Pharmacology in Nursing Women’s Health Drugs Karen Ruffin RN, MSN Ed.

Female Reproductive Functions Female sex steroid hormones –Estrogens –Progestins Pituitary gonadotropin hormones –Follicle stimulating hormone (FSH) –Luteinizing hormone (LH)

Female Reproductive Functions (cont’d) Development of primary and secondary sex characteristics Menstrual cycle

Estrogens Three major endogenous estrogens –Estradiol (principal & most active) –Estrone –Estriol Synthesized from cholesterol in ovarian follicles Basic chemical structure of a steroid

Exogenous Estrogenic Drugs– Synthetic Steroidal –Conjugated estrogens, estradiol transdermal, many others Nonsteroidal –Chlorotrianisene, diethylstilbestrol diphosphate, others –These drugs no longer available in the United States

Estrogens Required For The development and maintenance of the female reproductive system The development of female secondary sex characteristics

Estrogens: Indications Treatment of or prevention of disorders that result from estrogen deficiency –Atrophic vaginitis –Hypogonadism –Oral contraception (given with a progestin) –Dysmenorrhea –“Hot flashes” of menopause

Estrogens: Indications (cont’d) Treatment of or prevention of disorders that result from estrogen deficiency (cont’d) –Uterine bleeding –Palliative treatment of advanced breast and prostate cancer –Osteoporosis treatment and prophylaxis –Many other indications

Estrogens: Indications (cont’d) Continuous-combined hormone replacement therapy (CCHRT) –Fixed estrogen/progestin combination products –Reduce complications, such as endometrial hyperplasia, that occur from using estrogen alone

Estrogens: Contraindications Allergy to the medication Any estrogen dependent cancer Undiagnosed abnormal vaginal bleeding Pregnancy Active thromboembolic disorder or history

Estrogens: Adverse Effects Thrombolytic events—most serious Nausea—most common Hypertension, thrombophlebitis, edema Vomiting, diarrhea, constipation, abdominal pain May cause photosensitivity, chloasma

Estrogens: Adverse Effects (cont’d) Amenorrhea, breakthrough uterine bleeding Tender breasts, fluid retention, headaches Others

Progestins Synthetic derivatives of progesterone –medroxyprogesterone (Provera) –hydroxyprogesterone –megestrol (Megace) –Many others

Progestins: Indications Treatment of functional uterine bleeding caused by: –Hormonal imbalance, fibroids, or uterine cancer Treatment of primary and secondary amenorrhea

Progestins: Indications (cont’d) Palliative treatment of some cancers and endometriosis Prevention of threatened miscarriage Alleviation of symptoms of PMS

Progestins: Indications (cont’d) megestrol –Adjunct therapy for treatment of breast and endometrial cancers –Also used for management of anorexia, cachexia, or unexplained weight loss in AIDS patients –Used to stimulate appetite and promote weight gain in patients with cancer Used with estrogen replacement therapy after menopause

Progestins: Adverse Effects Liver dysfunction—cholestatic jaundice Thrombophlebitis, thromboembolic disorders, such as PE Nausea, vomiting Amenorrhea, breakthrough uterine bleeding, spotting Edema, weight gain or loss Others

Contraceptive Drugs Medications used to prevent pregnancy Oral medications –Monophasic, biphasic, and triphasic forms –Most contain estrogen-progestin combinations

Contraceptive Drugs (cont’d) Other contraceptive forms available –Long-acting injectable form of medroxyprogesterone (Depo-Provera) –Transdermal contraceptive patch –Intravaginal contraceptive ring

Contraceptive Drugs: Mechanism of Action Prevent ovulation by inhibiting the release of gonadotropins and increasing uterine mucous viscosity, resulting in: –Decreased sperm movement and fertilization of the ovum –Possible inhibition of implantation of a fertilized egg (zygote)

Contraceptive Drugs: Other Drug Effects Improve menstrual cycle regularity Decrease blood loss during menstruation Decreased incidence of functional ovarian cysts and ectopic pregnancies

Contraceptive Drugs: Indications Primarily used to prevent pregnancy Other uses –Treatment of endometriosis and hypermenorrhea –To produce cyclic withdrawal bleeding –Postcoital emergency contraception

Contraceptive Drugs: Adverse Effects Drawbacks to the use of these drugs include: –Hypertension –Thromboembolism, possible PE, MI, stroke –Alterations in lipid and carbohydrate metabolism –Increases in serum hormone concentrations These effects are due to the estrogen component

Contraceptive Drugs: Adverse Effects (cont’d) May also cause: –Edema, dizziness, headache, depression, nausea, vomiting, diarrhea, increased appetite, increased weight, breast changes, many others

Contraceptive Drugs: Interactions Drugs that decrease effectiveness of oral contraceptive drugs –Antibiotics, barbiturates, isoniazid, rifampin, griseofulvin

Contraceptive Drugs: Interactions (cont’d) Drugs that may have reduced effectiveness if given with oral contraceptive drugs –Anticonvulsants, beta-blockers, hypoglycemic drugs, oral anticoagulants, theophylline, TCAs, vitamins, hypnotics

Osteoporosis Low bone mass Increased risk of fractures Primarily affects women 20% of those with this condition are men

Osteoporosis

Osteoporosis: Risk Factors –Caucasian/Asian descent –Slender body build –Early estrogen deficiency –Smoking –Alcohol consumption –Low-calcium diet –Sedentary lifestyle –Family history

Drug Therapy for Osteoporosis Calcium supplements and vitamin D may be recommended for women at high risk for osteoporosis

Drug Therapy for Osteoporosis (cont’d) –Bisphosphonates alendronate (Fosamax), ibandronate (Boniva), risedronate (Actonel) –Selective estrogen receptor modifier (SERM) raloxifene (Evista) –Hormone calcitonin teriparatide (Forteo)

Drug Therapy for Osteoporosis (cont’d) Biphosphonates Work by inhibiting osteoclast-mediated bone resorption, thus preventing bone loss SERMs Stimulate estrogen receptors on bone and increasing bone density

Drug Therapy for Osteoporosis (cont’d) calcitonin –Directly inhibits osteoclastic bone resorption teriparatide –Only drug that stimulates bone formation –Derivative of parathyroid hormone –Action similar to natural parathyroid hormone

Drug Therapy for Osteoporosis: Indications Bisphosphonates and calcitonin –Both prevention and treatment of osteoporosis –Biphosphanates also used for glucocorticoid-induced osteoporosis and Paget’s disease

Drug Therapy for Osteoporosis: Indications (cont’d) raloxifene –Prevention of postmenopausal osteoporosis teriparatide –Used for those with highest risk of fracture (prior history of fractures)

Drug Therapy for Osteoporosis Adverse Effects SERMs –Hot flashes, leg cramps –Can increase risk of venous thromboembolism –Not used if patient is near age of menopause due to possible hot flashes –Leukopenia

Drug Therapy for Osteoporosis Adverse Effects (cont’d) Bisphosphonates –Headache, GI upset, joint pain –Risk of esophageal burns if medication lodges in esophagus before reaching the stomach

Fertility Drugs Various medical techniques used to treat infertility Include: –in vitro fertilization –Medication therapy: ovulation stimulation

Fertility Drugs (cont’d) clomiphene (Clomid, others) –Nonsteroidal ovulation stimulant –Blocks estrogen receptors in the uterus and brain, resulting in a false signal of low estrogen levels

Fertility Drugs (cont’d) Clomiphene (Clomid, others) (cont’d) –Causes increased production of Gn-RH, FSH, and LH –As a result, maturation of ovarian follicles is stimulated, leading to ovulation and increased chance of conception

Fertility Drugs (cont’d) Mentropins (Pergonal) –Standardized mixture of FSH and LH –Stimulates development of ovarian follicles, leading to ovulation –May also be given to men to stimulate spermatogenesis

Fertility Drugs (cont’d) chorionic gonadotropin alfa (Ovidrel) –Recombinant form of human chorionic gonadotropin –Causes rupture and ovulation of mature ovarian follicles, and maintenance of corpus luteum –Used to stimulate ovulation

Fertility Drugs: Indications Used primarily to induce ovulation in anovulatory patients Also may be used to promote spermatogenesis in infertile men

Fertility Drugs: Adverse Effects Tachycardia, phlebitis, DVT Dizziness, headache, flushing, depression, anxiety, nervousness, fatigue Nausea, bloating, constipation, others Ovarian hyperstimulation, multiple pregnancies, blurred vision, breast pain, others

Uterine-Active Medications Medications used to alter uterine contractions Used to: –Promote labor –Prevent the start or progression of labor –Postpartum use: to reduce the risk of postpartum hemorrhage

Uterine Stimulants Also called oxytocics Ergot derivatives Prostaglandins Progesterone antagonist oxytocin (hormonal drug)

Uterine Stimulants (cont’d) Ergot alkaloids Increase force and frequency of uterine contractions Used after delivery of the infant and placenta to prevent postpartum uterine atony and hemorrhage methylergonovine (Methergine)

Uterine Stimulants (cont’d) Prostaglandins Natural hormones Cause potent contraction of myometrium, smooth muscle fibers of the uterus Used to induce labor by softening the cervix and enhancing uterine muscle tone dinoprostone (Prostin E 2 ) and misoprostol (Cytotec)

Uterine Stimulants (cont’d) Progesterone antagonist mifepristone (Mifeprex) RU-486, the “abortion pill” Stimulates uterine contractions to induce abortion Given with a prostaglandin drug for elective abortions

Uterine Stimulants: oxytocin (Pitocin)—Synthetic Form Used to induce labor at or near full-term gestation, and to enhance labor when contractions are weak and ineffective

Uterine Stimulants: oxytocin (Pitocin)—Synthetic Form (cont’d) Other uses –Prevent or control postpartum uterine bleeding –Complete an incomplete abortion (after miscarriage) –Promote milk ejection during lactation

Uterine Stimulants: Adverse Effects Hypotension or hypertension, chest pain Headache, dizziness, fainting Nausea, vomiting, diarrhea Vaginal pain, cramping Leg cramps, joint swelling, chills, fever, weakness, blurred vision

Uterine Relaxants: Tocolytics Used to stop labor that begins before term to prevent premature birth Generally used after the 20th week of gestation

Uterine Relaxants: Tocolytics (cont’d) Uterine contractions that occur between the 20th and 37th weeks of gestation are considered premature labor Nonpharmacologic measures –Bedrest, sedation, hydration

Uterine Relaxants ritodrine (Yutopar) and terbutaline (Brethine) –Beta-adrenergic drugs –Stimulation of beta 2 -adrenergic receptors on the uterine smooth muscle –Results in relaxation of the uterus, thus stopping premature contractions –“Off-label” use Magnesium sulfate IV also used to stop labor

Uterine Relaxants: Adverse Effects Palpitations, tachycardia, hypertension, others Tremors, anxiety, insomnia, headache, dizziness, others Nausea, vomiting, anorexia, bloating, diarrhea, constipation Hyperglycemia, hypokalemia Dyspnea, hyperventilation, others

Nursing Implications Assess baseline VS, weight, blood glucose levels, renal and liver function studies Assess whether the patient smokes Assess history and medication history Assess contraindications, including potential pregnancy

Nursing Implications (cont’d) Before giving any uterine stimulants, assess the mother’s vital signs and fetal heart rate Uterine relaxants are used when premature labor occurs between the 20th and 37th weeks of gestation

Nursing Implications (cont’d) For biphosphonates, ensure that the patient has no esophageal abnormalities and can remain upright or in a sitting position for 30 minutes after the dose

Nursing Implications (cont’d) Estrogens and progestins –Take the smallest dose needed –Give IM doses deep in large muscle masses, and rotate sites –Give oral doses with meals to reduce GI problems –Teach patient about correct self- administration and what to do if a dose is missed

Nursing Implications (cont’d) Estrogens and progestins (cont'd) –Increased susceptibility to sunburn may occur—advise patient to wear sunscreen or avoid sunlight –Patients should report weight gain –Annual follow-up exams should be completed, including PAP smear and breast exam

Nursing Implications (cont’d) Follow specific administration guidelines carefully for IV administration of uterine relaxants or stimulants Monitor the patient’s vital signs and fetal condition during therapy

Nursing Implications (cont’d) Instruct patient taking fertility drugs to take the medication as ordered Recommend the patient keep a journal while on fertility drugs

Nursing Implications (cont’d) Biphosphonates –Instruct patient to take medication upon rising in the morning, with a full glass of water, and 30 minutes before eating –Emphasize that the patient should sit upright for at least 30 minutes after taking the medication

Nursing Implications (cont’d) SERMs –Instruct patient that the medication will need to be discontinued 72 hours before and during any prolonged immobility (such as surgery or a long trip)

Nursing Implications (cont’d) Monitor for therapeutic responses Monitor for adverse effects