Repro Drugs Flashcards

1
Q

Leuprolide

A

-GnRH analog with agonist properties when used in pulsatile fashion / antagonist when used continuously
Use: uterine fibroids, endometriosis, precocious puberty, prostate cx,infertility, breast cancer/androgen excess
Adverse: hypogonadism, decreased libido, ED, nausea vomiting, edema, depression, decreased bone density when >6 months

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2
Q

Ethinyl estradiol, DES, mestranol

A

-bind estrogen receptors
-hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy
Adverse: increase risk of endometrial cx, bleeding in postmenopausal, clear cell adenocarcinoma in vagina, increased clot risk, lipid effects (increase TG, cholesterol)

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3
Q

Clomiphene

A

Selective estrogen receptor modulator

  • antagonist at estrogen receptor in hypothalamus
  • prevents LH and FSH from pituitary, stimulates ovulation
  • used to treat infertility due to anovulation
  • may cause hot flashes, ovarian enlargement, visual disturbances, pituitary tumor
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4
Q

Tamoxifen

A

Selective estrogen receptor modulator

  • antagonist at breast, agonist at bone
  • increase risk of thromboembolic events and endometrial cancer
  • used to treat and prevent recurrence of ER/PR positive breast cancer
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5
Q

Raloxifene

A

Selective estrogen receptor modulators

  • antagonist at breast, uterus, agonist at bone
  • increased risk of thromboembolic event but NOT cancer
  • used to treat osteoporosis
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6
Q

Anastrozole, letrozole, exemestane

A

Aromatase inhibitors

  • inhibit peripheral conversion of androgens to estrogen
  • use: ER positive breast cancer in postmenopausal women
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7
Q

Hormone replacement therapy

A
  • use: relief of menopausal symptoms, osteoporosis
  • unopposed estrogen therapy increases risk for endometrial cancer, progesterone/progestin is added.
  • possible increased CV risk
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8
Q

Levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, megestrol

A

Progestins

  • bind progesterone receptors, decrease growth and increase vascularization of endometrium, thicken cervical mucus
  • use: contraception, endometrial cancer, abnormal uterine bleeding,
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9
Q

Mifepristone, ulipristal

A

Anti progestins

  • competitive inhibitors of progestins at progesterone receptors
  • use: termination of pregnancy (mifepristone with misoprostal), emergency contraceptive (ulipristal)
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10
Q

Combined contraceptives

A
  • progestin and ethinyl estradiol
  • estrogen and progestin inhibit FSH/LH and prevent estrogen surge, no ovulation
  • progestin=thickening of cervical mucus, limit access of sperm to uterus and endometrial proliferation is inhibited, thinner and less viable
  • contraindications: smokers, pts with CV disease, migraines, breast cancer and liver disease
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11
Q

Copper IUD

A
  • produces local inflammation rxn toxic to sperm and ova, preventing fertilization and implantation, no hormones
  • use: long acting reversible contraception, most effective emergency contraception
  • adverse: heavier, longer menses, dysmenorrhea, risk of PID with insertion
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12
Q

Tocolytics

A

Meds that relax the uterus

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13
Q

Terbutaline

A

-B2 agonist
Used to slow contraction frequency in labor and prolong time to delivery
Adverse: dizziness, drowsiness, breathing probs, irregular heartbeat, maternal hyperglycemia, pulmonary edema, hypotension, tachycardia
-Not for use for longer than 48-72 hours

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14
Q

Nifedipine

A

-Ca2+ channel blocker
-used to decrease contraction in preterm labor, peripheral vasodilator
Contraindicated: women with hypotension, caution with CHF, left sided failure

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15
Q

Indomethacin

A

NSAID

-used to slow contractions in preterm labor

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16
Q

Danazol

A

-synthetic androgen that acts as partial agonist at androgen receptors
Use: endometriosis, hereditary angioedema
Adverse: weight gain, edema, acne, hirsutism, masculinization, lower HDL levels, hepatotoxic, pseudotumor cerebri

17
Q

Testosterone, methyltestosterone

A

-agonists at androgen receptors
Use: treat hypogonadism, promote development of 2ndary sex characteristics, stimulate anabolism to promote recovery after burn/injury, stimulate RBC production in anemias, promote weight gain in wasting pts (AIDS)
Adverse: masculization of females, decrease intratesticular T in males by inhibiting LH release, high LDL, low HDL, cholestatic jaundice, elevated liver enzymes, hepatocellular carcinoma

18
Q

Finasteride

A

5alpha reductase inhibitor
-decreases conversion of testosterone to DHT
Use: BPH and male pattern baldness, female hirsutism
Adverse: orthostatic hypotension, dizziness, decreased libido, fatigue, jaundice
-caution with liver pts, should be avoided in pregnancy (RF X)

19
Q

Flutamide

A

Nonsteroidal competitive inhibitor at androgen receptors
Use: prostate carcinoma, androgen excess
Adverse: hot flashes, decreased libido, diarrhea, vomiting
-liver function should be monitored

20
Q

Ketoconazole

A

-inhibits steroid synthesis (inhibits 17,20 desmolase/17alpha hydroxylase)
Use: PCOS to reduce androgenic symptoms, steroid responsive metastatic prostate cancer
Adverse: gynecomastia and amenorrhea, orthostatic hypotension, dizziness, fatigue, jaundice, vomiting
-rarely causes reversible hepatotoxicity, may cause prolong QT interval, inhibits cortisol synthesis

21
Q

Spironolactone

A

Inhibits steroid binding, 17,20 desmolase/17alpha hydroxylase
Use: PCOS to reduce androgenic symptoms
Adverse: gynecomastia and amenorrhea, rarely polyuria, gastritis, fatigue, potential to cause hyperkalemia

22
Q

Tamsulosin

A

Alpha-1antagonist
Use: treat BPH by inhibiting smooth muscle contraction
-selective for alpha 1A/d vs vascular alpha 1B

23
Q

Sildenafil, vardenafil, tadalafil

A

Inhibit phophodiesterase type 5
-increase cGMP, prolong smooth muscle relaxation in response to NO, increase blood flow in corpus cavernosum of penis, decrease pulmonary vascular resistance
Use: ED, pulmonary hypertension, BPH
Adverse: headache, flushing, dyspepsia, cyanopia, hypotension in pts taking nitrates

24
Q

Minoxidil

A

-direct arteriolar vasodilator

Use: androgenetic alopecia, severe refractory hypertension

25
Q

Testosterone in plasma

A
  • partly bound to SHBG (sex hormone binding globulin)

- SHBG is increased by estrogen and decreased by T

26
Q

Progesterone

A

-progesterone receptor agonist
Use: prevention of spontaneous preterm delivery
Adverse: side effects are related to injection route (vaginal or IM)

27
Q

Magnesium sulfate

A

-reduces calcium influx
Use: postpone preterm labor by reducing uterine contraction
Adverse: maternal toxicity: muscle weakness, somnolence, double vision, slurred speech
Fetal: lethargy, hypotonia, respiratory depression
-less effective than nifidepine

28
Q

Oxytocin

A

-causes contraction of the uterus
Adverse: fetal distress, water intoxication, CV effects, hypotension
-at high doses causes antidiuretic effects (volume overload)
-can be used prophylactically to prevent postpartum hemorrhage

29
Q

Dinoprostone

A

PGE2 analog
-causes contraction of the uterus
Adverse: fetal heart rate abnormalities
Not for pts with prior C-section, increased risk of incisional uterine rupture

30
Q

Misoprostol

A

PGE1 analog
-cervical ripening and uterine contractions
-adverse: fetal heart rate abnormalities, pyrexia, N/V/D
Contraindicated in pts with prior C-section
-can also be used for postpartum hemorrhage and in adjunct with mifepristone in medical abortion

31
Q

Methylergonovine

A

Cause generalized smooth muscle contraction
Use: post partum hemorrhage
Adverse: N/V
-not for preeclampsia, hypertension, Hypersensitivity

32
Q

Carboprost

A

Increase uterine contractility and cause vasoconstriction
-treat postpartum hemorrhage
Adverse: N/V/D, hypertension, headache, pyrexia
Caution with asthma, hypertension

33
Q

Fulvestrant

A

Estrogen receptor antagonist
Use: treatment of tamoxifen resistant breast cancer
Adverse: hot flashes, injection site pain, liver enzyme abnormalities, joint probs
-Hypersensitivity rxns, caution in pts with bleeding disorders, caution in pts with hepatic impairment