Expiration date: 07/2025
Clinico-pharmacological group
01.008 (alpha1-blocker. The antihypertensive drug. The drug is used in violation of urination in benign prostatic hyperplasia)
pharmachologic effect
Selective competitive blocker of postsynaptic ?1-adrenergic receptors. It is the expansion of peripheral blood vessels, which leads to a decrease in peripheral vascular resistance and reduction in blood pressure. Promotes ratio of HDL / total cholesterol, reduce total triglycerides and cholesterol.
With prolonged use of observed regression of left ventricular hypertrophy, inhibition of platelet aggregation occurs and the elevation of tissue plasminogen activator. ?1-adrenoceptor blockade, located in the stroma and prostatic capsule, bladder neck results in a decrease in pressure resistance and urethra resistance reduction in its internal bore. Improves urodynamics and reduces symptoms of benign prostatic hyperplasia.
Pharmacokinetics
After oral administration, it is well absorbed from the gastrointestinal tract. Cmax in plasma achieved through 1.5-3.6 h. Plasma protein binding is 98-99%. Intensively metabolized in the liver. T1 / 2 of 19-22 hours is derived mainly through the intestine in the form of metabolites, 5% -. Unchanged in 9% excreted by the kidneys.
To the begining
Dosage
The initial dose is 1 mg / day. After 1-2 weeks, depending on the clinical situation, the dose may be increased to 2 mg / day, and then after 1-2 weeks - up to 4 mg, 8 mg, or 16 mg / day to achieve the optimal therapeutic effect. On average, the daily dose is 2-4 mg.
Maximum dose: 16 mg / day.
Drug interactions
In an application with antihypertensive agents may mutual reinforcement effects.
While the use of calcium channel blockers there is a certain risk of severe arterial hypotension.
In an application with nitrates, funds for general anesthesia, tricyclic antidepressants, ethanol may increase the hypotensive effect.
With simultaneous use of drugs which affect the rate of metabolism in the liver, possibly slowing down or speeding up the metabolism of doxazosin.
Pregnancy and lactation
There are no adequate and well-controlled studies safety of doxazosin during pregnancy and lactation (breastfeeding) was conducted. Application is possible only in cases where the potential benefit to the mother outweighs the potential risk to the fetus or child.
Side effects
Since the cardiovascular system: orthostatic reactions (including syncope), tachycardia, arrhythmias, peripheral edema.
From the digestive system: nausea.
CNS: dizziness, headache, fatigue, irritability, fatigue, drowsiness.
Other: Rhinitis.
testimony
Arterial hypertension. Benign prostatic hyperplasia (symptomatic treatment).
Contraindications
Hypersensitivity to the quinazoline derivative.
special instructions
To use caution in the human liver.
After receiving the initial dose of doxazosin may develop orthostatic hypotension (first dose phenomenon), particularly in a standing position. Often this condition is seen in patients with hypovolemia, sodium deficiency in the elderly. In this regard, it is recommended to take an initial dose before bedtime.
Clinical experience with doxazosin have no children.
Effects on ability to drive vehicles and management mechanisms
Between receiving doxazosin, especially early in treatment, care should be taken when performing work that requires high speed of psychomotor reactions, because of the possible development of drowsiness, dizziness.
Application for violations of liver function
To use caution in the human liver.