Instructions for Adenorm modified-release hard capsules 0.4 mg No. 30
Composition
active ingredient: tamsulosin;
1 capsule contains tamsulosin hydrochloride (as tamsulosin hydrochloride 0.15% SR, pellets) 0.4 mg;
excipients: spherical sugar, ethyl cellulose, hydroxypropyl methyl cellulose, povidone, hypromellose phthalate, cetyl alcohol, diethyl phthalate, talc;
composition of the hard gelatin capsule: gelatin, red iron oxide (E 172), yellow iron oxide (E 172), titanium dioxide (E 171), indigotine dye (E 132).
Dosage form
Modified-release capsules, hard.
Main physicochemical properties: hard gelatin capsules No. 2, with a light green cap and an orange body. The contents of the capsules are spherical pellets of white or almost white color.
Pharmacotherapeutic group
Drugs used in benign prostatic hyperplasia. α1-adrenergic receptor antagonists. ATC code G04C A02.
Pharmacological properties
Pharmacodynamics.
Adenorm 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 part of the urethra. This leads to a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic part of the urethra and an improvement in urine output. At the same time, the symptoms of obstruction and irritation associated with benign prostatic hyperplasia are reduced (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).
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 prevent surgery or catheterization.
α1-adrenergic receptor antagonists have the ability to lower blood pressure by reducing peripheral vascular tone. During trials of the drug Adenorm, no clinically significant decrease in blood pressure was observed.
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 Adenorm at the same time after a meal. The pharmacokinetics of tamsulosin is 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 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.
Clinical characteristics.
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 conducted 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.
Available data indicate that diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not affect the free fraction of tamsulosin in human plasma. Similarly, tamsulosin does not alter 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 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, when using the drug Adenorm, a decrease in blood pressure is possible, 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 Adenorm, 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 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 on the use of the drug in such patients have not been conducted.
In some patients taking tamsulosin, atonic pupil syndrome (IFIS, a variant of pinhole pupil syndrome) has been reported 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 to date. Atonic pupil syndrome has also been reported in patients who discontinued tamsulosin well in advance of cataract surgery.
Patients undergoing elective cataract or glaucoma surgery should not be initiated on tamsulosin hydrochloride. In preparation for surgery, surgeons and ophthalmologists should inquire about the patient's history of tamsulosin use 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
Adenorm is not indicated for use in women.
Fertility
Available data indicate that cases of ejaculation disorder, retrograde ejaculation and insufficient ejaculation have been observed during the use of tamsulosin.
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; the capsule should be swallowed whole with milk or water (approximately 150 ml), standing or sitting; the capsule should be taken whole, do not chew, as this will prevent the modified release of the active ingredient.
Children
The medicine 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 may cause severe hypotensive effects. Severe hypotensive effects have been observed with varying degrees of overdose.
Treatment.
In order to stop further absorption of the drug, vomiting can be induced artificially. In case of overdose with a significant amount of the drug, the patient should be washed with activated charcoal and low-osmotic laxatives, such as sodium sulfate.
Adverse reactions
From the nervous system: dizziness; headache; fainting.
On the part of the organs of vision: blurred vision, visual impairment.
Cardiovascular system: palpitations; orthostatic hypotension.
Respiratory and mediastinal disorders: rhinitis; epistaxis.
Gastrointestinal: constipation, diarrhea, nausea, vomiting.
Skin and mucous membranes: rash, itching, urticaria; angioedema; Stevens-Johnson syndrome; erythema multiforme, exfoliative dermatitis.
From the reproductive system: ejaculation disorders, including retrograde ejaculation and ejaculation failure.
General disorders: asthenia.
Cases of intraoperative iris instability (pinched pupil syndrome) during cataract and glaucoma surgery in patients using tamsulosin have been described (see section "Special warnings and precautions for use").
In addition to the above adverse reactions, cases of atrial fibrillation, arrhythmia, tachycardia and dyspnoea have been reported, the frequency of which cannot be reliably established.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 capsules in a blister; 3 blisters in a pack.
Vacation category
According to the recipe.
Producer
PJSC "Kyiv Vitamin Plant".
Location of the manufacturer and its business address
04073, Ukraine, Kyiv, Kopylivska St., 38.
