Pharm - PCOS Wk2 Flashcards
What is the MOST COMMON endocrine abnormality in patients of childbearing age?
Polycystic Ovary Syndrome PCOS
the Clinical presentation of PCOS is quite variable but manifests with some degree of…
hyperandrogenism, ovulatory dysfunction, polycystic ovaries, and insulin resistance
Many patients with PCOS will present with concerns related to…
acne, hirsutism, fertility, menstrual irregularities, obesity and dysglycemia
Pathophysiology of PCOS is complex but involves…
inappropriate gonadotropin secretion, insulin resistance with hyperinsulinemia, and excessive androgen production
High levels of estrogen and progesterone results in what?
suppress GnRH (Gonadotropin Releasing Hormones) release from the hypothalamus
Reduced GnRH results in what?
reduced FSH (Follicle-Stimulating Hormone) and LH (Luteinizing Hormone) release from the pituitary
Combined Oral Contraceptives are a combination of what?
estrogen and a progestin
the combined oral contraceptives in PCOS patients, the estrogen component does what?
suppresses LH resulting in a reduction of androgen production and increases production of SHBG in the liver (which reduces free testosterone)
the combined oral contraceptives in PCOS patients, the progestin component does what?
inhibits the LH surge resulting in reduced ovarian androgen production
What is first generation progrestin called?
nonrethindrone
what is second generation progrestin called?
norgestrel and levonorgestrel
First and second generation progrestins have what?
a higher risk of metabolic side effects and higher androgenic activity
What is third generation progrestin called?
norgestimate
what is the fourth generation progrestin called?
drospirenone
third and fourth generation progestins…?
cause fewer metabolic adverse effects
what generation of progestins are anti-androgenic?
fourth-generation progestins
what progestins has the greatest anti-androgenic activity among all progestins?
cyproterone acetate
When choosing an oral contraceptive beyond simple contraception, what will ultimately guide the selection
the activity of the progestin
what are the types of combinations of oral contraceptives?
- monophasic pills
- biphasic pills
- triphasic pills
what are monophasic pills?
the most common and provide a steady dose of hormones throughout the entire pack
what are biphasic pills?
contain two sets of pills at different strengths. Usually the dose of estrogen is the same throughout but the dose of the progestin changes
What are triphasic pills?
steady estrogen and three progestin dosages
what are the non-contraceptive benefits of oral contraceptives?
- increased bone mineral density
- decreased acne
- decreased ovarian, endometrial, colorectal cancers
- decreased peri-menopausal symptoms
- decreased risk of fibroids
- decreased benign breast disease
when using oral contraceptives what is the danger signal to watch for?
ACHES - abdominal pain, chest pain, headaches, eye problems, severe leg pain
Progestin only pills are sometimes referred to as ?
“mini pills”
progestins does what?
inhibit the LH surge preventing ovulation, thicken cervical mucus, and decrease motility of an ovum in the fallopian tubes
what are the two emergency postcoital contraceptions?
levonorgestrel and ulipristal acetate
a single does of levonorgestrel used within 24 hours of unprotected intercourse prevents ? of expected pregnancies
95%
efficacy of levonorgestrel is highest if treatment is ?
provided within 24 hours, but can be taken up to 5 days after unprotected intercourse
Health Canada has issued an advisory that levonorgestrel is less effective in individuals weighing ? and ineffective in those weighing more than ?
75 – 80 kg
80 kg
what are the adverse effects of levonorgestrel
- nausea
- vomiting
- dizziness
- fatigue
Ulipristal acetate needs to be taken…
5 days of unprotected intercourse or contraceptive failure
Ulipristal acetate is a ? that prevents ? from occupying its receptor by competitive inhibition and is believed to inhibit or delay ovulation
- selective progesterone receptor modulator
- progesterone
which emergency postcoital contraception is more effective when used 72-120 hours after unprotected intercourse
ulipristal is more effective than levonorgestrel
Ulipristal may be the better option when contraception is required after ? or in those with a ?
- 72 hours
- BMI over 25
what are the adverse effects of ulipristal acetate
- nausea
- headache
- dysmenorrhea
- abdominal pain
- fatigue
- dizziness
combined oral contraceptives help with…?
help with menstrual cyclicity, hirsutism, and acne
insulin sensitizers do what?
reduce concentrations and can ameliorate the consequences of hyperinsulinemia and hyperandrogenemia
what are the main insulin sensitizers?
metformin and thiazolidinediones
what does metformin do?
inhibits hepatic gluconeogenesis and reduces insulin concentrations and androgen production in the ovary
what is the first-line for dermatologic signs and symptoms of hyperandrogenism (hirsutism)
pharmacologic therapy with oral contraceptive therapy
what is the antiandrogen medication most often used for hirsutism?
spironolactone
what does spironolactone do?
Inhibits ovarian and adrenal steroidogenesis, competes for androgen receptors in hair follicles, and inhibits 5α-reductase activity
what does finasteride do?
Reduces 5α-dihydrotestosterone concentrations by 50% to 60% by inhibiting 5α-reductase in the skin and reproductive tissues
what does aromatase inhibitors do?
work by blocking the conversion of androgens to estrogens
- decreases estrogenic activity and reduces the negative feedback inhibition on the hypothalamus and pituitary allowing for an increase in FSH
what are the 2 main drug options of aromatase inhibitors
letrozole and clomiphene citrate
what is the only option available in Canada for aromatase inhibitors?
Letrozole
what are the adverse effects of letrozole?
- fatigue
- dizziness
- hot flashes
- edema
- nausea
