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

Exam 2: Lecture X, Estrogens Flashcards

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
Progesterone major effects
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
If implantation of ovum has not occurred, progesterone secretion....
stops
27
If implantation of ovum has occurred, progesterone secretion....
continues
28
Progesterone Toxicity
is low increase BP, decrease HDL
29
major clinical use of progestins....
oral or implanted contraceptives progesterone agonists
30
Progesterone agonist indication
``` Uterine bleeding dysmenorrhea premenstrual syndrome Endometriosis suppression of postpartum lactation carcinoma hypoventilation ```
31
Mifepristone (RU 485)(Mifeprex)
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
Mifepristone (RU 485)(Mifeprex) Adverse effects
``` Nausea Vomiting Abdominal pain Pelvic pain Vaginal bleeding ```
33
Danazol (Danocrine)
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
Danazol (Danocrine) side effects
``` Weight gain Edema Decreased breast size Acne Oily skin Libido changes Muscle cramps ```
35
2 major types of oral contraceptives
Combination estrogen-progestin tablets and Progestin only pills * Typically, progestins are more potent, and have more lasting physiological effect
36
Monophasic combination prep
constant dosage during the cycle | taken from 21 consecutive days out of 28
37
Biphasic and triphasic combination prep
dosage of 1 or both components is changed | once or twice during the cycle
38
Combination Estrogen-Progestin Tab MOA
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
Progesterone only pill...
taken continuously contraceptive less reliable doesn't interfere with lactation
40
some effects of chronic use hormonal contraceptives
``` 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
Severe disorders related to hormonal contraceptives
** 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
Benefits of oral contraceptives
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
Infertility treatment
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
Clomiphene Pharmacokinetics
Nonsteroidal partial antagonist induces ovulation well absorbed orally excreted primarily in urine significant protein binding, enterohepatic circulation
45
Clomiphene Adverse effects
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
Menotropin (Repronex)
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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