ED Drugs

Question 1

Alprostadil MOA

Answer 1

Synthetic PGE1; stimulates AC/cAMP/PKA pathway to decrease intracellular Ca2+ resulting in smooth muscle relaxation thus ERECTION

Question 2

Alprostadil Tox

Answer 2

Local action-avoids systemic effects; MC=penile, urethral, or testicular pain; rarely CV AE’s

Question 3

Alprostadil PK

Answer 3

Rapid onset (mins); Effects lasts up to several hours

Question 4

Alprostadil Admin

Answer 4

Administrations: Urethral Suppository vs. Intra-cavernosal Injection

Question 5

PDE-5 Inhibitors

Answer 5

Avanafil, Sildenafil Tadalafil, Vardenafil

Question 6

Avanafil Tox

Answer 6

h/a; NAION, sudden hearing loss, unstable angina

Question 7

Avanafil DME

Answer 7

3A4»2C; fecal/renal elim; .5-.75 hr onset, 5 hr half-life

Question 8

Sildenafil Tox

Answer 8

h/a, indigestion, visual disturbances, epistaxis; NAION, sudden hearing loss

Question 9

Sildenafil DME

Answer 9

3A4»2C; fecal/renal elim; >1 hr onset, 4 hr half-life

Question 10

Tadalafil Tox

Answer 10

h/a, indigestion, nausea, backache, myalgia, flushing, RTIs, nasopharyngitis; NAION, sudden hearing loss, angina, MI, tachycardia

Question 11

Tadalafil DME

Answer 11

3A4; fecal/renal elim; 2-4 hr onset, <35 hr half-life

Question 12

Vardenafil Tox

Answer 12

h/a, flushing, rhinitis; NAION, sudden hearing loss, angina, MI
UNIQUE = heart stuff

Question 13

Vardenafil DME

Answer 13

3A4 & 2C; fecal/renal elim; 1 hr onset & dec by high fat meal, 5 hr half-life

Question 14

Vardenafil DDI

Answer 14

NITRATES;

DDI’s with >70 drugs that inc risk of QT prolongation/arrhythmias

Question 15

Testosterone use in ED

Answer 15

May improve response of hypogonadal men to PDE-5 inhibitors

Question 16

Yohimbine MOA

Answer 16

Inc relaxation of penile smooth muscle in 2 ways; 1. alpha-2 receptor inhibitor
2. antagonizes presynaptic inhibition of NANC nerves to inc release of NO

Question 17

Yohimbine Tox

Answer 17

Crosses BBB easily: anxiety, antidiuresis, dizziness, flushing, h/a, HTN, inc motor activity, irritability, nervousness/restlessness, sinus tachycardia, tremor; Worsens renal fxn in failure/dysfxn=CI

Question 18

Yohimbine PK

Answer 18

Rapid (variable) absorption; complete rapid metabolism; 30 min half-life

Question 19

Yohimbine DDI

Answer 19

MAOI action at supra-clinical doses: tyramine & caffeine interactions possible

Question 20

PDE-5 inhibitor also used for BPH

Answer 20

Tadalafil (35 hour half life)

Question 21

Yohimbine CI

Answer 21

renal failure/dsyfxn