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Renal II Cumulative Final > Male GU Pharmacology > Flashcards

Male GU Pharmacology Flashcards

1
Q

Drug classes used to tx BPH

A

Alpha-1 adrenergic receptor antagonists

Steroid 5alpha reductase inhibitors

PDE-5 inhibitor (tadalafil)

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2
Q

Classes of drugs used to tx erectile dysfunction

A

PDE-5 inhibitors

PGE1 agonist (alprostadil)

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3
Q

What drugs are included in the alpha-1 adrenergic receptor antagonist class used to tx BPH?

A 
Terazosin
Doxazosin
Tamsulosin
Silodosin
Alfuzosin
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4
Q

What drugs are included in the steroid 5alpha reductase inhibitors class used to tx BPH?

A

Finasteride

Dutasteride

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5
Q

What drugs are included in the PDE-5 inhibitors class used to tx ED?

A

Sildenafil
Vardenafil
Tadalafil
Avanafil

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6
Q

Describe MOA of alpha1 receptor antagonists in terms of mediating LUTS

A

Alpha-1A receptor + NE stimulation normally leads to muscle contraction and bladder out let obstruction

Alpha-1D receptors + NE normally lead to detrusor instability

MOA of alpha-1 antagonists is to compete with NE to reduce spasm, promote muscle relaxation and improve urine flow

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7
Q

Specificity, uroselectivity, and AEs associated with terazosin and doxazosin

A

Specificity: alpha-1&raquo_space;> alpha-2; take 1 hour prior!

NOT uroselective

AEs: postural hypotension, dizziness, fatigue

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8
Q

Drug interactions associated with the alpha-1 adrenergic receptor antagonists (terazosin, doxazosin, tamsulosin, silodosin, and alfudosin)

A

PDE-5 inhibitors (sildenafil, vardenafil)

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9
Q

What drug interaction is important to keep in mind with select alpha-1 adrenergic receptor antagonists (particularly tamsulosin, silodosin, and alfuzosin)?

A

increase the concentration of CYP3A4 substrates

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10
Q

Specificity, uroselectivity, and AEs associated with tamsulosin and silodosin

A

Specificity: alpha-1A = alpha-1D > alpha-1B

Uroselective for alpha-1A = alpha-1D

AEs: reduced ejaculation; intraoperative floppy iris syndrome (IFIS)

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11
Q

Specificity, uroselectivity, and AEs associated with alfuzosin

A

Non-specific

Alpha-1 selective

AE: QT prolongation

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12
Q

Which of the alpha-1adrenergic receptor antagonists has functional uroselectivity, meaning that it distributes into the prostate more than the serum, but must be avoided in hepatic impairment?

A

Alfuzosin

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13
Q

T/F: alpha-1 adrenergic receptor antagonists are the best monotherapy for prompt relief of BPH symptoms

A

True

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14
Q

MOA of steroid 5-alpha reductase inhibitors used for BPH

A

Shrink prostate and Prevent further enlargement

Prevents steroid 5alpha reductase (SAR) type 1 and type 2 from converting serum T to DHT

DHT starvation causes epithelial atrophy, shrinkage, and gradual relief of LUTS (effects take ~3-6months)

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15
Q

What is the difference between finasteride and dunasteride in terms of selectivity?

A

Finasteride is specific to SAR-2

Dunasteride is a DUal inhibitor — SAR-1 and SAR-2

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16
Q

Which is more effective at decreasing serum DHT — finasteride or dutasteride?

A

Dutasteride is 20% better than finasteride at decreasing serum DHT

17
Q

AEs of finasteride and dutasteride

A

Erectile dysfunction
Gynecomastia
Depressed libido
Ejaculation disturbances

18
Q

Why must finasteride and dutasteride be used with caution in pts with liver abnormalities?

A

Metabolized by hepatic CYP3A

19
Q

When would you use combination therapy for BPH, meaning an alpha-1 adrenergic antagonist + 5alpha-reductase inhibitor?

A

Severe symptoms of BPH

Known to have large prostate

No response from monotherapy

20
Q

What drug is now approved by the FDA for treating patients with BOTH BPH and ED?

A

PDE-5 inhibitor: tadalafil

21
Q

MOA of PDE-5 inhibitors like tadalafil

A

PDE-5 inhibitors are competitive inhibitors of the PDE-5 enzyme —> preventing the conversion of cGMP to 5’-GMP [increases availability of cGMP to propagate smooth muscle relaxation so that erection is maintained]

22
Q

Clearance of all PDE-5 inhibitors

A

Hepatic CYP 3A4

23
Q

Onset, duration of action, stomach contents, and half-life of PDE-5 inhibitor: sildenafil (viagra)

A

Onset: take 1 hour prior

Duration of action = 4 hours

Stomach contents: empty

Half life = 4 hrs

24
Q

Onset, duration of action, stomach contents, and half-life of PDE-5 inhibitor: vardenafil (levitra)

A

Onset: take 1 hour prior

Duration of action = 4-5 hrs

Stomach contents: empty

Half life = 4 hrs

25
Q

Onset, duration of action, stomach contents, and half-life of PDE-5 inhibitor: tadalafil (cialis)

A

Onset: take 1 hour prior

Duration of action = 36 hours (longest MOA!)

Stomach contents do not matter

Half life = 18 hrs

26
Q

Onset, duration of action, stomach contents, and half-life of PDE-5 inhibitor: avanafil (stendra)

A

Onset: take 15 minutes prior (high dose) or take 30 minutes prior (nml dose) — FASTEST!

Duration of action = 4 hrs

Stomach contents do not matter

Half life = 4 hrs

27
Q

Adverse effects of sildenafil, vardenafil, and avanafil

A

Blue vision or blurred vision due to additional inhibition of PDE-6 in the retina

28
Q

PDE-5 inhibitor related side effects

A

Headache
Dyspepsia
Nasal congestion

PDE-6 related (sildenafil, vardenafil and avanafil) — blue/blurred vision

Specific to tadalafil: back pain, myalgia, limb pain

29
Q

Contraindications to PDE-5 inhibitor use for ED

A

Organic nitrates!! — leads to extreme and dangerous hypotension

Specific to vardenafil: pt needs to be hemodynamically stable

Specific to tadalafil: when used for BPH, concurrent alpha-1 blockers not recommended

Specific to sildenafil: concurrent alpha-blockers initiated at lowest recommended dose

30
Q

Second line ED therapies include vacuum erection devices, or penile injections with ______

A

Alprostadil

31
Q

MOA of alprostadil for ED

A

prostaglandin E1 analog —Leads to increases in cAMP, decreases in iCa++, smooth muscle relaxation, and erection

32
Q

AEs with alprostadil

A

Prolonged erection (priapism) — medical emergency; need to evacuate clogged blood because it can result in permanent corporal fibrosis and ED (can also occur with PDE-5 inhibitors but less common); tx is sympathomimmetic (phenylephrine) + aspiration

Renal II Cumulative Final (20 decks)

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