Reproductive System Medications

To promote female maturation

Primary action of estrogens and progestins

Estradiol

Principle endogenous estrogen:

Progesterone

Principle progestational hormone;

Positive effect: it decreases bone resorption. Keeps bone mass stable.

Estrogen’s effect on bone mass

increase of it in bloodstream, good for cholesterol

Effect of estrogen on HDL

Reduces it in blood stream, good for cholesterol

Effect of estrogen on LDL

Estrogen positive breast cancer

Breast cancer where estrogen speeds up growth

1. endometial hyperplasia and carcinoma

2. promotes growth of existing breast cancer

3. ovarian cancer

4. cardiovascular events

5. Other: jaundice, headache, chloasma, gallbladder disease

Adverse effects of estrogens: [5]

As menopausal hormone, can take away signs and symptoms of menopause

How is estrogen used therapeutically after menopause

1. menopausal hormone

2. female hypogonadism

3. acne

Therapeutic uses of estrogens: [3]

1. oral

2. transdermal

3. intravaginal

4. parenteral

Routes of administration for estrogens [4]

Selective estrogen receptor modulator (SERMs)

Activates estrogen in some tissues and blocks estrogen receptors selectively in others. Depending on the type of cancer, described as cancer blockers

1. tamoxifen

2. toremifene

3. raloxifene

Three available SERMs:

blocks estrogen receptors in the breast

Activates receptors in the endometrium

Tamoxifen MOA

Activates estrogen receptors in the endometrium.

How does tamoxifen increase risk of uterine cancer?

1. breast cancer treatment

2. protects against osteoporosis

Tamoxifen therapeutic uses: [2]

1. risk for endometrial cancer

2. risk for thromboembolism

3. produces hot flashes

Tamoxifen risks/ adverse effects: [3]

Raloxifene (evista)

Drug that acts like tamoxifen, but does not activate estrogen receptors in the endomerium

1. Individual high risk of breast cancer. Protects, does not treat

2. Diagnosis of osteoporosis.

Why would someone be prescribed raloxifene? [2]

Bone density scan

how to diagnose osteoporosis

1. strengthening exercises

2. diet (increased calcium and vitamin D

3. Drugs to decrease bone resorption

osteoporosis treatments: [3]

1. ralxifine

2. biphosphonates (ex: fosamax)

3. calcitonin

Drugs that decrease bone resorption [3]

It can irritate the esophagus

Why does fosamax need to be taken 30 minutes before a meal, and people need to stay sitting up?

Progestins

Compounds that act like progesterone

ovaries and placenta

Where are progestins produced? [2]

1. teratogenic effects

2. gynecologic effects

3. breast cancer

4. depression

5. breast tenderness

6. bloating

Adverse effects of progestins:[6]

hot flashes. Blood vessels dilate very quickly and patient gets very warm

Vasomotor symptoms of menopause

1. postmenopausal hormone therapy

2. dysnfnctional uterine bleeding

3. amenorrhea

4. infertility

5. prematurity prevention

6. endometrial carcinoma and hyperplasia

Therapeutic uses of progestins: [6]

Someone with diabetes at menopause can have sugars out of control due to hormone changes. Helps level out hormones and regulate blood sugars

How do progestins help with glycemic control after menopause?

assists with bone loss, altered lipid metabolism, sleep disturbances

Progestin menopausal hormone therapy benefits: [3]

1. cardiovascular events

2. endometrial cancer

3. breast cancer

4. ovarian cancer

5. galbladder disease

6. dementia

7. urinary incontinence

Menopausal hormone therapy risks: [7]

birth control

Interfering with the productive process at any step from gametogenesis to nidation

inhibits ovulation. no ovulation, no ova to be fertilized

Oral contraceptive MOA:

1. combination OCs (estrogen and progestin)

2. progestin-only “mini pills”

two main classifications of oral contraceptives

1. monophasic

2. biphasic

3. triphasic

Three major subgroups of combination OCs:

monophasic

combination OC with the same level of hormones the entire month

biphasic

combination OC with two different levels or hormones during the month

triphasic

combination OC that has three levels of hormones during the month. Mimics hormones throughout the menstrual cycle.

1. thromboembolic disorders

2. HTN

3. cancer

4. stroke in pts who get migraines

5. teratoenic effects

6. abnormal uterine bleeding

7. benign hepatic adenoma

8. glucose intolerance

Adverse effects of combination oral contraceptives: [8]

1. decreased risk of ovarian cancer, endometrial cancer ovarian cysts, PID, benign breast disease, iron defifiency anemia, and acne

2. Diminished cramps, lighter/predictable/shorter flow

Benefits of combination OCs: [2]

1. Rifampin (TB)

2. Ritonavir (HIV)

3. Antiepileptic drugs

4. st. John’s wort

Drugs and herbs that reduce the effects of OCs: [4]

1. warfarin

2. insulin

Drugs whos effects are DECREASED by OCs (speeds up their metabolism): [2]

1. Theophylline (asthma)

2. tricyclic antidepressants

3. diazepam

drugs whos effects are increased by OCs [3]

Does not cause theomboembolic disorders, headaaches, nausea, or most other adverse effects assciated with combination OCs. They are slightly safer

Benefit of progestin-only OC

1. breast

2. around ovaries

3. hairy places

Where should transdermal contraceptive patches NOt be placed? [3]

once a week for three weeks, followed by one week off to permit normal menstruation

Application of Ortho Evra

Nuvaring

Vaginal contraceptive ring that is placed for three weeks and removed for one

1. vaginitis

2. headaches

3. upper respiratory infection

4. sinusitis

5. weight gain

6. nausea

adverse effects of nuvaring: [6[

Subdermal etonogestrel implant (nexplanon)

Most effective contraceptive

irregular bleeding

adverse effect of nexplanon

Depot medroxyprogesterone acetate (MPA)

Birth control IM injection thaat protects against pregnancy for 3 month or longer

1. menstrual irregularities (no period)

2. bone loss

adverse effects of Depot medroxyprogesterone acetate (MPA) [2]

IUD.

Device that makes the uterus inhospitable.

Someone with multiple sexual partners. Risk of infection is already high due to a foreign body inside you. Multiple partners increases risk of infection.

who should not get an IUD?

1. Copper T 380A (ParaGard)

2. Levonorgestrel- releasing intrauterine system (Mirena)

Examples of IUDs: [2]

Mifepristone (RU 486) with misoprostol

drugs for medical abortion [2]

blocks uterine progesterone receptors

Mifepristone (RU 486) with misoprostol MOA

1. bleeding

2. cramping

3. nausea

4. vomiting

5. diarrhea

6. headache

adverse effects of Mifepristone (RU 486) with misoprostol

Testosterone

Major endogenous androgen

Androgens

produced by the testes, ovaries, and adrenal cortex. Promotes expression of male sex characteristics

management of androgen deficiency in males, especially if puberty is delayed

Primary clinical application of androgens

Virilization (development of sex characteristics) and hepatotoxicity

principle adverse effects of androgens [2]

1. pubertal transformation

2. spermatogenesis

Testosterone’s effects of sex characteristics in males: [2]

maintenance of normal libido

Testosterone’s effects of sex characteristics infemales:

testosterone helps with synthesis of erythropoeitin

Why do males have a higher hematocrit than women?

1. testosterone and testosterone esters

2. 17-alpha-alkylated compounds

two basic categories of androgens:

•Male hypogonadism

•Replacement therapy in menopausal women

•Delayed puberty

•Replacement therapy in menopausal women

•Wasting in patients with acquired immunodeficiency syndrome (AIDS)

•Anemias

therapeutic uses of androgens: [6]

○Virilization in women, girls, and boys

○Premature epiphyseal closure (end of long bones)

○Hepatotoxicity

○Effects on cholesterol levels (increased LDL)

○Use in pregnancy

○Increased growth of existing prostate cancer

○Edema (retention of salt and water)

○Abuse potential (athletic performance)

adverse effects of androgens:

fluoxymesterone

methyltestosterone

oral androgens: [2]

■Oral androgens: Fluoxymesterone and methyltestosterone

■Intramuscular testosterone esters

■Transdermal testosterone patches

■Transdermal testosterone gels

■Transdermal testosterone under arms

■Implantable subcutaneous testosterone pellets

■Testosterone buccal tablets

androgen preparations for male patients: [7]

erectile dysfunction, also known as impotence

Persistent inability to achieve or sustain an erection suitable for sexual intercourse

Phosphodiesterase type 5 inhibitors.

1. sidenafil

2. vardenafil

3. tadalafil

oral agents for treatment of ED: [3]

Papaverine plus phentolamine, and alprostadil

non-oral agents for ED treatment:

Sildenafil [Viagra]

ED drug that enhances normal erectile response in the presence of stimuli.

certain vasodilators (alpha-andrenergic blockers and nitrates)

Viagra can be dangerous when used with what?

•Hypotension

•Priapism

•Headache, dyspepsia, flushing, nasal congestion, diarrhea, rash, dizziness, mild transient visual disturbances, intensification of obstructive sleep apnea

•Rare side effects

• -arteritic ischemic optic neuropathy

• Sudden hearing loss

adverse side effects of viagra [5]

Priapism

sustained erection lasting longer than 4 hours. Is a medical emergency, can ose function if it lasts.

high fat meals

viagra absorption is slowed by what?

•Nitrates

• Could cause life-threatening hypotension

• 24 hours in between these medications for safety

•Alpha blockers (HTN meds)

• Can cause symptomatic postural hypotension

•Inhibitors of cytochrome P450 (CYP3A4)

• Can suppress metabolism of sildenafil

viagra drug interactions [3]

1. MI, stroke, dysrhythmia within past 6 months

2. resting hypotension

3. resting hypertension

4. heart failure

5. unstable angina

men with what conditions should use viagra with caution? [5]

Vardenafil (Levitra)

PDE5 inhibitor for ED that prolongs the QT interval

Tadalafil (Cialis)

PDE5 inhibitor for ED that lasts 36 hours

Avanafil (Stendra)

PDE5 inhibitor that has 15 minute onset

●Papaverine (smooth muscle relaxant) plus phentolamine (alpha-adrenergic blocking agent)

ED treatment that increases arterial blood flow and decreased venous outflow in the penis. Is injected directly into the corpus cavernosum

1. priapism

2. fibrotic nodules on corpus cavernosum

3. orthostatic hypotension with dizziness

adverse effects of Papaverine plus phentolamine

●Alprostadil (prostaglandin E₁₎

ED drug that increases arterial flow and decreases venous outflow in the penis. Should not be used more than 3 times per week or once in 24h

1. burning

2. prolonged erection

3. priapism

4. penile fibrosis

Adverse effects of ●Alprostadil (prostaglandin E_{1 {4]}

Benign Prostatic Hyperplasia

Nonmalignant prostate enlargement caused by growth of epithelial cells and smooth muscle cells.

Prostate specific antigen (PSA)

When prostate enlarges, produces more of this antigen

•Urinary hesitancy

•Urinary urgency

•Increased frequency of urination

•Dysuria

•Nocturia

•Straining to void

•Post-void dribbling

•Decreased force and caliber of urinary stream

•Sensation of incomplete bladder emptying

Signs and symptoms of benign prostatic hyperplasia [9]

1. surgery

2. watchful waiting drug therapy

Treatment for benign prostatic hyperplasia

1. mechanical (really large)

2. dynamic

two types of benign prostatic hyperplasia obstructions:

5-Alpha-reductase inhibitors

Drug treatment for benign prostatic hyperplasia mechanical obstruction

Alpha₁-adrenergic antagonists

Drug treatment for benign prostatic hyperplasia dynamic obstruction

inhibits 5-alpha-reductase. Most effective in patients with very large prostate

Finasteride (Proscar) MOA

1. decreases libido

2. gynecomastia

3. decreased PSA levels

Finasteride adverse effects [3]

1. Terazosin

2. Tamulosin

Alpha1-andrenergic antagonists that block receptors, relaxing smooth muscle of the bladder neck. Treatment for benign prostatic hyperplasia [2]

promotes vasodilation and can lower BP

Terazosin [Hytrin] effects on BP: