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.
References
- Scientific articles
- Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448. #1025
- Drug reference publications
- Sweetman SC, editor. Martindale: The complete drug reference. Tolterodine Tartrate. Pharmaceutical Press 2009. #1548
- Summary of Product Characteristics
- Norwegian medicines agency. Summary of Product Characteristics (SPC). Detrusitol SR. #1549
Similar drugs
© NAPOS 2024