| Identification | More | [Name]
Solifenacin succinate | [CAS]
242478-38-2 | [Synonyms]
1-azabicyclo[2.2.2]octan-8-yl (1s)-1-phenyl-3,4-dihydro-1h-isoquinoline-2-carboxylate butanedioic acid
solifenacin succinate
vesicare
IsoprenalinoeSulfate
1-Azabicyclo[2.2.2]octan-8-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate butanedioic acid | [EINECS(EC#)]
620-505-5 | [Molecular Formula]
C11H19NO7S | [MDL Number]
29339900 | [Molecular Weight]
309.336 | [MOL File]
242478-38-2.mol | [Description]
Orlistat is a prescription drug used for the treatment of obesity. Its major effect is preventing the absorption of fats through acting as a lipase inhibitor, further reducing the caloric intake. It can also reduce the blood pressure and can prevent the incidence of type II diabetes originated from various factors. Orlistat takes effect in the lumen of the stomach and small intestine through forming a covalent bond with the active serine site of gastric and pancreatic lipase, leading to its inactivation and failure to digest fat contained in the diet. The resultant low caloric absorptionleads to weight control. Study has also shown that orlistat has certain antitumor activity. |
| Questions And Answer | Back Directory | [Description]
Solifenacin succinate is an antimuscarinic medication that is used to treat an overactive bladder causing symptoms of frequency, urgency, or incontinence.
| [Proper Usage]
- This medication should be taken with liquids and swallowed whole. It may be taken with or without food.
- Take only the amount of this medication that has been prescribed for you by your doctor; taking more than the prescribed amount can cause adverse effects.
- If you miss a dose of this medication, begin taking it again the next day. Do not take two doses of solifenacin succinate in the same day.
| [Precautions]
- Individuals with any of the following medical problems should not take this medication: urinary retention, gastric retention, narrow angle or uncontrolled glaucoma, or severe kidney problems. Solifenacin succinate can aggravate each of these conditions.
- Solifenacin succinate may cause blurred vision; do not engage in potentially dangerous activities such as driving until you know the effect of the medication on your vision.
- This medication, like all anticholinergic medications, may cause drying of the mouth. Since continued dryness of the mouth can increase the risk of dental disease, alert your dentist if you are taking this medication.
- Like all anticholinergic medications, solifenacin succinate can cause or worsen constipation.
- Because of decreased sweating, this medication can cause heat prostration when used in a very hot environment.
- This medication has not been studied in pregnant women. However, it has been shown in animal studies to impact preand postnatal development. If you are pregnant, or planning to become pregnant, do not start this medication before you have discussed it with your physician.
- It is not known whether solifenacin succinate passes into breast milk. Women who taking this medication and wish to breastfeed should discuss it with their physician.
| [Possible Side effects]
- Side effects that are expected with this type of medication and do not require medical attention unless they continue or are bothersome: dry mouth; dry eyes; constipation, blurred vision, difficult urination.
- Less common side effect that should be reported to your physician: severe abdominal pain.
- Symptoms of overdose: severe central anticholinergic effects, including blurred vision; clumsiness or unsteadiness; confusion; seizures; severe diarrhea; excessive watering of the mouth; increasing 240 Multiple Sclerosis: A Self-Care Guide to Wellness muscle weakness (especially in the arms, neck, shoulders, and tongue); muscle cramps or twitching; severe nausea or vomiting; shortness of breath; slow heartbeat; slurred speech; unusual irritability, nervousness, or restlessness; unusual tiredness or weakness.
|
| Chemical Properties | Back Directory | [Melting point ]
~145° | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
Methanol (Slightly, Heated, Sonicated), Water (Slightly, Sonicated) | [form ]
Solid | [color ]
White to Off-White | [Optical Rotation]
[α]/D +35 to +45°, c =1 in H2O | [Water Solubility ]
H2O: 2mg/mL, clear | [Merck ]
14,8712 | [Stability:]
Hygroscopic | [InChIKey]
RXZMMZZRUPYENV-ZFHAYXBFNA-N | [SMILES]
C(C(=O)O)CC(=O)O.C(N1CCC2=CC=CC=C2[C@@H]1C1C=CC=CC=1)(=O)O[C@H]1CN2CCC1CC2 |&1:18,27,r| | [CAS DataBase Reference]
242478-38-2(CAS DataBase Reference) |
| Safety Data | Back Directory | [WGK Germany ]
WGK 3 | [RTECS ]
NW7136000 | [HS Code ]
29339900 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Repr. 2 |
| Hazard Information | Back Directory | [Chemical Properties]
White Solid | [Originator]
Yamanouchi (Japan) | [Uses]
Muscarinic M3 receptor antagoinst. Used in treatment of urinary incontinence. | [Uses]
sedative | [Uses]
Solifenacin succinate is a urinary antispasmodic of the antimuscarinic class. | [Definition]
ChEBI: Solifenacin succinate is a member of isoquinolines. | [Brand name]
Vesicare (Astellas). | [Synthesis Reference(s)]
[1]Kale, B. R., Hamid, H., & Alam, M. S. (2025). An Improved and Efficient Practical Process for the Synthesis of Enantiomerically Pure Solifenacin Succinate as an Antimuscarinic Agent. Current Organocatalysis, 12(1), 76–82. https://doi.org/10.2174/0122133372336988240910104559
[2]Trinadhachari, G. N., Kamat, A. G., Balaji, B. V., Prabahar, K. J., Naidu, K. M., Babu, K. R., & Sanasi, P. D. (2014). An Improved Process for the Preparation of Highly Pure Solifenacin Succinate via Resolution through Diastereomeric Crystallisation. Organic Process Research & Development, 18(8), 934–940. https://doi.org/10.1021/op500083y
[3]Niphade, N. C., Jagtap, K. M., Mali, A. C., Solanki, P. V., Jachak, M. N., & Mathad, V. T. (2011). Efficient and single pot process for the preparation of enantiomerically pure solifenacin succinate, an antimuscarinic agent. Monatshefte für Chemie - Chemical Monthly, 142(11), 1181–1186. https://doi.org/10.1007/s00706-011-0610-7 | [General Description]
Solifenacin succinate (Vesicare),(+)-(1S, 3'R)-quinuclidin-3'-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate, is a competative antagonistfor M1, M2, and M3 receptor subtypes. One of the issues surroundingthe use of such antagonists is the selectivity for thebladder over other tissue such as the salivary glands. It isreported that the selectivity of solifenacin for bladder muscarinicreceptors over salivary receptors is superior to theeffects observed with oxybutynin. | [Clinical Use]
Selective M3
antimuscarinic
Symptomatic treatment of urge incontinence and/or
increased urinary frequency and urgency | [Synthesis]
Enantiomerically pure solifenacin succinate can be synthesized via a Zn(OTf)2-catalyzed protocol using phenylethylamine and benzoyl chloride as starting materials, or through a one-pot process that retains chiral center configuration[1][3]. Alternative preparation methods involve resolution of diastereomeric mixtures through crystallization, including optimization with specific solvent systems such as ethanol in ethyl acetate[2]. The final salt formation is achieved by treating solifenacin with succinic acid in acetone, involving heating to 50–55°C followed by cooling to isolate crystals with high chemical and enantiomeric purity[3]. | [in vitro]
in radioligand receptor binding assay, the kivalues of solifenacin for human muscarinic m1, m2, m3, m4and m5receptors were 26, 170, 12, 110 and 31 nm, respectively. in isolated rat urinary bladder, solifenacin competitively antagonized carbachol-induced contractions, with a pa2value of 7.44±0.09[3].in bladder smooth muscle cells and salivary gland cells isolated from rats, solifenacin and the other antimuscarinic drugs inhibited carbachol-induced increases in intracellular ca2+levels in a concentration-dependent manner. thepki was 8.12for bladder smooth muscle cells, 3.6-fold more potent than that for salivary gland cells (pki=7.57) [1]. | [in vivo]
in anesthetized rats, solifenacin dose-dependently inhibited carbachol-induced intravesical pressure elevation and salivary secretion, and exhibited selectivity (3.7- to 6.5-fold) for urinary bladder over salivary gland [1]. in anesthetized rats, solifenacin and oxybutynin increased the maximum bladder capacity in a dose-dependent manner and also decreased the maximum intravesical pressure [3].in healthy young men, multidose study evaluated doses. in the single-dose of solifenacin succinate (5-, 10-, 20-, and 30-mg), mean time to maximal concentration and elimination half-life ranged from 3.3 to 4.8 and from 40.2 to 57.6 hours, respectively.in the multidose study, the ranges were 2.9 to 5.8 and 45.0 to 64.8, respectively. the single-dose administration was well tolerated. the common adverse events were dry mouth, blurred vision, and headache [4]. | [Drug interactions]
Potentially hazardous interactions with other drugs
Avoid if GFR<30 mL/min if also taking
itraconazole, ketoconazole or ritonavir.
Anti-arrhythmics: increased risk of antimuscarinic
side effects with disopyramide. | [Metabolism]
Extensively metabolised in the liver, mainly by the
cytochrome P450 isoenzyme CYP3A4 and is excreted
mainly as metabolites in urine and faeces. | [storage]
Store at -20°C | [References]
[1]. ohtake a, ukai m, hatanaka t, et al. in vitro and in vivo tissue selectivity profile of solifenacin succinate (ym905) for urinary bladder over salivary gland in rats[j]. european journal of pharmacology, 2004, 492(2): 243-250.
[2]. yang j, williams j a, yule d i, et al. mutation of carboxyl-terminal threonine residues in human m3 muscarinic acetylcholine receptor modulates the extent of sequestration and desensitization[j]. molecular pharmacology, 1995, 48(3): 477-485.
[3]. ohtake a, saitoh c, yuyama h, et al. pharmacological characterization of a new antimuscarinic agent, solifenacin succinate, in comparison with other antimuscarinic agents[j]. biological and pharmaceutical bulletin, 2007, 30(1): 54-58.
[4]. smulders r a, krauwinkel w j, swart p j, et al. pharmacokinetics and safety of solifenacin succinate in healthy young men[j]. the journal of clinical pharmacology, 2004, 44(9): 1023-1033.
[5]. cardozo l, lisec m, millard r, et al. randomized, double-blind placebo controlled trial of the once daily antimuscarinic agent solifenacin succinate in patients with overactive bladder[j]. the journal of urology, 2004, 172(5): 1919-1924. |
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