Instruction for use: Doxazosin (Doxazosini)

Trade name of the drug – Cardura, doxazosin, Zokson, Artezine, Kamiren, Urocard, doxazosin Sandoz, Kamiren XL, doxazosin Belupo, doxazosin Zentiva, Tonokardin, Doxazosin-Teva, doxazosin mesylate, Cardura Neo, Artezine retard, Doxazosin-ratiopharm, Doxazosin-FPO

The Latin name of the substance Doxazosin

Doxazosinum (genus. Doxazosini)

Chemical rational name: 1- (4-Amino-6,7-dimethoxy-2-quinazolinyl) -4 - [(2,3-dihydro-1,4-benzodioxin-2-yl) carbonyl] piperazine (in the form monomethanesulfonate)

Gross formula C23H25N5O5

Pharmacotherapeutic group: Alpha-blockers

Drugs affecting the metabolism of the prostate gland and correctors urodynamics

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

I15.0 Renovascular hypertension: hypertensive crisis; renovascular disease; accelerated hypertension; Isolated systolic 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

CAS code 74191-85-8

Description of Doxazosin

White powder. Easily soluble in dimethylsulfoxide, is soluble in dimethylformamide, difficult soluble in methanol, ethanol, water, acetone, methylene chloride.

Pharmacological Properties of Doxazosin

Pharmachologic effect - Mode of action - vasodilator, antispasmodic, antihypertensive, lipid-lowering.

Selectively blocks postsynaptic alpha1-adrenergic receptors (ratio of affinity for alpha1 / alpha2 less than 600). It reduces peripheral vascular resistance. The antihypertensive effect is partly due to the shielding of alpha 1-adrenergic receptors in the CNS. Adrenoliticheskoe effect is most pronounced in the vessels of the kidneys, skin, less - in splanchnic, pulmonary and cerebral vessels. During physical activity vasodilator effect is strongly expressed in the kidney and skin and downward - in the muscles. It reduces pre- and afterload, reduces myocardial oxygen demand. Systemic blood pressure decreased moderately without causing reflex tachycardia. It reduces total cholesterol, atherogenic lipoprotein fractions and increases HDL. It inhibits the synthesis of collagen in the vascular wall. It inhibits platelet aggregation and increases the concentration of tissue plasminogen activator. It reduces the tonus of smooth muscle of the stroma and prostate cancer cells capsule and bladder neck.

When ingestion absorbed quickly and adequately, simultaneous food slows the absorption for 1 hour. Bioavailability is 62-69%, which reflects the effect of "first pass" through the liver. Cmax achieved within 2-3 hours. At the evening reception the time to reach Cmax is extended to 5 hours. In plasma 98-99% of the drug is associated with proteins. Intensively biotransformed in the liver, primarily by demethylation and hydroxylation. It revealed several active metabolites. The final T1 / 2 -. 19-22 h Included in the enterohepatic circulation, and therefore the majority (63%) is excreted through the intestine with the feces, including 5-19% in an unmodified form; only 9% excreted through the kidneys.

The action begins to manifest itself in 1-2 hours after oral administration and reaches a peak after 5-6 hours. The antihypertensive effect develops gradually and lasts up to 24 hours, while maintaining the change of body position. Abnormal liver function prolongs the action. With prolonged use of blood pressure decreased by an average of 22/15 mm Hg. Art. It reduces the degree of left ventricular hypertrophy. The effect of the first dose as postural hypotension slightly expressed. Orthostatic hypotension can occur only with prolonged high doses. Effective with isolated systolic hypertension and its combination with metabolic disorders (obesity, hyperlipidemia, impaired glucose tolerance). In heart failure reduces the release of atrial natriuretic peptide. It is often used to treat elderly patients with BPH. High effectiveness in its conservative therapy: effect is estimated between 9 and 18 points IPSS (International System of total symptom scores). A marked reduction in the severity of obstructive and inflammatory symptoms associated with benign prostatic hyperplasia (incomplete emptying of the bladder, nocturia, frequent urination, burning sensation) and the improvement of urodynamic parameters observed in 66-71% of patients. Improvement usually occurs within 1-2 weeks of treatment, reaches a maximum of 14 weeks and is maintained for a long time. The drug in normotensive not accompanied by a decrease in blood pressure.

The effectiveness of the treatment of chronic heart failure and pheochromocytoma.

Indications for Doxazosin

Arterial hypertension (monotherapy or in combination with other antihypertensive drugs, including thiazide diuretics, beta-blockers, CCBs, ACE inhibitors), benign prostatic hyperplasia (as in the presence of hypertension and with normal blood pressure).

Contraindications for Doxazosin

Hypersensitivity.

Restrictions to application

Stenosis of the aortic and mitral valves, orthostatic hypotension, severe liver dysfunction, pregnancy, breast-feeding, age and 18 years of age.

Pregnancy and breast-feeding

Category effects on the fetus by FDA - C.

Side effect of Doxazosin

The effect of "first dose" - hypotension, dizziness, syncope (rare); postural orthostatic hypotension (long-term treatment), edema, tachycardia, arrhythmias, fatigue, shortness of breath, dizziness, headache, nervousness, irritability, abnormal drowsiness, blurred vision, rhinitis, dry mouth, abdominal discomfort, nausea, obstipation, pain chest, stroke, urinary incontinence (rare).

Overdose of Doxazosin

Symptoms: severe hypotension, syncope.

Treatment: The patient should be given a horizontal position on the back, head to torso level in case of failure - in / infusion and administration of pressor agents.

Interaction

Doxazosin increases the hypotensive effect of antihypertensive drugs. Estrogens, causing fluid retention, contribute to increased blood pressure. NSAIDs (especially indomethacin) may decrease the hypotensive effect of doxazosin. Doxazosin reduced pressor effect metaraminol, ephedrine. Blocks alpha-adrenergic effects of epinephrine, which can lead to severe hypotension and tachycardia. There were no adverse interaction with the simultaneous use of doxazosin and thiazide diuretics, furosemide, beta-blockers, CCBs, ACE inhibitors, antibiotics, oral hypoglycaemic agents, anticoagulants and uricosuric agents. Alcohol may exacerbate the adverse reactions.

Routes of administration

Inside.

Precautions for substance Doxazosin

It must be borne in mind that the first effect is especially pronounced at the receiving background therapy with diuretics, as well as sodium diet restriction. In elderly people reduce the dosage. When driving vehicles and work on production should take into account the possibility of orthostatic hypotension, as well as reduced concentration and reaction speed (usually at the beginning of treatment). To use caution with abnormal liver function (in the case of deterioration of the functional state of the liver drug overturned immediately). Before therapy of benign prostatic hyperplasia is necessary to exclude its malignant degeneration.