Instructions for use Fokusin modified-release hard capsules 0.4 mg blister No. 90
Composition
active ingredient: tamsulosin;
1 capsule contains tamsulosin hydrochloride 0.4 mg;
excipients: methacrylate copolymer dispersion, microcrystalline cellulose, dibutyl sebacate, polysorbate 80, colloidal silicon dioxide, calcium stearate;
capsule composition: gelatin, red iron oxide (E 172), yellow iron oxide (E 172), titanium dioxide (E 171), black iron oxide (E 172), indigo carmine (E 132).
Dosage form
Modified-release hard capsules.
Main physicochemical properties: hard gelatin capsules size No. 3 with olive cap and orange body. Capsule contents: white or almost white pellets.
Pharmacotherapeutic group
Drugs used in benign prostatic hypertrophy. α1-adrenergic receptor antagonists. ATC code G04C A02.
Pharmacological properties
Pharmacodynamics
Tamsulosin 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 leads to a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra and an improvement in 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, a feeling of incomplete bladder emptying, frequent urination, urge to urinate at night, urgency to urinate) are reduced.
These effects persist for a long time with long-term treatment and significantly discourage surgery or catheterization.
Alpha-1 adrenoceptor antagonists have the ability to lower blood pressure by reducing peripheral vascular tone. No clinically significant reduction in blood pressure was observed during drug testing.
Pharmacokinetics
Absorption: Tamsulosin is well absorbed from the gastrointestinal tract, and its bioavailability is almost 100%. Absorption of tamsulosin occurs somewhat more slowly after food intake. Uniform absorption is achieved when the patient takes the drug at the same time after a meal. The pharmacokinetics of tamsulosin are linear.
After taking a single dose of the drug after a meal, the peak concentration of tamsulosin in the blood plasma is reached after about 6 hours, and a stable concentration is formed on the fifth day after daily administration of the drug. Cmax is approximately two-thirds higher than that formed after taking a single dose.
Distribution: In men, tamsulosin is approximately 99% bound to plasma proteins. The volume of distribution of the drug is small (approximately 0.2 l/kg).
Metabolism: Tamsulosin hydrochloride is not subject to the first-pass effect and is slowly metabolized in the liver to form pharmacologically active metabolites that retain high selectivity for α1-adrenoceptors. Most of the active substance is present in the blood in unchanged form.
Elimination: Tamsulosin and its metabolites are excreted mainly in the urine. Approximately 9% of the dose remains as unchanged active substance.
After a single dose of the drug after a meal and at steady-state plasma concentrations, the half-lives are approximately 10 and 13 hours, respectively.
Indication
Treatment of functional disorders of the lower urinary tract 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
Interactions have only been studied 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.
In in vitro studies, diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin did not affect the free fraction of tamsulosin in human plasma. Similarly, tamsulosin did not change the free fractions of diazepam, propranolol, trichlormethiazide and chlormadinone in human plasma.
However, diclofenac and warfarin may increase the elimination rate of tamsulosin.
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) leads to an increase in Cmax and AUC to 1.3 and 1.6, 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 some cases, a decrease in blood pressure may occur during the use of the drug, which can sometimes 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 treatment with the drug, 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 and, if necessary, a test to determine the level of prostate-specific antigen (PSA) should be performed before starting and at regular intervals during treatment.
The drug should be prescribed with extreme caution to patients with severe renal insufficiency (creatinine clearance <10 ml/min), as clinical studies with tamsulosin have not been conducted in such patients.
Rare cases of angioedema have been reported following the use of tamsulosin. If angioedema occurs, the drug should be discontinued immediately and the patient monitored until the edema resolves. Re-administration of tamsulosin is not recommended.
Some patients who have taken or are taking tamsulosin have experienced intraoperative atonic iris syndrome (IFIS, a variant of pinhole syndrome) during cataract and glaucoma surgery, which may increase the risk of complications during or after such surgery.
It is generally recommended that tamsulosin be discontinued 1-2 weeks before cataract and glaucoma surgery, but the benefit of discontinuing tamsulosin has not been clearly established. Atonic pupil syndrome has also been reported in patients who have discontinued tamsulosin for a long period prior to cataract surgery.
Initiation of tamsulosin hydrochloride is not recommended in patients undergoing 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 section "Interaction with other medicinal products and other types of interactions").
Cases of allergic reactions to tamsulosin 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
The drug 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 effect of the drug on the ability to drive or use machines have not been conducted. However, patients should be warned about the possibility of dizziness.
Method of administration and doses
The recommended dose for adults is 1 capsule daily, after breakfast or after the first meal. The capsule should be swallowed whole, do not break or chew, as this will prevent the modified release of the active ingredient.
No dose adjustment is required in patients with renal impairment. No dose adjustment is required in patients with mild to moderate hepatic impairment (see also section "Contraindications").
Children
The drug should not be used in children.
The safety and efficacy of tamsulosin in children under 18 years of age have not been evaluated.
Overdose
Symptoms.
Overdose with tamsulosin hydrochloride can potentially cause severe hypotensive effects. Severe hypotensive effects have been observed with varying degrees of overdose.
In case 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 should be carried out and vasopressors should be prescribed. It is necessary to monitor renal function and carry out general supportive therapy. 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 the drug, vomiting can be induced artificially. In case of overdose of a significant amount of the drug, the patient should be washed with activated charcoal and low-osmotic laxatives, such as sodium sulfate.
Adverse reactions
| Body system | Common (>1/100, <1/10) | Uncommon (>1/1000, <1/100), | Rare (>1/10,000, <1/1,000) | Very rare (<1/10,000) | Unknown (cannot be estimated from available data) |
| Neurological disorders | Dizziness (1.3%) | Headache | Faint | - | - |
| From the organs of vision | - | - | - | - | Blurred vision*, visual impairment* |
| From the heart | - | Feeling of heart palpitations | - | - | - |
| Vascular disorders | - | Orthostatic hypotension | - | - | - |
| Respiratory-mediastinal disorders | - | Rhinitis | - | - | Nosebleed* |
| Gastrointestinal tract | - | Constipation, diarrhea, nausea, vomiting | - | - | Dry mouth* |
| Skin and mucous membranes | - | Rash, itching, hives | Angioedema | Stevens-Johnson syndrome | Erythema multiforme*, exfoliative dermatitis*, photosensitivity reaction* |
| Reproductive disorders | Ejaculation disorders, including retrograde ejaculation and ejaculatory failure | - | - | Priapism | - |
| General disorders | Asthenia | - | - | - | |
*- were noted in the post-registration period.
During post-marketing surveillance, 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").
Post-marketing experience: In addition to the above adverse reactions, cases of atrial fibrillation, arrhythmia, tachycardia and dyspnoea have been reported. As these cases were reported spontaneously, the frequency of reporting and the role of tamsulosin in this case cannot be reliably established.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after a medicinal product has been authorised by the regulatory authorities is an important procedure. It allows the continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report all suspected adverse reactions via national adverse reaction reporting systems.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
No. 90 (10x9): 10 capsules in a blister; 9 blisters in a cardboard box.
No. 90 (15x6): 15 capsules in a blister; 6 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
CC "Zentiva S.A."
Location of the manufacturer and address of its place of business
B-r. Teodor Pallady, 50, district 3, Bucharest, zip code 032266, Romania.
