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Overactive Bladder Medication

  • Author: Pamela I Ellsworth, MD; Chief Editor: Edward David Kim, MD, FACS  more...
Updated: Oct 12, 2015

Medication Summary

The goals of pharmacotherapy are to improve OAB symptoms, reduce morbidity, and prevent complications. Anticholinergics are the first-line agents used to treat overactive bladder (OAB). Individuals with genital atrophy may benefit from topical estrogen therapy, and, in select cases of refractory OAB, tricyclic antidepressants may be helpful.



Class Summary

Anticholinergics inhibit the binding of acetylcholine to the muscarinic receptor in the detrusor, thereby suppressing involuntary bladder contractions. They are associated with an increase in bladder volume voided, as well as a decrease in micturition frequency and sensation of urgency.

Angioedema of the face, lips, tongue, and/or pharynx has been noted in several of these agents in postmarketing surveillance, including solifenacin, darifenacin, trospium chloride, and fesoterodine. Warnings are noted in the prescribing information for these agents, and if patients experience such symptoms they should seek emergency care.

Oxybutynin (Ditropan, Ditropan XL, Oxytrol, Gelnique)


Oxybutynin inhibits the action of acetylcholine on smooth muscle and has a direct antispasmodic effect on smooth muscles. This, in turn, increases bladder capacity and decreases uninhibited contractions. Oxybutynin is relatively M3, M1 specific.

Tolterodine (Detrol, Detrol LA)


Tolterodine is a nonspecific competitive muscarinic receptor antagonist for OAB. However, it differs from other anticholinergic types in that it has selectivity for urinary bladder over salivary glands. Tolterodine exhibits a high specificity for muscarinic receptors. It has minimal activity or affinity for other neurotransmitter receptors and other potential targets, such as calcium channels.

Trospium (Sanctura)


Trospium is a nonspecific quaternary ammonium compound that is excreted intact in the urine and thus is not dependent on the cytochrome P450 system for its metabolism. Being a quarternary amine, it is less likely to penetrate the blood-brain barrier. It antagonizes acetylcholine's effect on muscarinic receptors. Its parasympathetic effect reduces smooth-muscle tone in the bladder. Trospium is indicated to treat symptoms of OAB (eg, urinary incontinence, urgency, frequency). It is available as a single dose, and the extended release formulation should not be taken at night.

Darifenacin (Enablex)


Darifenacin is an extended-release product that elicits competitive muscarinic receptor antagonistic activity. It reduces bladder smooth-muscle contractions. It has high affinity for the M3 receptors and less affinity for other muscarinic receptors. Darifenacin is indicated for OAB with symptoms of urge incontinence, urgency and frequency. Swallow it whole; do not chew, divide, or crush it.

Solifenacin (Vesicare)


Solifenacin is a competitive muscarinic-receptor antagonist that was approved by the US Food and Drug Administration (FDA) in late 2004 for the treatment of OAB with symptoms of urge incontinence, urgency, and urinary frequency. It shares a similar muscarinic receptor affinity as oxybutyinin and is available in 2 doses.

Fesoterodine (Toviaz)


Fesoterodine is the most recent anticholinergic agent to be approved. It is available in 2 doses, and the 8-mg dose has been shown to be superior to tolterodine (Detrol LA) 4mg in the reduction of UUI episodes. It shares a similar muscarinic receptor affinity as tolterodine.


Beta3-adrenergic agonists

Class Summary

These agents elicit a direct inhibition of afferent nerve firing independent of the relaxing effects on bladder smooth muscle.

Mirabegron (Myrbetriq)


Mirabegron is a beta-3 adrenergic receptor agonist that causes relaxation of the detrusor smooth muscle of the urinary bladder and increases bladder capacity. It is indicated for overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.


Neuromuscular Blockers, Botulinum Toxins

Class Summary

Detrusor injections of botulinum neurotoxin type A may be considered for adults with OAB who cannot use or do not adequately respond to anticholinergic medication.

OnabotulinumtoxinA (Botox)


OnabotulinumtoxinA is a neurotoxin derived from Clostridium botulinum. It prevents ACh release from presynaptic membrane, resulting in a temporary calming effect of muscle contractions by blocking the transmission of nerve impulses.


Tricyclic antidepressants

Class Summary

Tricyclic antidepressants that have been used to treat OAB include imipramine and doxepin. Some agents of this type may decrease bladder contractility. They are not indicated for the first-line treatment of OAB.

Imipramine (Tofranil)


Imipramine is useful in facilitating urine storage. It decreases bladder contractility and increases outlet resistance.

Doxepin (Sinequan)


Doxepin increases the concentration of serotonin and norepinephrine in the central nervous system (CNS) by inhibiting their reuptake by presynaptic neuronal membrane. These effects are associated with a decrease in symptoms of depression.



Class Summary

Hormones are used to treat OAB in association with atrophic urethritis and are not recommended as first-line therapies for OAB.

Estrogen (Premarin)


Detrusor overactivity can be associated with atrophic urethritis; topical application of estrogen vaginal cream should be considered in women with symptomatic atrophic urethritis/vaginits.

Contributor Information and Disclosures

Pamela I Ellsworth, MD Professor of Urology, University of Massachusetts Medical School; Chief, Division of Pediatric Urology, Department of Urology, UMassMemorial Medical Center

Pamela I Ellsworth, MD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Pediatrics, American College of Surgeons, American Urological Association, Phi Beta Kappa, Society of University Urologists, Society for Fetal Urology

Disclosure: Nothing to disclose.


Miriam T Vincent, MD, PhD, JD Professor and Chair, Department of Family Practice, State University of New York Downstate Medical Center

Miriam T Vincent, MD, PhD, JD is a member of the following medical societies: Alpha Omega Alpha, American Association for the Advancement of Science, American Bar Association, American Bar Association, American Academy of Family Physicians, Sigma Xi, Society of Teachers of Family Medicine

Disclosure: Nothing to disclose.

Aneela Naureen Hussain, MD, MBBS, FAAFM Diplomate, American Board of Family Medicine; Assistant Professor, Department of Family Medicine, State University of New York Downstate Medical Center; Consulting Staff, Department of Family Medicine, University Hospital of Brooklyn

Aneela Naureen Hussain, MD, MBBS, FAAFM is a member of the following medical societies: American Academy of Family Physicians, American Medical Association, American Medical Womens Association, Medical Society of the State of New York, Society of Teachers of Family Medicine

Disclosure: Nothing to disclose.

LiAnn N Handel, MD Resident Physician, Department of Urology, Rhode Island Hospital, The Warren Alpert Medical School of Brown University

LiAnn N Handel, MD is a member of the following medical societies: American Urological Association

Disclosure: Nothing to disclose.

Wellman W Cheung, MD, FACS Clinical Professor, Department of Urology and Department of Obstetrics and Gynecology, State University of New York Downstate Medical School

Wellman W Cheung, MD, FACS is a member of the following medical societies: American College of Surgeons, American Medical Association, American Urological Association, Chinese American Medical Society, Endourological Society, American Urogynecologic Society, International Urogynaecology Association, Society of Urodynamics, Female Pelvic Medicine and Urogenital Reconstruction

Disclosure: Received grant/research funds from Astallas for pi.

Nadia Hasan Khan, MD Clinical Assistant Instructor, Staff Physician, Department of Family Practice, State University of New York Downstate Medical Center

Nadia Hasan Khan, MD is a member of the following medical societies: American Academy of Family Physicians

Disclosure: Nothing to disclose.

Specialty Editor Board

Francisco Talavera, PharmD, PhD Adjunct Assistant Professor, University of Nebraska Medical Center College of Pharmacy; Editor-in-Chief, Medscape Drug Reference

Disclosure: Received salary from Medscape for employment. for: Medscape.

Chief Editor

Edward David Kim, MD, FACS Professor of Surgery, Division of Urology, University of Tennessee Graduate School of Medicine; Consulting Staff, University of Tennessee Medical Center

Edward David Kim, MD, FACS is a member of the following medical societies: American College of Surgeons, Tennessee Medical Association, Sexual Medicine Society of North America, American Society for Reproductive Medicine, American Society of Andrology, American Urological Association

Disclosure: Serve(d) as a director, officer, partner, employee, advisor, consultant or trustee for: Repros.

Additional Contributors

Bradley Fields Schwartz, DO, FACS Professor of Urology, Director, Center for Laparoscopy and Endourology, Department of Surgery, Southern Illinois University School of Medicine

Bradley Fields Schwartz, DO, FACS is a member of the following medical societies: American College of Surgeons, Society of Laparoendoscopic Surgeons, Society of University Urologists, Association of Military Osteopathic Physicians and Surgeons, American Urological Association, Endourological Society

Disclosure: Nothing to disclose.

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Communication between urothelium and suburothelium. ACh—acetylcholine; ATP—adenosine triphosphate; M2—muscarinic receptor subtype 2; M3—muscarinic receptor subtype 3; NO—nitric oxide; P2X1—purinergic receptor P2X, ligand-gated ion channel 1; P2X3—purinergic receptor P2X, ligand-gated ion channel 3; sGC—soluble guanyl cyclase; VR1—vanilloid receptor 1.
Overactive bladder (OAB) and quality of life (QoL). Short Form-36 (SF-36). Reprinted with permission from Blackwell.
Total community and institutional costs of overactive bladder (OAB) (in millions of dollars). UTI—urinary tract infection (UTI). Reprinted with permission from Elsevier.
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