Tamsulosin retard
Tamsulosin retard: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Tamsulosin retard
ATX code: G04CA02
Active ingredient: tamsulosin (Tamsulosin)
Manufacturer: JSC "Pharmaceutical Enterprise" Obolenskoe "(Russia)
Description and photo update: 2020-23-01
Prices in pharmacies: from 301 rubles.
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Tamsulosin retard is an α-1-adrenergic blocker, effective in the treatment of dysuric disorders against the background of benign prostatic hyperplasia.
Release form and composition
Dosage form - tablets with prolonged release, film-coated: biconvex, round, from yellow-brown to yellow; the core of the tablets on a cross section is almost white or white (10, 14, 15 or 20 tablets in blister contour packs, in a cardboard box 1, 2 or 3 packs and instructions for use of Tamsulosin retard).
Composition of 1 tablet:
- active substance: tamsulosin hydrochloride - 0.4 mg;
- auxiliary components: magnesium stearate - 0.625 mg; microcrystalline cellulose - 82.1 mg; aerosil (colloidal silicon dioxide) - 0.625 mg; hydroxypropyl methylcellulose (hypromellose) - 41.25 mg;
- shell of tablets: Opadray II 85F38111 yellow (titanium dioxide, talc, macrogol 3350, partially hydrolyzed polyvinyl alcohol, iron oxide black oxide, iron oxide red oxide, iron oxide yellow oxide) - 3 mg.
Pharmacological properties
Pharmacodynamics
Tamsulosin is one of the specific blockers of postsynaptic α-1-adrenergic receptors located in the smooth muscles of the prostatic urethra, bladder neck and prostate gland. Through the blockade of α-1-adrenergic receptors, the substance helps to improve the outflow of urine and reduce the tone of smooth muscles in these parts of the urinary system and the prostate gland. This is accompanied by a simultaneous decrease in symptoms of filling and emptying caused by detrusor hyperactivity and increased smooth muscle tone against the background of benign prostatic hyperplasia.
The ability of tamsulosin to affect the α-1A subtype of adrenergic receptors is 20 times higher than that when interacting with the α-1B subtype of adrenergic receptors located in vascular smooth muscles. Since Tamsulosin retard is highly selective, it does not cause a clinically significant decrease in systemic blood pressure (BP) both under normal conditions and against the background of arterial hypertension.
Pharmacokinetics
- absorption: getting into the intestine, tamsulosin hydrochloride is well absorbed. Its bioavailability is almost 100%. Food intake slows down the absorption of the drug. If the drug is taken every day after a regular breakfast, it allows you to achieve the same level of absorption. The kinetics of tamsulosin is linear. Its maximum concentration in blood plasma after a single oral dose of 0.4 mg is reached after 6 hours. The equilibrium concentration after repeated oral administration of a daily dose of 0.4 mg is achieved by the fifth day of therapy. The value of this parameter is 2/3 higher than that after a single dose;
- distribution: the volume of distribution of tamsulosin is small and is almost 0.2 l / kg. Its connection with plasma proteins is 99%;
- metabolism: the substance is metabolized slowly, while its less active metabolites are formed. For the most part, the dose taken is fixed in the blood unchanged. The conducted experiment revealed its ability to induce the activity of liver microsomal enzymes to a small extent. Correction of the dosage regimen in cases of minor / moderate hepatic insufficiency is not required;
- excretion: mainly the substance and its metabolites are excreted by the kidneys, approximately 9% of the drug is unchanged. With a single dose of 0.4 mg of tamsulosin hydrochloride after meals, its half-life is 10 hours, with repeated use - 13 hours. The presence of renal failure does not require a decrease in the dose of the drug, however, in severe pathology [creatinine clearance (CC) <10 ml / min] Tamsulosin retard should be used with caution.
Indications for use
Tamsulosin retard is indicated for the treatment of dysuric disorders in patients with benign prostatic hyperplasia.
Contraindications
Absolute:
- severe liver failure;
- orthostatic hypotension, including a history of;
- age up to 18 years;
- established hypersensitivity to the components of the drug.
Relative (taking Tamsulosin retard requires special care and careful medical supervision) with arterial hypotension and chronic renal failure (CC <10 ml / min).
Tamsulosin retard, instructions for use: method and dosage
Tamsulosin retard tablets are intended for oral administration.
A single dose (1 tablet once a day) is taken after breakfast with water. If swallowed, the integrity of the film coating (chewing) of the tablets must not be violated, as this may affect the rate of release of the drug.
Side effects
Possible adverse events Tamsulosin retard [> 10% - very often; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01% - very rare; frequency cannot be established from the available data - with an unspecified frequency]:
- cardiovascular system: infrequently - orthostatic hypotension, palpitations;
- gastrointestinal tract: infrequently - nausea, diarrhea, vomiting, constipation;
- nervous system: often - dizziness; infrequently - headache; rarely - fainting;
- reproductive system: infrequently - ejaculation disorders; very rarely - priapism;
- organs of the mediastinum, chest and respiration: infrequently - rhinitis;
- skin and subcutaneous tissue: infrequently - urticaria, itching, rash; rarely - angioedema; very rarely - Stevens-Johnson syndrome; frequency unknown - exfoliative dermatitis, exudative erythema multiforme;
- others: infrequently - asthenia; frequency unknown - epistaxis.
There are reports of the development of a narrow pupil syndrome (intraoperative instability of the iris) during surgery for glaucoma and cataracts in patients receiving tamsulosin hydrochloride.
Dyspnea, tachycardia, arrhythmia and atrial fibrillation were also noted among the adverse events associated with the use of the drug. Since data on the appearance of these effects were obtained by spontaneous messages in the post-registration period, the establishment of their frequency and causal relationship with tamsulosin intake is not possible.
Overdose
There have been no cases indicating an acute overdose of tamsulosin hydrochloride. Compensatory tachycardia and acute lowering of blood pressure are theoretically possible symptoms.
The presence of compensatory tachycardia requires symptomatic treatment. Heart rate and blood pressure can be restored by placing the patient in a horizontal position. If there is no effect, it is recommended to use drugs that increase the volume of circulating blood and, if necessary, vasoconstrictor drugs. It is important to monitor kidney function. Since the connection of tamsulosin with blood plasma proteins is close (almost 99%), the effect of dialysis is unlikely. In order to prevent subsequent absorption of the drug, gastric lavage, the use of activated charcoal or an osmotic laxative (for example, sodium sulfate) is recommended.
special instructions
The use of Tamsulosin retard, like other α-1-blockers, in some cases can lead to a decrease in blood pressure, which can cause fainting. The first manifestations of orthostatic hypotension (weakness, dizziness) should be a signal for the patient to adopt a sitting or lying position. In this position, he should remain until the signs of the condition disappear.
Surgical intervention for cataracts may be accompanied by the development of narrow pupil syndrome (intraoperative iris instability syndrome) during drug therapy. It is important for the surgeon to take this into account for the preoperative preparation of the patient and during the operation. Until now, the feasibility of discontinuing the drug 7-14 days before surgery has not been proven. Cases of intraoperative instability of the iris of the eye were noted with earlier discontinuation of the drug. Tamsulosin retard is not recommended for use in patients who are scheduled for surgery for these pathologies.
The occurrence of priapism and prolonged erection have been reported with the use of α-1-blockers. If an erection persists for more than 4 hours, it is important to seek immediate medical attention. In the absence of immediate treatment for priapism, damage to the tissues of the penis and an irreversible loss of potency are possible.
Before starting to use Tamsulosin retard, the patient should be examined in order to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before starting therapy and regularly during its implementation, a digital rectal examination and, if necessary, the determination of prostatic specific antigen should be performed.
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy with Tamsulosin retard tablets, due to the possible development of dizziness, drive vehicles, as well as perform other work related to the need for increased concentration of attention and a high reaction rate, should be done with caution.
Application during pregnancy and lactation
Tamsulosin retard is not intended for use in women.
Pediatric use
The use of the drug in patients under the age of 18 is contraindicated.
With impaired renal function
Chronic renal failure is a relative contraindication to the use of Tamsulosin retard.
For violations of liver function
Tamsulosin retard is not prescribed against the background of severe hepatic failure.
Drug interactions
No interactions were found between tamsulosin and nifedipine / enalapril / atenolol.
The combined use of tamsulosin with cimetidine is accompanied by a slight increase in the content of the former in the blood plasma, with furosemide - a decrease. Since the concentration of the drug does not go beyond the normal range, dose adjustment of Tamsulosin retard is not required.
The free fraction of the drug in human plasma in vitro under the influence of warfarin, simvastatin, glibenclamide, diclofenac, amitriptyline, chlormadinone, trichloromethiazide and propranolol does not change. Tamsulosin retard, in turn, also does not affect the free fractions of chlormadinone, trichloromethiazide, propranolol and diazepam.
In vitro studies have not established interactions at the level of hepatic metabolism with finasteride, glibenclamide, salbutamol and amitriptyline.
Recommended combinations to take into account:
- warfarin, diclofenac: an increase in the rate of elimination of tamsulosin is possible;
- strong inhibitors of the isoenzyme CYP3A4: the content of the drug may increase. Ketoconazole increases its area under the pharmacokinetic curve concentration - time and maximum concentration by 2.8 and 2.2 times, respectively. If the metabolism of the CYP2D6 isoenzyme is impaired, tamsulosin is not used. It is used with caution in combination with moderate / strong inhibitors of the CYP3A4 isoenzyme;
- paroxetine (a strong inhibitor of CYP2D6): increases the area under the concentration-time curve and the maximum concentration of the substance by 1.3 and 1.6 times, respectively (this increase was recognized as clinically insignificant);
- other antagonists of α-1-adrenergic receptors: a decrease in blood pressure is possible.
Analogs
Tamsulosin retard analogues are Fokusin, Tamsulosin-Binergiya, Sonizin, Taniz, Omsulozin, Tamzelin, Omnik Okas, Glansin, Tamsulon, Miktosin, Tulozin, Giperprost, Proflosin, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tamsulosin retard
The few reviews of Tamsulosin retard from patients indicate the effectiveness of the drug and the absence of side effects.
The price of Tamsulosin retard in pharmacies
Approximate price for Tamsulosin retard, tablets of 0.4 mg with prolonged release, film-coated, per package 30 pcs. ranges from 392 to 512 rubles.
Tamsulosin retard: prices in online pharmacies
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Drug name Price Pharmacy |
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Tamsulosin retard 0.4 mg film-coated tablets of prolonged action 30 pcs. 301 RUB Buy |
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Tamsulosin Retard tablets p.o. prolonged action 0.4mg 30 pcs. RUB 520 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
