Instructions Omlos capsules 0.4 g No. 30
Composition
active ingredient: tamsulosin hydrochloride; 1 capsule contains 0.4 mg of tamsulosin hydrochloride;
excipients:
capsule contents: microcrystalline cellulose, methacrylate copolymer dispersion, polysorbate 80, sodium lauryl sulfate, triethyl citrate, talc;
capsule shell: gelatin, FD&C indigo carmine blue 2 (E 132), titanium dioxide (E 171), black iron oxide (E 172), red iron oxide (E 172), yellow iron oxide (E 172).
Dosage form
Modified-release capsules, hard.
Main physicochemical properties: hard gelatin capsules with an orange body and an olive cap. The contents of the capsules are white to almost white granules.
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 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 emptying of the bladder, 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 in tamsulosin trials.
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, modified-release capsules, at the same time after a meal. The pharmacokinetics of tamsulosin are linear.
After a single dose of tamsulosin modified-release capsules taken after a meal, peak plasma concentrations of tamsulosin are reached approximately 6 hours after dosing, and steady-state concentrations are reached by the fifth day of daily dosing. Cmax 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 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 tamsulosin, modified-release capsules, after food and at steady-state plasma concentrations, the elimination 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
Interaction studies have only been performed in adults.
No drug interactions were observed when tamsulosin hydrochloride was used concomitantly with atenolol, enalapril, nifedipine or theophylline.
Concomitant use with cimetidine increases, and with furosemide decreases, the plasma concentration of tamsulosin, but since these levels remain within the normal range, there is no need for special dosage adjustment of tamsulosin.
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 AUC and Cmax to 2.8 and 2.2, respectively.
Tamsulosin hydrochloride should not be administered in combination with strong CYP3A4 inhibitors in patients who are poor CYP2D6 metabolisers.
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 rare cases, tamsulosin may cause a decrease in blood pressure, 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 tamsulosin, 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.
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 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 Interactions with other medicinal products and other forms of interaction).
Cases of allergic reactions to tamsulosin have been reported in patients with a history of allergy to sulfonamides. Caution should be exercised when using tamsulosin hydrochloride in patients with a history of allergy to sulfonamides.
Use during pregnancy and/or breastfeeding
Tamsulosin 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 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 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.
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) | 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 disorders | 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. As these cases were reported spontaneously, the frequency of reporting and the role of tamsulosin in this case cannot be reliably established.
Expiration date
3 years.
Do not use after the expiry date stated on the packaging.
Storage conditions
This drug does not require special temperature storage conditions.
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
ALKALOID AD Skopje.
Address
Boulevard Aleksandar Makedonski 12, Skopje, 1000, Republic of North Macedonia.
