Vesikar tablets 10 mg, 30 pcs. (Solyfenatsyn)
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$37.40
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$44.00
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tablets. Buy Vesikar tablets 10 mg, 30 pcs. (Solyfenatsyn) in newyork free shipping. Fast international shipping USA, AU, EU, UK and others.
tablets. Buy Vesikar tablets 10 mg, 30 pcs. (Solyfenatsyn) in newyork free shipping. Fast international shipping USA, AU, EU, UK and others.
release form
tablets.
Packing
30 pcs.
Pharmacological action of
Pharmaceutical group: antispasmodic.
Pharmaceutical effects: In vitro and in vivo pharmacological studies have shown that solifenacin is a specific competitive inhibitor of muscarinic receptors, predominantly the M3 subtype. It was also found that solifenacin has a low or lack of affinity for various other receptors and ion channels.
The effectiveness of the drug Vezikar in doses of 5 mg and 10 mg, studied in several double-blind, randomized, controlled clinical trials in men and women with overactive bladder syndrome, was observed during the first week of treatment and stabilized over the next 12 weeks of treatment.
The maximum effect of Vesicar can be detected after 4 weeks. Efficiency persists for prolonged use (at least 12 months).
Pharmacokinetics: General characteristics of
Absorption: Maximum plasma concentration (Cmax) is reached after 3-8 hours. The time to reach maximum concentration (tmax) is dose-independent. Сmax and the area under the curve (PPC) of the concentration dependence of time increase in proportion to the dose increase from 5 to 40 mg. Absolute bioavailability is 90%. Eating does not affect Cmax and PPC of solifenacin.
Distribution: The volume of distribution of solifenacin after intravenous administration is approximately 600 liters. Solifenacin to a large extent (about 98%) is associated with plasma proteins, mainly with β 1-acid glycoprotein.
Metabolism: Solifenacin is actively metabolized by the liver, mainly cytochrome P450 ZA4 (CYP3A4). However, there are alternative metabolic pathways through which solifenacin metabolism can occur. The systemic clearance of solifenacin is about 9.5 l / h, and the final half-life is 45-68 hours. After oral administration of the drug in plasma, the following metabolites were identified in addition to solifenacin: one pharmacologically active (4R-hydroxysolifenacin) and three inactive (N-glucuronide, N-oxide and 4R-hydroxy-N-solifenacin oxide).
Output: After a single dose of 10 mg of 14C-labeled solifenacin, after 26 days, about 70% of the radioactivity was detected in urine and 23% in feces. In urine, approximately 11% of the radioactivity was detected as unchanged active substance, about 18% as an N-oxide metabolite, 9% as a 4R-hydroxy-N-oxide metabolite, and 8% as a 4R-hydroxy metabolite (active metabolite).
The pharmacokinetics of solifenacin is linear in the therapeutic dose range.
Pharmacokinetics in certain categories of patients
Age: There is no need to adjust the dose depending on the age of the patients. Studies have shown that exposure to solifenacin (5 and 10 mg), expressed as AUC, was similar in healthy elderly individuals (65 to 80 years old) and healthy young individuals (<55 years old). The average absorption rate, expressed as tmax. was slightly lower, and the final half-life is approximately 20% longer in older people. These minor differences are not clinically significant. The pharmacokinetics of solifenacin has not been determined in children and adolescents. Gender: The pharmacokinetics of solifenacin is independent of the patient’s gender.
Race: Race does not affect the pharmacokinetics of solifenacin. Renal failure: AUC and Cmax of solifenacin in patients with mild to moderate renal failure are not significantly different from those in healthy volunteers. In patients with severe renal insufficiency (creatinine clearance) Hepatic insufficiency: In patients with moderate hepatic insufficiency (Child-Pugh score from 7 to 9), the C max value does not change, the BEP increases by 60%, t1 / 2 doubles. Pharmacokinetics in patients with severe hepatic impairment has not been determined.
Indications
Treatment of urgent (imperative) urinary incontinence, rapid urination and urgent (imperative) urination, characteristic of patients with overactive bladder syndrome.
Contraindications
urinary retention
severe gastrointestinal diseases (including toxic megacolon)
myasthenia gravis
angle-closure glaucoma
hypersensitive hepatic insufficiency CYP3A4 for example ketoconazole
Special instructions
Before starting treatment with Vesicar, it should be ascertained if there are any other causes of rapid urination (heart failure or kidney disease). If a urinary tract infection is detected, appropriate antibacterial treatment should be initiated. Vesicar should be used with caution in patients: • with clinically significant obstruction of the bladder outlet leading to a risk of urinary retention
• with gastrointestinal obstructive disease
• with a risk of decreased motility of the gastrointestinal tract
• with severe renal clearance (creatinine clearance • simultaneously taking a strong CYP3A4 inhibitor, for example , ketoconazole
• with hiatal hernia, gastroesophageal reflux, and patients taking medications (such as bisphosphonates) that may cause or strengthen esrdagitis
• with autonomic neuropathy
Patients with rare hereditary galactose tolerance disorders, lactase deficiency of the lapars (Sami), glucose-galactose malabsorption should not take the drug.
Effect on the ability to drive a car and drive mechanisms
Solifenacin, like other anticholinergics, can cause blurred visual perception, as well as (rarely) drowsiness and a feeling of fatigue, which can adversely affect the ability to drive and operate machinery.
Composition of
1 tab.: - solifenacin succinate 10 mg
Excipients:
lactose monohydrate - 102.5 mg,
corn starch - 30 mg,
hypromellose 3 mPa s mg-5 mg,
.
Film composition:
opadray pink 03F14895 (hypromellose 6 MPa s 62%, talc 18.59%, macrogol 8000 11.63%, titanium dioxide 7.75%, iron oxide red 0.03%) - 4 mg.
Dosage and administration of
5 mg once daily orally, washed down with liquid, regardless of the meal time.
If necessary, the dose may be increased to 10 mg once a day.
Side effects
Most often - dry oral mucosa (11% when taken at a dose of 5 mg per day, 22% - 10 mg per day).
Frequent (more than 1/100 and less than 1/10), infrequent (more than 1/1000 and less than 1/100), rare (more than 1/10000 and less than 1/1000).
From the digestive system: frequent - constipation, nausea, dyspepsia, abdominal pain, infrequent - gastroesophageal reflux disease, dry pharyngeal mucosa rare - intestinal obstruction, coprostasis.
From the nervous system: infrequent - drowsiness, taste disturbance.
From the sensory organs: frequent - blurred visual perception (disturbance of accommodation) infrequent - dry eyes.
From the respiratory system: infrequent - dryness of the nasal mucosa.
From the skin: infrequent - dry skin.
From the urinary system: infrequent - difficult urination rare - urinary retention.
Other: infrequent - urinary tract infections, fatigue, peripheral edema.
Drug Interactions
- Pharmacological Interactions
Concomitant drug treatment with anticholinergic properties can lead to more pronounced therapeutic and undesirable effects. After you stop taking solifenacin, you should take a break of about a week before starting treatment with another anticholinergic drug. The therapeutic effect can be reduced while taking cholinergic receptor agonists. Solifenacin can reduce the effect of drugs that stimulate gastrointestinal motility, such as metoclopramide and cisapride.
- Pharmacokinetic interaction of
In vitro studies have shown that in therapeutic concentrations, solifenacin does not inhibit CYP1A 1/2, 2C9, 2C19, 2D6 or ZA4 isolated from human liver microsomes. Therefore, solifenacin is unlikely to alter the clearance of drugs metabolized by these CYP enzymes.
Effects of other drugs on the pharmacokinetics of solifenacin.
Solifenacin is metabolized by CYP3A4. The simultaneous administration of ketoconazole (200 mg per day), a potent inhibitor of CYP3A4, caused a twofold increase in AUC depending on the concentration of time of solifenacin, and at a dose of 400 mg / day - a threefold increase. Therefore, the maximum dose of Vesicar should not exceed 5 mg if the patient is simultaneously taking ketoconazole or therapeutic doses of other strong CYP3A4 inhibitors (such as ritonavir, nelfinavir. Itraconazole). Concomitant treatment with solifenacin and a potent CYP3A4 inhibitor is contraindicated in patients with severe renal failure or moderate liver failure. Since solifenacin is metabolized by CYP3A4, pharmacokinetic interactions with other CYP3A4 substrates with higher affinity (verapamil, diltiazem) and with CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) are possible.
- Effect of solifenacin on the pharmacokinetics of other drugs
Oral contraceptives: No pharmacokinetic interaction of solifenacin and combined oral contraceptives (ethinyl estradiol \ levonorgestrel) has been identified.
Warfarin: Vesicar administration did not cause changes in the pharmacokinetics of R-warfarin or S-warfarin or their effect on prothrombin time.
digoxin: Vesicar administration did not affect the pharmacokinetics of digoxin.
Overdose of
The highest dose of solifenacin used by volunteers was 100 mg in a single dose. The following side effects were most often observed at this dose: headache (mild), dry mouth (moderate), dizziness (moderate), drowsiness (mild) and blurred vision (moderate). No cases of acute overdose have been reported. In cases of overdose, activated charcoal should be prescribed, gastric lavage should be done, but vomiting should not be caused.
As in cases of overdose of other anticholinergics, the symptoms should be treated as follows: • for severe anticholinergic effects of a central effect (hallucinations, severe irritability) - physostigmine or carbachol
• for seizures or severe excitability - benzodiazepines
• for respiratory failure
• for tachycardia - beta blockers
• for urinary retention - catheterization
• for mydriasis - instill pilocarpine in the eyes and / or place a pain Foot in a dark room.
As in the case of an overdose of other anticholinergic drugs, special attention should be paid to patients with an established risk of lengthening the QT interval (i.e., with hypokalemia, bradycardia and with the simultaneous administration of drugs that cause prolongation of the QT interval) and patients with heart diseases (myocardial ischemia, arrhythmias, congestive heart failure).
Terms and conditions
prescription
dosage form
tablets
Astellas Pharma BV Yurop, Netherlands
Vesikar tablets 10 mg, 30 pcs. (Solyfenatsyn) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Vesikar tablets 10 mg, 30 pcs. - Sale. PayPal accept. Free shipping florida. Fast international shipping.
tablets.
Packing
30 pcs.
Pharmacological action of
Pharmaceutical group: antispasmodic.
Pharmaceutical effects: In vitro and in vivo pharmacological studies have shown that solifenacin is a specific competitive inhibitor of muscarinic receptors, predominantly the M3 subtype. It was also found that solifenacin has a low or lack of affinity for various other receptors and ion channels.
The effectiveness of the drug Vezikar in doses of 5 mg and 10 mg, studied in several double-blind, randomized, controlled clinical trials in men and women with overactive bladder syndrome, was observed during the first week of treatment and stabilized over the next 12 weeks of treatment.
The maximum effect of Vesicar can be detected after 4 weeks. Efficiency persists for prolonged use (at least 12 months).
Pharmacokinetics: General characteristics of
Absorption: Maximum plasma concentration (Cmax) is reached after 3-8 hours. The time to reach maximum concentration (tmax) is dose-independent. Сmax and the area under the curve (PPC) of the concentration dependence of time increase in proportion to the dose increase from 5 to 40 mg. Absolute bioavailability is 90%. Eating does not affect Cmax and PPC of solifenacin.
Distribution: The volume of distribution of solifenacin after intravenous administration is approximately 600 liters. Solifenacin to a large extent (about 98%) is associated with plasma proteins, mainly with β 1-acid glycoprotein.
Metabolism: Solifenacin is actively metabolized by the liver, mainly cytochrome P450 ZA4 (CYP3A4). However, there are alternative metabolic pathways through which solifenacin metabolism can occur. The systemic clearance of solifenacin is about 9.5 l / h, and the final half-life is 45-68 hours. After oral administration of the drug in plasma, the following metabolites were identified in addition to solifenacin: one pharmacologically active (4R-hydroxysolifenacin) and three inactive (N-glucuronide, N-oxide and 4R-hydroxy-N-solifenacin oxide).
Output: After a single dose of 10 mg of 14C-labeled solifenacin, after 26 days, about 70% of the radioactivity was detected in urine and 23% in feces. In urine, approximately 11% of the radioactivity was detected as unchanged active substance, about 18% as an N-oxide metabolite, 9% as a 4R-hydroxy-N-oxide metabolite, and 8% as a 4R-hydroxy metabolite (active metabolite).
The pharmacokinetics of solifenacin is linear in the therapeutic dose range.
Pharmacokinetics in certain categories of patients
Age: There is no need to adjust the dose depending on the age of the patients. Studies have shown that exposure to solifenacin (5 and 10 mg), expressed as AUC, was similar in healthy elderly individuals (65 to 80 years old) and healthy young individuals (<55 years old). The average absorption rate, expressed as tmax. was slightly lower, and the final half-life is approximately 20% longer in older people. These minor differences are not clinically significant. The pharmacokinetics of solifenacin has not been determined in children and adolescents. Gender: The pharmacokinetics of solifenacin is independent of the patient’s gender.
Race: Race does not affect the pharmacokinetics of solifenacin. Renal failure: AUC and Cmax of solifenacin in patients with mild to moderate renal failure are not significantly different from those in healthy volunteers. In patients with severe renal insufficiency (creatinine clearance) Hepatic insufficiency: In patients with moderate hepatic insufficiency (Child-Pugh score from 7 to 9), the C max value does not change, the BEP increases by 60%, t1 / 2 doubles. Pharmacokinetics in patients with severe hepatic impairment has not been determined.
Indications
Treatment of urgent (imperative) urinary incontinence, rapid urination and urgent (imperative) urination, characteristic of patients with overactive bladder syndrome.
Contraindications
urinary retention
severe gastrointestinal diseases (including toxic megacolon)
myasthenia gravis
angle-closure glaucoma
hypersensitive hepatic insufficiency CYP3A4 for example ketoconazole
Special instructions
Before starting treatment with Vesicar, it should be ascertained if there are any other causes of rapid urination (heart failure or kidney disease). If a urinary tract infection is detected, appropriate antibacterial treatment should be initiated. Vesicar should be used with caution in patients: • with clinically significant obstruction of the bladder outlet leading to a risk of urinary retention
• with gastrointestinal obstructive disease
• with a risk of decreased motility of the gastrointestinal tract
• with severe renal clearance (creatinine clearance • simultaneously taking a strong CYP3A4 inhibitor, for example , ketoconazole
• with hiatal hernia, gastroesophageal reflux, and patients taking medications (such as bisphosphonates) that may cause or strengthen esrdagitis
• with autonomic neuropathy
Patients with rare hereditary galactose tolerance disorders, lactase deficiency of the lapars (Sami), glucose-galactose malabsorption should not take the drug.
Effect on the ability to drive a car and drive mechanisms
Solifenacin, like other anticholinergics, can cause blurred visual perception, as well as (rarely) drowsiness and a feeling of fatigue, which can adversely affect the ability to drive and operate machinery.
Composition of
1 tab.: - solifenacin succinate 10 mg
Excipients:
lactose monohydrate - 102.5 mg,
corn starch - 30 mg,
hypromellose 3 mPa s mg-5 mg,
.
Film composition:
opadray pink 03F14895 (hypromellose 6 MPa s 62%, talc 18.59%, macrogol 8000 11.63%, titanium dioxide 7.75%, iron oxide red 0.03%) - 4 mg.
Dosage and administration of
5 mg once daily orally, washed down with liquid, regardless of the meal time.
If necessary, the dose may be increased to 10 mg once a day.
Side effects
Most often - dry oral mucosa (11% when taken at a dose of 5 mg per day, 22% - 10 mg per day).
Frequent (more than 1/100 and less than 1/10), infrequent (more than 1/1000 and less than 1/100), rare (more than 1/10000 and less than 1/1000).
From the digestive system: frequent - constipation, nausea, dyspepsia, abdominal pain, infrequent - gastroesophageal reflux disease, dry pharyngeal mucosa rare - intestinal obstruction, coprostasis.
From the nervous system: infrequent - drowsiness, taste disturbance.
From the sensory organs: frequent - blurred visual perception (disturbance of accommodation) infrequent - dry eyes.
From the respiratory system: infrequent - dryness of the nasal mucosa.
From the skin: infrequent - dry skin.
From the urinary system: infrequent - difficult urination rare - urinary retention.
Other: infrequent - urinary tract infections, fatigue, peripheral edema.
Drug Interactions
- Pharmacological Interactions
Concomitant drug treatment with anticholinergic properties can lead to more pronounced therapeutic and undesirable effects. After you stop taking solifenacin, you should take a break of about a week before starting treatment with another anticholinergic drug. The therapeutic effect can be reduced while taking cholinergic receptor agonists. Solifenacin can reduce the effect of drugs that stimulate gastrointestinal motility, such as metoclopramide and cisapride.
- Pharmacokinetic interaction of
In vitro studies have shown that in therapeutic concentrations, solifenacin does not inhibit CYP1A 1/2, 2C9, 2C19, 2D6 or ZA4 isolated from human liver microsomes. Therefore, solifenacin is unlikely to alter the clearance of drugs metabolized by these CYP enzymes.
Effects of other drugs on the pharmacokinetics of solifenacin.
Solifenacin is metabolized by CYP3A4. The simultaneous administration of ketoconazole (200 mg per day), a potent inhibitor of CYP3A4, caused a twofold increase in AUC depending on the concentration of time of solifenacin, and at a dose of 400 mg / day - a threefold increase. Therefore, the maximum dose of Vesicar should not exceed 5 mg if the patient is simultaneously taking ketoconazole or therapeutic doses of other strong CYP3A4 inhibitors (such as ritonavir, nelfinavir. Itraconazole). Concomitant treatment with solifenacin and a potent CYP3A4 inhibitor is contraindicated in patients with severe renal failure or moderate liver failure. Since solifenacin is metabolized by CYP3A4, pharmacokinetic interactions with other CYP3A4 substrates with higher affinity (verapamil, diltiazem) and with CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) are possible.
- Effect of solifenacin on the pharmacokinetics of other drugs
Oral contraceptives: No pharmacokinetic interaction of solifenacin and combined oral contraceptives (ethinyl estradiol \ levonorgestrel) has been identified.
Warfarin: Vesicar administration did not cause changes in the pharmacokinetics of R-warfarin or S-warfarin or their effect on prothrombin time.
digoxin: Vesicar administration did not affect the pharmacokinetics of digoxin.
Overdose of
The highest dose of solifenacin used by volunteers was 100 mg in a single dose. The following side effects were most often observed at this dose: headache (mild), dry mouth (moderate), dizziness (moderate), drowsiness (mild) and blurred vision (moderate). No cases of acute overdose have been reported. In cases of overdose, activated charcoal should be prescribed, gastric lavage should be done, but vomiting should not be caused.
As in cases of overdose of other anticholinergics, the symptoms should be treated as follows: • for severe anticholinergic effects of a central effect (hallucinations, severe irritability) - physostigmine or carbachol
• for seizures or severe excitability - benzodiazepines
• for respiratory failure
• for tachycardia - beta blockers
• for urinary retention - catheterization
• for mydriasis - instill pilocarpine in the eyes and / or place a pain Foot in a dark room.
As in the case of an overdose of other anticholinergic drugs, special attention should be paid to patients with an established risk of lengthening the QT interval (i.e., with hypokalemia, bradycardia and with the simultaneous administration of drugs that cause prolongation of the QT interval) and patients with heart diseases (myocardial ischemia, arrhythmias, congestive heart failure).
Terms and conditions
prescription
dosage form
tablets
Astellas Pharma BV Yurop, Netherlands
Vesikar tablets 10 mg, 30 pcs. (Solyfenatsyn) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Vesikar tablets 10 mg, 30 pcs. - Sale. PayPal accept. Free shipping florida. Fast international shipping.
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