Reproductive- Pharmacology Flashcards

1
Q

Control of reproductive hormones

A

Pag. 636

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2
Q

Leuprolide

  • Mechanism
  • Clinical use
  • Adverse effects
A

GnRH analog

  • agonist when pulsatile fashion;
  • antagonist when used in continuous

Uterine fibroids, endometriosis, precocious puberty, prostate cancer, infertility

Hypogonadism, decrease libido, erectile dysfunction,
nausea, vomiting.

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3
Q

Estrogens

  • Names
  • Clinical use
A

Ethinyl estradiol, DES, mestranol.

Hypogonadism or ovarian failure, menstrual abnormalities (combined OCPs), hormone
replacement therapy in postmenopausal women

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4
Q

Estrogens

  • Adverse effects
  • Contraindications
A

risk of endometrial cancer (when given without progesterone), bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, risk of thrombi

ER ⊕ breast cancer, history of DVTs, tobacco use in women > 35 years old.

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5
Q

Selective estrogen receptor modulators (SERMs)

A

Clomiphene, Tamoxifen, Raloxifen

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6
Q

Clomiphene

  • Mechanism
  • Clinical use
  • Adverse effects
A

Antagonist at estrogen receptors in hypothalamus.

Used to treat infertility due to anovulation (eg, PCOS).

SERMs may cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visua disturbances.

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7
Q

Tamoxifen

  • Mechanism
  • Clinical use
  • Adverse effects
A

Antagonist at breast; agonist at bone, uterus;

Used to treat and prevent recurrence of ER/PR ⊕ breast cancer.

Risk of thromboembolic events and endometrial
cancer.

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8
Q

Raloxifen

  • Mechanism
  • Clinical use
  • Adverse effects
A

Antagonist at breast, uterus; agonist at bone;

Used primarily to treat osteoporosis.

Risk of thromboembolic events but no increased risk
of endometrial cancer (vs tamoxifen)

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9
Q

Aromatase inhibitors

  • Names
  • Mechanism
  • Clinical use
A

Anastrozole, letrozole, exemestane

Inhibit peripheral conversion of androgens to estrogen

ER ⊕ breast cancer in postmenopausal women.

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10
Q

Hormone replacement therapy

A

Used for relief or prevention of menopausal symptoms,
osteoporosis.

Unopposed estrogen replacement therapy  risk of endometrial cancer, progesterone/progestin is added. Possible increased cardiovascular risk.

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11
Q

Progestins

  • Names
  • Mechanism
A

Levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, megestrol

Bind progesterone receptors, decrease growth and increase vascularization of endometrium, thicken cervical mucus

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12
Q

Progestins

- Clinical use

A

Contraception, endometrial cancer, abnormal uterine bleeding.

Progestin challenge: presence of withdrawal bleeding
excludes anatomic defects (eg, Asherman syndrome) and chronic anovulation without estrogen

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13
Q

Antiprogestins

  • Names
  • Mechanism
  • Clinical use
A

Mifepristone, ulipristal.

Competitive inhibitors of progestins at progesterone receptors.

Termination of pregnancy (mifepristone with misoprostol); emergency contraception (ulipristal).

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14
Q

Combined contraception

  • Combination
  • Mechanism
  • Contraindications
A

Progestins and ethinyl estradiol

Inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge Ž no LH surge Ž no ovulation.

smokers > 35 years old, risk of cardiovascular disease, migraine, breast cancer, liver disease

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15
Q

Copper intrauterine device

  • Mechanism
  • Clinical use
  • Adverse effects
A

Produces local inflammatory reaction toxic to sperm and ova

Long-acting reversible contraception. Most effective emergency contraception

Heavier or longer menses, dysmenorrhea. Risk of PID with insertion

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16
Q

Tocolytics

  • Mechanism
  • Names
  • Clinical use
A

Medications that relax the uterus

terbutaline, nifedipine, indomethacin

Used to decrease contraction frequency in preterm labor and allow time for administration of steroids

17
Q

Danazol

  • Mechanism
  • Clinical use
  • Adverse effects
A

Synthetic androgen that acts as partial agonist at androgen receptors.

Endometriosis, hereditary angioedema

Weight gain, edema, acne, hirsutism, masculinization, low HDL levels, hepatotoxicity, pseudotumor cerebri

18
Q

Testosterone, methyltestosterone

  • Clinical use
  • Adverse effects
A

Treat hypogonadism and promote development of 2° sex characteristics; stimulate anabolism to promote recovery after burn or injury

Masculinization in females; decrease intratesticular testosterone Ž gonadal atrophy. Premature closure of epiphyseal plates. high LDL, low HDL.

19
Q

Antiandrogens

  • Finasteride
  • Flutamide
A

5α-reductase inhibitor, Used for BPH and male-pattern baldness. Adverse effects: gynecomastia and sexual dysfunction.

Nonsteroidal competitive inhibitor at androgen receptors. Used for prostate carcinoma.

20
Q

Antiandrogens

  • Ketoconazole
  • Spironolactone
A

Inhibits steroid synthesis (inhibits 17,20 desmolase/17α-hydroxylase).

Inhibits steroid binding, 17,20 desmolase/17α-hydroxylase.

*Used in PCOS to reduce androgenic symptoms. Both gynecomastia and amenorrhea

21
Q

Tamsulosin

  • Mechanism
  • Clinical use
A

α1-antagonist inhibiting smooth muscle contraction. Selective for α1A/D receptors (found on prostate) vs vascular α1B receptors.

Used to treat BPH

22
Q

Phosphodiesterase type 5 inhibitors

  • Names
  • Clinical use
  • Adverse effects
A

Sildenafil, vardenafil, tadalafil.

Erectile dysfunction, pulmonary hypertension, BPH (tadalafil only).

Headache, flushing, dyspepsia, cyanopia (blue-tinted vision). Risk of life-threatening hypotension in patients taking nitrates.

23
Q

Minoxidil

  • Mechanism
  • Clinical use
A

Direct arteriolar vasodilator

Androgenetic alopecia (pattern baldness), severe refractory hypertension.