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Advanced Pharmacology > Urology Medications > Flashcards

Urology Medications Flashcards

1
Q

Name 4 PDE-5 inihibitors

A

Sildenafil–Viagra
Tadalafil–Cialis
Vardenafil–Levitra and Staxyn
Avanafil–Stendra

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2
Q

How do PDE-5 inhibitors help with ED (this is their MOA)

A

They breakdown the isoenzyme that breaks down cGMP. cGMP is responsible for relaxing smooth muscle in the corpus cavernosum so that there is more blood flow

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3
Q

Sildenafil is known as

A

viagra

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4
Q

Sildenafil (Viagra)

A

PDE-5 Inhibitor
-PO
-onset 60 minutes
-1/2 life 3-4 hrs
-take with food
-take on empty stomach
-metabolized by CYP3A4
-do not take with NITRATES, VASODILATORS, OR ALPLHA BLOCKERS b/c can cause hypotension
-taken on empty stomach 1 hour before sex
ADE: disturbances in perception of blue and greens, sudden transient hearing loss d/t vasodilation, priapism

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5
Q

Tadalafil is known as

A

cialis

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6
Q

Tadalafil (Cialis)

A

PDE-5 Inhibitor

  • PO
  • onset 120 minutes
  • 1/2 life 18 hours
  • *also approved for BPH
  • metabolized by CYP3A4
  • take with or without food
  • ***caution with alpha blockers
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7
Q

Vardenafil is known as

A

Levitra; Staxyn

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8
Q

Vardenafil (Levitra; Staxyn)

A

PDE-5 Inhibitor

  • PO
  • onset 60 min
  • 1/2 life 4-5 hrs
  • food doesn’t matter but CAN’T TAKE WITH WATER
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9
Q

Avanafil is known as

A

Stendra

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10
Q

Avanafil (Stendra)

A

PDE-5 Inhibitor

  • PO
  • onset 30-45 minutes
  • 1/2 life 5 hr
  • food doesn’t matter
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11
Q

What is a synthetic prostoglandin E1 use for ED?

A

Alprostadil

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12
Q

Alprostadil

A

 Synthetic prostaglandin E1
 In the penile tissues, PGE1 allows relaxation of the smooth muscle of corpus cavernosum
 Given intraurethral [supp] or intrapenile [injection]
 Can be used 1st line—but most often used in those who are not candidates for oral agents
 Acts locally, which decreases chance of ADEs
 MOA—smooth muscle relaxants, exact physiological mechanism is unknown
 Systemic absorption is minimal
 Onset 5-10” [supp] or 2-25” [injection]—effects last 30-60”
ADEs—rare; hypotension, headache have been reported; local effects—penile pain, urethral
pain, testicular pain
Priapism may occur

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13
Q

What 3 types of drugs can be used for BPH

A
  1. alpha blockers
  2. 5 alpha reductase inhibitors
  3. PDE 5 inhibitor
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14
Q

MOA of alpha blockers in BPH

A 
 Blocking Alpha1A & Alpha1B receptors in the prostate cause the smooth muscles in the gland to relax, which leads to improved urine outflow 
 Selective agents only block Alpha1B—have no BP effects— nonselective ones decrease peripheral vascular resistance and lower BP
 Five agents in this class approved for BPH, a sixth one may be used but not FDA approved 
 4 nonselective and 2 selective alpha blockers—real prototype drug hard to identify
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15
Q

MOA of 5 alpha reductase inhibitors o BPH

A

inhibit 5 alpha reductase—which converts
testosterone to dihydrotestosterone[DHT], the more
potent, active compound that stimulates the prostate
to grow. By decreasing DHT the gland shrinks and urine
outflow improves.

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16
Q

MOA of PDE-5 inhibitors on BPH

A

-inhibition of PDE 5 allow vasodilation and relaxation of smooth muscles of the prostate and bladder-which improves the symptoms of BPH

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17
Q

Name 4 nonselective alphablockers

A
  1. Terazosin- Hytrin
  2. Alfuzosin- Uroxatral
  3. Prazosin- Minipress
  4. Doxazosin-Cardura
18
Q

Terazosin-Hytrin

Alpha blocker

A 
Trade name: Hytrin
FDA approved for BPH: yes
NONSELECTIVE alpha blocker
NO food effect
Metabolized in liver but not CYP450
19
Q

Alfuzosin-Uroxtral

Alpha blocker

A 
Trade name: Uroxatral
FDA approved for BPH: yes
NONSELECTIVE alpha blocker
Food HELPS with absorption
CYP450 substrate
**can prolong QT interval
20
Q

Prazosin- Minipress

Alpha blocker

A 
Trade name: minipress
FDA approved for BPH: NOOOO
NONSELECTIVE alpha blocker
No effect with food
CYP450: yes
21
Q

Doxazosin-Cardura

Alpha blocker

A 
Trade Name: cardura
FDA approved for BPH: yes
NONSELECTIVE alpha blocker
No food effecr
CYP450 metabolism? yes
22
Q

2 selective alpha blockers

A
  1. Tamulosin (Flomax)

2. Silodosin (Rapaflo)

23
Q

Tamulosin (Flomax)

Alpha blocker

A 
Trade name: Flomax
FDA approved for BPH: yes
SELECTIVE alpha blocker
Food helps with absorption
CYP450 metabolism: yes
24
Q

Silodosin (Rapaflo)

Alpha blocker

A 
Trade name: rapaflo
FDA approved for BPH: Yes
SELECTIVE alpha blockers
Food helps with absorption
CYP450: yes** (also substrate for P-glycoprotein)
25
Q

Name 2 - 5 alpha reductase inhibitors

A
  1. Finastride (Proscar)

2. Dutasteride (Avodart)

26
Q

FINASTERIDE (Proscar)

A

 Food does not affect absorption
 ½ life 6-12 hours [terminal ½ life of Avodart is 5 weeks, once the steady state is reached in 6 months]
 ADEs—decreased ejaculate, decreased libido, ED, gynecomastia, oligospermia
 All drugs in this category are teratogenic for women—those of child bearing age or those that are pregnant should not handle or ingest 5 alpha reductase inhibitors as they may lead to birth defects in the
genitalia of male fetus
 Rare drug interactions
 Finasteride is used [in small doses] for alopecia—
reduces DHT in scalp and serum which prevents hair
loss

27
Q

Dutasteride (Avodart)

A

-more potent than proscar and causes greater reduction in DHT

28
Q

What is finasteride use more for now days?

A

alopecia

29
Q

What PDE-5 inhibitor is also used for BPH

A

Tadalafil-Cialis

Inhibition of PDE-5 allow vasodilation and
relaxation of smooth muscles of the
prostate and bladder—which improves
the symptoms of BPH

30
Q

Anticholinergics are also called…

A

antimuscarinic

31
Q

Drug of choice for overactive bladder (incontinence/loss of bladder control)

A

Antimuscarinic meds

32
Q

How do antimuscarinic/anticholingerics work on bladder

A

Acetylcholine is the primary contractile neurotransmitter in the human detrusor, and antimuscarinics exert their effects on OAB/DO by inhibiting the binding of acetylcholine at muscarinic receptors M(2) and M(3) on detrusor smooth muscle cells and other structures within the bladder wall.

33
Q

Meds for detrusor over activity

A
  1. Propantheline (Pro-Banthine)
  2. Dicyclomine (Bentyl)
  3. Tricyclic antidepressants (TCAs)
34
Q

Antimuscarinic Medications—

Prototype—Oxybutynin (ditropan)

A

4 formulations:

  • Immediate release: 2.5–5 mg BID–QID, up to 20 mg/day
  • Extended release (ER) (Ditropan XL): 5–20 mg/day
  • Topical patch (Oxytrol): 3.9 mg, applied 2x/week
  • Topical gel (Gel): 1 gram applied every 24 hours
• Side effects (less frequent with ER and topical): 
 Dry mouth 
 Blurry vision 
 Constipation 
 Possibly cognitive

Interactions with CYP34A and 2D6
• Monitor PVR if UI worsens

35
Q

Antimuscarinic Medications—

Tolterodine [Detrol]

A

Initial dose: 1–2 mg BID immediate release, 2–4 mg
QD for ER (Detrol LA)

Side effects similar to those of oxybutynin-ER; possible decreased xerostomia (dry mouth)

Interactions with CYP34A and 2D6

36
Q

Antimuscarinic Medications—

Trospium [Sanctura]

A

 Dose is 20 mg twice daily; can dose once daily in elderly because of renal clearance
 Does come in an extended release form—Santura XR 60 mg daily
 Must be taken on an empty stomach
 Associated with 56%–60% reduction in weekly urge incontinence episodes
 No data in long-term-care populations
 Adverse events: dry mouth, constipation, headache, abdominal pain

37
Q

Antimuscarinic Medications—

Darifenacin [Enablex]

A

Dose is 7.5 or 15 mg/day
Median reduction in weekly UI episodes 55%–58% in patients on 7.5 mg and 60%–70% in patients on 15 mg
No data in long-term-care populations
Adverse events: dry mouth, constipation; may have limited cognitive effects
Interactions with CYP34A and 2D6

38
Q

Antimuscarinic - Fesoterodine [Toviaz]

A

Atropine like agent that is used to treat OAB—this quaternary amine has the fewest cholinergic effects—working mostly on muscarinic and nicotonic receptors in the detrusor
Increases bladder capacity
For those on drugs that may increase
cholinergic neurotransmitters [agents
for dementia]—this is one of the DOC (drug of choice)
for OAB in those individuals

**first line for person with cognitive deficits

39
Q

β 3 Agonist (NOT an antimuscarini)—Mirabergron [Myrbetriq]

A

 This agent relaxes the detrusor smooth muscle and increases bladder capacity

 Used for OAB [in patients that have failed other agents or have a contraindication to the use of the anticholingergics

 Myrbetriq 25-50 mg daily

  • Can increase BP [this effect is more marked at lower doses]
  • It increases digoxin levels; can decrease Metoprolol levels; can inhibit CYP2D6
  • If GFR is <30 cc/min—use the 25 mg dose
40
Q

What can be used for stress incontinence?

A
  1. estrogens-has a enhancing effect on the vaginal and urethral mucosa, and the pelvic floor muscles, rejuvenating the tissues and making them more elastic.
  2. alpha agonist-results in contraction of the internal urethral sphincter and increases the urethral resistance to urinary flow.
  3. ⍺ adrenergic agonist-stimulate urethral smooth muscle contraction

Advanced Pharmacology (18 decks)

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