Artezin
Artezin: 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: Artezine
ATX code: C02CA04
Active ingredient: doxazosin (doxazosin)
Manufacturer: PJSC "Valenta Pharmaceuticals" (Russia)
Description and photo update: 2019-26-08
Prices in pharmacies: from 182 rubles.
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Artesin is a synthetic drug with antihypertensive and vasodilating effects.
Release form and composition
Artesin is produced in the form of flat-cylindrical tablets, white with a cream shade (10 pcs. In a contour package).
The active ingredient is doxazosin, in 1 tablet - 1 mg, 2 mg or 4 mg.
Excipients: microcrystalline cellulose, lactose, potato starch, magnesium stearate, sodium lauryl sulfate, povidone, colloidal silicon dioxide.
Pharmacological properties
Pharmacodynamics
The active component of Artesin is doxazosin, a selective competitive blocker of postsynaptic α 1 -adrenergic receptors. It reduces OPSS (total peripheral vascular resistance) by reducing the tone of vascular muscles, resulting in a decrease in blood pressure (blood pressure).
A single use of Artezin provides a maximum hypotensive effect in the period from 2 to 6 hours after taking the pill, the total duration of the hypotensive effect lasts for 24 hours. During doxazosin therapy in patients with arterial hypertension, there are no differences in blood pressure in the supine and standing positions.
Artesin is effective in treating arterial hypertension accompanied by metabolic disorders in obese patients and a decrease in glucose tolerance. The drug reduces the likelihood of developing coronary artery disease (ischemic heart disease). Long-term use of doxazosin does not decrease the antihypertensive effect.
During therapy with doxazosin, a decrease in the plasma concentration of triglycerides and total cholesterol is observed. At the same time, there is a slight increase (by 4–13%) in the ratio of high density lipoproteins to total cholesterol.
Long-term treatment provides regression of left ventricular hypertrophy, inhibition of platelet aggregation, as well as an increase in the content of active plasminogen in tissues.
The effectiveness of Artesin in benign prostatic hyperplasia (BPH) is based on the ability of doxazosin to block α 1 - adrenergic receptors located in the bladder neck, in the stroma and capsule of the prostate gland. Due to this, resistance and pressure in the urethra decreases, and the resistance of the internal sphincter decreases. Taking Artezin for BPH leads to a significant improvement in urodynamic parameters and a decrease in the manifestations of the symptoms of the disease. The drug is effective in 66–71% of cases, begins to act after 1–2 weeks from the start of administration, the maximum effect is achieved after 14 weeks of therapy and lasts for a long time. In patients with normal blood pressure (normotonics), a decrease in blood pressure is not accompanied.
Pharmacokinetics
Doxazosin after oral administration in therapeutic doses is well (by 80–90%) absorbed in the gastrointestinal tract. Taking tablets at the same time with food slows down absorption for 1 hour. The time to reach C max (maximum plasma concentration) is 2-3 hours, and when taken at night - 5 hours. Bioavailability due to presystemic metabolism is 60-70%.
Doxazosin binds to plasma proteins by 98%.
Excretion of the substance from blood plasma occurs in two phases, the final half-life (T 1/2) reaches 19-22 hours, as a result of which it may be sufficient to take Artezin tablets once a day. The biotransformation of doxazosin is fast, occurs in the liver by O-demethylation and hydroxylation.
The substance is excreted through the intestines, to a greater extent (up to 65%) in the form of metabolites, the kidneys are excreted unchanged about 5%.
In the course of studies of the pharmacokinetics of doxazosin in patients with impaired renal function and elderly patients, no significant pharmacokinetic differences were found.
Indications for use
According to the instructions, Artezin is used in the following cases:
- Treatment of arterial hypertension (both monotherapy and simultaneously with other antihypertensive drugs);
- Treatment of benign prostatic hyperplasia (the medicine can be used with both high and normal blood pressure).
Contraindications
Tablets at a dosage of 1 mg
Absolute contraindications for tablets at a dosage of 1 mg are individual hypersensitivity to doxazosin, other quinazolines and any auxiliary components of Artezin, as well as children / adolescence under 18 years of age.
Artezin is prescribed with caution for mitral and aortic stenosis, orthostatic hypotension, liver dysfunction, in old age, during pregnancy and during lactation (breastfeeding).
Tablets in a dosage of 2 mg and 4 mg
Absolute:
- lactose intolerance caused by lactase deficiency, glucose-galactose malabsorption;
- severe liver failure;
- BPH in combination with orthostatic hypotension or a history of arterial hypotension;
- BPH in combination with obstruction of the upper urinary tract;
- urolithiasis, chronic urinary tract infections, anuria, overflow urinary incontinence, progressive renal failure;
- age up to 18 years;
- lactation period (breastfeeding);
- individual hypersensitivity to quinazoline derivatives, doxazosin, as well as any auxiliary components of the drug.
Artezin is prescribed with caution for mitral and aortic stenosis, heart failure with increased minute output, right ventricular failure due to pulmonary embolism or pericardial effusion, left ventricular failure with low filling pressure, impaired cerebral circulation, hepatic failure, pregnancy and at the same time in old with PDE-5 inhibitors (phosphodiesterase type 5).
Instructions for the use of Artezin: method and dosage
Artezin tablets are taken regardless of the meal, 1 pc. 1 time per day, morning or evening. The daily dose of the drug and the duration of treatment depend on the disease and are determined by the doctor.
The initial daily dose for arterial hypertension is 1 mg of Artezin. The drug is taken at bedtime, after taking the first dose, it is necessary to stay in bed for 6-8 hours to avoid the development of side effects manifested in the form of the "first dose phenomenon". If the therapeutic effect is insufficient, after a few weeks the daily dose can be doubled. In the future, gradually (every few weeks) the dose can be increased by 2 mg to the effective dose, which is usually 8 mg.
Do not exceed 16 mg of Artezin per day. After achieving a stable therapeutic effect, the dose of the drug is recommended to be reduced to a maintenance dose, which is usually 2-4 mg per day.
When treating prostatitis, before starting therapy, it is necessary to exclude malignant tumors of the prostate gland. The initial dose is 1 mg of Artezin per day, if necessary, it can be increased to 2-4 mg per day. The maximum daily dose should not exceed 8 mg.
Side effects
In the treatment of arterial hypertension, Artezin most often causes orthostatic hypotension, especially at the beginning of treatment. The drug can also cause: fainting, swelling, dizziness, drowsiness, fatigue, headache, nausea, rhinitis, asthenia, malaise, in rare cases - myocardial infarction, angina pectoris, bradycardia, cerebrovascular accident, palpitations, chest tachycardia, chest pain arrhythmia.
In the treatment of prostatitis, in addition to the above-described side effects, there may be:
- Dry mouth, hypesthesia, priapism, hyperexcitability, impotence, paresthesia, tremor, insomnia;
- Muscle cramps, arthralgia, muscle weakness, myalgia;
- Alopecia;
- Skin rash, urticaria;
- Bronchospasm, shortness of breath, cough, nosebleeds;
- Dysuria, urinary disturbance, hematuria, polyuria, nocturia and urinary incontinence;
- Gynecomastia;
- Decreased blood pressure, orthostatic hypertension;
- Loss of appetite, diarrhea, abdominal pain, hepatitis, constipation, increased activity of hepatic transaminases, dyspepsia, flatulence, jaundice, nausea, cholestasis;
- Purpura, leukopenia, thrombocytopenia;
- Blurred vision, tinnitus;
- Back pain, sensation of heat.
Drinking alcohol can increase unwanted side effects.
When using Artezin in higher dosages, it is possible to develop a pronounced decrease in blood pressure, which may be accompanied by fainting.
Overdose
A symptom of an overdose of doxazosin is a pronounced decrease in blood pressure with or without fainting.
For the treatment of the condition, it is recommended to lay the patient in a horizontal position with a low headboard and raise his legs above the level of the pelvis. After that, symptomatic treatment is carried out in the form of measures aimed at maintaining blood pressure.
Hemodialysis is ineffective in removing doxazosin.
special instructions
Artesin can be used concurrently with beta-blockers, indirect anticoagulants, oral hypoglycemic agents, thiazide diuretics, furosemide, ACE inhibitors, slow calcium channel blockers, antibiotics and uricosuric agents.
Non-steroidal anti-inflammatory drugs, sympathomimetic agents and estrogens can reduce the antihypertensive effect of Artezin. With the simultaneous use of drugs with phosphodiesterase inhibitors, care should be taken because of the possible increase in the hypotensive effect.
Before starting a course of BPH therapy, it is required to exclude malignant degeneration of the prostate.
The effectiveness of the first dose of Artesin will be more pronounced against the background of previous diuretic treatment and a sodium-restricted diet.
It should be borne in mind that the risk of developing orthostatic reactions is increased by: drinking alcoholic beverages, hot weather, prolonged standing, exercise. In addition, to prevent orthostatic reactions, it is recommended to avoid abrupt, unexpected changes in body position, for example, from a prone position to a standing position.
Artesin, like any vasodilating antihypertensive drugs, must be used with caution in case of heart disease requiring emergency care: with pulmonary edema due to aortic / mitral stenosis, right ventricular failure due to pulmonary embolism or pericardial effusion, left ventricular failure with low ventricular filling pressure, severe myocardial ischemia in patients with too rapid or pronounced decrease in blood pressure, which can lead to increased symptoms of angina pectoris.
There have been reports of cases of development of prolonged erection and priapism during therapy with α 1 -adrenergic blockers. If an erection persists for more than 4 hours, you should immediately seek medical attention. In the absence of immediate therapeutic help for stopping priapism, damage to the tissues of the penis with irreversible loss of potency is possible.
Doxazosin has no effect on the plasma concentration of PSA (prostate-specific antigen).
In some patients receiving or receiving treatment with α 1 -adrenergic blockers, intraoperative atonic iris syndrome (one of the variants of narrow pupil syndrome) was recorded during cataract surgery. Since it can cause an increase in complications during surgery, it is necessary to warn the operating surgeon about taking doxazosin at the moment or in the preoperative period.
Influence on the ability to drive vehicles and complex mechanisms
Due to the fact that Artezin can cause orthostatic reactions at the beginning of therapy or during the period of increasing doses, it is recommended to refrain from all potentially hazardous activities, including driving.
Application during pregnancy and lactation
So far, the experience of using Artezin in pregnant / lactating women has been limited. In this regard, the use of the drug is recommended only as directed by a doctor, provided that the expected benefit to the mother exceeds the potential risk to the fetus / child.
If it is necessary to use Artezin tablets at a dosage of 2 mg or 4 mg during lactation, breastfeeding should be discontinued during therapy.
Pediatric use
Due to the lack of data on the safety and efficacy of the drug in children and adolescents under 18 years of age, Artezin is not used in pediatric practice.
With impaired renal function
Artezin tablets at a dosage of 2 mg and 4 mg are contraindicated in patients with progressive renal failure.
For violations of liver function
Like other drugs that completely undergo biotransformation in the liver, Artezin is prescribed with caution to patients with hepatic insufficiency, especially at the same time as drugs that can adversely affect hepatic function. Deterioration of these laboratory indicators of the functional state of the liver requires immediate withdrawal of Artezin.
For tablets with a dosage of 2 mg and 4 mg, severe hepatic impairment is a contraindication.
Use in the elderly
Elderly patients Artezin is prescribed with caution due to the possible development of orthostatic hypotension. It is also necessary to take into account the increase with age in the likelihood of dizziness, fainting and visual impairment.
Drug interactions
- other antihypertensive drugs: doxazosin enhances their antihypertensive efficacy, which, if necessary, may require dose adjustment;
- other blockers of α-adrenergic receptors: it is not recommended to take simultaneously with doxazosin;
- thiazide diuretics, furosemide, β-blockers, slow calcium channel blockers, angiotensin-converting enzyme inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants, uricosuric drugs: no adverse interactions with doxazosin were noted with simultaneous use;
- digoxin, phenytoin: doxazosin does not affect the degree of their binding to plasma proteins;
- inducers of microsomal oxidation in the liver: it is possible to increase the effectiveness of doxazosin;
- inhibitors of microsomal oxidation in the liver: a decrease in the effectiveness of doxazosin is possible;
- estrogens, sympathomimetic drugs, NSAIDs (non-steroidal anti-inflammatory drugs), especially indomethacin: can reduce the hypotensive efficacy of doxazosin;
- cimetidine: increases the bioavailability of doxazosin;
- PDE-5 inhibitors (sildenafil, tadalafil, udenafil, vardenafil): combined use with doxazosin can lead to symptomatic hypotension; a 6-hour interval between their use is required, in order to reduce the risk of a fall in blood pressure, therapy begins with PDE-5 inhibitors;
- epinephrine: doxazosin inhibits its α-adrenostimulating effects and can lead to the development of arterial hypotension and tachycardia.
Analogs
Artezin's analogs are:
- By active substance: Kardura, Zoxon, Doxazosin, Urocard, Tonokardin, Kamiren, Doxaprostan;
- By the mechanism of action: Pirroxan, Ebrantil, Propokon, Setegis, Kornam, Prazosin, Terazosin, Urapidil Karino.
Terms and conditions of storage
Store at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Artezin
According to one of the indications, the drug is used to treat the prostate, and ultimately to improve sexual function in men. There are practically no reliable reviews of Artezin when used for the treatment of BPH.
As an antihypertensive drug, Artezin is effective when taken for a long time. Usually, from the second half of the course, patients notice an improvement in their condition, normalization of pressure, and the passage of headaches.
In any case, everyone recommends taking the drug only as directed by a doctor, strictly observing a certain dosage regimen.
The price of Artezin in pharmacies
Approximate price of Artezin (pack of 30):
- tablets 2 mg - 350-400 rubles;
- 4 mg tablets - 430-480 rubles.
Artezin: prices in online pharmacies
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Drug name Price Pharmacy |
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Artesin 2 mg tablets 30 pcs. 182 r Buy |
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Artesin 4 mg tablets 30 pcs. RUB 185 Buy |
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Artesin tablets 2mg 30 pcs. 395 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
