08-Drugs for female reproductive system Flashcards
What occurs with the binding of water soluble hormones bind to the outside surface of the cell?
Leads to manufacture of second messengers (cAMP or IP3) which alter cell function
What occurs when oxytocin binds to receptors outside of the myometrium?
Releases second messengers, increases calcium levels and stimulates uterine contraction
What is an example of a membrane spanning enzyme?
Insulin, binds to receptors which bind to an enzyme and affect activity then causing intracellular effects
What are lipid soluble endocrine hormones?
- Have capacity to bind to receptors inside and outside of the cell
- Ex. estrogen, testosterone, progesterone, thyroid hormone, cortisol, aldosterone
What occurs when the fat soluble endocrine hormones are released by endocrine glands?
Enter systemic circulation, pass biological membranes of the target cell, binds to intracellular receptor, drug-receptor complex is formed aand then can act on the DNA directly inside of the cell
What is an example of a fat soluble endocrine hormone working directly inside of a cell?
Testosterone binds inside muscle tissue (receptor), activates at the level of DNA for muscle to grow bigger
What 2 hormones are produced by the anterior pituitary?
LH and FSH
What are the roles of LH and FSH?
- Acts on sex organs to make sex steroids, important for growth and development
- Sex steroids (testosterone) is important for libido
- Maturation of follicles
The female body is pro-….?
Pro-pregnancy! Female gonads work to facilitate pregnancy
High estrogen levels cause what?
Surge in LH and FSH, which facilitates ovulation
Increased progestin does what?
Creates home for a fertilized egg to land, induces proliferation of the endometrium
What happens if there is no egg fertilized?
No implantation, GnRH, LH and FSH falls, estrogen and progesterone levels fall, signals beginning of the menstrual cycle
What are the three estrogens?
- Estradiol
- Estrone
- Estriol
Estradiol:
- Made by the ovary, conversion of testoserone to estrogen
- Drives changes associated with puberty
- Most potent of the 3 estrogens
Estrone:
- Less potent
- Primary form of circulating estrogen in women with menopasue
- As women age we see an increase in fat deposition (estrogen = fat soluble and stores well in fatty tissue, ovaries fail, estrone from the fat stores is released, circulating levels decline over time, this way there is no major shift
Estriol:
- Primary circulating form of estrogen during pregnancy
- Formed in the placenta
- When you are pregnant you will have the highest amount of estrogen you will ever have
What are the biological effects of estrogens?
- Growth and maturation of female reproductive organs
- Endometrium proliferation and thickening of vaginal mucosa
- Female fat pattern distribution (breast, buttocks and thighs)
- Increased bone deposition
- increased vascularity of the skin
- Decreased LDL formation and increased HDL cholesterol
- Increased coagulation
- Increased production of clotting factors (increases activity of clotting factors, more likely to get clots, if there is a history of increased coagulation or smoking can cause blood clots)
- Production of thin, clear, watery and elastic cervical mucus (allows for passage of sperm during ovulation)
What are the biological effects of progestins?
- Progesterone = most active endogenous progestin
- Increases mucus thickness and prevents sperm entry
- Limits and stabilizes endometrial growth
- Inhibits myometrial contractions (quiets the uterus to protect viability of the embyro)
- Increases body temperature
- Released during pregnancy because the body does not want to become pregnant again once it’s already pregnant
What are combination oral contraceptives?
- Have both an estrogen and a progestin
- Increased half life, orally viable
- Take hormones for 21 days, followed by 7 days of placebo to allow for menstruation to occur
What is important to ensure effectiveness?
Adherence, patient must take the pill every single day, and if they forget one day they can double up the next day and use another form of protection to prevent pregnancy
How do combination contraceptives inhibit ovulation?
- Low dose synthetic estrogens suppress FSH levels
- Low dose synthetic progestins suppress LH surge
- In the absence of LH and FSH, ovarian follicle does not mature and ovulation is inhibited
- Synthetic hormones exploit negative feedback loop preventing follicle maturation and ovulation; much like hormones produced by the placenta to halt the ovarian cycle
- Exploits negative feedback loop already in place
Synthetic progestins produce what?
- Thin and inactive endometrium
- Thick cervical mucus to inhibit sperm migration
What are extended formulations?
84 days of hormones and then 7 days of placebo, will still get normal menstrual cycle, blood does not accumulate, simply for convenience
What is the transdermal patch?
Changed every 7 days for three weeks, week 4 patch three to allow menstruation to occur