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Pharmacology > Sex Hormones & Antagonists > Flashcards

Sex Hormones & Antagonists Flashcards

1
Q

Estradiol (E2)

A
  • Decrease causes GnRH release, then LH & FSH release, then making estrogen
  • Most in ovulation
  • 2-3% free, rest binded to SHBG
  • Different during day
  • Most estrogen before menopause
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2
Q

Estradiol decreased where?

A
  • Ovarian insufficiency
  • Turner’s syndrome
  • Hypothyroidism
  • PCOS
  • Menopause
  • Hypogonadism
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3
Q

Turner’s syndrome definition

A

Girls with one X or 2 defective chromosomes

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4
Q

Rubinstein-Taybi syndrome (RSTS)

A
  • تاخیر رشد
  • ناتوانی فکری
  • انگشتان بزرگ
  • مشکلات تغذیه‌ای (دیسفاژی)
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5
Q

Estradiol increases where?

A
  • Ovarian, testicular & adrenal tumors
  • Female Precocious puberty
  • Gynecomastia
  • Liver cirrhosis & necrosis
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6
Q

Drugs that decrease E2

A

OCPs
Clomifen

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7
Q

Drugs that increase E2

A
  • Adrenocorticosteroids
  • Ampicillin
  • Phenothiazines
  • Tetracyclines
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8
Q

Estrone (E1)

A
  • Weaker than E2
  • Made from androstendione peripheral conversion & E2 metabolism
  • Most estrogen after menopause
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9
Q

Estriol (E3)

A
  • Main esterogen in pregnancy
  • Made in adrenal, fetus liver, placenta
  • Important factor for fetus health
  • Checking from 28-30w, weekly
  • Same hour of the day
  • Screening down syndrome, natural tube defects
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10
Q

Estriol decrease where?

A
  • Preterm delivery
  • Pre-eclampsia
  • Anemia
  • Severe liver disease
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11
Q

Estriol increases where?

A
  • Multiple birth
  • Oxytocin use
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12
Q

Progesterone function

A
  • Reconstruction & Growth of endometrium
  • Preparation for egg implantation
  • Low progesterone starts period
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13
Q

Corpus luteum

A
  • Produces progesterone
  • If no fertilization, destroyed
  • If yes stays and changes into placenta
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14
Q

Progesterone clinical use

A

1- Ovulation check
2- Infertility reason check
3- Abnormal vaginal bleeding check
4- Placenta health
5- Keeping pregnancy in the beginning
6- Adrenal problems help
7- Ectopic pregnancy & miscarriage check

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15
Q

Testosterone (function, regulation, rhythm)

A
  • Spermatogenesis
  • Secondary sex characteristics
  • In women, estrogen precursor
  • Androgenic & anabolic
  • Hypophysis negative feedback (LH)
  • Mostly SHBG, some albumin & free
  • Morning most, evening least
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16
Q

Testosterone increase in women (causes & problems)

A

Causes:
- Adrenal & Ovarian tumor
- Adrenal hyperplasia
- Trophoblastic tumor
- PCO
Problems:
- Masculinization
- Amenorrhea
- Hirsutism

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17
Q

Drugs that increase testosterone

A
  • Clomifen
  • Anti-seizure drugs
  • Barbiturates
  • Estrogens
  • OCPs
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18
Q

Drugs that decrease testosterone

A
  • Androgens
  • Dexamethasone
  • Digoxin
  • Alcohol
  • Steroids
  • Ketoconazole
  • Phenothiazines
  • Spironolactone
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19
Q

Diseases that increase testosterone

A
  • Hyperthyroidism
  • Androgen Insensitivity Syndrome
  • Encephalitis
  • Hypothalamus tumor
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20
Q

Testosterone clinical use

A

1- Late or early pubert
2- Assessing in alternative therapies
3- When using anti androgens
4- Masculinizing in women
5- Checking PCOS
6- Diagnosing Androgen-making tumors

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21
Q

Antiestrogen types

A

1- Receptor antagonist (SERMs)
tamoxifen
2- Aromatase inhibitor
anastrozole

22
Q

Tamoxifen

A
  • Breast cancer
  • Infertility relative to oligomenorrhea or secondary amenorrhea
23
Q

Tamoxifen mechanism of action

A

SERMs
Selective Estrogen Receptor Modulator
Antagonistic in Breast & CNS
Agonistic in Liver & Bone

24
Q

Tamoxifen pharmacokinetic

A

Complete absorption

25
Q

Tamoxifen bio-availability

A

Pill & Liquid

26
Q

Tamoxifen protein binding

A

99%

27
Q

Tamoxifen liver metabolism

A

CYP2D6 & CYP3A4/5
- Changes into more active metabolites like:
Endoxifen, 4-hydroxy tamoxifen, n-desmethyl tamoxifen

28
Q

Tamoxifen half life

A

5-7 days
N-desmethyl tamoxifen:
14d

29
Q

Tamoxifen clearing

A

Stool (65%, less than 30% not conjugated)
Urine (9%)

30
Q

Tamoxifen side effects

A
  • Cardiovascular:
    Vasodilation, Hot flashes, HTN, Peripheral edema
  • Skin:
    Rash
  • Endocrine:
    Water retention, Weight loss, Amenorrhea
  • GI:
    Vomiting, Diarrhea
  • Genitourinary:
    Vaginal discharge, Irregular period, Vaginal bleed
31
Q

Anastrozole use & dose

A
  • Advanced breast cancer / in addition
  • Menopausal women
  • 1mg/d
32
Q

Anastrozole mechanism of action

A

Strong Aromatase inhibitor
Aromatase system: Peripheral conversion of androgens to estrogen

33
Q

Anastrozole side effects

A
  • most common GI problems
  • Hot flashes, dizziness, drowsiness, headaches
  • Hair thinning, dry vagina & bleed, edema, joint & muscular pain, bone breaking, fever, weight gain
34
Q

Anastrozole pharmacokinetic

A
  • Fast & GI tract
  • 2h peak plasma level
  • 40% plasma proteins binding
  • Consistent concentration after 7d if single daily dose
35
Q

Anastrozole metabolism, clearing, half life

A
  • Liver metabolism
  • Urine clearing (metabolites)
  • 50h half life
36
Q

Progestin antagonists (Anti-progesterones)

A
  • Danazol
  • Mifepristone
37
Q

Danazol uses

A
  • Hip area pain
  • Infertility because of endometriosis
  • Fibrocystic breast disease
  • Hereditary angioedema (men&women)
38
Q

Danazol common side effects

A
  • Weight gain
  • Acne
  • Masculinization
  • Oily hair & skin
  • Hair loss
  • Water retention
  • Hot flashes
  • Irritability
  • Dry vagina
  • Breast size decrease
39
Q

Danazol allergic side effects

A
  • Rashes
  • Itchiness
  • Face & tongue swelling
  • Vertigo
  • Hard breathing
40
Q

Danazol side effects in men

A
  • Decrease sperm making
  • Abnormal semen amount
  • Less sperms & less mobility
41
Q

Androgen Antagonists (Anti-testosterone)

A

1- 5α-Reductase Inhibitor
(Finasteride)
2- Synthesis Inhibitor
(Ketoconazole)

42
Q

Finasteride contraindication

A

Pregnancy
(Especially boys)

43
Q

OCP

Definition, examples

A
  • Estrogen-progesterone mix
  • Safe in low doses (< 50mg Ethinyl Estradiol)
    Examples:
  • Ethinyl estradiol
  • Norgesterel
44
Q

OCP mechanism of action

Total, Progesterone

A
  • Inhibition of ovulation if taken before peak of LH
    Progesterone:
  • Endometer not suitable for implantation
  • Endometrial atrophy
  • Cervix mucos thickening & prevents sperms
45
Q

OCP side effects

A
  • Nausea
  • NO increased sex appeal near ovulation
  • لک صورت
  • Change in fat & sugar metabolism
  • HTN & increased clotting
46
Q

OCP interactions

A
  1. Phenobarbital (gets pregnant)
  2. Simetidine
  3. Grapefruit
  4. Alcohol
  5. Phenytoin
    2-6 cause overdose
47
Q

OCP other effects

A
  • Less period bleeding & pain
  • Less ectopic
  • Better for endometriosis
  • Less hirsutism
  • Less pimples
  • More bone density
  • Less ovarian & cervix cancer
  • Less benign breast diseases
  • Regulating menstruation
  • Less simple ovarian cyst
48
Q

Ethinyl estradiol

Type, Mechanism, pharmacokinetic, Side effects & interactions

A
  • Estrogen receptor activation
  • P450, Liver-intestine
  • Moderate: Bleed in between cycles, nausea
  • Severe: Thromboembolism, HTN
49
Q

Norgestrel

Type, Mechanism, pharmacokinetic, Side effects & interactions

A
  • Progestreone receptor activation
  • P450, liver-intestine
  • Weight gain, reversible bone density decrease (high doses)
50
Q

Clomifen

A
  • Estrogen receptor agonist to induce ovulation
  • Antagonistic in pituitary to increase GnRH

Pharmacology (6 decks)

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