Term
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Definition
Class: sex steroids, GnRH agonist
Mechanism: stimulate GnRH receptors in pituitary, pulsatile --> FSH/LH production, sustained --> reduce FSH/LH production
Indications: synthetic, fertility treatment (pulsatile), prostate cancer, endometriosis, uterine fibroids
Adverse effects: initial stimulation (before desensitization), suppression of sex hormones for prolonged time, mood disturbances, osteoporosis eventually
Half-life: 2-4min |
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Term
| leuprolide (goserelin, nafarelin) |
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Definition
Class: sex steroids, GnRH agonist
Mechanism: superagonist, stimulate GnRH receptors in pituitary, pulsatile --> stimulate FSH/LH, sustained --> inhibit FSH/LH
Indications: fertility treatment (pulsatile), prostate cancer, endometriosis, uterine fibroids
Adverse effects: initial stimulation, mood disturbances, eventually osteoporosis
Half-life: 6hrs |
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Term
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Definition
Class: sex steroid, GnRH antagonist
Mechanism: competitive antagonist of GnRH at receptors in pituitary, induces rapid inhibition of LH and FSH w/o initial surge
Indications: prevent premature LH surge
Adverse effects: women (hot flashes, osteoporosis, thin skin), men (reduced muscle, impotence)
Excretion: feces and urine |
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Term
| human chorionic gonadotropin (hCG) |
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Definition
Class: sex steroids, FSH and LH affects
Mechanism: mimics hCG and LH actions
Indications: infertility treatment in males and females, mimice LH surge, increase androgen production, treat prepubertal cryptorchidism
Adverse effects: ovarian hyper-stimulation, multiple births |
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Term
| menotropins (human menopausal gonadotropins) |
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Definition
Class: sex steroids, FSH and LH affects
Mechanism: mimic endogenous FSH, LH and hCG
Indications: infertility treatment in males and females
Adverse effects: ovarian hyper-stimulation syndrome, multiple births
Excretion: urine |
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Term
| urofollitropin, follitropin |
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Definition
Class: sex steroids, FSH and LH affects
Mechanism: mimics FSH
Indications: infertility treatment in males and females
Adverse effects: ovarian hyper-stimulation, multiple births
Excretion: urine |
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Term
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Definition
Class: sex steroids, FSH and LH affects
Mechanism: synthetic androgen w/ weak activity, inhibits production o fLH/FSH, blocks enzymes essential for production of estrogen and progesterone in ovaries
Indications: endometriosis (atrophies ectopic tissue), HEREDITARY ANGIOEDEMA, STIMULATION OF ERYTHROPOIESIS
Adverse effects: hot flashes, weight gain, fluid retention, acne, increased LDL, smaller breasts, increase muscle mass, increased facial/body hair, muscle cramps, mood swings, voice deepening and clitoral enlargement, GI upset, depression, liver disease
Metabolism: hepatic |
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Term
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Definition
Class: sex steroid, estrogen agonist
Mechanism: most potent, endogenous, produced in ovaries; bind estrogen receptors, interact w/ DNA to impact gene transcription in multiple tissues
Indications: premenopausal hypogonaism (replacement therapy), suppression of menopause symptoms, contraceptives
Adverse effects: inc. risk of endometrial carcinoma (when w/o progestin), (infants in utero exposure), thromboembolic disorder, increase gall bladder disease, migraines, nausea, vomiting |
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Term
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Definition
Class: sex steroids, estrogen agonist
Mechanism: agonist at estrogen receptors; mixture of water soluble salts and estrogen-sulfate esters, slow absorption thru gut
Indications: HRT
Adverse effects: inc. risk of endometrial carcinoma (when w/o progestin), (infants in utero exposure), thromboembolic disorder, increase gall bladder disease, migraines, nausea, vomiting |
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Term
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Definition
Class: sex steroids, estrogen agonist
Mechanism: pro-drug, demethylated to ethinyl estradiol; agonist at estrogen recpetors, slower hepatic metabolism, long half-life, orally active
Indications: OC
Adverse effects: inc. risk of endometrial carcinoma (when w/o progestin), (infants in utero exposure), thromboembolic disorder, increase gall bladder disease, migraines, nausea, vomiting |
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Term
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Definition
Class: sex steroids, estrogen agonist
Mechanism: agonist at estrogen receptors, synthetic analog of estradiol, slower hepatic metabolism, long half-life, orally active, useful in OC
Indications: OC
Adverse effects: inc. risk of endometrial carcinoma (when w/o progestin), (infants in utero exposure), thromboembolic disorder, increase gall bladder disease, migraines, nausea, vomiting |
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Term
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Definition
Class: sex steroids, non-steroidal
Mechanism: from plants, estrogen-like structure, estrogenic or anti-estrogenic activity, weak, not regulated as drug
Indication: HRT, benefits unclear
Adverse effects: risk/benefits not clear |
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Term
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Definition
Class: sex steroids, affecting FSH and LH
Mechanism: blocks (-) feedback of estrogen on hypothalamus and pituitary; stimulates FSH and LH production, SERM
Indications: anovulatory infertility, off-label used to treat male infertility
Adverse effects: ovarian hyper-stimulation, increased incidence of multiple births, hot flashes, other menopause like symptoms
Metabolism: hepatic |
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Term
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Definition
Class: sex steroid, biphosphonate
Mechanism: increase bone density by selective inhibition of osteoclasts
Indication: osteoporosis, Paget's disease
Adverse effects: diarrhea, nausea, abdominal pain, avascular necrosis of jaw
Pharmacokinetics:
Absorption: orally, 10%
Distribution: bound in bone
Excretion: rapid |
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Term
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Definition
Class: sex steroid, estrogen contraceptive
Mechanism: inhibits ovulation (suppresses LH and FSH levels, eliminates LH surge)
Indication: contraceptive used in combo with a progestin
Contraindication: thromboembolic disorder, hormone-dependent neoplasia, liver tumor/dysfx, pregnancy
Adverse Effects: increased risk of thromboembolic and other CV diseases, benign hepatoma, gall bladder disease |
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Term
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Definition
Class: sex steroids, cancer tx
Mechanism: pro-drug, metabolites = SERM, functional competitive estrogen receptor antagonist, decrease estrogenic stimulation of tumor cells, agonist activity in some tissues
Indications: breast cancer
Adverse effects: nausea, vomiting, hot flashes, inc. risk of endometrial carcinoma from estrogenic stimulation of uterus, blood clots
Absorption: oral
Distribution: ppb, enterohepatic circulation
Metabolism: hepatic
Half-life: 5-7d |
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Term
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Definition
Class: sex steroids, cancer tx
Mechanism: SERM, functional competitive estrogen receptor antagonist, decrease estrogenic stimulation of tumor cells, agonist activity in some tissues
Indications: tx and prevent osteoporosis in postmenopausal women, reduce risk and tx or invasive breast cancer (lower risk of endometrial ca)
Adverse effects: hot flashes, leg cramps, lower incidence of blood clots, higher incidence of stroke death and long QT
Absorption: oral
Distribution: enterohepatic circulation
Metabolism: hepatic
Half-life: 1-3d |
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Term
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Definition
Class: sex steroid, aromatase inhibitors
Mechanism: inhibit aromatase, effectively lower estrogen levels, reduce hormonal stimulation
Indication: adjuvant therapy of breast cancer with tamoxifen; FIRST LINE tx in post-menopausal women
Adverse effects: hot flashes, inc. risk of osteoporosis, worse serum lipid profile, joint pain, lower risk thrombotic than tamoxifen
Absorption: oral
Metabolism: hepatic |
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Term
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Definition
Class: sex steroids, aromatase inhibitor
Mechanism: inhibit aromatase, effectively lower estrogen levels, reduce hormonal stimulation
Indications: adjuvant therapy of breast cancer, FIRST line in post menopausal
Adverse effects: hot flashes, inc. risk of osteoporosis, (-) effect on serum lipid profile, joint pain, lower risk of thrombotic than tamoxifen
Absorption: oral
Metabolism: hepatic |
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Term
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Definition
Class: sex steroids, aromatase inhibitor
Mechanism: inhibit aromatase, effectively lower estrogen levels, reduce hormonal stimulation
Indication: adjuvant breast ca tx w/ tamoxifen, FIRST LINE in postmenopausal
Adverse effect: hot flashes, inc. risk of osteoporosis, adverse on serum lipid profile, joint pain, lower risk of thrombotic than tamoxifen
Absorption: oral
Metabolism: hepatic |
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Term
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Definition
Class: sex steroids, progestins
Mechanism: inhibit ovulation, prevent fertilization thru effects in endometrium and cervix, suppress LH and FSH, eliminate mid-cycle LH surge, decrease freq. of GnRH pulses, decrease penetration of cervix by sperm by changing water to viscous secretion
Indications: post-menopausal HRT, contraceptives, maintenance of pregnancy
Absorption: high lipophilic, transdermal practical, oral (first pass effect)
Distribution: ppb extensively
Metabolism: hepatic
Half-life: 5min |
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Term
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Definition
Class: sex steroids, progestins
Mechanism: pro-drug, metabolized to progesterone but longer acting, inhibit ovulation, prevent fertilization thru effects in endometrium and cervix, suppress LH and FSH, eliminate mid-cycle LH surge, decrease freq. of GnRH pulses, decrease penetration of cervix by sperm by changing water to viscous secretion
Indications: post-menopausal HRT, contraceptives, maintenance of pregnancy
Absorption: high lipophilic, transdermal practical, oral (first pass effect)
Distribution: ppb extensively
Metabolism: hepatic
Half-life: 6-24hrs |
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Term
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Definition
Class: sex steroid, progestin only
Mechanism: inhibit ovulation and produce direct effects on reproductive tract; may interfere with implantation
Indications: post-menopausal HRT, contraceptives (inhibits ovulation, prevent fertilization; esp. lactating does not interfere with it), maintenance of pregnancy
Contraindications: thromboembolic disorders, hormone-dependent neoplasia, liver tumors or dysfx, pregnancy
Risk factors: smoking, age, diabetes, HTN, gallbladder disease
Adverse effects: irregular breakthrough bleeding, edema, weight gain, depression, headache, impaired fertility upon withdraw
Pharmacokinetics:
Absorption - highly lipophilic, oral and transdermal
Distribution - ppb
Metabolism - hepatic
Half-life - 6-24hrs |
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Term
| norgestrel, levonorgestrel |
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Definition
Class: sex steroids, post-coital contraception
Mechanism: prevents ovulation/fertilization, may also interfere with implantation, reduces risk of pregnancy 50-90%
Indication: post-coital contraception
Adverse effects: nausea, vomiting, abdominal pain, fatigue, HA, dizziness, breast tenderness
Metabolism: hepatic |
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Term
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Definition
Class: sex steroids, progestin agonist
Advatage: anti-androgenic and anti-mineralcorticoid activity, available in combination type oral contraceptives
Mechanism: pro-drug, metabolized to progesterone but longer acting, inhibit ovulation, prevent fertilization thru effects in endometrium and cervix, suppress LH and FSH, eliminate mid-cycle LH surge, decrease freq. of GnRH pulses, decrease penetration of cervix by sperm by changing water to viscous secretion
Indications: post-menopausal HRT, contraceptives, maintenance of pregnancy
Absorption: high lipophilic, transdermal practical, oral (first pass effect)
Distribution: ppb extensively
Metabolism: hepatic
Half-life: 6-24hrs |
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Term
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Definition
Class: sex steroids, medical abortion
Mechanism: competitive antagonist at progesterone and glucocorticoids receptors; misoprostol = prostagland that stimulates uterine motility
Indications: terminate intrauterine pregnancies up to 49d gestation, induces decidual breakdown in endometrium followed by 2d later with misoprostal to induce contractions ; Cushing syndrome
Adverse effects: bleeding, nausea, vomit, abdominal pain, fatigue, sepsis 1/100,000
Absorption: oral
Distribution: plasma
Half-life: 20-40hr |
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Term
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Definition
Class: sex steroids, androgen
Mechanism: bind androgen receptor, translocate to nucleus, interact w/ cofactors, alter regulation of target genes
Indication: androgen replacement therapy (hypogonadism), catabolic or muscle-wasting conditions
Adverse effects: increased PSA, emotional lability, HTN, CVD events
Pharmacokinetics:
Absorption - gel, patch, IM
Distribution - highly ppb
Metabolism - rapid, hepatic; some tissues transform it to dihydrotestosterone by 5a-reductase |
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Term
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Definition
Class: sex steroid, adrogenic, synthetic
Mechanism: derivative of dihydrotestosterone, agonist of androgen receptors
Indications: alcoholic hepatitis, Turner's syndrome, wieght loss by HIV, hereditary angioedema
Adverse effects: liver toxicity, swelling of arms/legs, frequent/persistent erections, breast tenderness/enlargement, decreased fertility (males), voice changes, hair loss, facial hair growth, clitoral enlargement, menstrual irregularities, increased LDL, decreased HDL
Pharmacokinetics:
Absorption - oral
Metabolism - liver, not to estrogen |
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Term
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Definition
Class: sex steroid, androgen (Anti-)
Mechanism: weak partial agonist at androgen receptor, may inhibit spermatogenesis and libido
Indications: Palliative treatment of advanced prostate cancer |
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Term
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Definition
Class: sex steroid, andorgen antagonist
Mechanism: competitive antagonist at androgen receptors
Indications: metastatic prostate cancer with GnRH analog
Adverse effects: hot flashes, overall pain, weight gain, GI upset, liver toxicity, gyneocomastia if w/ GnRH analog
Pharmacokinetics:
Absorption-oral
Metabolism-hepatic
Excretion-urine and feces |
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Term
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Definition
Class: sex steroids, anti-androgenic
Mechanism: 5-a-reductase inhibitor, blocks conversion of testosterone to DHT
Indications: BPH, male pattern baldness
Adverse effects: decreased libido, erectile dysfunction, swelling in hands/feet, gynecomastia
Pharmacokinetics:
Absorption-oral
Metabolism-hepatic |
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