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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
Toxicity of clomiphene
Hot flashes Ovarian enlargement Multiple simultaneous pregnancies Visual disturbances
26
Mechanism of tamoxifen
Estrogen antagonist on breast tissue
27
Clinical use of tamoxifen
Treat and prevent recurrence of ER-positive breast cancer
28
Mechanism of raloxifene
Estrogen agonist on bone
29
Clinical use of raloxifene
Reduces resorption of bone used to treat osteoporosis
30
Clinical use of HRT
Used for relief or prevention of menopausal symptoms and osteoporosis
31
Toxicity of HRT
Unopposed estrogen replacement therapy increases the risk of endometrial cancer, so progesterone is added Possible increased CV risk
32
What is the mechanism and use of anastrozole/exemestane?
Aromatase inhibitors used in postmenopausal women with breast cancer
33
Mechanism of progestins
Bind progesterone receptors, reduce growth and increase vascularization of endometrium
34
Clinical use of progestins
Used in oral contraceptives and in the Tx of endometrial cancer and abnormal uterine bleeding
35
Mechanism of mifepristone
Competitive inhibitors of progestins at progesterone receptors
36
Clinical use of mifeprestone
Termination of pregnancy. Administered with misoprostol (PGE1)
37
toxicity of mifepristone
Heavy bleeding, GI effects (nausea, vomiting, anorexia) and abdominal pain
38
How do oral contraceptives work?
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
Contraindications for oral contraceptives
smokers \< 35 yo pts with a history of thromboembolism and stroke or history of estrogen-dependent tumor
40
Mechanism of ritodrine/terbutaline
ß2-agonists that relax the uterus
41
Clinical use of ritodrine/terbutaline
Reduce premature uterine contractions Ritodrine allows the fetus to "return to dreams" by preventing early delivery
42
What is the mechanism and use of tamsulosin?
alpha1-antagonist used to teat BPH by inhibiting smooth muscle contraction Selective for alpha1A,D receptors (found on prostate) vs vascular alpha1B receptors
43
Mechanism of sildenafil
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
Mechanism of vardenafil
Inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow and penil erection ## Footnote Sildenafil and vardenafil fill the penis
45
Clinical use of sildenafil
Tx erectile dysfunction
46
Clinical use of vardenafil
Tx erectile dysfunction
47
Toxicity of sildenafil
Headache Flushing Dyspepsia Impaired blue-green color vision Risk of life-thereatening hypotension in patients taking nitrates *"**H**ot and sweaty" but then **H**eadache, **H**eartburn and **H**ypotension*
48
Toxicity of vardenafil
Headache ## Footnote 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
Mechanism of danazol
Synthetic androgen that acts as partial agonist at androgen receptors
50
Clinical use of danazol
endometriosis and hereditary angioedema
51
Toxicity of danazol
Weight gain Edema Acne Hirsutism Masculinization Decreased HDL levels

Male Genital System (5 decks)

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