active substance: doxazosin;
1 tablet contains doxazosin mesilate 2,425 or 4,85 mg, which is equivalent to 2 or 4 mg doxazosin, respectively;
auxiliary substances: lactose, microcrystalline cellulose, microcrystalline granulated cellulose, sodium starch (type A), silicon colloidal dioxide, sodium lauryl sulfate, magnesium stearate.
Antihypertensive agents. Antiadrenergic agents with peripheral mechanism of action. Blockers of ?-adrenoreceptors. ATC code A04, collect statistical agencies С02С.
The treatment of hypertension. The majority of patients the drug can be used to control blood pressure as monotherapy. In the case where it is not possible to achieve proper control of blood pressure when used as monotherapy, this drug can be used in combination with other antihypertensive agents (thiazide diuretics, ?-adrenoreceptor blockers, calcium channel blockers or ACE inhibitors).
Of benign prostatic hyperplasia.
Treatment of obstruction of the urinary tract, and also symptoms associated with benign prostatic hyperplasia (BPH). Assign patients with BPH in the presence of hypertension,and at normal blood pressure.
Hypersensitivity to the derivative of hintline (e.g., prazosin, terazosin, doxazosin) or to any of the excipients of the drug
cases of orthostatic hypotension in history
BPH and concomitant obstruction of the upper urinary tract, chronic urinary tract infections and the presence of stones in the bladder;
arterial hypotension in patients with BPH.
Doxazosin as a monotherapy is contraindicated in patients with bladder overflow or anuria with or without progressive renal insufficiency.
Method of application and doses
The drug can be taken in the morning and in the evening.
Treatment usually begins with medication Zoxon 2, which contains less of the active ingredient. Drug taking 1 times a day: initial dose is 1 mg (1/2 tablet of the drug Zoxon 2) for 1-2 weeks to minimize the risk of orthostatic hypotension and/or syncope (see Section "Peculiarities of use") . After 1-2 weeks, the dose can be increased to 2 mg (1 tablet Zoxon 2) per day, if necessary. With insufficient effectiveness, the daily dose can be gradually increased, taking into account the individual patient's response to treatment, which is estimated depending on the achievement of the desired blood pressure level.
In most cases, using a dose of 2-4 mg per day (1 tablet Zoxon 2 or 1 tablet Zoxon 4), take 1 time a day. The maximum recommended dose is 16 mg.
Of benign prostatic hyperplasia.
Treatment usually begins with medication Zoxon 2, which contains less of the active ingredient. The recommended starting dose is 1 mg (1/2 tablets), which is taken once a day.
Depending on the individual characteristics of the patient's urodynamics and symptoms, the dose can be further increased to 2 mg (1 tablet Zoxon 2), then to 4 mg (1 tablet Zoxon 4) and to the maximum recommended dose - 8 mg.the Recommended dose titration interval is 1-2 weeks. The recommended dose is 2-4 mg daily (1 tablet Zoxon 2 or 1 tablet Zoxon 4), take 1 time a day.
Use in patients with impaired renal function.
Since the pharmacokinetics of doxazosine in patients with impaired renal function remain unchanged, and there is no evidence that the treatment of doxazosine worsens the course of existing renal failure, such patients do not require dose adjustment.
Use in patients with impaired liver function.
Patients with impaired liver function it is recommended to use the usual dose, however, you must carefully observe the individual patient's response to treatment doxazosin.
Patients of advanced age.
It is recommended to use the usual dose.
The tablets should be swallowed whole, without chewing, drinking water or soft drinks.
In patients with arterial hypertension, there were more frequent adverse reactions of orthostatic type (which in rare cases were accompanied by loss of consciousness) or non-specific adverse reactions.
In patients with BPH was observed the same profile of adverse reactions, and in patients with arterial hypertension.
The following classification is used to estimate the incidence of side effects: very often (? 1/10), often (? 1/100 and<1/10), infrequently (? 1/1000 and<1/100), rarely (? 1/10000 and<1/1000), very rarely (<1/10 000), and the frequency is unknown (cannot be estimated from existing data).
Classification systems organs in MedDRAчастотапобочные reaction
Infections and invasive respiratory tract infections, urinary tract infections
From the blood system and lymphatic systemizing regulatoria, thrombocytopenia
The immune reaction systeminstallation
Metabolic and nutritional restrictoneconnperuser, increased appetite, lack of appetite, anorexia
mental disorders, anxiety, depression, insomnia, nervousness
From the nervous estimatescoordinate, dizziness, orthostatic dizziness, headache
netaccountant, hypoesthesia, syncope, tremor
Very rare paresthesia
The bodies of preneogene reconnectcall of view
frequency neizvestnosti syndrome atonic iris
On the part of the hearing organ and vestibular apparatus of the radio frequency
necestou in the ears
From the side of the heart palpitations, tachycardia
nachstationare, myocardial infarction, chest pain, cerebrovascular accident
Very rare heart disease, arrhythmia
From sosudodwigatelny hypotension, orthostatic hypotension, hot flashes
The respiratory system thorax and sredazenergostroy, cough, dyspnea, rhinitis
Very recopilada existing bronchospasm
From the gastrointestinal tract, abdominal pain, dyspepsia, dry mouth, nausea
non-West, flatulence, vomiting, gastroenteritis, diarrhea
hepatobiliary systeminstaller from the norm from the liver
Very rare cholestasis, hepatitis, jaundice
From the skin and subcutaneous tissue
nechestolyubivye on the skin, alopecia
Very rare urticaria, purple
From the side of musculoskeletal system and connective danceschool in the back, myalgia
recomisioned spasms, muscular weakness
The kidneys and urinary putascaseira, urinary incontinence
infrequency, frequent urination, hematuria
Very recopilatory diuresis, micturition disorder, nocturia
From the reproductive system and mammary jeleznodorojnaya
Very radchenskoye, priapism
frequency Neizvestnaya ejaculation
General disorders, fatigue, malaise, chest pain, flu-like symptoms, peripheral edema
infrequent, swelling of the face
results of the investigation into the increase in body weight
The main symptom of doxazosin overdose is arterial hypotension. The patient should be immediately put on back with her head down. Treatment is symptomatic, aimed at stabilizing the indicators of hemodynamics and vital functions of the body. If the symptomatic measures are not enough, for treatment of shock in the first place it is necessary to apply plasma substitutes. After that, if necessary, to use decongestants. It is necessary to monitor the state of kidney function and, if necessary, apply supportive measures. Given the high degree of binding doxazosin plasma proteins, hemodialysis is not shown.
Application during pregnancy and lactation
The safety of the drug during pregnancy remains unknown. Therefore, the drug should be used only when the potential benefits of treatment, from the point of view of the doctor, justify the potential risk.
The use of doxazosin is contraindicated during lactation. When necessary, the application of doxazosin breast-feeding should be discontinued.
Experience of the drug in children there.
As the use of other blockers ?-adrenergic receptors, orthostatic hypotension in the application of this drug is developing in a very small percentage of patients, manifested by dizziness and weakness, or rarely loss of consciousness (syncope), especially at the beginning of therapy. In this regard, at the beginning of therapy it is necessary to monitor the level of blood pressure to minimize possible postural effects.
Prescribing therapy with any effective blocker of ?-adrenoreceptors, the patient should be informed about how to avoid symptoms of orthostatic hypotension and how to behave when they occur. The patient should also be warned of the need to avoid situations in which there is a risk of injury, given the possibility of dizziness or weakness at the beginning of treatment with doxazosin.
The use of acute heart disease.
As with other vasodilating antihypertensive drugs, doxazosin should be used with caution in patients with the following acute heart disease:
pulmonary oedema due to aortic or mitral stenosis;
hypersystolic heart failure
right ventricular heart failure due to pulmonary embolism or pericardial effusion;
left ventricular heart failure with low filling pressure.
Application in violation of liver function.
As with other drugs, completely metabolized by the liver, patients with signs of liver dysfunction doxazosin should be prescribed with extreme caution. Due to the lack of clinical experience in the use of the drug in patients with impaired hepatic function severe administration of the drug in this group of patients is not recommended.
Administration of inhibitors of PDE-5.
To use doxazosin with phosphodiesterase inhibitors-5 (e.g., sildenafil, tadalafil, and vardenafil) with caution because these drugs cause vasodilation, and therefore, can cause some patients to symptomatic hypotension.
To reduce the risk of orthostatic hypotension, it is recommended to start therapy with phosphodiesterase-5 inhibitors only if the patient has stable hemodynamics against the background of ?-blockers. In addition, it is recommended to start therapy with inhibitors of phosphodiesterase-5 with the lowest possible dose and withstand 6-hour interval between the use of doxazosin and inhibitors of phosphodiesterase-5.
The use of patients during the surgical removal of cataracts.
In some patients who took tamsulosin during surgical cataract removal or surgery, during the intervention, the development of intraoperative syndrome of atonic iris (IFIS, a variant of the narrow pupil syndrome) was observed. Some cases of the development of such a side effect and the use of other ? 1 blockers were reported, so it is impossible to exclude the possibility of developing this effect for other drugs of this class of medicines. So IFIS can lead to an increase in the frequency of procedural complications during surgery, in preparation for it should be reported to ophthalmologists, applies or used by the patient blockers ? 1-adrenoreceptor.
Patients with rare hereditary diseases such as galactose intolerance, lactase deficiency and malabsorption of glucose-galactose should not use this drug.
At the same time in patients with hypertension and BPH the drug is effective for both diseases, whereas in patients with normal blood pressure effect on blood pressure is negligible.
The ability to influence the reaction rate when driving motor transport or operating other mechanisms
Ability to drive vehicles and operate machinery may be impaired especially at the beginning of treatment. Nausea, fatigue and dizziness are possible, which can adversely affect activities requiring concentration, coordination of movements and the ability to make quick decisions.
Interaction with other medicinal products and other forms of interactions
Phosphodiesterase-5 inhibitors (e.g. sildenafil, tadalafil, vardenafil)
The combined use of doxazosin with PDE-5 inhibitors in some patients may cause symptomatic hypotension. The study of doxazosin in dosage forms with prolonged release of the active substance was not carried out.
Doxazosin largely binds to plasma proteins (98%). The results of in vitro studies using human blood plasma indicate that the drug does not affect the binding of the studied drugs (digoxin, phenytoin, warfarin or indomethacin) with proteins.
Not mentioned adverse interactions with the concomitant use of doxazosin and thiazide diuretics, furosemide, ?-adrenergic blocker, non-steroidal anti-inflammatory drugs, antibiotics, oral hypoglycemic funds, urikozuricescie means and anticoagulants in the clinical setting. However, there are no formal studies on drug interaction.
Doxazosin potentiates the hypotensive effect of other ?-adrenoblockers, as well as other antihypertensive agents.
It is known that a single use of doxazosin at a dose of 1 mg on the first day of a four-day course of oral administration of cimetidine (400 mg twice a day) led to an increase in the average level of AUC of doxazosin by 10% and did not cause any statistically significant changes in the average Cmax and the average half-life of doxazosin. Such an increase in the average level AUC of doxazosin, 10% with application of the cimetidine is in the range of interindividual variability (27%) of the average AUC of doxazosin compared with placebo.
The use of doxazosin in patients with benign prostatic hyperplasia, which is accompanied by clinical appearances, leads to a significant improvement in urodynamics and reduction of subjective symptoms of the disease. The positive effect of the drug in benign prostatic hyperplasia (BPH) is due to the selective blocking of ? 1-adrenoreceptors located in the stroma and capsule of the prostate gland, as well as in the neck of the bladder.
Doxazosin exerts a vasodilator effect through the competitive selective blocking of postsynaptic ? 1 -adrenergic receptors, which constitute more than 70% ?-adrenergic receptors in the prostate gland. The efficacy and safety of doxazosin in long-term treatment of BPH (for more than 48 months) has been proven.
The use of doxazosin in patients with hypertension leads to a clinically significant decrease in blood pressure due to a decrease in the overall peripheral vascular resistance. It is believed that this effect occurs due to the selective blocking of ? 1-adrenoreceptors located in the walls of blood vessels. When using the drug 1 time a day clinically significant antihypertensive effect lasts all day and lasts for 24 hours after the drug. Blood pressure decreases gradually, while the maximum decrease occurs within 2 to 6 hours after taking the drug. In patients with hypertension, the decrease in blood pressure during treatment with doxazosin was the same both in the sitting and standing position. In contrast, non-selective blocker of ?-adrenergic receptors, in long-term care doxazosin addiction to the drug was observed. In some cases, prolonged treatment increased renin activity in blood plasma and had tachycardia.
Unlike diuretics and ?-blockers, doxazosin has a positive effect on lipid profile, significantly increasing the ratio of HDL/total cholesterol (atherogenic index) and reducing the concentration of triglycerides and total cholesterol in blood plasma.
Given the proven relationship between hypertension and hyperlipidemia and coronary heart disease, treatment with doxazosin can reduce the risk of coronary heart disease.
Treatment with doxazosin has a positive effect on the regression of left ventricular hypertrophy, inhibits platelet aggregation and increases the activity of tissue plasminogen activator. Additionally, doxazosin improves insulin sensitivity.
Doxazosin does not cause adverse metabolic effects and may be used for patients suffering from bronchial asthma, diabetes mellitus, left ventricular hypertrophy or gout.
Among patients with arterial hypertension, treatment with doxazosin was accompanied by an improvement in erectile function. In addition to this fact, in patients taking doxazosin were significantly less likely to have any new violations of erectile function, compared to patients who took other antihypertensive drugs.
After taking doxazosin is very well absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached in 1-2 hours after administration.
Doxazosin is largely metabolized in the liver (by demethylation and hydroxylation). None of its metabolites do not have pharmacological activity.
Withdrawal of the drug from blood plasma two-phase. Terminal half-life is 22 hours, so that the drug can be taken once a day.
Pharmacokinetic studies conducted among elderly patients and patients with impaired renal function, did not reveal any significant changes compared to younger patients with normal renal function.
There are limited data on the use of the drug in patients with impaired liver function and the effects of drugs affecting liver metabolism (eg, cimetidine). The use of a single dose of doxazosin led to an increase in AUC by 43% and a decrease in clearance by 40%. As in the case of the use of any drug completely metabolised in the liver, doxazosin should be used with caution in patients with impaired liver function. Most of the administered dose is excreted from the body with feces in the form of inactive metabolites. Less than 5% of the administered dose is excreted in unchanged form.
The degree of binding doxazosin plasma proteins is 98%.
Doxazosin is extensively metabolized by O-demethylation and hydroxylation.
Basic physico-chemical properties
Saxon 2: almost white oblong pill about the size of 9х4 5 mm with a notch and engraved "ZX" and "2" on one side.
Zoxon 4: nearly white oblong tablets of approximately 12x6 mm in size with a notch and an engraving of "ZX" and " 4 " on one side.
Does not require special storage conditions. Keep out of reach of children.
Zoxon 2: №10, № 30 (10kHz): 10 tablets in a blister, 1 or 3 blisters in a cardboard box.
Zoxon 4: № 30 (10kHz): 10 tablets in a blister, 3 blisters in a cardboard box.
Category home away from home
In kabelovny 130, 102 37 Praha 10 doln? Mecholupy, Czech Republic.
LAPRIL 5 MG №20
Lopril tablets 5 mg of potent substance lisinopril is characterized by enhanced antihypertensive effect. The drug belongs to the inhibitors, has a persistent antihypertensive, vasodilating effect. With constant use of the product is a gradual stabilization of blood pressure and decreases vascular resistance.
Eating does not affect the bioavailability of the drug and the speed of its absorption.
When is discharged
Lopril is recommended to appoint patients with diagnosed diseases of the cardiovascular system, in particular for prevention:
Nephropathies of diabetic form.
Arterial, essential hypertension.
The medication can be prescribed as part of a combined treatment after a myocardial infarction.
How to use
The tablet is taken orally, without crushing, swallowed whole. The duration of the course and the dosage is determined by the attending physician according to clinical symptoms. For an adult patient, the initial rate of 5 mg is recommended, which is consumed once a day. The maximum allowed to apply 40 mg daily.