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Pharmacology > Gonadal Hormones Drugs > Flashcards

Gonadal Hormones Drugs Flashcards

1
Q

what are the 2 events of ovarian phase?

A

preovulatory phase = follicular phase
postovulatory phase = luteal phase

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2
Q

what are the uterine endometrial phases?

A

Preovulatory phase = proliferative phase
postovulatory phase = secretory phase

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3
Q

what are the different effects of Estrogen?

A

INC in size of uterus, fallopian tubes, vagina, & external genitalia

Thickening of vaginal epithelium (dyspareunia)

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4
Q

what is the basis of fertility awareness method used for family planning or contraception?

A

Spninnbark estrogen in the Uterus

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5
Q

Why are menopausal women more prone to osteoporosis and fractures?

A

Estrogen decreases bone resporption

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6
Q

WHat are the other effects of estrogen in the body?

A

Favorable lipid profile EXCEPT for TAGS
INC CBG, TBG, SHBG, Transggerrin & renin substrate
INC 1972 factors
INC gallstone formation
SUppression of FSH

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7
Q

WHat are the therapeutic uses of Estrogen?

A
  1. Replacement —> Menopause, Primary Hypogonadism
  2. Correct hormonal imablance —> Dysfunctional uterine bleeding
  3. Reverse an abnormal/unwanted process —> Dysemnorrhea, Acne, hirsutism, male breast & prostate cancer
  4. Contraception
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8
Q

What are C/Is of Estrogen?

A

Estrogen-dependent neoplasms
Undiagnosed genital bleeding
Thromboembolic disorders
Liver disease
Heavy smokers
Pregnancy

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9
Q

WHat are the goals of menopausal hormone therapy?

A

Relief of vasomotor symptoms
Tx of genitourinary symptoms
Tx of vulvovaginal symptoms
Prevention of bone fractures
CVS benefit if it starty early (<60yo, within 10 yrs of menopause)

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10
Q

What do we call amenorrhea that is <1 yr?

A

Perimenopause

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11
Q

What are the diff selective estrogen receptor modulator?

A

Tamoxifen
Raloxifene
Clomiphene

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12
Q

What is the MOA of Tamoxifen, therapeutic use & important AEs?

A

MOA:
Breast —> binds to ER w/o activating them —> prevents Estrogen from binding

Uterus —> activates Estrogen receptors —> uterine cell proliferation

Use: Palliative tx in ER-positive breast cancer

AE: Deep vein thrombosis (lethal), INC risk of endometrial cancer hot flashes

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13
Q

What is the use of Raloxifene?, & important AE?

A

Use: prevention & tx of postmenopausal osteoporosis, breast cancer prevention

AE: DVT, hot dlashes

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14
Q

What is the MOA of Clomiphene, Therapeutic use, & AE?

A

MOA: Increases Gonadotropin secretion

Use: PCOS (Induction of ovulation)

AE: Ovarian enlargement (significant), multiple births, hot flshes, eye symptoms

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15
Q

What are the 2 anti-estrogens?

A

Aromatase inhibitors
Estrogen receptor blocker

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16
Q

What is the MOA of Aromatase inhibtors & drugs?

A

Inhibit the enzyme which converts androgen (testosterone) to androgen

AnasTROZOLE
Exemestane
LeTROZOLE

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17
Q

What is the use of prescribing anti-estrogens?

A

breast cancers that are R to Tamoxifen

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18
Q

What is the MOA of Estrogen recpetor blocker & drug unde rit?

A

Prevents dimerization

FUlvestrant

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19
Q

What is the MOA of Progestins?

A

Similar to Estrogens & Steroids

INC in transcription of target genes in sensitive tissues

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20
Q

What are co-repressors of Progestins?

A

Progesin recpetor modulator
Antagonist (Mifepristone)

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21
Q

What are the effects of Progestin in the uterus?

A

DEC uterine motility
Cervical discharge
Endometrium —> secretory changes —> support embyro impant if pregnnacy occurs

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22
Q

What is the effect of Progestin in the breast?

A

Acinar & lobular development

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23
Q

What are the effects of Progestin to the brain?

A

DEC GnRH pulse in hypothalamus —> neg feedback
DEpressant or hypnotic effets —> taken at night to improve sleep
Thermogenic effect —> INC basal body temperature

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24
Q

What type of chart is used by women to track their temperature upon waking up? WHy is this done?

A

Basal body temperature

Determine if woman ovulates & fertility awareness method of contraception

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25
Q

What are the other effects of Progestin?

A

INC LDL w/ no change or slight DEC in HDL
Mild catabolic effect
Natriuretic effect

26
Q

What is the use of synthetic Progesterone?

A

Menopausal hormone treatment

27
Q

What are the 4 synthetic preparation of Progesterone?

A

21-Carbon progesterone analogs (Pregnanes)
19-Nortestosterone 13-Methyl derivatives (Estranes)
19-Nortestosterone 13-Ethyl derivatives (Gonanes)
With Anti-andronergic. & Anti-Mineralocorticoid effect

28
Q

WHat are the diff Pregnanes?

A

Dydrogesterone
Medroxyprogesterone
Megestrol

29
Q

What synethic preparation of Progesterone has little or no adrogenic effect?

A

L-Norgesterol
Desogesterol
Etonegesterel

30
Q

What are the AEs of Progestins?

A

INC in BP
DEC HDL
INC risk of breast carcinoma

31
Q

WHat are the therapeutic uses of Progestin?

A

Contraception
MHT/EPT
Ovarian suppression
Dysfunctional uterine bleeding
Threatened miscarriage

32
Q

WHat are the diff femal hormonal contraception?

A
  1. COmbined Estrogen + Progestin
  2. Progestin-only Contraceptives
  3. Emergency/Post-coital contraceptives
  4. Family planning methods
33
Q

What are the MOA of Combined Estrogen + Progestin?

A

Inhibit ovulation —> DEC FSH, DEC LH

ALters the endometrium —> x impalantation of embryo
Alters cervical mucus —> x penetrated by sperm
DEC fallopian tube secretion & motility

34
Q

What are the diff forms of combined estrogen-Progestins/Oral contraceptives?

A

Oral contraceptive pills
Vaginal ring
Dermal patch

35
Q

What are the 2 oral contraceptive pills?

A

Monophasic COCs
Multiphasic COCs

36
Q

Can you interchange use of tablets in multiphasic COCs?

A

No, all COCs must be taken at the same time for 21 days followed by a 7 day pill free period

37
Q

What combination of Estorgen & Progesterone in Vaginal ring?

A

Etonogestrel (Progestin) & Ethinyl estradiol

38
Q

WHat combined estrogen & progestin use used in dermal patches?

A

Norelgestromin & Ethinyl Estradiol => applied in skin every wk for 3 wks => another patch is applied a week after

39
Q

What are AEs of Combined estrogen & Progestin?

A

Risk for CVS complciations
Risk for cancers

40
Q

What are C/Is of Combined estrogen + Progestin?

A

Hx of thrombophlebitis, thromboembolic disease, CVS disease, or coronary artery disease

Markedly impaired liver function & liver tumors

Congeintal hyperlipidemia
Heavy smokers > 35 yo
Migraine w/ focal aura
DM w/ vascular involvement or >20yrs
Uncontrolled HTN
Breastfeeding <6wks postpartum
Major surgery w/ prolonged immobilization

41
Q

What are the MOA of Progestin-Only contraceptives?

A

Thicken cervival mucus
Alter endometrium
Inhibit ovulation

42
Q

What are the indicatoins of Progestin-only contraceptives?

A

Hepatic disease
HTN
Psychosis
Prior thromboembolism

43
Q

What are C/I ofo Progesitn-only contraceptives?

A

Current preggos
Breast cancer
Acute liver disease
Liver tumors
Undiagnose abnormal genital bleeding

44
Q

What are the diff forms of Progestin-only contraceptives?

A

Oral
Parenteral
Intrauterine system
Progestin implants

45
Q

What are “mini pills” or Progestin-only pills? What are it C/Is?

A

Lynestrenol (oral prep of Progestin-only)
ABSOLUTE C/I: Preggos, breast cancer

46
Q

What are AEs of Parenteral (DMPA) Progesterone-only contraceptives?

A

Breakthrough bleeding
Delayed conception
DEC HDL, INC LDL
Weight gain
Loss of bone mineral density

47
Q

WHat are C/Is of DMPA?

A

Breast cancer & Preggos

48
Q

What is the MOA of Levonorgestrel (intrauterine system of Progesterone-only contraceptive)?

A

Inhibit fertilization
Inhibt implantation

49
Q

What are AEs of Progestin-only contraceptives?

A

Irregular breakthrough bleeding —>Amenorrhea
Does not impair breast milk production unlike Estrogens & Do not INC risk of thromboembolism

50
Q

When should Emergency/Post-coital contaceptives be taken?

A

Taken w/in 72 hrs-120 hrs

51
Q

What are the 3 examples of emergency contraceptives?

A

Progestin
Combined Estrogen-Progestin
Selective Progesterone-Receptor Modulator

52
Q

What is the MOA of Androgens?

A

Converted by 5a-reductase to Dihdyrotestosterone —> binds to the androgen receptor in the cytoplsm

53
Q

What are the side effects of Androgens?

A

Early fetal life
Puberty
Necessary for spermatogenesis
Anabolic
INC renaly EPO secretion & RBCs
DEC HDL in high doses
Inhibition of APG via neg feedback

54
Q

What are the therapeutic uses of Androgens?

A

Androgen replacment therapy => Male hypogonadism, Andropause, male climcateric, ADAM

GYN use => postpartumbreast engorgement & female breast carcinoma

Improvement performance in sports

55
Q

What are AEs of Androgens?

A

Diminished fertility (Most imprtant)
Erythrocytosis with high doses
DEC HDL, INC LDL w/ high doses
Gynecomastia

56
Q

What are C/I of Androgens?

A

Preggos
Males w/ prostatic/breast cancer
Infants & young children

57
Q

What are the diff anti-androgens?

A

Competitive antagonists
5a-reductase inhibitors

58
Q

What are the diff competitive antagonists & its MOA?

A

Cyproterone Acetate
Flutamide
Bicalutamide
Spironolactone

MOA: Blocks the action of testosterone on the internal genitalia, SM, erythropoiesis & bone

59
Q

What are the uses & AEs of competitive antagonists?

A

Uses: Prostatic cancer, Hirsutism, Virilizing syndromes, male precocious puberty

AE: Gynecomastia

60
Q

What are the 2 5a-reductase inhibitors? MOA?

A

Finasteride
Dutasteride

MOA: Inhibits the eynzme that converts testosterone to DHT, preventing DHT effects on the external genitalia

61
Q

What are hte uses of 5a-reductase inhibtors & AEs?

A

Uses:
Benign prostatic hyperplaia
Male baldness
Female hirsutism

AE: Importence & DEC libido

Pharmacology (19 decks)

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