pharmachologic effect
Fokusin is a drug aimed at combating urinary disorders caused by benign prostatic hyperplasia.
The therapeutic effect of Fokusin is based on its ability to competitively and selectively block postsynaptic Alpha1-adrenergic receptors located in the bladder neck, smooth muscle of the prostate gland and prostatic urethra. In addition, the drug has the ability to block Alpha1D type adrenergic receptors, located mainly in the body of the bladder. As a result, the tone of the smooth muscles of the above organs decreases, and the functions of the detrusor (the muscles of the urethra) improve. This, in turn, entails a reduction in the symptoms of irritation and obstruction caused by prostatic hyperplasia.
According to the instructions for Focusin, the therapeutic effect of taking the drug develops within two weeks from the start of use. In rare cases, there is a decrease in the severity of symptoms after the first dose.
Pharmacological properties of the drug Fokusin
Tamsulosin reduces the tone of the smooth muscles of the prostate and urethra, helps reduce obstruction, stimulates bladder emptying and significantly improves urine outflow. During treatment with tamsulosin, there is a pronounced positive dynamics of functional dysuric symptoms: a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra leads to a weakening of the symptoms of obstruction and irritation caused by benign prostatic hyperplasia (BPH), improved bladder emptying, reducing the volume residual urine, making urination easier. The therapeutic effect of Fokusin lasts for a long time, which makes it possible to significantly delay the need for bladder catheterization or surgical intervention. α1-blockers, by reducing peripheral vascular resistance, can cause a decrease in blood pressure. No clinically significant reduction in blood pressure was observed during tamsulosin studies. Pharmacokinetics. After oral administration, tamsulosin is quickly and almost completely absorbed from the gastrointestinal tract, its bioavailability is about 100%. Absorption is enhanced if the drug is taken immediately after a meal. The kinetics of tamsulosin is linear. When a single dose (0.4 mg) of tamsulosin is taken after a meal, the maximum concentration in the blood plasma is achieved within 6 hours. In a state of equilibrium concentration (after 5 days of continuous course administration), the maximum concentration of tamsulosin in the blood plasma is 2/3 higher than after single dose of the drug. This increase was noted in elderly patients; the same can be expected in young patients. Plasma protein binding is 99%, the volume of distribution is small and amounts to 0.2 l/kg body weight. Tamsulosin is slowly metabolized and the first-pass effect is negligible. Most of the tamsulosin is present in the blood plasma in unchanged form. Tamsulosin is metabolized in the liver. Tamsulosin and its metabolites are especially actively excreted in the urine; about 9% of the drug is excreted unchanged. The half-life for a single dose is about 10 hours. At a stable level of the substance in the blood plasma (with constant use of the drug), the half-life is about 13 hours.
Side effects of Focusin
The use of Focusin and drug analogues in rare cases can cause unwanted effects. You should consult your doctor if you notice the following types of ailments while taking the medicine:
- headache, asthenia, dizziness, various sleep disorders;
- retrograde ejaculation, decreased libido;
- nausea, diarrhea, constipation or vomiting;
- tachycardia, orthostatic hypotension, palpitations, chest pain;
- skin rash, angioedema, itching and other manifestations of allergic reactions;
- back pain;
- rhinitis.
Special instructions for the use of the drug Fokusin
Focusin is used with caution when performing work that requires increased concentration and speed of psychomotor reactions (driving vehicles and machinery, working at height, etc.). As with the use of other α-adrenergic receptor blockers, treatment with tamsulosin may in some cases decrease blood pressure, and loss of consciousness has occasionally been reported. When the first signs of orthostatic hypotension (dizziness, weakness) appear, the patient should be seated or laid down until the symptoms of hypotension disappear, and then blood pressure levels should be regularly monitored. Before starting to use the drug, it is necessary to verify the diagnosis in order to exclude diseases whose symptoms may be similar to those of BPH. Before starting treatment and then at certain intervals, a rectal digital examination should be performed, and, if necessary, the level of prostate-specific antigen should be monitored. The drug is used with caution in patients with severe renal failure (creatinine clearance ≤10 ml/min).
Interactions of the drug Focusin
No interactions have been observed with the simultaneous use of Fokusin with atenolol, enalapril, nifedipine or theophylline. The simultaneous use of cimetidine leads to an increase in the plasma level of tamsulosin, and the simultaneous use of furosemide causes its decrease. At the same time, tamsulosin levels remain within normal limits, so there is no need to adjust the dose of tamsulosin. In vitro , diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin or warfarin do not change the fraction of free tamsulosin in human plasma. The drug does not affect the fractions of free diazepam, propranolol, trichloromethiazide or chlormadinone. When conducting in vitro on the microsomal fraction of the liver (to study the effect of drug metabolism on the cytochrome P450 enzyme system), no interaction with amitriptyline, salbutamol, glibenclamide and finasteriod was confirmed at the level of hepatic metabolism. Diclofenac and warfarin may increase the rate of elimination of tamsulosin. The simultaneous use of other α1A-adrenergic receptors can lead to potentiation of the hypotensive effect of the latter.
Focusin: price and where to buy?
The drug is widely available in pharmacies and online stores selling pharmaceutical products. Given the specifics of the drug, you can buy it only by presenting a prescription form certified by a doctor.
The cost for Focusin starts from 450 rubles. The variability of prices is determined by the region, the number of capsules in the package, and markups of a particular pharmacy chain.
Release form and indications
The drug is supplied to the shelves in the form of capsules, which are coated with gelatin. The case is transparent with a blue lid. Micropellets inside are white. One package contains 30 or 90 pieces.
Indications for use: impaired functionality of the urinary system, accompanied by impaired urine outflow due to prostatitis or adenoma.
The medicine has a narrow specialization, therefore, the restrictions on its use are significant. This:
- Intolerance to substances in the capsule;
- Chronically low blood pressure;
- Severe insufficient functionality of the liver and kidneys.
Negative reactions of the body to the medicine are expressed in:
- Dizziness, headaches, fainting;
- Blood pressure surges;
- Increased heart rate;
- Allergic rhinitis;
- Nausea with bouts of vomiting;
- Stool disorders;
- Ejaculation disorder;
- Extremely rare - priapism;
- Asthenic syndrome;
- Sustained constriction of the pupil.
Focusin, 400 mcg, modified release capsules, 90 pcs.
Before starting treatment with Focusin®, it is necessary to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before starting treatment and regularly during therapy, a prostate examination (digital rectal examination, PSA determination) should be performed. As with the use of other α1-blockers, during treatment with Fokusin®, in some cases a decrease in blood pressure may be observed, which can lead to fainting.
The drug Fokusin® 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 be seated or laid down.
There are reports of cases of prolonged erection and priapism during therapy with α1-blockers. If an erection persists for more than 4 hours, you should immediately seek medical help. If priapism therapy is not carried out immediately, it can lead to damage to the tissue of the penis and irreversible loss of potency.
If angioedema develops, as well as other immunological reactions, such as Stevens-Johnson syndrome, use of the drug should be stopped immediately. The patient should be monitored until this pathological condition is eliminated; re-prescription of tamsulosin is not allowed. During cataract surgery, intraoperative iris instability syndrome (small pupil syndrome) has occurred in some patients receiving tamsulosin hydrochloride at the time of surgery or in the past. The occurrence of intraoperative iris instability syndrome can lead to an increased risk of complications from the organ of vision during and after surgery.
Tamsulosin hydrochloride should not be used in combination with potent inhibitors of the CYP3A4 isoenzyme in patients with a slow metabolizer phenotype for the CYP2D6 isoenzyme.
Tamsulosin is not for use in women.
Impact on the ability to drive vehicles and engage in other potentially hazardous activities.
Caution should be exercised when driving vehicles and doing activities that require increased concentration and speed of psychomotor reactions. If dizziness occurs, you should refrain from driving and other potentially hazardous activities.
Overdose of the drug Focusin, symptoms and treatment
There have been no reports of cases of acute drug overdose. Theoretically, the development of acute hypotension is possible, requiring measures to maintain the function of the cardiovascular system. Treatment: cardiotropic therapy, parenteral administration of volume-substituting solutions, and, if necessary, vasoconstrictor drugs. Adjuvant therapy and monitoring of renal function should be carried out. The use of hemodialysis is ineffective due to the high degree of binding of the drug to plasma proteins. In order to reduce the absorption of the drug, vomiting should be induced, gastric lavage should be performed, and the use of activated charcoal or an osmotic laxative is indicated.
What kind of medicine is Focusin?
Focusin is an alpha-blocker that relaxes the bladder muscles and facilitates the process of urine outflow. The key advantage of the drug is its rapid therapeutic effect, however, a significant list of restrictions on its use does not allow it to be prescribed to all men. In addition, the medication provokes side effects, which requires its replacement with a milder medicine. These factors exclude self-medication with Focusin; it is prescribed only by a urologist after a comprehensive examination of the man.
The main active ingredient is tamsulosin at a concentration of 0.4 mg. Additional substances:
- Polysorbate 80;
- Microcrystalline cellulose;
- Dibutyl sebacate;
- Talc;
- Methacrylic copolymer dispersion;
- Colloidal aqueous silicon dioxide.
The shell is made on the basis of blue dye, gelatin and azorubine.
