Drugs Flashcards
(40 cards)
GnRH
Class: GnRH Agonist
MOA: Increases FSH and LH secretion from the Anterior Pituitary
Indications: Kallmann syndrome, female and male infertility, diagnosing LH responsiveness
Leuprolide
Class: Synthetic GnRH analog
MOA: Continuous, non-pulsatile administration causes desensitization of the GnRH receptor on the Anterior pituitary to decrease FSH and LH release (or testosterone in men)
Indications: Prostate cancer, central progressing precocious puberty, breast cancer
FSH, LH, CG
Class: Gonadotropins
MOA: Combinations of FSH, LH, and CG are used to increase sperm counts in men and for follicle maturation in women. FSH can be used alone but is more effective when used with LH or CG. LH and CG are ineffective alone
Indications: Male and female infertility due to pituitary insufficiency
* Causes pain from ovarian enlargement
Tamoxifen
Class: SERM
MOA: ER partial agonist, antagonizes estrogen in the breast, agonizes estrogen effects in the uterus in post menopausal women
Indications: Breast cancer
* Increased endometrial cancer due to weak estrogen effects there
Fulvestrant
Class: SERM
MOA: pure ER antagonist
Indications: Breast cancer
Clomiphene
Class: SERM
MOA: ER partial agonist; inhibits estradiol binding to receptors in anterior pituitary and hypothalamus, causes less negative inhibition and more FHS and LH release from anterior pituitary. LH and FSH surges allows for ovulation to happen
Indications: amenorrheic and infertile women who wish to become pregnant
Anastrazole
Class: aromatase inhibitor
MOA: inhibits estrogen synthesis by inhibiting aromatase; blocks the aromatization of testosterone –> 17B estradiol and Androstenedione –> estrone
Indications: Breast cancers that are resistant to Tamoxifen
Letrozole
Class: aromatase inhibitor
MOA: inhibits estrogen synthesis by inhibiting aromatase; blocks the aromatization of testosterone –> 17B estradiol and Androstenedione –> estrone
Indications: Breast cancers that are resistant to Tamoxifen
Mifepristone
Class: Progesterone receptor antagonist
MOA: used with Misoprostol. “abortion pill” prevents progesterone from binding its receptor and does not allow maintenance of a pregnancy. Causes decreased endometrial development and secretions, decreased lactation, and decreased thermogenic effects
Indications: desired abortion of fetus < 49 days
Combination synthetic estrogen and progesterone
- Inhibits ovulation
Class: contraceptives
MOA: Estrogen + Progestin combo - strong negative feedback. Decreased FSH and LH and prevention of LH, FSH surge. Prevents follicular development and prevents ovulation. Also thickens cervical mucous.
Adverse Effects: VT, strokes and MI, breakthrough bleeding, weight gain, erythema nodosum
Interfering Drugs: Rifampin, Anticonvulsants, Griseofulvin, HIV medications
Depo Provera - Medroxyprogesterone
- Inhibits ovulation
Class: contraceptives
MOA: Decreases gonadotropins. Suppresses ovulation and thickens cervical mucous
Indications: Good for women who can’t take estrogen or forget to take pills, or have chronic medical problems
Adverse Effects: Causes amenorrhea and spotting and weight gain
Vaginal Ring (Nuvaring)
- Inhibits ovulation
Class: contraceptives
MOA: Contains 15 mg of Ethinyl Estradiol and 120 mcg of etonogestrel (synthetic desogestrel). Insert ring into vagina and it stays for 3 weeks. Suppresses ovulation. Thickens cervical mucus. Prevents endometrial thickening.
Adverse Effects: More vaginal discharge
Continuous Progestin “Minipill”
- Changes cervical mucus
Class: contraceptives
MOA: Increases cervical viscosity, endometrial thickness, and fallopian tube mobility, reducing sperm penetration. Does not inhibit the mid-cycle gonadotropin surge.
Indications: use progestin only minipill when estrogen is contraindicated. Sickle-cell, CAD, SLE
Adverse Effects: Progestin withdrawal causes bleeding (mimics physiologic response). Must be taken every day at the same time. Efficacy increased while breast feeding
Seasonale/Seasonique
- Inhibits ovulation
Class: contraceptives
MOA: 3 month supply of combined estrogen and progestin followed by 7 placebo pills which allows menses.
Indications: endometriosis or dysmenorrhea
Effects: 4 periods per year
Lybrel
- Inhibits ovulation
Class: contraceptives
MOA: active pills for the entire year
Indications: endometriosis or dysmenorrhea
Effects: no real menses. Expect breakthrough bleeding.
Plan B - Levonorgestrel
- Inhibits ovulation
Class: contraceptives
MOA: inhibits ovulation, disrupts follicular development, interferes with maturation of corpus luteum
Indications: post sex emergency
Combination Estrogen and Progestin
Class: HRT
MOA: Replaces hormones that are decreasing in order to decrease symptoms
Indications: menopause - hot flashes and sweating. Long term - GU atrophy, osteoporosis, CVD
Adverse Effects: Must combine with progestin to reduce the probability of endometrial cancer
Flutamide
Class: Androgen receptor antagonist
MOA: competitive inhibitors of AR and inhibits both testosterone and DHT binding
Indications: prostate cancer
Bicalutamide
Class: Androgen receptor antagonist
MOA: competitive inhibitors of AR and inhibits both testosterone and DHT binding
Indications: prostate cancer
Finasteride
Class: 5a-reductase inhibitor
MOA: inhibits 5a-reductase which normally converts testosterone to DHT
Indications: BPH and Male pattern baldness
Sildenafil (Viagra)
Class: Erectile Dysfunction Drugs
MOA: Inhibit PDE5 and prolong erection time by maintaining smooth muscle relaxation and vasodilation
Indications: Erectile dysfunction
* Major difference between 3 ED drugs is half life. Viagra lasts 1 hour
Adverse Effects: Headache, flushing, dyspepsia, vision impairment
Contraindication: recent MI or stroke or hypotension
Vardenafil (Levitra)
Class: Erectile Dysfunction Drugs
MOA: Inhibit PDE5 and prolong erection time by maintaining smooth muscle relaxation and vasodilation
Indications: Erectile dysfunction
* Major difference between 3 ED drugs is half life. Levitra lasts 0.7-0.9 hours
Adverse Effects: Headache, flushing, dyspepsia, vision impairment
Contraindication: recent MI or stroke or hypotension
Tadalafil (Cialis)
Class: Erectile Dysfunction Drugs
MOA: Inhibit PDE5 and prolong erection time by maintaining smooth muscle relaxation and vasodilation
Indications: Erectile dysfunction
* Major difference between 3 ED drugs is half life. Cialis lasts 2 hours
Adverse Effects: Headache, flushing, dyspepsia, rhinitis, vision impairment
Contraindication: recent MI or stroke or hypotension, hepatic or renal impairment
Misoprostol
PGE1 analog
Causes uterine contractions
Used with Mifepristone for abortions
