Instructions Tamsin forte prolonged-release tablets 0.4 mg blister No. 30
Composition
active ingredient: tamsulosin hydrochloride;
1 prolonged-release tablet contains tamsulosin hydrochloride 0.4 mg;
Excipients: hypromellose (hydroxypropylmethylcellulose), microcrystalline cellulose, carbomer, colloidal anhydrous silicon dioxide, red iron oxide (E 172), magnesium stearate.
Dosage form
Extended-release tablets.
Main physicochemical properties: white, smooth-surfaced, round, biconvex tablets engraved 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 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 improves urine output.
At the same time, symptoms of obstruction and irritation associated with benign prostatic hyperplasia (difficulty starting urination, weak urine stream, dribbling after urination, feeling of incomplete bladder emptying, frequent urge to urinate at night, urinary urgency) are reduced.
The ability of α1A-adrenergic blockers to reduce blood pressure is associated with a decrease in peripheral resistance. Tamsulosin at a daily dose of 0.4 mg does not cause a clinically significant decrease in systemic blood pressure (BP) in either hypertensive or normotensive patients.
Pharmacokinetics
Absorption: Tamsin Forte is a controlled-release extended-release tablet that provides a sustained and slow release of tamsulosin, giving exposure with little fluctuation over 24 hours.
After oral administration in the fasted state, 57% of tamsulosin is absorbed from the intestine. The rate and extent of absorption of the prolonged-release tablets are not affected by a low-fat meal. The extent of absorption is increased by 64% and 149% (AUC and Cmax, respectively) with a high-fat meal compared to the fasted state.
Tamsulosin exhibits linear pharmacokinetics.
After a single dose of Tamsin Forte on an empty stomach, Cmax of the active substance in the blood plasma is observed after 6 hours. In the equilibrium state, which is achieved on the fourth day of taking the drug, the peak concentration is observed after 4-6 hours, regardless of food intake. The peak concentration in the 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 the maximum concentration regardless of food intake.
Distribution: Plasma protein binding is 99%. The volume of distribution 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 little effect on tamsulosin. Inhibition of the metabolizing enzymes CYP3A4 and CYP2D6 may lead to increased exposure to tamsulosin hydrochloride (see sections “Interaction with other medicinal products and other types of interactions” and “Special instructions for use”). None of the metabolites is more active than the active substance.
Elimination: Tamsulosin and its metabolites are excreted mainly by the kidneys, 4-6% of the dose is excreted unchanged. The half-life of tamsulosin after a single dose and at steady state is 19 and 15 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 of the drug; history of orthostatic hypotension; severe hepatic insufficiency.
Interaction with other medicinal products and other types of interactions
Interaction studies have only been performed in adults.
No drug interactions have been observed with the simultaneous use of tamsulosin hydrochloride with atenolol, enalapril or theophylline. Simultaneous use with cimetidine increases, and with furosemide - decreases, the concentration of tamsulosin in the blood plasma, but since these levels remain within the normal range, there is no need for special dosage adjustment of tamsulosin.
However, diclofenac and warfarin may increase the elimination rate of tamsulosin.
Concomitant use of tamsulosin hydrochloride with strong CYP3A4 inhibitors may lead to increased exposure to tamsulosin hydrochloride. Concomitant use with ketoconazole (a known strong CYP3A4 inhibitor) resulted in an increase in AUC and Cmax to 2.8 and 2.2, 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 AUC and Cmax to 1.6 and 1.3, 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 when using the drug, which can rarely 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 Tamsin Forte, 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) before starting and at regular intervals during treatment should be performed.
The drug should be prescribed with extreme caution to patients with severe renal insufficiency (creatinine clearance <10 ml/min), as clinical studies have not been conducted in such patients.
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 that tamsulosin be discontinued 1-2 weeks before cataract and glaucoma surgery, but the benefit of stopping tamsulosin has not been clearly established. Atonic pupil syndrome has also been reported in patients who have stopped tamsulosin for a long time before cataract surgery.
Tamsulosin hydrochloride is not recommended for 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").
Sometimes you can find tablet residue in the feces.
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
Tamsin Forte 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 and use machines have not been conducted. However, patients should be informed about the possible occurrence of dizziness.
Method of administration and doses
For oral use.
It is recommended to take the tablet daily, regardless of food intake. The tablet should be swallowed whole, without chewing or breaking it, as this will prevent the prolonged release of the active substance.
The duration of treatment is determined individually.
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 is not used to treat children.
The safety and efficacy of tamsulosin in children 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 the event of a sudden decrease in blood pressure due to overdose, supportive therapy should be carried out, aimed at restoring normal cardiovascular function (for example, the patient should be placed in 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 administered. Due to the high degree of binding of tamsulosin to plasma proteins, hemodialysis is unlikely to be appropriate.
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.
Side effects
| Body system | Common (>1/100, <1/10) | Uncommon (>1/1000, <1/100), | Rare (>1/10,000, <1/1,000) | Very rare (<1/10,000) | Frequency not known (cannot be estimated from the 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 | - | - | - |
| From the vascular side | - | Orthostatic hypotension | - | - | - |
| Respiratory-mediastinal disorders | - | Rhinitis | - | Nosebleed* | |
| Gastrointestinal tract | - | Constipation, diarrhea, nausea, vomiting | - | - | Dry mouth* |
| Skin and mucous membrane disorders | - | Rash, itching, hives | Angioedema | Stevens-Johnson syndrome | Erythema multiforme*, exfoliative dermatitis* |
| 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. These cases were reported spontaneously, the frequency of reports and the role of tamsulosin in this case cannot be reliably established.
Expiration date
3 years.
Storage conditions
Keep out of reach of children.
Protect from light and moisture.
Store in the original packaging at a temperature not exceeding 25 ºС in a dry place.
Packaging
10 tablets in a blister; 3 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
Synthon Hispania, SL
Address
C/ Castello, No. 1, Sant Boi de Llobregat, Barcelona, 08830, Spain/
C/ Castelló, n°1, Sant Boi de Llobregat, Barcelona, 08830, Spain.
