Instructions for Urimac prolonged-release hard capsules 0.4 mg blister No. 30
Composition
active ingredient: tamsulosin hydrochloride;
1 capsule contains tamsulosin hydrochloride 0.4 mg;
excipients: polysorbate 80, triacetin, methacrylate copolymer dispersion, sodium lauryl sulfate, microcrystalline cellulose, calcium stearate, gelatin capsule: gelatin, indigo carmine (E 132), black iron oxide (E 172), red iron oxide (E 172), yellow iron oxide (E 172), titanium dioxide (E 171), sodium lauryl sulfate.
Dosage form
The extended-release capsules are hard.
Main physicochemical properties: hard gelatin capsules No. 2 with an opaque brown-green cap and an opaque orange body, with the inscriptions: “CL 23” on the cap and “0.4” on the capsule body, containing free-flowing spherical granules from white to almost white.
Pharmacotherapeutic group
Drugs used in urology. Drugs used in benign prostatic hyperplasia. Alpha1-adrenergic receptor antagonists.
ATX code G04C A02.
Pharmacological properties
Pharmacodynamics.
Tamsulosin hydrochloride selectively and competitively blocks postsynaptic
α1-adrenergic receptors, in particular α1A and α1D, located in the smooth muscles of the prostate gland, bladder neck and prostatic urethra. This reduces 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 are reduced (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).
As a rule, the therapeutic effect develops 2 weeks after the start of taking the drug. These effects persist for a long time during long-term treatment and significantly reduce the need for 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 in trials of tamsulosin hydrochloride.
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. Absorption uniformity is achieved when the patient takes tamsulosin hydrochloride at the same time after a meal. The pharmacokinetics of tamsulosin are linear.
After a single dose of tamsulosin hydrochloride taken after a meal, peak plasma concentrations of tamsulosin are reached approximately 6 hours later, and steady-state concentrations are reached by the 5th day after daily dosing. The maximum concentration is approximately two-thirds higher than that achieved after a single dose.
Distribution: In men, tamsulosin is approximately 99% bound to plasma proteins. The volume of distribution 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 tamsulosin hydrochloride after food and at steady state, 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
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.
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 maximum concentration (Cmax) and area under the concentration-time curve (AUC) of 2.2 and 2.8, respectively.
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.
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 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 take a horizontal position until the above symptoms disappear.
Before starting treatment with the drug, you should undergo a medical examination 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. If necessary, a test to determine the level of prostate-specific antigen (PSA) is also 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 hydrochloride have not been conducted in such patients.
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").
Some patients taking tamsulosin have experienced atonic pupil syndrome (IFIS, a variant of pinhole pupil syndrome) during cataract and glaucoma surgery, which may increase the number of complications during such surgery.
As a rule, it is recommended to stop tamsulosin treatment 1-2 weeks before cataract and glaucoma surgery. However, the appropriateness and timing of stopping tamsulosin treatment have not yet been clearly established.
Atonic pupil syndrome has also been reported in patients who discontinued tamsulosin for a long period prior to cataract surgery.
Patients undergoing elective cataract or glaucoma surgery should not be started on tamsulosin hydrochloride. In preparation for surgery, ophthalmic surgeons 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 should be used with caution in combination with strong and moderate CYP3A4 inhibitors.
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 to patients with a history of allergy to sulfonamides.
Use during pregnancy or breastfeeding
The drug should not be used by 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 and fainting.
Method of administration and doses
The recommended dose for adults is 1 capsule daily, after breakfast; the capsule should be swallowed whole, not chewed, as this will prevent the modified release of the active ingredient, washed down with milk or water (approximately 150 ml), standing or sitting.
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 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. To normalize blood pressure and heart rate, the patient should be placed in a horizontal position. If this measure does not help, it is recommended to use plasma substitutes and, if necessary, vasoconstrictor drugs. Kidney function should be monitored and supportive therapy should be carried out. Hemodialysis is unlikely to be advisable, since tamsulosin is highly bound to plasma proteins.
Measures to prevent absorption, such as inducing vomiting, may be helpful. In the case of a significant overdose, gastric lavage should be performed, as well as the use of activated charcoal and an osmotic laxative, such as sodium sulfate.
Side effects
From the side of the central nervous system: dizziness, headache, fainting.
Cardiovascular system: palpitations, postural hypotension.
Respiratory system: rhinitis, nosebleeds.
On the part of the digestive tract: constipation, diarrhea, nausea, vomiting, dry mouth.
Skin: rash, urticaria, itching, angioedema, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, photosensitivity reaction.
From the reproductive system: priapism; ejaculation disorders, including retrograde ejaculation and ejaculation failure.
On the part of the organs of vision: blurred vision, visual impairment.
General disorders: asthenia.
Cases of intraoperative iris instability (pinched pupil syndrome) during cataract and glaucoma surgery have been described in patients who have taken tamsulosin for a long time (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 the worldwide post-marketing experience is the source of the above spontaneous cases, the frequency of reports and the role of tamsulosin in these cases cannot be reliably established.
Expiration date
2 years.
Storage conditions
Store at a temperature not exceeding 30 °C in the original packaging.
Keep out of reach of children.
Packaging
10 capsules in a blister, 3 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
MACLEODS PHARMACEUTICALS LIMITED.
Address
Village Theda, PO Lodhimaira, Tehsil Baddi, District Solan, Himachal Pradesh, 174101, India.
