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67 Cards in this Set

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Gonadal hormones:

What is the basic mechanism of steriod hormones?
The hormone diffuses into target cells and binds to receptor in cytoplasm or nucleus.

Then the hormone-receptor complex dimerizes in nucleus and binds to specific regions on DNA.

This complex then either promotes or inhibits transcription of specific genes.
Gonadal hormones:

What are the three physiologic estrogens? Activity level?
1. estradiol 17 beta (E2)(most estrogenic in action)
2. estron (E1): somewhat less estrogenic
3. estriol (E3): not very active metabolite
Gonadal hormones:

What actions does estrogen have on the reproductive system? (5)
Estrogen effect on repro system:
1. growth, development, and maintance of primary and secondary female sex characteristics
2. puberty body changes
3. regulation of menstrual cycle
4. growth of uterine endometrium during menstrual cycle
5. secretion of thin cervical mucus
Gonadal hormones:

What metabolic effects does estrogen have on the body? (5)
1. increase amt of HDL circulating (decrease LDL)
2. increase cholesterol saturation of bile
3. increase BP via production of a renin substrate
4. promotes clot formation
5. decrease bone resorption
6. increase liver protein synthesis
Gonadal hormones:

What effects does estrogen have on CNS function?
1. increases mood
2. "neurotropic effects" (induce survival of neurons) showing increase in memory and cognition
3. "neuroprotective" effects that aren't totally understood but are thought to protect agains ischemia and neurodegenerative disorders.
Gonadal hormones:

Can estrogens be used to treat acne?
Yes
Gonadal hormones:

What are the two pharmacokinetic drug interactions of estrogens?
1. inducers of cyto p450 to enhance metabolism of other drugs and others enhance estrogen metabolism alike

2. Antibiotics can reduce bioavailability by altering intestinal flora (problems with absorption?)
Gonadal hormones:

Physiologic actions of progesterone (6).
1. regulation of mestrual cycle (esp neg feedback during luteal phase)
2. induces secretory production of uterine endometrium (needed for implantation)
3. thickens cervical mucus
4. increases body temperature at ovulation
5. needed to maintain pregnancy (inhibits uterine contractility)
6. grows mammary glands in pregnancy
Gonadal hormones:

What does progesterone do to the effects of estradiol?
It enhances some effects but decreases others (all that was said0
Gonadal hormones:

What does MIFEPRISTONE do?
It is an antagonist at progestin and glucocorticoid receptor allowing for the termination of pregnancies <49 days
Gonadal hormones:

Adverse effects of MIFERPRISTONE? (5)
1. prolonged vaginal bleeding
2. abdominal pain
3. nausea
4. diarrhea
5. headache
Gonadal hormones:

What are the three main types of oral contraceptives?
1. combinations (COC's)
2. progestin-only
3. emergency
Gonadal hormones:

What are COC's made of and what is their MOA?
COC's: they consist of an estrogen and a progestin.

MOA: mimic negative feedback of E2 and progestin which prevents follicular development and ovulation (mimics the luteal phase). Biphasic and triphasic preps attempt to mimic the rise and fall in these hormones.

Progestin also thicken cervical mucus and prevents sperm transport.
Gonadal hormones:

What are the 8 adverse effects of COC's?
1. nausea/vomiting (E)
2. water retention (E or P)
3. mastalgia (E)
4. headache (E or P)
5. acne (p)
6. decreased glucose tolerance (E)
7. melasma, chloasma (E) -dark patches
8. irregular bleeding (E too low)
Gonadal hormones:

8 absolute contraindications of COC's:
1. Hx of clotting disorders
2. Hx of CV disease
3. hyperlipidemia
4. heavy smoker
5. pregnant
6. Hx of estrogen-dependant neoplasia
7. undiagnosed vaginal bleeding
8. impaired liver function
Gonadal hormones:

Five relative contraindications (want to beware of)?
1 diabetes mellitus
2. hypertension
3. migraine headaches (Jill)
4. gall bladder diseaes
5. major surgery
Gonadal hormones:

7 beneficial effects of COC's:
1. acne improves
2. bone density improves
3. decreased menstrual flow
4. less painful menstruation
5. decreased ovarian cysts
6. decreased risk of endometrial, ovarian, and colon cancers
7. decreased risk of pelvic inflammatory disease
Gonadal hormones:

What is etonorgestrel implant an example of?
A progestin-only contraceptive
Gonadal hormones:

What is depro-provera an example of?
A progestin-only contraceptive (IM)
Gonadal hormones:

What is the mechanism of action of progestin-only contraceptives? (2 main things)
Progestin only contraceptives inhibit ovulation, inhibit sperm transport by thickening cervical mucus.
Gonadal hormones:

What are 7 adverse effects of progestin-only contraceptives?
1. nausea
2. headache
3. weight gain
4. acne
5. mood changes
6. decrease in HDL and increase in LDL levels.
Gonadal hormones:

What are two main contraindications of progestin-only contraceptives?

What are two contra's of Depo-provera?
General:
1. un-dx vaginal bleeding
2. liver disease

Depo-provera:
1. increased risk of thromboembolism
2. loss of bone mineral density
Gonadal hormones:

What is the mechanism of emergency contraception?
When admistered within 72 hours of unprotected intercourse, high doses of ovarian steriods, can inhibit ovulation (most likely), inhibit sperm transport, and inhibit implantation of the blastocyst.
Gonadal hormones:

What is the Yuzpe regimen for emergency contraception?
Yuzpe regimen: two COC pills taken w/i 72 hrs of intercourse, followed by two COC's taken 12 hrs later.

Any COC prep is effective

Efficacy: reduces chance of preg 75%
Gonadal hormones:

What is the L-norgestrel-only regimen for emergency contraception?
L-norgestrel-only regimen:
First dose of l-norgestrel taken within 72 hrs of intercourse, followed by second dose 12 hr later (or take both doses at once)

Efficacy: 75-90% inhibition of pregnancy
Gonadal hormones:

What is one example of the Yuzpe regimen for emergency contraception?
Preven = ethinyl estradiol (EE) + levonorgestrel
Gonadal hormones:

What are two examples of the levonorgestreal only emergency contraception?
1. Plan B
2. Ovrette

(same as Yuzpe method, just double dose and repeat after 12 hrs)
Gonadal hormones:

What are four adverse effects of emergency contraception?
1. nausea
2. vomiting
3. dizziness
4. mastalgia
Gonadal hormones:

What is the physiologic basis for menopause?
Menapause is caused by decrease or end in supply of:
1. ovarian follicules
2. cells that secrete estradiol and progesterone
3. estradiol levels
4. no ability to maintain negative feedback causing elevations of gonadotropins.
Gonadal hormones:

What is perimenopause?

When can it begin?
The transition into menopause, showing an onset of symptoms such as vasomotor instability, insomnia, mood changes, and irregular cycles.

May begin in late 30's, early 40's.
Gonadal hormones:
VIP

What are the four intermediate effects of estrogen deficiency?
Intermediate:
Urogenital atrophy
urinary incontinence
genital tract infection
skin changes
Gonadal hormones:

what are the three long term effects of estrogen deficiency?
Long term effects of estrogen deficiency?
1. osteoporosis
2. CV disease
3. cognitive impairment
Gonadal hormones:

Four major indications for HRT in menopausal women?
1. vasomotor instability (hot flashes, night sweats)
2. mood changes
3. urogenital atrophy
4. prevention and treatment of osteoporosis.
Gonadal hormones:

Compare the estrogens used in HRT vs those used in OC's?
Activities of estrogens used in HRT are generally lower than in OC's. But the contraindications to estrogen use are similar to those for OC's.
Gonadal hormones:

What six positive effects are seen in patients on HRT's?
1. decrease vasomotor symptomss
2. decrease urogenital atrophy
3. decrease recurrent urinary symptoms
4. relief from fatigue
5. relief from depression
6. maintenance of bone mineral density
Gonadal hormones:

What are the adverse effects of HRT?
Estrogen assoc: nausea, mastalgia, headache, fluid retention

Progestin: weight gain, headache
Gonadal hormones:

Explain how the concombinent use of estrogen and progestin (in HRT) change endometrial cancer risk?
The use of unopposed estrogen for five years increases your chances of endometrial CA 5-fold but this risk is eliminated by addition of progestin.
Gonadal hormones:

Explain how the concombinent use of estrogen and progestin (in HRT) change breast cancer risk?
Progestin in the estrogen/progestin therapy contributes to the risk of breast CA. However there is little to no risk of breast CA with HRT < 5yrs.
Gonadal hormones:

What does HRT due to risk of colorectal CA?
Reduces the risk of colorectal CA
Gonadal hormones:
VIP

What did the Women's Health initiative find in regards to diseases that are increased in likelihood with administration of HRT? (5)
HRT treatment increased the likelihood of:
1. breast CA
2. stroke
3. venous thrombosis
4. dementia
5. cognitive impairments
Gonadal hormones:

What is so frickin special about SERM's
SERMS are paritial estrogen antagonists, preventing estrogen-sensitive breast CA's; and they are also partial estrogen agonists on the bone, preventing osteoporosis.
Gonadal hormones:

What are the anti-estrogenic and estrogenic actions of TAMOXIFEN?
TAMOXIFEN
1. inhibits estrogen-stimulated mammary tumor growth
2. inhibits bone resorption/increases bone density
3. increases uterine hyperplasia and risk of endometrial CA
4. Increases chance of DVT
Gonadal hormones:

What are the anti-estrogenic and estrogenic actions of RALOXIFENE?
RALOXIFENE:
1. inhibits estrogen-stimulated mammary tumor growth
2. inhibits bone resorption/increases bone density
3. decreases circulating LDL cholesterol (no effect on HDL)
4. increases chance of DVT
GONADAL HORMONES:

Three common side effects of SERMS?
1. hot flashes
2. leg cramps
3. teratogenic in pregnancy
GONADAL HORMONES:
Key concept

Major naturally occuring androgens are (4)
1. testosterone (T)
2. dihydrotestosterone (DHT)
3. androstenedione
4. dehydroepiandrosterone (DHEA)
GONADAL HORMONES:

What is the MOA of androgens?
1. testosterone diffuses into the cell and binds to the androgen receptor (or is converted to DHT and binds to receptor -or- is converted to estradiol and binds to estrogen receptor)
2. hormone-receptor complex dimerizes in cell nucleus and binds to DNA.
3. This promotes or inhibits transcription of specific genes = physiologic effect
GONADAL HORMONES:

Five reproductive actions of androgens:
Androgens:
1. growth and maintenance of primary and secondary sex characteristics in men
2. puberty girls
3. promote spermatogenesis (w/ FSH)
4. stimulate libido
GONADAL HORMONES:

Anabolic actions of androgens:
Anabolic actions of androgens:
Increase in:
1. protein synthesis
2. lean body mass
3. skeletal muscle growth
4. reduction of fat mass
GONADAL HORMONES:

What effects on growth do androgens have? (4)
Effects on growth (androgens)
1. stimulates skeletal growth
2. stimulates epiphyseal closure
3. causes growth at larynx during puberty
4. causes voice deepening
GONADAL HORMONES:

What are the metabolic effects of androgens? (5)
Androgens metabolic effects:
1. erythropoiesis
2. decreased synthesis of clotting factors
3. increased sebum production in skin
4. decresed HDL (increase LDL)
5. androgenic alopecia (male pattern baldness)
GONADAL HORMONES:
Key Concept

Some of the effects of androgens are due to testosterone itself while others are due to DHT and Estradiol 17beta. What are the effects of each?
Testosterone effects: actions on skeletal m., bone (erythropoiesis).

DHT effects: reproductive tissues (external genetalia), hair, skin

Estradiol 17 beta effects: breast, bone (epiphyseal closure).
GONADAL HORMONES:

What do 5alpha reductase and CYP 19 aromatase do? How are these functions exploited?
5-alpha reductase: converts testosterone to DHT

CYP 19: converts testosterone to estradiol

These enzymes are therapeutic targets.
GONADAL HORMONES:
Androgens in clinical practice

What are two types of alkylated androgens? How are they administered?

Pros and cons?
Alkylated androgens: (oral)
1. methyltestosterone
2. danazol - only indicated in women

Oral preps are convenient but not favored for HRT since first pass metabolism promotes hepatotoxicity.
GONADAL HORMONES:

Advantages of esterified preparations of androgens? How are they administered?
Esterifeid androgens (anything that starts with "testosterone")

Administered IM

Advantages: long duration of action, little hepatotoxicity, well tolerated.
GONADAL HORMONES:

Advantages of transdermal preparations of androgens?

One disadvantage?
Transdermals: convenient, little hepatotoxicity, steady-state levels, well-tolerated

Disadvantage: expensive
GONADAL HORMONES:

There therapeutic uses of androgens in males:
1. delayed puberty
2. primary or secondary hypogonadism
3. Rx of osteoporosis in males
GONADAL HORMONES:

Two therapeutic uses of androgens in females?
1. adjunct in HRT in menopause
2. treatment for endometriosis in women (DANAZOL)
GONADAL HORMONES:

What are anabolic steriods used for? (3)

Name four anabolic steroids
Anabolic steroids:
1. stanozolol
2. oxandrolone
3. nandrolone
4. oxymethalone

These are weak androgen but used for their anabolic actions:
1. Rx of anemia (oxymethalone, nandrolone)
2. Rx of hereditary angioedema (stanozolol)
3. stimulate weight gain after surgery, AIDS (oxandrolone)
GONADAL HORMONES:

What are four common (but not serious) adverse effects of androgens?
Common effects of androgens:
1. acne (virilizing)
2. hair scalp loss (virilizing due to DHT)
3. gynecomastia (feminizing due to estradiol)
4. obstructive sleep apnea (virilizing)
GONADAL HORMONES:

What are six potentially serious adverse effects of androgens?
Serious adverse effects of androgens:
1. hepatotoxicity
2. premature bone maturation
3. cardiovascular diseaes
4. edema
5. testicular atrophy
6. BPH and prostatic CA
GONADAL HORMONES:
VIP

Adverse effects of DANAZOL: (6)
1. acne
2. hirsutism
3. mild voice deepening
4. edema
5. hot flashes
6. urogenital atrophy
GONADAL HORMONES:
VIP

Adverse effects to high doses (performance enhancing) effects of androgens in women? (5)
High doses of androgens in women:
1. amenorrhea
2. virilization (acne, male pattern baldness, hirsuitism)
3. permanent voice deepening
4. CV disease
5. infertility/birth defects in offspring
GONADAL HORMONES:

What are three androgen antagonists that work through blocking androgen receptors?

How are they used?
Receptor blockers:
1. Bicalutamide & 2. Flutamide = both treat prostate CA

3. Spironolactone: treat hirsuitism in women.
GONADAL HORMONES:

What are two androgen antagonists that are synthesis inhibitors?

How are they used?
Synthesis inhibitors:

1. finasteride (Proscar)-blocks conversion to dihydrotestosterone by inhibiting 5 alpha reductase

2. dutasteride-inhibits 5 alpha reductase 1 and 2

Both are used to treat BPH and finasteride (proscar/propecia) is used to treat male pattern baldness.
GONADAL HORMONES:
VIP

Why and how are GnRH agonists (leuprolide) used?
GnRH agonists can be pro-fertility or antifertility depending on the regimen.

Pro-fertility: requires episodic administration, mimicking physiology

Anti-fertility effects: occur with chronic regimens because this desensitizes pituitary GnRh receptors and decreases gonadotropin secretion and testosterone secretion (creates a hypo-gonadal state = nonsurgical castration)
GONADAL HORMONES:

When is down regulation in males by GnRh agonists advised?
Situations of
1. precocious puberty
2. advanced prostate CA (alternative to castration)
GONADAL HORMONES:

What drug is a GnRH antagonist?

What does it do? When is it used?
GnRH antagonist: Abarelix

1. blocks GnRH receptor to reduce gonadotropin secretion and testosterone synthesis and release

2. indicated for treatment of precocious puberty and advanced prostate CA