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Ethinyl Estradiol and Norethindrone


General


Pronunciation

(ETH in il es tra DYE ole & nor eth IN drone)


Brand Names: U.S.

  • Alyacen 1/35
  • Alyacen 7/7/7
  • Aranelle
  • Balziva
  • Blisovi 24 Fe
  • Blisovi Fe 1/20
  • Brevicon
  • Briellyn
  • Cyclafem 1/35
  • Cyclafem 7/7/7
  • Dasetta 1/35
  • Dasetta 7/7/7
  • Estrostep Fe
  • Femcon Fe
  • femhrt
  • Fyavolv
  • Generess Fe
  • Gildagia
  • Gildess 1.5/30
  • Gildess 1/20
  • Gildess 24 Fe
  • Gildess FE 1.5/30
  • Gildess FE 1/20
  • Jevantique Lo
  • Jinteli
  • Junel 1.5/30
  • Junel 1/20
  • Junel Fe 1.5/30
  • Junel Fe 1/20
  • Junel Fe 24
  • Kaitlib Fe
  • Larin 1.5/30
  • Larin 1/20
  • Larin 24 Fe
  • Larin Fe 1.5/30
  • Larin Fe 1/20
  • Layolis Fe
  • Leena
  • Lo Loestrin Fe
  • Lo Minastrin Fe [DSC]
  • Loestrin 21 1.5/30
  • Loestrin 21 1/20
  • Loestrin 24 Fe
  • Loestrin Fe 1.5/30
  • Loestrin Fe 1/20
  • Lomedia 24 Fe
  • Microgestin 1.5/30
  • Microgestin 1/20
  • Microgestin 24 Fe
  • Microgestin Fe 1.5/30
  • Microgestin Fe 1/20
  • Minastrin 24 Fe
  • Modicon
  • Necon 0.5/35
  • Necon 1/35
  • Necon 10/11
  • Necon 7/7/7
  • Norinyl 1+35
  • Nortrel 0.5/35
  • Nortrel 1/35
  • Nortrel 7/7/7
  • Ortho-Novum 1/35
  • Ortho-Novum 7/7/7
  • Ovcon 35
  • Philith
  • Pirmella 1/35
  • Pirmella 7/7/7
  • Tarina FE 1/20
  • Tilia Fe
  • Tri-Legest Fe
  • Tri-Norinyl
  • Vyfemla
  • Wera
  • Wymzya Fe
  • Zenchent
  • Zenchent Fe

Indications


Use: Labeled Indications

Acne vulgaris: For the treatment of moderate acne vulgaris in females at least 15 years of age.

Limitations of Use: When used for acne, use only in females ≥15 years of age who have achieved menarche, who also desire combination hormonal contraceptive therapy, are unresponsive to topical treatments, have no contraindications to combination hormonal contraceptive use, and plan to stay on therapy for ≥6 months.

Contraception: For the prevention of pregnancy.

Vasomotor symptoms associated with menopause (femhrt, Jevantique Lo, Jinteli): Treatment of moderate to severe vasomotor symptoms associated with menopause.

Osteoporosis prevention (female) (femhrt, Jevantique Lo, Jinteli): Prevention of postmenopausal osteoporosis.

Limitations of use: For use only in women at significant risk of postmenopausal osteoporosis; consider use of nonestrogen medications.


Contraindications


Combination hormonal contraceptives: Hypersensitivity to any component of the formulation; breast cancer, endometrial cancer or other estrogen- or progestin-dependent neoplasms (current or a history of), hepatic tumors or disease, pregnancy, undiagnosed abnormal uterine bleeding; cholestatic jaundice of pregnancy or jaundice with prior contraceptive pill use

Use is also contraindicated in women at high risk of arterial or venous thrombotic diseases for example, women with: Cerebrovascular disease, coronary artery disease, diabetes mellitus with vascular disease, DVT or PE (current or history of), hypertension (uncontrolled; specified as persistent blood pressure values ≥160 mm Hg systolic or ≥100 mm Hg diastolic in some product labeling), headaches with focal neurological symptoms; major surgery with prolonged immobilization; valvular heart disease with complications; thrombophlebitis or thromboembolic disorders; thrombophilic conditions

Canadian labeling: Additional contraindications (not in US labeling): Angina pectoris or myocardial infarction (current or history of), ocular lesion arising from ophthalmic vascular disease (such as partial or complete loss of vision or visual field defect), migraine with focal aura (current or history of), pancreatitis associated with severe hypertriglyceridemia (current or history of), severe dyslipoproteinemia, over 35 years of age and smoke; women with hereditary or acquired predisposition for arterial or venous thrombosis, for example: factor V Leiden mutation, activated protein C (APC-) resistance, antithrombin-III-deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia (eg, due to MTHFR C677T, A1298 mutations), prothrombin mutation G20210A, and antiphospholipid-antibodies (anticardiolipin antibodies, lupus anticoagulant).

Products used for postmenopausal indications: Angioedema, anaphylactic reaction, or hypersensitivity to any component of the formulation; undiagnosed abnormal genital bleeding; DVT or PE (current or history of); active or history of arterial thromboembolic disease (eg, stroke, MI); breast cancer (known, suspected or history of); estrogen-dependent tumor (known or suspected); hepatic impairment or disease; known protein C, protein S, antithrombin deficiency or other known thrombophilic disorders; pregnancy.

Canadian labeling: Additional contraindications (not in US labeling): endometrial hyperplasia, classical migraine, lactation

Documentation of allergenic cross-reactivity for estrogens and progestins is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.


ALERT: U.S. Boxed Warning

Cigarette smoke and serious cardiovascular events:

Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptive use. This risk increases with age, particularly in women over 35 years of age, and with the number of cigarettes smoked. For this reason, combination oral contraceptives should not be used in women who are over 35 years and smoke.

Endometrial cancer:

There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy has been shown to reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Adequate diagnostic measures, including directed or random endometrial sampling when indicated, should be taken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal genital bleeding.

Cardiovascular disease:

Estrogen-alone therapy should not be used for the prevention of cardiovascular disease. The Womens Health Initiative (WHI) estrogen-alone substudy reported increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) during 7.1 years of treatment with daily oral conjugated estrogens 0.625 mg alone, relative to placebo.

Estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease. The WHI estrogen plus progestin substudy reported increased risks of DVT, pulmonary embolism (PE), stroke, and myocardial infarction (MI) in postmenopausal women (50 to 79 years of age) during 5.6 years of treatment with daily oral conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg), relative to placebo.

Breast cancer:

The WHI estrogen-plus-progestin substudy demonstrated an increased risk of invasive breast cancer.

Dementia:

Estrogen-alone therapy should not be used for the prevention of dementia. The WHI Memory Study (WHIMS) estrogen-alone ancillary study of the WHI reported an increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 5.2 years of treatment with daily conjugated estrogens (0.625 mg) alone, relative to placebo. It is unknown whether this finding applies to younger postmenopausal women.

Estrogen plus progestin therapy should not be used for the prevention of dementia. The WHIMS estrogen plus progestin ancillary study of the WHI reported an increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg), relative to placebo. It is unknown whether this finding applies to younger postmenopausal women.

Risk vs benefit:

In the absence of comparable data, these risks should be assumed to be similar for other doses of conjugated estrogens (with or without medroxyprogesterone acetate) and other dosage forms of estrogens (with or without progestins). Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman.


Dosing and Administration


Dosing: Adult

Acne: Adolescents ≥15 years and Adults: Females: Oral (Estrostep Fe, Tilia Fe, Tri-Legest Fe): Refer to dosing for contraception

Contraception: Females: One tablet once daily

Schedule 1 (Sunday starter): Dose begins on first Sunday after onset of menstruation; if the menstrual period starts on Sunday, take first tablet that very same day. (This schedule is not preferred for all products [eg, Generess Fe, Lo Loestrin Fe, Lo Minastrin Fe]). With a Sunday start, an additional method of contraception should be used until after the first 7 days of consecutive administration (all products).

Schedule 2 (Day 1 starter): Dose starts on first day of menstrual cycle taking 1 tablet daily.

Additional contraceptive dosing considerations:

Switching from a different contraceptive:

Oral contraceptive: Start on the same day that a new pack of the previous oral contraceptive would have been taken.

Transdermal patch, vaginal ring, injection: Start on the day the next dose would have been due.

IUD or implant: Start on the day of removal. A backup method of contraception may be needed.

Use after first trimester abortion or miscarriage: Therapy may be started immediately. If not started immediately, a back-up method of contraception may be needed

Use after childbirth (in women who are not breast-feeding) or after second trimester abortion or miscarriage: Therapy may be started ≥4 weeks postpartum. Pregnancy should be ruled out prior to treatment if menstrual periods have not restarted. An additional method of contraception (nonhormonal) should be used until after the first 7 days of consecutive administration.

Also refer to prescribing information for product specific information or CDC 2013 for general guidance.

Missed or late doses (CDC 2013):

If one dose is late (<24 hours since dose should have been taken) or if one dose is missed (24 to <48 hours since 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 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 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 use of emergency contraception in some situations (refer to guidelines for details).

Also refer to prescribing information for product specific information.

Postmenopausal indications:General dosing guidelines: When treating postmenopausal women, use estrogens for the shortest duration possible at the lowest effective dose consistent with treatment goals. Reevaluate patients as clinically appropriate to determine if treatment is still necessary. Consider use of an estrogen with a progestin in postmenopausal women with a uterus. Women who have had a hysterectomy generally do not need a progestin; however one may be needed if there is a history of endometriosis. Dosage needs to be adjusted based upon the patients response.

Osteoporosis prevention: Females: Oral (femhrt, Jevantique Lo, Jinteli): One tablet daily

Vasomotor symptoms associated with menopause: Females: Oral (femhrt, Jevantique Lo, Jinteli): Initial: One tablet daily; patient should be re-evaluated at 3- to 6-month intervals to determine if treatment is still necessary.


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Acne: Adolescent females ≥15 years: Oral (Estrostep Fe, Tilia Fe, Tri-Legest Fe): Refer to adult dosing for contraception; not to be used prior to menarche

Contraception: Females: Oral: Refer to adult dosing; not to be used prior to menarche.


Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturers labeling (has not been studied); use with caution and monitor blood pressure closely. Consider other forms of contraception.


Dosing: Hepatic Impairment

Use is contraindicated in patients with hepatic impairment.


Administration

Combination hormonal contraceptives:

Administer at the same time each day at intervals not >24 hours; without regard to meals.

For some products (eg, Generess Fe, Lo Loestrin Fe, Lo Minastrin Fe), if vomiting or diarrhea occurs within 3 to 4 hours of a dose, consider the dose to be missed. Additional guidelines are also available (see CDC 2013).

For the 21-tablet package, one dose is taken for 21 consecutive days, followed by 7 days off of the medication; a new course begins on the 8th day after the last tablet is taken.

For the 28-tablet package, one dose is taken daily without interruption.

Postmenopausal indications: The use of a progestin should be considered when administering estrogens to postmenopausal women with a uterus.

Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 2]).


Dietary Considerations

May be taken without regard to meals. Ensure adequate calcium and vitamin D intake when used for the prevention of osteoporosis.


Storage

Store at controlled room temperature.

Estrostep Fe: Protect from light.


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, oral:

femhrt: Ethinyl estradiol 0.0025 mg and norethindrone acetate 0.5 mg [white tablets] (28s)

Fyavolv:

0.5/2.5: Ethinyl estradiol 0.0025 mg and norethindrone acetate 0.5 mg [white-off-white tablets] (28s, 90s)

1/5: Ethinyl estradiol 0.005 mg and norethindrone acetate 1 mg [blue tablets] (28s, 90s)

Jevantique Lo: Ethinyl estradiol 0.0025 mg and norethindrone acetate 0.5 mg [white tablets] (28s)

Jinteli: Ethinyl estradiol 0.005 mg and norethindrone acetate 1 mg [white tablets] (28s, 90s)

Tablet, oral [monophasic formulation]:

Alyacen 1/35: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 peach tablets and 7 light green inactive tablets] (28s)

Balziva: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 light peach tablets and 7 white inactive tablets] (28s)

Blisovi 24 Fe: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 white tablets] and ferrous fumarate 75 mg [4 brown tablets] (28s)

Blisovi Fe 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 yellow tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Brevicon: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [21 blue tablets and 7 orange inactive tablets] (28s)

Briellyn: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 light peach tablets and 7 white-off-white inactive tablets] (28s)

Cyclafem 1/35: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 pink tablets and 7 light green inactive tablets] (28s)

Dasetta 1/35: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 orange tablets and 7 white inactive tablets] (28s) [contains soya lecithin, tartrazine]

Gildagia: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 peach tablets and 7 light green inactive tablets] (28s)

Gildess 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [white tablets]

Gildess 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [light green tablets]

Gildess FE 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 white tablets] and ferrous fumarate 75 mg [7 white-speckled brown tablets] (28s)

Gildess FE 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [21 light green tablets] and ferrous fumarate 75 mg [7 white-speckled brown tablets] (28s)

Gildess 24 Fe: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 white tablets] and ferrous fumarate 75 mg [4 white-speckled brown tablets] (28s)

Junel 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [yellow tablets] (21s)

Junel 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [pink tablets] (21s)

Junel Fe 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 yellow tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Junel Fe 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [21 pink tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Junel Fe 24: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 pale yellow tablets] and ferrous fumarate 75 mg [4 brown tablets] (28s)

Larin 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 pale yellow tablets] (21s) [contains soya lecithin]

Larin 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [21 green tablets] (21s) [contains soya lecithin]

Larin Fe 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 pale yellow tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s) [contains soya lecithin]

Larin Fe 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [21 green tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s) [contains soya lecithin]

Larin 24 Fe: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 pale yellow tablets] and ferrous fumarate 75 mg [4 brown tablets] (28s)

Loestrin 21 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [light yellow tablets] (21s)

Loestrin 21 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [pink tablets] (21s)

Loestrin 24 Fe: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 white tablets] and ferrous fumarate 75 mg [4 brown tablets] (28s)

Loestrin Fe 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 light yellow tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Loestrin Fe 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [21 pink tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Lomedia 24 Fe: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 white tablets] and ferrous fumarate 75 mg [4 brown tablets] (28s)

Microgestin 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [white tablets] (21s)

Microgestin 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [green tablets] (21s)

Microgestin 24 Fe: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 white tablets] and ferrous fumarate 75 mg [4 brown tablets] (28s)

Microgestin Fe 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 white tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Microgestin Fe 1.5/30: Ethinyl estradiol 0.03 mg and norethindrone acetate 1.5 mg [21 green tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Modicon: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [21 white tablets and 7 green inactive tablets] (28s)

Necon 0.5/35: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [21 light yellow tablets and 7 white inactive tablets] (28s)

Necon 1/35: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 dark yellow tablets and 7 white inactive tablets] (28s)

Norinyl 1+35: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 yellow-green tablets and 7 orange inactive tablets] (28s)

Nortrel 0.5/35: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [21 light yellow tablets and 7 white inactive tablets] (28s)

Nortrel 1/35:

Ethinyl estradiol 0.035 mg and norethindrone 1 mg [yellow tablets] (21s)

Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 yellow tablets and 7 white inactive tablets] (28s)

Ortho-Novum 1/35: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 peach tablets and 7 green inactive tablets] (28s)

Ovcon 35: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 light peach tablets and 7 green inactive tablets] (28s)

Philith: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 tan tablets and 7 white inactive tablets] (28s)

Pirmella 1/35: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [21 peach tablets and 7 green inactive tablets] (28s)

Tarina FE 1/20: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [21 white tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Vyfemla: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 light peach tablets and 7 white inactive tablets] (28s)

Wera: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [21 light peach tablets and 7 white inactive tablets] (28s)

Zenchent: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 orange tablets and 7 white inactive tablets] (28s)

Tablet, chewable, oral [monophasic formulation]: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 tablets] and ferrous fumarate 75 mg [7 tablets] (28s)

Femcon Fe: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 white tablets] and ferrous fumarate 75 mg [7 brown tablets] [spearmint flavor] (28s)

Generess Fe: Ethinyl estradiol 0.025 mg and norethindrone 0.8 mg [24 light green tablets] and ferrous fumarate 75 mg [4 brown tablets] (28s)

Kaitlib Fe: Ethinyl estradiol 0.025 mg and norethindrone 0.8 mg [24 light green tablets] and ferrous fumarate 75 mg [4 brown tablets]

Layolis Fe: Ethinyl estradiol 0.025 mg and norethindrone 0.8 mg [24 light green tablets] and ferrous fumarate 75 mg [4 brown tablets] [spearmint flavor] (28s)

Minastrin 24 Fe: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [24 white tablets] and ferrous fumarate 75 mg [4 brown tablets] [spearmint flavor] (28s)

Wymzya Fe: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 white tablets] and ferrous fumarate 75 mg [7 brown tablets] (28s)

Zenchent Fe: Ethinyl estradiol 0.035 mg and norethindrone 0.4 mg [21 light yellow tablets] and ferrous fumarate 75 mg [7 brown tablets] [spearmint flavor] (28s)

Tablet, oral [biphasic formulation]:

Lo Loestrin Fe:

Day 1-24: Ethinyl estradiol 0.01 mg and norethindrone acetate 1 mg [24 blue tablets]

Day 25-26: Ethinyl estradiol 0.01 mg [2 white tablets]

Day 27-28: Ferrous fumarate 75 mg [2 brown tablets] (28s)

Lo Minastrin Fe:

Day 1-24: Ethinyl estradiol 0.01 mg and norethindrone acetate 1 mg [24 blue chewable tablets]

Day 25-26: Ethinyl estradiol 0.01 mg [2 white tablets]

Day 27-28: Ferrous fumarate 75 mg [2 brown tablets] (28s) [DSC]

Necon 10/11:

Day 1-10: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [10 light yellow tablets]

Day 11-21: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [11 dark yellow tablets]

Day 22-28: 7 white inactive tablets (28s)

Tablet, oral [triphasic formulation]:

Alyacen 7/7/7:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 white-off-white tablets]

Day 8-14: Ethinyl estradiol 0.035 mg and norethindrone 0.75 mg [7 light peach tablets]

Day 15-21: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [7 peach tablets]

Day 22-28: 7 light green inactive tablets (28s)

Aranelle:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 light yellow tablets]

Day 8-16: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [9 white tablets]

Day 17-21: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [5 light yellow tablets]

Day 22-28: 7 peach inactive tablets (28s)

Cyclafem 7/7/7:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 white tablets]

Day 8-14: Ethinyl estradiol 0.035 mg and norethindrone 0.75 mg [7 light pink tablets]

Day 15-21: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [7 pink tablets]

Day 22-28: 7 light green inactive tablets (28s)

Dasetta 7/7/7:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 light peach tablets]

Day 8-14: Ethinyl estradiol 0.035 mg and norethindrone 0.75 mg [7 peach tablets]

Day 15-21: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [7 orange tablets]

Day 22-28: 7 white inactive tablets (28s)

Estrostep Fe:

Day 1-5: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [5 white triangular tablets]

Day 6-12: Ethinyl estradiol 0.03 mg and norethindrone acetate 1 mg [7 white square tablets]

Day 13-21: Ethinyl estradiol 0.035 mg and norethindrone acetate 1 mg [9 white round tablets]

Day 22-28: Ferrous fumarate 75 mg [7 brown tablets] (28s)

Leena:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 light blue tablets]

Day 8-16: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [9 light yellow-green tablets]

Day 17-21: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [5 light blue tablets]

Day 22-28: 7 orange inactive tablets (28s)

Necon 7/7/7, Ortho-Novum 7/7/7:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 white tablets]

Day 8-14: Ethinyl estradiol 0.035 mg and norethindrone 0.75 mg [7 light peach tablets]

Day 15-21: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [7 peach tablets]

Day 22-28: 7 green inactive tablets (28s)

Nortrel 7/7/7:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 light yellow tablets]

Day 8-14: Ethinyl estradiol 0.035 mg and norethindrone 0.75 mg [7 blue tablets]

Day 15-21: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [7 peach tablets]

Day 22-28: 7 white inactive tablets (28s)

Pirmella 7/7/7:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 white tablets]

Day 8-14: Ethinyl estradiol 0.035 mg and norethindrone 0.75 mg [7 light peach tablets]

Day 15-21: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [7 peach tablets]

Day 22-28: 7 green inactive tablets (28s)

Tilia Fe:

Day 1-5: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [5 white triangular tablets]

Day 6-12: Ethinyl estradiol 0.03 mg and norethindrone acetate 1 mg [7 white square tablets]

Day 13-21: Ethinyl estradiol 0.035 mg and norethindrone acetate 1 mg [9 white round tablets]

Day 22-28: Ferrous fumarate 75 mg [7 brown tablets] (28s)

Tri-Legest Fe:

Day 1-5: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [5 light pink tablets]

Day 6-12: Ethinyl estradiol 0.03 mg and norethindrone acetate 1 mg [7 light yellow tablets]

Day 13-21: Ethinyl estradiol 0.035 mg and norethindrone acetate 1 mg [9 light blue tablets]

Day 22-28: Ferrous fumarate 75 mg [7 brown tablets] (28s)

Tri-Norinyl:

Day 1-7: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [7 blue tablets]

Day 8-16: Ethinyl estradiol 0.035 mg and norethindrone 1 mg [9 yellow-green tablets]

Day 17-21: Ethinyl estradiol 0.035 mg and norethindrone 0.5 mg [5 blue tablets]

Day 22-28: 7 orange inactive tablets (28s)


Drug Interactions

Acitretin: May diminish the therapeutic effect of Contraceptives (Progestins). 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. Consider therapy modification

Agomelatine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Agomelatine. Monitor therapy

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

Amodiaquine: CYP2C8 Inhibitors may increase the serum concentration of Amodiaquine. Avoid combination

Anastrozole: Estrogen Derivatives may diminish the therapeutic effect of Anastrozole. Avoid combination

Anthrax Immune Globulin (Human): Estrogen Derivatives may enhance the thrombogenic effect of Anthrax Immune Globulin (Human). Monitor 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. Consider therapy modification

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. Consider therapy modification

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

Antihepaciviral Combination Products: Ethinyl Estradiol may enhance the hepatotoxic effect of Antihepaciviral Combination Products. Avoid combination

Aprepitant: May decrease the serum concentration of Contraceptives (Estrogens). Management: Use of a non-hormone-based contraceptive is recommended. Consider therapy modification

Aprepitant: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Armodafinil: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

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

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

Ascorbic Acid: May increase the serum concentration of Estrogen Derivatives. Monitor therapy

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. Consider therapy modification

Atazanavir: May increase the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Barbiturates: May diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of a non-hormonal contraceptive is recommended. Consider therapy modification

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

Bexarotene (Systemic): May decrease the serum concentration of Contraceptives (Estrogens). Management: Women of childbearing potential receiving bexarotene should use two reliable forms of contraception (including at least one nonhormonal form). Consider therapy modification

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

Bile Acid Sequestrants: May decrease the serum concentration of Contraceptives (Estrogens). Management: Administer estrogen-based oral contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Consider therapy modification

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

Boceprevir: May decrease the serum concentration of Contraceptives (Estrogens). Management: Patients receiving boceprevir, ribavirin, and peginterferon alfa should use two reliable forms of contraception. Norethindrone/ethinyl estradiol may be used for one of these when norethindrone dose is at least 1 mg/day. Consider therapy modification

Boceprevir: May increase the serum concentration of Contraceptives (Progestins). This has been seen specifically with norethindrone. Boceprevir may increase the serum concentration of Contraceptives (Progestins). This has been seen specifically with drospirenone. Management: Patients receiving boceprevir, ribavirin, and peginterferon alfa should use two reliable forms of contraception. Norethindrone/ethinyl estradiol may be used for one of these when norethindrone dose is at least 1 mg/day. Avoid drospirenone. Consider therapy modification

Bosentan: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Bosentan: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

C1 inhibitors: Estrogen Derivatives may enhance the thrombogenic effect of C1 inhibitors. Monitor therapy

C1 inhibitors: Progestins may enhance the thrombogenic effect of C1 inhibitors. Monitor therapy

CarBAMazepine: May diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of a nonhormonal contraceptive is recommended. Consider therapy modification

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

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

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

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

CloBAZam: May decrease the serum concentration of Contraceptives (Estrogens). Consider therapy modification

CloBAZam: May decrease the serum concentration of Contraceptives (Progestins). Consider therapy modification

Cobicistat: May decrease the serum concentration of Contraceptives (Estrogens). Management: Consider an alternative, non-hormone-based contraceptive in patients receiving cobicistat-containing products. Consider therapy modification

Cobicistat: May increase the serum concentration of Contraceptives (Progestins). Management: Consider an alternative, non-hormone-based contraceptive in patients receiving cobicistat-containing products. Consider therapy modification

Colesevelam: May decrease the serum concentration of Ethinyl Estradiol. Consider therapy modification

Colesevelam: May decrease the serum concentration of Norethindrone. Consider therapy modification

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

CYP1A2 Substrates: CYP1A2 Inhibitors (Moderate) may decrease the metabolism of CYP1A2 Substrates. Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

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

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. 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). Consider therapy modification

Dabrafenib: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Dabrafenib: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Darunavir: May decrease the serum concentration of Norethindrone. Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Dehydroepiandrosterone: May enhance the adverse/toxic effect of Estrogen Derivatives. Avoid combination

Efavirenz: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Elvitegravir: May decrease the serum concentration of Contraceptives (Estrogens). Management: Consider the use of an alternative, non-hormone-based contraceptive, in patients who are being treated with elvitegaravir-containing products. Consider therapy modification

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates. 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. Consider therapy modification

Eslicarbazepine: May decrease the serum concentration of Contraceptives (Estrogens). Management: Alternative non-hormonal means of birth control should be considered for women of child-bearing potential. Consider therapy modification

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

Exemestane: Estrogen Derivatives may diminish the therapeutic effect of Exemestane. Avoid combination

Exenatide: May decrease the serum concentration of Contraceptives (Estrogens). Management: Administer oral contraceptives at least one hour prior to exenatide. Consider therapy modification

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

Felbamate: May decrease the serum concentration of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of a nonhormonal contraceptive is recommended. Consider therapy modification

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

Flibanserin: Contraceptives (Estrogens) may increase the serum concentration of Flibanserin. Monitor therapy

Flibanserin: Contraceptives (Progestins) may increase the serum concentration of Flibanserin. Monitor therapy

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

Fosaprepitant: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Fosaprepitant: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Fosphenytoin: May diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal means of contraception is recommended. Consider therapy modification

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

Griseofulvin: May diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible. Avoid combination

Hemin: Estrogen Derivatives may diminish the therapeutic effect of Hemin. Avoid combination

Herbs (Estrogenic Properties): May enhance the adverse/toxic effect of Estrogen Derivatives. Monitor therapy

Herbs (Progestogenic Properties) (eg, Bloodroot, Yucca): May enhance the adverse/toxic effect of Progestins. Monitor therapy

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. Consider therapy modification

Immune Globulin: Estrogen Derivatives may enhance the thrombogenic effect of Immune Globulin. Monitor therapy

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

LamoTRIgine: Contraceptives (Estrogens) 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. Consider therapy modification

LamoTRIgine: May decrease the serum concentration of Contraceptives (Progestins). Management: Women using progestin-only "minipill " Ě products may be at risk for contraceptive failure; it is unclear if other progestin-containing products would be significantly impacted. Alternative, non-hormonal, means of contraception are recommended. Consider therapy modification

Lenalidomide: Estrogen Derivatives may enhance the thrombogenic effect of Lenalidomide. Monitor therapy

Lesinurad: May decrease the serum concentration of Contraceptives (Estrogens). Management: Use of an additional, nonhormonal contraceptive is recommended in patients being treated with lesinurad who desire effective contraception. Consider therapy modification

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

Lixisenatide: May decrease the serum concentration of Contraceptives (Estrogens). Management: Administer oral contraceptives 1 hour before or at least 11 hours after administration of lixisenatide. Consider therapy modification

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

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. Consider therapy modification

Lopinavir: May decrease the serum concentration of Contraceptives (Progestins). Lopinavir may increase the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Lumacaftor: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Lumacaftor: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Metreleptin: May decrease the serum concentration of Contraceptives (Estrogens). Metreleptin may increase the serum concentration of Contraceptives (Estrogens). Monitor therapy

Metreleptin: May decrease the serum concentration of Contraceptives (Progestins). Metreleptin may increase the serum concentration of Contraceptives (Progestins). Monitor therapy

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

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

Mitotane: May decrease the serum concentration of CYP3A4 Substrates. Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Modafinil: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Mycophenolate: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Mycophenolate: May decrease the serum concentration of Contraceptives (Progestins). Management: Use of an additional or alternative (nonhormonal) method of contraception should be considered. Consider therapy modification

Nafcillin: May increase the metabolism of Contraceptives (Estrogens). Management: Use of an alternative, nonhormonal form of contraception during nafcillin therapy is recommended. Consider therapy modification

Nelfinavir: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Nevirapine: May decrease the serum concentration of Contraceptives (Estrogens). Consider therapy modification

Nevirapine: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

NSAID (COX-2 Inhibitor): May enhance the thrombogenic effect of Estrogen Derivatives. NSAID (COX-2 Inhibitor) may increase the serum concentration of Estrogen Derivatives. Monitor therapy

Osimertinib: May increase the serum concentration of CYP3A4 Substrates. Osimertinib may decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

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

OXcarbazepine: May decrease the serum concentration of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal contraceptive is recommended. Consider therapy modification

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

Perampanel: May decrease the serum concentration of Contraceptives (Progestins). Management: Patients should use an alternative, non-hormonal based form of contraception for the duration of concurrent perampanel. Both oral and non-oral progestin-based contraceptives are likely to be impacted by this interaction. Consider therapy modification

Phenytoin: May diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal means of contraception is recommended. Consider therapy modification

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

Pirfenidone: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pirfenidone. Management: Use any such combination with caution and close monitoring for pirfenidone toxicity. Avoid the use of pirfenidone with moderate CYP1A2 inhibitors whenever CYP2C9, 2C19, 2C6, or 2E1 is also inhibited (either by the CYP1A2 inhibitor or by a third drug). Consider therapy modification

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. Consider therapy modification

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. Consider therapy modification

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

Protease Inhibitors: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Prucalopride: May decrease the serum concentration of Contraceptives (Estrogens). Consider therapy modification

Prucalopride: May decrease the serum concentration of Contraceptives (Progestins). Consider therapy modification

Retinoic Acid Derivatives: May diminish the therapeutic effect of Contraceptives (Progestins). Retinoic Acid Derivatives may decrease the serum concentration of Contraceptives (Progestins). 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). Consider therapy modification

Rifamycin Derivatives: May decrease the serum concentration of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal contraceptive is recommended. Consider therapy modification

Rifamycin Derivatives: May decrease the serum concentration of Contraceptives (Progestins). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended. Consider therapy modification

ROPINIRole: Estrogen Derivatives may increase the serum concentration of ROPINIRole. Monitor therapy

Rufinamide: May decrease the serum concentration of Ethinyl Estradiol. Consider therapy modification

Rufinamide: May decrease the serum concentration of Norethindrone. Consider therapy modification

Saquinavir: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Selegiline: Contraceptives (Estrogens) may increase the serum concentration of Selegiline. Monitor therapy

Selegiline: Contraceptives (Progestins) may increase the serum concentration of Selegiline. Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

St Johns Wort: May diminish the therapeutic effect of Contraceptives (Estrogens). 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. Consider therapy modification

St John's Wort: May diminish the therapeutic effect of Contraceptives (Progestins). 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. Consider therapy modification

St John's Wort: May decrease the serum concentration of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

Sugammadex: May decrease the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

Sugammadex: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

Telaprevir: May decrease the serum concentration of Contraceptives (Estrogens). Management: Two different nonhormonal forms of contraception are required for women of childbearing potential taking telaprevir. Hormonal contraceptives may be less effective during concurrent telaprevir and for up to 2 weeks after telaprevir discontinuation. Consider therapy modification

Telaprevir: May decrease the serum concentration of Contraceptives (Progestins). Management: Two different nonhormonal forms of contraception are required for women of childbearing potential taking telaprevir. Hormonal contraceptives may be less effective during concurrent telaprevir and for up to 2 weeks after telaprevir discontinuation. Consider therapy modification

Thalidomide: Contraceptives (Estrogens) may enhance the thrombogenic effect of Thalidomide. Monitor therapy

Thalidomide: Contraceptives (Progestins) may enhance the thrombogenic effect of Thalidomide. Monitor therapy

Thalidomide: Estrogen Derivatives may enhance the thrombogenic effect of Thalidomide. Monitor therapy

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

Thyroid Products: Estrogen Derivatives may diminish the therapeutic effect of Thyroid Products. Monitor therapy

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. Consider therapy modification

Tipranavir: May increase the serum concentration of Contraceptives (Progestins). 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. Consider therapy modification

TiZANidine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of TiZANidine. Management: If combined use cannot be avoided, initiate tizanidine in adults at 2 mg and increase in 2-4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Topiramate: May decrease the serum concentration of Contraceptives (Estrogens). 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. Consider therapy modification

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

Tranexamic Acid: Contraceptives (Progestins) may enhance the thrombogenic effect of Tranexamic Acid. Avoid combination

Tranexamic Acid: Contraceptives (Estrogens) may enhance the thrombogenic effect of Tranexamic Acid. Avoid combination

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. Avoid combination

Ursodiol: Estrogen Derivatives may diminish the therapeutic effect of Ursodiol. Monitor therapy

Vitamin K Antagonists (eg, warfarin): Contraceptives (Estrogens) may diminish the anticoagulant effect of Vitamin K Antagonists. In contrast, enhanced anticoagulant effects have also been noted with some products. Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Contraceptives (Progestins) 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. Consider therapy modification

Voriconazole: May decrease the metabolism of Contraceptives (Estrogens). Contraceptives (Estrogens) may increase the serum concentration of Voriconazole. Monitor therapy

Voriconazole: May increase the serum concentration of Contraceptives (Progestins). Contraceptives (Progestins) may increase the serum concentration of Voriconazole. Monitor therapy


Monitoring Parameters

Hormonal contraceptives: Assessment of pregnancy status (prior to therapy); blood pressure (prior to therapy and yearly); weight (optional; BMI at baseline may be helpful to monitor changes during therapy); assess potential health status changes at routine visits (CDC, 2013).

If all doses have not been taken on schedule and one menstrual period is missed, the possibility of pregnancy should be considered. If two consecutive menstrual periods are missed, a pregnancy test is recommended before a new dosing cycle is started.

Monitor patient for vision changes; blood pressure; signs and symptoms of thromboembolic disorders; signs or symptoms of depression; glycemic control in patients with diabetes; 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.

Postmenopausal indications: Routine physical examination that includes blood pressure and Papanicolaou smear, breast exam, mammogram. Monitor for signs of endometrial cancer in female patients with uterus. Adequate diagnostic measures, including endometrial sampling, if indicated, should be performed to rule out malignancy in all cases of undiagnosed abnormal genital bleeding. Monitor for loss of vision, sudden onset of proptosis, diplopia, migraine; signs and symptoms of thromboembolic disorders; glycemic control in patients with diabetes; lipid profiles in patients being treated for hyperlipidemias; thyroid function in patients on thyroid hormone replacement therapy.

Menopausal symptoms: Assess need for therapy at 3- to 6-month intervals

Prevention of osteoporosis: Bone density measurement

Note: Monitoring of FSH and serum estradiol is not useful when managing vasomotor symptoms associated with menopause.


Adverse Reactions


The following have been associated with femhrt. Also refer to adverse reactions observed with oral contraceptives for additional reactions observed with estrogen/progestin therapy:

>10%: Central nervous system: Headache (15% to 18%)

1% to 10%:

Central nervous system: Depression (4% to 6%), nervousness (2% to 5%)

Endocrine & metabolic: Breast pain (8% to 9%)

Gastrointestinal: Abdominal pain (8% to 10%), nausea and vomiting (5% to 7%), diarrhea (4% to 6%), dyspepsia (3% to 5%)

Genitourinary: Urinary tract infection (4% to 6%), vaginitis (5%)

Infection: Viral infection (9%)

Respiratory: Sinusitis (8% to 9%)

The following have been associated with Lo Loestrin Fe. Also refer to adverse reactions observed with oral contraceptives for additional reactions observed with estrogen/progestin therapy:

1% to 10%:

Central nervous system: Headache (7%), anxiety (2%), depression (2%), migraine (1%), mood disorder (1%, including mood swings, depression, anxiety)

Dermatologic: Acne vulgaris (3%)

Endocrine & metabolic: Menstrual disease (4%, including metrorrhagia, irregular menstruation, menorrhagia, and vaginal hemorrhage), weight changes (1% to 4%)

Gastrointestinal: Nausea and vomiting (7%), abdominal pain (3%)

Genitourinary: Abnormal uterine bleeding (5%, including metrorrhagia, irregular menstruation, menorrhagia, vaginal hemorrhage, and dysfunctional uterine bleeding), breast tenderness (4%), dysmenorrhea (4%)

The following reactions have been associated with oral contraceptive use:

Increased risk or evidence of association with use:

Cardiovascular: Arterial thromboembolism, cerebral hemorrhage, cerebral thrombosis, cerebrovascular accident, deep vein thrombosis, hypertension, increased blood pressure, mesenteric thrombosis, myocardial infarction, pulmonary embolism, thrombophlebitis, venous thrombosis (with or without embolism)

Central nervous system: Dementia, exacerbation of epilepsy, irritability

Dermatologic: Pruritus, skin rash

Endocrine & metabolic: Fibrocystic breast changes, galactorrhea, hypocalcemia, increased serum triglycerides

Gastrointestinal: Cholecystitis, gallbladder disease

Genitourinary: Abnormal uterine bleeding, endometrial hyperplasia

Hematologic & oncologic: Endometrial carcinoma, malignant neoplasm of breast, ovarian carcinoma, uterine fibroids (increase in size)

Hepatic: Exacerbation of hepatic hemangioma, hepatic adenomas, liver tumors (benign)

Local: Thrombophlebitis

Neuromuscular & skeletal: Arthralgia, leg cramps

Ocular: Retinal thrombosis

Renal: Impaired renal function

Respiratory: Exacerbation of asthma, pulmonary embolism

Adverse reactions considered drug related:

Cardiovascular: Edema, varicose vein aggravation

Central nervous system: Depression, migraine, mood changes

Dermatologic: Chloasma (may persist), melasma (may persist), rash (allergic)

Endocrine & metabolic: Amenorrhea, breakthrough bleeding, breast changes (enlargement, pain, secretion, tenderness), fluid retention, infertility (temporary after discontinuation of treatment), lactation decreased (with use immediately postpartum), menstrual flow changes, spotting, weight gain, weight loss

Gastrointestinal: Abdominal cramps, abdominal pain, appetite changes, bloating, carbohydrate intolerance, nausea, vomiting

Genitourinary: Change in cervical ectropion, change in cervical erosion, change in cervical secretions, vaginal candidiasis, vaginitis

Hematologic: Folate decreased, porphyria exacerbation

Hepatic: Cholestatic jaundice

Neuromuscular & skeletal: Chorea exacerbation

Ocular: Contact lens intolerance, corneal curvature changes (steepening)

Miscellaneous: Anaphylactic/anaphylactoid reactions (including angioedema, circulatory collapse, respiratory collapse, urticaria), SLE exacerbation

Adverse reactions in which association is not confirmed or denied: Acne, back pain, breast neoplasm, Budd-Chiari syndrome, cataracts, cervical carcinoma, cholelithiasis, colitis, cystitis-like syndrome, dizziness, dysmenorrhea, dyspnea, emotional lability, erythema multiforme, erythema nodosum, fatigue, headache, hemolytic uremic syndrome, hemorrhagic eruption, hepatitis, hirsutism, hypersensitivity reaction, hypomenorrhea, libido changes, lump in breast, malaise, muscle spasms, nervousness, optic neuritis (with or without partial or complete loss of vision), pancreatitis, pelvic pain, peripheral edema, premenstrual syndrome, renal function impaired, scalp hair loss, skin photosensitivity, vaginal dryness, venous thrombosis (ovarian), vulvovaginal pruritus, weakness


Warnings/Precautions


Concerns related to adverse effects:

- Breast cancer: [US Boxed Warning]: Based on data from the Women 's Health Initiative (WHI) studies, an increased risk of invasive breast cancer was observed in postmenopausal women using conjugated estrogens (CE) in combination with medroxyprogesterone acetate (MPA). This risk may be associated with duration of use and declines once combined therapy is discontinued (Chlebowski 2009). The risk of invasive breast cancer was decreased in postmenopausal women with a hysterectomy using CE only, regardless of weight. However, the risk was not significantly decreased in women at high risk for breast cancer (family history of breast cancer, personal history of benign breast disease) (Anderson 2012). An increase in abnormal mammogram findings has also been reported with estrogen alone or in combination with progestin therapy. Estrogen use may lead to severe hypercalcemia in patients with breast cancer and bone metastases; discontinue estrogen if hypercalcemia occurs. The use of combination hormonal contraceptives has not been shown to increase the risk for breast cancer. However, breast cancer is a hormonal sensitive tumor and the prognosis for women with a current or recent history of breast cancer may be worse with combination hormonal contraceptive use (CDC 2010). Use is contraindicated in patients with (or history of) breast cancer.

- Carbohydrate intolerance: May impair glucose tolerance; use caution in women with diabetes or prediabetes.

- Cervical cancer: The use of combination hormonal contraceptives has been associated with a slight increased risk of cervical cancer; however, studies are not consistent and may be related to additional risk factors (Gierisch 2013). Women awaiting treatment for cervical cancer may use combination hormonal contraceptives (CDC 2013).

- Chloasma: Combination hormonal contraceptives, hormone replacement therapy, as well as sun exposure and pregnancy, are triggers for chloasma. Women with a susceptibility to chloasma or additional risk factors should avoid exposure to sun or ultraviolet radiation during therapy (Handel 2014).

- Cholestasis: Risk of cholestasis may be increased with previous cholestasis of pregnancy or cholestasis with prior oral contraceptive use; use is contraindicated with a history of these conditions.

- Dementia: [US Boxed Warning]: Estrogens with or without progestin should not be used to prevent dementia. In the Women 's Health Initiative Memory Study (WHIMS), an increased incidence of probable dementia was observed in women ≥65 years of age taking CE alone or in combination with MPA.

- Endometrial cancer: [US Boxed Warning]: The use of unopposed estrogen in women with an intact uterus is associated with an increased risk of endometrial cancer. The addition of a progestin to estrogen therapy may decrease the risk of endometrial hyperplasia, a precursor to endometrial cancer. Adequate diagnostic measures, including endometrial sampling if indicated, should be performed to rule out malignancy in postmenopausal women with undiagnosed abnormal vaginal bleeding. There is no evidence that the use of natural estrogens results in a different endometrial risk profile than synthetic estrogens at equivalent estrogen doses. The risk of endometrial cancer appears to be dose and duration dependent; risk appears to be greatest with use ≥5 years and may persist following discontinuation of therapy.

- Endometriosis: Estrogens may exacerbate endometriosis. Malignant transformation of residual endometrial implants has been reported posthysterectomy with unopposed estrogen therapy. Consider adding a progestin in women with residual endometriosis posthysterectomy.

- Inherited thrombophilia: Women with inherited thrombophilias (eg, protein C or S deficiency) may have increased risk of venous thromboembolism (DeSancho 2010; van Vlijmen 2011). Use for postmenopausal indications is contraindicated in women with protein C, protein S, antithrombin deficiency, or other known thrombophilic disorders. Use of combination hormonal contraceptives is contraindicated in women with known thrombophilic conditions.

- Lipid effects: Combination hormonal contraceptives may adversely affect lipid levels, including serum triglycerides. The type of lipid disorder, the severity, and the presence of other cardiovascular risk factors should be considered when prescribing combination hormonal contraceptives to women with lipid disorders (CDC 2010). Women with hypertriglyceridemia or a family history of hypertriglyceridemia may be at increased risk of pancreatitis when using combination hormonal contraceptives. Adverse lipid effects are also observed with for postmenopausal indications.

- Ovarian cancer: Postmenopausal estrogens with or without progestins may increase the risk of ovarian cancer; however, the absolute risk to an individual woman is small. Although results from various studies are not consistent, risk does not appear to be significantly associated with the duration, route, or dose of therapy. In one study, the risk decreased after 2 years following discontinuation of therapy (M É łrch 2009). Although the risk of ovarian cancer is rare, women who are at an increased risk (eg, family history) should be counseled about the association (NAMS 2012). The risk of ovarian cancer is decreased in women using combination hormonal contraceptives (CDC 2013; Walker 2015). Oral contraceptives may be used to reduce the risk of ovarian cancer including those women with BRACA1 and BRACA2 mutations (Walker 2015).

- Retinal vascular thrombosis: Discontinue if unexplained loss of vision, proptosis, diplopia, papilledema, or retinal vascular lesions occur and immediately evaluate for retinal vein thrombosis.

- Thromboembolism: Oral contraceptives may increase the risk of thromboembolism; discontinue use of combination hormonal contraceptives if an arterial or venous thrombotic event occurs.

- Vaginal bleeding: Breakthrough or intracyclic bleeding and spotting may occur with combination hormonal contraceptives, especially during the first 3 months of therapy. In addition, occasional missed periods may occur. Presentation of irregular, unresolving vaginal bleeding warrants further evaluation to rule out malignancy or pregnancy. Amenorrhea or oligomenorrhea may occur after discontinuing combination hormonal contraceptives, especially when such a condition was preexistent.

Disease-related concerns:

- Asthma: Use caution in patients with asthma; may exacerbate disease.

- Cardiovascular disease: [US Boxed Warning]: Estrogens with or without progestin should not be used to prevent cardiovascular disease. Using data from the Women 's Health Initiative (WHI) studies, an increased risk of deep vein thrombosis (DVT) and stroke has been reported with CE and an increased risk of DVT, stroke, pulmonary emboli (PE) and myocardial infarction (MI) has been reported with CE with MPA in postmenopausal women 50 to 79 years of age. Additional risk factors include diabetes mellitus, hypercholesterolemia, hypertension, SLE, obesity, tobacco use, and/or history of venous thromboembolism (VTE). Risk factors should be managed appropriately; discontinue use immediately if adverse cardiovascular events occur or are suspected. Use is contraindicated in women with active DVT or PE (or a history of these conditions) or in women with active or recent arterial thromboembolic disease (stroke and MI), or a history of these conditions. Use combination hormonal contraceptives with caution in patients with risk factors for cardiovascular disease (eg, hypertension, hypercholesterolemia, morbid obesity, diabetes, or women who smoke); use of combination hormonal contraceptives may increase the risk of arterial or venous thrombotic events (CDC 2010). Use of combination hormonal contraceptives may be contraindicated in women at high risk of arterial or venous thrombotic diseases.

- Diseases exacerbated by fluid retention: Use with caution in patients with diseases which may be exacerbated by fluid retention, including cardiac or renal dysfunction.

- Epilepsy: Use caution with epilepsy; may exacerbate disease.

- Fibroids: Discontinue use with the onset of enlargement, pain, or tenderness of preexisting uterine fibroids (leiomyomata ).

- Gallbladder disease: Use of combination hormonal contraceptives may have a risk of gallbladder disease; may worsen existing gallbladder disease. Use of postmenopausal estrogen may be associated with an increased risk of gallbladder disease requiring surgery.

- Hepatic adenomas or carcinomas: Use of combination hormonal contraceptives is associated with hepatic adenomas (rare); rupture may cause fatal intra-abdominal hemorrhage. Long term use may be associated with an increased risk of hepatocellular carcinoma (rare). Use is contraindicated with preexisting hepatic tumors.

- Hepatic impairment: Estrogens may be poorly metabolized in women with hepatic impairment. Discontinue if jaundice develops during therapy or if liver function becomes abnormal. Use is contraindicated with preexisting hepatic disease.

- Hepatic hemangiomas: Use with caution in patients with hepatic hemangiomas; may exacerbate disease.

- Hereditary angioedema: Exogenous estrogens may exacerbate angioedema symptoms in women with hereditary angioedema (Geng 2013; Zuraw 2013).

- Hypertension: The risk of hypertension may be increased with age, dose, and duration of use. Combination hormonal contraceptives should not be used in women with persistent blood pressure values ≥160 mm Hg systolic or ≥100 mm Hg diastolic. Women with less severe hypertension (140 to 159 mm Hg systolic or 90 to 99 mm Hg diastolic) or those with hypertension that is adequately controlled should generally not use combination hormonal contraceptives (CDC 2013). Other risk factors for cardiovascular disease (eg, older age, smoking, diabetes) should be considered when prescribing contraceptives (CDC 2010). Some products are specifically contraindicated with persistent blood pressure values ≥160 mm Hg systolic or ≥100 mm Hg diastolic.

- Hypoparathyroidism: Use caution in patients with hypoparathyroidism; estrogen-induced hypocalcemia may occur.

- Migraine: Evaluate new, recurrent, severe, or persistent headaches. Use of combination oral contraceptives is contraindicated in women with headaches with focal neurological symptoms.

- Otosclerosis: Use caution in patients with otosclerosis.

- Porphyria: Use with caution in patients with porphyria; may exacerbate disease.

- SLE: Use with caution in patients with SLE; may exacerbate disease.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist with hormonal contraceptives, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

- Thyroid replacement therapy: Estrogens may increase thyroid-binding globulin (TBG) levels leading to increased circulating total thyroid hormone levels. Women on thyroid replacement therapy may require higher doses of thyroid hormone while receiving estrogens.

Special populations:

- Contact lens wearers: Any changes with lens tolerance or vision should be evaluated by an ophthalmologist.

- Elderly: Although hormone therapy is recommended to be initiated in healthy symptomatic women within 10 years of menopause or <60 years of age who do not have contraindications for use, symptoms may continue in women >60 years of age. The continuation of hormone therapy in women >65 years of age should consider the risks and benefits for the individual woman and should not be discontinued only because of the woman 's age (NAMS 2015).

- Pediatric: Combination hormonal contraceptives are not for use prior to menarche.

- Smokers: [US Boxed Warning]: The risk of cardiovascular side effects is increased in women who smoke cigarettes; risk increases with age (especially women >35 years of age) and the number of cigarettes smoked; women who use combination hormonal contraceptives should be strongly advised not to smoke. Should not be used in patients >35 years of age who smoke.

- Surgical patients: Whenever possible, should be discontinued at least 4 weeks prior to and for 2 weeks following elective surgery associated with an increased risk of thromboembolism or during periods of prolonged immobilization.

Dosage form specific issues:

- Lactose: Tablets may contain lactose; avoid use in patients with lactase deficiency, galactose intolerance or glucose-galactose malabsorption.

- Obesity: Safety and efficacy of some products (eg, Generess Fe, Lo Loestrin Fe; Lo Minastrin Fe) have not been established in women with a BMI >35 kg/m2.

- Tartrazine: Some products may contain tartrazine, which may cause allergic reactions in certain individuals.

Special handling:

- Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 2]).

Other warnings/precautions:

-Appropriate use: When initiating a combination oral contraceptive, consideration should be given to safety, effectiveness, availability and acceptance to the patient (CDC 2013). Consider initiating with a monthly bleeding monophasic formulation containing ethinyl estradiol 30 to 35 mcg plus a progestin, and adjusting based on adverse events and patient preference (Ott 2014).

- HIV infection protection: Combination hormonal contraceptives do not protect against HIV infection or other sexually-transmitted diseases (CDC 2010; CDC 2013).

- Laboratory changes: The use of estrogens and/or progestins may change the results of some laboratory tests (eg, coagulation factors, lipids, glucose tolerance, binding proteins). The dose, route, and the specific estrogen/progestin influences these changes. In addition, personal risk factors (eg, cardiovascular disease, smoking, diabetes, age) also contribute to adverse events; use of specific products may be contraindicated in women with certain risk factors.

- Risks vs benefits: [US Boxed Warning]: Estrogens with or without progestin should be used for the shortest duration possible at the lowest effective dose consistent with treatment goals and risks for the individual woman. Hormone therapy for menopausal symptoms is generally initiated in healthy symptomatic women within 10 years of menopause or <60 years of age who do not have contraindications for use (Stuenkel 2015). Patients should be reevaluated as clinically appropriate to determine if treatment is still necessary. Available data related to treatment risks are from Women 's Health Initiative (WHI) studies, which evaluated oral CE 0.625 mg with or without MPA 2.5 mg relative to placebo in postmenopausal women. Other combinations and dosage forms of estrogens and progestins were not studied. Outcomes reported from clinical trials using CE with or without MPA should be assumed to be similar for other doses and other dosage forms of estrogens and progestins until comparable data becomes available. Women who are early in menopause, who are in good cardiovascular health, and who are at low risk for adverse cardiovascular events can be considered candidates for estrogen with or without progestin therapy for the relief of menopausal symptoms (ACOG 565 2013). Women at high risk of cardiovascular disease or intermediate to high risk of breast cancer should use nonhormonal therapy to treat vasomotor symptoms of menopause (Stuenkel 2015). Use of a transdermal product should be considered over an oral agent in women requiring systemic therapy who have moderate risk factors for coronary heart disease (ACOG 556 2013; Schenck-Gustafsson 2011; Stuenkel 2015). Nonoral routes of therapy are recommended for women at increased risk for venous thromboembolism (Stuenkel 2015; Tremollieres 2011)


Pregnancy Risk Factor

X


Pregnancy Considerations

Use is contraindicated in pregnant women. Pregnancy status should be evaluated prior to prescribing combination hormonal contraceptives (CDC 2013); treatment should be discontinued if pregnancy occurs. In general, the use of combination hormonal contraceptives, when inadvertently used early in pregnancy, have not been associated with teratogenic effects. Available evidence is inconsistent if BMI alters the efficacy of combination oral contraceptives (CDC 2010); however, the manufacturers of some products (eg, Generess Fe, Lo Loestrin Fe; Lo Minastrin Fe) note that safety and efficacy have not been established in women with a BMI >35 kg/m2.

Due to increased risk of venous thromboembolism (VTE) postpartum, combination hormonal contraceptives should not be started in any woman <21 days following delivery. Women without risk factors for VTE and who are not breast-feeding may start combination hormonal contraceptives during 21 to 42 days postpartum. After 42 days postpartum, restrictions for use are not related to postpartum status and should be based on other medical conditions (CDC 2011). The manufacturer states that combination hormonal contraceptives should not be started until ≥4 weeks after delivery in women who choose not to breast-feed.


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Pharmacology

Combination oral contraceptives inhibit ovulation via a negative feedback mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior pituitary. The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, combination hormonal contraceptives produce alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Combination hormonal contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility.

In postmenopausal women, exogenous estrogen is used to replace decreased endogenous production. The addition of progestin reduces the incidence of endometrial hyperplasia and risk of endometrial cancer in women with an intact uterus.


Absorption

Ethinyl estradiol: Rapid


Distribution

Ethinyl estradiol: Vd: 2-4 L/kg


Metabolism

Ethinyl estradiol: Hepatic via oxidation and conjugation in GI tract; hydroxylated via CYP3A4 to metabolites; first-pass effect; enterohepatic recirculation; reversibly converted to estrone and estriol


Excretion

Ethinyl estradiol: Urine (as estradiol, estrone, and estriol); feces


Half-Life Elimination

Ethinyl estradiol: 19-24 hours


Protein Binding

Ethinyl estradiol: >95% to albumin


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience lack of appetite, more hungry, weight gain, cramps, bloating, enlarged breasts, alopecia, decreased libido, menstrual irregularities, diarrhea, or dark patches on face. Have patient report immediately to prescriber signs of severe cerebrovascular disease (change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), angina, edema, shortness of breath, trouble bleeding, coughing up blood, severe dizziness, passing out, severe nausea, vomiting, severe headache, depression, loss of strength and energy, severe abdominal pain, urinary retention, change in amount of urine passed, lump in breast, breast soreness or pain, nipple discharge, vaginal bleeding, vaginitis, vision changes, bulging eyes, or contact lens discomfort (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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