Bladder Function and Pharmacology Flashcards
What anticholinergics are commonly used in in diseases of bladder function?
- Darifenacin
- Fesoterodine
- Oxybutynin
- Solifenacin
- Tolterodine
- Trospium
- Botulinum Toxin
What Sympathomimetics are commonly used in diseases of Bladder function?
- Mirabegron
- Pseudoephedrine
- Ephedra, Ma Huang
What Ancillary drugs are commonly used in disease of Bladder function?
- Methionine
* Bovine Collagen Implant
What drugs are used in the Management of Urinary Retention?
- Bethanechol
- Neostigmine
- Methylnaltrexone
- Naloxone
In what type of incontinence would you use antimuscarinic drugs?
• how do they work?
• Name them.
Use for:
• URGE incontinence
*these work by BLOCKING the M3 receptor that stimulates the bladder (detrussor) to contract
- Darifenacin
- Fesoterodine
- Oxybutynin
- Solifenacin
- Tolterodine
- Trospium
- Botulinum Toxin
In what type of incontinence would you use cholinomimetic drugs?
• how do they work?
• Name them.
Opiate Induced Urinary Retention is treated with Cholinoimetics
Bethanecol
In what type of incontinence would you used Alpha-agonist drugs?
• how do they work?
• Name them.
Use for:
• STRESS incontenence
*these work by AGONIZING ß3 causing relaxation of the detrussor and AGONIZING alpha-1 to stimulate internal urethral sphincter contraction
Drugs:
• Mirabegron
• Ephedra
• Pseudoephedra
Explain the mechanism of action of Botox.
Botox blocks SNAREs are prevents ACh release
Explain the mechanism of action of methionine.
Creates AMMONIA FREE urine by acidifying urine pH
Explain the mechanism of action of collagen.
Helps to support the external urethral sphincter
What is opiate-induced urinary retention and how is it treated clinically?
Opiate Induced Urinary Retention is treated with Cholinoimetics
Bethanecol
What is the action of the M3 receptor stimulation on the bladder?
• neurotransmitter used?
• Nerve that secretes it?
Pelvic n. uses Ach to stimulated M3 can cause BLADDER CONTRACTION
What is the action of ß3 receptor stimulation on the bladder?
• Neurotransmitter used?
• Nerve that secretes it?
Hypogastric n. releases NE to simulate SMOOTH MUSCLE RELAXATION
• Don’t want to have to pee while you’re trying to fight
What is the action of Alpha-1 receptors stimulation on the bladder?
• Neurotransmitter used?
• Nerve that secretes it?
Hyopgastric n. releases NE to simulate URETHRAL CONTRACTION
• again keeps you from peeing while fighting
What is the action of the nicotinic receptor stimulation on the urethra?
• Neurotransmitter used?
• Nerve that secretes it?
Pudendal n. acts at UG diaphragm to release Ach causing Contraction of the External Urethral Spincter
What are the most commonly prescribed drugs for urinary incontinence?
Antimuscarinic Drugs
• Tolterodine and Oxybutynin
What is the 1st line of care in people with urinary incontinence?
Behavioral Therapy, Pt. education, fluid management, bladder retraining, Pelvic floor exercises
Bottom line is there is a lot you want to do before starting someone on drugs because of side effects
Where do the following drugs act: • Darifenacin • Oxybutynin • Trospium • Tolterodine
- what receptor do they act on?
• Key feature of each?
Non-Selective Muscarinic Antagonists
Once daily Dosing:
• Darifenacin
• Oxybutyrin
Neglible CYP metabolism:
• Trospium
Extended release Availability:
• Tolterodine
• Oxybutyrin
What is the point of giving muscarinic drugs that are extendend release?
• which two have this availability?
Extended Release:
• Tolterodine
• Oxybutyrin
Reduces the MAJOR MUSCARINIC ANTAGONIST side effect of DRY MOUTH
What is the most common reason for people to stop using Muscarinic Receptor Therapy?
• Name the drugs used in this therapy?
DRY MOUTH
Drugs: • Darifenacin • Trospium • Oxybutynin • Tolterodine
What adverse effects should you monitor in someone taking muscarinic antagonists?
• Name Them.
- Urinary Retention
- CV effects - may include palpitations, tachycardia, prolonged QT interval
- GI effects - Mild constipation to severe obstruction
Drugs: • Darifenacin • Trospium • Oxybutynin • Tolterodine
In what patients should you Monitor Urinary Retention especially closely in?
• People with BPH
Drugs: • Darifenacin • Trospium • Oxybutynin • Tolterodine
What are the contraindications for Muscarinic Antagonist use?
- Angle Closure / Narrow Angle Glaucoma
- Urinary and Gastric Obstruction
- Need for mental alertness
- Alzheimer’s type Dementia
Why might someone want to use Botox to treat Urinary incontinence?
• who is it most effective in?
- Benefit is long lasting, lasts for several months
* Botox - most effective in patients who responded to anticholinergics but couldn’t tolerate the adverse effects
Botox
• MOA
- Inhibits Afferent Cholinergic Impulses by inhibiting SNARE-complex-dependent proteins
- Phenotypic change in SUBurothelial tissue to ablate the excitatory effect of local chemical mediators
Where do the following drugs act?
• Mirabegron
• Pseudoephedrine
• Ephedra, Ma Huang
*how does mirabegron differ from the others?
These drugs agonize ß3 and alpha 1 receptors to relax bladder and contract internal urethral sphincter respectively
How is Mirabegron different?
• long acting drug that undergoes extensive hepatic metabolism
• others are minimally broken down and are shorter acting
What is a common side effect to all of the sympathomimetic drugs used in urinary incontinence?
• name the drugs.
Drugs:
• Mirabegron
• Ephedra
• Pseudoephedra
Side Effect: SYMPATHETIC STIMULATION • HTN • Tachycardia-Tachyarrythmia • Anxiety - Restlessness - nervousness - insomnia
Methionine
• MOA
• Administration
• use in urinary incontence
Makes yo Piss Stank-less
• Controls odor, dermatitis, and ulceration
• Take with Food, Milk, or other liquid
MOA:
• Creates Ammonia-Free urine by acidifying urine pH
Bovine Collagen
• MOA
• Who is it used for?
• Interactions?
MOA:
• Injected into the submucosal tissue of urethra and/or bladder neck
• Forms a soft cohesive network of Fibers around Urethral Lumen
Interactions:
• Don’t give with IMMUNOSUPPRESIVE therapy or CORTICOSTEROIDS
Bovine Collagen
What are some adverse rxns?
- Urinary Retention
- Hematuria
- Injection Site Rxn
- Worsening Incontinence
- Erythema
- Urticaria
- Abscess formation
What drugs are used to MAKE YOU PEE MORE?
(in urinary retention)
• what do these drugs act on?
• Administration frequency?
Bethanechol - MUSCARNIC agonist
Neostigmine - Acetylcholinesterase inhibitor
**Both of these drugs must be administered several times per day
Bethanechol
• MOA
• Adverse Effects
MOA:
• CHOLINESTERASE-RESISTANT muscarinic agonist
ADVERSE EFFECTS: CV - lightheadedness, syncope GI - Diarrhea, stomach cramps Neurologic - dizziness Opthalmic - Excessive tear production, miosis
Neostigmine
• MOA
• Adverse Effects
MOA:
• Acetylcholinesterase Inhibitor
Adverse Effects: • AV block, Brady-arrhythmia • Cardiac Arrest, Cardiac Dysrythmia • HypOtension, Syncope • Tachycardia
Opiate Adverse Effects on Urination
• how do we manage these problems in people who need to take opiates chronically?
Opiate Effects:
• Mu (µ) and Delta (∆) receptors are acted on in sacral cord inhibiting parasympathetic OUTFLOW
• DETRUSSOR doesn’t get activated
Management:
• Opiate Antagonists
• Bethanechol
Which of the anticholenergic drugs are M3 specific?
• M3 specific = Darifenacin –> no obvious benefit to this specificity
