Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology > Repro drugs > Flashcards

Repro drugs Flashcards

1
Q

Leuprolide and Geserelin

A

Mechanism: GnRH analog
pulsatile -> agonist properties
continuous -> antagonistic properties (downregulation of GnRH receptor in pituitary)

Clinical use:

  • Infertility (pulsatile)
  • Prostate cancer (continuous), following androgen receptor block with flutamide)
  • Uterine fibroids (continuous)
  • Precocious puberty (continuous)

Toxicity: Antiandrogen, nausea, vomiting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Estrogens

A

ethinyl estradiol, DES, mestranol

Mechanism: Bind estrogen receptors (intracytoplasmic steroid receptors)

Clinical use:

  • Hypogonadism or ovarian failure
  • menstrual abnormalities
  • Hormone replacement therapy in postmenopausal women
  • Men w androgen-dependent prostate cancer

Toxicity:

  • Increased risk of endometrial cancer
  • Bleeding (postmenopausal women)
  • Increased risk of thrombi (estrogen increases pro-coagulative factors)
  • Clear cell adenocarcinoma of vagina (in utero DES exposure)

CONTRAINDICATIONS: ER(+) Breast cancer, Hx of DVTs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Clomiphene

A

Mechanism: Selective estrogen receptor modulator. Partial agonist at estrogen receptor (perceived antagonism) in hypothalamus -> disinhibits hypothalamus from neg feedback -> increased GnRH-> increased LH and FSH fro pituitary -> ovulation

Clinical use: Infertility due to anovulation (ex PCOS)

Toxicity: host flashes, ovarian enlargement, multiple simultaneous pregnancies, visual distrubances

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Tamoxifen

A

Mechanism: Selective estrogen receptor modulator. Antagonist at estrogen receptors at breast, agonist at bone and uterus.

Clinical use: Treat and prevent recurrence of ER/PR(+) breast cancer

Toxicity: Increased risk of endometrial cancer and thromboembolic events

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Raloxifene

A

Mechanism: Selective estrogen receptor modulator. Antagonist at estrogen receptors at breast AND uterus, agonist at bone.

Clinical use: osteoporosis

Toxicity:

  • Increased risk of thromboembolic events
  • NO increased risk for endometrial cancer (since not agonist at uterus unlike tamoxifen)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Anastrozole/Letrozole/Exemestane

A

Mechanism: Aromatase inhibitors -> decrease synthesis of estrogen

Clinical use: Postmenopausal women with ER (+) cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Progestins

A

Mechanism: synthetic progesterone binds progesterone receptors -> decreases growth and increases vascularization of endometrium

Clinical use:
Used in OCP (mucus thickening)
Treat endometrial cancer (mitigate unopposed estrogen)
Abnormal uterine bleeding (maintain uterine lining)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Mifepristone (RU-486)

A

Mechanism: Competitive inhibitor of progestins at progesterone receptor

Clinical use: Termination of pregnancy. Administered with misoprostol (PGE1) which increases excitation of myometrium

Toxicity: Heavy bleeding, GI distress, abdominal pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Oral contraceptives (synthetic progestins, estrogen)

A

Mechanism: Estrogen and progestins inhibit LH/FSH -> prevent estrogen surge -> no LH surge -> no ovulation

Progestins -> thickening of cervical mucus, inhibit endometrial proliferation

Clinical use: contraception, PCOS

Toxicity: Contraindicated in: smokers >35yrs (increase cardiovascular risk), Hx of thromboembolism and stroke or hx of estrogen-dependent tumor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Terbutaline, ritodrine

A

Mechanism: beta2-agonists (terbutaline has beta1 and beta2 agonist effects), relax uterus (tocolytic) -> decrease contraction frequency

Clinical use: to delay labor

Note: beta2 agonism also bronchodilates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Danazol

A

Mechanism: Synthetic androgen that acts as partial agonist at androgen receptors (still get neg feedback), Also increases synthesis of C1 esterase inhibitor in liver -> use for hereditary angioedema

Clinical use: Endometriosis, hereditary angioedema

Toxicity: Weight gain, edema, psuedotumor cerebri, acne, masculinization, decreased HDL levels, hepatotoxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Testosterone, methyltestosterone

A

Mechanism: Agonist at androgen receptor

Clinical use:

  • Hypogonadism and promotes secondary sex characteristics
  • Stimulate anabolism for recovery after burn or injury

Toxicity:

  • Masculinization in females
  • Decreased intratesticular testosterone in males -> gonadal atrophy
  • Premature closure of epiphyseal plates
  • Increased LDL, decreased HDL
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Finasteride

A

Mechanism: 5alpha-reductase inhibitor-> decreased conversion of testosterone to DHT

Clinical use: BPH, male-pattern baldness (Rogaine)

Toxicity:

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Flutamide

A

Mechanism: Nonsteroidal competitive inhibitor at androgen receptor

Clinical use: prostate cancer

Toxicity:

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Ketoconazole

A

Mechanism: Inhibits 17,20-desmolase -> inhibits steroid synthesis (cholesterol -x-> pregnenolone)

Clinical use: PCOS to decrease androgenic symptoms

Toxicity: gynecomastia and amenorrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Spironolactone

A

Mechanism: Inhibits steroid binding, 17alpha-hydroxylase and 17,20-desmolase

Clinical use: PCOS to decrease androgenic symptoms

Toxicity: gynecomastia and amenorrhea

17
Q

Tamulosin, Terazosin

A

Mechanism: alpha1 antagonist -> inhibits smooth muscle contraction in prostate, will also have effect at vascular alpha1 receptors -> decreased BP

Clinical use: BPH with patient with HTN

Toxicity:

18
Q

Sildenafil, vardenafil, tadalafil

A

Mechanism: PDE5 inhibitor -> increases cGMP (via NO) -> smooth muscle relaxation in corpus cavernosum -> increased blood flow -> erection

Clinical use: erectile dysfunction

Toxicity: HA, flushing, dyspepsia (indigestion), cyanopsia (blue-tinted vision), priapism
Life-threatening hypotension risk in patients taking nitrates

19
Q

Minoxidil

A

Mechanism: Direct arteriolar vasodilator

Clinical use: androgenetic alopecia, severe refractory HTN

Toxicity:

20
Q

Hormone replacement therapy - use and risks

A

Use: Relief or prevention of vasomotor menopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis (increased estrogen decreases osteoclast activity)

-Progesterone added since unopposed estrogen replacement therapy increases risk of endometrial cancer

Associated risks: increased cardiovascular risk

Pharmacology (19 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions