Doxazozin (doxazosin) tablets 1 mg. №30

Description

Doxazozin 1 mg Composition
active substance: doxazosin;

1 tablet contains doxazosin mesylate in terms of doxazosin 1 mg;

Doxazozin 1 mg excipients: microcrystalline cellulose lactose monohydrate, corn starch calcium stearate.

Doxazozin 1 mg Dosage form
Pills.

Basic physical and chemical properties: white tablets, beveled.

Pharmacotherapeutic group
Antihypertensive drugs. Antiadrenergic drugs with a peripheral mechanism of action. Blockers of α-adrenergic receptors. ATX code С02С А04.

Pharmacodynamics
Mechanism of action

Doxazosin is a potent and selective antagonist of postsynaptic α1-adrenergic receptors. Blocking these receptors leads to a decrease in systemic blood pressure. Doxazosin is intended for oral administration once a day in patients with essential hypertension.

Pharmacodynamic effects

It has been demonstrated that doxazosin does not cause undesirable metabolic effects and can be used in patients with diabetes mellitus, gout or insulin resistance.

Doxazosin can be prescribed to patients with bronchial asthma, left ventricular hypertrophy and elderly patients. The use of the drug helps to reduce left ventricular hypertrophy, suppresses platelet aggregation and enhances the activity of tissue plasminogen activator. In addition, the use of doxazosin increases insulin sensitivity in those patients in whom such sensitivity is impaired.

It was also reported that in addition to the antihypertensive effect, the use of doxazosin causes a moderate decrease in the concentration of total cholesterol, low density lipoproteins and triglycerides in blood plasma, and therefore, this drug may be especially useful in patients with arterial hypertension and hyperlipidemia.

The use of doxazosin in patients with recurrent BPH leads to a significant improvement in urodynamics and a decrease in symptoms. It is believed that the effect of the drug in BPH is achieved due to the selective blockade of α1-adrenergic receptors located in the muscular stroma and capsule of the prostate gland, as well as in the bladder neck.

Pharmacokinetics
Suction. When administered orally in humans (young men or elderly people of any sex), doxazosin is rapidly absorbed from a bioavailability of about ⅔ of the dose.

Metabolism / Elimination. 98% of doxazosin binds to blood plasma proteins. It has been shown that doxazosin is extensively metabolized in the human body and in the studied experimental animals, and is excreted from the body mainly in the feces.

The half-life (T ½) of the drug from blood plasma is 22 hours, which makes it possible to take the drug once a day.

With oral administration of doxazosin, the concentration of drug metabolites in the blood plasma is low. The plasma concentration of the active metabolite 6′-hydroxydoxazosin in humans is 40 times lower than the plasma concentration of the primary compound, which indicates that the antihypertensive effect of the drug is mainly due to doxazosin.

Currently, there are only limited data on the use of the drug in patients with impaired liver function and on the effect of drugs that can alter hepatic metabolism (for example, cimetidine). As with the use of other drugs, it is completely metabolized by the liver, patients with signs of liver dysfunction should be used with caution in patients with signs of liver dysfunction.

Indications
Arterial hypertension. The drug is indicated for the treatment of hypertension and can be used as monotherapy for blood pressure control in most patients. In case of ineffectiveness of monotherapy for the treatment of arterial hypertension, the drug can be used in combination with thiazide diuretics, β-adrenoreceptor blockers, calcium channel blockers and angiotensin-converting enzyme inhibitors.

Benign prostatic hyperplasia. It is indicated for the treatment of urinary tract obstruction and symptoms associated with benign prostatic hyperplasia (BPH). The drug can be prescribed to patients with BPH both in the presence of arterial hypertension and at normal blood pressure.

Contraindications
Hypersensitivity to the active substance or to quinazoline derivatives (for example, prazosin, terazosin, doxazosin) or to any of the excipients of the drug specified in the “Composition” section; history of orthostatic hypotension with BPH and concomitant upper urinary tract obstruction, chronic urinary tract infections and bladder stones; during lactation (only when used for the treatment of arterial hypertension (see section “Use during pregnancy or lactation”), arterial hypotension (only applies to patients with BPH). Doxazosin as monotherapy is contraindicated in patients with bladder overflow or anuria with progressive renal failure with or without it.