Spontaneous hypertension - both in monotherapy and in combination therapy (in most patients Doxazosin is effective in monotherapy, but if it is necessary to use combination therapy, it is administered with a thiazide diuretic, beta adrenergic antagonist, Calcium channel blocker or angiotensin converting enzyme inhibitor ). Benign prostatic hyperplasia - symptomatic treatment.
Composition:
1 tabl contains 1 mg, 2 mg or 4 mg doxazosin as doxazosin mesilate. The preparation contains lactose.
Action:
A selective, competitive antagonist of α receptors1adrenergic. By blocking the receptor within peripheral vessels, doxazosin causes their expansion, decrease in peripheral resistance and reduction of blood pressure. It also improves the dynamics of urination and reduces symptoms in patients with symptomatic benign prostatic hyperplasia, probably due to selective inhibition of α-receptors1-adrenergic in the smooth muscle layers of the prostate gland and the neck of the bladder. After initiation of treatment, there is a gradual decrease in blood pressure, which may result in orthostatic disorders. The maximum reduction in blood pressure usually occurs after 2-6 h after drug administration in the form of tablets. There was no evidence of tolerance to antihypertensive effect of the drug during long-term treatment with doxazosin. Occasionally, an increase in plasma renin activity and tachycardia may occur during treatment. It is well absorbed from the gastrointestinal tract, reaching a maximum concentration in the blood after about 2 hours, and the absolute bioavailability is 63%. The blood pressure lowering effect of doxazosin is maintained for 24 h. It binds plasma proteins approximately 98%. It is metabolized in the liver to inactive metabolites. Less than 5% of the dose is excreted unchanged. T0,5 is 22 hours.
Contraindications:
Hypersensitivity to Doxazosin, other quinazoline derivatives or to other components of the preparation. Orthostatic hypotension. Hypotension, including history. Breastfeeding period. Patients with benign prostatic hyperplasia associated with obstruction of the upper urinary tract, chronic urinary tract infection or bladder stones. Monotherapy in patients with incontinence caused by bladder overflow or anuria with or without progressive renal failure.
Precautions:
Do not use the preparation in children. When initiating treatment and during dose escalation, patients should be closely monitored for the risk of orthostatic hypotension or syncope. In patients with severe coronary artery disease, too rapid or too great a reduction in blood pressure may exacerbate symptoms of angina. In patients on low-sodium diets and those treated with diuretics, the risk of circulatory disorders is increased. Due to the vasodilator effect, caution should be exercised when using doxazosin in patients with pulmonary edema caused by aortic or mitral valve stenosis, heart failure with high cardiac output, with right heart failure due to pulmonary embolism or pericardial effusion, with left ventricular heart failure with low pressure filling the heart. Caution should also be exercised in patients with hepatic insufficiency and patients should not be used in patients with severe hepatic impairment. Before the planned cataract surgery, the ophthalmologist should determine whether the patient is or has been treated with doxazosin, due to possible complications during the procedure (intraoperative flaccid syndrome). Patients with renal insufficiency should be monitored, especially at increasing doses. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
It must not be used during pregnancy unless clearly necessary. The use of the preparation during breast-feeding is contraindicated.
Side effects:
Common: respiratory tract infections, urinary tract infections; apathy; headache, drowsiness, dizziness (also of labyrinthine origin); palpitations, tachycardia; orthostatic disorders of blood pressure, drowsiness, edema; dyspnoea, stuffy nose, bronchitis, cough, runny nose; nausea, dyspepsia, abdominal pain, dry mouth; itching; back pain, myalgia; increasing urinary urgency, cystitis, urinary incontinence; ejaculation disorders; weakness, chest pain, flu-like symptoms, peripheral edema. Uncommon: drug allergic reactions, gout, hypokalemia, thirst, increased appetite, anorexia; nightmares, amnesia, emotional instability, agitation, depression, anxiety, insomnia, nervousness; tremors, taste disorders, cerebrovascular events, hypoestasia, fainting; lachrymation disorders, photophobia; tinnitus; myocardial infarction, angina pectoris, arrhythmia; peripheral circulation disorders; bronchospasm, laryngitis, epistaxis; lack of appetite, increased appetite, constipation, bloating, vomiting, gastroenteritis, diarrhea; increased liver enzymes; rash; muscle stiffness, joint pain; dysuria, increased urinary frequency, hematuria; impotence; site pain, generalized edema, fever, chills, swollen face, paleness, weight gain. Rare: hypoglycaemia; blurred vision; swelling of the larynx; muscle contraction, weakness in muscle strength; polyuria; lowering body temperature in the elderly. Very rare: a reduction in the number of erythrocytes, leukocytes and platelets; orthostatic dizziness, paresthesia; blurred vision; bradycardia, arrhythmia; hot flushes, increased bronchoconstriction; hepatitis, cholestasis, jaundice; urticaria, alopecia, purpura; increased urea and creatinine in the plasma, increased diuresis, disruption of urination, urination at night; gynecomastia, priapism; tiredness, bad mood. In addition: intraoperative flaccid syndrome, reverse ejaculation.
Dosage:
Orally. Adults.Hypertension: treatment starts with a dose of 1 mg per day in a single dose, then depending on the effectiveness of treatment, every 2-3 weeks the dose can be doubled, depending on the individual needs of the patient: initially up to 2 mg, then up to 4 mg once a day. The usual effective dose is 4 mg a day and a maximum of 16 mg a day. Benign prostatic hyperplasia: the treatment starts with a dose of 1 mg per day in a single dose, then depending on the effectiveness of treatment, every 1-2 weeks the dose can be doubled, depending on the individual needs of the patient: initially up to 2 mg, then up to 4 mg once a day. The average maintenance dose is 2-4 mg doxazosin per day, and a maximum of 8 mg per day.