[8] Drugs for Reproductive Endocrinology Flashcards

1
Q

Testosterone is converted to DHT via?

A

5-alpha Reductase

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2
Q

Testosterone is converted to Estradiol via?

A

Aromatase

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3
Q

Common precursor of androgen and estrogen

A

Progesterone

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4
Q

Most potent form of estrogen

A

Estradiol

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5
Q

Steroid hormones are derived from?

A

Cholesterol

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6
Q

In postmenopausal women, hormones come from?

A

Adipose tissue

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7
Q

Adrenal Medulla produces which adrenal hormones

A

Norepinephrine

Adrenaline

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8
Q

Glomerulosa layer produces

A

Aldosterone

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9
Q

Fasciculata produces

A

Glucocorticoids

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10
Q

Reticularis produces

A

Sex Hormones

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11
Q

Adrenal Cortex produces which adrenal hormones

A

Androgens

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12
Q

[T/F] There is complete selectivity between Progestins, Androgens, and Estrogens

A

F, their close structural similarities make cross reactivity possible

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13
Q

Location of LH Receptors in Males

A

Leydig Cells

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14
Q

Location of FSH Receptors in Males

A

Sertoli Cells

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15
Q

Effect of LH binding on Males

A

Increased testosterone synthesis

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16
Q

Effect of FSH binding on Males

A

Increased Androgen Binding Protein synthesis

Increased Sperm Cells

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17
Q

Location of LH Receptors in Females

A

Thecal Cells

18
Q

Location of FSH Receptors in Females

A

Granulosa Cells

19
Q

Effect of LH binding on Females

A

Increased Androgen Synthesis (Androstenedione)

20
Q

Effect of FSH binding on Females

A

Increased aromatase activity (conversion of testosterone -> estradiol)

21
Q

Increase in basal body temperature is from progesterone or estrogen?

A

Progesterone

22
Q

Orally active form of Estorgen

A

Ethinyl Estradiol

23
Q

Central Effect of COC

A

Progestin suppresses LH secretion

Estrogen suppresses FSH

24
Q

Peripheral Effect of COC (3)

A
  1. Reduced sperm transport
  2. Changed endometrium
  3. Thickened cervical mucosa
25
Q

What component of COCs increase the chance of Thrombosis?

A

Estrogen: Increases production of clotting factors 1972 (IX, X, VII, II)

26
Q

Effect of OCs on MI and Stroke

A

No increased risk

27
Q

What component of COCs affect Carbohydrate Metabolism

A

Progestin component affects insulin sensitivity

28
Q

[Effect of OCs]

Endometrial Cancer
Ovarian Cancer
Breast Cancer

A

E: Reduced by 50%

O: Reduced by 40-80% depending on time

B: MAY be associated with 20% increased risk

29
Q

Preferred oral contraceptives for Lactating Women

A

Progestin-Only Pills (Minipill)

No effect on quantity or quality of breastmilk

30
Q

This drug is used in palliative treatment in postmenopausal women with breast CA but may increase the risk of endometrial CA

A

Tamoxifen

31
Q

This drug is approved for prevention of postmenopausal osteoporosis and is a partial agonist-antagonist in target tissues

A

Raloxifene

32
Q

1st line drug for ovulation induction

A

Clomiphene Citrate

33
Q

This must be supplemented with Clomiphene to allow fetus implantation

A

Estrogen (Since Clomiphene is an antagonist to uterine tissues)

34
Q

This drug is a pure estrogen receptor antagonist

A

Fulvestrant

35
Q

Most important androgen secreted by the testis

A

Testosterone

36
Q

% Free Testosterone

A

2%

37
Q

Route of Administration of Testosterone

A

Transdermally or parenterally, ineffective when given orally

38
Q

Why is GnRH released in a pulsatile fashion?

A

Continuous administration of GnRH causes depression of pituitary activity

39
Q

Mechanism of Action: Leuprolide

A

GnRH Agonist

Suppresses gonadotropin secretion and inhibits ovarian production of estrogens and progesterone

40
Q

Mechanism of Action: Ganirelix and Cetrorelix

A

GnRH Antagonist

41
Q

Mechanism of Action: Cyproterone acetate

Uses

A

Androgen Receptor Antagonist

Treatment of hirsutism