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Renal II Drugs > Male Disorders > Flashcards

Male Disorders Flashcards

1
Q

Alpha1 adrenergic antagonists (days to resolve)

A
  1. Doxazosin
  2. Terazosin
  3. Alfuzosin
  4. Tamsulosin
  5. Silodosin
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2
Q

BPH alpha1 adrenergic antagonists (months to resolve)

A
  1. Alfuzosin
  2. Tamsulosin
  3. Silodosin
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3
Q

Steroid 5alpha-reductase inhibitors

A
  1. Finasteride

2. Dutasteride

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4
Q

PDE5 inhibitors

A
  1. Sildenafil
  2. Vardenafil
  3. Tadalafil
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5
Q

Erectile dysfunction

A
  1. PDE5 inhibitors

2. Prostaglandin E1

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6
Q

BPH

A
  1. Alpha1 adrenergic Rc antagonists
  2. Steroid 5alpha-reductase inhibitors
  3. PDE5 inhibitors
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7
Q

Alpha 1 adrenoRc

A

Prostate - alpha 1A (muscle contraction)
Detrusor - alpha 1D > alpha 1A (instability)
SC - alpha 1D (control of urinary function)
BV - alpha 1B > alpha 1A (vascular resistance)

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8
Q

Alpha 1 antagonists compete with what to reduce spasm, promoter muscle relaxation and improve urine flow?

A

NE

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9
Q

Terazosin

A
  • alpha 1 > alpha 2&raquo_space; beta
  • NON-SPECIFIC for alpha 1 subtypes
  • NO uroselectivity
  • AE - postural hypotension titrate 1st dose, fatigue
  • drug interaction with PDE-5 inhibitor
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10
Q

Doxazosin

A
  • alpha 1 > alpha 2&raquo_space; beta
  • NON-SPECIFIC for alpha 1 subtypes
  • NO uroselectivity
  • AE - postural hypotension titrate 1st dose, fatigue
  • drug interaction with PDE-5 inhibitor
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11
Q

Alfuzosin

A
  • alpha 1 > alpha 2&raquo_space; beta
  • NON-SPECIFIC for alpha 1 subtypes
  • YES Uroselective (functional) –> distributed into prostate > serum, avoid in HEPATIC impairment (take it after same meal everyday)
  • AE - QT prolongation
  • Drug interaction with Cyp450
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12
Q

Tamsulosin

A
  • Sub-type specific so used more
  • Alpha 1A ~ alpha 1D > alpha 1B
  • YES Uroselective
  • AE - reduced ejaculation, intraoperative floppy iris syndrome (IFIS)
  • Drug interaction with Cyp450
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13
Q

Silodosin

A
  • Sub-type specific so used more
  • Alpha 1A ~ alpha 1D > alpha 1B
  • YES Uroselective
  • AE - reduced ejaculation, intraoperative floppy iris syndrome (IFIS)
  • Drug interaction with Cyp450
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14
Q

Why does the prostate enlarge?

A
  1. Age

2. DHT

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15
Q

T —> DHT

A

SAR type 1 and II or Steroid 5alpha-reductase

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16
Q

Direct and indirect effects of SAR II inhibition

A
  1. Direct - T accumulation and DHT depletion

2. Indirect - less AR Rc occupied

17
Q

Finasteride

A

SpeciFic inhibitor (SAR II)

18
Q

Dutasteride

A

DUal inhibitor

SAR I and II

19
Q

Tadalafil

A
  • for BPH
  • Onset: 15 min (take 1h before)
  • Span of efficacy: 36h 1x weekend
  • Advice: none
  • t1/2 (h): 18h
  • clearance: hepatic CYP 3A4
  • alpha 1 blockers not recommended when this is used
  • Risk D: consider therapy modification
  • SE: headache, dyspepsia, nasal congestion, back pain, myalgia, limb pain (NSAIDs ok)
20
Q

What modulates smooth muscle tone of penis?

A
  1. Neuronal input (NANC)
  2. Endothelial lining
    NO –> GC –> cGMP –> PHE-5 –> GMP –> SM relaxation and erection
21
Q

Slidenafil (Viagra)

A
  • Onset: 15mins (take 1h before)
  • Span of efficacy: 3 to 4h
  • Advice: empty stomach
  • t1/2 (h): ~4h
  • clearance: hepatic CYP 3A4
  • SE: headache, dyspepsia, nasal congestion, blue vision (PDE-6)
  • give alpha 1 blockers at LOWEST recommended dose in patients receiving sildenafil
22
Q

Varfenafil

A
  • Onset: 15mins (take 1h before)
  • Span of efficacy: 4 to 5h
  • Advice: empty stomach
  • t1/2 (h): ~4h
  • clearance: hepatic CYP 3A4
  • SE: headache, dyspepsia, nasal congestion, blue vision (PDE-6)
  • Patients must be stable, intiate this at LOWEST recommended dose
23
Q

PDE inhibitor selectivity

A
  1. PDE5 -> corpus cavernosum
  2. PDE6 ~ 10 fold -> retina (sildenafil, Varfenafil) —> AE: BLUE VISION DISTURBANCE
  3. PDE1 ~ 80 fold -> vasculature, heart, brain —> little clinical sig
  4. PDE11 ~ 800 fold -> heart, pituitary, testes —> negligible
  5. PDE3 ~ 4000 fold -> heart —> negligible
24
Q

PDE-5 inhibitor plus what is contraindicated?

A

Organic nitrates (glyceryl trinitrate) –> extreme hypotension

25
Q

Prostaglandin E1 (PGE1)

A

INTRACAVERNOSAL INJECTION - GPCR via AC –> inc cAMP –> SM relaxation
Be able to tell difference btw this and the other mechanism for NO release and activation of cGMP!!!! BOARDS
Others: Papaverine, Phenotlamine

Renal II Drugs (2 decks)

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