Pharmacology [Repro] Flashcards
What is the mechanism of sildenafil?
Inhibit phosphodiesterase 5, resulting in increased cGMP and smooth muscle relaxation in corpus cavernosum
What is the mechanism of vardenafil?
Inhibit phosphodiesterase 5, resulting in increased cGMP and smooth muscle relaxation in corpus cavernosum
What are the indications for leuprolide?
Pulsatile - infertility
Continuous - prostate cancer, uterine fibroids, precocious puberty, endometriosis
What is the mechanism of leuprolide?
GnRH agonist when administered in pulses, antagonistic effect when continuous
What are the side effects of leuprolide?
Antiandrogen, nausea, vomiting
To what drug class does leuprolide belong?
GnRH analog
What are the indications for testosterone (and methyltestosterone)?
Hypogonadism, anabolic stimulation after burn or severe injury
What are the side effects of testosterone (and methyltestosterone)?
Masculinization in females, gonadal atrophy, premature closure of epiphyseal plates, dyslipidemia
To what drug class does testosterone (and methyltestosterone) belong?
Androgen
What are the indications for finasteride?
BPH, male pattern baldness
What is the mechanism of finasteride?
5α-reductase inhibitor
What are the side effects of finasteride?
Gynecomastia
To what drug class does finasteride belong?
Antiandrogen
What are the indications for flutamide?
Prostate carcinoma
What is the mechanism of flutamide?
Non-steroidal competitive inhibitor of testosterone receptor
To what drug class does flutamide belong?
Antiandrogen
What are the indications for ketoconazole?
Hirsutism of PCOS
What is the mechanism of ketoconazole?
General inhibition of steroid synthesis
What are the side effects of ketoconazole?
Gynecomastia, amenorrhea
To what drug class does ketoconazole belong?
Antiandrogen
What are the indications for spironolactone?
Hirsutism of PCOS
What is the mechanism of spironolactone?
Inhibits steroid binding
What are the side effects of spironolactone?
Gynecomastian, amenorrhea
To what drug class does spironolactone belong?
Anti-androngen
What are the indications for ethinyl estradiol?
Hypogonadism, ovarian failure, menstrual abnormalities, HRT in postmenopausal women, androgen-dependent prostate cancer
What are the contraindications for ethinyl estradiol?
Oestrogen receptor-positive breast cancer, hx DVT
What are the side effects of ethinyl estradiol?
Increased risk of endometrial cancer, vaginal bleeding in postmenopausal women
To what drug class does ethinyl estradiol belong?
Oestrogen
What is the mechanism of ethinyl estradiol?
Binds estrogen receptor
What are the indications for Diethylstilbestrol (DES)?
Hypogonadism, ovarian failure, menstrual abnormalities, HRT in postmenopausal women, androgen-dependent prostate cancer
What are the contraindications for Diethylstilbestrol (DES)?
Oestrogen receptor-positive breast cancer, hx DVT
What is the mechanism of Diethylstilbestrol (DES)?
Binds estrogen receptor
What are the side effects of Diethylstilbestrol (DES)?
Increased risk of endometrial cancer, vaginal bleeding in postmenopausal women, clear cell adenocarcinoma in women exposed in utero
To what drug class does Diethylstilbestrol (DES) belong?
Oestrogen
What are the indications for mestranol?
Hypogonadism, ovarian failure, menstrual abnormalities, HRT in postmenopausal women, androgen-dependent prostate cancer
What are the contraindications for mestranol?
Oestrogen receptor-positive breast cancer, hx DVT
What is the mechanism of mestranol?
Binds estrogen receptor
What are the side effects of mestranol?
Increased risk of endometrial cancer, vaginal bleeding in postmenopausal women
To what drug class does mestranol belong?
Oestrogen
What are the indications for clompihene?
Infertility and PCOS
What is the mechanism of clompihene?
Partial agonist at estrogen receptor, prevents feedback inhibition
What are the side effects of clompihene?
Hot flashes, ovarian enlargement, multiple pregnancy, visual disturbances
To what drug class does clompihene belong?
SERM
What are the indications for tamoxifen?
ER-positive breast cancer
What is the mechanism of tamoxifen?
Antagonist at estrogen receptor; specific for breast tissue
To what drug class does tamoxifen belong?
SERM
What are the indications for raloxifene?
Osteoporosis (reduces bone resorption)
What is the mechanism of raloxifene?
Agonist at estrogen receptor; specific to bone
To what drug class does raloxifene belong?
SERM
[…] and […] are both used for HRT in post-menopausal women to avoid an increased risk of […] cancer.
Oestrogen and progesterone are both used for HRT in post-menopausal women to avoid an increased risk of endometrial cancer.
What are the indications for anastrazole?
Breast cancer inpostmenopausal women
What is the mechanism of anastrazole?
Aromatase inhibitor
What are the indications for exemestane?
Breast cancer in postmenopausal women
What is the mechanism of exemestane?
Aromatase inhibitor
What are the indications for progestins?
Contraception, endometrial cancer, abnormal uterine bleeding
What is the mechanism of progestins?
Binds progesterone receptor; reduces proliferation of endometrium, thickens cervical mucus
What are the indications for mifepristone (RU-486)?
Abortion; administered with misoprostol
What is the mechanism of mifepristone (RU-486)?
Competitive inhibitor at progesterone receptor
What are the side effects of mifepristone (RU-486)?
Heavy bleeding, abdominal pain
What are the indications for misoprostol (PGE1)?
Abortion; administered with mifepristone
What is the mechanism of misoprostol (PGE1)?
Synthetic prostaglandin analog
What are the indications for terbutaline?
Relaxation of premature uterine contractions
What is the mechanism of terbutaline?
β2-agonist
What are the indications for tamsulosin?
BPH
What is the mechanism of tamsulosin?
α1-antagonist, inhibits smooth muscle contraction, selective for prostatic receptors
What are the indications for sildenafil?
Erectile dysfunction
What are the side effects of sildenafil?
Headache, flushing, impaired blue-green color vision, hypotension, dyspepsia
What are the contraindications for sildenafil?
Patients taking nitrates (lethal hypotension)
What are the indications for vardenafil?
Erectile dysfunction
What are the contraindications for vardenafil?
Patients taking nitrates (lethal hypotension)
What are the side effects of vardenafil?
Headache, flushing, impaired blue-green color vision, hypotension, dyspepsia
To what drug class does sildenafil belong?
PDE5 inhibitor
To what drug class does vardenafil belong?
PDE5 inhibitor
What are the indications for danazol?
Endometriosis, hereditary angioedema
What is the mechanism of danazol?
Partial agonist at androgen receptor
What are the side effects of danazol?
Weight gain, edema, acne, hirsutism, masculinization, hepatotoxicity, dyslipidemia
To what drug class does danazol belong?
Androgen
What are the indications for combined oestrogen/progestin?
Contraception
What are the contraindications for combined oestrogen/progestin?
Smokers >35 y/o, hx DVT, stroke, ER+ cancer
What is the mechanism of combined oestrogen/progestin?
In combination prevents ovulation
What are the side effects of combined oestrogen/progestin?
Thrombosis