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Bladder AntispasmodicAka: Bladder Relaxant, Flavoxate, Urispas, Hyoscyamine sulfate, Cystospaz, Tolterodine, Detrol, Vesicare, Solifenacin, Enablex, Darifenacin, Oxybutynin, Oxybutynin XR, Ditropan
- Indications
- Urge Incontinence
- Urinary Catheter leakage
- Mechanism
- Anticholinergic Medications
- Inhibit involuntary detrusor contractions
- Adverse Effects
- Anticholinergic side effects (e.g. Dry Mouth)
- Seen less with Tolterodine then with Oxybutynin
- Preparations: Non-selective Agents
- Long-acting Oral agents: (preferred)
- Detrol LA (Tolterodine LA) 2 to 4 mg daily
- Similar efficacy compared to Oxybutinin XR
- Tolterodine causes less Dry Mouth
- Diokno (2003) Mayo Clin Proc 78:687
- Ditropan XL or Oxytrol XR (Oxybutynin XR) 5 to 10 to 30 mg daily
- Reduces Urge Incontinence 28%
- Dry Mouth is more common
- Least likely to cause Constipation
- CNS effects such as Dizziness and Sedation are more common
- Sanctura XR (trospium XR)
- No drug interactions with CYP3A4 metabolized agents
- Less CNS effects (does not cross BBB)
- Dry Mouth is less common
- Transdermal agents
- Tolterodine transdermal patch
- Oxybutynin transdermal patch (Oxytrol) apply 2x/week
- As effective as oral agent
- Less anticholinergic side effects
- Frequently causes skin reaction
- Dmochowski (2003) Urology 62:237
- Short acting oral agents
- Tolterodine (Detrol) 1 to 2 mg PO bid
- Oxybutynin (Ditropan) 2.5 to 5 mg PO qid
- Preparations: M3 Selective Antimuscarinics
- Mechanism
- Selective for M3 muscarinic receptor blockade
- Less drowsiness and Dizziness than agents above
- Higher rate of Constipation, Dry Mouth, vision change
- Agents
- Solifenacin (Vesicare) 5 to 10 mg PO daily
- Darifenacin (Enablex) 7.5 to 15 mg PO daily
- Preparations: Older agents now replaced by those above
- Flavoxate (Urispas) 100 to 200 mg PO qid
- Hyoscyamine (Cystospaz) 0.125 to 0.5 mg PO qid
- Dicyclomine (Bentyl) 10 to 20 mg PO qid
- References
- Appell (2001) Mayo Clin Proc 76:358
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| 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. |
| 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. |
| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Flavoxate, FLAVOXATE PREPARATION |
| Spanish | flavoxato |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | 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, Urispas |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| 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 | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | oxybutynin, OXYBUTYNIN @ @ UNIDENTIFIED, OXYBUTYNIN PREPARATION, OXYBUTYNIN UNIDENTIFIED |
| Spanish | oxibutinina |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | tolterodine, TOLTERODINE PREPARATION |
| Spanish | tolterodina |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | darifenacin, darifenicin |
| Spanish | darifenacina |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Allphar brand of oxybutynin hydrochloride, Aventis brand of oxybutynin hydrochloride, Byk brand of oxybutynin hydrochloride, Cystrin, Ditropan, Dridase, Janssen brand of oxybutynin hydrochloride, Ortho brand of oxybutynin hydrochloride, Sanofi Synthelabo brand of oxybutynin hydrochloride |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Detrol, Detrusitol, Pharmacia brand of tolterodine tartrate, Pharmacia Spain brand of tolterodine tartrate, Unidet |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Solifenacin |
| Spanish | solifenacina |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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