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Reproduction Pharmacology > Drugs for Urinary Incontinence or Retention > Flashcards

Drugs for Urinary Incontinence or Retention Flashcards

1
Q

Anticholinergics

A 
Darifenacin 
Fesoterodine 
Oxybutynin 
Solifenacin
Tolterodine 
Trospium  
Botulinum Toxin
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2
Q

Sympathomimetics

A

Mirabegron
Pseudoephedrine †
Ephedra †

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3
Q

Ancillary Drugs

A

Methionine

Bovine Collagen Implant

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4
Q

Overactive Bladder (OAB)

A

Substantial medical and QOL sequelae of OAB

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5
Q

Treatment of Urinary Incontinence typically begins with?

A

Noninvasive approaches such as behavioral therapy, including patient education, fluid management, bladder retraining, pelvic floor exercises, biofeedback, and timed bladder emptying.

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6
Q

If noninvasive does not work?

A

Surgical procedures and catheterization are appropriate for some patients or add pharmacotherapy when behavioral modification fails.

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7
Q

Most commonly prescribed drugs?

A

Antimuscarinic medications: tolterodine & oxybutynin.

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8
Q

Reluctance in nursing home use due to?

A

Lack of efficacy data in these populations, often severe cognitive impairment, and risk of drug-drug interactions.

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9
Q

Incontinence [Urge (detrusor overactivity)]
Common Causes
Usual Symptoms
Drug Treatments

A

Strokes, Alzheimer Parkinson disease BPH with overflow

Urgency & frequency, day or night (nocturia)

Anticholinergics: Oxybutynin & Tolterodine

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10
Q

Incontinence [Stress (outlet incompetence)]
Common Causes
Usual Symptoms
Drug Treatments

A

Urological procedures, multigravida, Estrogen deficiency

Minimal urine loss with coughing, sneezing, running, or laughing

Topical estrogen, Alpha-agonists Non-drug method

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11
Q

Incontinence [Mixed]
Common Causes
Usual Symptoms
Drug Treatments

A

Multiple etiologic factors

Symptoms of urge and/or stress and/or overflow

Focus treatment on predominant symptoms

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12
Q

Incontinence [Atonic bladder]
Common Causes
Usual Symptoms
Drug Treatments

A

Severe diabetic neuropathy, Stroke

Complete loss of bladder control

Catheterization

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13
Q

Incontinence [Functional]
Common Causes
Usual Symptoms
Drug Treatments

A

Inability to reach bathroom, changes in mental
status, UTIs, medications

Symptoms of incontinence vary according to type
of external cause

Therapy choice to eliminate cause

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14
Q

Salivary glands:
Receptors
Effects of Blockage

A

M1, M3, M4

Dry mouth

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15
Q

Cardiac tissue:
Receptors
Effects of Blockage

A

M2

Tachycardia, palpitations

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16
Q

Eye (ciliary muscle, iris)
Receptors
Effects of Blockage

A

M3, M5

Dry eyes, blurred vision

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17
Q

GI tract:
Receptors
Effects of Blockage

A

M1, M2, M3

Slowing of transit time (constipation), effects on sphincter tone and gastric acid secretion

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18
Q

CNS, brain (cortex and hippo-campus):
Receptors
Effects of Blockage

A

M1, M2, M3, M4, M5

Effects on memory, cognition and psychomotor speed, confusion, delirium, hallucinations, sleep disruption

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19
Q

Bladder (detrusor muscle):
Receptors
Effects of Blockage

A

M2 (opposes β- receptor), M3 (direct effect)

Decreased contraction, urinary retention

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20
Q

Adverse Effects of Anticholinergic Drugs

Peripheral Effects

A 
Dry mouth 
Mydriasis 
Constipation
Urinary retention
Tachycardia
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21
Q

Adverse Effects of Anticholinergic Drugs

Central Effects

A 
Sedation
Confusion/delirium
Hallucinations
Slowed cognitive function
Sleep disruption
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22
Q

Tertiary Amines are?

A 
Oxybutynin
Tolterodine
Fesoterodine
Solifenacin
Darifenacin
23
Q

Quaternary Amine is?

A

Trospium means want effect CNS.

24
Q

Which has > M3- selectivity?

A

Darifenacin

25
Q

Oral bioavailability Poor:

A

Darifenacin
Oxybutynin
Trospium

26
Q

CYP Metabolism only one with almost no CYP activity?

A

Trospium

27
Q

Trospium & Fesoterodine have rapid

A

Urinary Excretion

28
Q

Solifenacin half life:

A

45–68 hrs

29
Q

Oxybutynin & Tolterodine both have?

A

Short half lives (2hrs), but have extended release formulations.

30
Q

Fesoterodine is rapidly hydrolyzed to?

A

5-hydroxymetghyl-tolterodine; parental drug is not detectable in systemic circulation.

31
Q

Elderly patients may be taking multiple anticholinergics, so monitor for adverse effects:

A

– Urinary retention, especially in BPH
– CV effects may include palpitations, tachycardia, & a prolonged QTc interval
– GI effects: mild constipation to severe obstructions

32
Q

Elderly patients may be taking multiple anticholinergics Contraindications:

A

– Angle closure or narrow-angle glaucoma
– Urinary and gastric obstruction
– Need for mental alertness
– Alzheimer’s type dementia

33
Q

Risk of withdrawal & dry mouth

A

Dry Mouth: Oxybutynin = Tolterodine > Solifenacin & Fesoterodine

34
Q

Botox injections are more successful in patients with?

A

Anticholinergic intolerability as compared to patients with poor medication efficacy.

35
Q

Botox Mechanism:

A

Inhibits vesicular release of excitatory neurotransmitters and axonal expression of other SNARE-complex dependent proteins in the urothelium/suburothelium mediating intrinsic or spinal reflexes thought to cause detrussor overactivity.

36
Q

Sympathetic postganglionic neurons release?

A

Norepinephrine, which activates β3 adrenergic receptors to relax bladder smooth muscle & activates α1 adrenergic receptors to contract urethral smooth muscle.

37
Q 
Mirabegron
Receptor binding:
Oral bioavailability:
CYP Metabolism:
Urinary Excretion:
Half-life:
A

β-3 agonist; increases bladder capacity by relaxing detrusor s.m.
≤ 35%; decreased by food
3A4&raquo_space; 2D6; also butylcholinesterase, UGT, & alcohol dehydrogenase
~10% as parental drug
~50 hrs

38
Q 
Pseudoephedrine
Receptor binding:
Oral bioavailability:
CYP Metabolism:
Urinary Excretion:
Half-life:
A 
Direct & indirect α & β agonist; α>β effects
Almost complete
Minimal
≤ 75%; increase with acidic urine
9-16 hrs, depending on urinary pH
39
Q 
Ephedra
Receptor binding:
Oral bioavailability:
CYP Metabolism:
Urinary Excretion:
Half-life:
A 
Indirect nonselective α & β agonist
~85%
Minimial
Up to 99%; increase with acidic urine
~5 hrs
40
Q

Mirabegron side effects?

A

– Increase BP; monitoring recommended, especially in hypertensives.
– Tachycardia

41
Q

Pseudoephedrine side effects?

A

– Hypertension, tachyarrhythmia, A-fib
– Insomnia
– Anxiety, feeling nervous, restlessness

42
Q

Ephedra side effects?

A

– Hypertension, tachyarrhythmia, CHF, MI
– Insomnia
– Symptoms of CNS stimulation

43
Q

Have MAOI interaction?

A

Mirabegron
Pseudoephedrine
Ephedra
Check patient drug history

44
Q

Methionine Mechanism & use?

A

• Creates ammonia-free urine by acidifying urine pH
• Used to control odor, dermatitis, and ulceration in
incontinent adults

45
Q

Methionine adverse effects?

A

Most common adverse effects: Drowsiness; nausea and vomiting.

46
Q

Bovine Collagen mechanism & use?

A

For incontinence due to intrinsic sphincter deficiency.
Injected into submucosal tissue of urethra and/or bladder neck & forms a soft cohesive network of fibers increasing tissue bulk around the urethral lumen.

47
Q

Bovine Collagen Adverse Reactions:

A

Urinary retention, hematuria, injection site reaction, worsening incontinence, erythema, urticaria, abscess formation.

48
Q

Management Of Urinary Retention Includes?

A

Assessment of post-void residual urine volume Strengthening of cholinergic-mediated detrussor
muscle contraction

49
Q 
Bethanechol 
Receptor binding:
Oral bio-availability:
Metabolism:
Urinary Excretion:
Half-life:
A 
Muscarinic agonist in urinary bladder and GI tract
Ionized; doesn’t cross BBB
Poor; % undetermined
Not inactivated by cholinesterases
Undetermined
Short duration: 1 hr orally, 2 hrs s.c.
50
Q 
Neostigmine
Receptor binding:
Oral bio-availability:
Metabolism:
Urinary Excretion:
Half-life:
A

Inhibits acetylcholinesterase, augments action of Ach at both muscarinic and nicotinic receptors
Poor, ~2%
Inactivated by cholinesterases & hepatic microsomal enzymes
≤ 70% as parental drug
< 1 hr

51
Q

Bethanechol side effects:

A 
– CV: Lightheadedness, Syncope
– GI: Diarrhea, Stomach cramps
– Neurologic: Dizziness
– Ophthalmic: Excessive tear production, miosis
– Renal: Urgent desire to urinate
52
Q

Neostigmine side effects:

A 
– AV block
– Bradyarrhythmia
– Cardiac arrest
– Cardiac dysrhythmia
– Hypotension
– Syncope
– Tachycardia
53
Q

Opiate Adverse Effects

A
  • Urinary retention (oral, < 5% ; epidural/intrathecal, ≤ 70%)
  • Cholinomimetic agents such as bethanechol may be helpful to treat urinary retention induced by opioids

Reproduction Pharmacology (9 decks)

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