Other Hormone Meds Flashcards
MC complaint women have during menopause is?
Hot flashes
We give this during menopause to relieve GU atrophy; reduce pain w/sex, relieves vasomotor instability (hot flashes), improve sleep, reduce bone resorption in osteoporosis, stabilize mood swings…
Estrogen, can use estrogen vaginal products too
AEs/Risk in estrogen therapy?
CV risk, cancer, thrombosis…esp. endometrial cancer and BREAST CANCER (so we need a good Hx)
If a pt has a uterus, what do you need to use with the estrogen?
Progestin…if they’re had a hysterectomy, then you don’t need to add progestin
We use medroxyprogesterone for progestin therapy in menopause, what’s the good and the bad for that?
Benefits: lowers risk of irregular bleeding, endometrial hyperplasia, carcinoma, protection against breast carcinoma, enhancement of estrogen prophylaxis of osteoporosis
AEs: bloating, weight gain, irritability, depression, unpredictable endometrial bleeding
The women’s health initiate study looked at long term risks of hormone replacement therapy
Lung cancer, breast cancer, endometrial cancer, ovarian cancer (estrogen)
Estrogen + Cyclic progesterone, estrogen + continuous progesterone, intermittent are the three therapy regimens, explain.
Cyclic = mimics female cycle
Continuous refers to progesterone
Intermittent is the progesterone 3 days on, 3 days off
Vaginal estrogen products are indicated just for what?
Vaginal atrophy, no systemic effects except the femring
Bazedoxifene w/ conjugated estrogens (Duavee)…the B is a selective estrogen receptor modulator (agonist/antagonist) so it acts as an agonist of estrogen receptors in some estrogen sensitive tissues and antagonist in others (uterus)…reduces risk of endometrial hyperplasia, what is it used for?
Moderate to severe vasomotor symptoms from menopause and preventions of postmenopausal osteoporosis
Duavee has what adverse reactions and preg category?
CV disorders, hypertriglyceridemia, malignant neoplasms, gallbladder disease
Preg cat X
Non-hormonal options for menopause include what drug classes?
Vaginal lubricants
Selective Estrogen Receptor Modulators (SERMs - raloxifene)
SSRIs (Paroxetine mesylate)
SNRIs (venlafaxine)
Clonidine, gabapentin, methyldopa
Herbals/phytoestrogens for menopause?
Red clover, soy isoflavones, black cohosh, other
What are the three selective estrogen receptor modulators (SERMs) we talk about?
Ospemifene
Tamoxifen
Raloxifene
SERMs are agonists where we want them and antagonists mostly to reduce cancer risk, but might cause hot flashes, what are the other AEs?
CV risk, stroke, DVT, PE, endometrial cancer risk
This drug is used for treatment of moderate to severe dyspareunia caused by valvular and vaginal atrophy (menopause) but is NOT approved for osteoporosis
Ospemifene
Some CYP DIs
This drug is not really used for much outside of breast cancer and prevention of breast cancer in high risk women…again NOT for osteoporosis
Tamoxifen
This drug can be used to prevent/treat osteoporosis in postmenopasual women…not for premenopausal women (teratogen)
Raloxifene PO…DIs include bile acid resins, warfarin, thyroid hormones
Drug that mediates ovulation through increased output of pituitary gonadotropins and estrogens by inhibiting the action of stronger estrogens on the body’s negative feedback system…basically it’s to treat ovulation failure, help her get pregnant, nom ore than 3 courses recommended.
Clomiphene (Clomid) PO
AEs look like menopause (b/c increased LH/FSH)…also increases possibility of multiple fetuses
Drug class that inhibits production of estrogen by blocking _________, a cytochrome p450 enzyme that distinguishes estrogen from progesterone
Aromatase inhibitors like Letrozole, Anastrozole, Exemestane
Two progesterone antagonists are? What do they do?
Mifepristone (Mifeprex): termination of intrauterine pregnancy up to 70 days of gestation
Mifepristone (Korlym): treat hyperglycemia in pts with Cushing syndrome
Anabolic actions of androgens stimulate the production of RBCs in pts w/refractory anemia (renal disease)…testosterone is inactivated when administered orally why?
First pass effect
Clinical use of androgens (testosterone) in men and women?
Senile osteoporosis and anemia
Men: replacement therapy with testosterone deficiency; testicular insufficiency, impotence, primary hypogonadism
Women: hypopituitarism (w/estrogen), metastatic breast cancer and endometriosis
This act declared anabolic androgens and prohormones as schedule III drugs b/c high potential for abuse/misuse?
Anabolic steroid control acts of 1990 and 2004
AEs of androgens?
Adult males: azoospermia, oligospermia, priapism, impotence, gynecomastia, PREMATURE CLOSURE OF BONE EPIPHYSES IN PRE-PUBERTAL MALES (GROWTH STUNTED)
Females get masculinized
Androgens that are long-acting come in what form, what about short acting?
Long: IM/SQ
Short: transdermal
There are also oral androgens and anabolic androgens, used for what?
Oral: replacement, carcinoma of breast, post-pubertal cryptorchidism
Anabolic: weight gain where protein breakdown is at fault…anemia’s form deficient RBC production
(See drug chart)
Androgen derivative used to treat endometriosis and fibrocytic breast disease, orally active synthetic androgen that supremes pituitary ovarian axis?
Danazol (Danocrine) PO
Clinical uses for anti-androgens and androgen antagonists?
Prostate cancer, endometriosis, advanced breast cancer, female hirsutism, alopecia, acne, precocious puberty in males, BPH
For BPH we use what drugs?
A-blockers (zosins)…tamsulosin and alfuzosin are only for BPH
Also 5a Reductase inhibitor: Finasteride
What is the main indication for using Finasteride?
BPH: halts BPH profession and reduces prostate size and symptoms over time, also can be used for male pattern baldness
AEs with Finasteride?
Decreased libido, ED…
Preg cat X: women have to not come into any contact w/crushed or broken tablets, semen from a male partner exposed to Finasteride also bad
Main causes of ED?
Med, Arteriosclerosis, smoking and diabetes are big factors too
PDE5 is responsible for degradation of cGMP in the corpus cavernosum, so inhibiting it increases blood flow there…no effect in the absence of sexual stimulation** so used for what?
ED, pulmonary arterial HTN, BPH
Vardenafil/Sildenafil lasts for 4 hours
Tadalafil lasts 36 hours
What do you have to keep in mind when giving sildenafil (Viagra)?
What about Vardenafil (levitra)?
Reduced dose in renal/hepatic impairment for viagra
Levitra, don’t use with severe liver impairment or on hemodialysis
Tadalafil has two other indications, which are?
Adcirca brand: pulmonary arterial HTN
Cialis: BPH
AEs of PDE5-Is?
Upset stomach, nasal congestion, diarrhea, rash
HA, flushing of skin, HoTN, priapsm, vision changes (PDE6 actually bust still effects it by blurring/color changes)
DIs for PDE5-Is?
Nitrates and a-blockers
Nitrates are CI, a-blockers it’s just a caution, maybe don’t use with pt who already has low HoTN
A-blockers for BPH: use tamsulosin b/c it’s selective for that, less HoTN
Two FDA-approved androgens are?
Non-FDA approve supplement for ED?
FDA: fluoxymesterone, methyl testosterone, testosterone enanthate, testosterone propionate
Alprostadil
Non-FDA: Yohimbine HCl
This drug is an alternative to conventional treatment, particularly for ED due to neurogenic, vasculogenic, psychogenic, or mixed etiology?
Not preferred
Alprostadil
There’s also injectable and urethral pellet options
CI in men w/conditions that predispose them to priapism or ED in men with fibrotic conditions of the penis
In female sexual dysfunction, what works?
Non-pharm first
Dopamine agonists in women with Parkinson’s
FLIBANSERIN IS THE ONLY MED APPROVED FOR FEMALE SEXUAL DYSFUNCTION
There are herbal supplements
The MoA of this drug exhibits sertonergic and dopaminergic activity that treats premenopausal women with acquired generalized hypactive secual desire disorder (HSDD)
Flibanserin (Addyi)
Don’t use with co-existing psych condition, problems in relationship, post-menopause, or to enhance performance
AEs: look out for dizzy, drowsiness, HoTN, syncope…alcohol makes that worse, take these at bedtime
