section name header

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

Classifications

Therapeutic Classification: contraceptive hormones

Indications

REMS


Action

Monophasic Oral Contraceptives

  • Provide a fixed dosage of estrogen/progestin over a 21-day cycle. Ovulation is inhibited by suppression of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg.

Biphasic Oral Contraceptives

  • Ovulation is inhibited by suppression of FSH and LH. May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg. In addition, smaller dose of progestin in phase 1 allows for proliferation of endometrium. Larger amount in phase 2 allows for adequate secretory development.

Triphasic Oral Contraceptives

  • Ovulation is inhibited by suppression of FSH and LH. May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg. Varying doses of estrogen/progestin may more closely mimic natural hormonal fluctuations.

Fourphasic Oral Contraceptives

  • Ovulation is inhibited by suppression of FSH and LH. May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg. Doses of estrogen decrease while doses of progestin increase over the 28-day cycle.

Extended-cycle

  • Provides continuous estrogen/progestin for 84 days, then off for 7 days (low-dose estrogen-only tablet taken during these 7 days with LoSeasonique and Seasonique), resulting in 4 menstrual periods/yr.

Progressive Estrogen

  • Contains constant amount of progestin with 3 progressive doses of estrogen.

Progestin-Only Contraceptives/Contraceptive Implant/Intrauterine Levonorgestrel/Medroxyprogesterone Injection

  • Mechanism not clearly known. May alter cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg. Ovulation may also be suppressed.

Emergency Contraceptive Pills

  • Inhibit ovulation/fertilization; may also alter tubal transport of sperm/egg and prevent implantation.

Vaginal Ring, Transdermal Patch

  • Inhibits ovulation, decreases sperm entry into uterus, decreases likelihood of implantation.

Anti-acne effect

  • Combination of estrogen/progestin may increase sex hormone binding globulin resulting in decreased unbound testosterone, which may be a cause of acne.
Therapeutic effects:
  • Prevention of pregnancy.
  • Decreased severity of acne.
  • Decrease in menstrual blood loss.
  • Decrease in premenstrual dysphoric disorder.
  • Decrease in vasomotor symptoms or symptoms of vulvar and vaginal atrophy due to menopause.
  • Increase in folate levels and prevention of neural tube defects.

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.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: edema, hypertension, Raynaud’s phenomenon, 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:, amenorrhea, breakthrough bleeding, dysmenorrhea, spotting, uterine imbedment/uterine rupture

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:

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

Intrauterine Contraceptive

Vaginal Ring Contraceptive

Transdermal Patch

Acne

Availability

Combination Estrogen/Progestin Oral Contraceptives

Extended-Cycle Contraceptive

Levonorgestrel

Etonorgestrel

Ulipristal

Medroxyprogesterone

Vaginal Ring Contraceptive

Transdermal Patch

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

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

Pill Image

drospirenone-ethinyl-estradiol_195-8394.jpg
ethinylestradiol-norethindrone_334-307.jpg
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