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44 Cards in this Set
- Front
- Back
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What is the MOA of alfuzocin?
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Antagonist of alpha-1 adrenergic receptors
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What drug is subtype specific for alpha1D receptors?
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Tamsulosin.... flomax
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What two drugs are generally uroselective?
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Alfuzocin, tamsulosin
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What is a major AE of tamsulosin?
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reduced ejaculation
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What are the major AE's of terazocin & doxazocin?
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Postural hypotension (titrate 1st dose)
Fatigue |
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What is the dosage for drugs that tx BPH?
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All are 1x daily po
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What makes Alfuzosin functionally uroselective?
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distributes to prostate > serum
(take right after same meal every day) |
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Which 5ARI drug is specific for 5AR-2... Which is nonspecific?
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Specific: Finasteride
Non-S: Dutasteride (dual inhibitor) |
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What is the general course of treatment/results in using 5ARI's?
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Take ~ 3 months for measurable effect
Similar efficacy b/w drugs Similar AE's b/w drugs |
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What is a good "option" for androgen "starvation" in prostatic tumors?
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Inhibit AR receptor binding
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What are the dosages of anti-androgens?
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Flutamide (prototype): 3x/day
Bicalutamide: 1x/day (now favored) |
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What are NANC neurons?
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nonadrenergic, noncholinergic
release NO --> guanylate cyclase --> GTP to cGMP --> relaxation of sm & ERECTION |
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What is the MOA of Sildenafil?
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Inhibits PDE-5 --> inc cGMP --> maintain erection
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What PDE-5 inhibitor has the longest half-life?
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Tadalafil (cialis)
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What is the main AE of dildenafil and vardenafil?
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Blue vision disturbance --> via PDE6
(also vasculature, heart, brain, effects) |
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What are the main AE's of tadalafil?
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back pain, myalgia, limb pains
NOT blue vision |
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What drug combo is a major contraindication of PDE-5 inhibitors?
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use w/ organic nitrates
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What drug combo is contraindicated w/ vardenafil?
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all alpha-blockers
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What type of drugs are Finasteride and dutasteride and what is the MOA?
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Steroid 5-alpha reductase inhibitors (SARI, 5ARI)
MOA: prevent enlargement/shrinks prostate (symptom relief 3-6 mo) |
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What type of drugs are terazosin and Doxazosin (the -zosins)?
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Alpha1-adrenergic receptor antagonists
MOA: in prostate, blocks SM contraction (competitive w/ NE) |
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What drug class do you choose for rapid relief of LUTS?
Delayed? |
Rapid: alpha-1 ad blockers (relief in days)
Delayed: SARI's (months) |
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What are some locations of alpha1 receptors?
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prostate (SM), detrusor muscle, spinal cord (control urinary function)
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What subtype of alpha-adrenergic receptors are in the prostate?
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Alpha 1A
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What drugs are NOT specific for any subtypes of alpha-1 receptors?
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quinazolines (terazosin, doxazosin, alfuzocin)
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What is the dosage for alpha1-antagonists when treating BPH?
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1x daily dose po for BPH
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How is alfuzosin uroselective?
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It distributes more into the prostate than the serum
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A hyperplastic prostate has an excess of what enzyme?
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SAR-II
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What enzyme converts T to DHT?
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5-alpha reductase
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What tissue is targeted in BPH treatment w/ 5ARI?
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epithelium --> decrease epithelial volume
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What drug inhibits specifically SAR II?
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Finasteride
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What drug inhibits both SAR I & II (dual inhibition?
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Dutasteride
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What is the target of androgen starvation treatment for prostate cancer?
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intracellular androgen receptors
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What is the MOA of flutamide?
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binds to AR and prevents T/DHT binding, dimerization, AR transport, transcription
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Flutamide is usually used in combination with what?
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leuprolide --> a GNRF agonist that depletes the ability to make T from the adrenals
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What are the non-steroidal anti-androgens?
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flutamide, nilutamide, bicalutamide (now favored b/c give 1x per day)
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What is the MOA of sildenafil (vardenafil, tadalafil)?
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inhibits PDE-5 --> inc cGMP and maintain erection
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What ED drug is long acting?
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tadalafil (cialis) --> ~ 36 hrs
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what is onset and span of efficacy for sildenafil and vardenafil?
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onset in 15 min.... spand of 3-4 and 4-5 hrs respectively
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Where are the different subsets of PDE located?
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PDE-5 --> corpus cavernosum
6 --> retina (AE bluvision for sildenafil and vardenafil) 1 --> vasc, heart, brain |
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PDE-5 related side effects?
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HA, dyspepsia, nasal congestion
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What ED drugs could give the side effect of blue vision?
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sildenafil and vardenafil
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What ED drug could give the SE of back pain, myalgia, and limb pain?
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tadalafil
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What are the contraindications for PDE-5 inhibitors?
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use w/ organic nitrates (hypotension)
alpha blockers with vardenafil |
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What is the MOA of PGE1 in the intracavernosal injections?
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PGE1 --> ATP to cAMP --> smooth muscle relaxation
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