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 • Tamsulosin general information

      • Active – active substance / start: tamsulosin

      • Tamsulosin

Flomax Tamsulosin 0,2, 0,4 mg
Most popular brand: Flomax
Active ingredient: Tamsulosin
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Active – active substance / start: tamsulosin

Bazetu; hypersimple; Omnic (Omnic Okas); Omsulozin; Revokarin; Sonizin; Tamsulosin; Tamsulosin hydrochloride; Tamsulon (Tamsulon – FS); Taniz – K; Tulozin; Fokusin.

Tamsulosin – antidizuricescoe means. Corrector of urodynamics used when urinary disorders associated with benign prostatic hyperplasia (BPH), the prostate gland. It is a selective competitive blocker of the alpha 1 / d – adrenergic receptors. Reduces smooth muscle tone of the prostate, bladder neck and prostatic urethra, thereby improving the flow of urine, and reduces the symptoms of urinary tract obstruction irritation associated with benign prostatic hypertrophy. It is used in men for the treatment of disorders dizuricheskih with prostate cancer.

Active – active substance:
Tamsulosin / Tamsulosin.

Dosage Forms:
The capsules.
pills.

Tamsulosin

Properties / Action:
Tamsulosin – corrector of urodynamics; antidizuricescoe Means, used for urinary disorders associated with benign prostatic hyperplasia (BPH), the prostate gland. It is a selective competitive blocker of alpha 1 – and alfa1d – adrenoceptor.
Tamsulosin selectively and competitively blocks postsynaptic alpha1 / d – adrenoreceptors located in the smooth muscle of the prostate, bladder neck, detrusor, the prostatic urethra (urethral), as well as in the body of the bladder. This leads to a reduction in smooth muscle tone of the prostate, bladder neck and prostatic urethra.
The treatment tamsulosin noted positive dynamics of functional dizuricheskih symptoms: improving bladder emptying, reducing the residual urine volume, urinary oblegchanie, easing symptoms of obstruction and irritation caused by benign prostatic hypertrophy (BPH), the prostate gland.
Typically, the therapeutic effect of tamsulosin develops within 2 weeks after initiation of treatment and stored for a long time, which can significantly delay the need for time-catheterization of the bladder or surgery.
Tamsulosin hardly binds to alfa1v – adrenergic receptors of vascular smooth muscle. Tamsulosin ability to influence the alpha 1 – adrenergic receptors 20 times greater than its ability to interact with alfa1v – adrenoceptors. Due to the high selectivity of Tamsulosin does not cause clinically significant systemic reduction of blood pressure in patients with hypertension, and in patients with normal blood Dahlen.

Pharmacokinetics:
Once inside Tamsulosin is rapidly and almost completely absorbed in the digestive tract. Bioavailability of tamsulosin is about 100%. Absorption is improved if taken immediately after meals Tamsulosin. It characterized by linear kinetics. After a single oral 400 mg maximum concentration (Cmax) is achieved after 6 hours in plasma. In the state of equilibrium concentration (after 5 days course tamsulosin), the maximum plasma concentration of 60 – 70% higher than after a single dose. Such an increase was noted in elderly patients; the same can be expected in younger patients. Plasma protein binding is 99%. The volume of distribution is small (0.2 l / kg). Tamsulosin is not subject to “the effect of the first passage through the liver” and slowly metabolized with the formation of pharmacologically active metabolites that retain high selectivity for alpha 1 – adrenoceptor. Most tamsulosin is present in the blood in an unmodified form. Tamsulosin mainly excreted by the kidneys in the form of conjugates; 9% is excreted unchanged form. The half-life (T1 / 2) at the single dose of about 10 hours, at constant reception – 13 hours; Terminal half-life – 22 hours.

Indications:
Tamsulosin is used in men for the treatment of functional symptoms (treatment dizuricheskih disorders, dysuria) for benign prostatic hyperplasia (prostate cancer) and a number of diseases of the prostate and lower urinary tract.

Dosage and administration:
Tamsulosin taken orally 400 mg per day after breakfast, drinking plenty of water. Capsule or tablet to chew not recommended as this may influence the rate of release of tamsulosin.
Because of the high selectivity and lack of hypotensive effect is not necessary in the selection of a dose of tamsulosin.
For minor to moderate hepatic dysfunction, as well as for violations of renal function dose adjustment Tamsulosin is also not required.

Overdose:
There were no cases of acute overdose tamsulosin.
Symptoms. Theoretically, after Tamsulosin overdose there is a possibility of acute arterial hypotension and compensatory tachycardia, which may require the application of measures to maintain the functions of the cardio – vascular system (cardiotropic therapy).
Treatment. It is necessary to put the patient; If hypotension symptoms persist, you should enter obemozameschayushie solutions or vasoconstrictor drugs. To prevent further absorption of tamsulosin may gastric lavage, activated charcoal or osmotic laxative (sodium sulphate). It is necessary to monitor renal function. The use of hemodialysis is ineffective due to the high degree of tamsulosin binding to plasma proteins.

Contraindications:

  • Individual intolerance (including a history of hypersensitivity) tamsulosin;
  • orthostatic hypotension;
  • severe hepatic impairment.
    Tamsulosin is used with caution:
  • severe renal insufficiency (creatinine clearance less than 10 ml / min).

    Side effects:
    Cardio – vascular system: orthostatic hypotension, palpitations, tachycardia, chest pain (in rare cases).
    From the nervous system: dizziness (rarely), headache, fatigue, sleep disorders – drowsiness or insomnia (in rare cases).
    On the part of the digestive system: nausea, vomiting, constipation or diarrhea (rare).
    With the respiratory system: rhinitis (sometimes).
    With the genitourinary system: retrograde ejaculation, decreased libido, priapism (rarely).
    Allergic reactions: skin rash, pruritus, angioedema (rare).
    Other:. back pain (rare)

    Special instructions and precautions:
    Before the start of tamsulosin is necessary to verify the diagnosis. The patient must be examined in order to exclude the presence of other diseases that can cause similar symptoms as benign prostatic hyperplasia. It is necessary to exclude carcinoma (cancer) of prostate. Before you start treatment and regularly during therapy with tamsulosin must be performed digital rectal examination and, if necessary, determination of prostate specific antigen (PSA).
    As with other alpha1 – blockers in the treatment of tamsulosin in some cases there may be a decrease in blood pressure, which can sometimes lead to fainting. Tamsulosin should be used with caution in patients with a predisposition to orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lay and leave in this position until the symptoms of this condition will not disappear.
    Tamsulosin administered with caution to patients with severe liver function impairment and a decrease in creatinine clearance below 10 ml / min. In patients with impaired renal function does not require dose reduction of tamsulosin.

    Effects on ability to drive and use machines:
    In the period of treatment with tamsulosin must be careful when driving and occupation of other potentially hazardous activities that require high concentration and speed of psychomotor reactions (high-altitude work, etc.).

    Drug Interactions:
    In an application with cimetidine was a slight increase in tamsulosin concentration in blood plasma, and with th – decreased concentration, but it does not require changes in the dose of tamsulosin.
    and warfarin may slightly increase the rate of elimination of tamsulosin.
    The other alpha1 – blockers (.. alfuzosin doxazosin, prazosin, terazosin), acetylcholinesterase inhibitors, alprostadil. anesthetics, diuretics (furosemide, spironolactone.), levodopa, antidepressants, beta – blockers (propranolol, atenolol, metoprolol, etc….), blockers of slow calcium channel blockers (nifedipine, amlodipine, etc…), nitrates (nitroglycerin dinitrate, isosorbide.. mononitrate, etc.), ACE inhibitors (enalapril. captopril, etc..) and ethanol may increase the severity of the hypotensive effect of tamsulosin.
    Diazepam, , trichlormethiazide, chlormadinone (Belarus), . diclofenac, glibenclamide. simvastatin and warfarin did not alter the free fraction of tamsulosin in human plasma in vitro. In turn also serves Tamsulosin free fractions of diazepam, propranolol, trichloromethiazide, chlormadinone.
    In in vitro studies found no interaction between tamsulosin at the level of hepatic metabolism with amitriptyline, salbutamol th, glibenclamide and finasteride th.
    In the appointment of tamsulosin concurrently with theophylline th drug interactions were found.

    Storage:
    List B. Store at temperatures between 15 ° and 25 ° C.
    The expiration date on the package.
    Terms of pharmacy holiday – by prescription.

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