Repro - Pharmacology Flashcards

1
Q

What effect do GnRH agonists have on the reproductive HPA axis?

A

GnRH agonists are stimulatory if given as pulses, inhibitory if given continuously

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2
Q

What effect does anastrozole have on the female HPA axis?

A

It is an aromatase inhibitor that prevents estrogen formation from androgens

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3
Q

What is the mechanism of action and result of finasteride administration?

A

It is an reductase inhibitor that blocks the conversion of testosterone to dihydrotestosterone

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4
Q

How do the clinical uses of leuprolide differ depending on the way in which it is administered?

A

Leuprolide is a gonadotropin-releasing hormone agonist when dosed in a pulsatile fashion and a gonadotropin-releasing hormone antagonist when dosed continuously

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5
Q

What adverse effects are associated with leuprolide use?

A

Antiandrogenic actions, nausea, and vomiting

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6
Q

Name three common clinical uses for leuprolide.

A

Infertility (pulsatile), prostate cancer (continuous, used with flutamide), and uterine fibroids

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7
Q

Is leuprolide dosed in a pulsatile or continuous fashion for the treatment of prostate cancer? Why?

A

Leuprolide is given continuously to inhibit gonadotropin-releasing hormone; this decreases circulating androgens that can stimulate prostate adenocarcinoma

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8
Q

How can testosterone be used to treat hormonal deficiencies?

A

Administration of testosterone can be used in hypogonadism and to help develop secondary sexual characteristics

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9
Q

What is the role of testosterone in patients who have suffered from a burn?

A

Testosterone stimulates anabolism, which helps promote recovery from burns or other severe injuries

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10
Q

What role can testosterone play in the treatment of a malignancy generally seen in women?

A

Testosterone can be used to treat estrogen receptor-positive breast cancer

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11
Q

What genital exam finding would you expect in a male using exogenous testosterone?

A

Testicular atrophy; because exogenous testosterone blocks the release of luteinizing hormone, intratesticular testosterone will decrease, causing testicular atrophy

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12
Q

How would exogenous testosterone affect the height of a child that has not completed puberty?

A

This child may be shorter than expected because of premature closure of the epiphyseal plates

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13
Q

What serum lipid panel findings would you expect in a patient who has been taking testosterone?

A

Elevated low-density lipoprotein and decreased high-density lipoprotein

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14
Q

What is the mechanism of action of finasteride?

A

Finasteride is a reductase inhibitor, which blocks the conversion of testosterone to the more potent dihydrotestosterone

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15
Q

What is the mechanism of action of flutamide?

A

Competitive testosterone receptor antagonist

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16
Q

Name two drugs that function as antiandrogens as an additional effect of their interference with steroid signaling.

A

Ketoconazole (an antifungal) blocks desmolase, decreasing steroid synthesis; spironolactone (a diuretic) blocks steroid binding

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17
Q

What are two adverse effects common to both ketoconazole and spironolactone?

A

Gynecomastia and amenorrhea

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18
Q

Flutamide is used to treat what condition?

A

Prostate carcinoma

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19
Q

What antiandrogenic drugs can be used to treat the hirsutism associated with polycystic ovarian syndrome?

A

Ketoconazole or spironolactone

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20
Q

What are the mechanisms of action of ethinyl estradiol, diethylstilbestrol, and mestranol?

A

Binding to estrogen receptors and acting as agonists

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21
Q

Name four conditions in women that are treated with estrogens.

A

Hypogonadism, ovarian failure, menstrual abnormalities; and as hormone replacement therapy in postmenopausal women

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22
Q

Name a condition in elderly men that can be treated with estrogens

A

Androgen-dependent prostate cancer

23
Q

What are the adverse effects of treatment with exogenous estrogens?

A

An increased risk of endometrial carcinoma, abnormal uterine bleeding in postmenopausal women, and hypercoagulability

24
Q

You diagnose a woman with clear-cell adenocarcinoma of the vagina; what should you ask about in her history?

A

In utero exposure to diethylstilbestrol

25
Q

Name two conditions that are contraindications to estrogen therapy.

A

Estrogen receptor-positive breast cancer and a history of deep vein thrombosis

26
Q

How does the interaction of clomiphene at the hypothalamus result in an increase in ovulation?

A

Clomiphene is a partial estrogen receptor agonist at the hypothalamus, blocking negative feedback on luteinizing hormone and follicle-stimulating hormone; elevated follicle-stimulating hormone and luteinizing hormone cause increased ovulation

27
Q

What are two primary clinical uses for clomiphene?

A

The treatment of infertility and polycystic ovarian syndrome

28
Q

What are four adverse effects associated with clomiphene use?

A

Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances

29
Q

How is tamoxifen used in breast cancer?

A

Because it acts as an estrogen antagonist in the breast, it is used to treat and prevent recurrences of breast cancer in estrogen receptor-positive tumors

30
Q

Which selective estrogen receptor modulator reduces the resorption of bone and is used to treat osteoporosis?

A

Raloxifene; it acts as an estrogen receptor agonist in bones

31
Q

What are indications for hormone replacement therapy?

A

Menopausal symptoms (eg, hot flashes, vaginal atrophy) and osteoporosis that is caused by decreased estrogen levels

32
Q

In hormone replacement therapy, unopposed estrogen can increase the risk of what disease?

A

Endometrial cancer; it also may increase the risk of cardiovascular events

33
Q

Why is progesterone added to hormone replacement therapy?

A

To reduce the risk of endometrial cancer

34
Q

What is the mechanism of action of anastrozole and exemestane?

A

Anastrozole and exemestane function by inhibiting aromatase, the enzyme that converts androgens to estrogens

35
Q

In what clinical scenario are anastrozole and exemestane used?

A

In postmenopausal women with hormone-responsive breast cancer

36
Q

What effect do progestins have on the endometrium?

A

Upon binding the progesterone receptor, they reduce the growth of the endometrial lining while increasing its vascularization

37
Q

Name three clinical uses of progestins.

A

In oral contraceptive pills, to treat endometrial cancer, and to treat abnormal uterine bleeding

38
Q

What is the mechanism of action of mifepristone (RU-486)?

A

It is a competitive inhibitor of progestins at progesterone receptors

39
Q

What is the primary clinical use of mifepristone?

A

Termination of pregnancy in conjunction with the administration of misoprostol (PGE1)

40
Q

What are the known toxicities of mifepristone?

A

Heavy bleeding, gastrointestinal effects (nausea, vomiting, anorexia), and abdominal pain

41
Q

How reliable are oral contraceptive pills in the prevention of pregnancy?

A

They are very reliable (<1% failure when used correctly) but must be taken daily to be effective

42
Q

What is the effect of oral contraceptive pills on malignancy?

A

Women taking oral contraceptive pills have lower rates of endometrial and ovarian cancer

43
Q

A woman who takes oral contraceptive pills asks you about her risk for ectopic pregnancy; what is the relationship between the two?

A

Oral contraceptive pills decrease the risk of ectopic pregnancy (and pregnancy in general)

44
Q

Name six systemic adverse effects of oral contraceptive pills.

A

Elevated triglycerides, hypertension, depression, weight gain, nausea, and hypercoagulability

45
Q

How do oral contraceptive pills work?

A

They work by preventing an estrogen surge and thus the luteinizing hormone surge that causes ovulation

46
Q

Dinoprostone is an analogue of what molecule?

A

PGE2

47
Q

How is dinoprostone used in pregnancy?

A

Dinoprostone causes cervical dilation and uterine contractions, inducing labor

48
Q

What is the role of ritodrine and terbutaline during labor?

A

These are β2-agonists, which relax the uterus and reduce contractions (remember: ritodrine allows the fetus to “return to dreams” by stopping premature labor)

49
Q

What is the mechanism of action of tamsulosin?

A

Tamsulosin is an α1-receptor agonist used to treat benign prostatic hyperplasia

50
Q

Why does tamsulosin relax the smooth muscles of the prostate but not the systemic vasculature?

A

It is selective for α1AD-receptors found on the prostate, rather than the α1B-receptors on systemic vessels

51
Q

What is the primary clinical use for sildenafil and vardenafil?

A

The treatment of erectile dysfunction (remember: sildenafil and vardenafil fill the penis)

52
Q

A patient presents with symptoms of flushing, reflux, headache, and blue-green vision; what drug has he likely ingested?

A

Sildenafil or vardenafil (remember: Hot and sweaty, but then Headache, Heartburn, Hypotension)

53
Q

Sildenafil and vardenafil should not be used in patients taking what other class of drug?

A

Nitrates; the concomitant use can precipitate life-threatening hypotension

54
Q

How do sildenafil and vardenafil cause the increase of penile blood flow and resultant erection?

A

By inhibiting cGMP phosphodiesterase, there is an increase in cGMP resulting in increased nitric oxide and smooth muscle relaxation in the corpus cavernosum