Doxazosin-OBL pills 2 mg N30
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Active ingredients
Doxazosin
Release form
Pills
Composition
1 tablet contains: doxazosin mesilate 2.44 mg, which corresponds to the content of doxazosin 2 mg. Auxiliary substances: lactose monohydrate — 90.16 mg, calcium phosphate — 35 mg, povidone K30 — 0.6 mg, sodium lauryl sulfate — 0.3 mg, calcium stearate — 1 mg, talc - 0.5 mg.
Pharmacological effect
Vasodilator, spasmolytic, hypotensive, hypolipidemic. Selectively blocks postsynaptic alpha1-adrenergic receptors. Due to the decrease in muscle tone of blood vessels, it reduces OPS and lowers blood pressure. Decreases plasma triglycerides, total cholesterol and HDL cholesterol. At the same time, there is a slight increase in the HDL ratio with respect to total cholesterol (by 4–13%). Suppresses platelet aggregation and increases the content of active plasminogen in the tissues. Reduces the tone of smooth muscle cells of the stroma and the capsule of the prostate gland, as well as the bladder neck. Lowers resistance and pressure in the urethra, reduces the resistance of the internal sphincter.
Pharmacokinetics
Well absorbed after ingestion. Absorption - 80–90% (simultaneous ingestion slows down absorption for 1 hour), Cmax is reached after 3 hours, when taken in the evening after 5 hours. Bioavailability - 60–70% (presystemic metabolism). Plasma protein binding is about 98%. It is rapidly metabolized in the liver by o-demethylation and hydroxylation. Excretion from plasma occurs in 2 phases, T1 / 2 - 19–22 hours. It is excreted through the intestine mainly as metabolites, 5% is excreted in the urine unchanged.
Indications
Arterial hypertension (monotherapy and in combination with other antihypertensive drugs: thiazide diuretics, beta-blockers, calcium channel blockers or ACE inhibitors), benign prostatic hyperplasia (in the presence of arterial hypertension and with normal blood pressure).
Contraindications
Hypersensitivity, pregnancy, breastfeeding, age up to 18 years.
Use during pregnancy and lactation
Contraindicated. At the time of treatment should stop breastfeeding.
Dosage and administration
Inside, regardless of the meal, not chewing and drinking plenty of water,Once a day (in the morning or in the evening). In case of arterial hypertension: doses range from 1 to 16 mg / day (maximum); the initial dose is 1 mg 1 time per day (before bedtime), after which the patient should stay in bed for 6–8 hours (the development of the “first dose” phenomenon, especially expressed against the background of prior diuretic administration) is possible. With insufficient therapeutic effect, the daily dose is increased to 2 mg only after 1–2 weeks of continuous treatment, then with an interval of 1–2 weeks, the dose is increased by 2 mg to achieve the optimal therapeutic effect. After reaching a stable therapeutic effect, the dose is usually reduced (the average therapeutic dose with maintenance therapy is 2–4 mg / day). In benign prostatic hyperplasia without arterial hypertension: usually 2–4 mg / day, the maximum dose is 8 mg / day.
Side effects
When doxazosin is used, especially at the beginning of treatment, orthostatic hypotension is most often observed, which in rare cases can lead to fainting. In order to prevent orthostatic hypotension, patients should avoid unexpected and sudden changes in body position (going from lying to standing). There may be: headache, dizziness, general feeling of weakness, fatigue, drowsiness, rhinitis, nausea. Patients with arterial hypertension are rarely observed: tachycardia, arrhythmia, chest pain, angina attacks, myocardial infarction, cerebrovascular disorders. There have been isolated cases of allergic reactions (skin rash, jaundice, thrombocytopenic purpura, elevated transaminase level, transyamnaz, I have already, I have already, I have already, I have already, I am no longer able to have a transaminase, I have already had a number of allergies) priapism, urinary incontinence, increased appetite, constipation, increased diuresis, myalgia, arthralgia.
Overdose
Symptoms: marked lowering of blood pressure, sometimes accompanied by fainting. Treatment: the patient must be placed in a horizontal position (head down, legs raised), symptomatic therapy.
Interaction with other drugs
Strengthens the hypotensive effect of antihypertensive drugs. Compatible with thiazide diuretics, furosemide, beta-blockers, calcium channel blockers, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and uricosuric agents. When combined with inducers of microsomal oxidation in the liver, an increase in the effect is possible; with inhibitors, a decrease.NSAIDs (especially indomethacin), estrogens and sympathomimetic agents reduce the hypotensive effect. Lowers the pressure effect of ephedrine. Eliminating the alpha-adrenostimulating effects of epinephrine can lead to a distortion of its pressor action and the development of tachycardia.
special instructions
With extreme caution, the drug should be prescribed to patients with impaired liver function, especially in cases where drugs are used at the same time that can adversely affect liver function. In cases of deterioration of the functional state of the liver, the drug is immediately canceled. In order to prevent orthostatic reactions, patients should avoid unexpected and abrupt changes in body position (transition from a prone position to a standing position). against the background of previous diuretic therapy and adherence to a diet with restriction of sodium intake. Before starting therapy, it is necessary to exclude malignancies Renaissance of the prostate gland. Impact on the ability to drive vehicles and control mechanisms During the period of treatment, patients should be careful when driving and doing other potentially hazardous activities that require increased concentration and psychomotor reactions (risk of dizziness, weakness). so that doxazosin can cause orthostatic reactions at the beginning of treatment or during the period of increasing doses, it is advisable for patients to to abstain from all potentially hazardous activities, in particular from driving vehicles and other vehicles and mechanisms.