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Ethinyl Estradiol and Norelgestromin


General


Pronunciation

(ETH in il es tra DYE ole & nor el JES troe min)


Brand Names: U.S.

  • Ortho Evra [DSC]
  • Xulane

Indications


Use: Labeled Indications

Contraception: For the prevention of pregnancy

Limitations of use: The topical patch may be less effective in patients weighing ≥90 kg (198 lb).


Contraindications


Breast cancer or other estrogen- or progestin-dependent neoplasms (current or a history of), hepatic tumors (benign or malignant) or hepatic disease, pregnancy, undiagnosed abnormal uterine bleeding.

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), hypercoagulopathies (inherited or acquired), hypertension (uncontrolled), headaches with focal neurological symptoms, migraine headaches with aura or migraine headaches if >35 years of age, thrombogenic valvular or rhythm diseases of the heart (eg, subacute bacterial endocarditis with valvular disease or atrial fibrillation), women >35 years of age who smoke.

Canadian-labeling: Additional contraindications (not in US labeling): Hypersensitivity to any component of the formulation; actual or history of thrombophlebitis or thromboembolic disorders; thrombophilia; myocardial infarction; carcinoma of the endometrium; steroid dependent jaundice, cholestatic jaundice, or history of jaundice of pregnancy; ocular lesions due to ophthalmic vascular disease including partial or complete loss of vision or defect in visual fields; persistent blood pressure ≥160 mm Hg systolic or ≥100 mm Hg diastolic; severe dyslipoproteinemia; hereditary or acquired predisposition for venous or arterial thrombosis; major surgery associated with an increased risk of post-operative thromboembolism; prolonged immobilization.

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 hormonal contraceptive use. This risk increases with age, particularly in women older than 35 years, and with the number of cigarettes smoked. For this reason, hormonal contraceptives, including norelgestromin/ethinyl estradiol, should not be used by women who are older than 35 years and smoke.

Risk of venous thromboembolism:

The risk of venous thromboembolism among women 15 to 44 years of age who used the contraceptive patch, compared with women who used several different oral contraceptives, was assessed in 5 US epidemiologic studies using electronic health care claims data. The relative risk estimates ranged from 1.2 to 2.2; one of the studies found a statistically significant increased risk of venous thromboembolism for current users of the contraceptive patch.

Hormone exposure:

The pharmacokinetic profile for the contraceptive patch is different from the pharmacokinetic profile for oral contraceptives in that it has higher steady-state concentrations and lower peak concentrations. Area under the concentration-time curve (AUC) and average concentration at steady state for ethinyl estradiol are approximately 60% higher in women using the contraceptive patch compared with women using an oral contraceptive containing ethinyl estradiol 35 mcg. In contrast, peak concentrations for ethinyl estradiol are approximately 25% lower in women using the contraceptive patch. It is not known whether there are changes in the risk of serious adverse events based on the differences in pharmacokinetic profiles of ethinyl estradiol in women using the contraceptive patch compared with women using oral contraceptives containing ethinyl estradiol 30 to 35 mcg. Increased estrogen exposure may increase the risk of adverse events, including venous thromboembolism.


Dosing and Administration


Dosing: Adult

Females: Contraception: Topical:

Apply one patch each week for 3 weeks (21 total days); followed by one week that is patch-free. Each patch should be applied on the same day each week ( "patch change day " �) and only one patch should be worn at a time. No more than 7 days should pass during the patch-free interval.

Schedule 1 (Sunday starter): Dose begins on first Sunday after onset of menstruation; if the menstrual period starts on Sunday, apply one patch that very same day. With a Sunday start, an additional method of contraception (nonhormonal) must be used until after the first 7 days of consecutive administration unless the menstrual period starts on Sunday. Each patch change will then occur on Sunday.

Schedule 2 (Day 1 starter): Dose starts on first day of menstrual cycle, applying one patch during the first 24 hours of menstrual cycle. Each patch change will then occur on that same day of the week. The US labeling does not indicate that a back-up method of contraception is needed as long as the patch is applied on the first day of cycle. The Canadian labeling recommends a back-up method of non-hormonal contraception be used concurrently for the first 7 consecutive days of the first treatment cycle.

Additional dosing considerations:

No bleeding during patch-free week/missed menstrual period: If patch has been applied as directed, continue treatment on usual "patch change day " �. If used correctly, no bleeding during patch-free week does not necessarily indicate pregnancy. However, if no withdrawal bleeding occurs for 2 consecutive cycles, pregnancy should be ruled out. If patch has not been applied as directed, and one menstrual period is missed, pregnancy should be ruled out prior to continuing treatment.

If a patch becomes partially or completely detached for <24 hours: Try to reapply to same place, or replace with a new patch immediately. Do not reapply if patch is no longer sticky, if it is sticking to itself or another surface, or if it has material sticking to it.

If a patch becomes partially or completely detached for >24 hours (or time period is unknown): Apply a new patch and use this day of the week as the new "patch change day " � from this point on. An additional method of contraception (nonhormonal) must be used until after the first 7 days of consecutive administration.

Switching from oral contraceptives or vaginal ring:

US labeling: Complete current cycle and apply the first patch on the day the next pill cycle would be started or ring would be inserted. If there is no menstrual bleeding within 7 days of taking the last active tablet, the patient can initiate the first patch application; however, pregnancy must be ruled out. If patch is applied later than 7 days after the last active pill or removal of the vaginal ring, an additional method of contraception (nonhormonal) should be used until after the first 7 days of consecutive administration

Canadian labeling: Apply the first patch on the first day of withdrawal bleeding. If there is no withdrawal bleeding within 5 days of taking the last active tablet, rule out pregnancy prior to applying first patch. If the patch is applied after the first day of withdrawal bleeding, a non-hormonal contraceptive should be used concurrently for 7 days. If more than 7 days have elapsed after the last active tablet was taken, evaluate patient prior to starting patch to rule out ovulation or pregnancy.

Use after childbirth: Therapy should not be started <4 weeks after childbirth. 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.

Use after abortion or miscarriage:

US labeling: Therapy may be started immediately if abortion/miscarriage occurs within the first trimester. If therapy is not started within 5 days, follow instructions for first time use. An additional method of contraception (nonhormonal) should be used until after the first 7 days of consecutive administration. If abortion/miscarriage occurs during the second trimester, therapy should not be started for at least 4 weeks. Follow directions for use after childbirth.

Canadian labeling: Therapy may be started immediately if abortion/miscarriage occurs prior to 20 weeks gestation. An additional method of contraception is not necessary if therapy is started immediately. If abortion/miscarriage occurs at or beyond 20 weeks gestation, therapy may be started on day-21 post-abortion or on the first day of the first spontaneous menstrual cycle, whichever comes first.


Dosing: Pediatric

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


Dosing: Renal Impairment

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


Dosing: Hepatic Impairment

Contraindicated in patients with hepatic impairment.


Administration

New patches should be applied on the same day each week. Apply to clean, dry, intact, healthy skin on the buttock, abdomen, upper outer arm, or back. Avoid areas that will be rubbed by tight clothing. Do not apply to the breasts or to skin that is red, irritated, or cut. Alternate application sites; do not apply to the same place as the previous patch. Do not apply make-up, creams, lotions, powders, or other topical products to the skin where the patch will be placed. Remove the patch and the plastic liner from the foil pouch, being careful not to remove the clear liner when removing the patch. Apply patch by first peeling back half of the clear protective liner. Avoid touching surface of patch. Apply patch to skin and remove the rest of the liner. Press patch down firmly onto skin using palm of the hand; apply pressure for 10 seconds. Run fingers over entire surface area to smooth out any wrinkles in the patch. The patch should be checked daily to ensure all edges are sticking. When changing the patch each week, the new patch may be applied in the same anatomic area but should be applied to a new spot in that area. Do not use supplemental adhesives or wraps to hold patch into place. Do not cut, damage or alter the size of the patch; contraceptive efficacy may be impaired.

Forgetting to apply the patch at the start of cycle (week 1/day 1): Apply first patch as soon as remembering, using this day of the week as the new "patch change day " � from this point on. An additional method of contraception (nonhormonal) must be used until after the first 7 days of consecutive administration.

Forgetting to change patch in the middle of the cycle (week 2/day 8 or week 3/day 15): If <48 hours from normal "patch change day, " � apply new patch immediately. No back-up contraception is needed. If >48 hours from normal "patch change day, " � apply a new patch and use this day of the week as the new "patch change day " � from this point on. An additional method of contraception (nonhormonal) must be used until after the first 7 days of consecutive administration.

Forgetting to remove patch at end of cycle (week 4/day 22): Take off as soon as remembering, start new cycle on usual "patch change day. " �

Changing the "patch change day " �: The "patch change day " � can be changed to an earlier day in the week by first completing the current cycle. Then, during the "patch-free interval " �, select an earlier day to start the new cycle. Shortening the patch free interval may increase the incidence of spotting or breakthrough bleeding. Do not allow >7 consecutive patch-free days.

Skin irritation: If patch is in an uncomfortable location, it can be removed and a new patch applied to a different location until the next "patch change day. " �

To dispose of patch, fold the sticky sides together and dispose in the trash within a child-resistant container. Do not flush down the toilet.

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


Storage

Store at controlled room temperature of 20 � �C to 25 � �C (68 � �F to 77 � �F); do not refrigerate or freeze.


Dosage Forms/Strengths


Dosage Forms

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

Patch, transdermal:

Ortho Evra: Ethinyl estradiol 0.75 mg and norelgestromin 6 mg [releases ethinyl estradiol 35 mcg and norelgestromin 150 mcg per day] (1s DSC], 3s [DSC])

Xulane: Ethinyl estradiol 0.53 mg and norelgestromin 4.86 mg [releases ethinyl estradiol 35 mcg and norelgestromin 150 mcg per day] (3s)


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

Asunaprevir: May decrease the serum concentration of Norelgestromin. 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

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 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

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

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 " � 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

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

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 patches have not been applied 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.


Adverse Reactions


The following reactions have been reported with the contraceptive patch. Adverse reactions associated with oral combination hormonal contraceptive agents are also likely to appear with the topical contraceptive patch (frequency difficult to anticipate). See individual oral contraceptive monographs for additional information.

>10%:

Central nervous system: Headache (21%)

Endocrine & metabolic: Breast changes (22%; including breast engorgement, discomfort, mastalgia)

Gastrointestinal: Nausea (17%)

Local: Application site reaction (17%)

1% to 10%:

Cardiovascular: Increased blood pressure (<3%), pulmonary embolism (<3%)

Central nervous system: Anxiety ( ≤6%), mood disorder ( ≤6%), dizziness (3%), fatigue (3%), migraine (3%), insomnia (<3%), malaise (<3%)

Dermatologic: Acne vulgaris (3%), pruritus (3%), chloasma (<3%), contact dermatitis (<3%), erythema (<3%), skin irritation (<3%)

Endocrine & metabolic: Menstrual disease (6%), weight gain (3%), change in libido (<3%), dyslipidemia (<3%), fluid retention (<3%), galactorrhea (<3%), premenstrual syndrome (<3%)

Gastrointestinal: Abdominal pain (8%), vomiting (5%), diarrhea (4%), abdominal distention (<3%), cholecystitis (<3%)

Genitourinary: Dysmenorrhea (8%), vaginal hemorrhage (6%), vulvovaginal candidiasis (4%), genital discharge (<3%), uterine spasm (<3%), vaginal dryness (<3%), vulvar dryness (<3%)

Neuromuscular & skeletal: Muscle spasm (<3%)

<1% (Limited to important or life-threatening): Alopecia, altered serum glucose, arterial thrombosis, benign mammary fibroadenoma, blood cholesterol abnormal, cerebrovascular accident, cervical dysplasia, cholelithiasis, cholestasis, cholestatic jaundice, colitis, contact lens intolerance (or complication), deep vein thrombosis, dysgeusia, eczema, edema, emotional disturbance, erythema multiforme, erythema nodosum, hepatic adenoma, hepatic neoplasm, hyperglycemia, hypersensitivity reaction, hypertension, hypertensive crisis, increased appetite, insulin resistance, intracranial hemorrhage, lesion (hepatic), malignant neoplasm of breast, malignant neoplasm of cervix, mass (breast), migraine with aura, myocardial infarction, skin photosensitivity, skin rash, thrombosis, urticaria, uterine fibroids


Warnings/Precautions


Concerns related to adverse effects:

- Breast cancer: 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 women 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, 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. Canadian labeling contraindicates use in women with steroid dependent jaundice, cholestatic jaundice, or history of jaundice of pregnancy.

- 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. Consider alternative contraception for women with uncontrolled dyslipidemia.

- 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: Combination hormonal contraceptives may increase the risk of venous thromboembolism. [US Boxed Warning]: The pharmacokinetic profile of the patch is different from oral contraceptives; steady state concentrations of ethinyl estradiol are ~60% higher following use of the patch than with oral tablets containing ethinyl estradiol 35 mcg. Peak concentrations are lower with the patch. The risk of venous thromboembolism (VTE) may be further increased with use of the contraceptive patch due to increased estrogen exposure in comparison to oral contraceptives. The increased estrogen exposure may increase the risk of adverse events, including venous thromboembolism. Discontinue use of combination hormonal contraceptives if an arterial or venous thrombotic event occurs. Women with inherited thrombophilias (eg, protein C or S deficiency) may have increased risk of venous thromboembolism (DeSancho 2010; van Vlijmen 2011). Use is contraindicated in women with hypercoagulopathies (inherited or acquired).

- Vaginal bleeding: Breakthrough or intracyclic bleeding and spotting may occur, 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:

- Cardiovascular disease: Use 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 is contraindicated in women at high risk of arterial or venous thrombotic diseases.

- Depression: Use with caution in patients with a history of depression; discontinue if serious depression recurs.

- Gallbladder disease: May have a risk of gallbladder disease; may worsen existing gallbladder disease.

- Hepatic adenomas: 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: Combination hormonal contraceptives may be poorly metabolized in women with hepatic impairment. Discontinue if jaundice develops during therapy or if liver function becomes abnormal.

- Hereditary angioedema: Estrogens may induce or exacerbate 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). The manufacturer contraindicates use in women with uncontrolled hypertension and recommends monitoring women with well-controlled hypertension; discontinue therapy if blood pressure rises significantly.

- Migraine: Evaluate new, recurrent, severe or persistent headaches. Use in patients with migraine headaches with aura, or migraine headaches of any type if >35 years of age is contraindicated.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, 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:

- Pediatric: 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. Use is contraindicated 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. The Canadian labeling contraindicates use in patients who have undergone major surgery associated with an increased risk of post-operative thromboembolism and in patients with prolonged immobilization.

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.

- Ovarian cancer: 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).


Pregnancy Considerations

Pregnancy status should be evaluated prior to prescribing (CDC 2013); treatment should be discontinued if pregnancy occurs. In general, the use of combination hormonal contraceptives when inadvertently taken early in pregnancy have not been associated with teratogenic effects. The topical patch may be less effective in patients weighing ≥90 kg (198 lb).

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 21-42 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 breastfeed, or ≥4 weeks after a second trimester abortion or miscarriage.


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Pharmacology

Combination hormonal 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.


Absorption

Topical: Equivalent when applied to abdomen, buttock, upper outer arm, and upper torso

Ethinyl estradiol and norelgestromin: Rapid; reaches plateau by ~48 hours. Absorption of ethinyl estradiol may be increased with heat exposure due to sauna, whirlpool, or treadmill.

The AUC plasma concentration of ethinyl estradiol at steady state are ~60% higher following use of the patch than with those observed following an oral 35 mcg tablet. Peak plasma concentrations of ethinyl estradiol are 25% lower with the patch than with the tablet.


Metabolism

Topical: First-pass effect avoided

Ethinyl estradiol: Forms metabolites

Norelgestromin: Hepatic to norgestrel and others


Excretion

Metabolites of ethinyl estradiol and norelgestromin: Urine and feces


Half-Life Elimination

Topical: Ethinyl estradiol: ~17 hours; Norelgestromin: ~28 hours


Protein Binding

Ethinyl estradiol: Albumin

Norelgestromin and norgestrel: >97%; norelgestromin to albumin and norgestrel to sex-hormone-binding globulin


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 weight gain, cramps, bloating, macromastia, menstrual irregularities, decreased libido, skin irritation, or facial skin discoloration. Have patient report immediately to prescriber signs of hepatic impairment, angina, dyspnea, hemoptysis, severe dizziness, syncope, considerable nausea, strength differences from one side to another, difficulty speaking or thinking, change in balance, blurred vision, edema of extremities, extremity discoloration, painful extremities, severe headache, depression, intolerable asthenia, considerable dyspepsia, urinary retention, oliguria, lump in breast, mastalgia, nipple discharge, vaginal hemorrhaging, vaginitis, vision changes, exophthalmos, 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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