Darifenacin hydrobromide
نویسندگان
چکیده
In the title compound {systematic name: (S)-3-[(aminocar-bonyl)diphenylmethyl]-1-[2-(2,3-di-hy-dro-benzofuran-5-yl)ethyl]pyrrolidinium bromide}, C(28)H(31)N(2)O(2) (+)·Br(-), the pyrrolidine rings adopts an envelope conformation. The two phenyl rings make a dihedral angle of 72.5 (1)°. The four coplanar atoms of the pyrrolidine ring makes dihedral angles of 33.1 (2) and 82.8 (2)° with the two phenyl rings. The mol-ecular conformation is influenced by a C-H⋯O inter-action. In the crystal packing, there are two N-H⋯Br hydrogen bonds running in opposite directions. They appear to form C(10) and C(9) chain motifs in the unit cell. In addition, the mol-ecular packing is further stabilized by C-H⋯Br and C-H⋯O hydrogen bonds. The C atom bonded to the benzofuran ring system is disordered in a 0.66:0.34 ratio.
منابع مشابه
Dissolution Rate Enhancement, Design and Development of Buccal Drug Delivery of Darifenacin Hydroxypropyl β-Cyclodextrin Inclusion Complexes
Darifenacin is a urinary antispasmodic. The oral absorption of darifenacin is poor due to its low solubility and poor bioavailability (15-19%). Darifenacin was complexed with hydroxylropyl beta-cyclodextrin (Hpβ-CD). The best results were obtained with the coevaporation that interacts in a 1 : 1 drug : cyclodextrin molar ratio. The solid inclusion complexes were found to be amorphous in the cha...
متن کاملA comparison of the efficacy of darifenacin alone vs. darifenacin plus a Behavioural Modification Programme upon the symptoms of overactive bladder
PURPOSE This study assessed the benefit of adding behavioural modification to darifenacin treatment for overactive bladder (OAB). MATERIALS AND METHODS The ABLE trial was a randomised, open-label, parallel-group, multicentre study of 12 weeks of darifenacin treatment [with voluntary up-titration from 7.5 mg once daily (qd) to 15 mg qd at week 2] alone or in combination with a Behavioural Modi...
متن کاملContribution of the M3 muscarinic receptors to the vasodilator response to acetylcholine in the human forearm vascular bed.
AIMS Acetylcholine (ACh) is a muscarinic agonist that causes receptor-mediated, endothelium-dependent vasodilatation in the forearm vasculature. Previous indirect evidence suggests this effect may be mediated by muscarinic M(3) receptors. Darifenacin is a recently developed antimuscarinic drug with greater M(3) selectivity, and our main objective was to investigate whether darifenacin affects d...
متن کاملDarifenacin Has No Clinically Relevant Effect on Warfarin or Digoxin Pharmacodynamics/kinetics in Healthy Males
Darifenacin is a muscarinic M3 selective receptor antagonist developed for the treatment of overactive bladder (OAB). OAB is common in older patients, who may also receive warfarin or digoxin. As darifenacin is a substrate for cytochrome P450 (CYP) enzymes 2D6 and 3A4, and for the p-glycoprotein pump (p-gp) (Skerjanec et al., 2004), interactions with other substrates such as warfarin (CYP3A4) a...
متن کاملChoice of antimuscarinic agents for overactive bladder in the older patient: focus on darifenacin
Overactive bladder (OAB) is a difficult condition to live with and is very costly to the community. OAB affects 16% of the adult population and rises with increasing age. We describe the necessary steps in evaluation and behavioral therapy prior to initiating medical therapy. There are several medications that have been used for the treatment of patients who suffer from OAB. This manuscript dis...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره 65 شماره
صفحات -
تاریخ انتشار 2009