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Pharmacology > Sex Hormones > Flashcards

Sex Hormones Flashcards

1
Q

Therapeutic Estrogens

A

Estradiol, Ethinyl-estradiol, Estrone

Indications: primary hypogonadism, postmenopausal hormonal therapy, oral contraceptives, suppress ovulation in patients with intractable dysmenorrhea or hirsutism, fertility treatments

Side Effects: nausea, fluid retention, breakthrough bleeding, change in menstrual flow, breast tenderness

Adverse Effects: thromblytic complications; endometrial/breast carcinoma; HTN (IN MEN: feminization of genitalia & impotence)

Contraindications: pregnancy, incomplete bone growth, undiagnosed genital bleeding, stroke, thrombophlebitis, thromboembolic disease, heart disease; women with Hx of breast/uterine CA (BRCA gene)

DRUG INTERACTIONS: Decrease efficacy of anticoagulants and hypoglycemics; increase effects of tricyclic antidepressants; increase effects of oxytocin on uterus; St. John’s wort may lose efficacy of contraceptive or HRT of estrogens

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2
Q

Estradiol

A

Therapeutic estrogen

  • main estrogen in premenopausal women
  • poor oral bioavailability
  • effective as a patch (ESTRADERM, ESTROGEL)
  • IM lasts for weeks (DEPO Estradiol
  • Topical with vaginal cream (Estring)
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3
Q

Ethinyl-esradiol

A

Therapeutic Estrogen

- commonly used for orl contraceptives

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4
Q

Estrone

A

Therapeutic Estrogen

- natural estrogen-main ingredient of conjugated estrogens (PREMARIN)

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5
Q

HRT Formations

DON’T HAVE TO KNOW ALL FOR TEST- JUST KNOW THAT MANY FORMS EXIST, including those in cream and patch forms, not just oral

A

Estrogen alone caused uterine (endometrial CA)- now combo with progestins (Medroxyprogesterone-MPA)
- various regimens now used- estrogen for 25 days with inclusion of MPA during last 10-13 days of estrogen, 5-6 days with no hormones

combo formulas

 - PREMPRO (estrone plus MPA) given at fixed daily dose
 - PREMPHASE (Estrone for 28 days and MPA last 14-28 days)

Newer combos of estrogens with progestins:

  • FEM HRT (estradiol plus norethindrone acetate)
  • ORTH PREFEST(estradiol plus norgestimate)
  • Vaginal creams (PREMARIN) or a ring device (ESTRING): can be used instead of oral doses . Reduces vaginal dryness, yeast infections and urinary tract infections.

CombiPatch (estradiol/norethindrone acetate) transdermal patch
Alcohol free, lasts 3.5 days

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6
Q

Tamoxifen

A

Selective Estrogen Receptor Modulator (SERM)

Good Effects: reduces breast CA risk, lowers LDL cholesterol, strengthens bones

Bad Effects: Increases uterine CA risk, increases blood clot risk (2-3 fold increase with DVT, PE)

  • commonly used as an adjuvant with chemo or radiation in treatment
  • preventative agent for women at high risk for breast CA

-* resistance usually develops in 5 years, may reflect alterations in the ER receptors in the tumors

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7
Q

Raloxifene (Evista)

A
  • High affinity for both ER-a and ER-b (antagonist in breast, agonist in bone)
  • Treatment of osteoporosis in post-menopausal women
  • INVASIVE breast cancer in post-menopausal women (Less effect than tamoxifen against non-invasive)
    More effective in women with a uterus than tamoxifen against invasive breast cancer, about the same as tamoxifen in women without a uterus
  • Does not cause proliferation of the endometrium or breast tumor cells
  • No indication for pre-menopausal women, or men

Side effects: 2-3 fold ↑ risk of deep vein thrombosis and pulmonary embolism; Hot flashes (~25%)

Interactions: Ampicillin reduces absorption of raloxifene; Raloxifene reduces warfarin efficacy

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8
Q

Clomiphene

A

ANTI-ESTROGEN

  • Weak agonist and strong antagonist for ER-a or ER-b (partial agonist)
  • Oppose the negative feedback effects of endogenous estrogen. ↑amplitude of the LH and FSH pulses
  • Major use: induction of ovulation in women with an intact hypothalamic-pituitary-ovarian axis (fertility treatment)

Adverse effects: multiple births, ovarian cysts

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9
Q

HRT Effects of Treatment (Estrogen effects associated tih HRT during menopause

A

GOOD:
strengthens bones, decreases LDL, increases HDL, reduces menopausal symptoms (hot flashes)

BAD:
increases risk for breast CA & uterine CA (uterine CA risk can be reduced or eliminated by using progesterone with estrogen), increases risk of blood clot (* increased risk of MI/stroke, especially in FIRST YEAR)
- therefore, contraindicated in women with personal/family Hx of CA or CV disease

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10
Q

ICI 182,870 / Fulvestrant (Faslodex)

A

ANTI-ESTROGEN

  • pure estrogen antagonist
  • effective in treating tamoxifen-resistant tumors
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11
Q

Progestins - Therapeutic progesterone

A

Naturally occurring progesterone (low oral bioavailability)

 - Micronized particles suspended in oil and packaged in gelatin capsules (PROMETRIUM)
 - Vaginal gel (CRINONE)
 - Slow-release intrauterine device (PROGESTASERT)

Mechanism of Action: Interacts with PR to mimic the stimulatory affects of progesterone

Physiological Target: Reproductive Tract

  • Decreases estrogen-driven endometrial proliferation
  • Establishment and maintenance of pregnancy

Common Uses:

  • Oral contraceptives
  • HRT to limit estrogen’s effects on the endometrium
  • Uterine Bleeding disorders
  • Premature labor (decrease uterine contractions)
  • Stimulate Appetite in AIDS or cancer patients
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12
Q

Mifepristone (RU 486) (mifeprex)

A

Anti-progesterone (PR antagonist)

  • Used in first trimester to terminate pregnancy(along with prostaglandins to increase uterine contractions)
  • Post-coital contraceptive (prevent implantation)
  • Investigational: induction of labor after fetal death and treatment of endometriosis.

Adverse Effects: vaginal bleeding, abdominal pain and cramping

Contraindicated in patients with vaginal bleeding, adrenal dysfunction or asthma (due to anti-glucocorticoid actions)

Interactions:

  • Decreases efficacy of anticoagulants.
  • Inhibits hepatic metabolism by CYP3A4 (eg.anti-retroviral protease inhibitors, calcium-channel blockers, carbamazepine)
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13
Q

Mestranol / Ethinyl Estradiol

A

Contraception- therapeutic estrogens

  • Absorbed efficiently in GI tract. Mestranol is biologically inactive and must be metabolized to ethinyl estradiol. Peak plasma levels within 1 hr after oral administration
  • Clearance is ~ 60% 24 hr after oral dose
  • Ethinyl estradiol is 2X more potent than mestranol
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14
Q

Norethindrone

A

Contraception- therapeutic estrogens
19-NOR Steroids : * Progestins

  • Removal of 19-carbon changed major hormonal effect from an androgen to progestin while maintaining oral activity
  • *Estranes: have some androgenic activity as well as estrogenic/anti-estrogenic actions. Rapidly absorbed (Norethindrone)
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15
Q

Norgestrel, Norgestimate, Desogestrel

A

Contraception- therapeutic estrogens
- Gonanes (progestins)

  • More potent than estranes and less androgenic activity and are now used in the 3rd generation combination oral contraceptives
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16
Q

Monophasic Contraceptive

A

The concentrations of estrogens and progestins are fixed in the pill, which is taken for 21 days followed by 7 days of “hormone-free” pills.

Estrogen (fixed) + Progestin (fixed)

17
Q

Biphasic Contraceptive

A
  • Lower concentration in the first 7-10 days and then higher concentration for the next 11-14 days
  • The rationale is to limit exposure to the higher concentration of the progestin.

Estrogen (fixed amt) + progestin (2 concentrations)

18
Q

Triphasic Contraceptive

A

Fixed concentration of estrogen with 3 different concentrations of progestins

19
Q

Progestin Only Contraceptives

A
  • Oral formulations of norethindrone (micronor) or levonorgestrel (ovrette) taken daily
  • Subdermal implants of levonorgestrel (norplant) for slow-release and long-term contraceptive actions (up to five years)
  • IM injections of medroxyprogesterone (depo-provera) that provides effective contraception for 3 months
  • IUD that releases low amounts of progesterone locally (progestasert).
20
Q

Emergency Contraceptives

A
  • Drugs used for the prevention of pregnancy following unprotected intercourse or a known or suspected barrier contraceptive failure.
  • Emergency hormone contraceptive regimens are highly effective and decrease the risk of pregnancy by 75 percent

To be effective these must be taken * within 72 hours of intercourse*

  • May also inhibit ovulation or fertilization depending on timing of administration
  • Alteration of the endometrium, sperm penetration, and tubal motility are also affected (prevent implantation).

ESTABLISHED PREGNANCIES ARE NOT HARMED

Two products are available:
Plan B: 0.75 mg levonorgestrel
Preven: 0.25 mg levonorgestrel and 0.05 mg ethinyl estradiol (this product includes a pregnancy test kit)

21
Q

Extended Regimen Contraception

A

Levonorgestrel / ethinyl estradiol 0.15 mg / 0.03 mg
And either placebo or ethinyl estradiol tablets 0.01 mg tablets)
Brand Names: Jolessa, Quasense, Seasonale, Seasonique

91-day courses of tablets
Advantages
• Period once every 3 months
• Period last about 3 days with decreased bleeding

Side Effects: Breakthrough bleeding and spotting

Seasonique:
Incorporates low-dose estrogen rather than placebo tablets in an effort to limit bloating, hormonal fluctuations, and breakthrough bleeding.

22
Q

Benefits of Oral Contraceptives

A

Initiating Method:
• Start First day of next menstrual period
• Some suggest starting on first Sunday following onset of menses
- Usually avoids menstrual period on weekends
- Most clinicians recommend backup for at least 2 cycles

Other Beneficial effects

  1. Decreases Dysmenorrhea
  2. Decreases benign breast and ovarian cysts
  3. Regulates cycle in anovulatory women
  4. Decreased blood loss during menstruation
  5. 50% reduction in ovarian and endometrial cancer.
23
Q

Oral Cotraceptive- Drug Interactions

A

Drugs that disrupt liver metabolism and increase

  • oral contraceptive metabolism
  • anti-seizure medications, St. John’s wort
  • antibiotics tetracycline and ampicillin
  • HIV protease inhibitors
  • Anti-tuberculosis drugs such as rifampin

Oral contraceptives effect the activity of other drugs

  • Decrease efficacy of anticoagulants
  • Inhibit or increase metabolism of benzodiazepines depending on the drug
  • Inhibit metabolism of beta-blockers
  • Inhibit metabolism of corticosteroids, and tricyclic antidepressants
24
Q

Oral Contraceptive Contraindications

A
  1. Absolute- KNOW THESE
  • History of thromboembolism, MI, stroke
  • Impaired liver function
  • Known or suspected breast cancer
  • Undiagnosed abnormal vaginal bleeding
  • Known or suspected pregnancy
  • Smokers over age 35 (may use progestin-only)
  1. Relative
  • Migraine headaches
  • Hypertension - ok if <35, or healthy, or BP controlled
  • Elective surgery: Discontinue 4wks. prior to major surgery
  • Gallstones/ Cholecystitis
  • Epilepsy: anti-seizure meds may decrease effectiveness of OCP’s
  • Diabetes: small risk or worsening vascular disease.
25
Q

Adult Male Hypogonadism

A 
Symptoms:
Decreased libido
Erectile dysfunction
Infertility
Fatigue, weakness
Depression, loss of motivation, irritability
Vasomotor phenomena
Signs:
Decreased body hair
Decreased muscle mass
Small prostate and testes
Gynecomastia
Osteoporosis
Anemia

Treatment:

  • Transdermal testosterone esters
  • Monitoring for both beneficial and deleterious effects required, age dependent
  • can occur in the aging male resulting from decreased testosterone
26
Q

Androgens

A

Treatable Conditions:
Male hypogonadism, prostate CA, male pattern baldness

Potential Side Effects of Excessive Androgen Treatment:

  • Reduced spermatogenesis and fertility due to feedback inhibition of LH and FSH secretion from anterior pituitary
  • Acne, particularly in women due to androgen stimulation of sebaceous glands beneath skin
  • Virilization (including facial hair and hirsutism) in women and children
  • In older men, increased risk of benign prostate hyperplasia and prostate cancer
  • Hepatotoxicity (for 17α-alkylated androgens)

Anabolic Steroid and Androgen Abuse in Sports:
- 100-200 x normal daily production in men

27
Q

Testosterone (Histerone)

A

Androgen

  • oral admin. leads to absorption into the hepatic circulation and rapid catabolism
  • Effective in transdermal patches
28
Q

Testosterone derivatives (Androgens)

A

Androgen

  • 17-α-alkylated androgens: decreased breakdown by liver, but can elicit hepatic toxicity
29
Q

Flutamide (Evlexin) & Bicalutamide (Casodex)

A

Androgen receptor ANTAGonist

Used in conjunction with GnRH analogs to treat metastatic prostate cancer

Treat Hirsutism in women (due to hepatoxicity should not use for cosmetic purposes)

30
Q

Finasteride (Proscar/ Propecia)

A

5-α-reductase inhibitors

used to treat benign prostatic hypertrophy (finasteride) and male patterned baldness (PROPECIA)

Contraindicated for women of childbearing age:
Can cause male children to develop as female in utero

Pharmacology (15 decks)

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