Autonomic Pharmacology and Urogenital Tract

Question 1

What is the cholinergic receptor?

Answer 1

Muscarinic M3 receptor

Question 2

What does stimulation of cholinergic receptor do?

Answer 2

Contracts detrusor muscle of bladder

Relaxes trigone and sphincter

Question 3

What are the adrenergic receptors? (3)

Answer 3

1. Beta 2
2. Alpha 1
3. Beta 1

Question 4

What do each of the adrenergic receptors do when stimulated? (3)

Answer 4

1. Beta 2 –> relaxes bladder smooth muscle
2. Alpha 1 –> contracts sphincter
3. Beta 1 –> increases renin release

Question 5

What are the 2 cholinergic receptor activating agents?

Answer 5

1. Bethanechol

2. Neostigmine

Question 6

What do the cholinergic receptor activating agents generally do? (3)

Answer 6

1. Stimulate bladder emptying
2. Tx of urinary retention problems post surgery
3. Only used w/no obstructive problems

Question 7

Bethanechol - Class

Answer 7

Muscarinic cholinergic receptor agonist (nonselective, high resistance to hydrolysis)

Question 8

Bethanechol - MOA

Answer 8

Stimulates M3 receptors –> contracts detrusor, relaxes trigone and sphincter –> urination

Question 9

What does DUMBBELLSS mean?

Answer 9

Diarrhea, Urination, Miosis, Bradycardia, Bronchospasm, Emesis, Lacrimation, Lethargy and Salivation and Seizures

Question 10

Bethanechol - SE

Answer 10

DUMBBELLSS urination

Question 11

Bethanechol - Uses

Answer 11

Post-op urinary retention (w/ no obstruction)

Question 12

Neostigmine - Class (2)

Answer 12

AchE inhibitor; carbamate ester

Muscarinic cholinergic receptor agonist

Question 13

Neostigmine - MOA

Answer 13

Forms covalent bond w/ AchE that is resistant to hydrolysis
Hydrolysis can occur but at a slow rate (30min-6hr)
Does not enter CNS; poorly soluble

Question 14

Neostigmine - SE

Answer 14

Excess activation of muscarinic and nicotinic Ach receptors by excess Ach in synapse –> parasympathetic effects predominate=> DUMBELLSS

Question 15

Neostigmine - Uses

Answer 15

Post-op paralytic ileus and urinary retention

Short acting, requiring frequent dosing; oral or parenteral every 4 hours

Question 16

What are the 7 cholinergic receptor blocking agents (anti-cholinergics)?

Answer 16

Tolterodine, oxybutynin, darifenacin, solifenacin, trospium, fesoterodine, propiverine

Question 17

What do the cholinergic receptor blocking agents generally do? (3)

Answer 17

1. Relaxes bladder
2. Slows voiding of bladder
3. Tx of bladder spasms post surgery or due to inflammation

Question 18

Oxybutynin - Class

Answer 18

Anticholinergic; muscarinic receptor antagonist

Question 19

Oxybutynin - MOA

Answer 19

Muscarinic antagonist, somewhat M3 selective –> reduces detrusor muscle tone

Question 20

Oxybutynin - Uses

Answer 20

Relieve post surgical bladder spasms and reduce involuntary voiding in pts w/ neurologic disease –> improve bladder capacity and continence, reduce infection and renal damage
Oral, IV, intracatheter, transdermally

Question 21

Oxybutynin - SE (5)

Answer 21

Tachycardia, constipation, increased intraocular pressure, xerostomia, pruritus (w/ transdermal administration)

Question 22

Tolterodine - Class

Answer 22

Anticholinergic; muscarinic receptor antagonist

Question 23

Tolterodine - MOA

Answer 23

M3-selective muscarinic antagonist

Question 24

Tolterodine - Uses

Answer 24

Adults w/ urinary incontinence

Question 25

Propiverine - Class

Answer 25

Anticholinergic; muscarinic receptor antagonist

Question 26

Propiverine - Uses

Answer 26

Reduce incontinence in institutionalized elderly pts

Question 27

Darifenacin, Solifenacin, Trospium, Fesoterodine - Class

Answer 27

Anticholinergic; muscarinic receptor antagonist

Question 28

Darifenacin, Solifenacin, Trospium, Fesoterodine - Uses

Answer 28

Overactive bladder

Question 29

What are the 2 adrenergic receptor activating agents?

Answer 29

Ephedrine, pseudoephedrine

Question 30

Which receptors do ephedrine and pseudoephedrine stimulate?

Answer 30

Alpha-1 agonists

Question 31

What do adrenergic receptor activating agents (ephedrine and pseudoephedrine) treat?

Answer 31

Urinary incontinence (and decongestant)

Question 32

What are the 7 adrenergic receptor blocking agents?

Answer 32

Prazosin, terazosin, doxazosin, tamsulosin, propranolol, metoprolol, and atenolol

Question 33

What do adrenergic receptor blocking agents treat?

Answer 33

Sx of urinary obstruction (benign prostatic hyperplasia - BPH)

Question 34

Prazosin; Terazosin; Doxazosin, Tamsulosin - MOA

Answer 34

Reversible alpha-1 adrenergic receptor antagonist; allows NE to exert neg feedback on its own release (via a2)

Question 35

Prazosin; Terazosin; Doxazosin, Tamsulosin - Uses

Answer 35

Primarily used in men w/ HTN and benign prostatic hyperplasia (reduces bladder obstruction symptoms)

Question 36

Prazosin; Terazosin; Doxazosin, Tamsulosin - Half lives

Answer 36

Prazosin < terazosin < doxazosin

Question 37

Prazosin; Terazosin; Doxazosin, Tamsulosin - Toxicity (6)

Answer 37

Retention of salt and water; dizziness, palpitations, headache, lassitude, positive test for antinuclear factor (no rheumatic symptoms)

Question 38

Propranolol - Class and MOA (6)

Answer 38

1. Nonselective ß-adrenergic receptor antagonist 2. Local anesthetic action 3. Inhibits renin production (ß1) 4. Half-life 3-5hrs 5. Given orally (sustained release prep available) or parenterally 6. Highly lipid soluble

Question 39

Propranolol - Toxicity (6)

Answer 39

Bradycardia; asthma; fatigue; vivid dreams; cold hands; withdrawal from ß-receptor upregulation --> nervousness, tachycardia, angina, increase BP, MI

Question 40

Propranolol - C/I (5)

Answer 40

Bradycardia, cardiac conduction disease, asthma, peripheral vascular insufficiency, diabetes

Question 41

Metoprolol, Atenolol - Class and MOA

Answer 41

1. ß-adrenergic receptor antagonist (ß1>>>ß2) | 2. Reduce renin secretion

Question 42

Metoprolol, Atenolol - Toxicity (4)

Answer 42

Bradycardia, fatigue, vivid dreams, cold hands