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Pharmacology & Medical Chemistry II > Exam 2: Lecture X, Estrogens > Flashcards

Exam 2: Lecture X, Estrogens Flashcards

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1
Q

Primary Sex hormones Females

A

Estrogen and progesterone

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2
Q

Production of Estrogen and Progesterone is regulated by…

A

FSH and LH

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3
Q

FSH effects

A

estrogen secretion

Estrogen secretion from ovaries

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4
Q

LH effects

A

progesterone secretion

Progesterone secretion from ovaries

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5
Q

Most potent ovaries estrogen in women is….

A

estradiol (estrogen)

Highly bound to sex hormone-binding globulin (SHBG)

effective orally, due to intensive hepatic metabolism semisynthetic agents are used

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6
Q

Estrogen receptors found mostly in…

A

cells of principal targets

also found in AP/Hypothalamus

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7
Q

Principal targets are…

A

reproductive system

ie. Uterus, vagina, and mammary glands

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8
Q

Progesterone effects on estrogen receptor expression

A

decreases

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9
Q

Prolactin effects on estrogen receptor expression

A

increases in mammary gland, liver but no effect uterus

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10
Q

Estrogen Effects 1

A 
growth of genital structure
breast development
development of secondary sexual characteristics
maturation of OVA
sexual behavior modifications
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11
Q

Estrogen effects 2

A 
Metabolic effects
changes in serum protein level
preservation of bone mass
increase absorption in GI tract
increase plasma triglyceride level
enhanced blood coagulability
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12
Q

Estrogen clinical use

A

stimulate development of secondary sex characteristics (11-13yr old)

replacement therapy in hypo-ovarian condition
menopausal symptom treatment
postmenopausal replacement therapy
vaginitis
itching pain during sex
genital swelling
pain peeing
contraception
prostate cancer
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13
Q

Estrogen pharmacokinetics

A

natural and synthetic used clinically

absorbed well GI

can be absorbed skin - mucous membranes, given as patches or creams

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14
Q

Natural estrogens metabolism in liver speed

A

fast

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15
Q

Synthetic estrogens metabolism in liver speed

A

slow

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16
Q

Long term doses in women associated with following toxicity…..

A

2-3 fold increase gall-bladder disease

3 fold increase venous thrombosis

1.5 fold increase stroke

hypertension

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17
Q

Moderate doses in women associated with following toxicity…..

A

stimulatory effects vagina,uterus, breast tissue

breast tenderness

endometrial hyperplasia

breakthrough bleeding

hyperpigmentation

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18
Q

Estrogens contraindications

A

estrogen dependent tumors

vaginal bleedings

liver disease

gall-bladder disease

history of thromboembolism

cig smoke significantly increase risk of serious cardia event

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19
Q

Estrogen antagonist

A

have small effect by themselves, but they compete with natural estrogens for binding sites

Tamoxifen/Clomiphene

20
Q

Tamoxifen (nolvadex)

A

Treatment of estrogen-dependent breast cancer, blocks estrogen receptors in tumor. binds to receptor in nucleus

targets breast/uterus and bones

v important non-steroidal agent

Little toxicity, prevent osteoporosis

21
Q

Clomiphene (Clomid)

A

Infertility treatment

non-steroidal agent

targets Hypo/AP, inhibits estrogen receptors

prevents normal regulation by neg feedback

increases secretion of GnRH, LH + FSH…induce ovulation

22
Q

Clomiphene (Clomid) Adverse effects

A

Adverse effects are mild and disappear with drug discontinuation

headaches
skin allergies
reversible hair loss
eye symptoms

Contraindication:
-patients with enlarged ovaries (reported risk of ovarian cancer)

23
Q

Progesterone is synthesize and secreted from…

A

placenta, Adrenal cortex and testes

24
Q

Progesterone metabolized in…

A

liver and has a very short half life and bioavailability

25
Q

Progesterone major effects

A

through negative feedback affects hypothalamus and pituitary, decrease release of LH

raises body temp
development of secretory tissue in boobies
vascularization of uterine wall
maturation of uterine endometrium

26
Q

If implantation of ovum has not occurred, progesterone secretion….

A

stops

27
Q

If implantation of ovum has occurred, progesterone secretion….

A

continues

28
Q

Progesterone Toxicity

A

is low

increase BP, decrease HDL

29
Q

major clinical use of progestins….

A

oral or implanted contraceptives

progesterone agonists

30
Q

Progesterone agonist indication

A 
Uterine bleeding
dysmenorrhea
premenstrual syndrome
Endometriosis
suppression of postpartum lactation
carcinoma
hypoventilation
31
Q

Mifepristone (RU 485)(Mifeprex)

A

An orally active steroid antagonist of progesterone and glucocorticoids

Binds to cytosolic steroid receptors of these hormones and alters genes

Abortifacient (Europe) – single dose followed by PGE1(misoprostol) administration

Abortion with low incidence of serious toxicity

Possibility of vaginal bleeding requires administration by a physician

Reportedly used in malignancy treatment, treat endometriosis

Progesterone Antagonists

32
Q

Mifepristone (RU 485)(Mifeprex) Adverse effects

A 
Nausea 
Vomiting
Abdominal pain
Pelvic pain
Vaginal bleeding
33
Q

Danazol (Danocrine)

A

An orally active steroid antagonist of:
- progesterone, glucocorticoids and androgen receptors

Binds with steroid transport protein in the blood
Inhibits several P450 enzymes in gonadal steroid synthesis

Treatment of endometriosis and fibrocystic disease of the breast

34
Q

Danazol (Danocrine) side effects

A 
Weight gain
Edema
Decreased breast size
Acne
Oily skin
Libido changes
Muscle cramps
35
Q

2 major types of oral contraceptives

A

Combination estrogen-progestin tablets and Progestin only pills

  • Typically, progestins are more potent, and have more lasting physiological effect
36
Q

Monophasic combination prep

A

constant dosage during the cycle

taken from 21 consecutive days out of 28

37
Q

Biphasic and triphasic combination prep

A

dosage of 1 or both components is changed

once or twice during the cycle

38
Q

Combination Estrogen-Progestin Tab MOA

A

Estrogen inhibit FSH = follicle development
Progestin inhibit LH = ovulation

affects uterine tubes/endometrium
makes cervical mucus inhospitable for sperm

Results in endometrium unsuitable for implantation

39
Q

Progesterone only pill…

A

taken continuously

contraceptive less reliable

doesn’t interfere with lactation

40
Q

some effects of chronic use hormonal contraceptives

A 
Depression of ovarian function 
Follicular development is minimal, and corpora lutea is absent
Ovaries become smaller
Cervix shows some hypertrophy and polyp formation
Some breast enlargement 
Tendency to suppress lactation
Some detrimental effect upon the liver
Weight gain
Nausea
Mood changes
Skin pigmentation
Reversible hypertension
41
Q

Severe disorders related to hormonal contraceptives

A

** Incidences of serious toxicity is low **

Serious changes in blood coagulation
Thromboembolism
Venous thromboembolic disease
Myocardial infarction (related to smoking)
Stroke
Carcinogenesis – a complicated picture:
reduced incidences of endometrial and ovarian carcinoma and
- reduced incidences of endometrial hyperplasia
- cervical carcinoma – unchanged
- breast cancer – no definite conclusion

42
Q

Benefits of oral contraceptives

A

Relatively safe method of contraception for young women, not so much for older

reduction in dose reduces mild/severe adverse effects in young women

43
Q

Infertility treatment

A

Targets hypothalamus and anterior pituitary gland

Inhibits estrogen receptors in the hypothalamus and anterior pituitary gland

Prevents normal regulation by the negative feedback

Increases secretion of GnRH, also LH + FSH - surge gonadotropin secretion

Surge of gonadotropin secretion – induces ovulation

44
Q

Clomiphene Pharmacokinetics

A

Nonsteroidal partial antagonist induces ovulation

well absorbed orally

excreted primarily in urine

significant protein binding, enterohepatic circulation

45
Q

Clomiphene Adverse effects

A

Adverse effects are mild and disappear with the drug discontinuation:

  • headaches
  • skin allergies
  • reversible hair loss
  • eye symptoms

Contraindication:
- patients with enlarged ovaries (reported risk of ovarian cancer)

46
Q

Menotropin (Repronex)

A

Combination of LH+FSH in different proportionally (originally 1:1)

  • originally extracted from urine of postmenopausal women (hMG)
  • recombinant gonadotropins to a great degree replaced human gonadotropins
  • daily injections (IM, SC) for 10 days

used in men to stimulate sperm production

Recombinant human (FSH) followed by one-two large doses of LH

Pharmacology & Medical Chemistry II (43 decks)

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