Solifenacin

(1S, 3'R )-1- azabicyclo [2.2.2 ] oct -8-yl -1-phenyl - 3,4- dihydro-1H -isoquinoline -2-carboxylate

• C23H26N2O2 ( solifenacin )
• C23H26N2O2 · C4H6O ( solifenacin · succinic acid )

• 242478-37-1 ( solifenacin )
• 242478-38-2 ( solifenacin · succinic acid )

G04BD08

• Yellow oil ( solifenacin )
• Colorless, slightly yellowish crystals ( solifenacin · succinic acid )

Spasmolytic

• 362.47 g · mol -1 ( solifenacin )
• 480.55 g · mol -1 ( · solifenacin succinate )

About 143 ° C ( · solifenacin succinate )

Template: Infobox chemical / molecular formula search available

Solifenacin is a drug from the pharmacological group of urological anticonvulsants to treat symptoms of overactive bladder (English " overactive bladder ", " OAB ").

Chemistry

Solifenacin is in pharmacy as solifenacin succinate - that as the salt of succinic acid - application.

Pharmacology

Areas of application and clinical effects

Solifenacin is for the symptomatic treatment of urge incontinence or urinary urgency and the imperative of urinary frequency, as can occur with the syndrome of overactive bladder in patients admitted.

Mechanism of Action

The urinary bladder is innervated by parasympathetic cholinergic nerves. Acetylcholine effects on muscarine receptors, mainly on the subtype M3, a detrusor smooth muscle contraction of the muscle. As receptor antagonist inhibits the muscarinic M3 solifenacin competitively and specifically, as it has only a low or no affinity for various other receptors or ion channels.

Considering the study results presented below can be the statement " there is little or no affinity for various other receptors and ion channels ", however, very doubtful:

In the publication by S. S. Hegde et al. (2004) reported that about twelve times better binding of solifenacin on human M3 as taking place at M2 muscarinic receptors. The ratio with respect to the M1 receptors is about 2.5. More favorable results from animal tests are not transferable to humans. This opinion is in any case the Federal Institute for Drugs and Medical Devices ( BfArM), the solifenacin has awarded no M3 - selectivity (as of August 2004). So far, the BfArM has only awarded to the drug darifenacin in vitro ( " test tube " ) an M3 selectivity, but with the note that it is not yet clear whether this is at all a clinical advantage (as of December 2004).

Side effects

Due to the pharmacological effect of solifenacin anticholinergic side effects of generally light can be caused to moderate severity. The incidence is dose dependent.

The side effect most frequently described, which is considerably less in the incidence but lower than other anticholinergics is dry mouth, which occurs daily at the dose of 5 mg solifenacin at about 11% of patients. In addition, side effects such as constipation, nausea, abdominal pain, blurred vision occur in very lesser extent, among others.

The statement that " the side effect most frequently described, dry mouth, much less common than among other anticholinergics " occurs is to discuss the following aspects:

In a clinical study, solifenacin was (both licensed doses were evaluated together ) directly with a retarded anticholinergic compared. Under solifenacin more patients reported dry mouth as under the reference substance (30 % vs. 24 %). The same is true for constipation ( 6.4 % vs. 2.5%). Visual disturbances were less frequent among solifenacin on (0.7% versus 1.7 %).

Interactions

There are no clinically relevant drug-drug interactions of solifenacin known.

Trade names

Vesicare (A, CH), Vesikur (D)