by women who have had to undergo complicated organ transplants.
    • Combination hormonal contraceptives are not recommended for women who have had multiple organ transplants.

  • Systemic lupus erythematosus (SLE):

    • SLE women are more at risk for heart disease, stroke and VTE.
    • Women with SLE should not use combination hormonal contraceptives if they have antiphospholipid antibodies. This is because there is a greater risk of arterial or venous embolism.

Ethinyl estradiol and ethynodiol diacetate: Drug Interaction

Risk Factor C (Monitor therapy)

Ajmaline

Estrogen Derivatives may enhance the adverse/toxic effect of Ajmaline. Specifically, the risk for cholestasis may be increased.

Anthrax Immune Globulin (Human)

Estrogen Derivatives may enhance the thrombogenic effect of Anthrax Immune Globulin (Human).

Antidiabetic Agents

Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents.

Ascorbic Acid

May increase the serum concentration of Estrogen Derivatives.

C1 inhibitors

Estrogen Derivatives may enhance the thrombogenic effect of C1 inhibitors.

C1 inhibitors

Progestins may enhance the thrombogenic effect of C1 inhibitors.

Chenodiol

Estrogen Derivatives may diminish the therapeutic effect of Chenodiol. Management: Monitor clinical response to chenodiol closely when used together with any estrogen derivative.

CloZAPine

CYP1A2 Inhibitors (Weak) may increase the serum concentration of CloZAPine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.

Corticosteroids (Systemic)

Estrogen Derivatives may increase the serum concentration of Corticosteroids (Systemic).

CYP3A4 Inducers (Moderate)

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

CYP3A4 Inhibitors (Moderate)

May increase the serum concentration of Estrogen Derivatives.

CYP3A4 Inhibitors (Strong)

May increase the serum concentration of Estrogen Derivatives.

Dantrolene

Estrogen Derivatives may enhance the hepatotoxic effect of Dantrolene.

Deferasirox

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Erdafitinib

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Flibanserin

Estrogen Derivatives (Contraceptive) may increase the serum concentration of Flibanserin.

Flibanserin

Progestins (Contraceptive) may increase the serum concentration of Flibanserin.

Guanethidine

Estrogen Derivatives (Contraceptive) may diminish the therapeutic effect of Guanethidine.

Herbs (Estrogenic Properties)

May enhance the adverse/toxic effect of Estrogen Derivatives.

Herbs (Progestogenic Properties) (eg, Bloodroot, Yucca)

May enhance the adverse/toxic effect of Progestins.

Immune Globulin

Estrogen Derivatives may enhance the thrombogenic effect of Immune Globulin.

Lenalidomide

Estrogen Derivatives may enhance the thrombogenic effect of Lenalidomide.

Metreleptin

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Metreleptin may increase the serum concentration of Estrogen Derivatives (Contraceptive).

Metreleptin

May decrease the serum concentration of Progestins (Contraceptive). Metreleptin may increase the serum concentration of Progestins (Contraceptive).

Mivacurium

Estrogen Derivatives may increase the serum concentration of Mivacurium.

Nonsteroidal Anti-Inflammatory Agents (COX-2 Selective)

May enhance the thrombogenic effect of Estrogen Derivatives. Nonsteroidal Anti-Inflammatory Agents (COX-2 Selective) may increase the serum concentration of Estrogen Derivatives.

Proguanil

Ethinyl Estradiol may diminish the therapeutic effect of Proguanil.

ROPINIRole

Estrogen Derivatives may increase the serum concentration of ROPINIRole.

Sarilumab

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Selegiline

Estrogen Derivatives (Contraceptive) may increase the serum concentration of Selegiline.

Selegiline

Progestins (Contraceptive) may increase the serum concentration of Selegiline.

Siltuximab

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Succinylcholine

Estrogen Derivatives may increase the serum concentration of Succinylcholine.

Thalidomide

Estrogen Derivatives (Contraceptive) may enhance the thrombogenic effect of Thalidomide.

Thalidomide

Progestins (Contraceptive) may enhance the thrombogenic effect of Thalidomide.

Thalidomide

Estrogen Derivatives may enhance the thrombogenic effect of Thalidomide.

Theophylline Derivatives

Estrogen Derivatives may increase the serum concentration of Theophylline Derivatives. Exceptions: Dyphylline.

Thyroid Products

Estrogen Derivatives may diminish the therapeutic effect of Thyroid Products.

Tocilizumab

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Ursodiol

Estrogen Derivatives may diminish the therapeutic effect of Ursodiol.

Valproate Products

Estrogen Derivatives (Contraceptive) may decrease the serum concentration of Valproate Products.

Voriconazole

May decrease the metabolism of Estrogen Derivatives (Contraceptive). Estrogen Derivatives (Contraceptive) may increase the serum concentration of Voriconazole.

Voriconazole

May increase the serum concentration of Progestins (Contraceptive). Progestins (Contraceptive) may increase the serum concentration of Voriconazole.

Risk Factor D (Consider therapy modification)

Acitretin

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Given the potential for progestin-only preparations to fail to prevent pregnancy during acitretin therapy, such products should not be relied upon. Alternative, nonhormonal forms of contraception must be employed during acitretin therapy.

Anticoagulants

Estrogen Derivatives may diminish the anticoagulant effect of Anticoagulants. More specifically, the potential prothrombotic effects of some estrogens and progestin-estrogen combinations may counteract anticoagulant effects. Management: Carefully weigh the prospective benefits of estrogens against the potential increased risk of procoagulant effects and thromboembolism. Use is considered contraindicated under some circumstances. Refer to related guidelines for specific recommendations.

Anticoagulants

Progestins may diminish the therapeutic effect of Anticoagulants. More specifically, the potential prothrombotic effects of some progestins and progestin-estrogen combinations may counteract anticoagulant effects. Management: Carefully weigh the prospective benefits of progestins against the potential increased risk of procoagulant effects and thromboembolism. Use is considered contraindicated under some circumstances. Refer to related guidelines for specific recommendations.

Aprepitant

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Use of a non-hormone-based contraceptive is recommended.

Aprepitant

May decrease the serum concentration of Progestins (Contraceptive). Management: Alternative or additional methods of contraception should be used both during treatment with aprepitant or fosaprepitant and for at least one month following the last aprepitant/fosaprepitant dose.

Armodafinil

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: The manufacturer recommends that patients use nonhormonal contraceptives, in addition to or in place of hormonal contraceptives, during and for one month following treatment with armodafinil.

Artemether

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Consider the use of an alternative (i.e., non-hormonal) means of contraception in all women of childbearing potential who are using artemether.

Artemether

May decrease the serum concentration of Progestins (Contraceptive). Management: Consider the use of an alternative (i.e., non-hormonal) means of contraception in all women of childbearing potential who are using artemether.

Asunaprevir

May decrease the serum concentration of Ethinyl Estradiol. Management: For patients using hormone-based contraception, a high-dose oral contraceptive containing at least 30 mcg of ethinyl estradiol combined with norethindrone acetate/norethindrone is recommended during treatment with asunaprevir.

Atazanavir

May increase the serum concentration of Progestins (Contraceptive). However, atazanavir may lead to decreased ethinyl estradiol concentrations and decreased effectiveness of oral contraceptive products. Management: Consider an alternative or additional method of contraception, particularly with combined estrogen/progestin products. Depot medroxyprogesterone acetate may be used without a need for additional contraception.

Barbiturates

May diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of a non-hormonal contraceptive is recommended.

Barbiturates

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Use of alternative, nonhormonal contraceptives is recommended.

Bexarotene (Systemic)

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Women of childbearing potential receiving bexarotene should use two reliable forms of contraception (including at least one nonhormonal form).

Bexarotene (Systemic)

May decrease the serum concentration of Progestins (Contraceptive). Management: Women of childbearing potential receiving bexarotene should use two reliable forms of contraception (including at least one nonhormonal form).

Bile Acid Sequestrants

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Administer estrogen-based oral contraceptives at least 1 to 4 hours prior to or 4 to 6 hours after administration of a bile acid sequestrant.

Bile Acid Sequestrants

May decrease the serum concentration of Progestins (Contraceptive). Management: Administer oral progestin-containing contraceptives at least 1 to 4 hours prior to or 4 to 6 hours after administration of a bile acid sequestrant.

Bosentan

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Use an alternative (i.e., non-hormonal) means of contraception for all women of childbearing potential who are using bosentan, and do not rely on hormonal contraceptives alone.

Bosentan

May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative (i.e., non-hormonal) means of contraception for all women of childbearing potential who are using bosentan, and do not rely on hormonal contraceptives alone.

Brigatinib

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Females of childbearing potential should use an alternative, non-hormonal contraceptive during brigatinib therapy and for at least 4 months after the final brigatinib dose.

Brigatinib

May decrease the serum concentration of Progestins (Contraceptive). Management: Females of childbearing potential should use an alternative, non-hormonal contraceptive during brigatinib therapy and for at least 4 months after the final brigatinib dose.

CarBAMazepine

May diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of a nonhormonal contraceptive is recommended.

CarBAMazepine

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Use of alternative, nonhormonal contraceptives is recommended.

Carfilzomib

May enhance the thrombogenic effect of Estrogen Derivatives (Contraceptive). Management: Consider alternative, non-hormonal methods of contraception in patients requiring therapy with carfilzomib.

Carfilzomib

May enhance the thrombogenic effect of Progestins (Contraceptive). Management: Consider alternative, non-hormonal methods of contraception in patients requiring therapy with carfilzomib.

Cladribine

May diminish the therapeutic effect of Hormonal Contraceptives. Management: Women using systemically acting hormonal contraceptives should add a barrier method during cladribine dosing and for at least 4 weeks after the last dose in each treatment course.

CloBAZam

May decrease the serum concentration of Estrogen Derivatives (Contraceptive).

CloBAZam

May decrease the serum concentration of Progestins (Contraceptive).

Cobicistat

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Consider an alternative, nonhormone-based contraceptive in patients receiving cobicistat-containing products.

Cobicistat

May increase the serum concentration of Progestins (Contraceptive). Management: Consider an alternative, nonhormone-based contraceptive in patients receiving cobicistatcontaining products. Drospirenone is specifically contraindicated with atazanavir and cobicistat.

Colesevelam

May decrease the serum concentration of Ethinyl Estradiol. Management: Oral contraceptives containing ethinyl estradiol and norethindrone should be administered at least 4 hours before colesevelam.

Cosyntropin

Estrogen Derivatives may diminish the diagnostic effect of Cosyntropin. Management: Discontinue estrogen containing drugs 4 to 6 weeks prior to cosyntropin (ACTH) testing.

CYP3A4 Inducers (Strong)

May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling.

Dabrafenib

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects).

Dabrafenib

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Females of reproductive potential should use an alternative, highly effective, nonhormonal means of contraception during and at least 2 weeks (dabrafenib alone) or 4 months (dabrafenib + trametinib) after discontinuation of dabrafenib treatment.

Dabrafenib

May decrease the serum concentration of Progestins (Contraceptive). Management: Females of reproductive potential should use an alternative, highly effective, non-hormonal means of contraception during and at least 2 weeks (dabrafenib alone) or 4 months (dabrafenib + trametinib) after discontinuation of dabrafenib treatment.

Darunavir

May decrease the serum concentration of Progestins (Contraceptive). Management: Consider using an alternative or additional means of contraception. Injected depot medroxyprogesterone acetate may be used without a need for additional contraception.

Efavirenz

May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction.

Elagolix

Estrogen Derivatives (Contraceptive) may diminish the therapeutic effect of Elagolix. Management: Use an alternative, non-hormonal contraceptive during treatment with elagolix and for at least 1 week following discontinuation of elagolix treatment.

Elvitegravir

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Consider the use of an alternative, non-hormone-based contraceptive, in patients who are being treated with elvitegravir-containing products.

Enzalutamide

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring.

Eslicarbazepine

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Alternative non-hormonal means of birth control should be considered for women of child-bearing potential.

Eslicarbazepine

May decrease the serum concentration of Progestins (Contraceptive). Management: Alternative, non-hormonal means of birth control should be considered for women of child-bearing potential.

Exenatide

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Administer oral contraceptives at least one hour prior to exenatide.

Exenatide

May decrease the serum concentration of Progestins (Oral Contraceptive). Management: Administer oral contraceptives at least one hour prior to exenatide.

Felbamate

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of a nonhormonal contraceptive is recommended.

Felbamate

May decrease the serum concentration of Progestins (Contraceptive). Management: Contraceptive failure is possible. Use of an alternative, nonhormonal method of contraception is recommended.

Fosamprenavir

Progestins (Contraceptive) may decrease serum concentrations of the active metabolite(s) of Fosamprenavir. Fosamprenavir may decrease the serum concentration of Progestins (Contraceptive). Management: Consider using an alternative or additional means of contraception. Injected depot medroxyprogesterone acetate may be used without a need for additional contraception.

Fosaprepitant

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). The active metabolite aprepitant is likely responsible for this effect. Management: Alternative or additional methods of contraception should be used both during treatment with fosaprepitant or aprepitant and for at least one month following the last fosaprepitant/aprepitant dose.

Fosaprepitant

May decrease the serum concentration of Progestins (Contraceptive). The active metabolite aprepitant is likely responsible for this effect. Management: Alternative or additional methods of contraception should be used both during treatment with aprepitant or fosaprepitant and for at least one month following the last aprepitant/fosaprepitant dose.

Fosphenytoin

May diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal means of contraception is recommended.

Fosphenytoin

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended.

Hyaluronidase

Estrogen Derivatives may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving estrogens (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required.

Ivosidenib:

 May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Consider alternative methods of contraception (ie, non-hormonal) in patients receiving ivosidenib.

Ivosidenib

May decrease the serum concentration of Progestins (Contraceptive). Management: Consider alternative methods of contraception (ie, non-hormonal) in patients receiving ivosidenib.

LamoTRIgine

Estrogen Derivatives (Contraceptive) may decrease the serum concentration of LamoTRIgine. Management: Monitor for increased serum concentrations/effects of lamotrigine in patients in whom a hormonal contraceptive is discontinued/dose decreased (this includes during a pill-free week). A reduced dosage of lamotrigine may be needed.

Lesinurad

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Use of an additional, nonhormonal contraceptive is recommended in patients being treated with lesinurad who desire effective contraception.

Lesinurad

May decrease the serum concentration of Progestins (Contraceptive). Management: Use of an additional, nonhormonal contraceptive is recommended in patients being treated with lesinurad who desire effective contraception.

Lixisenatide

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Administer oral contraceptives 1 hour before or at least 11 hours after administration of lixisenatide.

Lixisenatide

May decrease the serum concentration of Progestins (Contraceptive). Management: Administer oral contraceptives 1 hour before or at least 11 hours after administration of lixisenatide.

Lomitapide

Ethinyl Estradiol may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 40 mg/day.

Lopinavir

May decrease the serum concentration of Progestins (Contraceptive). Lopinavir may increase the serum concentration of Progestins (Contraceptive). Management: Consider using an alternative or additional means of contraception. Injected depot medroxyprogesterone acetate and etonogestrel implants may be used without a need for additional contraception.

Lorlatinib

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences.

Lumacaftor

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Do not rely on hormone-based contraceptives with concurrent use of lumacaftor/ivacaftor; an alternative, non-hormonal, method of contraception should be used if this combination is required.

Lumacaftor

May decrease the serum concentration of Progestins (Contraceptive). Management: Do not rely on hormone-based contraceptives with concurrent use of lumacaftor/ivacaftor; an alternative, non-hormonal, method of contraception should be used if this combination is required.

MiFEPRIStone

May diminish the therapeutic effect of Progestins (Contraceptive). MiFEPRIStone may increase the serum concentration of Progestins (Contraceptive). Management: Women of childbearing potential should use an effective, nonhormonal means of contraception during and 4 weeks following mifepristone treatment.

MiFEPRIStone

May diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). MiFEPRIStone may increase the serum concentration of Estrogen Derivatives (Contraceptive). Management: Women of childbearing potential should use an effective, nonhormonal means of contraception during and 4 weeks following mifepristone treatment.

Mitotane

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane.

Modafinil

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: The manufacturer recommends that patients use nonhormonal contraceptives, in addition to or in place of hormonal contraceptives, during and for one month following treatment with modafinil.

Mycophenolate

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Average AUC values were unchanged, but there was evidence of substantial patient-to-patient variability in response to this combination. Management: Women of childbearing potential who are receiving mycophenolate mofetil should consider using an alternative and/or additional form of contraception.

Mycophenolate

May decrease the serum concentration of Progestins (Contraceptive). Management: Use of an additional or alternative (nonhormonal) method of contraception should be considered.

Nafcillin

May increase the metabolism of Estrogen Derivatives (Contraceptive). Management: Use of an alternative, nonhormonal form of contraception during nafcillin therapy is recommended.

Nelfinavir

May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction.

Nevirapine

May decrease the serum concentration of Estrogen Derivatives (Contraceptive).

Nevirapine

May decrease the serum concentration of Progestins (Contraceptive). Management: Instruct patients receiving nevirapine to use an alternative or additional nonhormonal contraceptive. Nevirapine product labeling however suggests that depo-medroxyprogesterone acetate may be used as a sole method of contraception.

OXcarbazepine

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal contraceptive is recommended.

OXcarbazepine

May decrease the serum concentration of Progestins (Contraceptive). Management: Contraceptive failure is possible. Use of an additional or alternative, nonhormonal method of contraception is recommended.

Perampanel

May decrease the serum concentration of Progestins (Contraceptive). Management: Patients should use an alternative, nonhormonal-based form of contraception both during the concurrent use of perampanel and for 1 month after discontinuing perampanel.

Phenytoin

May diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal means of contraception is recommended.

Phenytoin

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended.

Pitolisant

May diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). Management: The combination of hormonal contraceptives with pitolisant should be avoided, and an alternate means of contraception should be used.

Pitolisant

May diminish the therapeutic effect of Progestins (Contraceptive). Management: The combination of hormonal contraceptives with pitolisant should be avoided, and an alternate means of contraception should be used.

Pitolisant

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Combined use of pitolisant with a CYP3A4 substrate that has a narrow therapeutic index should be avoided. Other CYP3A4 substrates should be monitored more closely when used with pitolisant.

Pomalidomide

May enhance the thrombogenic effect of Estrogen Derivatives. Management: Canadian pomalidomide labeling recommends caution with use of hormone replacement therapy and states that hormonal contraceptives are not recommended. US pomalidomide labeling does not contain these specific recommendations.

Pomalidomide

Progestins may enhance the thrombogenic effect of Pomalidomide. Management: Canadian pomalidomide labeling recommends caution with use of hormone replacement therapy and states that hormonal contraceptives are not recommended. US pomalidomide labeling does not contain these specific recommendations.

Primidone

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Use of alternative, nonhormonal contraceptives is recommended.

Protease Inhibitors

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Use oral contraceptives containing at least 35mcg ethinyl estradiol with atazanavir/ritonavir, or no more than 30mcg in patients receiving atazanavir alone. Use of an alternative, non-hormonal contraceptive is recommended with other protease inhibitors. Exceptions: Indinavir.

Retinoic Acid Derivatives

May diminish the therapeutic effect of Progestins (Contraceptive). Retinoic Acid Derivatives may decrease the serum concentration of Progestins (Contraceptive). Management: Two forms of effective contraception should be used in patients receiving retinoic acid derivatives. Particularly, microdosed progesterone-only preparations may be inadequately effective. Exceptions: Adapalene; Bexarotene (Topical); Tretinoin (Topical).

Rifamycin Derivatives

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal contraceptive is recommended.

Rifamycin Derivatives

May decrease the serum concentration of Progestins (Contraceptive). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended.

Rufinamide

May decrease the serum concentration of Ethinyl Estradiol.

Saquinavir

May decrease the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction.

St John's Wort

May diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Consider an alternative to St John's wort if possible. If this combination is used, an alternative, nonhormonal contraceptive is recommended.

St John's Wort

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Consider using a product other than St John's wort. Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended.

St John's Wort

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling.

Sugammadex

May decrease the serum concentration of Progestins (Contraceptive). Management: Patients receiving any hormonal contraceptive (oral or non-oral) should use an additional, nonhormonal contraceptive method during and for 7 days following sugammadex treatment.

Sugammadex

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Patients receiving any hormonal contraceptive (oral or non-oral) should use an additional, nonhormonal contraceptive method during and for 7 days following sugammadex treatment.

Tipranavir

Estrogen Derivatives may enhance the dermatologic adverse effect of Tipranavir. The combination of tipranavir/ritonavir and ethinyl estradiol/norethindrone was associated with a high incidence of skin rash. Tipranavir may decrease the serum concentration of Estrogen Derivatives. Management: Women using hormonal contraceptives should consider alternative, non-hormonal forms of contraception.

Tipranavir

May increase the serum concentration of Progestins (Contraceptive). Management: Use an alternative or additional method of contraception due to possibly decreased contraceptive effectiveness. Injected depot medroxyprogesterone acetate does not appear to participate in this interaction.

TiZANidine

CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use is necessary, initiate tizanidine at an adult dose of 2 mg and increase in 2 to 4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions.

Tobacco (Smoked)

May enhance the adverse/toxic effect of Estrogen Derivatives (Contraceptive). Specifically, the risk of serious cardiovascular events (eg, stroke, venous thromboembolism, myocardial infarction) may be increased. Management: Avoid cigarette smoking in patients who use estrogen containing contraceptives whenever possible. If combined, monitor for signs and symptoms of serious cardiovascular events (eg, stroke, venous thromboembolism, myocardial infarction).

Topiramate

May decrease the serum concentration of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Risk appears greatest for higher topiramate doses (200 mg/day or greater). Some have recommended using at least 50 mcg/day of ethinyl estradiol, but the effectiveness of this is unclear. Consider a nonhormonal form of contraception.

Topiramate

May decrease the serum concentration of Progestins (Contraceptive). Management: Caution patients that this combination may be associated with reduced contraceptive effectiveness. Consider adding an additional (non-hormonal) contraceptive method.

Vitamin K Antagonists (eg, warfarin)

Estrogen Derivatives (Contraceptive) may diminish the anticoagulant effect of Vitamin K Antagonists. In contrast, enhanced anticoagulant effects have also been noted with some products.

Vitamin K Antagonists (eg, warfarin)

Progestins (Contraceptive) may diminish the anticoagulant effect of Vitamin K Antagonists. In contrast, enhanced anticoagulant effects have also been noted with some products. Management: When possible, concomitant hormonal contraceptives and coumarin derivatives should be avoided in order to eliminate the risk of thromboembolic disorders. Consider using an alternative, nonhormonal contraceptive.

Risk Factor X (Avoid combination)

Anastrozole

Estrogen Derivatives may diminish the therapeutic effect of Anastrozole.

Antihepaciviral Combination Products

Ethinyl Estradiol may enhance the hepatotoxic effect of Antihepaciviral Combination Products. Management: Use of ethinyl estradiol must be discontinued prior to use of this combination; ethinyl estradiol can be restarted 2 weeks after cessation of the antihepaciviral combination product.

Dasabuvir

Ethinyl Estradiol may enhance the hepatotoxic effect of Dasabuvir.

Dehydroepiandrosterone

May enhance the adverse/toxic effect of Estrogen Derivatives.

Encorafenib

May decrease the serum concentration of Estrogen Derivatives (Contraceptive).

Encorafenib

May decrease the serum concentration of Progestins (Contraceptive).

Exemestane

Estrogen Derivatives may diminish the therapeutic effect of Exemestane.

Glecaprevir and Pibrentasvir

Ethinyl Estradiol may enhance the adverse/toxic effect of Glecaprevir and Pibrentasvir. Specifically, the risk for ALT elevation may be increased with this combination.

Griseofulvin

May diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible.

Hemin

Estrogen Derivatives may diminish the therapeutic effect of Hemin.

Indium 111 Capromab Pendetide

Estrogen Derivatives may diminish the diagnostic effect of Indium 111 Capromab Pendetide.

Ixazomib

May decrease the serum concentration of Progestins (Contraceptive). More specifically, use of ixazomib with dexamethasone may decrease the serum concentrations of contraceptive progestins. Management: Patients of childbearing potential should use a nonhormonal barrier contraceptive during and 90 days following ixazomib treatment.

Ospemifene

Estrogen Derivatives may enhance the adverse/toxic effect of Ospemifene. Estrogen Derivatives may diminish the therapeutic effect of Ospemifene.

Tranexamic Acid

Progestins (Contraceptive) may enhance the thrombogenic effect of Tranexamic Acid.

Tranexamic Acid

Estrogen Derivatives (Contraceptive) may enhance the thrombogenic effect of Tranexamic Acid.

Ulipristal

May diminish the therapeutic effect of Progestins. Progestins may diminish the therapeutic effect of Ulipristal. Management: Ulipristal for uterine fibroids (Canadian indication): avoid progestins within 12 days of stopping ulipristal; as emergency contraceptive (U.S. indication): avoid progestins within 5 days of stopping ulipristal.

Monitoring parameters:

  • Assessment of pregnancy status (prior to therapy);
  • weight (optional;
  • BMI at baseline may be helpful to monitor changes during therapy);
  • blood pressure (prior to therapy and yearly);
  • assess potential health status changes at routine visits.
  • If all doses have not been taken on schedule and 1 menstrual period is missed, the possibility of pregnancy should be considered.
  • If 2 consecutive menstrual periods are missed, assess pregnancy status before a new dosing cycle is started.
  • Monitor patient for:
    • vision changes;
    • blood pressure;
    • signs or symptoms of depression;
    • glycemic control in patients with diabetes;
    • signs and symptoms of thromboembolic disorders;
    • lipid profiles in patients being treated for hyperlipidemias.
  • Adequate diagnostic measures should be performed to rule out malignancy in all cases of undiagnosed abnormal vaginal bleeding.

How to administer Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia)?

  • Administer at the same time every day; one dose is taken daily without interruption.
  • Guidelines are available if severe diarrhea or vomiting occur during or within 24 hours of taking an oral contraceptive tablet.
  • Combined hormonal contraceptives may be initiated at any time during the menstrual cycle if it is reasonably sure the woman is not pregnant.
  • Back-up contraception should be used for weak unless contraception is initiated within the first 5 days of menstrual bleeding or the woman abstains from sexual intercourse.
  • Combined hormonal contraceptives may be started immediately following or within the weak of a first or second-trimester abortion; backup contraception is needed for a weak unless contraception is started at the time of surgical abortion.

Mechanism of action of Ethinyl estradiol and ethynodiol diacetate (Kelnor, Zovia):

  • Combination hormonal contraceptives can inhibit ovulation through a negative feedback mechanism on hypothalamus.
  • This alters the normal pattern gonadotropin production of a follicle stimulating hormone (FSH), and luteinizing hormone from the anterior pituitary.
  • FSH in the follicular phase and midcycle surge of gonadotropins is inhibited. 
  • Combination hormonal contraceptives can also cause alterations in the genital system, including cervical mucus changes, which makes it difficult for sperm penetration, even if there is ovulation.
  • Alterations in the endometrium can also cause unfavorable conditions for nidation.
  • Combinations of hormonal contraceptives drugs could alter tubal transport of the eggs through the fallopian tubes. 
  • The fertility of sperm may also be affected by progestational drugs.
  • Combination hormonal contraceptives can inhibit ovulation through a negative feedback mechanism on hypothalamus.
  • This alters the normal pattern gonadotropin production of a follicle stimulating hormone (FSH), and luteinizing hormone from the anterior pituitary.
  • FSH in the follicular phase and midcycle surge of gonadotropins is inhibited. 
  • Combination hormonal contraceptives can also cause alterations in the genital system, including cervical mucus changes, which makes it difficult for sperm penetration, even if there is ovulation.
  • Alterations in the endometrium can also cause unfavorable conditions for nidation.
  • Combinations of hormonal contraceptives drugs could alter tubal transport of the eggs through the fallopian tubes. 
  • The fertility of sperm may also be affected by progestational drugs.

Absorption:

  • Ethinylestradiol (EE) and ethynodiol diacetate: Rapidly absorbed

Protein binding:

  • EE: Albumin
  • Norethindrone: Albumin and sex hormone-binding globulin (SHBG); SHBG capacity affected by plasma EE levels

Metabolism:

  • EE: Hepatic; forms metabolites
  • Ethynodiol diacetate: Hepatic; rapidly converted to norethindrone (active) and other metabolites

Excretion:

  • EE: Urine, feces
  • Ethynodiol diacetate: Urine, feces as metabolites
  • Pharmacokinetic note: Also see Norethindrone monograph.
  • [/bg_collapse]

International Brand names of Ethinyl estradiol and ethynodiol diacetate:

  • Kelnor 1/35
  • Kelnor 1/50
  • Ovulen 50
  • Zovia 1/35E (28)
  • Zovia 1/50E (28)
  • Demulen 30

Ethinyl estradiol and ethynodiol diacetate Brand Names in Pakistan:

There is no brand available in Pakistan.

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