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Drugs to Treat Infertility
Female and Male infertility
13
Medical
Undergraduate 4
03/22/2009

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Cards

Term

Female Infertility

Casue?

Treatments?

 

Definition
  • Infertility is caused by the lack of growth of the follicle and ovulation
  • Treatment Options
    • First Line: Clomiphene (ER antag)
    • Second Line:
      • Gonadotropins (Supply FSH or LH)
      • Menotropins (FSH and LH)
      • Pair with GnRH Antag
Term

Clomid

MOA?

USe?

ADR?

Definition
  • Clomiphene®
  • Rx: induce ovulation in anovulatory (irregular periods) women with a funcitonal HPO axis
  • MOA: (Estrogen Receptor Antag)
    • blocks estrogen receptors on the HP axis so no more negative feedback
    • results in increase release of FSH and LH, leading to follicular developement and ovulation
  •  ADR:
    • Birth-defects (if taken when pregnant)
    • blurred vision
    • dose-related increase in multiple births
    • hot flashes
    • ovarian enlargement, ovarian cysts
Term
Gonadotropins as Second Line Therapy for Infertility
Definition

FSH: follicle-stimulating hormone

recombinant or ultra-purified forms

injected sq daily for 7-10 days

– follicular development monitored by ultrasound

– also used to mature multiple follicles to harvest many eggs for In Vitro Fertilization (Assisted Reproductive Technology)

 

LH: luteinizing hormone

-adminster after the last day of FSH dose, to micmic the LH surge

hcg: human chorionic gonadotropin

– recombinant or purified forms

– produced by placenta, diagnostic for pregnancy

given one day after last dose of FSH

activates LH receptor, thus mimicking LH surge

Term

Menotropins as Second Line Therapy for Infertility

 

Definition

• menotropins

– purified from urine of postmenopausal women

– ~ equal content of LH and FSH

 

*can be used instead of gonadotropins bc it contains FSH and LH

Term
Gonadorellin
Definition

synthetic GnRH

To test activity of pituitary gland

-will inject GnRH and it should stimulate Pituitary to release FSH and LH

-so then measure amount of FSH and LH produced.

Term
Adverse Effects of Gonadotropins
Definition

·         25% of the patients treatment with gondaotropins result in multiple births.

·          Anything that over stimulate the ovaries can lead to ovarian cysts. 

·         A very important adverse effect that occur in the gonadotropin but not much in Clomiphene is called ovarian hyper-stimulation syndrome.

o    It is very serious and occurs in 6% of the patients.

o   So when the ovaries are stimulated by the gonadotropins, they secrete an uknown substance that increases the permeability of the blood vessels.

o    And then as a result fluid will accumulate in various cavities (the abdominal, the pericardium, the thorax)

o   So the patient starts to retent fluid in these cavities that leads to pain, distention and can lead to a thrombo-embolic event. 

o   You can think of it will almost a congestive heart failure type of event especially if u have fluid around the heart. 

o   So the patient has to be counseled to watch out for any fatigue, SOB, abdominal distention or other symptoms of heart failure.

Term

Ganirelix and Cetrorelix

Definition

GnRH Receptor Antagonists

*its important that we don’t administer the LH until after the last day of the FSH dose.

-GnRH Receptor Antag is used to prevent any early endogenous release of LH and release of FSH while giving exogenous administration

Term
Male HPT axis
Definition

·         Again the hypothalamus releases GnRH

·         and activates the GnRH receptors on the pituitary

·         and cause the release of FSH and LH.

·         But in the testes, when it is activated, it causes the release of Testosterone.

o   So the testes makes most of the testosterone and a little bit is produce by the adrenal gland in both males and females but the testes make the majority.

 

Term

5-Alpha Reductase

Definition
  • converts testosterone to a more potent and efficacious agonist called “dihyrotestosteorne.”
  • So dihydrotestosterone is more potent at the androgen receptor than is testosterone.
Term
Aromatase
Definition

o   converts testosterone to estrogen.

This is how males have circulating levels of estrogen. And estrogen in males is important for increasing bone and mineral density and can cause gynecomasty. And  

estrogen can also feedback and inhibit the production of testosterone.

Term

Male Infertility

What cause it?

How to treat?

Definition

Cause: due to insufficeint FSH and LH levels.

-FSH stimulates production of proteins require for sperm growth

-LH stimulates testosterone synthesis and sperm production

 Treatment:

-Clomiphene: increase FSH and LH levels

-gonadotropins: spermatogensis and testes maturation

 

 

Term
Clomiphene for Male Infertility
Definition

clomiphene increases male LH and FSH

– used to evaluate male reproductive axis and treat infertility

Term
Gonadotropins for Treating Male infertility
Definition

induce testes maturation, testosterone production and spermatogenesis

6 - 24 months for full effect

 

– adverse effect: gynecomastia (via conversion of testosterone to estrogens)

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