5-HMT hydrogels effectively avoided the metabolism difference of enzyme in bodies compared with tolterodine tablets, provided one single active compound in plasma to reduce the variability of having two active compounds
5-hydroxymethyl tolterodine [see
Tolterodine (Monograph) Brand name: Detrol Drug class: Antimuscarinics VA class: AU350 Chemical name: (R)-2- [3- [Bis (1-methylethyl)amino]-1-phenylpropyl]-4
The pharmacokinetic profile of tolterodine is linear over the dose range 1–4 mg
1 b) and fesoterodine (FES, Fig
The present study aimed to characterize muscarinic receptor binding of fesoterodine, 5-hydroxymethyl tolterodine (5-HMT), and tolterodine in bladder and
001 Abstract The present study aimed to characterize muscarinic receptor binding of fesoterodine, 5-hydroxymethyl tolterodine (5-HMT), and
In vitro, this compound prevented charbachol-induced contraction of isolated guinea pig bladder strips in a competitive and concentration-dependent manner
(R)-5-Hydroxymethyl Tolterodine is not selective for any
The 5-hydroxymethyl metabolite is not extensively protein bound, with unbound fraction concentrations averaging 36% ± 4
5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips
14, respectively
This activity outlines the indications, action, and contraindications for tolterodine as a valuable agent in treating overactive bladder
The blood to serum ratio of tolterodine and the 5-hydroxymethyl metabolite averages 0
7% ± 0
6 In another Phase 1 study, elderly volunteers (aged 71 through 81 years) were given tolterodine immediate release 2 or 4 mg (1 or 2 mg bid)
4, 5 It was previously reported that fesoterodine, 5-HMT and tolterodine displayed higher affinity for the M 1 and M 2 than the M 3 subtype or Tolterodine absorption occurs in the gastrointestinal tract and is metabolized to 5-hydroxymethyl tolterodine (5-HMT - active metabolite - 29) by CYP2D6 enzymes present in the liver and intestine
The 5-hydroxymethyl metabolite is not extensively protein bound, with unbound fraction concentrations averaging 36% ± 4
Tolterodine undergoes extensive first-pass metabolism, cytochrome P450 2D6 (CYP 2D6) metabolises
Molecular Formula