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Indications

REMS

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: Raynaud’s phenomenon, edema, hypertension, THROMBOEMBOLISM, thrombophlebitis.

Derm: melasma, rash.

EENT: contact lens intolerance, optic neuritis, retinal thrombosis.

Endo: hyperglycemia.

F and E: Drosperinone-containing products only: hyperkalemia.

GI: abdominal cramps, bloating, cholestatic jaundice, gallbladder disease, liver tumors, nausea, PANCREATITIS, vomiting.

GU: Intrauterine levonorgestrel only: uterine imbedment/uterine rupture, amenorrhea, breakthrough bleeding, dysmenorrhea, spotting.

MS: Injectable medroxyprogesterone only: bone loss.

Neuro: depression, headache.

Misc: BREAST CANCER (ESPECIALLY WITH PROLONGED USE), HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA), weight change.

Interactions

Drug-Drug:

Drug-Natural Products:

Drug-Food:

Availability

Combination Estrogen/Progestin Oral Contraceptives

(generic available)

Extended-Cycle Contraceptive

Levonorgestrel

(generic available)

Etonorgestrel

Ulipristal

Medroxyprogesterone

(generic available)

Vaginal Ring Contraceptive

Transdermal Patch

Route/Dosage

Monophasic Oral Contraceptives

Biphasic Oral Contraceptives

Triphasic Oral Contraceptives

Fourphasic Oral Contraceptives

Extended-Cycle Contraceptive

Progestin-Only Oral Contraceptives

Progressive Estrogen Oral Contraceptives

Emergency Contraceptive

Injectable Contraceptive

medroxyprogesterone (Depo-Provera)

Intrauterine Contraceptive

Vaginal Ring Contraceptive

Transdermal Patch

Acne

US Brand Names

Estetrol/Drospirenone: Nextstellis

ethinyl estradiol/desogestrel: Apri-28, Cyred EQ, Enskyce, Isibloom, Juleber, Kalliga, Reclipsen

ethinyl estradiol/drospirenone: Beyaz, Jasmiel, Lo-Zumandimine, Loryna, Nikki, Ocella, Safyral, Syeda, Tydemy, Vestura, Yasmin, Yaz, Zumandimine

ethinyl estradiol/ethynodiol: Kelnor 1/35, Kelnor 1/50, Zovia 1/35

ethinyl estradiol/levonorgestrel: Afirmelle, Altavera, Aubra EQ, Aviane, Ayuna, Balcoltra, Chateal EQ, Falmina, Joyeaux, Kurvelo, Lessina, Levora-28, Lutera, Marlissa, Portia-28, Sronyx, Tyblume, Vienva

ethinyl estradiol/norethindrone: Alyacen 1/35, Aurovela 1/20, Aurovela 1.5/30, Aurovela 24 Fe, Aurovela Fe 1/20, Aurovela Fe 1.5/30, Balziva, Blisovi 24 Fe, Blisovi Fe 1/20, Blisovi Fe 1.5/30, Briellyn, Charlotte 24 Fe, Cyonanz, Dasetta 1/35, Finzala, Fyavolv, Gemmily, Generess Fe, Hailey 1.5/30, Hailey 24 Fe, Hailey Fe 1/20, Hailey Fe 1.5/30, Jinteli, Junel 1/20, Junel 1.5/30, Junel Fe 1/20, Junel Fe 1.5/30, Junel Fe 24, Kaitlib Fe, Larin 1/20, Larin 1.5/30, Larin 24 Fe, Larin Fe 1/20, Larin Fe 1.5/30, Layolis Fe, Loestrin 1/20, Loestrin 1.5/30, Loestrin Fe 1/20, Loestrin Fe 1.5/30, Merzee, Mibelas 24 Fe, Microgestin 1/20, Microgestin 1.5/30, Microgestin 24 Fe, Microgestin Fe 1/20, Microgestin Fe 1.5/30, Minastrin 24 Fe, Necon 0.5/35, Nexesta Fe, Nortrel 0.5/35, Nortrel 1/35, Nylia 1/35, Philith, Tarina 24 Fe, Tarina Fe 1/20 EQ, Taysofy, Taytulla, Tilia Fe, Vyfemla, Wera, Wymzya Fe, Zenchent Fe

ethinyl estradiol/norgestimate: Estarylla, Mili, Mono-Linyah, Nymyo, Previfem, Sprintec-28, VyLibra

ethinyl estradiol/norgestrel: Cryselle-28, Elinest, Low-Ogestrel

ethinyl estradiol/desogestrel: Azurette, Bekyree, Kariva, Mircette, Pimtrea, Simliya, Viorele, Volnea

ethinyl estradiol/norethindrone: Lo Loestrin Fe

ethinyl estradiol/desogestrel: Velivet

ethinyl estradiol/levonorgestrel: Enpresse-28, Levonest, Trivora-28

ethinyl estradiol/norethindrone: Alyacen 7/7/7, Aranelle, Dasetta 7/7/7, Leena, Nortrel 7/7/7, Nylia 7/7/7, Tri-Legest Fe

ethinyl estradiol/norgestimate: Tri-Estarylla, Tri-Linyah, Tri-Lo-Estarylla, Tri-Lo-Marzia, Tri-Lo-Mili, Tri-Lo-Sprintec, Tri-Mili, Tri-Nymyo, Tri-Sprintec, Tri-VyLibra, Tri-VyLibra Lo

estradiol valerate/dienogest: Natazia

ethinyl estradiol/levonorgestrel: Amethia, Amethyst, Ashlyna, Camrese, Camrese Lo, Daysee, Dolishale, Iclevia, Introvale, Jaimiess, Jolessa, LoJaimiess, LoSeasonique, Quartette, Rivelsa, Seasonique, Setlakin, Simpesse

norethindrone: Aygestin, Camila, Deblitane, Emzahh, Errin, Heather, Incassia, Jencycla, Lyleq, Nora-BE, Sharobel

Drospirenone: Slynd

etonogestrel: Nexplanon

levonorgestrel: Aftera, Athentia Next, Curae, EContra One-Step, Her Style, My Choice, My Way, New Day, Opcicon One-Step, Plan B One-Step, Take Action

ulipristal: Ella

medroxyprogesterone: Depo-Provera, Depo-subQ Provera 104

levonorgestrel: Kyleena, Liletta, Mirena, Skyla

ethinyl estradiol/etonogestrel: EluRyng, Enilloring, Haloette, NuvaRing

ethinyl estradiol/levonorgestrel: Twirla

ethinyl estradiol/norelgestromin: Xulane, Zafemy

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: contraceptive hormones

Pharmacokinetics

Absorption: Ethinyl estradiol: rapidly absorbed; Norethindrone: 65% absorbed; Desogestrel and levonorgestrel: 100% absorbed; Dienogest: 91% absorbed. Others are well absorbed after oral administration. Slowly absorbed from implant, SUBQ or IM injection. Some absorption follows intrauterine implantation.

Distribution: Unknown.

Protein Binding: Ethinyl estradiol: 97–98%; Drospirenone: 97%; Dienogest: 90%; Ulipristal: >94%.

Metabolism/Excretion: Ethinyl estradiol and norethindrone: undergo extensive first-pass hepatic metabolism. Desogestrel: is rapidly metabolized to 3-keto-desogestrel, the active metabolite. Most agents are metabolized by the liver.

Half-life: Ethinyl estradiol: 6–20 hr; Levonorgestrel: 45 hr; Norethindrone: 5–14 hr; Desogestrel (metabolite): 38 ± 20 hr; Drospirenone: 30 hr; Norgestimate (metabolite): 12–20 hr; Dienogest: 11 hr; others: unknown; Ulipristal: 32 hr.

Time/Action Profile

(prevention of pregnancy)

ROUTEONSETPEAKDURATION
PO1 mo1 mo1 mo†
Implant1 mo1 mo5 yr
Intrauterine system1 mo1 mo5 yr
IM1 mo1 mo3 mo
SUBQunknown1 wk3 mo

†Only during mo of taking contraceptive.

Patient/Family Teaching

Pronunciation

Estetrol/Drospirenone: ES-te-trol/droe-SPY-re-nown

ethinyl estradiol/desogestrel: ETH-in-il es-tra-DYE-ole/dess-oh-JESS-trel

ethinyl estradiol/drospirenone: ETH-in-il es-tra-DYE-ole/droe-SPY-re-nown

ethinyl estradiol/ethynodiol: ETH-in-il es-tra-DYE-ole/e-thye-noe-DYE-ole

ethinyl estradiol/levonorgestrel: ETH-in-il es-tra-DYE-ole/lee-voe-nor-JESS-trel

ethinyl estradiol/norethindrone: ETH-in-il es-tra-DYE-ole/nor-eth-IN-drone

ethinyl estradiol/norgestimate: ETH-in-il es-tra-DYE-ole/nor-JES-ti-mate

ethinyl estradiol/norgestrel: ETH-in-il es-tra-DYE-ole/nor-JESS-trel

ethinyl estradiol/desogestrel: ETH-in-il es-tra-DYE-ole/dess-oh-JESS-trel

ethinyl estradiol/norethindrone: ETH-in-il es-tra-DYE-ole/nor-eth-IN-drone

ethinyl estradiol/desogestrel: ETH-in-il es-tra-DYE-ole/dess-oh-JESS-trel

ethinyl estradiol/levonorgestrel: ETH-in-il ess-tra-DYE-ole/lee-voe-nor-JESS-trel

ethinyl estradiol/norethindrone: ETH-in-il es-tra-DYE-ole/nor-eth-IN-drone

ethinyl estradiol/norgestimate: ETH-in-il es-tra-DYE-ole/nor-JESS-ti-mate

estradiol valerate/dienogest: es-tra-DYE-ole VAL-er-ate/dye-EN-oh-jest

ethinyl estradiol/levonorgestrel: ETH-in-il ess-tra-DYE-ole/lee-voe-nor-JESS-trel

norethindrone: nor-eth-IN-drone

etonogestrel: e-toe-no-JESS-trel

levonorgestrel: LEE-voe-nor-JESS-trel

ulipristal: u-li-PRISS-tal

medroxyprogesterone: me-DROX-ee-proe-JESS-te-rone

levonorgestrel: LEE-voe-nor-JESS-trel

ethinyl estradiol/etonogestrel: ETH-in-il ess-tra-DYE-ole/e-toe-noe-JESS-trel

ethinyl estradiol/levonorgestrel: ETH-in-il ess-tra-DYE-ole/LEE-voe-nor-JESS-trel

ethinyl estradiol/norelgestromin: ETH-in-il ess-tra-DYE-ole/nor-el-JESS-troe-min