Bladder Antispasmodic

Aka: Bladder Antispasmodic, Urinary Tract Antispasmodic, Urinary Antispasmodic, Bladder Relaxant, Bladder Antimuscarinic, Muscarinic Antagonists for Urge Incontinence, Oxybutynin, Oxybutynin XR, Oxytrol for Women, Ditropan, Flavoxate, Urispas, Hyoscyamine sulfate, Cystospaz, Tolterodine, Detrol, Vesicare, Solifenacin, Enablex, Darifenacin, Beta-3 Adrenergic Agonist, Mirabegron, Myrbetriq, Vibegron, Gemtesa

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II. Indications

  1. Urge Incontinence
  2. Urinary Catheter leakage

III. Mechanism

  1. Anticholinergic Medications
  2. Inhibit involuntary detrusor contractions

IV. Efficacy

  1. First-line management for Urge Incontinence are non-pharmacologic measures
    1. Decrease Caffeine intake
    2. Schedule voiding times
    3. Bladder TrainingExercises
  2. All Bladder Relaxants are only modestly effective
    1. Reduce Urinary Frequency and Incontinence by approximately 1 episode daily
    2. Expect 1 in 7 patients to benefit
    3. Expect 1 in 5 patients to have significant side effects (typically Anticholinergic)
  3. References
    1. Shamliyan (2012) Ann Intern Med 156(12):861-74 [PubMed]

V. Adverse Effects

  1. Anticholinergic side effects (antimuscarinic agents, no beta-3 agonists)
    1. Anticholinergic symptom examples: Dry Mouth, confusion, Tachycardia, Blurred Vision
    2. See Medication Use in the Elderly (Beers List, STOPP)
    3. Seen less with Tolterodine then with Oxybutynin
    4. Seen less with long acting agents and transdermal agents

VI. Preparations: Non-selective Agents (M1/M2/M3 antimuscarinics)

  1. Long-acting Oral agents: (preferred of the non-selective agents)
    1. Detrol LA (Tolterodine LA) 2 to 4 mg daily
      1. Similar efficacy compared to Oxybutinin XR
      2. Tolterodine causes less Dry Mouth
      3. Diokno (2003) Mayo Clin Proc 78:687-95 [PubMed]
    2. Ditropan XL or Oxytrol XR (Oxybutynin XR) 5 to 10 to 30 mg daily
      1. Ditropan XL is now generic
      2. Reduces Urge Incontinence 28%
      3. Dry Mouth is more common
      4. Least likely to cause Constipation
      5. CNS effects such as Dizziness and sedation are more common
    3. Sanctura XR (trospium XR)
      1. No Drug Interactions with CYP3A4 metabolized agents
      2. Renal clearance
      3. Less CNS effects (does not cross BBB)
      4. Dry Mouth is less common
    4. Toviaz XR (Fesoterodine XR)
      1. Risk of high drug levels in decreased metabolism of Cytochrome P450 2D6
  2. Transdermal agents
    1. Tolterodine transdermal patch
    2. Oxybutynin transdermal patch (Oxytrol) apply 2x/week
      1. As effective as oral agent
      2. Less Anticholinergic side effects
      3. Frequently causes skin reaction
      4. Dmochowski (2003) Urology 62:237-42 [PubMed]
    3. Oxytrol for Women (OTC, Oxybutynin patch)
      1. Indicated for women over age 18 years with at least 3 months of urinary urgency with frequency or Urinary Incontinence
      2. Cost is $30 per month (OTC out-of-pocket cost) versus $270 for prescription
      3. Contraindicated in men (due to Overflow Incontinence risk due to BPH related urinary obstruction)
      4. (2013) Presc Lett 20(9):51
  3. Short acting oral agents (avoid now that Ditropan XL is now generic)
    1. Increased Anticholinergic side effects (Dry Mouth, Constipation)
    2. Tolterodine (Detrol) 1 to 2 mg PO bid
    3. Oxybutynin (Ditropan) 2.5 to 5 mg PO qid

VII. Preparations: M3 Selective Antimuscarinics

  1. Indications
    1. Urge Incontinence (preferred agents due to less cognitive effects)
  2. Mechanism
    1. Selective for M3 muscarinic receptor blockade
    2. Less drowsiness and Dizziness than agents above
    3. Higher rate of Constipation, Dry Mouth, vision change
  3. Agents
    1. Solifenacin (Vesicare) 5 to 10 mg PO daily
    2. Darifenacin (Enablex) 7.5 to 15 mg PO daily

VIII. Preparations: Beta-3 Adrenergic Agonist

  1. Agents
    1. Mirabegron (Myrbetriq)
    2. Vibegron (Gemtessa)
      1. Does not appear to have Blood Pressure, Heart Rate effects or CYP450 2D6 interactions
        1. Contrast with Mirabegron
  2. Indications
    1. Consider in patients intolerant to the Anticholinergic effects of the anti-muscarinic agents
    2. Examples: Cognitive Impairment, Glaucoma
  3. Mechanism: Beta-3 Agonist
    1. Relaxes Smooth Muscle including the Bladder
    2. Secondary increase in Bladder storage capacity
  4. Efficacy
    1. Similar to effectiveness to antimuscarinics (e.g. Oxybutynin)
    2. However, substantially more expensive than antimuscarinics (>$400 per month)
  5. Adverse effects (Mirabegron)
    1. No Anticholinergic side effects
    2. Hypertension
    3. Tachycardia
    4. Headache
    5. Dizziness
    6. Gastrointestinal Upset
  6. Drug Interactions (Mirabegron)
    1. Inhibits CYP450 2D6
    2. Raises levels of Metoprolol, Desipramine, Digoxin

IX. Preparations: Older agents now replaced by those above

  1. Flavoxate (Urispas) 100 to 200 mg PO qid
  2. Hyoscyamine (Cystospaz) 0.125 to 0.5 mg PO qid
  3. Dicyclomine (Bentyl) 10 to 20 mg PO qid

X. References

  1. (2021) Presc Lett 28(3): 17
  2. (2012) Presc Lett 19(10): 57-8
  3. Appell (2001) Mayo Clin Proc 76:358-63 [PubMed]

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Related Studies

Cost: Medications

oxybutynin (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
OXYBUTYNIN 5 MG TABLET Generic $0.31 each
OXYBUTYNIN 5 MG/5 ML SYRUP Generic $0.02 per ml
OXYBUTYNIN CL ER 10 MG TABLET Generic $0.58 each
OXYBUTYNIN CL ER 15 MG TABLET Generic $0.76 each
OXYBUTYNIN CL ER 5 MG TABLET Generic $0.63 each
flavoxate (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
FLAVOXATE HCL 100 MG TABLET Generic $0.67 each
tolterodine (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
TOLTERODINE TART ER 2 MG CAP Generic $3.50 each
TOLTERODINE TART ER 4 MG CAP Generic $3.06 each
TOLTERODINE TARTRATE 1 MG TAB Generic $1.28 each
TOLTERODINE TARTRATE 2 MG TAB Generic $1.08 each
detrol (on 6/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
DETROL 1 MG TABLET Generic $1.28 each
DETROL 2 MG TABLET Generic $1.08 each
DETROL LA 2 MG CAPSULE Generic $3.50 each
DETROL LA 4 MG CAPSULE Generic $3.06 each
vesicare (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
VESICARE 10 MG TABLET $10.07 each
VESICARE 5 MG TABLET $10.10 each
enablex (on 4/19/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ENABLEX 15 MG TABLET Generic $7.50 each
ENABLEX 7.5 MG TABLET Generic $7.31 each
darifenacin (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
DARIFENACIN ER 15 MG TABLET Generic $7.50 each
DARIFENACIN ER 7.5 MG TABLET Generic $7.31 each
myrbetriq (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
MYRBETRIQ ER 25 MG TABLET $10.37 each
MYRBETRIQ ER 50 MG TABLET $10.35 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Ontology: Flavoxate (C0016225)

Definition (NCI) A synthetic parasympatholytic with antimuscarinic, muscle relaxant and urinary antispasmodic properties. Flavoxate binds and inhibits muscarinic receptors, thereby suppressing the micturition reflex and increases urinary bladder capacity by modifying the micturition center in the brain stem. In addition, this agent has been found to inhibit cyclic AMP formation in striatal membranes of the brain through stimulation of pertussis toxin-sensitive G protein-coupled receptors which in turn suppress isovolumetric urinary bladder contraction.
Definition (MSH) A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D005422
SnomedCT 372768002, 53641000
English Flavoxate, 4H-1-Benzopyran-8-carboxylic acid, 3-methyl-4-oxo-2-phenyl-, 2-(1-piperidinyl)ethyl ester, Flavoxate [Chemical/Ingredient], flavoxATE, flavoxate, FLAVOXATE, Flavoxate (product), Flavoxate (substance)
Swedish Flavoxat
Czech flavoxát
Finnish Flavoksaatti
Russian FLAVOKSAT, ФЛАВОКСАТ
Polish Flawoksat
Japanese 塩酸フラボキサート, フラボキサート
Spanish flavoxato (producto), flavoxato (sustancia), flavoxato, Flavoxato
French Flavoxate
German Flavoxat
Italian Flavossato
Portuguese Flavoxato
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Urispas (C0042049)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D005422
English urispas, Urispas, Byk Brand of Flavoxate Hydrochloride, Cahill May Roberts Brand of Flavoxate Hydrochloride, Negma Brand of Flavoxate Hydrochloride, Ortho Brand of Flavoxate Hydrochloride, Shire Brand of Flavoxate Hydrochloride
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: oxybutynin (C0069805)

Definition (NCI) A tertiary amine possessing antimuscarinic and antispasmodic properties. Oxybutynin blocks muscarinic receptors in smooth muscle, hence inhibiting acetylcholine binding and subsequent reduction of involuntary muscle contractions. Oxybutynin is used to reduce bladder contractions by relaxing bladder smooth muscle.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C005419
SnomedCT 35768004, 372717000
LNC LP18095-7, MTHU003379
English 4-(diethylamino)-2-butynyl-alpha-cyclohexyl-alpha-hydroxybenzeneacetate, 4-(diethylamino)-2-butynyl-alpha-phenylcyclohexaneglycolate, oxybutynin, OXYBUTYNIN @ @ UNIDENTIFIED, OXYBUTYNIN UNIDENTIFIED, Benzeneacetic Acid, alpha-cyclohexyl-alpha-hydroxy-, 4-(diethylamino)-2-butynyl Ester, 4-Diethylamino-2-butynyl alpha-phenylcyclohexaneglycolate, oxybutynin (medication), urological antispasmodics oxybutynin, OXYBUTYNIN, oxybutynin [Chemical/Ingredient], Oxybutynin, Oxybutynin (product), Oxybutynin (substance)
Spanish oxibutinina (producto), oxibutinina (sustancia), oxibutinina
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Cystospaz (C0305774)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
English Cystospaz, cystospaz
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: tolterodine (C0388753)

Definition (NCI) A benzhydryl compound and a muscarinic receptor antagonist possessing both antimuscarinic and antispasmodic properties. Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, competitively blocks muscarinic receptors, thereby inhibiting acetylcholine binding. This antagonistic action results in an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, indicating an antimuscarinic action on the lower urinary tract. The 5-hydroxymethyl metabolite appears to contribute significantly to the therapeutic effects.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C099041
SnomedCT 109113000, 372570008
LNC LP171645-7
English tolterodine, tolterodine [Chemical/Ingredient], TOLTERODINE, Tolterodine (product), Tolterodine (substance), Tolterodine
Spanish tolterodina (producto), tolterodina (sustancia), tolterodina
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: darifenacin (C0529351)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C101207
SnomedCT 416385001, 416140008
English (S)-1-(2-(2,3-dihydro-5-benzofuranyl)ethyl)-alpha,alpha-diphenyl-3-pyrrolidineacetamide, darifenacin, darifenacine, darifenacin (medication), DARIFENACIN, darifenacin [Chemical/Ingredient], darifenicin, Darifenacin (product), Darifenacin (substance), Darifenacin
Spanish darifenacina (producto), darifenacina (sustancia), darifenacina
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Ditropan (C0591395)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C005419
English Cystrin, ditropan, Aventis brand of oxybutynin hydrochloride, Byk brand of oxybutynin hydrochloride, Dridase, Janssen brand of oxybutynin hydrochloride, Ortho brand of oxybutynin hydrochloride, Sanofi Synthelabo brand of oxybutynin hydrochloride, Allphar brand of oxybutynin hydrochloride, Ditropan
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Detrol (C0719805)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C099041
English Detrol, Pfizer brand of tolterodine tartrate, detrusitol, detrol, Detrusitol, Unidet
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: ANTISPASMODICS,URINARY (C0876271)

Concepts Pharmacologic Substance (T121)
English ANTISPASMODICS,URINARY, [GU201] ANTISPASMODICS,URINARY, [GU200] ANTISPASMODICS,URINARY, antispasmodic urinary, urinary antispasmodics, Antispasmodics, Urinary
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Solifenacin (C1099677)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C441209
SnomedCT 407031006, 407030007
English solifenacin, 2(1H)-Isoquinolinecarboxylic acid, 3,4-dihydro-1-phenyl-,1- azabicyclo(2.2.2)oct-3-yl ester, (R-(R*,S*))-, SOLIFENACIN, Solifenacin (product), Solifenacin (substance), Solifenacin
Spanish solifenacina (producto), solifenacina (sustancia), solifenacina
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Enablex (C1310721)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C101207
English Enablex
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: VESICARE (C1601338)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C441209
English VESICARE, Vesicare, vesicare, Astellas Pharma US and GlaxoSmithKline brand of solifenacin succinate., VESIcare
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: urinary tract antispasmodics (C2064921)

Concepts Pharmacologic Substance (T121)
English urological agents antispasmodics, urinary tract antispasmodics (medication), urinary tract antispasmodics
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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