Monograph
G04BD07 - Tolterodine |
Propably not porphyrinogenic |
PNP |
Rationale
Metabolised primarily by CYP 2D6, and to some extent 3A4, but has not been found to inhibit or induce CYP 2C9 or 3A4 in therapeutic use.
Chemical description
Tolterodine is a synthetic tertiary amine antimuscarinic agent.
Therapeutic characteristics
Tolterodine tartrate is used in the management of urinary frequency, urgency, and incontinence in detrusor instability, with actions similar to those of atropine. Given orally. Common adverse reactions of tolterodine that can be confused with an acute porphyric attack are vomiting, constipation, abdominal pain and dyspepsia.
Metabolism and pharmacokinetics
Tolterodine is mainly metabolised in the liver by the cytochrome P450 isoenzyme CYP2D6 to the active 5-hydroxymethyl derivative, which is further metabolised to carboxylic acid an N-dealkylated 5- carboxylic acid. In poor metabolisers tolterodine is N-dealkylated by CYP 3A4. Listed by Rendic (2002) as a substrate for CYP 2C9, 2C19, 2D6, and 3A4, but not as an inhibitor or inducer. No evidence of Cyp-inductive properties. The manufacturer states that tolterodine does not appear to cause clinically important interactions with drugs metabolised by major microsomal cytochrome P-450 (CYP) isoenzymes.
IPNet drug reports
Uneventful use reported in 2 patients with acute porphyria.
Similar drugs
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448.
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| * | Drug reference publications | |
| 2. | Sweetman SC, editor. Martindale: The complete drug reference. Tolterodine Tartrate. Pharmaceutical Press 2009.
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| * | Summary of Product Characteristics | |
| 3. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Detrusitol SR.
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Tradenames
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Detrusitol 1 mg, filmomhulde tabletten · Detrusitol 2 mg, filmomhulde tabletten · Detrusitol SR 2 mg, capsules met verlengde afgifte, hard · Detrusitol SR 4 mg, capsules met verlengde afgifte, hard · Tolterodinetartraat Accord 1 mg filmomhulde tabletten · Tolterodinetartraat Accord 2 mg filmomhulde tabletten · Tolterodinetartraat Aurobindo SR 2 mg, harde capsules met verlengde afgifte · Tolterodinetartraat Aurobindo SR 4 mg, harde capsules met verlengde afgifte · Tolterodinetartraat retard 2 mg Teva, capsules met verlengde afgifte · Tolterodinetartraat retard 4 mg Teva, capsules met verlengde afgifte · Tolterodinetartraat Sandoz 1 mg, filmomhulde tabletten · Tolterodinetartraat Sandoz 2 mg, filmomhulde tabletten · Tolterodinetartraat Sandoz retard 2 mg, capsules met verlengde afgifte, hard · Tolterodinetartraat Sandoz retard 4 mg, capsules met verlengde afgifte, hard · Tolterodinetartraat Viatris 1 mg filmomhulde tabletten · Tolterodinetartraat Viatris 2 mg capsules met verlengde afgifte, hard · Tolterodinetartraat Viatris 2 mg filmomhulde tabletten · Tolterodinetartraat Viatris 4 mg capsules met verlengde afgifte, hard · Uroline 2mg, capsules met verlengde afgifte, hard · Uroline 4mg, capsules met verlengde afgifte, hard 
Detrusitol · Detrusitol 1 mg compr. pellic. · Detrusitol 2 mg compr. pellic. · Detrusitol Retard 2 mg g?l. lib. prol. · Detrusitol Retard 4 mg g?l. lib. prol. · Tolterodine · Tolterodine Retard Teva 4 mg g?l. lib. prol. · Urolina · Urolina 2 mg g?l. lib. prol. · Urolina 4 mg g?l. lib. prol. 
Detrusitol 2 mg Comprimidos Recubiertos con Pelicula · DETRUSITOL NEO 4 mg, CAPSULAS DURAS DE LIBERACION PROLONGADA · Tolterodina · Tolterodina Accord 4 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina Macleods 2 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina Macleods 4 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina neo Aurovitas 4 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina neo Cinfa 4 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina neo Kern Pharma 4 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina neo Normon 4 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina neo Ratiopharm 4 mg Capsulas Duras de Liberacion Prolongada efg · TOLTERODINA NEO SANDOZ 4 mg CAPSULAS DURAS DE LIBERACION PROLONGADA EFG · Tolterodina neo Stada 4 mg Capsulas Duras de Liberacion Prolongada efg · Tolterodina Pharmathen 4 mg Capsulas Duras de Liberacion Prolongada efg · UROTROL 2 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · UROTROL NEO 4 mg CAPSULAS DURAS DE LIBERACION PROLONGADA 
Tolterodina 
Uroflow 1 · Uroflow 2 
Blerone · Detrusitol · Detrusitol XL · Efflosomyl · Inconex · Mariosea · Mariosea XL · Neditol · Neditol XL · Preblacon XL · Santizor · Toldelo · Tolterma · Tolterma XL · Tolterodine · Tolthen 
Detrusitol Retard · Tolterodin Rivopharm · Tolterodin Stada · Tolterodine Sandoz · Tolterodintartrat Accord · Tolterodintartrat Teva 
Defur · Detrusitol · Detrusitol SR · Tolterodin-aristo · Tolterodine Sandoz · Tolterodinetartraat aurobindo SR · Tolzurin 
Defur · Ranolteril · Titlodine · Tolzurin · Urimper · Uroflow 1 · Uroflow 2 · Uroflow SR 
Detrusitol · Detrusitol retard · Tolterodin-ratiopharm · Urolina 
Detrusitol Retard · Tolterodin Actavis 
Detrusitol · Detrusitol Sr · Tolterodin Ratiopharm · Tolterodin SanoSwiss · Tolterodin Viatris · Tolterodine Sandoz 
Uroflow 
Detrusitol®
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