Adenorm selectively and competitively blocks postsynaptic Î±1-adrenoreceptors, in particular Î±1A and Î±1D, 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 urethra and improve urine flow. Simultaneously, the severity of obstructive symptoms and irritation associated with benign prostatic hyperplasia (shortness start urination, weakening of the urine stream, dripping after urination closure, feeling of incomplete bladder emptying, frequent urination, urination at night, urgency of urination).
These effects persist for a long time with long-term treatment and significantly delay surgery or catheterization.
Î‘1-adrenoreceptor antagonists have the ability to reduce blood pressure by reducing the peripheral vascular tone. When testing the drug Adenorm, there was no clinically pronounced decrease in blood pressure.
Suction. Tamsulosin is well absorbed in the digestive tract, and its bioavailability is almost 100%. Tamsulosin absorption is somewhat slower after a meal. Absorption uniformity is achieved when the patient takes Adenorm at the same time after a meal. The pharmacokinetics of tamsulosin is linear.
When taking a single dose of the drug after a meal, the peak concentration of tamsulosin in the blood plasma is reached in approximately 6 hours, and a stable concentration is formed on the 5th day after daily administration of the drug. At the same time, Cmax is approximately â…” higher than that achieved after taking a single dose.
Distribution. In men, tamsulosin is approximately 99% bound to plasma proteins. The volume of distribution of the drug is low (about 0.2 l / kg).
Metabolism. Tamsulosin hydrochloride is not subject to the effect of the first passage and is slowly metabolized in the liver with the formation of pharmacologically active metabolites, which retain a high selectivity for Î±1-adrenergic receptors. Most of the active substance is present in the blood unchanged.
Elimination. Tamsulosin and its metabolites are excreted mainly in the urine. About 9% of the dose remains as unchanged active ingredient.
After a single dose of the drug after a meal and at a stable plasma concentration, TÂ½ is about 10 and 13 hours, respectively.
treatment of functional disorders of the lower urinary tract with prostatic hyperplasia.
the recommended dose for adults is 1 capsule daily after breakfast; the capsule should be swallowed whole with milk or water (about 150 ml), standing or sitting; take the capsule whole without chewing, as this will prevent the modified release of the active ingredient.
hypersensitivity to tamsulosin hydrochloride, including drug-induced angioedema, or any of the excipients; a history of orthostatic hypotension; severe liver failure.
nervous system: dizziness; headache; fainting.
On the part of the organ of vision: blurred vision, blurred vision.
Since the cardiovascular system: a feeling of heartbeat; orthostatic hypotension.
Respiratory-mediastinal disorders: rhinitis; nose bleed.
On the part of the digestive tract: constipation, diarrhea, nausea, vomiting.
On the part of the skin and mucous membranes: rash, itching, hives; angioedema; Stevens-Johnson syndrome; erythema multiforme, exfoliative dermatitis.
On the part of the reproductive system: ejaculation disorders, including retrograde ejaculation and ejaculation failure.
General disorders: asthenia.
Cases of intraoperative instability of the iris of the eye (narrowed pupil syndrome) during cataract surgery and glaucoma in patients who took tamsulosin are described (see SPECIAL INDICATIONS).
In addition to the above adverse reactions, cases of atrial fibrillation, arrhythmia, tachycardia and dyspnea have been reported, the incidence of which cannot be reliably established.
as with the use of other Î±1-adrenoreceptor blockers, in some cases, the use of the drug Adenorm may decrease blood pressure, which can sometimes lead to loss of consciousness. When the first signs of orthostatic hypotension (dizziness, weakness) appear, the patient should sit down or take a horizontal position until the above symptoms disappear.
Before you begin treatment with the drug Adenorm, you should undergo a medical examination in order to establish other related diseases that can cause the same symptoms as benign prostatic hyperplasia. Before treatment, it is necessary to conduct a rectal examination of the prostate gland and, if necessary, a test to determine the level of specific antigen of the prostate gland (PSA) before and after the same periods during treatment.
It is necessary to administer the drug to patients with severe form of renal failure (creatinine clearance <10 ml / min) with extreme caution, since no clinical studies on the use of the drug in these patients have been performed.
Some patients who have used tamsulosin have had atonic pupil syndrome (IFIS, a variant of the narrowed pupil) during surgery for cataracts and glaucoma, which may cause an increase in the number of complications during or after such an operation.
As a rule, 1â€“2 weeks before surgery for cataracts and glaucoma, it is recommended to stop treatment with tamsulosin, however, the benefits of stopping treatment with tamsulosin are not clearly established to date. It was also reported on the atonic pupil syndrome in patients who stopped using tamsulosin long before cataract surgery.
Patients before planned surgery for cataracts or glaucoma are not recommended to start using tamsulosin hydrochloride. In preparation for surgery, surgeons and ophthalmologists should find out whether the patient has used (or uses) tamsulosin in order to prevent possible complications associated with IFIS.
Tamsulosin hydrochloride should not be given in combination with potent inhibitors of CYP 3A4 in patients with low metabolism of CYP 2D6.
Tamsulosin hydrochloride should be used with caution in combination with potent and mild inhibitors of CYP 3A4 (see INTERACTIONS).
The drug contains sugar, which should be considered in patients with diabetes.
There are cases of allergic reactions to tamsulosin in patients with a history of allergies to sulfonamides. Caution should be exercised when using tamsulosin hydrochloride in patients who have previously experienced an allergy to sulfonamides.
Use during pregnancy and lactation. Adenorm is not indicated for use in women.
Fertility Available evidence suggests that during the use of tamsulosin, there were cases of impaired ejaculation, retrograde ejaculation, and insufficient ejaculation.
Children. The drug should not be used in children. The safety and efficacy of tamsulosin in children (under the age of 18) was not evaluated.
Influence on ability to drive vehicles and work with complex mechanisms. Studies of the effect of the drug on the ability to drive vehicles or mechanisms were not performed. However, patients should be warned about the possibility of dizziness.
interaction studies were conducted only in adults.
With the simultaneous use of tamsulosin with atenolol, enalapril, nifedipine or theophylline, drug interactions were not observed. Simultaneous use with cimetidine increases, and with furosemide, it reduces the concentration of tamsulosin in the blood plasma, but since these levels remain within the normal range, there is no need for special adjustment of the dose of tamsulosin.
Diazepam, propranolol, trichloromethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin are not known to affect the free fraction of tamsulosin in human blood plasma. Similarly, tamsulosin does not alter the level of free fractions of diazepam, propranolol, trichloromethiazide, and chlormadinone in human plasma.
However, diclofenac and warfarin may increase the rate of elimination of tamsulosin.
The simultaneous use of tamsulosin hydrochloride with strong inhibitors of CYP 3A4 can lead to an increase in the effect of tamsulosin hydrochloride. Simultaneous use with ketoconazole (a known potent inhibitor of CYP 3A4) resulted in an increase in AUC and Ð¡max to 2.8 and 2.2, respectively.
Tamsulosin hydrochloride should not be given in combination with strong CYP 3A4 inhibitors in patients with low CYP 2D6 metabolism.
Tamsulosin hydrochloride should be used with caution in combination with potent and mild inhibitors of CYP 3A4.
The simultaneous use of tamsulosin hydrochloride and paroxetine (a powerful inhibitor of CYP 2D6) leads to an increase in Cmax and AUC to 1.3 and 1.6, respectively, but this is not clinically significant.
Simultaneous use with other Î±1-adrenoreceptor blockers may enhance the hypotensive effect.
the symptoms. An overdose of tamsulosin hydrochloride can cause severe hypotensive effects. Severe hypotensive effect was noted at different degrees of overdose.
Treatment. In the event of a sharp decrease in pressure due to overdose, supportive therapy should be carried out aimed at restoring the normal function of the cardiovascular system (for example, the patient must assume a horizontal position). If this measure does not work, conduct an infusion therapy and prescribe vasopressor agents. It is necessary to monitor the function of the kidneys and carry out general maintenance therapy. Due to the high degree of binding of tamsulosin to plasma proteins, hemodialysis is hardly advisable.
In order to stop further absorption of the drug, it is possible to induce vomiting artificially. In case of overdose with a significant amount of the drug, the patient must wash the stomach with activated carbon and low-osmosis laxatives, such as sodium sulfate.
in the original packaging at a temperature not higher than 25 Â° C.