Description
Release form
Tablets.
Packing
30 pcs. 4 mg each.
Pharmacological action of
Doxazosin is a selective competitive blocker of postsynaptic 1-adrenergic receptors. Due to the decrease in vascular muscle tone, doxazosin reduces OPSS, which leads to a decrease in blood pressure.
After a single dose of the drug, a maximum hypotensive effect is observed from 2 to 6 hours, and in general, the antihypertensive effect persists for 24 hours. During treatment with doxazosin in patients with arterial hypertension, there are no differences in the values of blood pressure in standing and lying down.
Effective in hypertension, including accompanied by metabolic disorders (obesity, decreased glucose tolerance).
Reduces the risk of developing coronary heart disease.
Taking the drug in normotonics is not accompanied by a decrease in blood pressure. With prolonged use of doxazosin in patients, there is no decrease in the antihypertensive effect.
During treatment with doxazosin, a decrease in the concentration level of plasma triglycerides, total cholesterol (OX) is observed. At the same time, there is a slight (4 13%) increase in the HDL / OH ratio.
With prolonged treatment with 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. Therefore, the appointment of the drug to patients with symptoms of benign prostatic hyperplasia leads to a significant improvement in urodynamics and a decrease in the manifestation of the symptoms of the disease.
Has an effect in 66 71% of patients, the onset of action after 1 2 weeks of treatment, maximum after 14 weeks, the effect persists for a long time.
Contraindications
Hypersensitivity, including to other quinazoline derivatives or any of the auxiliary components of the drug.
Age under 18 years (efficacy and safety not established).
Caution: impaired liver function aortic and mitral stenosis orthostatic hypotension.
Use during pregnancy and lactation
To date, the experience with the use of Artezin ® in patients with arterial hypertension during pregnancy and during breastfeeding is insufficient.
Therefore, despite the absence of teratogenic and embryotoxic effects (according to experimental studies), Artesin ® can be prescribed during pregnancy and during breastfeeding only after careful weighing by the attending physician the benefit / risk ratio.
Special instructions
Particular care must be taken in case of impaired liver function, especially with the simultaneous use of drugs with hepatotoxic effects. In case of deterioration of the functional state of the liver, the drug is immediately canceled.
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).
Caution should be exercised when used together with PDE inhibitors (drugs for the treatment of erectile dysfunction), as this may lead to symptomatic hypotension in some patients.
Alcohol intake can increase adverse reactions.
The effect of the first administration of the drug is especially pronounced against the background of previous diuretic therapy and a diet with a restriction of sodium intake.
Before starting therapy, it is necessary to exclude cancerous degeneration of the prostate gland.
Effect on the ability to drive vehicles and work with mechanisms
Due to the fact that Artesin ® is able to cause orthostatic reactions, it is advisable to refrain from all potentially dangerous activities, in particular from driving and other vehicles and mechanisms.
Composition
1 tablet contains:
Active ingredient:
doxazosin mesylate (in terms of doxazosin) – 4 mg.
Excipients:
potato starch – 20 mg
lactose monohydrate – 165.12 mg
povidone – 2 mg
crospovidone (Collidone CL) – 6 mg
magnesium stearate – 2 mg.
Dosage and Administration
Inside.
Take 1 time per day (morning or evening), regardless of food intake, without chewing and drinking plenty of water.
To ensure the dosage regimen below, it is possible to use Artezin ® in the dosage form: 1 and 2 mg tablets.
With arterial hypertension, the initial dose is 1 mg / day at bedtime. After taking the first dose, the patient should be in bed for 6-8 hours. This is required in connection with the possibility of the development of the phenomenon of the first dose, especially pronounced against the background of the previous intake of diuretics.
If the therapeutic effect is insufficient, the daily dose can be increased to 2 mg after 1-2 weeks. Subsequently, after every 1-2 weeks the dose can be increased by 2 mg. In the vast majority of patients, the optimal therapeutic effect is achieved at a dose of 8 mg / day. The maximum dose is 16 mg / day (can not be exceeded).
After achieving a stable therapeutic effect, the dose is usually somewhat reduced (the average therapeutic dose with maintenance therapy is usually 2-4 mg / day).
In the treatment of patients with benign prostatic hyperplasia (BPH), the initial dose is 1 mg / day in order to minimize the possibility of developing orthostatic hypotension and / or fainting. If necessary depending on the urodynamic indicators and the presence of symptoms of BPH, the dose is increased (with an interval of 1-2 weeks) to 2-4 mg / day.
The maximum allowable dose is 8 mg / day. The recommended maintenance dose is 2 4 mg / day.
The drug is used for a long time. The duration of treatment is determined by the doctor.
Side effects of
Arterial hypertension
In clinical trials, orthostatic hypotension, which in rare cases can lead to fainting, was most often observed, especially at the beginning of treatment.
General reactions: asthenia, fatigue, malaise, allergic reactions, skin rash, urticaria.
From the CCC side: peripheral edema, fainting.
From the side of the central nervous system and peripheral nervous system: dizziness, headache, drowsiness.
From the gastrointestinal tract: nausea.
From the respiratory system: rhinitis.
And the following adverse reactions were noted in patients with arterial hypertension (a causal relationship has not been established): bradycardia, tachycardia, palpitations, chest pain, angina pectoris, myocardial infarction, impaired cerebral circulation and arrhythmia.
BPH
Patients with BPH have the same side effects as those with hypertension, as well as:
General reactions: allergic reactions, skin rash, urticaria, back pain, sensation of heat (hot flashes), weight gain.
From the CCC side: decreased blood pressure, orthostatic hypotension.
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 gastrointestinal tract: abdominal pain, constipation, diarrhea, dyspepsia, flatulence, nausea, loss of appetite.
From the hemopoietic organs: leukopenia, purpura, thrombocytopenia.
From the hepatobiliary system: increased activity of hepatic transaminases, cholestasis, hepatitis, jaundice.
From the side of the musculoskeletal system: arthralgia, muscle cramps, muscle weakness, myalgia.
From the respiratory system: bronchospasm, cough, shortness of breath, nosebleeds.
From the skin: alopecia.
From the sensory organs: blurred visual perception, tinnitus.
From the urinary system: dysuria, hematuria, impaired urination, nocturia, polyuria, urinary incontinence.
Drug interaction
Doxazosin enhances the hypotensive effect of antihypertensive drugs.
There was no adverse interaction with the simultaneous use of doxazosin and thiazide diuretics, furosemide, β-blockers, BKK, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and uricosuric agents.
Does not affect the degree of binding to plasma proteins of digoxin, phenytoin.
With simultaneous use with inducers of microsomal oxidation in the liver, an increase in the effectiveness of doxazosin is possible, with inhibitors, a decrease.
NSAIDs (especially indomethacin), estrogens, and sympathomimetic drugs can reduce the hypotensive effect of doxazosin.
Eliminating -adrenostimulating effects, can lead to the development of tachycardia and arterial hypotension.
Cimetidine increases the bioavailability of doxazosin.
PDE inhibitors may enhance the hypotensive effect (use caution).
Overdose
Symptoms: marked decrease in blood pressure, sometimes accompanied by fainting.
Treatment: transfer of the patient to the supine position with the lower extremities raised above the head, symptomatic therapy dialysis is ineffective.
Storage Conditions
In a dry, dark place at a temperature not exceeding 25 ° C.
Keep out of the reach and sight of children.
active substance
Doxazosin
Terms leave through pharmacies
In retseptu
lekarstvennaja form
tablets
Prescribing
For nursing mothers as prescribed by the doctor, For adults as prescribed by the doctor, Pregnant women as prescribed by the doctor
Indications
Indications
Hypertension of the prostate, Hypertension
