Description
Release form
Tablets.
Packing
30 pcs.
Pharmacological action
Selective competitive blocker of postsynaptic 1-adrenergic receptors. Due to a decrease in vascular muscle tone, doxazosin reduces OPSS, which leads to a decrease in blood pressure. 4
After a single dose of the drug, a maximum decrease in blood pressure is observed within 2-6 hours. Antihypertensive effect persists for 24 hours.
During treatment with Artezin® in patients arterial hypertension there are no differences in blood pressure values in standing and lying. Effective for arterial hypertension, including accompanied by metabolic disorders (obesity, decreased glucose tolerance). Reduces the risk of coronary heart disease.
The use of the drug in patients with normal blood pressure is not accompanied by a decrease in blood pressure.
With prolonged use of Artesin in patients, there is no change in tolerance to the therapeutic antihypertensive effect.
During treatment with artesin, a decrease in the level of triglycerides and total cholesterol in the blood plasma is observed. At the same time, there is an increase (by 4-13%) in the HDL / total cholesterol ratio.
With prolonged use of the drug, regression of left ventricular hypertrophy, suppression of platelet aggregation, and an increase in the content of active plasminogen in the tissues are observed.
Due to the fact that doxazosin blocks 1-adrenergic receptors located in the stroma and capsule of the prostate gland and in the neck of the bladder, there is a decrease in resistance and pressure in the urethra, a decrease in the resistance of the internal sphincter, which in turn leads to a significant improvement in urodynamics and a decrease in symptoms of benign prostatic hyperplasia.
The drug is effective in 66-71% of patients, a stable clinical effect develops after 1-2 weeks of treatment, the maximum effect – after 14 weeks. The effect persists for a long time.
Indications
– arterial hypertension (both in monotherapy and in combination with other antihypertensive agents / thiazide diuretics, beta-blockers, slow calcium channel blockers or ACE inhibitors /)
– benign hypertension in the presence of prostate gland and with normal blood pressure).
Contraindications
– under 18 years of age (efficacy and safety not established) – for 2 mg and 4 mg tablets
– hypersensitivity to doxazosin, quinazolone derivatives or other components of the artesin drug.
With caution, the drug should be used for aortic and mitral stenosis, orthostatic hypotension, impaired liver function, patients under the age of 18 (efficacy and safety not established) for 1 mg tablets.
Use during pregnancy and lactation
To date, experience with the use of Artezin® during pregnancy and during breastfeeding in patients with arterial hypertension is not enough.
Therefore, despite the absence of teratogenic and embryotoxic effects according to experimental studies, Artesin® can be prescribed during pregnancy and during breastfeeding only after a thorough assessment of the expected benefits of therapy for the mother and the possible risk to the fetus or infant.
Special instructions
Particular caution should be exercised when prescribing Artezin to patients with impaired liver function, especially when drugs that can adversely affect liver function are used at the same time. In cases of deterioration of the functional state of the liver, the drug should be discontinued.
In order to prevent orthostatic reactions, patients should avoid sudden and abrupt changes in body position (moving from a lying position to a standing position).
Before starting therapy, it is necessary to exclude malignant tumors of the prostate gland.
The effect of the first dose is especially pronounced against the background of previous diuretic therapy and a sodium-restricted diet.
Alcohol intake can increase adverse reactions.
Influence on the ability to drive vehicles and control mechanisms
Due to the fact that the drug is capable of causing orthostatic reactions at the beginning of treatment or during the period of increasing doses, it is advisable for patients to refrain from all potentially dangerous activities, in particular from driving vehicles and other vehicles and mechanisms.
Composition
1 tab.:
– doxazosin mesylate 2.44 mg, which corresponds to the content of doxazosin 2 mg.
Excipients:
potato starch,
lactose,
povidone (Collidone 25),
crospovidone (Collidone CL),
magnesium stearate.
Dosage and administration
The drug Artesin is prescribed orally 1 time / day. (morning or evening), regardless of food intake, without chewing and drinking plenty of water.
With arterial hypertension, the initial daily dose is 1 mg at bedtime.
After taking the first dose, the patient should be in bed for 6-8 hours. This is necessary due to the possibility of the development of the phenomenon of the first dose, especially against the background of the previous intake of diuretics.
If the therapeutic effect is insufficient, after 1-2 weeks the daily dose can be increased to 2 mg. Subsequently, every 1-2 weeks, you can increase the dose by 2 mg. In most patients, the optimal therapeutic effect is achieved with a daily dose of 8 mg. The maximum daily dose is 16 mg.
After achieving a stable therapeutic effect, the dose is usually reduced (the average therapeutic dose with maintenance therapy is usually 2-4 mg / day.).
With benign prostatic hyperplasia, Artesin® is prescribed in an initial dose of 1 mg / day. If necessary, increase the dose to 2-4 mg / day. The maximum daily dose is 8 mg.
The duration of treatment is long and is determined by the attending physician.
Side effects
Arterial hypertension: In clinical studies, orthostatic hypotension, which in rare cases can lead to fainting, was most often observed, especially at the beginning of treatment.
From the cardiovascular system: swelling, fainting.
From the side of the central nervous system and peripheral nervous system: dizziness, headache, drowsiness.
From the digestive system: nausea.
From the respiratory system: rhinitis.
General reactions: asthenia, fatigue, malaise.
The following side effects were also observed in patients with arterial hypertension (a causal relationship with the drug was not established): bradycardia, tachycardia, palpitations, chest pain, angina pectoris, myocardial infarction, cerebrovascular accident, arrhythmia.
Benign prostatic hyperplasia:
In patients with benign prostatic hyperplasia the same side effects as in patients with arterial hypertension, as well as:
From the cardiovascular system: decreased blood pressure, orthostatic hypertension.
From the side of the central nervous system and peripheral nervous system: dry mouth, priapism, hypesthesia, paresthesia, tremors, impotence, insomnia, increased irritability.
From the endocrine system: gynecomastia.
From the digestive system: abdominal pain, constipation, diarrhea, dyspepsia, flatulence, loss of appetite, nausea, increased activity of hepatic transaminases, cholestasis, jaundice, hepatitis.
From the hemopoietic organs: leukopenia, purpura, thrombocytopenia.
From the musculoskeletal system: arthralgia, muscle cramps, muscle weakness, myalgia.
From the respiratory system: bronchospasm, cough, shortness of breath, nosebleeds.
Dermatological reactions: alopecia.
From the sensory organs: blurred visual perception, tinnitus.
From the urinary system: dysuria, hematuria, impaired urination, nocturia, polyuria, urinary incontinence.
Allergic reactions: skin rash, urticaria.
Other: back pain, sensation of heat (flushing in the skin of the face).
Drug Interactions
Doxazosin enhances the antihypertensive effect of antihypertensive drugs (dose adjustment required when used in combination).
There was no adverse interaction with the simultaneous use of doxazosin and thiazide diuretics, furosemide, beta-blockers, slow calcium channel blockers, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and uricosuric agents.
The drug Artesin does not affect the degree of binding to plasma proteins of digoxin and phenytoin.
With the simultaneous use of microsomal oxidation enzymes in the liver with inducers, the effectiveness of doxazosin may decrease, with inhibitors, an increase.
Cimetidine increases the AUC of doxazosin.
NSAIDs (especially indomethacin), estrogens, and sympathomimetic drugs can reduce the hypotensive effect of doxazosin.
Eliminating the alpha-adrenostimulating effects of epinephrine, doxazosin can lead to the development of tachycardia and arterial hypotension.
Caution should be exercised while it is used with phosphodiesterase inhibitors (drugs for the treatment of erectile dysfunction), since in some patients an increase in hypotensive effect is possible.
Overdose
Symptoms: marked decrease in blood pressure, sometimes accompanied by fainting.
Treatment: The patient should be given a horizontal position with his legs raised. Conduct symptomatic therapy. Hemodialysis is ineffective.
Deystvuyuschee substances
doxazosin
Pharmacy
Prescription
Dosage form
tablet
Prescribing
Pregnant doctor, Adult prescribing, Nursing moms prescribing
Indications
hypertension, prostatic hyperplasia
Possible product names
ARTESIN 0.002 N30 TABLE
Artesin 2mg tab. X30 (R)
Artesin 2mg tab 30
tab Artesin 2mg tab N30 (pack n10x3) ind pack
Artesin tab 2mg x 30
