NR 566 Final Study Guide. Advanced Pharmacology for Care of the Family – Chamberlain University. Graded A+

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Week 1 Ch 50 estrogen and progestins - ✔✔ Menopause 1. is the associated loss of estrogen which typically begins 2. During the initial phase, the menstrual cycle becomes 3. Eventually, ov... ulation and menstruation - ✔✔1. at approximately age 51 to 52 years, with 95% of women entering menopause between the ages of 45 and 55 years. 2. irregular, anovulatory cycles may occur, and periods of amenorrhea may alternate with menses 3. cease entirely Physiologic Alterations Accompanying Menopause 1. Vasomotor Symptoms; hot flashes and night sweats) develop in approximately 2. Genitourinary Syndrome of Menopause; the urethra and vagina have the highest 3. Mental Changes; Many women report 4. Bone Loss; In the absence of estrogen, bone resorption accelerates, leading 5. Altered Lipid Metabolism; studies have shown increases in 6. Female Sexual Interest-Arousal Disorder - ✔✔1. 70% of postmenopausal women. Episodes are characterized by sudden skin flushing, sweating, and a sensation of uncomfortable warmth. These episodes can occur at night, resulting in drenching sweats 2. concentrations of ERs; when estrogen levels decline during menopause, these structures begin to atrophy resulting in urge incontinence and urinary frequency; Urethritis and UTIs can also occur 3. cognitive changes such as difficulty in problem solving and short-term memory loss. Others experience depression or an increase in anxiety 4. to a 12% loss of bone density leading to Osteoporosis which can cause compression fractures of the vertebrae causing a decrease in height and produce a hump. In osteoporotic women, fractures of the hip and wrist can result from minimal trauma 5. LDL cholesterol & decreases in HDL cholesterol. which play a role in the increase in CV disease after menopause. 6. more common during this stage of life Estrogen Therapeutic Uses: 1. Menopausal hormone therapy- When estrogen is used for this purpose, 2. Female hypogonadism-In the absence of ovarian estrogens, 3. Acne-Estrogens, in the form of 4. Cancer palliation-sometimes used for palliative therapy 5. Gender-affirmation therapy-for - ✔✔1. it is usually accompanied by the use of progestins 2. pubertal transformation will not take place. (variety of causes see pg 428) This treatment promotes breast development, maturation of the reproductive organs, and pubic and axillary hair. This tx regimen consists of continuous low-dose therapy (for approx a year) followed by cyclic administration of estrogen in higher doses 3. oral contraceptives, can help control acne. Tx is limited to patients at least 14-15 years old who want contraception 4. in management of advanced prostate CA in men and in a select type of metastatic breast CA in men& women 5. transgender women; not approved by the FDA) but prescribed off-label Forms of Estrogen 1. Estrogen is available in conjugated and esterified forms. Esterified estrogens 2. Until mid-2016, synthetic conjugated estrogens A (Cenestin) and B (Enjuvia) were available; however, 3. Phytoestrogens (plant-based compounds)-commonly used by women as a 4. Phytoestrogens are not as potent as estradiol, but they carry some of the same risks. 5. Selective estrogen receptor modulators (SERMs) are drugs that activate ERs in some tissues and block them in others. These drugs were developed in an effort - ✔✔1. are plant based; conjugated estrogens are natural preparations derived from the urine of pregnant horses. 2. the manufacturer has withdrawn them from the market 3. "natural" way to manage symptoms associated with menopause 4. Women should not use phytoestrogens if they have a history of thromboembolic events or a personal or family history of breast, uterine, or ovarian cancer. 5. to provide the benefits of estrogen (e.g., protection against osteoporosis, maintenance of the urogenital tract, reduction of LDL cholesterol) while avoiding its drawbacks (e.g., promotion of breast cancer, uterine cancer, and thromboembolism) Estrogen-Adverse Effects 1. principal concerns with estrogen therapy are the potential for 2. endometrial hyperplasia and endometrial cancer can be resolved 3. Estrogens have been associated with what common SE 4. menopause may produce or uncover 5. Nausea is the most 6. (blank) a patchy brown facial discoloration, though not dangerous, may cause significant distress - ✔✔1. endometrial hyperplasia, endometrial cancer, breast cancer, and cardiovascular thromboembolic events 2. by prescribing a progestin 3. Fluid retention with edema, gallbladder disease, jaundice, and headache; especially migraine headache 4. gallbladder disease. Jaundice may develop in women with preexisting liver dysfunction, especially those who experienced cholestatic jaundice of pregnancy 5. frequent undesired response to the estrogens 6. Chloasma, Contraindications of Estrogen 1. Estrogens should not be taken by patients with a history of 2. They should not be prescribed to women who 3. Patients with a hx of - ✔✔1. DVT, pulmonary embolus, or conditions such as stroke or MI that occurred secondary to a thromboembolic event. 2. are pregnant or who have vaginal bleeding without a known cause. 3. liver disease, estrogen-dependent tumors, or breast cancer (except when indicated for management) also should not take estrogens. Estrogen-Interactions 1. Estrogens are major substrates of 2. In addition, they may decrease the effectiveness of some 3. Estrogens can also interact with - ✔✔1. CYP1A2 and CYP3A4; inducers/inhibitors of these isoenzymes may raise/lower estrogen levels 2. antidiabetic drugs and thyroid preparations. 3. anticoagulants and other drugs that affect clotting. Local vs. systemic estrogen options and why one would be chosen over the other 1. Oral-Owing to convenience, the oral route is used 2. Transdermal estradiol is available in four formulations: 3. Compared with oral formulations, transdermal formulations have four advantages: 4. Intravaginal options come as inserts, creams, and vaginal rings & 5. The other vaginal ring (Femring) is used for systemic effects to 6. Parenteral; is used only for emergencies d/t - ✔✔1. more than any other. estradiol—is available alone and in combination with progestin 2. Emulsion (Estrasorb), Spray, Gels & Patches 3a. The total dose of estrogen is greatly reduced 3b. There is less nausea and vomiting. 3c. Blood levels of estrogen fluctuate less. 3d. There is a lower risk for DVT, pulmonary embolism, and stroke. 4. are used only for local effects, primarily treatment of vulval and vaginal atrophy associated with menopause. 5. control of hot flashes and night sweats as well as local effects-Tx of vulval and vaginal atrophy 6. acute, emergency control of heavy uterine bleeding Clinical Practice Guidelines for menopause Not all women who experience distressing symptoms of menopause should be treated with oral estrogen or combination estrogen/progestin therapy. Key points include: 1. intravaginal preparations are most useful for treating sx associated 2. transdermal estrogen preparations have fewer adverse effects, use lower doses of estrogen, and have 3. progesterone is contraindicated in women who have undergone a - ✔✔1. with local estrogen deficiency such as vaginal and vulvar atrophy; these preparations are assoc with a lower risk of systemic effects 2. less fluctuation of estrogen levels than do oral preparations 3. hysterectomy but required in women with an intact uterus who undergone hormone replacement therapy Summary of Key Prescribing Considerations -Estrogens 1. Therapeutic Goal: Management of symptoms and structural changes associated 2. Baseline Data: Heart rate, blood pressure, weight. Pregnancy test, thyroid-stimulating hormone (TSH), & 3. Monitoring: Blood pressure, weight. Serum triglycerides, TSH if thyroid replacement required, & 4. Identifying High-Risk Patients: Estrogen therapy should not be prescribed for patients with: 5. Evaluating Therapeutic Effects: Therapeutic effects depend on the reason prescribed. - ✔✔1. with decreased endogenous estrogen. (Other uses include palliation of metastatic breast cancer in selected cases.) 2. serum triglyceride (or full lipid panel). Screening for breast CA and CV disease. Gynecologic exam, if indicated. 3. Regular breast and pelvic exams as recommended for age. Schedule endometrial biopsy for unscheduled bleeding that continues for 6 months. 4. Abnormal vaginal bleeding of unknown cause • Estrogen-dependent cancer or breast cancer (except when used as treatment for certain metastatic cancers) • History of DVT or pulmonary embolism • Stroke, MI, or other arterial thromboembolism occurring within the past year • Abnormal liver function or disease • Pregnancy 5. For menopausal HT, patients report relief of symptoms and the vagina is pink and moist on gynecologic exam. 6. Minimizing Adverse Effects of Estrogen: • Nausea is common early in treatment. Advise patients that this adverse effect - ✔✔6. diminishes with time. In the meantime, avoidance of cooking odors and warm, stuffy environments may help. Dry foods and raw fruits and vegetables help as well as Guided imagery with muscle relaxation, yoga, and music therapy • Menopausal HT with estrogen alone increases the risk for endometrial carcinoma. Adding a progestin lowers this risk to the pretreatment level. • Adverse effects similar to those caused by OCs (abnormal vaginal bleeding, hypertension, benign hepatic adenoma, reduced glucose tolerance) Black Box Warning for Estrogen Therapy 1. Endometrial cancer risk is increased in women with a 2. Estrogen may increase the risk for 3. Estrogen is not indicated for - ✔✔1. uterus who take unopposed estrogen. 2. deep vein thrombosis and stroke. 3. cardiovascular disease or dementia and may increase the risk for dementia in women aged 65 years and older. Patient Education Estrogens From textbook 1. Inform the patient that nausea can be reduced by 2. Remind patients that estrogens present a small risk of 3. To minimize risk of undetected breast cancer, remind patients of the need to receive 4. To reduce cardiovascular risk, advise women to avoid smoking, perform regular exercise, - ✔✔1. taking estrogens with food and by dosing at night. Explain that nausea diminishes over time. 2. breast cancer and endometrial cancer. 3. periodic mammograms. Instruct the patient to report any persistent or recurrent vaginal bleeding, to r/o endometrial carcinoma 4. decrease intake of saturated fats, and take appropriate drugs for HTN, DM, and high cholesterol Patient-Centered Care Across The Life Span Estrogens 1. Children 2. Pregnant women 3. Breastfeeding women 4. Older adults-Beers Criteria include estrogens among - ✔✔1. Estrogens are not indicated for prepubertal children. 2. Estrogens are contraindicated during pregnancy. 3. Estrogens may affect infant development and may decrease both the quantity and quality of milk produced. 4. those identified as potentially inappropriate for use in geriatric patients. >65 (may increase dementia risk) Patient Education about Estrogen SE from lecture 1. Nausea is common early in treatment but. 2. Menopausal HT with this hormone alone increases the risk for . 3. adverse effects include abnormal - ✔✔1. diminishes with time. To reduce nausea: avoid cooking odors and warm, stuffy environments, consume dry foods and raw fruits and vegetables, use guided imagery with muscle relaxation, yoga, and music therapy 2. endometrial carcinoma 3. vaginal bleeding, hypertension, benign hepatic adenoma, and reduced glucose tolerance) Summary of Key Prescribing Considerations-Progestins 1. Therapeutic Goal: Goals for noncontraceptive uses are to counteract 2. Baseline Data: Heart rate, blood pressure, and weight. 3. Monitoring: Blood pressure. Assessment for fluid retention, including weight. Consider referral for 4. Identifying High-Risk Patients: Progestins are contraindicated in the presence of 5. Minimizing Adverse Effects: Progestins can cause breakthrough bleeding, spotting, and amenorrhea. Warn patients that - ✔✔1a. endometrial hyperplasia caused by unopposed estrogen during HR 1b. management of dysfunctional uterine bleeding, amenorrhea, and endometriosis 1c. support of pregnancy in women with corpus luteum deficiency & also used in in vitro fertilization cycles and to prevent risk for preterm birth. 2. Pregnancy test. Screening for breast and cardiovascular disease. Pelvic exam as indicated for age. 3. transvaginal ultrasound or hysteroscopy for occurrence of undx'ed bleeding for >6 months. 4. undx'ed vaginal bleeding, active thrombophlebitis or a hx of thromboembolic disorders, active liver disease, breast CA & women who've had a hysterectomy 5. this may occur, and instruct them to report any abnormal or prolonged vaginal bleeding. Black Box Warning Estrogen and Progestin Therapy 1. Estrogen plus progestin may increase the risk for 2. Estrogen plus progestin is not indicated for 3. Estrogen plus progestin may increase the risk for - ✔✔1. thromboembolic events such as DVT, stroke, myocardial infarction, and pulmonary embolism. 2. CV disease or dementia and may increase the risk for dementia in women aged 65 years and older. 3. breast cancer Patient-Centered Care Across The Life Span Progestins 1. Children 2. Pregnant women-High-dose therapy during the first 4 months of pregnancy has been associated 3. Breastfeeding women 4. Older adults-Progestins are only indicated if the patient is taking - ✔✔1. Progestins are not indicated for prepubertal children. 2. with an increased incidence of birth defects (limb reductions, heart defects, masculinization of the female fetus). 3. Progestins may contribute to neonatal jaundice. 4. estrogen and has a uterus. Transgender Woman (male phenotype) HT 1. Goals 2. Treatment 3. Monitoring needs 4. Risks - ✔✔1. Stimulate dev of female secondary sex characteristics; requires medication to decrease testosterone levels 2. estrogen, antiandrogens, gonadotropin-releasing hormone (GnRH) agonists, or others 3. Estradiol, Testosterone, Prolactin, Triglycerides & Potassium if spironolactone used as antiandrogen 4. HT risks are the same as for HR pts. For estrogen, thromboembolic events remain the greatest risk factor Patient Education about Progestin SE from lecture 1. breakthrough (blank, blank & blank) may occur 2. report abnormal or - ✔✔1. bleeding, spotting, and amenorrhea 2. prolonged vaginal bleeding >6mo Transgender Man (female phenotype) HT 1. Goals 2. Treatment 3. Monitoring needs 4. Risks - ✔✔1. Stop menstruation, Stimulate development of male secondary sex characteristics 2. testosterone as would be done in hypogonadism 3. Serum testosterone levels every 3 months until optimal, then 1-2 times a year, Hb/Hct, cholesterol 4. Acne, possible male-pattern hair loss, Polycythemia Hypercholesterolemia, Liver impairmentThromboembolic disorders with increased risk of MI and stroke Selecting the Right Birth Control method 1. Effectiveness 2. Safety 3. Personal Preferences 4. Other Factors - ✔✔1. Most Effective are subdermal implants, Intramuscular medroxyprogesterone acetate (Depo-Provera), Sterilization & Intrauterine device (IUD) - Reasonably effective are: Oral contraceptives (OC), Contraceptive ring, & Contraceptive Patch 2. OC contraindications: thrombus concerns, >35 years who smokers, & those with hx of breast carcinoma - OCs can cause significant side effects & Benefit/Risk analysis required 3. Improves consistent and correct use, Education increases consistent and correct use 4. Family planning goals, Age, Frequency of sexual activity Capacity for adherence - cost -access - developmental What behaviors would make one birth control method more effective over another? 1. personal preference is a major factor in providing the motivation needed for consistent implementation of a birth control method. 2. If family planning goals have already been met 3. For women who engage in coitus frequently, 4. Conversely, when sexual activity is limited, 5. Because barrier methods combined with spermicides can offer some protection against STDs 6. If adherence is a problem (as it can be with OCs, condoms, and diaphragms), - ✔✔1a. even the best form of contraception will be less effective if improperly practiced, 1b. Practitioners should take pains to educate patients about the contraceptive methods available so that selection and use can be based on understanding 2. sterilization of either the male or female partner may be desirable. 3. OCs or a long-term method (e.g., Nexplanon, Depo-Provera, IUD) are reasonable choices 4. use of a spermicide, condom, or diaphragm may be more appropriate. 5. these combinations may be of special benefit to individuals who have multiple partners. 6. use of a long-term method (e.g., vaginal contraceptive ring, IUD, Nexplanon, Depo-Provera) can confer more reliable protection. Factors to consider when selecting birth control-Diagram - ✔✔ Prototype Drugs Drugs for Birth Control 1. Combination Oral Contraceptive 2. Progestin-Only Oral Contraceptive 3. Long-Acting Contraceptives - ✔✔1. Ethinyl estradiol/norethindrone 2. Norethindrone-aka "minipills" 3. Subdermal etonogestrel implant (Nexplanon), Depot medroxyprogesterone acetate (Depo-Provera) Mechanism of Action of OC 1. Combination OCs reduce fertility primarily 2. The estrogen in combination OCs suppresses, 3. progestin in combination OCs acts in the - ✔✔1. by inhibiting ovulation. 2. release of FSH from the pituitary (and thereby inhibits follicular maturation) 3. hypothalamus and pituitary to suppress the midcycle luteinizing hormone surge, which normally triggers ovulation Summary of Key Prescribing Considerations Combination Oral Contraceptives 1. Therapeutic Goal: 2. Baseline Data: Assess for 3. Monitoring: 4. Identifying High-Risk Patients: Contraindications to use include 5. Evaluating Therapeutic Effects: If combination oral contraceptives are being used for menstrual symptoms, 6a. Minimizing Adverse Effects: Educate patients on proper protocol for missed doses 6b. Effectiveness of oral contraceptives can be reduced with - ✔✔1. Prevention of unwanted pregnancy. 2. hx of HTN, DM, thromboembolism, cerebrovascular or cardiovascular disease, breast CA. UA pregnancy test 3. No routine monitoring required. 4. current pregnancy, hx of thromboembolus, breast CA, and women over 35 years of age who continue to smoke tobacco. Use with caution in women with diabetes, hypertension, and cardiac disease. 5. it is important to evaluate for decrease in cramping, menstrual flow, or duration of menses. 6a. (depending on medication type and cycle). 6b. some medications, including certain common antibiotics. Baseline assessment Considerations for OCs 1. If the history reveals an absolute contraindication to OC use 2. In women with relative contraindications 3. A full examination with pelvic exam is Some states in the United 4. States are allowing pharmacists to - ✔✔1. OCs should not be prescribed. 2. OCs should be used with caution. 3. not needed to prescribe OCs. 4. prescribe OCs, thus eliminating the need for a healthcare visit. Absolute Contraindications to the Use of Combination Oral Contraceptives - ✔✔1. Thrombophlebitis, thromboembolic disorders, cerebral vascular disease, coronary occlusion, or a past history of these conditions, or a predisposition 2. Abnormal liver function 3. Known or suspected breast cancer 4. Undiagnosed abnormal vaginal bleeding 5. Known or suspected pregnancy 6. Smokers older than 35 years Relative Contraindications to the Use of Combination Oral Contraceptives - ✔✔Hypertension Cardiac disease Diabetes History of cholestatic jaundice of pregnancy Gallbladder disease Uterine leiomyoma Epilepsy Migraine SE of OCs- Thromboembolic disorders. 1. Major factors that increase the risk for thromboembolism are 2. Several measures can help minimize thromboembolic phenomena: 2a. The estrogen dose in OCs should be 2b. OCs containing drospirenone or desogestrel should 2c. OCs should not be prescribed for 2d. OCs should be discontinued at least - ✔✔1. heavy smoking, a history of thromboembolism, and thrombophilias 2a. no greater than required for contraceptive efficacy. In past hx OCs contained 100 µg of ethinyl estradiol Today's OCs contain no more than 50 µg 2b. generally be avoided because they may pose a higher risk for developing VTE. 2c. heavy smokers, women with a history of thromboembolism, or those with other risk factors for thrombosis. 2d. 4 weeks before surgery in which postoperative thrombosis might be expected. Patient Education-Thrombosis and Thromboembolism 1. Women should be informed about the symptoms of thrombosis and thromboembolism (e.g.,.... Black Box Warning-Oral Contraceptive Pills 2. Cigarette smoking increases the risk of - ✔✔1. leg tenderness or pain, sudden chest pain, shortness of breath, severe headache, sudden visual disturbance) and instructed to consult the prescriber if these occur. 2. serious cardiovascular side effects from combination oral contraceptive pills. SE of OCs- Cancer. 1. OCs present no known risk for cancer—with the important exception of 2. OCs protect against (blank & blank) CA and have no effect on (blank), which is caused by human papillomaviruses. 3. OCs do increase risk of breast CA for some women, specifically 4. estrogens can promote the growth of - ✔✔1. promoting (not causing) breast cancer growth 2. ovarian and endometrial; cervical cancer 3. women who have the BRCA1 gene mutation BUT not the BRCA2 mutation 4. existing breast carcinoma; which is why this is a absolute contraindication SE of OCs-Hypertension 1/2. f hypertension develops and OCs are determined to be the cause, two options are open: [Show More]

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