Sex hormone pharmacology

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Parent steroid of estrogens; androgens; proestins; mineralcorticoids; and glucocorticoids

Cholesterol
Form of estrogen produced in ovaries. Stronger or weaker?

E2; estradiol stronger
Form of estrogen produced in adipose tissue. Stronger or weaker?

E1; estrone weaker
Receptor responsible for estrogen mediated cell signaling.

Estrogen response element
Another level of regulation of estrogen; tamoxifen is an example of this.

Selective Estrogen receptor modifier
Enzyme important in synthesis of dihydrotestosterone

5 alpha reductase
Effect of circulating estrogen levels on LH and FSH

inhibition
Estrogen preparations 4 types

conjugated equine estrogens; ethinyl estradio; transdermal estradiol; estradio cypionate/valerate
isolated from pregnant mares; for HRT

conjugated equine estrogens (premarin and prempro)
oral contraceptives; modification makes it orally active

ethinyl estradiol
HRT contraception; patch

transdermal estradiol
intramuscular HRT for estrogen

estradio cypionate and valerate
metabolism of estrogen

hepatic; inducers of CYP450 increase elimination
enterohepatic cycling

conjugated estrogens excretedinto bile; reconstitued by bacteria; and reabsorbed by the GI
uses of estrogen/estrogen preparations

HRT post ovisectomy and postmenopausal; contracption; acne; dysmenorrhea; endometriosis
progestin preparations

progesterone esters; synthetic analogues (norgestrel; levonorgestrel; norethindrone; desogestrel); drospirenone
use for intramuscular injectsion in Depo-provera and HRT

Medroxyprogesterone acetate
Used in combination contraceptive and postcoital contraceptive; high androgenic activity

Norgestrel and levorgestrel (poscoital); high androgenic activity
Used in combination contraceptive and postcoital contraceptive; moderate androgenic activity

norethindrone
Used in combination contraceptive and postcoital contraceptive; lowest androgenic activity; but not used because of this side effect

desogestrel; dvt
Use in some oral contraceptives; has both antialdosterone and antiandrogenic effects

drospirenonone
Uses of progesterone

dysmenorrhea; endometriosis; uterine bleeding; oral contraceptives; HRT to decrease endometrial cancer
MOA of oral contraceptives

1. inhibit LH surge at the pituitary 2. endometrial atrasia 3. increase thickness of cervical mucus (progesterone)
Components of oral contraceptives

ethinyl estradio and progesterone analogue
How triphasic compare to di and mono phasic preparations

Estrogen remains the same; progesterone levels increase incrimentally. Less hormone exposurein triphasic preparations.
Monophasic therapies; durgs and dosages.

Contains EE and drospirenone. Drugs: Yasmin and Yaz. Anti aldosterone and antil-androgen due to drospirenone.
What are the extened time pills

Lybrel (1 year); seasonale (84 days + 7days free); seasonique (84 days + 7 day of EE)
Common side effects of contraceptive use

N/V weight gain; breast tenderness; edema. Breast cancer; gall stones; serum binding protein elevated; increases coagulation (infarction; DVT; stroke)
Adverse effects of contraceptive use

Hirsutism; glucose intolerance; HDL decrease and IDL increase; depression
4 general Contra indications to contraceptive use

Breast cancer/liver tumor; DVT/PE/CVA/IHD; smokers >35; <6wks postpartum and breast feeding
Formulation (2) and use for progestin only contraception

Norgestrel and norethindrone; prenant women where estrogen is contraindicated
Three options of morning after contraception.

Levonorgestrel (plan B); ulipristal acetate (progesteron receptor modulator); IUD inseration.
Three non-oral contraceptives

Injection (lunelle); vaginal ring (nuva ring); contraceptive patch (ortho Evera)
Three non-oral progesteron only

IUD (levonorgestrel); implant (etonorgestrel); IM injection of medroxyprogesterone acetate
Estrogen sx associated with menopause

osteoporosis; vasomotor sx; urogenital atrophy; vaginitis
Selective estrogen receptor modulator for treating osteoperosis

Raloxifene; antagonist in uterus and breast; agonist in bone and lipid (decreases LDL).
Regiments available for estrogen replacement therapy

cyclic therapy (estrogen then methylprogesterone) and continuous (conjugated estrogen and medroxyprogesterone)
Conclusion on HRT

Risks outweigh benifits.
Two drugs that acts on hypo pituitary axis to decrease LH surge

Luprolide (GnRH agonist; downregulates GnRH receptors) and Ganirelix (GnRH receptor antagonist)
FSH and LH analogues

Urofollitropin (FSH); placental hCG (LH); menotropins (hMG->FSH&LH). Ovarian hyperstimulation syndrome.
DopaR agonist; treat hyper prolactinemia and parkinson's

Bromocriptine
Three androgen preparations

testosterone; metyltestosterone; oxandrolone and nandrolone
Uses of androgen preparation

hypogonadism; revers protein loss in trauma; buff up
Adverse effects of androgen use

masculination; acne; sleep apnea; erythrocytosis; gynecomastia; azoospermia; lower HDL; increase aggressivness; hepatic enzyme elevation
anti androgens (4)

finasteride; flutamide; spironolactone; ketoconazole
androgen receptor antagonists

fluamide and spironolactone (also aldosterone antagonist)
MOA of ketoconazole; uses

decreases androgen prouction; also antifungal drug
selective estrogen recptor modulators (4)

tamoxifen; toremifene; raloxifene; clomiphene
antagonis at breast; agonist at endometrium; treat breast cancer; worry about endometrial cancer

Mechanism of action and use of tamoxifen and toremifene
agonist at bone antagonist in breast and endometrial cancer

raloxifene MOA and uses
stimulate ovulation; inihibit negative feed back of LH/FSH at hypo and stimulates GnRH release

clomiphene MOA and uses
decreases estrogen synthesis (3)

Danazole letrozole anastrozole
decrease estrogen receptors (sequesteres it)

fluvestrant
competative progesterone antagonist; uses?

mifeprestone (induce abortion)
non-steroidal estrogen; not used much

diethystilbestrol

Author

770aky

189617

Card Set

Sex hormone pharmacology

Description

pharmacology

Updated

2012-12-15T17:21:10Z

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