Terazozin - instructions for use, dose, side effects, contraindications

Excipients: starch - 9.87 mg, anhydrous anhydrous 117.0 mg magnesium stearic acid - 1.0 mg, microcrystalline cellulosePH 102 - 19.5 mg, dye quinoline yellow aluminum varnish 40% (E 104) - 0.04 mg, dye sunset yellow aluminum varnish 40% (E 110) - 0-1 mg.

1 tablet of 5 mg contains:

active substance: terazosin guidedihydrogen chloride in terms of terazosin 5 mg;

Excipients: starch - 9,85 mg, anhydrous lactose - 113,4 mg, magnesium stearic acid 1.0 mg, microcrystalline cellulose PH 102 19.5 mg, iron dye (II) oxide (E 172) - 0.03 mg, dyesIron (III) oxide red (orange hue No. 34690) (E 172) -0.27 mg.

Description:

Tablets 2 mg: round, flat, with beveled edges tablets pink with orange shade of color. On one side is engraved "NU" or "APO", or "PRO", on the other side - "T2". Marble is allowed.Tablets 5 mg: round, flat, with beveled edges of a tablet of light brown with a pink shade of color. On one side is engraved "NU" or "APO", or "PRO", on the other side - "T5". Marble is allowed.

Pharmacotherapeutic group:alpha1-adrenoblocker.

ATX: & nbsp

G.04.C.A.03 Terazozin

Pharmacodynamics:

Benign prostatic hyperplasia (BPH)

Symptoms caused by BPH are associated with obstruction of the bladder outlet tract, which occurs as a result of static obstruction, due to an increase in the prostate gland, and dynamic obstruction, which depends on the tone of the smooth muscles of the prostate and the neck of the bladder controlled by the sympathetic nervous system.

The stimulation of alpha 1-adrenergic receptors in the smooth muscles of the bladder neck and the prostate gland results in smooth muscle contraction and an increase in muscle tone.

Reduction of symptoms associated with BPH, with the appointment of Terazozin, may be associated with a decrease in muscle tone caused by the blockade of alpha 1-adrenergic receptors in the smooth muscles of the neck of the bladder and prostate.

Arterial hypertension

The antihypertensive effect of Terazosin is a direct consequence of peripheral vasodilation. The exact mechanism of lowering blood pressure (BP) is unknown, vascular relaxation, apparently, is caused mainly by a selective blockade of postsynaptic alpha 1-adrenergic receptors.

The blood pressure decreases both in the prone position and in the standing position. In clinical studies, the degree of BP reduction was measured at the end of the interval between doses (24 hours). A decrease in blood pressure was revealed both in a prone position of 5-10 mm Hg. (systolic) and 3.5 - 8 mm Hg. Art. (diastolic). Decrease in blood pressure in the standing position was more by 1-3 mm Hg. Art.

Measurements of the greatest (maximum) decrease in blood pressure (2-3 hours after ingestion) with prolonged use of Terazozin indicate that this decrease is somewhat greater than the overall decrease in blood pressure (within 24 hours), which indicates a decrease in hypotensive effect in 24 hours , presumably due to a decrease in the concentration of Terazosin in the blood at the end of the interval between doses.

A more pronounced effect on blood pressure, related to the maximum concentration in the blood plasma, depends more on the position of the body (more in the standing position),than the action of Terazosin after 24 hours; in the standing position in the first few hours after taking the drug, there was also an increase in the heart rate (heart rate) by 6-10 beats per minute. During the first 3 hours after admission, 12.5 % patients systolic blood pressure decreased by 30 mm Hg. Art.

Pharmacokinetics:

Therasozin is rapidly and completely absorbed when ingested. Food has almost no effect on bioavailability. Free base level in blood plasma reaches a maximum for about 1 hour, and then decreases with a half-life of approximately 12 hours. About 90-94% of the drug binds to blood plasma proteins. It is excreted mainly with bile (60%) and kidneys (40%, 10 of them % in unchanged form).

Indications:

Benign prostatic hyperplasia - as a symptomatic therapy.

Arterial hypertension.

Contraindications:

Hypersensitivity to terazosin and other alpha-adrenergic blocking agents, lactation, age under 18 years (efficacy and safety not established), arterial hypotension.

Carefully:renal and / or hepatic insufficiency, advanced age, angina pectoris, CHD or other decompensated diseases of the cardiovascular system, impaired cerebral circulation, type 1 diabetes mellitus.

Pregnancy and lactation:

Terazosin is not recommended for use in pregnancy, unless the potential benefit from its use is greater than the potential risk to the fetus and / or child.

It is not known whether Terazozin with breast milk. In connection with the possibility of side effects in infants, if you need to take the drug by nursing mothers, you should consider ending breastfeeding.

Dosing and Administration:

Benign prostatic hyperplasia (BPH)

The dose of Terazosin should be selected based on the patient's individual response to the therapy.

Initial dose

The initial dose for all patients that should not be exceeded during the first week is 1 mg at bedtime. It is necessary to strictly monitor the patient when prescribing the drug (the risk of developing acute arterial hypotension).

Subsequent doses

The dose should be gradually increased at intervals of one week to 2 mg, 5 mg, or 10 mg once a day to achieve the desired reduction in symptoms and / or rate of outflow (as the urologists say) urine.Usually, to achieve a therapeutic effect, maintenance doses of 5-10 mg per day are required once a day. Duration of treatment and dosage of the drug should be carefully titrated. In order to achieve a statistically significant improvement in the objective parameters of the rate of urinary outflow, it may take 4 weeks for Terazosin. Symptom reduction may occur as early as the second week, but may last up to 6 or more weeks. In some patients, the clinical effect may not occur, despite a thorough titration of the dose of the drug. After 18 months of therapy, the patient's clinical condition must be re-evaluated completely.

After the appointment of the maximum recommended dose, the use of Terazosin should be discontinued if the improvement in urofluometrics slightly differs from the baseline or improvement in the American Association of Urology (AUA) does not affect the quality of life. Treatment

Terazosin should be discontinued if the side effects are more severe than BPH symptoms, or if the patient develops complications from the urinary tract during the administration of Terazosin.

If Terazosin is discontinued for several days or more, therapy should be resumed from the initial dose.

Arterial hypertension

The dose and intervals between doses (12-24 hours) of Terazosin should be selected according to the BP reduction response for each patient individually.

When Terazosin is prescribed for already antihypertensive therapy, the patient should be carefully monitored in case of arterial hypotension. If a diuretic or other antihypertensive agent is added to the therapy plan for Terazosin, it may be necessary to reduce the dose of Terazosin and re-titrate it under the supervision of the doctor.

Initial dose

The initial dose for all patients that should not be exceeded is 1 mg at bedtime. It is necessary to monitor the patient in order to reduce the risk of a pronounced decrease in blood pressure.

Subsequent doses

The dose can be gradually increased in order to achieve the desired decrease in blood pressure. The usual dosage ranges from 1 mg to 5 mg once a day. For some patients, a dose of 20 mg per day is sufficient. This dose is the maximum recommended daily dose.

At the end of the interval between doses, blood pressure should be measured in order to be sure of maintaining the proper blood pressure level. It may also be useful to measure blood pressure 2 or 3 hours after taking the drug in order to make sure that the decrease in blood pressure is stable.

If the action of Terazosin significantly decreases after 24 hours, you can try to increase the dose or prescribe the drug twice a day. In the latter case, you should also find out whether side effects such as dizziness, palpitation, or orthostatic hypotension are observed 2 to 3 hours after taking the drug.

If admission Terazozina interrupted for several days or more, therapy should be restarted from the initial dose of the drug.

Side effects:

The most serious side effect was syncope, occurring in 1% of patients.

The most common side effects were: dizziness (18.8%), headache (14.1%), asthenia (11%), drowsiness (4.8%), nasal obstruction (4.6%), tachycardia (4, 6%).

Other; fever, neck pain, shoulder pain, atrial fibrillation (however, the cause-and-effect relationship with the drug was not established), constipation, flatulence, anxiety, bronchitis,nasal bleeding, flu-like symptoms, conjunctivitis, priapism, urinary tract infections, urinary incontinence (mainly in postmenopausal women), arthralgia, arthritis, myalgia, peripheral edema, nausea, decreased potency, impaired vision, decreased hematocrit, hemoglobin , hypoproteinemia, hypoalbuminemia, impaired clarity of visual perception. There are reports of thrombocytopenia, gout.

The most frequent side effects, manifested with the discontinuation of Terazosin, were dizziness (3.5%), asthenia (2.1%), headache (1.7%).

Overdose:

Symptoms: marked decrease in blood pressure, impaired coordination of movements, fainting.

Treatment: symptomatic therapy, maintenance of cardiovascular system. Hemodialysis is ineffective.

Interaction:

Beta-adrenoblockers, diuretics, nitrates, blockers of "slow" calcium channels, sympatholytics, angiotensin-converting enzyme (ACE) inhibitors, ethanol, alprostadil, levodopa, local anesthetics, antidepressants, antipsychotics (neuroleptics), muscle relaxants (baclofen and tizanidine) increase the hypotensive effect of terazosin.

Simultaneous appointment of Terazosica and verapamil to patients with arterial hypertension resulted in a significant increase in the area under the curve (AUC) maximum and minimum concentrations of Terazosin. The pharmacokinetics of verapamil did not change. Symptomatic arterial hypotension, tachycardia were observed. Therefore, caution should be exercised while prescribing these medicines at the same time.

Anxiolytics and hypnotics cause an increase in hypotensive and sedative action.

Glucocorticosteroids cause a weakening of the hypotensive effect. Estrogens and combined oral contraceptives - weaken the hypotensive effect.

Non-steroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin) can cause a decrease in the hypotensive effect due to the suppression of the synthesis of prostaglandins and / or fluid and sodium retention.

Adsorbents and antacids reduce the absorption of the drug.

Special instructions:

To prevent the development of the "first dose" phenomenon, treatment should begin with a minimum effective dose (1 mg / day before bedtime), after which the patient should be in bed for 6-8 hours.

The risk of orthostatic hypotension (the phenomenon of the "first dose") is highest for 30-90 min. after taking the drug and increased in patients who simultaneously receive beta-blockers and diuretics, with a decrease in fluid volume in the body, hypo-salt diet, as well as with the resumption of treatment with the drug after a break (several days).

In the event of a temporary cessation of treatment, the therapy is resumed with the same dose.

During treatment, the concentration of a specific antigen of the prostate gland (PSA).

Before starting therapy for benign prostatic hyperplasia, prostate cancer should be excluded. The effectiveness of the therapy for this disease is evaluated after 4-6 weeks of treatment with maintenance doses.

The patient should be informed of the increased risk of developing orthostatic hypotension with alcohol, prolonged standing or exercise, and in hot weather.

Within 12 hours after taking the first dose, after increasing the dosage or discontinuing therapy, care should be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Application in elderly patients

Terazozin should be used with caution in elderly patients in connection with the possibility of developing orthostatic hypotension. With age, the risk of dizziness, visual impairment and fainting increases in elderly patients taking Terazozin. Patients over 75 years of age can have only a slight positive effect of treatment with this drug.

Use in patients with impaired renal function

The use of Terazosin in patients with impaired renal function requires careful monitoring of the patient's condition. Limited low-dose pharmacokinetic studies (1 mg) did not show any significant differences in the pharmacokinetics of Terazosin compared to patients with normal renal function. Approximately 40% of the ingested Terazosin is secreted by the kidneys in unchanged form or in the form of metabolites.

Form release / dosage:

Tablets of 2 mg and 5 mg.

10, 14, 20, 28, 30, 50 and 100 tablets in high-pressure polyethylene bottles. 1 bottle with instructions for use in a cardboard pack.

By 7, 10, 14, 20, 30 and 50 tablets in a contoured cell packaging made of polyvinylchloride film and aluminum foil printed lacquered. 1, 2, 3, 4, 5 contour packs of 7, 10, 14 and 20 tablets; 1, 2, 3 contour packs of 30 tablets; 1, 2 contour packs of 50 tablets together with instructions for use in a cardboard bundle.

Packaging:(1) - polyethylene bags (1) - plastic drums
(1) - polyethylene bags (1) - plastic containers
(100) - polyethylene bottles
(100) - polyethylene bottles - cardboard boxes
(1000) - polyethylene bottles
(1000) - polyethylene bottles - cardboard boxes
(500) - polyethylene bottles
(500) - polyethylene bottles - cardboard boxes

Storage conditions:

In dry, the dark place at a temperature of 15 to 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014281 / 01

Date of registration:22.10.2008

The owner of the registration certificate:New Farm Inc.New Farm Inc.

Manufacturer: & nbsp

New Farm Inc. Canada

Representation: & nbspVECTOR-MEDICA CJSC VECTOR-MEDICA CJSC Russia

Information update date: & nbsp18.09.2015

Illustrated instructions

Instructions

Terazozin (Terazosin)