Tamsulosin
Tamsulosin: 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. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Tamsulosin
ATX code: G04CA02
Active ingredient: tamsulosin (tamsulosin)
Manufacturer: Pharmaceutical company VERTEX, CJSC (Russia); Borisov Plant of Medical Products, JSC (Republic of Belarus); Synthon Hispania SL (Spain) for Moskhimpharmaceuticals them. N. A. Semashko (Russia)
Description and photo update: 2018-26-10
Prices in pharmacies: from 244 rubles.
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Tamsulosin is an α1-adrenergic blocker for the treatment of urinary disorders in benign prostatic hypertrophy.
Release form and composition
Dosage forms:
- sustained-release capsules: No. 3, green, gelatinous hard; filler - from almost white to white pellets (10, 15, 18 or 20 pcs. in blister packs, in a cardboard box 1, 3 or 6 packs of 10 pcs., or 2, 4 or 6 packs of 15 pcs., or 5 packs of 18 pcs., or 3 packs of 20 pcs.; 30, 60 or 90 pcs. in high density polyethylene cans, in a cardboard box 1 can);
- enteric capsules of prolonged action: No. 2, gelatinous solid; light orange body and olive-colored lid on the top are marked with a black stripe, on the lid there is an inscription in black ink “TSL 0.4”; filler - from almost white to white pellets (10 pcs. in blisters, in a cardboard box 1, 2, 3, 5, 6, 9 or 10 blisters);
- prolonged-release tablets: round, biconvex, white, on one side there is an inscription “T9SL”, on the other side - “0.4” (10 pcs. in blisters, 3 packs in a cardboard box).
Composition for 1 capsule with prolonged release:
- active ingredient (substance-pellets): tamsulosin hydrochloride - 0.4 mg;
- auxiliary substances (substance-pellets): sugar spheres (sucrose - 99%, hypromellose - 1%), methacrylic acid copolymer, polyethylene glycol, ethyl cellulose;
- capsule: titanium dioxide, yellow iron oxide (iron oxide), patented blue dye, gelatin.
Composition for 1 enteric capsule of prolonged action:
- active substance (pellet core): tamsulosin hydrochloride - 0.4 mg;
- auxiliary substances (core of pellets): microcrystalline cellulose, methacrylic acid and ethyl acrylate copolymer (1: 1), triethyl citrate, talc, purified water;
- auxiliary substances (pellet shell): methacrylic acid and ethyl acrylate copolymer (1: 1), talc, triethyl citrate, purified water;
- capsule body: titanium dioxide, dye iron oxide red, dye iron oxide yellow, gelatin;
- ink: pharmaceutical glaze [45% shellac solution in ethanol (20% esterified)], black iron oxide dye, n-butyl alcohol, propylene glycol, isopropanol, ammonium hydroxide 28%, ethanol, purified water.
Composition for 1 tablet of prolonged action:
- active substance: tamsulosin hydrochloride - 0.4 mg;
- excipients: hypromellose, microcrystalline cellulose, carbomer, red iron oxide (E172), magnesium stearate, colloidal anhydrous silicon dioxide.
Pharmacological properties
Pharmacodynamics
The active component of the drug is tamsulosin, a specific blocker of postsynaptic α 1 -adrenergic receptors located in the smooth muscles of the bladder neck, prostate and prostatic urethra. This blockade helps to reduce smooth muscle tone and improve urine outflow, while reducing the severity of filling / emptying symptoms due to increased smooth muscle tone and detrusor hyperactivity in benign prostatic hyperplasia. The effectiveness of tamsulosin against the α 1A subtype of adrenergic receptors is 20 times higher than its ability to influence α 1Ba subtype of adrenergic receptors located in vascular smooth muscles. Tamsulosin, due to such high selectivity, does not cause a clinically significant decrease in systemic blood pressure (blood pressure) both in hypertension and with a normal initial blood pressure.
Pharmacokinetics
- absorption: tamsulosin has good intestinal absorption and almost 100% bioavailability; absorption slows down somewhat after eating. It is possible to achieve the same level of absorption with daily intake of the drug, for example, after the first breakfast. Tamsulosin has linear kinetics. A single oral administration at a dose of 0.4 mg gives the maximum concentration of the substance in the blood plasma after 6 hours. Repeated intake in a daily dose of 0.4 mg can achieve equilibrium concentration of the 5th day, while its value at 2 / 3 exceeds the index as a result of single dose;
- distribution: tamsulosin binds to blood plasma proteins by 99%, V d (volume of distribution) is insignificant, about 0.2 l / kg;
- metabolism: tamsulosin is subject to slow hepatic metabolism, which results in the formation of less active metabolites. Most of the substance is in the blood plasma in an unchanged form. According to experimental studies, the ability of tamsulosin to induce the activity of microsomal hepatic enzymes to an insignificant extent was found, and therefore, patients with mild and moderate hepatic impairment do not need to correct the dosage regimen;
- excretion: the substance and its metabolites are mainly excreted by the kidneys, up to 9% while excreted unchanged. The half-life (T 1/2) after a single oral dose of 0.4 mg of tamsulosin after meals is 10 hours, after multiple doses - 13 hours.
Indications for use
According to the instructions, Tamsulosin is recommended for the treatment of dysuric disorders caused by BPH (benign prostatic hyperplasia).
Contraindications
Absolute contraindications for all forms of drug release:
- orthostatic hypotension (including anamnestic data);
- decompensated liver failure;
- belonging to the female sex;
- children and adolescents under 18 years of age;
- malabsorption of glucose-galactose, insufficiency of sucrase-isomaltase, fructose intolerance (for capsules with prolonged release);
- increased individual sensitivity to tamsulosin, other components of the drug.
Relative contraindications for capsules:
- arterial hypotension;
- severe renal failure with creatinine clearance (CC) less than 10 ml / min.
Instructions for use Tamsulosin: method and dosage
Tamsulosin capsules and tablets are intended for oral administration.
Recommended dosage: adult patients over 18 years of age take 1 capsule or tablet daily.
Taking the drug:
- capsules: in the morning after breakfast, drink plenty of water. The capsules should not be chewed or bitten, as this may affect the rate of release of the active substance;
- tablets: regardless of mealtime, swallowing whole without chewing or breaking, so as not to disrupt the release of the active substance.
Side effects
The incidence of adverse reactions from systems and organs, taking into account the recommendations of the World Health Organization (on a scale: very often - ˃ 10%; often - from 1/100 to 1/10; infrequently - from 1/1000 to 1/100; rarely - from 1/10 000 to 1/1000; extremely rare - ˂ 1/10 000, including individual events; with an unknown frequency - according to the available data, it is not possible to determine the frequency of side effects):
- cardiovascular system: infrequently - orthostatic hypotension, palpitations; with an unknown frequency - arrhythmia, tachycardia, atrial fibrillation, shortness of breath;
- gastrointestinal tract: infrequently - nausea / vomiting, constipation, diarrhea;
- central and peripheral nervous system: often - dizziness; infrequently - headache; rarely - fainting;
- reproductive system: often - ejaculation disorders; extremely rare - priapism;
- respiratory organs, chest and mediastinum: infrequently - rhinitis;
- skin and subcutaneous tissue: infrequently - rash, urticaria, itching; rarely - angioedema; extremely rare - Stevens-Johnson syndrome; with an unknown frequency - erythema multiforme, exfoliative edema;
- other reactions: infrequently - asthenia; with an unknown frequency - epistaxis, intraoperative instability of the iris, the so-called. constricted pupil syndrome (IRIS), during cataract / glaucoma surgery.
Overdose
Information on cases of acute overdose of tamsulosin was not recorded.
The most likely symptoms of an overdose may be a pronounced decrease in blood pressure, compensatory tachycardia. In this case, symptomatic therapy is recommended.
It is possible to restore the heart rate and normalize blood pressure by adopting the Trendelenburg position (lying on the back at an angle of 45 ° with the pelvis raised in relation to the head). In the absence of a result from the procedure, it is recommended to use drugs that increase the volume of circulating blood, and, if necessary, vasoconstrictor drugs. Monitoring of renal function is required. Hemodialysis is inappropriate due to the fact that tamsulosin is largely bound to blood plasma proteins. To prevent further absorption of the substance, it is advisable to wash the stomach, take activated charcoal or an osmotic laxative, such as sodium sulfate.
special instructions
Tamsulosin, like other α1-blockers, in some episodes can cause a significant decrease in blood pressure, as a result of which the patient may develop fainting. The first signs of orthostatic hypotension are dizziness and weakness. When they appear, it is necessary to sit or lay down the patient and hold him in this position until the symptoms disappear.
Before prescribing Tamsulosin, it is required to make sure that the patient does not have other pathologies that can cause symptoms similar to BPH.
Before taking the drug and regularly during treatment, it is necessary to undergo a digital rectal examination, and, if necessary, the determination of prostate specific antigen (PSA).
In the course of surgical interventions for cataract / glaucoma, some patients taking or previously taking tamsulosin may develop intraoperative instability of the iris of the eye (the so-called constricted pupil syndrome), as a result of which complications may develop during surgery or in the postoperative period. The expediency of discontinuing Tamsulosin therapy 1–2 weeks before surgery for cataract / glaucoma has not been proven, since cases of constricted pupil syndrome have been reported in patients who discontinued the drug and at an earlier preoperative period. It is not recommended to start taking the drug for patients who are scheduled for surgery for cataract / glaucoma. At the preoperative examination, the surgeon and ophthalmologist should consider the presence or absence of preoperative tamsulosin. This will allow them to prepare for the possible development of intraoperative iris instability during the operation.
The development of angioedema requires immediate discontinuation of therapy. The administration of tamsulosin to such patients is contraindicated again.
In case of impaired renal function, as well as with mild and moderate hepatic insufficiency, correction of the dosage regimen is not required.
Influence on the ability to drive vehicles and complex mechanisms
Studies on the effect of the drug on the ability to drive vehicles and other complex mechanisms have not been conducted. However, given side effects such as dizziness, it is important to be careful when performing potentially hazardous activities that require increased concentration and psychomotor speed.
Application during pregnancy and lactation
Tamsulosin is intended for use exclusively in male patients.
Pediatric use
In pediatrics, the use of Tamsulosin is contraindicated.
With impaired renal function
Tamsulosin capsules should be taken with caution in patients with severe renal impairment (CC <10 ml / min). Reducing the dose of the drug is not required.
For violations of liver function
Tamsulosin tablets are contraindicated in patients with severe liver failure.
Use in the elderly
Correction of the dosage regimen of the drug in elderly patients is not required.
Drug interactions
- atenolol, enalapril, nifedipine and theophylline: drug interactions with tamsulosin were not found;
- cimetidine: may increase the plasma concentration of tamsulosin;
- furosemide: reduces the concentration of tamsulosin, but does not require dose adjustment, since it remains within the therapeutic range;
- propranolol, diazepam, chlormadinone, trichloromethiazide, diclofenac, warfarin, amitriptyline, simvastatin, glibenclamide: in vitro do not change the free fraction of tamsulosin in blood plasma, which, in turn, also does not change the free fractions of propranolol, trichloromethiazepam; diclofenac, warfarin can increase the rate of elimination of tamsulosin;
- amitriptyline, salbutamol, glibenclamide and finasteride: in vitro interaction with glibenclamide at the level of hepatic metabolism was not found;
- strong inhibitors of the isoenzyme CYP3A4: an increase in the plasma concentration of tamsulosin is possible. For example, ketoconazole (a strong inhibitor of the isoenzyme CYP3A4), with simultaneous use, increased the AUC (area under the concentration-time pharmacokinetic curve) and C max (maximum concentration) of tamsulosin by 2.8 and 2.2 times, respectively. Patients with impaired metabolism of the CYP2D6 isoenzyme should not be prescribed tamsulosin in combination with strong inhibitors of the CYP3A4 isoenzyme. In combination with strong and moderate inhibitors of the isoenzyme CYP3A4, the drug must be used with caution;
- paroxetine (a strong inhibitor of the isoenzyme CYP2D6): when administered simultaneously with tamsulosin, it increased its C max and AUC by 1.3 and 1.6 times, respectively, but such an increase was recognized as clinically insignificant;
- other α1-blockers: a decrease in blood pressure is possible.
Analogs
Tamsulosin analogs are: Glansin, Hyperprost, Miktosin, Omsulozin, Omnik, Omnik Okas, Sonizin, Proflosin, Tamzelin, Tamsulozin Canon, Tamsulozin Bakter, Tamsulozin retard, Tamsulozin-Teva, Tamsulozin-OBL, Tamsulozin-Teva.
Terms and conditions of storage
Store in a place protected from light and moisture, at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tamsulosin
There are few reviews of Tamsulosin, perhaps this is due to the specifics of the disease, since it affects the intimate sphere. Doctors agree that the drug is effective, safe and relatively inexpensive.
The opinions of the patients were divided, one drug helped after the first course of admission, but there are complaints of intolerable and unpredictable pain, in which even strong pain relievers are useless. The positive point is that the pain syndrome is transient and passes some time after stopping the intake.
Price for Tamsulosin in pharmacies
Estimated price for Tamsulosin capsules with extended release: for 90 pcs. in the package - 733 rubles, for 30 pcs. in the package - 479 rubles.
Tamsulozin: prices in online pharmacies
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Drug name Price Pharmacy |
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Tamsulosin Bakter 0.4 mg film-coated tablets with prolonged release 30 pcs. 244 RUB Buy |
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Tamsulosin retard 0.4 mg film-coated tablets of prolonged action 30 pcs. 301 RUB Buy |
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Reviews Tamsulosin retard 301 RUB Buy |
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Tamsulosin Bakter 0.4 mg enteric capsules with prolonged release 30 pcs. 382 r Buy |
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Tamsulosin Canon 0.4 mg enteric capsules with prolonged release 30 pcs. 393 r Buy |
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Tamsulosin bakter tab. with prolong. exs. p / pl.ob. 0.4 mg No. 30 431 r Buy |
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Tamsulosin Retard tablets p.o. prolonged action 0.4mg 30 pcs. RUB 520 Buy |
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Tamsulosin -vertex capsules prolong release 0.4 mg 30 pcs. RUB 530 Buy |
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Tamsulosin prolonged tablets. release p.p. 0.4mg 30 pcs. 639 RUB Buy |
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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!
