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Pharmacology- Katzung (Spring 2019) > Endocrine Drugs - Gonadal Hormones And Inhibitors > Flashcards

Endocrine Drugs - Gonadal Hormones And Inhibitors Flashcards

1
Q

What are the clinical applications of ethinyl estradiol?

A
  1. Hypogonadism in girls and women.
  2. Oral hormonal contraceptive.
  3. Intractable dysmenorrhea or uterine bleeding.
  4. Parenteral contraceptive.
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2
Q

What are the pharmacokinetics of ethinyl estradiol?

A
  1. Oral/parenteral/transdermal administration.
  2. Metabolism relies on cytochrome P450 systems.
  3. Enterohepatic recirculation occurs.
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3
Q

What are the features of ethinyl estradiol’s moderate toxicity?

A
  1. Breakthrough bleeding
  2. Nausea
  3. Breast tenderness
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4
Q

What are the features of ethinyl estradiol’s serious toxicity?

A
  1. Thromboembolism
  2. Gallbladder disease
  3. Hypertriglyceridemia
  4. Migraine headache
  5. Hypertension
  6. Depression
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5
Q

What is the toxicity of ethinyl estradiol in post menopausal women?

A
  1. Breast cancer

2. Endometrial hyperplasia (unopposed estrogen)

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6
Q

What complication might follow if ethinyl estradiol is combined with a CYP450 inducer?

A

Can lead to breakthrough bleeding and reduced contraceptive efficacy.

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7
Q

What is the mestranol?

A

A prodrug that is converted to ethinyl estradiol, contained in some contraceptives.

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8
Q

What is the mechanism of action of norgestrel?

A

Activation of progesterone receptor leads to changes in the rates of transcription of progesterone-regulated genes.

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9
Q

What are the clinical applications of norgestrel?

A
  1. Oral hormonal contraceptive
  2. Parenteral contraceptive
  3. Post coital contraceptive
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10
Q

What are the pharmacokinetics of norgestrel?

A
  1. Oral/parenteral/transdermal administration.
  2. Metabolism relies on CYP450.
  3. Enterohepatic circulation.
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11
Q

What are the toxicities of norgestrel?

A
  1. Weight gain

2. Reversible decrease in bone mineral density (high doses).

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12
Q

Mention 2 progesterone derivatives.

A
  1. Medroxyprogesterone acetate

2. Megestrol acetate

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13
Q

Mention 2 older 19-nortestosterone derivatives.

A
  1. Norethindrone

2. Ethynodiol

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14
Q

Mention 4 newer 19-nortestosterone derivatives.

A
  1. Desogestrel
  2. Norelgestromin
  3. Norgestimate
  4. Etonogestrel
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15
Q

Mention a spironolactone derivative.

A

Drospirenone.

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16
Q

Mention a major selective estrogen receptor modulator (SERM).

A

Tamoxifen

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17
Q

What is the mechanism of action of tamoxifen?

A
  1. Estrogen antagonist actions in breast tissue and CNS.

2. Estrogen agonist effects in liver and bone.

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18
Q

What is the clinical application of tamoxifen?

A

Prevention and adjuvant treatment of hormone-responsive breast cancer.

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19
Q

How is tamoxifen administered?

A

Orally

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20
Q

What are the toxicities of tamoxifen?

A
  1. Hot flushes
  2. Thromboembolism
  3. Endometrial hyperplasia
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21
Q

Mention a similar drug to tamoxifen?

A

Toremifene

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22
Q

What is the mechanism of action of raloxifene?

A

Antagonist effects in breast, CNS, and endometrium and agonist effects in the liver.

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23
Q

What are the clinical applications of raloxifene?

A

Approved for osteoporosis and prevention of breast cancer in selected patients.

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24
Q

What is the mechanism of action of clomiphene?

A

Antagonist effect in pituitary increases gonadotropin secretion.

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25
Q

What is the clinical application of clomiphene?

A

Used for ovulation induction.

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26
Q

What is the mechanism of action of fulvestrant?

A

Estrogen receptor antagonist in all tissues.

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27
Q

What is the clinical application of fulvestrant?

A

Adjuvant treatment of hormone-responsive breast cancer that is resistant to first-line antiestrogen therapy.

28
Q

How is fulvestrant administered?

A

IM

29
Q

What are the toxicities of fulvestrant?

A
  1. Hot flushes
  2. Headache
  3. Injection site reactions
30
Q

What is the mechanism of action of anastrozole?

A

Reduces estrogen synthesis by inhibiting aromatase enzyme.

31
Q

What is the clinical application of anastrozole?

A

Adjuvant treatment of hormone-responsive breast cancer.

32
Q

How is anastrozole administered?

A

Orally

33
Q

What are the toxicities of anastrozole?

A
  1. Hot flushes
  2. Musculoskeletal disorders
  3. Reduced bone mineral density
  4. Joint symptoms (Arthralgias, arthritis, arthrosis, cervical spondylosis, osteoarthritis, and disk herniation)
34
Q

Mention a drug similar to anastrozole?

A

Letrozole

35
Q

Mention an irreversible aromatase inhibitor.

A

Exemestane

36
Q

What is the mechanism of action of danazol?

A

Weak CYP450 inhibitor and partial agonist of progestin and androgen receptors.

37
Q

What is the clinical application of danazol?

A

Endometriosis and fibrocystic breast disease.

38
Q

How is danazol administered?

A

Orally

39
Q

What are the toxicities of danazol?

A
  1. Acne
  2. Hirsutism
  3. Weight gain
  4. Menstrual disturbances
  5. Hepatic dysfunction
40
Q

What is the mechanism of action of mifepristone?

A

Progestin and glucocorticoid receptor antagonist.

41
Q

What is the clinical application of mifepristone?

A

Used in combination with a prostaglandin (misoprostol) for medical abortion.

42
Q

How is mifepristone administered?

A

Orally

43
Q

What are the toxicities of mifepristone?

A
  1. GI disturbances (mostly due to coadministration of misoprostol).
  2. Vaginal bleeding
  3. Atypical infection
44
Q

What is the mechanism of action of testosterone?

A

Androgen receptor agonist

45
Q

What are the clinical applications of testosterone?

A
  1. Male hypogonadism

2. Weight gain in patients with wasting syndromes

46
Q

How is testosterone administered?

A
  1. Transdermal
  2. Buccal
  3. SC implant
47
Q

What are the toxicities of testosterone?

A

In females –> virilization

In males –> high doses can cause gynecomastia, testicular shrinkage, infertility.

48
Q

Mention 2 oral androgens.

A
  1. Fluoxymesterone

2. Methyltestosterone

49
Q

What is the clinical use of testosterone esters?

A

Long-acting androgens for parenteral administration.

50
Q

Mention 2 anabolic steroids.

A
  1. Oxandrolone

2. Nandrolone decanoate

51
Q

What can anabolic steroids cause?

A
  1. Increased ratio of anabolic-to-androgenic activity in lab animals.
  2. Cholestatic jaundice
52
Q

What is the mechanism of action of finasteride?

A

Inhibition of 5α-reductase that converts testosterone to dihydrotestosterone.

53
Q

What is the clinical application of finasteride?

A
  1. BPH

2. Male-pattern hair loss

54
Q

How is finasteride administered?

A

Orally

55
Q

What are the toxicities of finasteride?

A

Rarely –> impotence and gynecomastia.

56
Q

Mention a drug similar to finasteride.

A

Dutasteride

57
Q

What is the mechanism of action of flutamide?

A

Competitive inhibition of androgen receptor.

58
Q

What is the clinical application of flutamide?

A

Advanced prostate cancer.

59
Q

How is flutamide administered?

A

Orally

60
Q

What are the toxicities of flutamide?

A
  1. Gynecomastia
  2. Hot flushes
  3. Impotence
  4. Hepatotoxicity
61
Q

Mention 2 drugs similar to flutamide, but with lower risk for hepatotoxicity.

A
  1. Bicalutamide

2. Nilutamide

62
Q

What diuretic is also used for the treatment of hirsutism?

A

Spironolactone

63
Q

What is the mechanism of action of ketoconazole?

A

Inhibition of CYP450 enzymes involved in androgen synthesis.

64
Q

What is the clinical application of ketoconazole?

A

Advanced prostate cancer that is resistant to first-line antiandrogen drugs.

65
Q

How is ketoconazole administered?

A

Orally

66
Q

What are the toxicities of ketoconazole?

A
  1. Interferes with synthesis of other steroids.

2. Many drug interactions due to CYP450 inhibition.

67
Q

What is the mechanism of action of ethinyl estradiol?

A

Activation of estrogen receptors leads to changes in the rates of transcription of estrogen-regulated genes.

Pharmacology- Katzung (Spring 2019) (52 decks)

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