NR 566 Final Exam Study Guide: Week 5, 6, 7 & 8- Advanced Pharmacology for Care of the Family

566 Final Exam Study Guide

Week 5

 Prevention of osteoporosis with hormone replacement therapy

o Selective Estrogen Receptor Modulators (SERMs)

 Tamoxifen (Nolvadex-D), Toremifene (Fareston), Raloxifene (Evista),

and Bazedoxifene (Duavee - postmenopausal women drug)

 These drugs provide benefits of estrogen (protection against

osteoporosis, maintenance of the urogenital tract, reduction

of LDL cholesterol) while avoiding its drawbacks (promotion

of breast cancer, uterine cancer, and thromboembolism)

o Prevention of osteoporosis requires lifelong hormone replacement

 When stopped, bone loss decreases by 12%.

 LIfelong treatment increases health risks.

o All women (and men) should practice primary prevention of bone loss by

ensuring adequate intake of calcium and vitamin D, performing regular

weight-bearing exercise, and avoiding smoking and excessive alcohol use.

- When and when not to use progestin for hormone replacement therapy and why -

 When To Use:

o Menopausal Hormone Therapy

 Counteracts adverse effects of estrogen on endometrium in women

undergoing menopausal hormone therapy.

o Dysfunctional Uterine Bleeding

 Cessation of bleeding can be achieved with 10-14 day treatment.

 Withdrawal bleeding can take place when treatment stops.

o Amenorrhea

 Progestin helps induce menstrual flow in select women experiencing

amenorrhea.

 If endogenous estrogen levels are normal, give progestin for 5-10

days.

 If estrogen levels are low, need to induce endometrial proliferation

with estrogen before giving progestin.

o Endometrial Hyperplasia and Carcinoma

 Can provide palliation in women with metastatic endometrial

carcinoma - do not prolong life.

 Only approved long-term progestin therapy is for protection against

endometrial cancer.

 Progestin can suppress endometrial hyperplasia - a potentially

precancerous condition

o Help Support early pregnancy with the corpus luteum deficiency syndrome

and in women undergoing IVF.

o Hydroxyprogesterone Acetate (Makena) - helps prevent preterm birth.

 When Not To Use (Contraindications):

o Absolute Contraindications

 Undiagnosed abnormal vaginal bleeding.

o Relative Contraindications

 Active Thrombophlebitis

 Hx of thromboembolic disorders

 Active Liver Disease

 Carcinoma of the breast

o Do Not Use:

 Prepubertal Children

 High-dose therapy in first 4 months of pregnancy (birth defects)

Local vs. systemic estrogen options and why one would be chosen over the other -

 Systemic Options

o Oral

 Most active estrogenic compound - ESTRADIOL

 Estradiol is available alone or in combination with

progestins

 Popular because of its convenience.

o Transdermal

 Four Formulations

 Emulsion (Estrasorb), Spray (Evamist), Gels

(EstroGel, Elestrin, and Divigel)

 Four Advantages Over Oral Formulations:

 The total dose of estrogen is greatly reduced

(because the liver is bypassed).

 There is less nausea and vomiting.

 Blood levels of estrogen fluctuate less.

 There is a lower risk for DVT, pulmonary embolism,

and stroke.

o Intravaginal

 Femring

 Control hot flashes and night sweats as well as local

effects (treatment of vulval and vagnial atrophy).

o Parental

 IV and IM administrations - use of these routes are rare.

 Used in acute, emergency control of heavy uterine

bleeding.

 Local Options

o Intravaginal

 Primarily treatment for vulvar and vaginal atrophy associated

with menopause.

 Available as inserts, creams, and vaginal rings

 Intravaginal Inserts - Imvexxy, Vagifem, and Yuvafem

 Creams - Estrace Vaginal, Premarin Vaginal

 Rings - Estring (other vaginal ring, Femring, is

systemic effects)

Transdermal estrogen therapy has fewer adverse effects.

- Management of oral contraceptives (OCs)

o How to change patients from one combination oral contraceptive to another.

 Go straight from one type to the other, without taking a gap in between. Start the

new pill the day after taking the last active pill in the last pill packet. This also applies

with 'placebo' pills.

o “No gap method”

o How to initiate treatment (when in the cycle is it best to start- may vary based on

type of contraceptive)

 OCs: The sequence begins on either the first day of the menstrual cycle or the

first Sunday after the onset of menses. With the first option, protection is

conferred immediately; hence no backup contraception is needed. With a

Sunday start, which is done to have menses occur on weekdays rather than the

weekend, protection may not be immediate; hence an alternate form of birth

control should be used during the first 7 days of the pill pack.

o What teaching needs to be done

 Educate pts on proper protocol for missed dose

 Women should be informed about the symptoms of thrombosis and

thromboembolism (e.g., leg tenderness or pain, sudden chest pain, shortness

of breath, severe headache, sudden visual disturbance) and instructed to

consult the prescriber if these occur.

o What baseline data is needed?

 Assess for hx of HTN, diabetes, thromboembolism, cerebrovascular or cardiovascular

disease, breast CA. Urine pregnancy test.

o Contraindications for OCs

 Pregnancy, history of thromboembolism, breast cancer, and women over 35 years of

age who continue to smoke tobacco.

 Use with caution in women with diabetes, hypertension, and cardiac disease.

- How to achieve an extended cycle with oral contraceptives

 To achieve an extended schedule cycle, the user would simply purchase four packets of a 28-

day product (each of which contains 21 active pills) and then take the active pills for 84 days

straight.

- What behaviors would make one birth control method more effective over another?

Family planning goals, age, frequency of intercourse, Pt capacity for

adherence.

oBe able to evaluate a patient scenario and suggest an appropriate birth control

method (type of prescribed contraception: OC, long-term methods, IUD, etc).

- What effect does CYP450 inhibitors or inducers have on OCs?

o Recall examples of CYP450 inhibitors and inducers from NR565 (Chapter 4 in

textbook)

 Inhibitors: Valproate, Isoniazid, Sulfonamides, Amiodarone, Chloramphenicol,

Ketoconazole, Grapefruit Juice, Quinidine

 Inducers: Carbamazepine, Rifampin, Alcohol, Phenytoin, Griseofulvin,

Phenobarbital, Sulfonylureas

o How does this impact prescribing of OCs?

 Women taking OCs in combination with any CYP450 inducers and inhibitors should be

alert for indications of reduced OC blood levels, such as breakthrough bleeding or

spotting.

o If these signs appear, it may be necessary to either:

 (1) increase the estrogen dosage of the OC

 (2) combine the OC with a second form of birth control (e.g., condom)

 (3) switch to an alternative form of birth control

- Benefits and drawbacks of progestin-only contraception

 Benefits: Do not cause thromboembolic disorders, headaches, nausea, or most of the other

adverse effects associated with combination OCs

 Drawbacks: Less effective and are more likely to cause irregular bleeding (breakthrough

bleeding, spotting, amenorrhea, inconsistent cycle length, variations in the volume and

duration of monthly flow). Irregular bleeding is the major drawback of these products and the

principal reason that women discontinue them.

- What are the most effective forms of contraception?

 Etonogestrel subdermal implant

o Nexplanon

 Surgical sterilization

o Male: Vasectomy

o Female: Tubal ligation

 IUD

o Copper T 380A (ParaGard)

o Levonorgestrel T (Mirena)

- Testosterone replacement

o Administration

 Transdermal Patches - male hypogonadism

o Applied daily to the upper arm, back, or abdomen.

 Testosterone gel is also available.

o Patient Teaching

 Transdermal patches:

o good hand washing is required after application

o cover application site with clothing after medication has dried

o wash the application site before skin-to-skin contact with another

person

 females and children may experience negative effects from

exposure to testosterone

 if cross contamination occurs, wash the affected area with

soap and water to prevent absorption

- Treatment of delayed puberty

o When is it appropriate to initiate androgen therapy (short course and long-term)

 Short term: The psychologic pressures of delayed sexual maturation are causing a boy

significant distress. In these cases, a limited course of androgen therapy is indicated.

o Both fluoxymesterone (Androxy, Halotestin) and methyltestosterone (Methitest) are

approved for this purpose.

 Long term: If delayed puberty is the result of true hypogonadism

- Androgen therapy

o Effects

▪ Therapeutic

 Manage hypogonadism and subsequent testosterone deficiency through

testosterone supplementation

▪ Adverse

 Virilization in women, girls, and boys

 Premature Epiphyseal Closure

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