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men diseases
| Question | Answer |
|---|---|
| what are the 3 LHRH agonists | leuprolide, goserlin, triptorelin pamoate |
| what are the 3 anti-androgens | flutamide, nilutamide, bicalutamide |
| GnRH agonist MOA | constant delivery leads to down-regulation of receptors on pituitary resulting in decreased production of LH and FSH |
| RnRH side effect and treatment for it | hot flashes.. initial flare of symptoms so anti- androgens should be given at beginning of treatment |
| uses for GnRH agonists | estrogen receptor positive breast cancer, endometriosis, advanced prostate cancer |
| anti-androgens MOA and use...... NOT CURATIVE | blocks androgen receptors on prostate... mainly used for flare protection in GnRH therapy, palliative for metastatic prostate cancer....NOT CURATIVE |
| ADR of anti-androgens | endocrine related...decreased libido, gynecomastia, Nilutamide can cause visual disturbances |
| static component of BPH | hyperplasia of the prostate narrowing the urethra |
| dynamic component of BPH | prostatic smooth muscle tone through ALPHA-adrenergic receptors |
| Drugs to treat BPH | 5 alpha reductase inhibitors (static) and alpha1 adrenergic antagonists (dynamic) |
| 5 alpha-reductase inhibitors | finasteride and dutasteride |
| 5 alpha-reductase inhibitors MOA | reduce size of prostate (6 months) by blocking conversion of testosterone to DHT...not as god as alpha 1 blockers |
| 5 alpha-reductase inhibitors metabolism | through P450 3A4 |
| 5 alpha-reductase inhibitors ADR | impotence and decreased libido |
| most receptors on prostate are... | alpha 1A subtype and bladder is mostly A1 |
| alpha 1 blockers | alfuzosin and tamsulosin |
| alpha 1 blockers ADR | postural hypotension and syncope, sexual dysfunction |
| Tamsulosin | alpha 1A and 1D (bladder) selective.....favors blockade in the prostate..... little effect on blood pressure....MUST BE TAKEN WITH FOOD |
| Alfuzosin | distributes in prostate.... should not be used with hepatic impairment |
| combination therapy | 5 alpha reductase inhibitor and alpha blocker for moderate to severe BPH symptoms |
| ED treatments 3 types | Phosphodiesterase inhibitors (PDE5), intrapenile therapies, endocrine therapy |
| PDE5 inhibitors.. first line therapy MOA | inhibits phosphodiesterase 5 enzyme to inhibit the degradation of cGMP which leads to decreased intracellular Ca+ and relaxation of smooth muscle |
| PDE5 found..... | corpora cavernosa, lung, kidney, and platelets |
| PDE5 inhibitors | sildenafil, tadalafil, vardenafil |
| taladafil lasts | up to 36 hours |
| ADR of PDE5 inhibitors | don't use with nitrates, be careful with alpha blockers (hypotension), may cause TRANSIENT HEARING LOSS AND TINITIS |
| Yohimbine (alpha 2 blocker) | 2nd or third line therapy |
| Yohimbine ADR | CNS reactions, inhibits MAO's, and avoid tyramine containing foods (cheese, wine, liver) |
| Intra-urethral (alprostadil) | intraurethral suppository, synthetic vasodilator like PGE1 |
| intracavernosous injections 3 types | alprostadil, papavarine (nonspecific inhibitor of PDE), phentolamine (alpha receptor blocker) |
| intrapenile injections ADR | priapism (long lasting boner) |