After oral tamsulosin is rapidly and almost completely absorbed from the gastrointestinal tract. The bioavailability of the drug – about 100%. After a single oral administration at a dose equipoise steroid of the active substance in plasma is reached after 6 hours.
At equilibrium of the active substance in plasma at 60-70% higher than the after a single dose.
Binding to plasma proteins – 99%. Tamsulosin has a slight volume of distribution (approximately 0.2 l / kg).
Tamsulosin is not subject to the effect of “first pass” and slowly biotransformed in the liver with the formation of pharmacologically active metabolites that retain a high selectivity to the α 1Aadrenoretseptoram. Most of the active substance is present in blood in an unmodified form.
Tamsulosin excreted by equipoise steroid the kidneys, 9% of the dose is excreted unchanged.
T1 / 2 at a single dose of tamsulosin -10 hours after multiple dose -13 h, the final half-life – 22 hours.
Treatment dizuricheskih disorders caused by benign prostatic hyperplasia.
Hypersensitivity to tamsulosin hydrochloride or any other component of the formulation.
Precautions: chronic renal failure (creatinine clearance below 10 ml / min), hypotension (including orthostatic..), Severe liver failure.
Dosing and Administration
Inside, after eating, 1 capsule per day, at one and the same time of day, drinking plenty of water. The capsule should not be any broken into parts or chew because equipoise steroid wherein the broken sustained release of the active substance.
Rarely – headache, dizziness, fatigue, sleep disturbances (insomnia or drowsiness), retrograde ejaculation, decreased libido, pain, back pain, rhinitis; in rare cases -ortostaticheskaya hypotension, tachycardia, palpitations, chest pain.
On the part of the digestive system: rarely – nausea, vomiting, constipation or diarrhea. In very rare cases, hypersensitivity reactions – skin rash, itching, angioedema.
Cases of acute overdose have not been described.
Symptoms: theoretically possible occurrence of acute hypotension, compensatory tachycardia.
Treatment: The patient should be put to restore blood pressure and normalize heart rate. Spend kardiotropnyh therapy. It is necessary to monitor renal function and to apply the general supportive therapy.
If the symptoms persist, you should enter obemozameschayuschie solutions vasoconstrictor drugs. To prevent further absorption of tamsulosin may gastric lavage, activated charcoal or osmotic laxative.Dialysis is not effective as tamsulosin binds strongly to plasma proteins.
Interaction with other drugs
Cimetidine increases the concentration of tamsulosin in plasma furosemide reduces the (substantial clinical significance has not, change the dosing is not required).
Diclofenac and indirect anticoagulants equipoise steroid increases the excretion of tamsulosin.
Diazepam, propranolol, trichloromethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin does not alter tamsulosin free fraction in human plasma in vitro. In turn, tamsulosin does not change the free fractions of diazepam, propranolol, trichlormethiazide and chlormadinone.
In in vitro studies found no interaction at the level of hepatic metabolism with amitriptilipom, salbutamol, glibenclamide and finasteride.
Other alpha 1-blockers, acetylcholinesterase inhibitors, alprostadil, anesthetics, diuretics, levodopa, antidepressants, beta-blockers, blockers “slow” calcium channel blockers, nitrates and ethanol may exacerbate the severity of the hypotensive effect of tamsulosin.
As with other α1-blockers tamsulosin may cause a decrease in blood pressure, rarely causing faint. At the first signs of orthostatic hypotension (dizziness, weakness), you must sit down or put the patient until symptoms disappear.
Treatment with tamsulosin must be preceded by a preliminary examination of the patient in order to exclude any other disease, flowing with the same symptoms as benign prostatic hyperplasia. Treatment should be preceded by a pre-digital rectal examination of the prostate and measuring the level of prostate specific antigen (PSA), which later, in the course of treatment is repeated regularly.
In the period of treatment should refrain equipoise steroid from activities potentially hazardous activities that require high concentration and psychomotor speed reactions. stabol