Tulosin caps with modified high. 0.4 mg per bl. in pack №10x3

Tulosin caps with modified high. 0.4 mg per bl. in pack №10x3

Name

Tulosin caps with modified high. 0.4 mg per bl. in pack №10x3

Description

Modified-release capsules are hard gelatin, self-closing, with a transparent green body and an opaque green cap; the contents of the capsules are white pellets, odorless or almost odorless.

Main active ingredient

Tamsulosin hydrochloride

Release form

Modified-release capsules are hard gelatin, self-closing, with a transparent green body and an opaque green cap; the contents of the capsules are white pellets, odorless or almost odorless. 1 caps. tamsulosin hydrochloride 400 mcg Excipients: microcrystalline cellulose, copolymer of methacrylic acid with ethyl acrylate (1:1) (in the form of a 30% aqueous dispersion solution), calcium stearate. Pellet shell composition: copolymer of methacrylic acid and ethyl acrylate (1:1) (in the form of a 30% aqueous dispersion solution), talc, triethyl citrate, Tween 80 (polysorbate 80). Composition of the capsule shell: body - indigo carmine, quinoline yellow, gelatin; cap - indigo carmine, quinoline yellow, titanium dioxide, gelatin. 10 pieces. - blisters (1) - cardboard packs. 10 pieces. - blisters (3) - cardboard packs.

Dosage

0.4 mg per bl. in pack №10x3

special instructions

Tamsulosin should be used with caution in patients predisposed to orthostatic hypotension, because and in the case of taking other alpha1-blockers, in some patients blood pressure may decrease during the course of treatment, which sometimes leads to fainting. When the first signs of orthostatic hypotension (dizziness or weakness) appear, the patient should be seated or laid down until the symptoms disappear. Before starting drug therapy, the patient should be examined to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before starting treatment and regularly during therapy, a digital rectal examination and, if required, a prostate specific antigen (PSA) test should be performed. In patients with severe renal failure (SC

pharmachologic effect

Alpha1-adrenergic blocker. Tulosin selectively and competitively blocks postsynaptic β1A-adrenergic receptors located in the smooth muscles of the prostate gland, bladder neck and prostatic urethra, as well as β1D-adrenergic receptors, mainly located in the body of the bladder. This leads to a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra and improved detrusor function. This reduces the symptoms of obstruction and irritation associated with benign prostatic hyperplasia. As a rule, the therapeutic effect develops 2 weeks after starting the drug, although some patients experience a decrease in the severity of symptoms after taking the first dose. Tulosin's ability to act on β1A-adrenergic receptors is 20 times greater than its ability to interact with β1B-adrenergic receptors, which are located in vascular smooth muscles. Due to such high selectivity, the drug does not cause any clinically significant decrease in systemic blood pressure in both patients with arterial hypertension and in patients with normal baseline blood pressure.

Pharmacokinetics

Absorption After oral administration, tamsulosin is quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability of the drug is about 100%. After a single dose of the drug orally, the Cmax of the active substance in plasma is reached after 6 hours. Immediately after a meal, the absorption of tamsulosin decreases. The uniformity of absorption increases if the patient takes the drug every day after the same meal. At steady state (after 5 days of course administration), the Cmax values ​​of the active substance in the blood plasma are 60-70% higher than the Cmax after a single dose of the drug. Distribution Plasma protein binding - 99%. Tamsulosin has a small Vd - approximately 0.2 l/kg. Metabolism Tamsulosin practically does not undergo the “first pass” effect and is slowly biotransformed in the liver with the formation of pharmacologically active metabolites that retain high selectivity for β1A-adrenergic receptors. None of the metabolites are more active than the parent substance. Most of the active substance is present in the blood unchanged. Excretion Tamsulosin and its metabolites are primarily excreted by the kidneys, with approximately 9% of the dose excreted unchanged. T1/2 of tamsulosin with a single dose is 10 hours, after multiple doses is 13 hours, final T1/2 is 22 hours. Pharmacokinetics in special clinical cases In case of liver failure, dose clarification is not required. If renal function is impaired, the dose of the drug does not need to be specified.

Indications for use

- treatment of functional symptoms of benign prostatic hyperplasia.

Directions for use and doses

Tulosin is taken orally at a dose of 400 mcg (1 capsule/day). Capsules are taken after the first meal with a sufficient amount of water. The capsule should not be broken or chewed.

Use during pregnancy and lactation

Tulosin is for men only.

Precautionary measures

Use with caution in severe liver failure. Should be used with caution in chronic renal failure (creatinine clearance less than 10 ml/min).

Interaction with other drugs

The simultaneous use of cimetidine increases the concentration of tamsulosin in the blood plasma, furosemide reduces its concentration in the blood plasma. However, in both cases, the tamsulosin content remains within the therapeutically active concentration range and no dose adjustment is required. Diclofenac and indirect anticoagulants slightly increase the rate of elimination of tamsulosin. Concomitant use of tamsulosin with other alpha1-blockers and other drugs that lower blood pressure can lead to a pronounced increase in the hypotensive effect. No interaction was found with simultaneous use of tamsulosin with atenolol, enalapril, nifedipine or theophylline. Plasma tamsulosin concentrations did not change in the presence of diazepam, trichlormethiazide, amitriptyline, diclofenac, glibenclamide, simvastatin or warfarin. Tamsulosin did not change the concentrations of diazepam, propranolol, trichlormethiazide and chlormadinone.

Contraindications

- hypersensitivity to the components of the drug. Use with caution in chronic renal failure (CR

Compound

1 caps. tamsulosin hydrochloride 400 mcg Excipients: microcrystalline cellulose, copolymer of methacrylic acid with ethyl acrylate (1:1) (in the form of a 30% aqueous dispersion solution), calcium stearate. Pellet shell composition: copolymer of methacrylic acid and ethyl acrylate (1:1) (in the form of a 30% aqueous dispersion solution), talc, triethyl citrate, Tween 80 (polysorbate 80). Composition of the capsule shell: body - indigo carmine, quinoline yellow, gelatin; cap - indigo carmine, quinoline yellow, titanium dioxide, gelatin. 10 pieces. - blisters (1) - cardboard packs. 10 pieces. - blisters (3) - cardboard packs.

Overdose

Cases of acute overdose have not been described. Symptoms: acute arterial hypotension is theoretically possible. Treatment: the patient should be laid down to restore blood pressure and normalize heart rate. Cardiotropic therapy is carried out. Renal function should be monitored and general supportive care should be used. If symptoms persist, volume replacement solutions or vasoconstrictors should be administered. To prevent further absorption of tamsulosin, gastric lavage, activated charcoal or an osmotic laxative may be taken. Dialysis is not effective because tamsulosin binds tightly to plasma proteins.

Side effect

From the side of the central nervous system: 1-10% - dizziness, drowsiness or insomnia; 0.1-1% - headache. From the digestive system: 0.1-1% - nausea, vomiting, diarrhea or constipation. From the reproductive system: 0.1-1% - retrograde ejaculation, decreased libido;

Storage conditions

The drug should be stored out of the reach of children at a temperature below 25°C.

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Price for Tulosin capsules with modified high. 0.4 mg per bl. in pack №10x3

Instructions for use for Tulosin caps with modified high. 0.4 mg per bl. in pack №10x3

Benign prostatic hyperplasia (BPH) is the most common disease in older men. According to autopsy studies, the first signs of BPH are found in 8% of men aged 31 to 40 years [1]. In men over 61 years of age, the incidence of this disease reaches 70% or more, and after 80 years of age - 90% [2]. Considering the trend of the aging population of the planet, we can assume an increasing relevance of the problem of diagnosing and treating BPH.

If twenty years ago there was practically no real alternative to surgical treatment of BPH, today there is a whole range of different conservative methods. Among them, drug therapy for BPH is one of the most dynamically developing areas of urology [3, 4, 5].

α1-adrenergic receptor blockers (α1-AR) have become standard drugs in the treatment of BPH [6, 7, 8, 9]. Recent studies have proven the leading role of α1-AR in the pathogenesis of the disease. Their stimulation increases the tone of the smooth muscle elements of the bladder neck, prostatic urethra and prostate, largely maintaining intraurethral pressure [10]. The contractile function of the prostate is also under the control of α1-AR, which are localized mainly in the stromal elements of the gland, occupying up to 60% of the organ’s volume. The effects of α1-AR activation, as well as an increase in their number and density in prostate tissue in BPH, lead to the development of a dynamic component of bladder outlet obstruction [11]. As BPH progresses, functional and morphological changes in the detrusor develop, accompanied by hypoxia of smooth muscle elements and leading to disturbances in biochemical processes (including energy balance) in the detrusor cells [4].

Based on this, α1-AR blockers should not only reduce urethral resistance by reducing the tone of the smooth muscles of the prostate and urethra, but also eliminate secondary changes in the detrusor as a result of improving blood supply to the bladder, thus influencing the elimination of the dynamic component of bladder outlet obstruction.

Currently, the most widely used in the treatment of BPH are the so-called selective α-blockers that act on subtype 1 α-AR: tamsulosin, alfuzosin, terazosin, doxazosin. They selectively block postsynaptic α1A adrenergic receptors of the smooth muscles of the prostate gland, bladder neck and prostatic urethra. This type of receptor, accounting for 70% of all α-ARs, is localized primarily in the prostate [10]. Perhaps it is these receptors that play the greatest role in the development of the dynamic component of bladder outlet obstruction.

The effectiveness of selective α-blockers in eliminating obstructive and especially irritative symptoms is approximately the same, while the severity of side effects due to lowering blood pressure (orthostatic hypotension, drowsiness, dizziness, palpitations and tachycardia) is different [12, 13]. Tamsulosin has a 20-fold greater ability to block alpha1A-adrenergic receptors than its effect on alpha-adrenergic receptors in vascular smooth muscle. Clinically, this is manifested by its negligible effect on systemic blood pressure.

The effective and safe use of tamsulosin in patients with prostatic hyperplasia has been proven by numerous studies [14-18]. It has been reliably demonstrated that tamsulosin, compared with placebo, significantly reduces the severity of symptoms, as well as urinary disorders caused by prostate hyperplasia. In addition, these studies showed that the use of tamsulosin is safe and is accompanied by a small number of adverse reactions [19-22]. At the same time, the accumulation of additional clinical experience with the use of tamsulosin makes it possible to further evaluate the value of this drug in the treatment of patients with prostate hyperplasia.

In Russia, the α1-blocker drug Tulosin has been registered and approved for use, which, according to publications, is the most prescribed drug. Tulosin is bioequivalent to the original drug tamsulosin and is a pharmaceutical generic (Hungary).

Purpose of the study: to determine the effectiveness and safety of Tulosin in patients with BPH.

MATERIALS AND METHODS

A post-registration study of the pharmaceutical drug Tulosin was carried out at the Urological Clinic of Kazan State Medical University from April to November 2009.

The effectiveness of the drug was assessed:

1. based on an analysis of changes in urination parameters using the international IPSS and quality of life system;
2. based on changes in urodynamic parameters: maximum urine flow rate and average urination rate;
3. based on the determination of residual urine;
4. based on ultrasound data of the prostate gland.

The study group included 30 patients aged 50 to 82 years, meeting the following criteria:

• confirmed diagnosis of BPH, established in a urological hospital;
• the severity of symptoms on the IPSS scale is more than 9 points (moderate symptoms);
• the volume of residual urine is not more than 100 ml;
• patients who have not previously taken medications for the treatment of BPH.

Exclusion criteria were:

• complicated course of BPH;
• urinary tract infection;
• oncological diseases;
• concomitant somatic diseases (severe cardiovascular and cerebrovascular diseases);
• renal and liver failure.

Patients were observed in three stages. At the first stage, patients were selected with mandatory written consent to participate in the study and compliance with the doctor’s recommendations. The patient was given the drug with a regimen of 1 capsule (0.4 mg) per day after the first meal. Treatment was carried out for 2 months, with mandatory monitoring of the patients' condition every month (second and third stages). At the control stages, changes in the symptoms of the disease were clarified (IPSS and Qol questionnaire); laboratory tests, including blood tests and determination of creatinine levels. An ultrasound examination of the prostate gland was performed to determine its volume and the volume of residual urine, the rate of urination was determined, and side effects, if any, were determined.

The safety of the drug was assessed by recording and analyzing adverse events, as well as determining a general blood test over time and determining biochemical blood parameters.

RESEARCH RESULTS

Based on the examination data, it turned out that the main complaints of patients before the start of treatment were frequent urination at night 2-4 times, a sluggish stream of urine. Digital rectal examination revealed an enlarged prostate gland with signs characteristic of benign hyperplasia. The average size of the enlarged prostate gland is determined by ultrasound data. The initial parameters of the main criteria are presented in Table 1.

Table 1. Average values ​​of initial indicators (stage 1)

Table 2. Dynamics of prostate volume according to TRUS data

The study group consisted of patients who had not previously received drug therapy. The mean serum PSA value was 1.5 ± 1.1 ng/ml.

Data from transrectal ultrasound (TRUS) of the prostate are one of the criteria for the degree of effectiveness of the drug used to assess the therapeutic effect in patients with benign prostatic hyperplasia. For ease of comparison of the results obtained, the prostate volume indicator is highlighted. Table 2 shows the dynamics of changes in prostate volume during treatment.

Laboratory blood tests were without pathological changes. In 8 out of 30 patients, no residual urine was noted, despite an enlarged prostate gland and the presence of other symptoms. BPH stage I was determined in 24 patients, stage II in 6 patients, for whom, for various reasons, surgical treatment could not yet be performed, or they refused surgery.

As follows from Table 2, while taking tamsulosin, a slight decrease in prostate volume was noted after one and two months of observation. However, these changes turned out to be unreliable.

When determining the amount of residual urine during treatment, we found that Tulosin helps reduce the amount of residual urine, and significant changes were noted within a month after taking the drug (stage 2). Patients noted an improvement in the quality of urination, a decrease in nocturnal pollakiuria, and a feeling of satisfaction after urination (Figure 1).

Figure 1. Dynamics of changes in residual urine volume.

Objective criteria for the effectiveness of Tulosin in patients with BPH should be considered indicators of urodynamic studies of the lower urinary tract: maximum and average urinary flow rate. The studies were conducted on Toshiba Satellite A 10-131 Delphis UDS 9.4-W equipment from Laborie Medical Technologies before the drug was prescribed, after a month and after two months of treatment.

During a two-month observation of patients in the selected group, a significant improvement in urodynamic parameters was established (Figure 2). Thus, uroflowmetry indicators performed at the second and third visits significantly increased compared to the baseline.

Figure 2. Changes in urodynamic parameters

The dynamics of obstructive and irritative symptoms were assessed using the international system for assessing prostate diseases IPSS Qol, with quality of life determined at each visit. Baseline IPSS scores averaged 17.67 ± 5.2, which corresponds to moderate symptoms. It was found that after treatment with Tulosin, patients noted an improvement in symptoms within a month. In 7 patients, nocturnal pollakiuria disappeared. The number of patients with minor symptoms increased consistently over two months.

29 out of 30 patients at the second stage noted a significant reduction in symptoms, improvement in condition and quality of life (Table 3, Figure 3). In one patient, the IPSS scores did not change and remained at the level of the first visit, although the amount of residual urine in him decreased from 100 ml to 47 ml after two months, and when assessing the quality of life, the patient classified it as mixed feelings.

Figure 3. Dynamics of average IPSS values.

Most patients showed a significant decrease in the average value of quality of life assessment from the first visit to the third, which indicates the effectiveness of treatment (Figure 4).

Figure 4. Dynamics of quality of life (QOL) indicators.

After two months of treatment, the number of patients who assessed their condition as good increased to 11 patients, and satisfactory in 18 patients (Figure 5).

Figure 5. Treatment results

Thus, the treatment was effective in 29 patients, which was 96.6%.

During the clinical trial, no patient dropped out of the study group due to adverse events. One patient developed diarrhea 10 days after the start of treatment. This turned out to be unrelated to the study drug, so treatment was continued.

Side effects such as hypertension, dizziness, nausea, which sometimes occur when taking drugs from the α1-blocker group, were not observed in our study. No changes in blood parameters were noted. During the observation period, no deterioration in blood biochemical parameters was noted. Creatinine and liver tests were within normal limits.

Table 3. Change in symptoms (IPSS) in patients with BPH

CONCLUSION

Thus, a clinical study conducted to study the effectiveness and safety of the pharmaceutical drug Tulosin as monotherapy in patients with BPH allows us to conclude that during the therapy there was a decrease in bladder outlet obstruction, which is confirmed by an increase in urination rate and a decrease in the amount of residual urine. In addition, the severity of BPH symptoms decreased, as evidenced by the obtained questionnaire data on the International IPSS Prostatic Symptoms Scale and an improvement in the quality of life of patients.

No adverse events were identified while taking the drug. After completion of the clinical studies, 29 patients continued treatment with Tulosin. Only one patient was operated on; he underwent transvesical adenomectomy.

The drug Tulosin has a high level of effectiveness and safety and can be recommended for the treatment of patients with benign prostatic hyperplasia, manifested by severe irritative symptoms with moderate bladder outlet obstruction. P

Key words: benign prostatic hyperplasia, drug treatment, alpha blockers, Tulosin.

Keywords: benign prostatic hyperplasia, drug treatment, a-blockers, Tulosin.

LITERATURE

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2. Shabad A.L. Textbook on urology: Textbook. 3rd ed., revised and expanded. M. Medicine, 1990.
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4. Laurent O.B., Vishnevsky E.L. Treatment of urinary disorders in patients with benign prostatic hyperplasia with α-blockers. M. 1998.
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6. Vinarov A.3. Drug treatment of patients with prostatic hyperplasia: Dis. Dr. med. Sci. M. 1999.
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8. Kirby R., Andersson KE, Lepor H., Steers WD Alpha (l)-adrenoceptor selectivity and the treatment of benign prostatic hyperplasia and lower urinary tract symptoms //Prostate Cancer. 2000. No. 3. P. 76-83.
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14. Schalken JA Molecular and cellular prostate biology: origin of prostatespecific antigen expression and implications for benign prostatic hyperplasia // BJU Int. 2004. Vol.93. Suppl 1. P. 5-9.
15. Ren RM, Kou M., Lan XX Efficacy and safety of tamsulosin for the treatment of benign prostatic hyperplasia: a meta analysis // Chin Med J. 2010. Vol. 123. No. 2. P. 234-238.
16. Michel MC The forefront for novel therapeutic agents based on the pathophysiology of lower urinary tract dysfunction: alpha-blockers in the treatment of male voiding dysfunction how do they work and why do they differ in tolerability? //J. Pharmacol Sci. 2010. Vol.112. No. 2. P. 151-157. Epub 2010 Feb 4.
17. Roehrborn CG Efficacy of alpha-Adrenergic Receptor Blockers in the Treatment of Male Lower Urinary Tract Symptoms // Rev Urol. 2009. Fall.11. Suppl 1. P. 1-8.
18. Nickel JC, Sander S., Moon TD A meta-analysis of the vascular-related safety profile and efficacy of alpha-adrenergic blockers for symptoms related to benign prostatic hyperplasia //Int J Clin Pract. 2008. Vol.62. No. 10. P. 1547-1559.
19. Dong Z., Wang Z., Yang K., Liu Y., Gao W., Chen W. Tamsulosin versus terazosin for benign prostatic hyperplasia: a systematic review // Syst Biol Reprod Med. 2009. Vol.55. No. 4. P. 129-136.
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