Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Endocrinological Pharmacology > female reproductive endocrinology, 9. Estrogens and antiestrogens, 10. Progestins and antiprogestins 11. Contraceptives > Flashcards

female reproductive endocrinology, 9. Estrogens and antiestrogens, 10. Progestins and antiprogestins 11. Contraceptives Flashcards

1
Q

ovarian hormones- estrogen

A

ovarian hormones

  • Female reproductive development and function – growth of genital structure, appearance of secondary sexual characteristics, growth spurt during puberty
  • Metabolic effects – modifies protein levels, TG ↑, LDL ↓, HDL ↑
  • Blood coagulability ↑, bone resorption ↓

estrogens:

  1. ethinyl-estradiol
  2. mestranol
    conjugated estrogen: (premarin),
  3. estradiol

Side effects – Estrogens:

  • Moderate - toxicity
  • Breast tenderness
  • Breakthrough bleeding
  • Nausea
  • Severe toxicity
  • Thromboembolism
  • Gallbladder disease
  • Hypertriglyceridemia
  • Migraine
  • Hypertension
  • Depression
  • In postmenopausal women
  • Breast cancer
  • Endometrial hyperplasia + cancer
  • Increased risk of cardiovascular events

*In hypogonadal girls
Dosage should be adjusted to prevent premature epiphyseal closure of long bones (subsequent short stature)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Anti-estrogens

A

SERM= selective estrogen receptor modulators

  • estrogen antagonist - breast, CNS, uterus
  • estrogen agonist - liver, bone

Tamoxifen
Raloxifene
Clomifene

estrogen-receptor-antagonist: Fulvestrant

Synthesis inhibitors:
aromatase inhibitors: Anastrozole (Letrozole, Exemestane)
(Cyp450 inhibitor: danazol)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

GnHR analogue

A

(Leuprolide)
Groserelin

continious stimulation suppresses GnHR release- estrogen–, progesterone–

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

GnHR antagonist

A

Degarelix

gamirelix

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Ovarian hormones- progesterone

A

Progestins:

  1. Pregans
  2. Estrans
  3. Gonans
  4. Pregans:
    a) medroxyprogesterone-acetate
    b) Cyproterone acetate
    b) Drospirenone (Drospirone??)
  5. Estrans:
    a) Norethisterone
  6. Gonans:
    a) levonorgestrel
    b) desogestrel
  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Anti-progestins

A

Mifepristone

  • (combined with Misoprostol for abortion)
  • glucocorticoid-R-antagonist
  • progestin-R-antagonist

Ulipristal acetate

  • SPRM- selective progestin receptor modulator
  • Emergency birth pill
  • (or high level of Levonorgestrel)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Contraceptive

A

1-2-3 phases

Ethinyl-estradiol
+
Levonorgestrel or desogestrel or Drospirenone or Norethisterone or cyproterone acetate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Ethinyl-estradiol

Mestranol

A

Estrogens

  • Female reproductive development and function – growth of genital structure, appearance of secondary sexual characteristics, growth spurt during puberty
  • Metabolic effects – modifies protein levels, TG ↑, LDL ↓, HDL ↑
  • Blood coagulability ↑, bone resorption ↓
  • Synthetic estrogen, improved bioavailability
  • Oral, parenteral, transdermal patch
  • Metabolism by hepatic CYP450
  • Interaction with P450 inducers may lead to bleeding and reduced
    contraceptive efficacy
  • Hypogonadism in girls
  • Hormone replacement therapy
  • Prevent bone loss and osteoporosis
  • Oral hormonal contraceptives
  • Parenteral contraceptive

Side effects – Estrogens:

  • Moderate - toxicity
  • Breast tenderness
  • Breakthrough bleeding
  • Nausea
  • Severe toxicity
  • Thromboembolism
  • Gallbladder disease
  • Hypertriglyceridemia
  • Migraine
  • Hypertension
  • Depression
  • In postmenopausal women
  • Breast cancer
  • Endometrial hyperplasia + cancer
  • Increased risk of cardiovascular events

*In hypogonadal girls
Dosage should be adjusted to prevent premature epiphyseal closure of long bones (subsequent short stature)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Conjugated estrogen (Premarin) - Estradiol

A

Estrogens

  • Female reproductive development and function – growth of genital structure, appearance of secondary sexual characteristics, growth spurt during puberty
  • Metabolic effects – modifies protein levels, TG ↑, LDL ↓, HDL ↑
  • Blood coagulability ↑, bone resorption ↓
  • Conjugated estrogen (estradiol) of biological source
  • Oral, parenteral, transdermal patch
  • Hypogonadism in girls
  • Hormone replacement therapy (premature ovarian
    failure, menopause, surgical removal of ovaries)
  • Prevent bone loss and osteoporosis

Side effects – Estrogens:

  • Moderate - toxicity
  • Breast tenderness
  • Breakthrough bleeding
  • Nausea
  • Severe toxicity
  • Thromboembolism
  • Gallbladder disease
  • Hypertriglyceridemia
  • Migraine
  • Hypertension
  • Depression
  • In postmenopausal women
  • Breast cancer
  • Endometrial hyperplasia + cancer
  • Increased risk of cardiovascular events

*In hypogonadal girls
Dosage should be adjusted to prevent premature epiphyseal closure of long bones (subsequent short stature)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Tamoxifen

A

SERM – Selective estrogen receptor modulators

  • Estrogen antagonist activity → breast, CNS, uterus
  • Estrogen agonist activity → liver, bone
  • Oral
  • Partial agonist in the endometrium
  • Hormone-responsive breast cancer (also as prophylaxis)
  • Side effects:
    hot flushes,
    thromboembolism,
    endometrial hyperplasia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Raloxifene

A

SERM – Selective estrogen receptor modulators

  • Estrogen antagonist activity → breast, CNS, uterus
  • Estrogen agonist activity → liver, bone
  • Oral
  • Treatment and prevention of osteoporosis in postmenopausal women
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Clomifene

A

SERM – Selective estrogen receptor modulators

  • Estrogen antagonist activity → breast, CNS, uterus
  • Estrogen agonist activity → liver, bone
  • Oral
  • Ovulation induction
    (selectively inhibits estrogen receptors in pituitary → reduced negative feedback → increased LH and FSH)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Fulvestrant

not on the list

A

Estrogen receptor antagonists

  • Non-selective antagonist
  • Intramuscular injection
  • Breast cancer resistant to 1st line tamoxifen
  • Side effects: hot flushes, headache, injection site
    reaction
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Anastrozole

A

Synthesis inhibitors

Aromatase inhibitors
(- Letrozole (non-steroidal))
(- Exemestane (steroidal))

  • Anastrozole
  • Oral
  • Adjuvant treatment of hormone-responsive breast cancer (advanced disease)
  • anticancer
  • Side effects:
  • hot flushes,
  • musculoskeletal disorders,
  • reduced bone mineral density,
  • joint symptoms
  • Nausea, vomiting, diarrhea
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Danazol

not on the list

A

synthesis inhibitor:

  • CYP450 inhibitor, partial agonist of progestin and androgen receptors
  • Oral
  • Endometriosis
  • Fibrocystic breast disease
  • Side effects: acne, hirsutism, weight gain, menstrual
    disturbances, hepatic dysfunction
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Goserelin

Leuprolide

A
  • Synthetic peptide with GnRH agonist activity
  • Parenteral
  • Long-acting
  • Continuous administration of GnRH agonists suppresses gonadotropin secretion and thereby inhibits ovarian production of estrogens and progesterone
    → inhibits the release of FSH and LH → both androgen and estrogen syntheses are reduced

indications:

  • Ovarian suppression in women undergoing controlled ovulation induction
  • Ovarian suppression in endometriosis, leiomyoma
  • Central precocious puberty
  • Prostate cancer
  • Breast cancer

Side effects:

  • headache,
  • nausea,
  • injection site reaction,
  • symptoms of hypogonadism with continuous treatment (impotence in male)
17
Q

Degarelix

Ganirelix

A

Degarelix

  • GnRH antagonist
  • Parenteral
  • GnRH receptor inhibition → altered release FSH and LH → testosterone synthesis ↓
  • Prostate cancer
  • Controlled ovarian stimulation (suppress endogenous LH and FSH) (1st stage)

Side effects:

  • Nausea, vomiting
  • Headaches
18
Q

Progesterone

A
  • Low oral bioavailability
  • Biologic source
  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
19
Q

Pregnans

A

Medroxyprogesterone
Drospirone
Cyproterone acetate

20
Q

Estrans

A

Norethisterone

21
Q

Gonans

A

Norgestrel

Desogestrel

22
Q

Medroxyprogesterone

A

Progestins

  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

PREGANS

  • Synthetic progesterone
  • Improved oral bioavailability
  • Metabolism by hepatic CYP450
  • Hormone replacement therapy
  • Hormonal contraceptives
  • Infertility treatment
  • Prevent estrogen-induced endometrial cancer
  • Assisted reproductive technology methods
    (promote and maintain pregnancy)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
23
Q

Drospirone / Drospirenone

A

Progestins

  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

PREGANS

  • Synthetic progesterone
  • Improved oral bioavailability
  • Metabolism by hepatic CYP450
  • Hormone replacement therapy
  • Hormonal contraceptives
  • Infertility treatment
  • Prevent estrogen-induced endometrial cancer
  • Assisted reproductive technology methods
    (promote and maintain pregnancy)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
24
Q

Cyproterone acetate

A

Progestins

  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

PREGANS

  • Synthetic progesterone
  • Improved oral bioavailability
  • Metabolism by hepatic CYP450
  • Hormone replacement therapy
  • Hormonal contraceptives
  • Infertility treatment
  • Prevent estrogen-induced endometrial cancer
  • Assisted reproductive technology methods
    (promote and maintain pregnancy)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
25
Q

Norethisterone

A

Progestins

  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

ESTRANS

  • Synthetic progesterone
  • Improved oral bioavailability
  • Metabolism by hepatic CYP450
  • Hormone replacement therapy
  • Hormonal contraceptives
  • Infertility treatment
  • Prevent estrogen-induced endometrial cancer
  • Assisted reproductive technology methods
    (promote and maintain pregnancy)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
26
Q

Levonorgestrel

A

Progestins

  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

GONANS

  • Synthetic progesterone
  • Improved oral bioavailability
  • Metabolism by hepatic CYP450
  • Hormone replacement therapy
  • Hormonal contraceptives
  • Infertility treatment
  • Prevent estrogen-induced endometrial cancer
  • Assisted reproductive technology methods
    (promote and maintain pregnancy)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
27
Q

Desogestrel

A

Progestins

  • Induce secretory changes in the endometrium, breast proliferation
  • Maintenance of pregnancy
  • Metabolic effects (modify carbohydrate metabolism, stimulate fat deposition)

GONANS

  • Synthetic progesterone
  • Improved oral bioavailability
  • Metabolism by hepatic CYP450
  • Hormone replacement therapy
  • Hormonal contraceptives
  • Infertility treatment
  • Prevent estrogen-induced endometrial cancer
  • Assisted reproductive technology methods
    (promote and maintain pregnancy)

Side effects – Progestins:

  • HDL↓,LDL↑
  • Hypertension
  • Weight gain
  • Reversible decrease of bone density
  • Breast cancer risk ↑
28
Q

Mifepristone

A

Anti-progestins

  • Progestin and glucocorticoid receptor antagonist
  • Oral
  • Medical abortion, in combination with prostaglandin-E analogue (Misoprostol); can be used up to 49 days after last menstrual period
  • Cushing’s syndrome (not extensively used)

Side effects:

  • abdominal pain
  • GI disturbances (mostly due to coadministration of misoprostol),
  • headache
  • vaginal bleeding,
  • atypical infection
29
Q

Ulipristal acetate

A

Anti-progestins

  • SPRM (selective progestin receptor modulator)
  • Oral
  • Emergency birth pill
  • Myoma growth suppression
30
Q

Hormonal contraceptives - Preparations available + types of oral contraceptives

A

▪ Preparations available:

  • Oral pills
  • Long-acting ‘depot’ injections (effective for 8-13 weeks)
  • Subcutaneous implants (effective for 3-6 years)
  • Transdermal patch (effective for 1 week, can be used 3 weeks in a row)
  • Vaginal ring (3 weeks ring in, 1-week break)
  • Intrauterine devices – IUD (effective for ∼5 years)
  • may also contain spermicidal agent (detergent), provide STD protection

types of oral preparations:
(1) Combinations of estrogens and progestins
(2) Continuous progestin therapy without concomitant administration of estrogens
(also known as the ‘mini-pill’ – progestin only birth control)

Combination agents are further divided into monophasic forms (constant dosage of both components during the cycle) and biphasic or triphasic forms (dosage of preparation components is changed once or twice during the cycle).

Monophasic

Biphasic
(days 1-10, 11-21)

Triphasic
(days 1-7, 8-14, 15-21)

Estrogen component:
Ethinyl-estradiol

Progestin component:
Levonorgestrel 
Desogestrel 
Drospirenone 
Norethisterone 
Cyproterone acetate
31
Q

Mechanism of action of contraceptives

A
  • Combinations of estrogens and progestins exert their contraceptive
    effect through selective inhibition of pituitary function (LH and FSH ↓),
    results in inhibition of ovulation (no LH surge)
  • Some agents also produce changes in the cervical mucosa, uterine
    endometrium, and motility and secretion of the uterine tubes; all of which decrease the likelihood of conception and implantation
32
Q

▪ Further clinical uses and beneficial effects of hormonal contraceptives

A
  • Prevent estrogen deficiency in young women with primary hypogonadism
  • Treatment of acne, hirsutism, dysmenorrhea, endometriosis
  • Combination hormonal contraceptives reduce the risk of ovarian cysts,
    endometrial cancer, benign breast cancer, pelvic inflammatory disease (PID)
  • Lower incidence of ectopic pregnancies, iron deficiency anemia, and
    rheumatoid arthritis
33
Q

Side effects of hormonal contraceptives

A

Mild:

  • Nausea
  • Edema
  • Endocrine disturbances
  • Headache
  • Withdrawal bleeding

Moderate:

  • Breakthrough bleeding
  • Weight gain
  • Skin pigmentation
  • Acne
  • Hirsutism
  • Ureteral dilation
  • Vaginal infections
  • Amenorrhea
Severe:
- Thromboembolism (MI, stroke, DVT, PE)
- GI disturbances
- Depression
- Increased risk of cervical
and breast cancer (?)
34
Q

▪ Contraindications of hormonal contraceptives

A
  • Recurrent thromboembolic/cardiovascular events
  • Estrogen-dependent neoplasm
  • Vaginal bleeding of unknown origin
  • Prior to epiphyseal closure
  • Smoking (?)
35
Q

emergency contraceptive

A

Postcoital contraceptive (‘emergency contraception’ or ‘morning-after pill’)

Prevent pregnancy if administered within 72 h’ after unprotected intercourse.

Preparations: high-dose progestin (levonorgestrel), or ulipristal acetate (SPEM).

Side effects: 
nausea, 
vomiting, 
headache, 
breast tenderness, 
abdominal pain.

Endocrinological Pharmacology (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions