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Male Genital System > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is the mechanism of leuprolide?

A

GnRH analog with agonist properties when used in pulsatile fashion; antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary → decreased FSH/LH)

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2
Q

Clinical use of leuprolide

A

Infertility (pulsatile)

Prostate cancer (continuous – use with flutamide)

Uterine fibroids

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3
Q

Toxicity of leuprolide

A

Antiandrogen

Nausea

Vomiting

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4
Q

Mechanism of testosterone

A

agonist at androgen receptors

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5
Q

Clinical use of testosterone

A

Treats hypogonadism and promotes development of secondary sex characteristics

Stimulation of anabolism to promote recovery after burn or injury

Treats ER-positive breast cancer (exemestane)

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6
Q

Toxicity of testosterone

A

Causes masculinization in females

Reduces intratesticular testosterone in males inhibiting release of LH (via neg. feedback), leading to gonadal atrophy

Premature closure of epiphyseal plates

Increase LDL

Decreased HDL

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7
Q

What are the 4 antiandrogen drugs?

A

Finasteride

Flutamide

Ketoconazole

Spironolactone

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8
Q

Mechanism of finasteride

A

5a-reductase inhibitor which decreases T conversion to DHT

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9
Q

Clinical use of finasteride

A

Useful in BPH

Promotes hair growth (treat baldness)

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10
Q

Mechanism of flutamide

A

Nonsteroidal competitive inhibitor of androgens at the testosterone receptor

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11
Q

Clinical use of flutamide

A

Used in prostate carcinoma

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12
Q

Mechanism of ketoconazole

A

Inhibits steroid synthesis (inhibits desmolase)

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13
Q

Mechanism of spironolactone

A

Inhibits steroid binding

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14
Q

Clinical use of ketoconazole

A

Tx of polycystic ovarian syndrome to prevent hirsutism

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15
Q

Side effect of spironolactone

A

Side effect of gynecomastia and amenorrhea

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16
Q

Side effect of ketoconazole

A

Side effect of gynecomastia and amenorrhea

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17
Q

Clinical use of spironolactone

A

Used in Tx of polycystic ovarian syndrome to prevent hirsutism

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18
Q

What are the estrogen drugs?

A

Ethinyl estradiol

DES

Mestranol

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19
Q

Mechanism of estrogens

A

Bing to estrogen receptors

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20
Q

Clinical use of estrogens

A

Hypogonadism or ovarian failure

Menstrual abnormalities

HRT in postmenopausal women

Use in men with androgen-dependent prostate cancer

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21
Q

Toxicity of estrogens

A

Increased risk of:

Endometrial cancer

Bleeding in postmenopausal women

Clear cell adenocarcinoma of vagina in females exposed to DES in utero

Increased risk of thrombi

Contraindications: ER-positive breast cancer, history of DVTs

22
Q

What are the selective estrogen receptor modulator drugs?

A

Clomiphene

Tamoxifen

Raloxifene

23
Q

Mechanism of clomiphene

A

Partial agonist at estrogen receptors in hypothalamus

Prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation

24
Q

Clinical use of clomiphene

A

Used to treat infertility and PCOS

25
Q

Toxicity of clomiphene

A

Hot flashes

Ovarian enlargement

Multiple simultaneous pregnancies

Visual disturbances

26
Q

Mechanism of tamoxifen

A

Estrogen antagonist on breast tissue

27
Q

Clinical use of tamoxifen

A

Treat and prevent recurrence of ER-positive breast cancer

28
Q

Mechanism of raloxifene

A

Estrogen agonist on bone

29
Q

Clinical use of raloxifene

A

Reduces resorption of bone

used to treat osteoporosis

30
Q

Clinical use of HRT

A

Used for relief or prevention of menopausal symptoms and osteoporosis

31
Q

Toxicity of HRT

A

Unopposed estrogen replacement therapy increases the risk of endometrial cancer, so progesterone is added

Possible increased CV risk

32
Q

What is the mechanism and use of anastrozole/exemestane?

A

Aromatase inhibitors used in postmenopausal women with breast cancer

33
Q

Mechanism of progestins

A

Bind progesterone receptors, reduce growth and increase vascularization of endometrium

34
Q

Clinical use of progestins

A

Used in oral contraceptives and in the Tx of endometrial cancer and abnormal uterine bleeding

35
Q

Mechanism of mifepristone

A

Competitive inhibitors of progestins at progesterone receptors

36
Q

Clinical use of mifeprestone

A

Termination of pregnancy. Administered with misoprostol (PGE1)

37
Q

toxicity of mifepristone

A

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

38
Q

How do oral contraceptives work?

A

Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. no estrogen surge → no LH surge → no ovulation

Progestins cause thickening of the cervical mucus thereby limiting access of sperm to uterus

Progestins also inhibit endometrial proliferation, thus making endometrium less endometrium less suitable for the implantation of an embryo

39
Q

Contraindications for oral contraceptives

A

smokers < 35 yo

pts with a history of thromboembolism and stroke or history of estrogen-dependent tumor

40
Q

Mechanism of ritodrine/terbutaline

A

ß2-agonists that relax the uterus

41
Q

Clinical use of ritodrine/terbutaline

A

Reduce premature uterine contractions

Ritodrine allows the fetus to “return to dreams” by preventing early delivery

42
Q

What is the mechanism and use of tamsulosin?

A

alpha1-antagonist used to teat BPH by inhibiting smooth muscle contraction

Selective for alpha1A,D receptors (found on prostate) vs vascular alpha1B receptors

43
Q

Mechanism of sildenafil

A

Inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow and penil erection

Sildenafil and vardenafil fill the penis

44
Q

Mechanism of vardenafil

A

Inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow and penil erection

Sildenafil and vardenafil fill the penis

45
Q

Clinical use of sildenafil

A

Tx erectile dysfunction

46
Q

Clinical use of vardenafil

A

Tx erectile dysfunction

47
Q

Toxicity of sildenafil

A

Headache

Flushing

Dyspepsia

Impaired blue-green color vision

Risk of life-thereatening hypotension in patients taking nitrates

“Hot and sweaty” but then Headache, Heartburn and Hypotension

48
Q

Toxicity of vardenafil

A

Headache

Flushing

Dyspepsia

Impaired blue-green color vision

Risk of life-thereatening hypotension in patients taking nitrates

“Hot and sweaty” but then Headache, Heartburn and Hypotension

49
Q

Mechanism of danazol

A

Synthetic androgen that acts as partial agonist at androgen receptors

50
Q

Clinical use of danazol

A

endometriosis and hereditary angioedema

51
Q

Toxicity of danazol

A

Weight gain

Edema

Acne

Hirsutism

Masculinization

Decreased HDL levels

Male Genital System (5 decks)

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