| Watchedfields: | changed |
| Verifiedrevid: | 470611677 |
| Width: | 200 |
| Tradename: | Detrol, Detrusitol, others |
| Dailymedid: | Tolterodine |
| Pregnancy Au: | B3 |
| Routes Of Administration: | By mouth |
| Atc Prefix: | G04 |
| Atc Suffix: | BD07 |
| Legal Au: | S4 |
| Legal Ca: | Rx-only |
| Legal Uk: | POM |
| Legal Uk Comment: | [1] |
| Legal Us: | Rx-only |
| Legal Us Comment: | [2] [3] |
| Legal Eu: | Rx-only |
| Legal Eu Comment: | [4] |
| Bioavailability: | 77% |
| Protein Bound: | Approximately 96.3% |
| Elimination Half-Life: | 1.9–3.7 hours |
| Index2 Label: | as salt |
| Cas Number: | 124937-51-5 |
| Cas Number2: | 124937-52-6 |
| Pubchem: | 443879 |
| Pubchem2: | 443878 |
| Iuphar Ligand: | 360 |
| Drugbank: | DB01036 |
| Drugbank2: | DBSALT000467 |
| Chemspiderid: | 391967 |
| Chemspiderid2: | 391966 |
| Unii: | WHE7A56U7K |
| Unii2: | 5T619TQR3R |
| Kegg: | D00646 |
| Kegg2: | D01148 |
| Chebi: | 9622 |
| Chebi2: | 32245 |
| Chembl: | 1382 |
| Chembl2: | 1200871 |
| Synonyms: | PNU-200583E |
| Iupac Name: | (S)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-methylphenol |
| C: | 22 |
| H: | 31 |
| N: | 1 |
| O: | 1 |
| Smiles: | Cc1ccc(c(c1)[C@H](CCN(C(C)C)C(C)C)c2ccccc2)O |
| Stdinchi: | 1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1 |
| Stdinchikey: | OOGJQPCLVADCPB-HXUWFJFHSA-N |
Tolterodine, sold under the brand name Detrol among others, is a medication used to treat frequent urination, urinary incontinence, or urinary urgency.[5] Effects are seen within an hour. It is taken by mouth.[6]
Common side effects include headache, dry mouth, constipation, and dizziness. Serious side effects may include angioedema, urinary retention, and QT prolongation. Use in pregnancy and breastfeeding are of unclear safety.[5] [7] It works by blocking muscarinic receptors in the bladder thus decreasing bladder contractions.[8]
Tolterodine was approved for medical use in 1998.[8] It is available as a generic medication.[5] In 2020, it was the 271st most commonly prescribed medication in the United States, with more than 1million prescriptions.[9] [10]
Detrusor overactivity (DO, contraction of the muscular bladder wall) is the most common form of urinary incontinence (UI) in older adults. It is characterized by uninhibited bladder contractions causing an uncontrollable urge to void. Urinary frequency, urge incontinence and nocturnal incontinence occur. Abnormal bladder contractions that coincide with the urge to void can be measured by urodynamic studies. Treatment is bladder retraining,[11] pelvic floor therapy or with drugs that inhibit bladder contractions such as oxybutynin and tolterodine.
Known side effects:
The following reactions have been reported in people who have taken tolterodine since it has become available:
Tolterodine is not recommended for use in people with myasthenia gravis and angle closure glaucoma.
Tolterodine acts on M2 and M3[12] subtypes of muscarinic receptors whereas older antimuscarinic treatments for overactive bladder act more specifically on M3 receptors.
Tolterodine, although it acts on all types of receptors, has fewer side effects than oxybutynin (M3 and M1 selective, but more so in the parotid than in the bladder) as tolterodine targets the bladder more than other areas of the body.
It is marketed by Pfizer in Canada and the United States under the brand name Detrol. In Egypt it is also found under the trade names Tolterodine by Sabaa and Incont L.A. by Adwia.
In the US, Detrol is marketed by Viatris after Upjohn was spun off from Pfizer.[13] [14] [15]