Women and Men's Health

Question 1

Estrogen

Answer 1

Estrogen is highly present in days 1-14 of menstrual cycle (follicular phase), helping increase levels for egg release

DRUG NAMES: estradiol (one human body uses), ethynyl

Question 2

Estrogen MOA

Answer 2

MOA: Binds to estrogen receptors (intranuclear) and regulates gene expression

Uses: contraception, uses commonly with progestin
- osteoporosis, acne, menorrhagia

Routs: oral, transdermal, IV, parenteral

Question 3

Progestin

Answer 3

progesterone
-Highly present in days 14-28 of menstrual cycle (luteal phase) to prepare body for pregnancy

Used for:
contraception (alone or in combo with estrogen)
-combination with estrogen post menopause

Question 4

Progestin Drugs (5)

Answer 4

medroxyprogesterone [Provera]
norgestrel [Ovrette]
norethindrone [Camilla]
drospirenone [Yaz]
lovonorgestrel [Seasonal]

Question 5

Oral Contreceptives (OC)

Answer 5

MOA: inhibits ovulation, underlying mechanism unknown

Question 6

Classifications of OC’s (2)

Answer 6

progestin-only OC’s (minipills)
combination OC’s (COCs)

Question 7

OC’s AE

Answer 7

N/V
DVT
HTN
headache
weight gain
depression
cancers

Question 8

OC’s Drug Interactions

Answer 8

antibiotics, HIV drugs, antiepileptic drugs (phenytoin, carbamazepine), smoking, St Johns Wart

Drugs whose effects are increased by OCs: theophylline and imipramine

Drugs whose effects are decreased by OCs: warfarin

Question 9

Yaz and Yazmin (ethinyl estradiol + drospirenone)*

Answer 9

newer synthetic progestin with anti-mineralocorticoid activity

AE: Same AE of OC, increased risk of blood clots, hyperkalemia

Indicated for:
-Oral contraception
-treatment of moderate acne
-Symptoms of PREMENSTRUAL DYSPHORIC DISORDER

Question 10

OC’s extended cycle

Answer 10

ethinyl estradiol/levonorgestrel [Seasonique*,seasonale] - 3 mo.

ethinyl estradiol/levonorgestrel [Lybel] - 12 mo.

Question 11

Combination contraceptives w/novel delivery systems (2)

Answer 11

transdermal contraceptive patch [Ortho-eva] = ethinylestradiol + norelgestromin
vaginal contraceptive ring [Nuvaring] = ethinylestradiol + etonogestrel

Question 12

Long acting contraceptives

Answer 12

contain progestin only

Drugs: depot medroxyprogesterone acetate (MPA)- IM, subq

IUD device:
-Levonorgesterl releasing intrauterine system [Mirena] *

AE: increased risk of HTN, increased risk of blood clots, birth defects, thromboembolism,

Question 13

Emergency contraception (EC)

Answer 13

MOA: may prevent ovulation but effectiveness late in cycle suggests other mechanisms

Plan B One Step:
-PROGESTIN ONLY: levonorgesterl 1.5mg as a single dose
-Administer within 72 hours of intercourse

2-dose regimen:
-2 doses of 0.75mg levonorgestrel separated by 12 hours
-First dose within 72hr, 2nd dose 12h after

Question 14

Drug for Medical Abortion

Answer 14

Mifepristone (RU486) [Mifeprex]

MOA: partial agonist of progesterone receptor -> blocks uterine progesterone receptors -> detachment of the conceptus -> terminate pregnancy

AE: vaginal bleeding, abd. pain, N/V, diarrhea, headache

Question 15

Drug that promote follicular maturation

Answer 15

Clomiphene citrate [Clomid]

MOA: partial agonist of of estrogen R -> blocks estrogens R -> inhibit feedback effect of estrogen on pituitary gland -> increase secretion of FSH and LH which stimulate ovary -> promote follicular maturation and possibly ovulation

AE: hot flushes, N/V, breast engorgement, 10% multiple births (twins)

Question 16

Drug that stimulate ovulation

Answer 16

Human chorionic gonadotrophin (hHCG) [Pregnyl, Novarel]

MOA: promote follicular maturation and ovulation
uses: infertility therapy due to anovulation

AE: ovarian hyperstimulation syndrome, multiple births

Question 17

Alternatives for HT for women w/multiple risk factors

Answer 17

phytotherapy: black cohosh
Paroxetine [Brisdelle]

Question 18

Drug for Hormone Therapy

Answer 18

conjugated estrogens (peramin)
- can be used in combinations w/medroxyprogesterone MDP [Provera]

estradiol micronised [Estrace], transdermal therapy estradiol [Vivell-Dot]

estrogen/progestin combo (estradiol + norethindrone) [Activella]

Question 19

HT- Regimen

Answer 19

Continuous: estrogen + progestin administered continuously (no monthly bleeding)

Sequential: estrogen from day 1-28 and progestin added on days 14-28 (for monthly bleeding)

Question 20

HT and Menopause

Answer 20

Hormonal therapy can be used to decrease symptoms, prevent osteoperosis and fractures, and prevent colorectal cancer

AE of therapy include: CV events (MI, stroke, PE, DVT), breast cancer, ovarian cancer, urinary incontinence

When used in combination with progestin, there is a decreased risk of endometrial cancer than using JUST estrogen alone

DO NOT GIVE IN:
-Undiagnosed vaginal bleeding, anything with blood clots, breast cancer, migraine, etc

Question 21

Calcium and Vitamin D

Answer 21

Calcium carbonate -> has higher elemental calcium, has acid-dependent absorption (take with OJ), can be taken with or with Vitamin D

Calcium citrate - better absorption but less elemental calcium.

cholecalciferol -> vitamin D3, taken with Ca+

Ca+ needs Vit. D for absorption - D3 (cholecalciferol)

Question 22

Antiresorptive therapy

Answer 22

drugs that reduce bone resorption

Bisphosphonates -> first line in most patients
MOA: kills osteoclasts (which break down bone) -> increase bone mineral density more than estrogens and raloxifene

Drugs: alendronate [Fosamax], ibandronate [Boniva]

AE: hypocalcemia, back pain, take on empty stomach, N/V, heartburn, ulcers

Question 23

Antiresorptive therapy II

Answer 23

Estrogen [Premarin] (no longer used)

raloxifene [Evista]

denosumab [Prolia] - monoclonal antibody that binds to RANKL and prevents osteoclast formation -> decreased bone resorption -> increase in bone mass

Question 24

Bone forming therapy

Answer 24

Drugs that promote bone formation

Teriparatide [Forteo] - recombinant human PTH, for patients at high risk of fracture
MOA: increase activity of osteoblast and decrease osteoclast

AE: ortho hypotension
BBW: osteosarcoma

Question 25

Androgens

Answer 25

Testosterone - management of androgen deficiency in males

Oxandrolone - treatment of muscle mass loss in AIDS patients

Question 26

Erectile Dysfunction

Answer 26

phosphodiesterase 5 inhibitor I (PDE5):
MOA: increase cGMP -> increase erectile response to sexual stimuli

sildenafil [viagra] or [Revatio]

PDE5 inhibitors II:
MOA: similar to viagra

tadalafil [Cialis] (longer half life)
Indications: ED, BPH, pulmonary hypertension **** (QUESTION APPARENTLY)

Question 27

Erectile Dysfunction Drug AE

Answer 27

AE: hypotension, priapism (condition where penis wont return to flaccid state), ototoxiciy, dont take with nitrates or with BB

Question 28

Selective estrogen receptor modulators or SERMs, partial ER agonists

Answer 28

Tamoxifen [Nolvadex]
Toremifene [Fareston]

Question 29

Pure estrogen receptor antagonist

Answer 29

Fulvestrant [Faslodex]

Question 30

Aromatose Inhibitors

Answer 30

Anastrozole [Arimidex]
Exemestane [Aromasin]

Question 31

Trastuzumab [Herceptin]

Answer 31

monoclonal antibody for IV therapy of metastatic breast cancer -> anti-HER2 -> blocks HER2 receptors

Question 32

Drug for prostate cancer

Answer 32

Leuprolide [Lupron] - GnRH agonist
Flutamide [Eulexin] - androgen receptor blockers
Bicalutamide [Casodex] - androgen receptor blockers