Composition, structure and packing
Tablets are white or white with kremovatym color ploskotsilindricheskie, with bevel.
1 tab. doxazosin mesilate 1.22 mg, which corresponds to the content of doxazosin 1 mg.
Excipients: potato starch, lactose, microcrystalline cellulose, povidone (kollidon 25), colloidal silicon dioxide (aerosil), sodium lauryl sulfate, magnesium stearate.
Tablets are white or white with kremovatym color ploskotsilindricheskoy form.
1 tab. doxazosin mesilate 2.44 mg, which corresponds to the content of doxazosin 2 mg.
Excipients: potato starch, lactose, microcrystalline cellulose, povidone, colloidal silicon dioxide (aerosil), sodium lauryl sulfate (sodium dodecyl sulphate), magnesium stearate.
Tablets are white or white with kremovatym color.
1 tab. doxazosin (via mesylate) 4 mg.
Excipients: lactose, potato starch, povidone (kollidon 25), magnesium stearate, krospovidon.
Clinico-pharmacological group: alpha 1-blocker. Antihypertensives.
The drug, used in violation of urination in benign prostatic hyperplasia.
Pharmacological action
Selective competitive antagonist of postsynaptic α1-adrenergic receptors. By reducing the muscle tone of vessels doxazosin reduces TPVR, which leads to a decrease in blood pressure. After a single dose of the drug the maximum reduction in blood pressure observed during the 2-6 hours hypotensive effect persists for 24 hours
During treatment with Artezin hypertensive patients with no difference between the values of BP in the standing position and lying. Effective with hypertension, including accompanied by metabolic disorders (obesity, reduced glucose tolerance). Reduces the risk of CHD. Acceptance of the drug in "normotensive" not accompanied by a reduction in BP. With prolonged use Artezina patients no change of tolerance to the therapeutic antihypertensive effect. During treatment Artezinom decrease triglycerides and total cholesterol in blood plasma. At the same time has been an increase (at 4-13%) ratio of HDL / total cholesterol.
Prolonged use of the drug observed regression of left ventricular hypertrophy, the suppression of platelet aggregation and increased content in the tissues of active plasminogen.
Due to the fact that doxazosin blocks α1-adrenergic receptors located in the stroma and capsule of the prostate and bladder neck, a decrease in resistance and pressure in the urethra, reducing the resistance of internal sphincter, which in turn leads to significant improvement in urodynamic parameters and reduce the symptoms of benign prostatic hyperplasia. The drug is effective in 66-71% of patients, stable clinical effect develops after 1-2 weeks of treatment, the maximum effect - in 14 weeks. The effect persists for a long time.
Pharmacokinetics
Absorption and distribution
After oral administration in therapeutic doses of doxazosin is well absorbed from the gastrointestinal tract. Absorption - 80-90%. Simultaneous food intake delays absorption. Time to reach Cmax - 3 hours, at the Gala Dinner - 5 pm Bioavailability - 60-70%. Linking to plasma proteins - about 98%.
Metabolism
Actively metabolized in the liver by O-demethylation and hydroxylation.
Withdrawal
Withdrawal of blood plasma occurs in 2 phases with the final T1 / 2 - 19-22 h, which allows you to assign a drug once a day. Eliminated through the intestines, primarily in the form of metabolites. Urinary recovery of about 10%, 5% - unchanged.
Pharmacokinetics in special clinical situations
In patients with impaired liver function, as well as when taking drugs that affect liver metabolism, may be in breach of the biotransformation doxazosin. Pharmacokinetic studies with doxazosin in elderly patients and patients with kidney disease did not reveal any significant pharmacokinetic characteristics.
Statement
hypertension (as monotherapy or in combination with other antihypertensive therapy / thiazide diuretics, beta-blockers, calcium channel blockers slow or ACE inhibitors /).
benign prostate hyperplasia (as in the presence of arterial hypertension and normal blood pressure).
Dosage regimen
The drug is prescribed inside 1 time / day (morning or evening), regardless of the meal, without chewing, and drinking plenty of water. When hypertension initial daily dose is 1 mg at bedtime. After the first dose the patient should be in bed for 6-8 hours is necessary due to the possibility of "first dose phenomenon", especially against the background of previous diuretic usage.
In case of insufficient therapeutic effect after 1-2 weeks the daily dose can be increased to 2 mg. Thereafter every 1-2 weeks can increase the dose of 2 mg. In most patients the optimal therapeutic effect is achieved at a daily dose of 8 mg. The maximum daily dose - 16 mg. After reaching a stable therapeutic effect of the dose is usually lower (average therapeutic dose for maintenance therapy is usually equal to 4.2 mg / day).
In benign prostatic hyperplasia Artezin appointed at the initial dose of 1 mg / day.
If necessary, dose increased to 2.4 mg / day. The maximum daily dose - 8 mg. The duration of treatment determines the physician.
Side effect
Since the cardiovascular system: orthostatic hypotension, fainting - a phenomenon first dose, edema, tachycardia, arrhythmia.
From the central nervous system and peripheral nervous system: dizziness, headache, insomnia, asthenia, abnormal sleepiness, impaired cerebral circulation.
On the part of the digestive system: dry mouth, dyspepsia, increased activity of hepatic transaminases, cholestasis, hepatitis, jaundice, constipation.
On the part of the respiratory system: dyspnea, rhinitis, nasal bleeding.
From the senses: blurred vision.
The part of the hemopoietic system: thrombocytopenia, thrombocytopenic purpura, leukopenia.
From the urinary system: polyuria, haematuria, rarely - urinary incontinence. Allergic reactions: skin rash, hives, itching.
Other: weakness, chest pain and / or back, seldom - priapism.
Contraindications
Hypersensitivity to the drug's components;
Hypersensitivity to derivatives quinazolone;
tablet 2 mg and 4 mg: children's age (efficacy and safety have not been established).
With care use in patients with aortic and mitral stenosis, orthostatic hypotension, abnormal liver function (including with liver failure), pregnancy and during breastfeeding, in the form of tablets 1 mg - in children and adolescents under age 18 years.
Pregnancy and lactation
The drug can be given during pregnancy and during breast-feeding only after careful assessment of the expected benefit of therapy for the mother and the possible risk to the fetus or infant.
Application for violations of liver function
With care use in patients with disorders of liver function.
Application for violations of renal function
Pharmacokinetic studies with doxazosin in patients with kidney disease did not reveal any significant pharmacokinetic differences.
Cautions
"The phenomenon of the first dose, especially pronounced on the background of the previous admission of diuretics and diet with restriction of sodium. Particular caution should be exercised in the appointment of the drug to patients with hepatic impairment, especially in those cases when they are used drugs that can adversely affect liver function. In cases of deterioration of functional liver drug should be abolished.
In order to prevent orthostatic reactions patients should avoid sudden and sharp changes in body position (the transition from the supine position to standing position). Before starting therapy it is necessary to exclude malignant tumor of the prostate.
Using alcohol can increase adverse reactions. Effects on ability to drive vehicles and management mechanisms
Due to the fact that the drug can cause orthostatic response at the beginning of treatment or during the period of increasing doses of appropriate patients to refrain from any potentially dangerous activities, in particular from management and other motor vehicles and machinery. Overdose Symptoms: marked reduction of blood pressure, sometimes accompanied by fainting.
Treatment: the patient should be given a horizontal position with legs elevated. Spend symptomatically. Hemodialysis is ineffective.
Drug Interactions
Doxazosin enhances the hypotensive effect of antihypertensive agents (when used in combination require dosage adjustment). There was no adverse interaction with the simultaneous use of doxazosin and antibiotics, oral hypoglycemic means of indirect anticoagulants and urikozuricheskih funds. The drug has no effect on the degree of plasma protein binding of digoxin and phenytoin.
When applied simultaneously with inducers of microsomal oxidation enzymes in the liver may reduce the effectiveness of doxazosin, with inhibitors - improvement.
Cimetidine increases the AUC doxazosin. NSAIDs (especially indomethacin), estrogens (fluid retention), and sympathomimetic drugs can reduce the hypotensive effect of doxazosin. By eliminating the alpha-adrenostimuliruyuschie effects of epinephrine, doxazosin can cause tachycardia and arterial hypotension.
Terms and Conditions of storage
List B. The drug should be stored in a dry, protected from light and away from children at or above 25 ° C. Shelf life - 3 years.
Tablets are white or white with kremovatym color ploskotsilindricheskie, with bevel.
1 tab. doxazosin mesilate 1.22 mg, which corresponds to the content of doxazosin 1 mg.
Excipients: potato starch, lactose, microcrystalline cellulose, povidone (kollidon 25), colloidal silicon dioxide (aerosil), sodium lauryl sulfate, magnesium stearate.
Tablets are white or white with kremovatym color ploskotsilindricheskoy form.
1 tab. doxazosin mesilate 2.44 mg, which corresponds to the content of doxazosin 2 mg.
Excipients: potato starch, lactose, microcrystalline cellulose, povidone, colloidal silicon dioxide (aerosil), sodium lauryl sulfate (sodium dodecyl sulphate), magnesium stearate.
Tablets are white or white with kremovatym color.
1 tab. doxazosin (via mesylate) 4 mg.
Excipients: lactose, potato starch, povidone (kollidon 25), magnesium stearate, krospovidon.
Clinico-pharmacological group: alpha 1-blocker. Antihypertensives.
The drug, used in violation of urination in benign prostatic hyperplasia.
Pharmacological action
Selective competitive antagonist of postsynaptic α1-adrenergic receptors. By reducing the muscle tone of vessels doxazosin reduces TPVR, which leads to a decrease in blood pressure. After a single dose of the drug the maximum reduction in blood pressure observed during the 2-6 hours hypotensive effect persists for 24 hours
During treatment with Artezin hypertensive patients with no difference between the values of BP in the standing position and lying. Effective with hypertension, including accompanied by metabolic disorders (obesity, reduced glucose tolerance). Reduces the risk of CHD. Acceptance of the drug in "normotensive" not accompanied by a reduction in BP. With prolonged use Artezina patients no change of tolerance to the therapeutic antihypertensive effect. During treatment Artezinom decrease triglycerides and total cholesterol in blood plasma. At the same time has been an increase (at 4-13%) ratio of HDL / total cholesterol.
Prolonged use of the drug observed regression of left ventricular hypertrophy, the suppression of platelet aggregation and increased content in the tissues of active plasminogen.
Due to the fact that doxazosin blocks α1-adrenergic receptors located in the stroma and capsule of the prostate and bladder neck, a decrease in resistance and pressure in the urethra, reducing the resistance of internal sphincter, which in turn leads to significant improvement in urodynamic parameters and reduce the symptoms of benign prostatic hyperplasia. The drug is effective in 66-71% of patients, stable clinical effect develops after 1-2 weeks of treatment, the maximum effect - in 14 weeks. The effect persists for a long time.
Pharmacokinetics
Absorption and distribution
After oral administration in therapeutic doses of doxazosin is well absorbed from the gastrointestinal tract. Absorption - 80-90%. Simultaneous food intake delays absorption. Time to reach Cmax - 3 hours, at the Gala Dinner - 5 pm Bioavailability - 60-70%. Linking to plasma proteins - about 98%.
Metabolism
Actively metabolized in the liver by O-demethylation and hydroxylation.
Withdrawal
Withdrawal of blood plasma occurs in 2 phases with the final T1 / 2 - 19-22 h, which allows you to assign a drug once a day. Eliminated through the intestines, primarily in the form of metabolites. Urinary recovery of about 10%, 5% - unchanged.
Pharmacokinetics in special clinical situations
In patients with impaired liver function, as well as when taking drugs that affect liver metabolism, may be in breach of the biotransformation doxazosin. Pharmacokinetic studies with doxazosin in elderly patients and patients with kidney disease did not reveal any significant pharmacokinetic characteristics.
Statement
hypertension (as monotherapy or in combination with other antihypertensive therapy / thiazide diuretics, beta-blockers, calcium channel blockers slow or ACE inhibitors /).
benign prostate hyperplasia (as in the presence of arterial hypertension and normal blood pressure).
Dosage regimen
The drug is prescribed inside 1 time / day (morning or evening), regardless of the meal, without chewing, and drinking plenty of water. When hypertension initial daily dose is 1 mg at bedtime. After the first dose the patient should be in bed for 6-8 hours is necessary due to the possibility of "first dose phenomenon", especially against the background of previous diuretic usage.
In case of insufficient therapeutic effect after 1-2 weeks the daily dose can be increased to 2 mg. Thereafter every 1-2 weeks can increase the dose of 2 mg. In most patients the optimal therapeutic effect is achieved at a daily dose of 8 mg. The maximum daily dose - 16 mg. After reaching a stable therapeutic effect of the dose is usually lower (average therapeutic dose for maintenance therapy is usually equal to 4.2 mg / day).
In benign prostatic hyperplasia Artezin appointed at the initial dose of 1 mg / day.
If necessary, dose increased to 2.4 mg / day. The maximum daily dose - 8 mg. The duration of treatment determines the physician.
Side effect
Since the cardiovascular system: orthostatic hypotension, fainting - a phenomenon first dose, edema, tachycardia, arrhythmia.
From the central nervous system and peripheral nervous system: dizziness, headache, insomnia, asthenia, abnormal sleepiness, impaired cerebral circulation.
On the part of the digestive system: dry mouth, dyspepsia, increased activity of hepatic transaminases, cholestasis, hepatitis, jaundice, constipation.
On the part of the respiratory system: dyspnea, rhinitis, nasal bleeding.
From the senses: blurred vision.
The part of the hemopoietic system: thrombocytopenia, thrombocytopenic purpura, leukopenia.
From the urinary system: polyuria, haematuria, rarely - urinary incontinence. Allergic reactions: skin rash, hives, itching.
Other: weakness, chest pain and / or back, seldom - priapism.
Contraindications
Hypersensitivity to the drug's components;
Hypersensitivity to derivatives quinazolone;
tablet 2 mg and 4 mg: children's age (efficacy and safety have not been established).
With care use in patients with aortic and mitral stenosis, orthostatic hypotension, abnormal liver function (including with liver failure), pregnancy and during breastfeeding, in the form of tablets 1 mg - in children and adolescents under age 18 years.
Pregnancy and lactation
The drug can be given during pregnancy and during breast-feeding only after careful assessment of the expected benefit of therapy for the mother and the possible risk to the fetus or infant.
Application for violations of liver function
With care use in patients with disorders of liver function.
Application for violations of renal function
Pharmacokinetic studies with doxazosin in patients with kidney disease did not reveal any significant pharmacokinetic differences.
Cautions
"The phenomenon of the first dose, especially pronounced on the background of the previous admission of diuretics and diet with restriction of sodium. Particular caution should be exercised in the appointment of the drug to patients with hepatic impairment, especially in those cases when they are used drugs that can adversely affect liver function. In cases of deterioration of functional liver drug should be abolished.
In order to prevent orthostatic reactions patients should avoid sudden and sharp changes in body position (the transition from the supine position to standing position). Before starting therapy it is necessary to exclude malignant tumor of the prostate.
Using alcohol can increase adverse reactions. Effects on ability to drive vehicles and management mechanisms
Due to the fact that the drug can cause orthostatic response at the beginning of treatment or during the period of increasing doses of appropriate patients to refrain from any potentially dangerous activities, in particular from management and other motor vehicles and machinery. Overdose Symptoms: marked reduction of blood pressure, sometimes accompanied by fainting.
Treatment: the patient should be given a horizontal position with legs elevated. Spend symptomatically. Hemodialysis is ineffective.
Drug Interactions
Doxazosin enhances the hypotensive effect of antihypertensive agents (when used in combination require dosage adjustment). There was no adverse interaction with the simultaneous use of doxazosin and antibiotics, oral hypoglycemic means of indirect anticoagulants and urikozuricheskih funds. The drug has no effect on the degree of plasma protein binding of digoxin and phenytoin.
When applied simultaneously with inducers of microsomal oxidation enzymes in the liver may reduce the effectiveness of doxazosin, with inhibitors - improvement.
Cimetidine increases the AUC doxazosin. NSAIDs (especially indomethacin), estrogens (fluid retention), and sympathomimetic drugs can reduce the hypotensive effect of doxazosin. By eliminating the alpha-adrenostimuliruyuschie effects of epinephrine, doxazosin can cause tachycardia and arterial hypotension.
Terms and Conditions of storage
List B. The drug should be stored in a dry, protected from light and away from children at or above 25 ° C. Shelf life - 3 years.
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