Flashcards in Pharm 37 Objectives Deck (44)
What is the rationale for the replacement use of estrogen and estrogen/progestin in postmenopausal osteoporosis and for menopausal symptoms?
-prevention of accelerated bone loss after menopause who cannot take non-estrogen medications
-relief of menopausal symptoms: hot flashes, depression, insomnia, symptoms of vulvar, vaginal, and urethral atrophy
-take the lowest dose for the shortest duration needed
What are the effects of estrogens on clotting factors?
enhance blood coagulation by increasing synths of coagulation factors
What are the effects of estrogen on cholesterol tests?
decrease LDL while increasing HDL
What are the effects of estrogen on thyroid hormone disposition?
high levels of exogenous estrogen increase thyroxine binding globulin
-cause hypothyroidism in those taking thyroid replacement
What are the effects of estrogen on FSH and LH?
high levels suppress FSH and LH in menstrual cycle
What are the types of estrogens used therapeutically?
What is the therapeutic action of estrogen?
What is the therapeutic action of progestin?
create a hostile environment
What are the adverse effects of estrogen?
nausea, breast tenderness, hypertension, melisma, headache
What are the adverse effects of progestin?
breast tenderness, headache, fatigue, mood changes
What are the contradictions of estrogen?
-DVT, PE or history of
-Stroke or history of
-Breast cancer or history of
-Breastfeeding <21 days
-Age >35 + >15 cigarettes/day
-Ischemic heart disease/cardiomyopathy
-Major surgery with prolonged immobilization
-Migraine with aura
-Liver cancer or severe cirrhosis
What are the potential mechanism of action of combined oral contraceptives?
-Feedback inhabitation of -GnRH section from the hypothalamus leading to decreased gonadotropic secretion and inhabitation of ovulation
-Reduce FSH secretion and maturation of follicle (estrogen component)
-Inhibit the midcycle LH surge required for ovulation (progestin component)
What are the most common drug interactions with combined oral contraceptives?
-antibiotics: cause N/V/D and forgetfulness during illness
-penicillins and tetracylines
-rifampin and griseofulvin
What is the rational for the various dosage schedules?
What estrogen is most commonly found in combined oral contraceptives?
What is the starting dose of EE?
start low at 20 mcg and titrate up to 30 to 35 mcg
When do you increase estrogen dose?
if there is early or mid-cycle spotting/BTB, vasomotor symptoms, atrophic vaginitis
When do you decrease the estrogen dose?
if there is nausea, breast tenderness, hypertension, melisma, headache
What is a low estrogen dose?
What are the most common progestins used in contraception?
Rank each by relative androgenic potencies (most to least androgenic)
evonorgestrel/norgestrel > norethindrone > desogestrel/norgestimate > dosperinone/dienogest (anti-adrogenic)
List the other type of hormonal contraceptive agents other than COCs
-patch (Xulane or Evra)
-vaginal ring (NuvaRing or Annovera)
Limitations/CI of Xulane, Evra - Patch
higher incidence of thrombosis d/t higher estrogen level
- less effective in pts over 198 Ibs (90 kg)
Limitations/CI of NuvaRing, Annovera - Vaginal Ring
Nuva: no need for back up methods if out for less than 48 hours
Anno: if out for >2 hours need 7 days of back up method and unknown effectiveness in pts BMI >29
Limitations/CI of Nexplanon - Implant
-liver disease or liver tumor
-unexplained vaginal bleeding
What is progestin-only contraception place in therapy?
-Premenstrual dysphoric disorder (PMDD)-Yaz
What are the advantages of progestin-only contraception?
-Less interface w/breast feeding
-Less risk of thrombosis
-No estrogenic SEs
What are the disadvantages of progestin-only contraception?
-Must be taken at the same time every day, within 3 hrs
-Taken every day, not cyclically: NO placebo pills
-Less effective contraceptive
What is the MOA of Levonorgestrel (Plan-B One-Step)?
a progestin that prevents ovulation and fertilization by altering tubal transport of sperm and/or ova