Instruction for use: Artezine

Trade name of the drug – Artezine

Active substance: Doxazosinum

Dosage Form: Tablets: flat faced form, white or white with Valium a color shade.

Composition (per tablet): doxazosin mesylate (calculated as doxazosin) - 4 mg

Excipients: Potato starch - 20 mg; lactose monohydrate - 165.12 mg; Povidone - 2 mg; crospovidone (Kollidon CL) - 6 mg; magnesium stearate - 2 mg

Pharmacotherapeutic group:

Alpha1-blocker [alpha-blockers]

Alpha1-blocker [Drugs affecting the metabolism of the prostate gland and correctors urodynamics]

ATX C02CA04 Doxazosin

The nosological classification (ICD-10)

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

N40 Hyperplasia of prostate gland: Prostate adenoma; BPH; Prostatauxe; prostate Hypertrophy; Dysuric disorders caused by benign prostatic hyperplasia; Dizuricheskie disorder with benign prostatic hyperplasia; Dysuria with prostate cancer; Benign prostatic giperpalaziya; Benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2; Benign prostatic hyperplasia I degree; Benign prostatic hyperplasia II degree; Benign prostatic hypertrophy; The disease of the prostate gland; Acute urinary retention related to benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2 in combination with prostatitis; paradoxical ischuria

Pharmacological Properties of Artezine

Pharmachologic effect - Mode of action - vasodilator, hypotensive.

Pharmacokinetics

After oral administration in therapeutic doses, doxazosin is well absorbed in the gastrointestinal tract, absorption - 80-90% (simultaneous reception of food slows the absorption of 1 hour), Tmax - 3 hours, during the evening reception - 5 hours Bioavailability -. 60-70% (first-pass metabolism ).

Binding to plasma proteins - about 98%. Excretion of plasma takes place in two phases, with the end of T1 / 2 - 19-22 hours, allowing the drug to assign 1 time per day.

Rapidly metabolized in the liver by on-demethylation and hydroxylation.

Displayed through the intestine, mainly in the form of metabolites (65%), only 5% excreted by the kidneys unchanged.

Pharmacokinetic studies with doxazosin in the elderly and in patients with kidney disease showed no significant differences.

Pharmacodynamics

Doxazosin is a selective competitive blocker of postsynaptic α1-adrenergic receptors. By reducing vascular muscle tone doxazosin reduces round, resulting in a decrease in blood pressure.

After a single dose of the drug the maximum hypotensive effect observed in the period from 2 to 6 hours, and the whole anti-hypertensive effect lasts for 24 hours. During treatment with doxazosin in hypertensive patients with no differences in blood pressure values in the standing and lying down.

Effective with hypertension, including accompanied by metabolic disorders (obesity, impaired glucose tolerance).

It reduces the risk of developing coronary heart disease.

The drug in normotensive not accompanied by a decrease in blood pressure.

With prolonged use of doxazosin in patients with no reduction of the antihypertensive effect.

During treatment with doxazosin a decrease in plasma concentrations of triglycerides, total cholesterol (TC). At the same time there is some (by 4-13%) increase in HDL-C / TC ratio.

Prolonged treatment drug observed left ventricular hypertrophy regression, inhibition of platelet aggregation and the elevation of tissue plasminogen active.

Due to the fact that the blocks doxazosin α1-adrenergic receptors are located in the stroma and prostatic capsule and bladder neck, there is a decrease of resistance and pressure in the urethra, internal sphincter resistance decrease. Therefore, the appointment of the drug to patients with symptomatic benign prostatic hyperplasia results in a significant improvement in urodynamics and reduce symptoms of the disease symptoms.

Has effect in 66-71% of patients, onset of action - within 1-2 weeks of treatment, maximum - after 14 weeks, and the effect lasts for a long time.

Indications for Artezine

hypertension (in combination with other antihypertensive drugs, including thiazide diuretics, β-blockers, CCBs, ACE inhibitors); benign prostatic hyperplasia, in the presence of both hypertension and in the normal blood pressure.

Contraindications for Artezine

hypersensitivity, including other derivatives of the quinazoline and any ancillary components of the formulation; age of 18 years (effectiveness and safety have been established).

Precautions: abnormal liver function; aortic and mitral stenosis; orthostatic hypotension.

Pregnancy and breast-feeding

At the moment, experience with Artezin® the drug in patients with arterial hypertension during pregnancy and lactation is not sufficient. Therefore, despite the absence of teratogenic and embryotoxic action (according to experimental studies), Artezin® can be administered during pregnancy and lactation only after careful weighing of the attending physician benefit / risk ratio.

Artezine Dosage and Administration

Inside.

Take 1 times a day (morning or evening), regardless of the meal, not chewing and drinking plenty of water.

To ensure the below dosage regimen Artezin® possible to use the drug in the dosage form: tablets of 1 and 2 mg.

When hypertension the initial dose is 1 mg / day at bedtime. After the first dose the patient should be in bed for 6-8 hours. It is required in connection with the development of the first dose of the phenomenon, particularly marked in the background prior diuretics.

When insufficient therapeutic effect daily dose can be increased to 2 mg every 1-2 weeks. Subsequently, every 1-2 weeks the dose can be increased to 2 mg. The vast majority of patients, the optimal therapeutic effect is achieved at a dose of 8 mg / day. The maximum dose - 16 mg / day (can not be exceeded).

After reaching a stable dose of a therapeutic effect is usually somewhat lower (average therapeutic dose is usually 2-4 mg / day during maintenance therapy).

In the treatment of patients with benign prostatic hyperplasia (BPH), the initial dose - 1 mg / day in order to minimize the possibility of orthostatic hypotension and / or syncope. If necessary, depending on the performance and availability of urodynamics BPH symptoms, the dose is increased (every 1-2 weeks) to 2-4 mg / day.

The maximum permissible dose - 8 mg / day. The recommended maintenance dose - 2-4 mg / day.

The drug is used for a long time. Duration of treatment is determined by the physician.

Side effect of Artezine

Arterial hypertension

the most commonly observed in clinical trials, especially in the beginning of treatment, orthostatic hypotension, which in rare cases may cause fainting.

General reaction: asthenia, fatigue, malaise, allergic reactions, skin rash, urticaria.

From the CCC: peripheral edema, fainting.

From the central and peripheral nervous system: dizziness, headache, somnolence.

On the part of the digestive tract: nausea.

The respiratory system: rhinitis.

Also note the following adverse reactions in patients with arterial hypertension (cause-effect relationship has not been established): bradycardia, tachycardia, palpitations, chest pain, angina pectoris, myocardial infarction, cerebrovascular disease and arrhythmias.

BPH

In patients with BPH found the same side effects, and that in hypertensive patients, as well as:

General reactions: allergic reactions, skin rash, urticaria, back pain, feeling of heat (hot flushes), weight gain.

From the CCC: lowering blood pressure, orthostatic hypotension.

From the central and peripheral nervous system: dry mouth, priapism, hypoesthesia, paraesthesia, tremor, impotence, insomnia, irritability.

From the Endocrine: gynecomastia.

On the part of the digestive tract: abdominal pain, constipation, diarrhea, dyspepsia, flatulence, nausea, loss of appetite.

From the side of hematopoiesis: leukopenia, purpura, thrombocytopenia.

On the part of the hepatobiliary system: elevated liver transaminases, cholestasis, hepatitis, jaundice.

From the musculoskeletal system: arthralgia, muscle cramps, muscle weakness, myalgia.

The respiratory system: bronchospasm, cough, shortness of breath, nasal bleeding.

With the Skin: alopecia.

From the senses: blurred vision, tinnitus.

From the urinary system: dysuria, hematuria, violation of urination, nocturia, polyuria, urinary incontinence.

Overdose of Artezine

Symptoms: marked reduction of blood pressure, sometimes accompanied by fainting.

Treatment: the patient's transfer to a lying position with the head elevated above the level of the lower limbs, symptomatic therapy; Dialysis is ineffective.

Interaction

Doxazosin increases the hypotensive effect of antihypertensive drugs.

There were no adverse interaction with the simultaneous use of doxazosin and thiazide diuretics, furosemide, β-blockers, CCBs, ACE inhibitors, antibiotics, oral hypoglycaemic agents, anticoagulants and uricosuric agents.

It does not affect the degree of binding to plasma proteins, digoxin, phenytoin.

In an application with inducers of microsomal oxidation in the liver may increase the effectiveness of doxazosin with inhibitors - lowering.

NSAIDs (especially indomethacin), estrogen and sympathomimetic agents may reduce the antihypertensive effect of doxazosin.

Eliminating adrenostimuliruyuschee α-effects may lead to hypotension and tachycardia.

Cimetidine increases the bioavailability of doxazosin.

PDE inhibitors may enhance the hypotensive effect (caution).

SPECIAL INSTRUCTIONS for Artezine

Particular caution should be taken when abnormal liver function, especially for the simultaneous use of drugs with hepatotoxic. In case of deterioration of the functional state of the liver drug overturned immediately.

In order to prevent orthostatic reactions, patients should avoid unexpected and sudden shifts in body position (transition from a lying position to a standing position).

Caution must be exercised when combined with PDE inhibitors (for the treatment of erectile dysfunction), since some patients may result in symptomatic hypotension.

Drinking alcohol can increase adverse reactions.

The effect of the first dose of the drug is especially pronounced against the background of previous diuretic therapy and a diet with restriction of sodium intake.

Before therapy is necessary to exclude the malignant degeneration of the prostate gland.

Effects on ability to drive and use machines. Due to the fact that Artezin® can cause orthostatic reaction, at the beginning of treatment or during the period of increasing dosages to patients it is advisable to refrain from any potentially dangerous activities, in particular from road transport management and other vehicles and machinery.

Manufacturer

Publicly-Traded Company "Valenta Pharmacevtika." 141101, Moscow region., town Schelkovo, st. Factory 2.Tel .: (495) 933-48-62; fax: (495) 933-48-63.

Storage conditions of Artezine

In a dry, dark place at a temperature no higher than 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use beyond the expiration date printed on the package.

Conditions of supply of pharmacies

On prescription.