Instructions for Prostazan-Vista prolonged-release tablets 0.4 mg No. 30
Composition
active ingredient: tamsulosin hydrochloride;
1 prolonged-release tablet contains 0.4 mg of tamsulosin hydrochloride;
Excipients: hypromellose, microcrystalline cellulose, carbomer, colloidal anhydrous silicon dioxide, red iron oxide (E 172), magnesium stearate.
Dosage form
Extended-release tablets.
Main physicochemical properties: white, without a break line, round tablets embossed with “T9SL” on one side and “0.4” on the other side.
Pharmacotherapeutic group
Drugs used in benign prostatic hyperplasia. α1-adrenergic receptor antagonists. ATC code G04C A02.
Pharmacological properties
Pharmacodynamics.
Tamsulosin hydrochloride selectively and competitively blocks postsynaptic α1-adrenoceptors, in particular α1A and α1D, located in the smooth muscles of the prostate gland, bladder neck and prostatic urethra. This helps to reduce the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra and improve urine output. At the same time, the symptoms of obstruction and irritation associated with benign prostatic hyperplasia (difficulty starting urination, weakening of the urine stream, dribbling after urination, feeling of incomplete bladder emptying, frequent urination, urge to urinate at night, urgency to urinate) are reduced.
The ability of α1A-adrenergic blockers to reduce blood pressure is associated with a decrease in peripheral resistance. Prostazan-Vista in a daily dose of 0.4 mg does not cause a clinically significant decrease in systemic blood pressure (BP) in both patients with arterial hypertension and patients with normal initial blood pressure. Pharmacokinetics.
Absorption. Prostazan-Vista is a prolonged-release tablet that provides a prolonged and slow release of tamsulosin, giving exposure with slight fluctuations over 24 hours. After oral administration on an empty stomach, 57% of tamsulosin is absorbed in the intestine.
The rate and extent of absorption of the prolonged-release tablets are not altered by the administration of a low-fat meal. The extent of absorption is increased by 64% and 149% (area under the pharmacokinetic concentration-time curve (AUC) and maximum plasma concentration (Cmax), respectively) with a high-fat meal compared to administration in the fasted state.
Tamsulosin exhibits linear pharmacokinetics.
After a single dose of Prostazan-Vista on an empty stomach, Cmax of the active substance is observed after 6 hours. In the equilibrium state, which is achieved on the 4th day of tamsulosin administration, Cmax is observed after 4-6 hours regardless of food intake. The peak concentration in blood plasma increases from approximately 6 ng/ml after the first dose to 11 ng/ml in the equilibrium state.
As a result of the prolonged release, the lowest plasma concentration of tamsulosin is 40% of Cmax, regardless of food intake.
Distribution: Plasma protein binding is 99%. The volume of distribution of tamsulosin is small (approximately 0.2 l/kg).
Metabolism. Tamsulosin hydrochloride has a low first-pass effect, being slowly metabolized. Most of the active substance is present in the blood in unchanged form. It is metabolized in the liver. In vitro results show that CYP3A4 and also CYP2D6 are involved in the metabolism, other CYP isoenzymes have a negligible effect on tamsulosin. Inhibition of the metabolic enzymes CYP3A4 and CYP2D6 may lead to increased exposure to tamsulosin hydrochloride (see sections "Interaction with other medicinal products and other types of interactions", "Special instructions for use"). None of the metabolites is more active than the active substance.
Elimination: Tamsulosin and its metabolites are excreted primarily by the kidneys, with 4-6% of the dose excreted unchanged. The half-life of tamsulosin after a single dose and at steady state is 19 and 15 hours, respectively.
Indication
Treatment of lower urinary tract symptoms in benign prostatic hyperplasia.
Contraindication
Hypersensitivity to tamsulosin hydrochloride, including drug-induced angioedema, or to any of the excipients; history of orthostatic hypotension; severe hepatic impairment.
Interaction with other medicinal products and other types of interactions
Interaction studies were conducted only in adults.
No drug interactions have been observed when tamsulosin hydrochloride is used concomitantly with atenolol, enalapril, nifedipine or theophylline. Concomitant use with cimetidine increases and furosemide decreases the plasma concentration of tamsulosin, but since these levels remain within the normal range, no special dosage adjustment of tamsulosin is required.
However, diclofenac and warfarin may increase the elimination rate of tamsulosin. Concomitant use of strong CYP3A4 inhibitors may lead to increased exposure to tamsulosin hydrochloride. Concomitant use with ketoconazole (a strong CYP3A4 inhibitor) resulted in an increase in AUC and Cmax of approximately 2.8 and 2.2 times, respectively. Tamsulosin hydrochloride should not be administered in combination with strong CYP3A4 inhibitors in patients with poor CYP2D6 metabolism.
Tamsulosin hydrochloride should be used with caution in combination with strong and moderate CYP3A4 inhibitors.
Concomitant use of tamsulosin hydrochloride and paroxetine (a strong CYP2D6 inhibitor) resulted in an increase in Cmax and AUC by almost 1.3 and 1.6 times, respectively, but this is not clinically significant.
Concomitant use with other α1-adrenergic blockers may enhance the hypotensive effect.
Application features
As with other α1-adrenergic blockers, in rare cases, tamsulosin may cause a decrease in blood pressure, which can suddenly lead to loss of consciousness. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit down or take a horizontal position until the above symptoms disappear.
Before starting the use of the drug Prostazan-Vista, a medical examination should be performed to identify other concomitant diseases that may cause the same symptoms as benign prostatic hyperplasia. Before starting treatment, a rectal examination of the prostate gland should be performed and, if necessary, a test to determine the level of prostate-specific antigen (PSA) before starting and at equal intervals during treatment. The drug should be prescribed with special caution to patients with severe renal insufficiency (creatinine clearance < 10 ml/min), since clinical studies in such patients have not been conducted.
Some patients who have taken or are taking tamsulosin have experienced atonic pupil syndrome (IFIS, a variant of pinhole pupil syndrome) during cataract and glaucoma surgery, which may lead to an increased number of complications during or after such surgery.
It is generally recommended to discontinue tamsulosin 1–2 weeks before cataract and glaucoma surgery, but the benefit of stopping tamsulosin has not yet been clearly established. Atonic pupil syndrome has also been reported in patients who have discontinued tamsulosin for a long period before cataract surgery. Patients are not recommended to start tamsulosin hydrochloride before elective cataract or glaucoma surgery. In preparation for surgery, surgeons and ophthalmologists should inquire whether the patient has taken (or is taking) tamsulosin in order to prevent possible complications associated with IFIS.
Tamsulosin hydrochloride should not be administered in combination with strong CYP3A4 inhibitors in patients with poor CYP2D6 metabolism.
Tamsulosin hydrochloride should be used with caution in combination with strong and moderate CYP3A4 inhibitors (see Interactions with other medicinal products and other forms of interaction).
Sometimes tablet residues are found in feces.
Cases of allergic reactions to tamsulosin hydrochloride have been reported in patients with a history of allergy to sulfonamides. Caution should be exercised when administering tamsulosin hydrochloride to patients with a history of allergy to sulfonamides.
Use during pregnancy or breastfeeding
Prostazan-Vista is not indicated for use in women.
Fertility.
Ejaculation disorders have been reported in short- and long-term clinical trials with tamsulosin. Cases of ejaculation disorders, retrograde ejaculation and insufficient ejaculation have been reported in the post-marketing period.
Ability to influence reaction speed when driving vehicles or other mechanisms
Studies on the effects of tamsulosin on the ability to drive and use machines have not been conducted. However, patients should be warned about the possibility of drowsiness, blurred vision, dizziness and fainting.
Method of administration and doses
The recommended dose is 1 tablet daily, regardless of food intake. The tablet should be swallowed whole, without breaking or chewing it, as this will interfere with the long-term and controlled release of the active ingredient. The duration of treatment is determined individually.
Patients with renal insufficiency and patients with mild to moderate hepatic insufficiency do not require dose adjustment (see section "Contraindications").
Children.
The medicine should not be used in children.
The safety and efficacy of tamsulosin in children have not been evaluated.
Overdose
Symptoms. Overdose of tamsulosin hydrochloride can cause severe hypotension. A strong hypotensive effect has been observed with varying degrees of overdose. Treatment. In the event of a sharp decrease in blood pressure due to overdose, supportive therapy should be carried out aimed at restoring normal cardiovascular function (for example, the patient should take a horizontal position). If this measure is ineffective, infusion therapy and vasopressors should be administered. Renal function should be monitored and general supportive therapy should be carried out. Due to the high degree of binding of tamsulosin to plasma proteins, hemodialysis is unlikely to be advisable.
In order to stop further absorption of tamsulosin, vomiting can be induced artificially. In case of overdose with a significant amount of tamsulosin, the patient should be washed with activated charcoal and low-osmotic laxatives, such as sodium sulfate.
Side effects
All adverse reactions are listed by system organ class and frequency: very common (≥ 1/10), common (≥ 1/100 - < 1/10), uncommon (≥ 1/1000 - < 1/100), rare (≥ 1/10000 - < 1/1000), very rare (< 1/10000), frequency unknown (cannot be estimated from the available data).
| Organ systems | Often | Infrequently | Rarely | Very rare | Frequency unknown |
| From the nervous system | Dizziness (1.3%) | Headache | Fainting (syncope). | | |
| From the organs of vision | | | | | Blurred vision*, visual impairment* |
| Cardiovascular system | | Feeling your heart beating (palpitations) Orthostatic hypotension | | | |
| Respiratory, thoracic and mediastinal disorders | | Rhinitis | | | Nosebleed* |
| Gastrointestinal tract | | Constipation, diarrhea, nausea, vomiting | | | Dry mouth* |
| Skin and subcutaneous tissue disorders | | Rash, itching, hives | Angioedema | Stevens-Johnson syndrome | Erythema multiforme*, exfoliative dermatitis*, photosensitivity reactions* |
| Reproductive system and mammary gland function | Ejaculation disorders, including retrograde ejaculation and ejaculatory failure | | | Priapism | |
| General disorders and administration site conditions | | Asthenia | | | |
* Observed in the post-registration period.
Post-marketing experience: Cases of intraoperative iris instability (pinched pupil syndrome) during cataract and glaucoma surgery have been described in patients taking tamsulosin (see section "Special warnings and precautions for use"). In addition to the above adverse reactions, cases of atrial fibrillation, arrhythmia, tachycardia and dyspnea have been reported. As with other alpha-blockers, drowsiness, dry mouth, and edema may occur. These adverse reactions have been reported spontaneously - the frequency and role of tamsulosin in this case cannot be reliably established.
Reporting of suspected adverse reactions.
Reporting adverse reactions after registration of a medicinal product is of great importance. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of a medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua
Expiration date
3 years.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
10 tablets in a blister, 3 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
Sinton Hispania, S.L.
Location of the manufacturer and its business address.
Calle C/Castello, no. 1, Sant Boi de Llobregat, Barcelona, 08830, Spain.
