How Do Estrogens/Progestins Work?

Estrogens/progestins are combination hormonal medications used for contraception and in the treatment of uterine fibroids and other female hormonal disorders. Estrogens and progestins are synthetic formulations of the natural female sex hormones progesterone and estrogen and have similar effects.

Estrogens are a group of endogenous hormones responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Progesterone is the other female sex hormone that prepares the endometrium, the inner lining of the uterus, for implantation and continuation of pregnancy.

Estrogens/progestins work by binding to estrogen and progesterone receptors, protein molecules in cells that respond to these hormones. Estrogens/progestins medications interfere with the functions of endogenous estrogen and progesterone to control excessive bleeding, prevent pregnancy, and relieve menopausal symptoms.

Estrogens/progestins formulations may contain different types of estrogens, progesterone, and other substances known as gonadotropin-releasing hormone (GnRH) antagonists that block the activity of GnRH produced by the hypothalamus. Some estrogen/progestin drugs may also contain iron to supplement iron loss from excessive bleeding.

Estrogens/progestins work in the following ways in the treatment of uterine fibroids:

• GnRH antagonists bind to GnRH receptors in the pituitary gland and prevent GnRH from stimulating the release of the follicular stimulating hormone (FSH) and luteinizing hormone (LH). This reduces ovarian production of estrogen and progesterone, reducing the bleeding associated with fibroids.
• The estrogen in the medication supplements the loss of natural circulating estrogen due to the medication and prevents bone loss due to reduced estrogen levels.
• The progestin in the medication supplements the reduced progesterone level caused by the medication and protects the uterus from potential adverse effects from unopposed estrogen.

Estrogens/progestins work in the following ways in preventing pregnancy:

• Suppress ovulation and maturation of the ovum by reducing the release of GnRH from the hypothalamus, and the release of FSH and LH from the pituitary gland.
• Thicken the cervical mucus, hindering the passage of sperm into the uterus.
• Thin the uterus lining (endometrium) preventing implantation of the fertilized egg.

Estrogens/progestins may be administered in the following ways:

• Oral tablets or capsules are taken every day for the duration of treatment for uterine fibroids, not exceeding 24 months. The medication should be started as soon as possible, but no later than 7 days after the start of menstrual bleeding.
• Oral tablets for contraception typically start on the first day of menstruation and are taken every day in varying cycles during the period birth control is followed.
• Soft flexible rings are placed inside the vagina, which releases measured daily doses during the period contraception is practiced. The vaginal ring is left in place for 21 days with a gap of 7 days during which menstrual bleeding occurs, after which a new ring may be placed.

The uses of estrogens/progestins include:

FDA-approved:

• Management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women
• Contraception in females with reproductive potential
• Treatment of moderate acne vulgaris
• Premenstrual dysphoric disorder (a severe form of premenstrual syndrome)
• Hormone replacement therapy for the treatment of moderate to severe vasomotor symptoms in menopausal women with an intact uterus, and prevention of osteoporosis in postmenopausal women with an intact uterus

Off-label uses:

• Dysmenorrhea (painful menstruation)
• Dysfunctional uterine bleeding
• Endometriosis (a disorder in which endometrial tissue grows outside the uterus)
• Polycystic ovarian syndrome (PCOS)

Side effects of estrogens/progestins may include the following:

• Decrease in bone mineral density
• Hot flashes, hyperhidrosis (excessive sweating), or night sweats
• Headaches and migraines
• Premenstrual syndrome
• Menstrual cramps
• Breakthrough bleeding
• Change in menstrual flow
• Spotting or scanty vaginal bleeding
• Amenorrhea (absence of menstruation)
• Dysmenorrhea (painful menstruation)
• Irregular menstruation
• Vulvovaginal mycotic (fungal) infection
• Vaginal candidiasis (Candida yeast infection)
• Vaginal discharge
• Vaginitis (vaginal inflammation)
• Metrorrhagia (vaginal bleeding between periods)
• Menorrhagia (heavy and prolonged menstrual periods)
• Abnormal uterine bleeding
• Uterine fibroid
• Uterine fibroid prolapse, degeneration, or expulsion
• Vaginal ring-related events such as:
  • Expulsion
  • Vaginal pain and discomfort
  • Foreign body sensation
  • Vaginal injury and bleeding from ring breakage
  • Penile disorders or reactions in male partners
• Breast symptoms such as:
  • Enlargement or swelling
  • Cyst
  • Tenderness
  • Pain or discomfort
  • Galactorrhea (milky secretion from the nipples)
• Changes in libido
• Increase in systolic or diastolic blood pressure
• Hypertension (high blood pressure)
• Myocardial infarction (heart attack)
• Cerebral hemorrhage
• Varicose vein aggravation
• Venous/arterial thromboembolic (blood clot-related) events including:
  • Deep vein thrombosis/DVT (blood clot in deep veins)
  • Pulmonary embolism/PE (blood clot in the lungs)
  • Stroke
  • Myocardial infarction (heart attack)
  • Intracardiac thrombosis
  • Cerebrovascular thrombosis
  • Retinal vein thrombosis
  • Thrombophlebitis (inflammation in the wall of a vein with an associated blood clot)
• Edema
• Weakness
• Fatigue
• Influenza
• Arthralgia (joint pain)
• Nausea
• Vomiting
• Abdominal pain, discomfort, or tenderness
• Abdominal distention
• Dyspepsia (indigestion)
• Bloating
• Stomach cramps
• Diarrhea
• Appetite changes
• Anorexia (loss of appetite)
• Depression
• Anxiety
• Nervousness
• Irritability
• Emotional lability (mood swings)
• Suicidal ideation
• Dizziness
• Somnolence (drowsiness)
• Alopecia (hair loss)
• Hirsutism (inappropriate male pattern hair growth in women)
• Skin reactions such as:
  • Acne
  • Rash
  • Urticaria (hives)
  • Hemorrhagic eruption
  • Chloasma/melasma (facial skin pigmentation disorder)
  • Erythema multiforme (round lesions like a bullseye)
  • Erythema nodosum (tender bumps under the skin)
• Hypersensitivity reactions such as:
  • Anaphylaxis (severe allergic reaction)
  • Angioedema (swelling in the tissue under the skin or mucous membranes)
• Increase in liver enzymes (ALT and AST)
• Hyperkalemia (high potassium in the blood)
• Increase in blood cholesterol levels
• Weight changes
• Upper respiratory tract infection
• Respiratory symptoms
• Low trauma fractures
• Cholestasis (impaired bile flow from the liver)
• Cholestatic jaundice
• Gallbladder disease
• Hepatic adenoma (benign liver tumor)
• Pancreatitis (inflammation of the pancreas)
• Optic neuritis (inflammation of the optic nerve)
• Contact lens intolerance

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with travel medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of estrogen/progestin drugs include:

• Altavera
• Alyacen 1/35
• Alyacen 7/7/7
• Amethia
• Amethia Lo
• Amethyst
• Annovera
• Apri
• Aranelle
• Ashlyna
• Aubra
• Aviane
• Azurette
• Balziva 28
• Bekyree
• Beyaz
• Blisovi 24 Fe
• Blisovi Fe 1.5/30
• Blisovi Fe 1/20
• Briellyn
• Camrese
• Camrese Lo
• Caziant
• Chateal
• Cryselle
• Cyclafem 0.5/35
• Cyclafem 1/35
• Cyclafem 7/7/7
• Cyclessa
• Cyonanz
• Cyred
• Cyred EQ
• Dasetta 1/35
• Dasetta 7/7/7
• Daysee
• Delyla
• Desogen
• desogestrel/ethinyl estradiol
• dienogest/estradiol valerate
• drospirenone/ethinyl estradiol
• drospirenone/ethinyl estradiol/levomefolate
• elagolix/estradiol/norethindrone acetate
• Elifemme
• Elinest
• EluRyng
• Emoquette
• Enpresse
• Enskyce
• Estarylla
• Estrostep Fe
• etonogestrel/ethinyl estradiol
• etynodiol/ethinyl estradiol
• FaLessa
• FaLessa Kit
• Falmina
• Fayosim
• Femhrt
• Femynor
• Fyavolv
• Generess Fe
• Gianvi
• Hailey 1.5/30
• Introvale
• Isibloom
• Jevantique Lo
• Jinteli
• Jolessa
• Juleber
• Junel 1.5/30
• Junel 1/20
• Junel Fe 1.5/30
• Junel Fe 1/20
• Junel Fe 24
• Kaitlib Fe
• Kariva
• Kelnor
• Kimidess
• Kurvelo
• Larin 1.5/30
• Larin 1/20
• Larin 24 FE
• Larin FE 1.5/30
• Larin FE 1/20
• Larissia
• Layolis FE
• Leena
• Lessina 21
• Lessina 28
• Levonest
• levonorgestrel oral/ethinyl estradiol
• Levora
• Lillow
• Lo Loestrin Fe
• Lo Minastrin Fe
• Loestrin 1.5/30
• Loestrin 1/20
• Loestrin 24 Fe
• Loestrin Fe 1.5/30
• Loestrin Fe 1/20
• Lomedia 24 Fe
• Loryna
• LoSeasonique
• Low-Ogestrel
• Lutera
• Lybrel
• Marlissa
• Melodetta 24 FE
• Merzee
• mestranol/norethindrone (discontinued)
• Mibelas 24 FE
• Microgestin 1.5/30
• Microgestin 1/20
• Microgestin Fe 1.5/30
• Microgestin Fe 1/20
• Microgynon
• Mili
• Minastrin 24 FE
• Mircette
• Mono-Linyah
• Mononessa
• Myfembree
• Myzilra
• Natazia
• Necon 0.5/35
• Necon 1/50 (DSC)
• Nexesta Fe
• Nordette
• Norethin 1/35E
• norethindrone acetate/ethinyl estradiol
• norethindrone acetate/ethinyl estradiol/ferrous fumarate
• norethindrone/ethinyl estradiol
• norethindrone/ethinyl estradiol/ferrous fumarate
• norgestimate/ethinyl estradiol
• norgestrel/ethinyl estradiol
• Norinyl 1+35
• Norinyl 1/50 (DSC)
• Nortrel 0.5/35
• Nortrel 1/35
• Nortrel 7/7/7
• NuvaRing
• Nylia 1/35
• Nylia 7/7/7
• Ocella
• Ogestrel
• Oriahnn
• Orsythia
• Ortho Cyclen-28
• Ortho Tri-Cyclen
• Ortho Tri-Cyclen Lo
• Ortho-Cept
• Ovranette
• Philith
• Pimtrea
• Pirmella 1/35
• Pirmella 7/7/7
• Portia 21
• Portia 28
• Previfem
• Quartette
• Quasense
• Reclipsen
• relugolix/estradiol/norethindrone
• Rivelsa
• Safyral
• Seasonale
• Seasonique
• segesterone/ethinyl estradiol
• Setlakin
• Solia
• Sprintec 28
• Sronyx
• Syeda
• Tarina 24 FE
• Tarina FE 1/20
• Taytulla
• Tilia Fe
• Tri-Estarylla
• Tri-Linyah
• Tri-Lo Sprintec
• Tri-Lo-Estarylla
• Tri-Lo-Marzia
• Tri-Lo-Mili
• Tri-Mili
• TriCyclen
• TriFemynor
• TriLegest Fe
• Trinessa
• TriNessa Lo
• TriPrevifem
• TriSprintec
• Trivora 28
• Tydemy
• Velivet
• Vestura
• Vienva
• Viorele
• Vyfemla
• Wera
• Wymzya FE
• Yaela
• Yasmin
• Yaz
• Zarah
• Zenchent Fe (DSC)
• Zovia