Ethinyl estradiol and desogestrel tablets are a combination of oral hormonal contraceptive pills that inhibit ovulation and prevents pregnancy.
Indications of Ethinyl estradiol and desogestrel:
-
Contraception:
- It is indicated for the prevention of conception.
-
Off Label Use of Ethinyl estradiol and desogestrel in Adults:
- Abnormal uterine bleeding
- Dysmenorrhea
- Hirsutism
- Menstrual bleeding (menorrhagia)
- Polycystic ovary syndrome (PCOS) in women with menstrual irregularities and hirsutism/acne
Ethinyl estradiol and desogestrel dosage for females for contraception:
- One tablet per oral every 24 hours.
-
Schedule 1 (Sunday starter):
- The dose should be administered on the first Sunday after the onset of menstruation.
- If the menstrual period starts on Sunday, take the first tablet on the same day. With a Sunday start, an additional method of contraception should be commenced until after the first week of consecutive administration.
-
Schedule 2 (Day 1 starter):
- Dose starts on the first day of the menstrual cycle taking 1 tablet every 24 hours.
- If all doses have not been taken on schedule and one menstrual period is missed, pregnancy should be ruled out. If two consecutive menstrual periods are missed, a pregnancy test is necessary before administering a new dosing cycle.
-
Missed or late doses:
-
If one dose is late (<24 hours or 24 to <48 hours):
- Take the dose as soon as possible. Continue remaining doses at the usual time (even if that means 2 doses on the same day).
-
If ≥2 consecutive doses are missed (≥48 hours ):
- Take the most recently missed dose as soon as possible, any other missed doses should be discarded.
- Remaining doses should be continued at the usual time (even if that means taking 2 doses on the same day);
- use other contraception methods until hormonal pills have been taken for one week.
- If doses were missed during the last week of hormonal tablets (eg, days 15 to 21 of a 28-day pack), a hormone-free interval should be skipped by finishing the current pack and starting a new pack.
- If unable to start a new pack immediately, other methods of contraception should be used until hormonal pills from a new pack have been taken for one week.
- Consider the use of emergency contraception in some situations (refer to guidelines for details).
-
Ethinyl estradiol and desogestrel treatment dose in children:
Refer to adults dosing.
Ethinyl estradiol and desogestrel pregnancy Risk Factor: X
- It is not recommended for use during pregnancy.
- If pregnancy does occur, combination hormonal contraceptives should be used.
- If used in an early pregnancy, combination hormonal contraceptives have not been shown to cause any adverse effects for the mother or baby.
- Postpartum women should not start combination hormonal contraceptives within 21 days of delivery. This is due to an increased risk of venous embolism (VTE) in postpartum women.
- Postpartum day 42 reduces the risk to baseline.
- Women can use combination hormonal contraceptives between 21 and 42 days after birth depending on their individual risk factors for Venous embolism.
Use of desogestrel and ethinyl estradiol during breastfeeding
- Breast milk contains contraceptive steroids.
- Combination hormonal contraceptives can cause jaundice and breast-engorgement in breastfeeding infants.
- The adverse effects of maternal use of hormonal contraceptives during breastfeeding have not been shown to be detrimental to infant growth.
- The hormonal contraceptives can reduce milk production. However, the manufacturer suggests that you use other contraceptives until your child is weaned.
- When starting treatment for breastfeeding women, it is important to evaluate the benefits/risks and other options to hormonal combination contraception.
Ethinyl estradiol and desogestrel dose adjustment in renal disease:
There are no dosage adjustments provided in manufacturer's labeling (has not been studied) Use with caution and blood pressure monitoring should be done. Other forms of contraception should be considered.
Ethinyl estradiol and desogestrel dose adjustment in liver disease:
The drug therapy is contraindicated in patients with hepatic derangement.
Side effects of ethinyl estradiol and desogestrol:
Reactions listed are based on reports in clinical trials or observational studies with ethinyl estradiol/desogestrel or other oral contraceptives.
-
Central Nervous System:
- Depression
- Headache
- Migraine
- Mood Changes
-
Dermatologic:
- Erythema Multiforme
- Erythema Nodosum
- Skin Rash
- Urticaria
-
Endocrine & Metabolic:
- Decreased Libido
- Fluid Retention
- Increased Libido
- Weight Gain
- Weight Loss
-
Gastrointestinal:
- Abdominal Pain
- Diarrhea
- Nausea
- Vomiting
-
Genitourinary:
- Breast Hypertrophy
- Breast Tenderness
- Mastalgia
- Vaginal Discharge
-
Hypersensitivity:
- Hypersensitivity Reaction
-
Ophthalmic:
- Contact Lens Intolerance
Contraindication to Ethinyl estradiol and desogestrol:
- Hypersensitivity to ethinyl esteradiol, desogestrel or any other component of the formulation
It is not recommended to use hormonal contraception in:
- Breast cancer/endometrial carcinoma
- hormone-sensitive malignancy,
- Hepatic tumors (benign and malignant)
- Cholestatic jaundice during pregnancy or hormonal contraceptive use
- pregnancy,
- abnormal genital bleeding (cause unknown),
- concurrent therapy with hepatitis C drug combinations containing ombitasvir/ paritaprevir/ ritonavir with or without dasabuvir.
- For example, conditions that predispose to arterial or vein thrombosis
- Coronary artery disease
- Diabetes mellitus and vascular disease
- thrombophlebitis,
- Thromboembolism
- Hypercoagulopathies acquired or inherited
- thrombophilias,
- Uncontrolled hypertension is defined as systolic >=160mm Hg or diastolic>=100mm Hg.
- Valvular heart disease and thrombogenic complications
- Headaches with focal neurological symptoms
- Longevity of immobility
- Women over 35 years old
- smokers.
Additional contraindications are listed in the Canadian labeling
- Ocular lesions, such as partial or total visual loss or defect
- Pancreatitis is associated with severe hypertriglyceridemia
- thrombophilias
- severe dyslipoproteinemia
- Migraine and aura
- Predispositions to arterial or venous thrombosis may be hereditary or acquired.
- Resistance to activated protein C (APC), and mutation Factor V Leiden,
- Antithrombin-III deficiencies
- protein C deficiency,
- protein S deficiency,
- Hyperhomocysteinemia (eg due to MTHFR C677T and A1298 mutations).
- Prothrombin mutation G20210A
- antiphospholipid-antibodies (anticardiolipin antibodies, lupus anticoagulant).
It is not known if estrogens or progestins cross-react with each other. Cross-sensitivity is possible due to chemical structures and/or pharmacologic effects that are the same. However, it cannot be excluded with certainty.
Warnings and precautions
-
Breast cancer
- Combination hormonal contraceptives are not associated with breast cancer in women who are at high risk (family history, susceptibility genes (BRCA1, BRCA2)).
- Combination hormonal contraceptives may make it worse for women who have had breast cancer in the past. This is because it is a hormone sensitive tumor.
- Women with breast cancer history or who have had it are advised to not use this product.
-
Cervical cancer:
- Hormonal contraception is linked to an increased risk of cervical cancer. However, there are not enough studies and they may also be associated with other risk factors.
- Hormonal therapy may improve the prognosis for an existing disease.
- Women awaiting treatment for cervical carcinoma can use combination hormonal contraceptives.
-
Chloasma
- Combination hormonal contraceptives as well as pregnancy and sun exposure are some of the triggers for chloasma.
- Women with higher risk factors or a tendency to develop should not be exposed to sunlight or ultraviolet radiation during treatment.
-
Cholestasis:
- Cholestasis risk increases with previous cholestatic jaundice during pregnancy, or with previous oral contraceptive use. Therefore, its use is not recommended.
-
The Lipid Effects
- Combining hormonal contraceptives can lead to abnormal lipid levels, including serum triglycerides.
-
Retinal vascular embolism:
- Unexplained visual loss, proptosis or papilledema should be stopped immediately and a retinal vein thrombosis evaluation should be performed.
-
Thromboembolic disorders
- The risk of venous embolism is higher in the first year, and lower than that associated with hormonal therapy during pregnancy.
- According to some studies, the risk of developing breast cancer in preparations containing third- or fourth-generation progestins/high doses ethinyl estradiol is greater.
- There is an increased risk of venous thromboembolism in patients with inherited thrombophilias (eg, protein C or S deficiency/factor V Leiden mutation/prothrombin mutation/antithrombin deficiency).
- The risk of developing thrombosis can be increased by hormonal contraception, smoking, hypertension, obesity, age >35, and other factors like smoking, hypertension, obesity, or overweight.
- Hormonal contraception increases the risk of arterial thrombosis (eg stroke, MI), so it should not be used in women who have had strokes or are suffering from ischemic heart disease.
- Women with high rates of arterial or vein thrombosis should not use combination hormonal contraceptives.
-
Vaginal bleeding
- In the initial 3 months of therapy, missed periods, intra-cyclic bleeding/spotting and breakthrough can all be observed.
- Unresolved, irregular vaginal bleeding should be treated immediately to rule out malignancy and pregnancy.
- After stopping combination hormonal contraceptives, amenorrhea/oligomenorrhea can occur especially when such a condition was preexistent.
-
Cardiovascular disease
- Use with caution in patients with risk factors for cardiovascular disease such as smokers/ hypertension/deranged lipid profile/ elderly/DM.
- The incidence of cardiovascular disease may be increased by hormonal contraception.
-
Depression
- Patients at high risk for depression should be cautious. If you have severe depression, discontinue use of this drug.
-
Diabetes:
- Combination hormonal contraception can cause impaired glucose tolerance. However, it has limited effect on daily insulin requirements and has no long-term effects on diabetes control for women with nonvascular diseases.
- Women with concomitant nephropathy/neuropathy/retinopathy, other vascular disease/DM >20 years duration should be regularly monitored based on the severity of the condition.
- It is not recommended for women with diabetes mellitus or vascular disease.
-
Fluid retention can lead to more severe diseases
- Fluid retention can occur so it is important to avoid fluid retention in patients suffering from fluid retention.
-
Endometrial and ovarian cancers:
- Combination hormonal contraceptives are less likely to cause endometrial/ovarian cancer in women who use them.
- Oral contraceptives may be beneficial in reducing the risk for ovarian cancer, especially those with BRCA1 or BRCA2 mutations.
- Women awaiting treatment for ovarian or endometrial cancer can receive combination hormonal therapy.
-
Gallbladder disease
- Drug therapy can lead to an increase in gallbladder disease risk or worsening of existing gallbladder diseases.
-
Hepatic adenomas and carcinomas
- Combination hormonal contraceptives should not be used in conjunction with ruptured hepatic tumors. This could lead to life-threatening intra-abdominal hemorhage.
- Combination hormonal therapy (rare) may increase the risk of developing hepatocellular carcinoma.
- Women with hepatocellular cancer should not take the drug.
-
Hepatic impairment
- Poor metabolism of hormonal combination contraceptives can be caused by hepatic derangement.
- In the event of liver dysfunction or jaundice, it is important to stop taking the drug.
- Women with mild (compensated), but not severe (decompensated), cirrhosis may be treated with combination hormonal contraceptives.
-
Hepatitis
- Women with severe viral hepatitis, flares or women who are pregnant by combination hormonal contraceptives should not use them.
- Patients with chronic hepatitis have not shown that the drug increases the severity or rate of cirrhotic fibrisis.
- It has not been shown to cause severe liver dysfunction or liver failure in women who are carriers.
-
Hereditary angioedema:
- The therapy might cause angioedema or hereditary symptoms.
-
Hypertension:
- Hypertension is more common in older people, with higher doses and longer periods of time.
- It should not be prescribed for hypertension or vascular disease.
- Treatment of mild hypertension (140-159 mmHg systolic, 90-99 mmHg diastolic) and controlled hypertension may be worth the risks.
- When prescribing contraceptives, it is important to consider the risk factors for cardiovascular disease such as older age/smoking/DM.
- The manufacturer forbids the use of this product in women suffering from uncontrolled hypertension.
-
Migraine
- You should always be on the lookout for any new, persistent, severe or severe headaches.
- In migraines that don't have aura, you can use combination hormonal contraceptives (including menstrual migraines).
- It is not recommended for women suffering from headaches with focal neurological symptoms.
-
Renal impairment
- It is important that women with kidney disease are prescribed another method of contraception.
-
Transplantation of solid-organs:
- Women who have had to undergo complicated organ transplants have experienced serious medical complications (eg, graft rejection/rejection/cardial allograft vasculopathy).
- Combination hormonal contraceptives are not recommended for women who have had complicated organ transplants (Curtis 2016,b).
-
Systemic lupus erythematosus (SLE):
- Systemic lupus, or SLE, is a condition in which women with systemic erythematosus (SLE), have a higher incidence of stroke, heart disease, and venous embolism.
- Women with SLE and positive or unknown antiphospholipid antibodies should not use hormonal contraceptives in combination. The risk of arterial or venous embolism is higher.
Ethinyl estradiol and desogestrel: 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). |
|
CYP2C19 Inducers (Moderate) |
May decrease the serum concentration of CYP2C19 Substrates (High risk with Inducers). |
|
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. |
|
CYP2C19 Inducers (Strong) |
May increase the metabolism of CYP2C19 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. |
|
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 CYP2C19 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP2C19 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. |
|
Enzalutamide |
May decrease the serum concentration of CYP2C19 Substrates (High risk with Inducers). Conversely, concentrations of active metabolites may be increased for those drugs activated by CYP2C19. Management: Concurrent use of enzalutamide with CYP2C19 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP2C19 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. |
|
Dehydroepiandrosterone |
: 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:
- Different parameters including assessment of pregnancy before therapy/blood pressure before therapy and yearly/ weight (Body mass index at baseline), and potential health status changes assessment routinely should be checked.
- If all doses have not been taken on schedule and 1 menstrual period is missed, pregnancy should be ruled out.
- If 2 consecutive menstrual periods are missed, assess pregnancy status before starting a new dosing cycle.
- Monitoring for visual changes/ BP/signs/symptoms of thromboembolism/ signs/symptoms of depression/ glycemic control in patients with DM/ lipid profiles in patients being treated for hyperlipidemias should be done.
- Diagnostic measures such as endometrial sampling, if needed should be done to rule out malignancy in case undiagnosed abnormal vaginal bleeding.
How to administer Ethinyl estradiol and desogestrel?
- Administer at the same time each day at intervals not exceeding 24 hours.
- For the 21-tablet package, a single tablet is taken for 21 consecutive days, followed by one week off medication period, the new course should be started on the 8th day after the last tablet is taken.
- For the 28-tablet package, one tablet should be taken once daily without interruption.
- According to the manufacturer, an alternate method of contraception should be used if vomiting/diarrhea develops.
- Additional guidelines are available. Combined hormonal contraceptives can be started at any time during the menstrual cycle if pregnancy is ruled out.
- Back-up contraception should be used for one week unless contraception is started within the first 5 days of menstrual bleeding or abstinence from sexual intercourse.
- Combined hormonal contraceptives should be administered immediately following or within one week of a first or second-trimester abortion.
- Backup contraception is required for one week unless contraception is started at the time of surgical abortion.
Ethinyl estradiol and desogestrel Mechanism of action:
- Combination hormonal contraceptives can cause a negative feedback mechanism to the hypothalamus, leading to ovulation inhibition.
- This alters the normal pattern gonadotropin production of a Follicle-stimulating Hormone (FSH), and luteinizing hormone from the anterior pituitary.
- The follicular phase FSH is inhibited and the midcycle surge gonadotropins are not. Combination hormonal contraceptives can cause genital tract changes, including changes to the cervical mucus.
- This makes it difficult for sperm penetration, even if there is ovulation. Alterations in the endometrium can also cause unfavorable conditions for nidation.
- Combination hormonal contraceptives can cause alteration in the tubal transport and ovary through the fallopian tube. Alteration in sperm fertility can be caused by progesterone drugs.
The absorptionDesogestrel, Ethinyl estradiol are rapid and complete Protein binding ofEtonogestrel, (active metabolite), 98% to 99 percent, primarily to the sex hormone binding globulin. Ethinyl estradiol, 98.3% is primarily bound to albumin. Metabolism: Desogestrel: Hepatic via CYP2C9 to active metabolite etonogestrel (3-keto-desogestrel); Etonogestrel metabolized via CYP3A4 Ethinyl estradiol: Hepatic; forms metabolites Bioavailability: Monophasic preparations: Etonogestrel: ~84%; Ethinyl estradiol: ~83%; biphasic and triphasic preparations increased the bioavailability of etonogestrel and ethinyl estradiol. Half-life elimination: Monophasic preparations: Etonogestrel: 38 ± 20 hours; Ethinyl estradiol: 26 ± 6.8 hours Time to peak: Monophasic preparations: Etonogestrel: 1.4 ± 0.8 hours; Ethinyl estradiol: 1.5 ± 0.8 hours; Time to the peak of etonogestrel and Ethinyl estradiol varies by day in the cycle for biphasic and triphasic preparations Excretion: Etonogestrel and Ethinyl estradiol: Urine and feces (as metabolites)
Ethinyl estradiol and desogestrel Brand Names (International):
- Apri;
- Azurette;
- Bekyree;
- Caziant;
- Cyclessa [DSC];
- Cyred;
- Cyred EQ;
- Desogen [DSC];
- Emoquette;
- Enskyce;
- Isibloom;
- Juleber;
- Kariva;
- Kimidess [DSC];
- Mircette;
- Ortho-Cept (28) [DSC];
- Pimtrea;
- Reclipsen;
- Simliya;
- Velivet;
- Viorele
- Apri 21
- Apri 28
- Freya 21
- Freya 28
- Linessa 21
- Linessa 28
- Marvelon
- Mirvala 21
- Mirvala 28
- Reclipsen 21
- Reclipsen 28
- Alenvona
- Bemasive
- Bimizza
- Celoxin
- Ciclidon
- Cimizt
- Daisy
- Daisy-30
- Dal
- Desmin
- Desolett
- Desolett 28
- Desolon
- Desoren
- Destrel
- Destrol 28
- Estraceptin
- Femilon
- Feminet
- Gedare
- Gracial 28
- Lamuna
- Lestramyl
- Liana
- Lovina
- Madeline
- Marvelon
- Marvelon 21
- Marvelon 28
- Marviol
- Mercilon
- Meuri
- Microdiol
- Minny
- Minny 28
- Miravelle Suave
- Munalea
- Neolette
- Novelon
- Novial
- Novinet
- Novynette
- Oilezz
- Praline
- Primera 30
- Regulon
- Suavuret
- Varnoline
Ethinyl estradiol and desogestrel Brands in Pakistan:
Brands in Pakistan will be posted later.