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42 Cards in this Set
- Front
- Back
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Where do hormones bind to the cell and what is their role?
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Within the cytoplasm or nucleus.
The activated steroid-receptor complex initiates RNA synthesis. |
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Sex hormones are fat soluble. What advantage does this give for administration.
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Can be taken orally or applied topically and is absorbed through mucous membranes.
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What is the most potent form of endogenous estrogen?
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Estradiol (E2). The other estrogens, estrone and estriol, have 1/10th the potency.
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What is one problem with oral administration of estrogen?
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First pass clearance by the liver limites the bio-availability.
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How does oral administration with synthetic estrogens differ from endogenous estrogens?
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Less first pass hepatic metabolism results in greater bioavailability.
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Estrogen replacement by menopausal women has been used for....?
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Reduced vasoactive response, tissue atrophy, better sleep, osteoporosis.
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What unexpected results did the WHI show?
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increased risk of stroke, blood clots, ovarian cancer, endometrial cancer and breast cancer
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Conjugated estrogens/Premarin
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Indications: Px & Tx of osteoporosis and menopausal sxs.
MOA:alters gene transcription Char: PO, topical. Prog. should be added when female still has a uterus. Side Effect: vaginal bleeding, breast tenderness, risk of DVT, atherosclerosis and CAD, uterine CA, breast CA |
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Premarin Minor Side Effects
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breast pain, increased breast size, palpitations, fever, hives, hoarseness, joint pain, stiffness or swelling, rash, erythema of skin, SOB, wheezing, edema and weight gain
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Premarin Contraindications
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DVT or breast, ovarian or uterine CA
Category X |
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Medroxyprogesterone/Provera
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Class: progesterone derivative
Indications: Contraception, DUB MOA: alters gene transcription Char: PO, Depo form is IM |
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Provera Side Effects
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acne, weight gain, edema, insomnia, anxiety, risk for DVT, cervicitis, increases ratio of LDL to HDL
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Provera C/I
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prior Hx of DVT, breast, ovarian or uterine CA
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Oral Contraceptives (combined)
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combination of E (suppresses ovulation) and Progestin (prevents implantation and makes the cervical mucus impenetrable to sperm)
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Yaz 28 and Loestrin 24
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24 days of active hormone pills followed by 4 days of placebo. May have increased risk of osteoporosis
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Benefits of OCP
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Taken over 5 years decreases risk of ovarian and endometrial CA, colorectal Ca, and improves PID, dysmenorrhea, PMS, and anemia
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"Mini-pill"/progestin only
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not as effective as COCP, may produce irregular menses, implants (Levo-norgestrel/Norplant)
S.E: DVT, CVD, HTN, stroke (esp. women who smok and over 35yr) |
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OCP interactions
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penicillin (amoxil, tetracycline, cephalosporins, sulfa), seizer meds, St. John's wort
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Medroxyprogesterone acetate/Depo-Provera IM
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150mg aqueous suspension in upper arm or upper outer gluteal area.
Given 4 X yr offers immediate protection |
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The "morning after" pill:Progestin only
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1.5 mg either as 2 doses 12 hrs apart or a single dose
Plan B |
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The "morning after" pill:Compined E and P
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is now believed to be less effective and less well-tolerated (can take 4 Ovral pills, 2 q12 hrs X 2 doses
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Mifepristone/Mifeprex
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Progestin antagonist with partial agonist activity
Indications: abortifacient in 2 first months of pregnancy MOA:blockade of P receptors Often used with Misoprostol/Cytotec, an E1 analog. Also used in Zollinger-Ellison syndrome to make more mucus. |
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Mifepristone/Mifeprex Side Effects
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abdominal pain, uterine cramping, vaginal bleeding or spotting for an avg. of 9-16 days (8% for up to 30days)
N/V/D, dizziness, fatigue, fever |
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Mifepristone/Mifeprex Risks/CI
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excessive bleeding or imcomplete termination of a pregnancy requires emergent medical intervention
CI: IUD, extopic pregnancy, hemorrhagic d/o or on anticoagulant therapy, long term prednisone |
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SERMS (selective estrogen receptor modulators)
Clomiphene/Clomid |
The action is different in different tissues and can selectively inhibit or stimulate E-like action in various tissues
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Clomiphene/ Clomid
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E-receptor agonist
Indications: infertility, amenorrhea MOA: interferes with normal neg. feedback of E on GnRH resultin in increased GnRH, LH, FSH Char: PO carefully Side Effects: vaginal dryness, bleeding, breast tenderness, anxiety, hot flashes. CI: Hx of LV dz, breast CA or uterine CA Risk of multiple births |
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Testosterone is made in what cells?
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Leydig cells of the testes, ovaries, zona reticularis
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What enzyme metabolizes T?
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5-alpha reductase to dihydrotestosterone (DHT)
aromatase to E |
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What are the 2 primary effects of T?
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androgenic (male genitalia, 2ndary sex characteristics, sperm production and fertility and libido) and anabolic (protein metabolism and development and preservation of muscle, bone mass and bone strength. also increases RBC production. (4wks of development T is turned on for male development)
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Routes of administration of Testosterone
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PO(least effective dt 1st pass metab), topical(patch/cream), buccal, sub-lingual, IM
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In males, XS androgens can cause what conditions?
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acne, baldness, gynecomastia, prapism, prostatic hyperplasia, prostatic cancer, and reduced sperm count and infertility dt neg. feedback
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In females, XS androgens can cause what conditions?
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xs body hair, acne, deepening voice, clitoral enlargement and menstrual irregularities
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In children, XS androgens can cause what conditions?
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abN rate of sexual maturation, diminished height dt premature closing of growth plates
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What are additional adverse effects of testosterone?
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abN lipid levels (incresed LDL and lower HDL), fluid retention, increased blood viscosity/ischemia
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Testosterone cypionate
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Char: IM, patch, gel, SL lozenges. Not used PO.
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Anabolic steroids
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synthetic derivatives and have greater anabolic effects
Approved use: refractory anemia, servers osteoposrosis, server wasting conditions(AIDS, CA) |
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Anti-androgen Tx
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Most often used for advanced prostatic CA. Tx is palliative and not a cure.
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Leuprolide/Lupron
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Class:anti-androgen and anti-estrogen
Indication:Prostatic CA, precocious puberty, endometriosis, uterine fibroids, IVF MOA:synthetic analog of GnRH and interrupts production of T and E Char: SQ, IM SE: decreased libido, impotence, N/V, hot flashes, night sweats, arthralgias, myalgias, osteoporosis |
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Finasteride/Proscar
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Class:Anti-androgen
Indication: BPH, male-pattern baldness, prostate CA MOA: limits conversion of T to DHT by inhibiting type 2 5-alpha reductase Char: PO, can't donate blood. pregnant women should not be near dt risk of birth defects SE: decreased libido, ED, impotency, depression, breast welling and tenderness |
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2 meds for BPH
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5-alpha reductase inhibitors and alpha blockers
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Alpha blockers:
Doxazosin/Cardura Terazosin/Hytrin Tamsulosin/Flomax & Urimax Silodosin/Urief |
alpha 1 receptor agonists
Indications: BPH Relax smooth muscle in prostate and bladder neck. Lower dose than for HTN. SE: weakness, orthostatic hypotension, nasal congestion |
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Phosphodiesterase type 5 inhibitors:
Sildenafil citrate/Viagra |
Class: PDE5 inhibitor
Indication: ED, pulmonary HTN MOA: blocks degradative enzyme on cGMP causing relaxation of the sm. muscle cells lining the blood vessels of the corpus cavernosum, therfore erection is maintained CI: not for pts on NO donors, NG, Isosorbide dinitrate, when sex is inadvisable, severe LV or KD dysfxn, hypotension, hereditary degenerative retinal d/o SE: h/a, flushing, dyspepsia, nasal congestion, vision changes, rarely: acute angle closure glaucome, arrhythmias, severe hypoTN, MI, stroke, priapism |
