Generic and Brand Names
- Sex Hormones
- Estrogens
- estradiol (Estrace)
- estrogens, conjugated (C.E.S., Premarin)
- estrogens, esterified (Menest)
- estropipate (Ortho-Est, Ogen)
- Progestins
- desogestrel (Kariva, Cyclessa)
- drospirenone (Yasmin, YAZ)
- etonogestrel (Implanon)
- levonorgestrel (Mirena, Plan B)
- medroxyprogesterone (Provera)
- norethindrone acetate (Aygestin)
- norgestrel (Ovrette)
- progesterone
- ulipristal (Ella)
- Estrogen Receptor Modulators
- raloxifene (Evista)
- toremifene (Fareston)
- Fertility Drugs
- cetrorelix (Cetrotide)
- chorionic gonadotropin (Chorex, Profasi, Pregnyl)
- clomiphene (Clomid)
- follitropin alfa (Gonal-F)
- follitropin beta (Follistim)
- ganirelix (Antagon)
- lutropin alfa (Luveris)
- menotropins (Pergonal, Repronex)
- Uterine Motility Drugs
- Oxytocics
- Ergonovine (Ergotrate)
- methylergonovine (Methergine)
- oxytocin (Pitocin, Syntocinon)
- Abortifacients
- carboprost (Hemabate)
- dinoprostone (Cervidil, Prepidil Gel, Prostin E2)
- mifepristone (Mifeprex)
Female Sex Hormones
Female sex hormones (estrogen and progesterone) either replace missing hormone or suppress the body's own output.
Estrogen is the most potent endogenous female sex hormone. It controls the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), drives proliferation of the endometrial lining, and competes with androgens for receptor sites. Losing it produces the menopausal changes in the uterus, vagina, breasts, and cervix. Progestins turn the proliferative endometrium into a secretory endometrium, inhibit FSH and LH, and prevent follicle maturation, ovulation, and uterine contraction. Their contraceptive mechanism is not fully known, but circulating progestins and estrogens appear to "trick" the hypothalamus and pituitary into withholding gonadotropin-releasing hormone (GnRH), FSH, and LH, so no follicle develops and no ovulation occurs.
Indications
Estrogens go to hormone replacement therapy (HRT) in small doses when ovarian activity is blocked or absent, palliation of menopausal discomfort in the first few years, female hypogonadism and ovarian failure, prevention of postpartum breast engorgement, slowing bone loss in osteoporosis, and palliation of cancers with known receptor sensitivity. Progestins are used for contraception and for the endometrial and ovulation-suppressing actions described above.
Across age groups: these drugs have had little testing in children and can cause premature epiphyseal closure, so use caution in a growing child and use the smallest possible dose for oral contraceptives in teenage girls. Adult women on any of these drugs need an annual exam including breast exam and Pap smear; estrogen users should not smoke (thrombotic risk); fertility patients need strong psychological support and a clear explanation of the multiple-birth risk; men treated for certain cancers should be warned about estrogenic effects. Not indicated in pregnancy or lactation given the risk to fetus or neonate. In older adults, HRT is no longer commonly used postmenopause.
Pharmacokinetics (Estrogen)
Here are the characteristic interactions of female sex hormone estrogen and the body in terms of absorption, distribution, metabolism, and excretion:
| Route | Onset | Peak | Duration |
|---|---|---|---|
| PO | Slow | Days | Unknown |
| Half-life (T1/2) | Metabolism | Excretion |
|---|---|---|
| Unknown | Liver | Urine |
Pharmacokinetics (Progestins)
Here are the characteristic interactions of female sex hormone progestin and the body in terms of absorption, distribution, metabolism, and excretion:
| Route | Onset | Peak | Duration |
|---|---|---|---|
| PO | Varies | Unknown | Unknown |
| Half-life (T1/2) | Metabolism | Excretion |
|---|---|---|
| Unknown | Liver | Kidney (urine), intestines (feces) |
Contraindications and Cautions
Estrogens are contraindicated with estrogen allergy (hypersensitivity); idiopathic vaginal bleeding, breast cancer, or estrogen-dependent cancer (drug can worsen them); a history of thromboembolic disorders, CVA, or heavy smoking (thrombus and embolus risk); hepatic dysfunction or impairment (estrogen affects liver function and its own metabolism); pregnancy (serious fetal defects); and lactation. Use caution with metabolic bone disease (estrogen's bone-conserving effect can aggravate it) and renal insufficiency (impaired excretion plus fluid and electrolyte effects).
Progestins are contraindicated or cautioned with pelvic inflammatory disease (PID), STDs, endometriosis, or pelvic surgery, because progestins act on uterine vasculature. Drospirenone is contraindicated in patients at risk for hyperkalemia because of its antimineralocorticoid effect. Use caution with epilepsy, migraine, asthma, and cardiac or renal dysfunction (potential exacerbation).
Adverse Effects
Estrogen: GI (nausea, vomiting, abdominal cramp, bloating, colitis, acute pancreatitis, cholestatic jaundice, hepatic adenoma); GU (breakthrough bleeding, menstrual irregularities, dysmenorrhea, amenorrhea, libido changes); and systemic effects (fluid retention, electrolyte disturbance, headache, dizziness, mental changes, weight changes, edema). Progestin systemic effects mirror estrogen. The dermal patch adds local skin irritation; vaginal gel adds headache, nervousness, constipation, breast enlargement, and perineal pain; intrauterine systems add abdominal pain, endometriosis, abortion, PID, and device expulsion; vaginal use adds local irritation and swelling.
Interactions
Estrogen: barbiturates, rifampin, tetracyclines, and phenytoin lower serum estrogen; corticosteroids gain increased therapeutic and toxic effect; nicotine raises thrombus and embolus risk; grapefruit juice inhibits estradiol metabolism; St. John's wort alters estrogen metabolism and can make estrogen-containing contraceptives less effective. Progestins: barbiturates, carbamazepine, phenytoin, griseofulvin, penicillin, tetracyclines, and rifampin reduce progestin effectiveness, and St. John's wort can make progestin-containing contraceptives less effective.
Estrogen Receptor Modulators
Estrogen receptor modulators stimulate or block specific estrogen receptor sites. They aim to deliver some of estrogen replacement's benefit while limiting its harms, raising bone mineral density without stimulating the endometrium.
Indication: prevention and treatment of osteoporosis in postmenopausal women.
Across age groups, the same cautions apply: little pediatric testing and risk of premature epiphyseal closure in growing children; adults need annual exams with breast exam and Pap smear; not indicated in pregnancy or lactation; and HRT is no longer common in older postmenopausal women.
Pharmacokinetics
Here are the characteristic interactions of estrogen receptor modulators and the body in terms of absorption, distribution, metabolism, and excretion:
| Route | Onset | Peak | Duration |
|---|---|---|---|
| PO | Varies | 4-7 h | 24 h |
| Half-life (T1/2) | Metabolism | Excretion |
|---|---|---|
| 27.7 h | Liver | Intestines (feces) |
Contraindications and Cautions
Contraindicated with allergy to the drug (hypersensitivity) and with pregnancy or lactation. Use caution with a history of venous thrombosis or smoking, since combining smoking and estrogen raises clot risk.
Adverse Effects
Raloxifene can cause GI upset, nausea, and vomiting. Fluid balance changes can cause headache, dizziness, visual changes, and mental changes. Specific estrogen receptor stimulation can cause hot flashes, skin rash, edema, and vaginal bleeding.
Interactions
Cholestyramine reduces raloxifene absorption. Highly protein-bound drugs (diazepam, ibuprofen, indomethacin, naproxen) compete for binding sites. Warfarin taken with raloxifene decreases prothrombin time.
Nursing Considerations (Sex Hormones and Estrogen Receptor Modulators)
Nursing Assessment
Screen for the cautions and contraindications above (drug allergy, cardiovascular disease, metabolic bone disease, thromboembolism history). Get a baseline physical (bowel sounds, skin, vital signs, mental status). Assist with pelvic and breast exams, collect the Pap smear, and take a menstrual history. Arrange an ophthalmic exam for contact lens wearers, because hormonal changes alter eye fluid and corneal curvature and can change lens fit and visual acuity. Monitor labs (urinalysis, renal and hepatic function) for dose reduction needs and toxicity.
Nursing Diagnoses
Ineffective tissue perfusion related to drug-induced vascular changes and thromboembolism risk. Excess fluid volume related to fluid retention. Acute pain related to GI pain and headache.
Implementation with Rationale
Give with food to prevent GI upset, and use small, frequent meals for nausea and vomiting. Provide an analgesic for headache. Watch for swelling and for vision or contact lens changes that signal fluid retention. Provide comfort and safety measures (adequate lighting, raised side rails) and teach the regimen for understanding and compliance.
Evaluation
Monitor response (relief of menopausal signs, prevention of pregnancy, lower CAD risk factors, cancer palliation) and adverse effects (GI upset, edema, secondary sex characteristic changes, headache, thromboembolic episodes, breakthrough bleeding). Confirm the patient can name the drug, its indication, and adverse effects, and monitor compliance.
Fertility Drugs
Fertility drugs stimulate the female reproductive system. They suit women without primary ovarian failure who cannot conceive after 1 year of unprotected intercourse. They either directly stimulate follicles and ovulation or push the hypothalamus to raise FSH and LH, driving follicular development and ovum maturation.
Indications
Treatment of infertility in women with functioning ovaries whose partners are fertile, and stimulation of multiple follicle development to harvest ova for in vitro fertilization. Menotropins also stimulate spermatogenesis in men with low sperm counts and otherwise normal testes. Cetrorelix blocks premature LH surges in women undergoing controlled ovarian stimulation by acting as a GnRH antagonist. Follitropin alfa and follitropin beta are injected FSH molecules that stimulate follicular development for infertility treatment and ova harvesting.
Pharmacokinetics
Here are the characteristic interactions of fertility drugs and the body in terms of absorption, distribution, metabolism, and excretion:
| Route | Onset | Peak | Duration |
|---|---|---|---|
| PO | 5-8 d | Unknown | 6 wk |
| Half-life (T1/2) | Metabolism | Excretion |
|---|---|---|
| 5 days | Liver | Intestines (feces) |
Contraindications and Cautions
Contraindicated with allergy to the drug; primary ovarian failure (these drugs only stimulate functioning ovaries); pregnancy (serious fetal effects); and idiopathic uterine bleeding (may mask a problem the drug would worsen). Use caution with thyroid or adrenal dysfunction (drugs act on the hypothalamic-pituitary axis), ovarian cysts (can enlarge under stimulation), lactation, thromboembolic disease, and respiratory disease (fluid and blood flow shifts can overtax the lungs).
Adverse Effects
Greatly increased risk of multiple births and birth defects. Ovarian overstimulation brings abdominal pain, distention, ascites, and pleural effusion. Others: headache, fluid retention, nausea, bloating, uterine bleeding, ovarian enlargement, gynecomastia, and febrile reactions, possibly from stimulated progesterone release.
Nursing Considerations
Nursing Assessment
Screen for the cautions and contraindications above (allergy, primary ovarian failure, thyroid or adrenal dysfunction, ovarian cysts, idiopathic uterine bleeding, thromboembolic disease). Get a baseline physical (skin, vital signs, neuro status). Assist with pelvic and breast exams, collect the Pap smear, and take a menstrual history. Monitor labs (hormone levels, renal and hepatic function) for dose changes and for ovarian hyperstimulation.
Nursing Diagnoses
Acute pain related to headache, fluid retention, or GI upset. Sexual dysfunction related to altered hormone control. Disturbed body image related to treatment and diagnosis.
Implementation with Rationale
Find the cause of dysfunction before starting therapy. Do a pelvic exam before each use to rule out ovarian enlargement, pregnancy, or uterine problems. Check urine estrogen and estradiol levels before therapy to confirm ovarian function. Give an appropriate dose of human chorionic gonadotropin as indicated. Stop the drug at any sign of ovarian overstimulation and arrange hospitalization to monitor and support the patient. Give a calendar of treatment days, the adverse effects to expect, and instructions on timing of intercourse. Warn clearly about the multiple-birth risk so the patient can decide with full information. Offer support for the low self-esteem that comes with infertility, provide comfort measures, and teach the regimen.
Evaluation
Monitor response (ovulation) and adverse effects (abdominal bloating, weight gain, ovarian overstimulation, multiple births). Confirm the patient can name the drug, its indication, and adverse effects, and monitor compliance.
Uterine Motility Drugs: Oxytocics
Uterine motility drugs drive uterine contraction to assist labor (oxytocics) or to induce abortion (abortifacients). Oxytocics mimic the hypothalamic hormone oxytocin stored in the posterior pituitary, acting directly on neuroreceptor sites to contract the uterus and working best in the gravid uterus. Oxytocin, the synthetic form, also contracts the lacteal glands in the breast, promoting milk ejection in lactating women.
Indications
Prevention and treatment of uterine atony after delivery, lowering the risk of postpartum hemorrhage. Oxytocin (Pitocin) is the recommended first-line uterotonic for both prevention and treatment of postpartum hemorrhage; when atony does not respond, methylergonovine, carboprost, and misoprostol are added in sequence before surgical measures (AAFP; Oxytocin, StatPearls).
Pharmacokinetics
Here are the characteristic interactions of oxytocics and the body in terms of absorption, distribution, metabolism, and excretion:
| Route | Onset | Peak | Duration |
|---|---|---|---|
| IV | Immediate | Unknown | 60 min |
| IM | 3-5 min | Unknown | 2-3 h |
| Half-life (T1/2) | Metabolism | Excretion |
|---|---|---|
| 1-6 min | Tissues | Kidneys (urine) |
Contraindications and Cautions
Contraindicated with allergy to oxytocics; cephalopelvic disproportion, unfavorable fetal position, complete uterine atony, or early pregnancy (all can be compromised by uterine stimulation). Use caution with coronary disease and hypertension, because the arterial contraction these drugs cause can raise blood pressure or compromise coronary blood flow.
Adverse Effects
Excessive effects: uterine hypertonicity and spasm, uterine rupture, postpartum hemorrhage, decreased fetal heart rate. Common effects: GI upset, nausea, headache, dizziness. Ergotism from ergonovine and methylergonovine: nausea, blood pressure changes, weak pulse, dyspnea, chest pain, numbness and coldness in extremities, confusion, excitement, delirium, convulsions, coma. Oxytocin has caused severe water intoxication with coma and even maternal death with prolonged use.
Nursing Considerations
Nursing Assessment
Screen for cautions and contraindications (allergy, lactation status, uterine atony, hypertension). Get a baseline physical (neuro status, vital signs, labor pattern, uterine tone). Monitor labs (coagulation studies, complete blood count).
Nursing Diagnoses
Acute pain related to increased frequency and intensity of uterine contractions or headache. Excess fluid volume related to ergotism or water intoxication.
Implementation with Rationale
Confirm fetal position (where appropriate) and cephalopelvic proportions to prevent delivery complications. When giving oxytocin to stimulate labor, regulate delivery with an infusion pump between contractions. Monitor blood pressure and fetal heart rate frequently during and after administration. Track uterine tone, involution, and bleeding. Provide comfort measures and teach the regimen.
Evaluation
Monitor response (uterine contraction, prevention of hemorrhage, milk let-down) and adverse effects (blood pressure changes, uterine hypertonicity, water intoxication, ergotism). Confirm the patient can name the drug, its indication, and adverse effects, and monitor compliance.
Abortifacients
Abortifacients stimulate uterine activity, dislodging implanted trophoblasts and preventing implantation of a fertilized egg. Keep the brand names straight: carboprost is Hemabate (a prostaglandin F2-alpha analogue), dinoprostone is prostaglandin E2 sold as Cervidil, Prepidil Gel, and Prostin E2, and mifepristone (Mifeprex) is a progesterone antagonist used with misoprostol for medical abortion (Dinoprostone monograph, Drugs.com).
Indications
Evacuation of uterine contents through intense uterine contractions. Approved to terminate pregnancy at 12-20 weeks from the date of the last menstrual period.
Pharmacokinetics
Here are the characteristic interactions of abortifacients and the body in terms of absorption, distribution, metabolism, and excretion:
| Route | Onset | Peak | Duration |
|---|---|---|---|
| Intravaginal | 10 min | 15 min | 2-3 h |
| Half-life (T1/2) | Metabolism | Excretion |
|---|---|---|
| 5-10 h | Tissues | Kidneys (urine) |
Contraindications and Cautions
Contraindicated with allergy to abortifacients and prostaglandins; after 20 weeks from the last menstrual period (too late in the pregnancy); and lactation (serious neonatal effects). Use caution with active PID and CV, hepatic, renal, or pulmonary disease (can be exacerbated); asthma, hypertension, and adrenal disease; and acute vaginitis or a scarred uterus (aggravated by contractions).
Adverse Effects
From exaggerated desired effects: abdominal cramping, heavy uterine bleeding, perforated uterus, uterine rupture. Others: headache, nausea, vomiting, diarrhea, diaphoresis, backache, rash.
Nursing Considerations
Nursing Assessment
Screen for cautions and contraindications (allergy, active PID, CV disease). Get a baseline physical (neuro status, vital signs, skin). Monitor labs (leukocyte count, hemoglobin and hematocrit, complete blood count) for excess bleeding.
Nursing Diagnoses
Acute pain related to uterine contractions or headache. Ineffective coping related to abortion or fetal death.
Implementation with Rationale
Give by the indicated route, following the manufacturer's storage and preparation directions. Confirm the gestational age before administering. Confirm the abortion or uterine evacuation is complete by assessing vaginal bleeding and passage of tissue, to avoid later bleeding problems. Monitor blood pressure frequently during and after administration. Track uterine tone, involution, and bleeding during and for several days after use. Provide comfort measures and teach the regimen.
Evaluation
Monitor response (evacuation of the uterus) and adverse effects (GI upset, blood pressure changes, nausea, hemorrhage). Confirm the patient can name the drug, its indication, and adverse effects, and monitor compliance.
Frequently Asked Questions
Why must estrogen patients be told not to smoke? Estrogen raises the risk of clots, and nicotine compounds it, so combining smoking with estrogen sharply increases the risk of thromboembolic events such as stroke, deep vein thrombosis, and pulmonary embolism. Screening for thromboembolic risk and counseling against smoking is a recurring nursing job across this whole class.
What is the difference between an oxytocic and an abortifacient? Both drive uterine contraction, but the goal differs. Oxytocics such as oxytocin and methylergonovine are used after delivery to contract the uterus and prevent or treat postpartum hemorrhage. Abortifacients such as dinoprostone and carboprost produce intense contractions to evacuate uterine contents.
Which drug is first-line for postpartum hemorrhage? Oxytocin (Pitocin) is the recommended first-line uterotonic for both preventing and treating postpartum hemorrhage. If atony does not respond, methylergonovine, carboprost, and misoprostol are added in sequence before surgical intervention (AAFP; Oxytocin, StatPearls).
Carboprost is Hemabate, so what are Cervidil and Prepidil? Carboprost is sold as Hemabate. Cervidil, Prepidil Gel, and Prostin E2 are all forms of dinoprostone (prostaglandin E2). Mifepristone is sold as Mifeprex. Mixing these brand names up is a common error, and one this guide previously contained, so confirm the generic name before giving any of them (Dinoprostone monograph, Drugs.com).
Why does the multiple-birth risk come up with fertility drugs? Fertility drugs stimulate multiple follicles to develop and release ova, which greatly raises the chance of twins or higher-order multiples and of birth defects. Patients deserve an honest explanation of that risk up front so they can make an informed decision, alongside support for the emotional weight of infertility treatment.
What is the most dangerous adverse effect to watch for with fertility drugs? Ovarian hyperstimulation. Watch for abdominal pain, distention, ascites, and pleural effusion. Do a pelvic exam before each cycle to rule out ovarian enlargement, and stop the drug and arrange hospitalization at any sign of overstimulation.