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

1 tablet contains active substance: terazosin hydrochloride dihydrate (terazosin) 2.374 mg or 5.935 mg (2.00 mg or 5.00 mg); Excipients: lactose monohydrate 118.00 / 115.285 mg, starch corn 14.00 / 14.00 mg, dye quinoline yellow (E104) 1.026 mg / -, coloring iron oxide yellow (E172) - / 0.14 mg, iron oxide red dye ( E172) - / 0.04 mg, crospovidone 6.00 / 6.00 mg, povidone-KZO 2.00 / 2.00 mg, talc 5.85 / 5.85 mg, magnesium stearate 0.75 / 0.75 mg.

Description:

Tablets 2 mg: Round flat cylindrical with a bevel of a yellow colored tablet with inclusions. On one side - engraving "93", on the other - "761".

Tablets 5 mg: round cylindrical with a bevel of a yellow-brown tablet

colors (inclusions are allowed). On one side - engraving "93", on the other - "762".

Pharmacotherapeutic group:alpha1-blocker

ATX: & nbsp

G.04.C.A.03 Terazozin

Pharmacodynamics:

The blocker of peripheral postsynaptic alpha 1-adrenergic receptors.

Symptoms caused by benign prostatic hyperplasia (BPH) are associated with obstruction of the bladder outlet tract, which occurs as a result of static obstruction, due to the enlargement of 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.

By blocking alpha 1-adrenergic receptors of the smooth muscles of the prostate and bladder neck, terazosin contributes to the normalization of urination in patients with BPH.

Reduction of symptoms associated with BPH, with the use of terazosin may be associated with a decrease in muscle tone, caused by blockade of alpha] -adrenoceptors in the smooth muscles of the neck of the bladder and the prostate gland.

It causes the expansion of arterioles and venules, reduces the overall peripheral vascular resistance and venous return to the heart, resulting in decreased pre- and post-loading on the heart and blood pressure (BP). The onset of antihypertensive action 15 minutes after ingestion (single dose). The duration of antihypertensive action is 24 h.The maximum effect when taking a single dose is achieved within 2-3 hours. A persistent antihypertensive effect is achieved after 6-8 weeks of therapy. Slightly affects cardiac output, renal perfusion and glomerular filtration rate. Long-term use of terazosin usually does not cause the development of reflex tachycardia.

Terazosin promotes normalization of lipid metabolism: reduces the concentration of cholesterol, triglycerides and lipoproteins of low and very low density in the blood, while increasing the number of high density lipoproteins.

With the systematic use of terazosin, there is regression of left ventricular hypertrophy.

Pharmacokinetics:

After oral administration terazosin quickly and almost completely absorbed from the gastrointestinal tract. Eating does not affect absorption. The bioavailability of terazosin is 80-100%. For terazosin, the effect of "primary transmission" is not typical, therefore almost the entire dose of unchanged terazosin enters the systemic circulation. The maximum concentration in the blood serum is achieved within 1-2 hours after ingestion.The connection with plasma proteins is 90-94% and does not depend on the concentration of terazosin in the blood plasma.

Terazosin is metabolized in the liver by hydrolysis, demethylation and dealkylation to form 5 metabolites, one of which (the piperazine derivative of terazosin) is pharmacologically active. Approximately 60% of the dose is taken through the intestine (of which 20% is unchanged, the rest is metabolites), 40% by the kidneys (10% of them are unchanged). It is not known whether terazosin with breast milk. The half-life (T1/2) is 8-13 hours

With hepatic insufficiency the clearance of terazosin decreases.

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) showed no clear differences in the pharmacokinetic parameters of terazosin compared to patients with normal renal function.

Indications:

- Benign prostatic hyperplasia (symptomatic treatment).

Arterial hypertension (as part of combination therapy).

Contraindications:

Hypersensitivity to terazosin, other quinazolines, as well as any of the components of the drug, to other alpha-blockers; arterial hypotension; propensity to orthostatic disturbances of regulation, including in the anamnesis; severe violations of liver function; simultaneous use with phosphodiesterase-5 inhibitors (PDE5), including with sildenafil, tadalafil and vardenafil; concomitant obstruction of the upper urinary tract; chronic infectious diseases of the urinary tract or stones in the bladder; decrease in the rate of urine outflow; anuria; age to 18 years; lactose intolerance, lactase deficiency, glucose-galactose malabsorption, pregnancy and the period of breastfeeding.

Carefully:Ischemic heart disease (CHD) or other heart diseases: pulmonary edema with aortic or mitral stenosis, cardiac failure with an increase in minute release, right ventricular failure due to pulmonary embolism or exudative pericarditis, left ventricular failure with low ventricular filling pressure (see Fig.section "Special instructions"), cerebral circulation disorders, hypertensive retinopathy of III or IV degree, type 1 diabetes mellitus, mild and moderate liver function disorder; simultaneous application of terazosin with thiazide diuretics or other antihypertensive agents; renal dysfunction, elderly age over 65 years.

Pregnancy and lactation:

When pregnancy, the drug Terazozin-Teva is not recommended.

It is not known whether terazosin with breast milk. If you need to use the drug Terazozin-Teva during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside. Tablets Terazozin-Teva take whole, without chewing, washing down a glass of water, regardless of food intake. Patients are informed of the possibility of developing orthostatic hypotension and the need to take Terazosin-Teva at night before bedtime in the "sitting" or "lying" position, after which they stay in bed for 6-8 hours.

BPH (symptomatic treatment)

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

The initial dose for all patients that should not be exceeded is 1 mg (recommended terazosin in another dosage form: 1 mg tablets) once a day before bedtime, after which the patient should be in bed for 6-8 hours. When taking the first dose, you need to carefully monitor blood pressure to reduce the risk of developing orthostatic hypotension.

The dose can be increased 1-2 weeks to 2 mg once a day. In this dose, the drug Terazozin-Teva continues to be taken within 14 days; after which they switch to taking 5 mg once a day for 7 days. After four weeks from the beginning of admission, evaluate the effectiveness of the therapy. With insufficient clinical effect, the dose of Terazosin-Teva is increased to 10 mg per day. The maximum daily dose is 10 mg. The recommended maintenance dose is 5-10 mg per day.

If the use of Terazozin-Teva is interrupted for several days or more, the therapy is resumed from the initial dose.

Arterial hypertension (as part of combination therapy)

The dose and the intervals between doses (12-24 hours) of Terazosin-Teva preparation should be selected individually for each patient, in accordance with the BP reduction reaction.

The initial dose for all patients that should not be exceeded is a dose of 1 mg (recommended terazosin in another dosage form: 1 mg tablets) 1 time per day before bedtime. At the end of the period of time 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 effect of the drug Terazozin-Teva after 24 hours is significantly reduced, you can try to increase the dose or apply the drug 2 times a day. In the latter case, it should be determined whether adverse reactions such as dizziness, palpitations or orthostatic hypotension occur 2-3 hours after taking the drug.

The dose is increased gradually, doubling the dose with an interval of at least 1 week, until the desired level of blood pressure reduction is reached. Usually the maintenance dose of the drug Terazosin-Teva ranges from 2 to 10 mg per day. The maximum daily dose is 20 mg / day. If it is necessary to stop the therapy for a few days or more, resumption of reception should be started again from the initial dose (1 mg / day) with further gradual increase.

When using the drug Terazozin-Teva in addition to the already conducted antihypertensive therapy, the patient should be carefully monitored in case of arterial hypotension. When used concomitantly with thiazide diuretics or other antihypertensive drugs, it may be necessary to reduce the dose of Terazozin-Teva or even to cancel and re-titrate the dose under the supervision of the doctor.

In patients with impaired renal function correction of the dose is not required.

In elderly patients correction of the dose is not required, but regular monitoring of the patient's condition is necessary.

In patients with impaired liver function should select the daily dose with extreme caution. There is insufficient experience in using Terazosin-Teva in patients with severe hepatic insufficiency.

Side effects:

Like other alpha-blockers, terazosin can cause a syncope. Fainting can occur within 1-1,5 hours after taking the initial dose of the drug. In single cases, before a syncope, the number of cardiac contractions can sharply increase to 120-160 beats / min. After taking the first dose of the drug, a marked decrease in blood pressure may occur, which can lead to orthostatic dizziness, in severe cases - to fainting.The most typical syncopal episodes that occurred in the period of 30-90 minutes after the first dose, and also associated with a rapid increase in the dose or the use of other antihypertensive therapy.

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual reports.

From the side of the blood and lymphatic system: very rarely - thrombocytopenia.

From the cardiovascular system (SSS): often fainting (especially with a rapid change in the position of the body from the "lying" position in the "standing" position or in the "sitting" position - postural hypotension), palpitation, tachycardia, chest pain, peripheral edema, very rarely - atrial fibrillation (however, the causal relationship with taking the drug was not installed).

From the nervous system: often - dizziness, weakness, headache, asthenia, increased irritability, drowsiness, paresthesia; infrequently - depression, syncopal conditions.

From the respiratory system, chest and mediastinum: very often - nasal congestion, rhinitis, sinusitis; unknown frequency - shortness of breath.

On the part of the digestive system: often - nausea, constipation, diarrhea, vomiting.

From the sense organs: very often - visual impairment, amblyopia; often - reduced visual acuity, violation of color perception; unknown frequency - vertigo.

From the side of the musculoskeletal and connective tissue: often - pain in the back; unknown frequency - pain in the limbs.

On the part of the reproductive system: often - erectile dysfunction; infrequently - decreased libido; very rarely - priapism; unknown frequency - impotence. Allergic reactions: often - skin rash, itching; infrequently - hives, anaphylactoid reactions.

From the urinary system: often - urinary tract infections and urinary incontinence (mainly in postmenopausal women).

Other: infrequently - an increase in body weight.

In addition, there have been reports of adverse reactions during clinical trials and when used in clinical practice: influenza-like syndrome, upper respiratory tract infection, pharyngitis, urinary tract infections, anxiety, insomnia, conjunctivitis, tinnitus,arrhythmia, symptoms of vasodilation, bronchitis, cough, abdominal pain, dryness of the oral mucosa, dyspepsia, flatulence, chest pain, neck pain, shoulder pain, arthralgia, arthritis, myalgia, urinary urgency in women during menopause), angioedema, exacerbation of gout, nosebleeds, increased sweating, fever; a small but statistically significant decrease in hematocrit, hemoglobin, leukocytes, hypoproteinemia, hypoalbuminemia, which may indicate hemodilution. Treatment with terazosin for 24 months. has no significant effect on the concentration of total or free prostate-specific antigen (PSA).

A clear connection between the development of adverse reactions with the use of terazosin has not been established.

Overdose:

Symptoms: marked decrease in blood pressure, impaired coordination of movements, fainting, disturbance of water-electrolyte balance.

Treatment: gastric lavage, the use of adsorbents, symptomatic therapy. If the patient's blood pressure is significantly lowered, it is necessary to put him on his back, raise his legs, and correct the BCC. There is no specific antidote.Hemodialysis is ineffective. If necessary, vasopressor preparations are administered, correction of water-electrolyte balance, control of kidney function is performed.

Interaction:

According to the results of clinical studies, simultaneous administration of terazosin and angiotensin converting enzyme inhibitors or diuretics was accompanied by a greater incidence of symptoms of orthostatic hypotension, and other side effects. With the simultaneous use of terazosin with other antihypertensive agents, an increase in antihypertensive action is possible. With simultaneous use with thiazide diuretics or other antihypertensive drugs, it may be necessary to reduce the dose of the drug or even its elimination and repeated titration of the dose under the supervision of the doctor.

Simultaneous use of terazosin with other alpha-blockers is not recommended due to an increase in the incidence of adverse reactions.

With simultaneous use with vasodilators and nitrates, the antihypertensive effect of terazosin can be enhanced.

Absorption of terazosin decreases with simultaneous intake of adsorbents and antacids.Simultaneous use of Terazosin-Teva and PDE5 inhibitors (for example, sildenafil, tadalafil, vardenafil) may be the cause of the development of a pronounced decrease in blood pressure.

Non-steroidal anti-inflammatory drugs (especially indomethacin) and estrogens can reduce the antihypertensive effect of terazosin, due to suppression of prostaglandin synthesis and / or fluid and sodium retention.

Sympathomimetics can weaken the antihypertensive effect of terazosin (the risk of developing arterial hypotension) and weaken the vasodilating effect in response to dopamine, ephedrine, norepinephrine, metharaminol, methoxamine, and phenylephrine.

Terazosin reduces the antihypertensive effect of clonidine administered intravenously.

Special instructions:

Before the treatment of patients with BPH with Terazozin-Teva, a malignant neoplasm of the prostate or other causes leading to a delay in urine should be excluded. The effectiveness of the therapy is evaluated after 4-6 weeks of treatment with maintenance doses of the drug Terazozin-Teva. Reduction of symptoms of BPH is possible already in the second week of therapy, but the onset of therapeutic effect can last up to 6 or more weeks.

After applying the maximum recommended dose, taking Terazosin-Teva should be discontinued if the improvement in uroflowmetry is slightly different from baseline. Treatment with the drug should be discontinued if the resulting side effects are more serious than the symptoms of BPH, or if the patient develops complications from the urinary tract when taking the drug.

Regardless of the indications for which Terazosin-Teva is taken, the initial dose of Terazosin-Teva preparation should not exceed 1 mg in order to avoid the development of the "first dose effect".

To reduce the risk of developing orthostatic arterial hypotension (the "first dose effect"), the first dose of the drug Terazozin-Teva is recommended to be taken in the evening before bedtime, after which the patient should be in bed for 6-8 hours. The risk of a marked decrease in blood pressure is highest within 30-90 minutes after taking the drug, as well as increased in patients who simultaneously receive beta-blockers and diuretics, with a decrease in the volume of circulating blood, a low-salt diet, and also with the resumption of treatment with Ter azosine-Teva after a break (several days).

The patient should be informed that at the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until the state of health improves, as well as the increased risk of a pronounced decrease in blood pressure with alcohol, long-term standing or performing physical exercises, as well as at high ambient temperatures.

Caution should be exercised when using the drug Terazozin-Teva with thiazide diuretics or other antihypertensive agents; If necessary combined therapy, the dose of Terazosin-Teva is reduced. Simultaneous use of PDE5 inhibitors, including sildenafil, tadalafil, vardenafil, and Terazozin-Teva, can lead to a marked decrease in blood pressure in some patients. In order to minimize the risk of developing orthostatic hypotension, before starting the use of PDE5, it is necessary to ensure that blood pressure in the patient is stable against the background of treatment with the drug Terazozin-Teva.

The choice of maintenance dose of Terazosin-Teva in elderly patients, especially in patients with BPH at the age of more than 65 years,it is recommended to be conducted with caution under medical supervision, due to the high risk of orthostatic hypotension in this group of patients.

In connection with the manifestation of vasodilator action, the preparation Terazozin-Teva should be used with caution in patients with ischemic heart disease or other heart diseases: pulmonary edema with aortic or mitral stenosis, cardiac failure with an increase in minute release, right ventricular failure due to pulmonary artery embolism or exudative pericarditis, left ventricular insufficiency with low filling pressure of the ventricles.

In some patients who had previously taken tamsulosin, during the surgical intervention for cataracts, "intraoperative syndrome of flabby iris" (ISDR, a kind of narrow pupil syndrome) was noted. Separate reports have also been obtained with the use of other alpha1-adrenergic blockers, so the possible effect of the class of these drugs can not be ruled out.

When conducting a surgical procedure (for cataracts), it is necessary to inform the ophthalmologist about the use of blockers alpha 1 - adrenergic receptors.

When used in patients with impaired liver function, care should be taken in connection with the fact that the metabolism of terazosin is carried out in the liver. Data on the use of the drug Terazozin-Teva in patients with severe hepatic insufficiency are absent.

During treatment, the concentration of PSA does not change.

Effect on the ability to drive transp. cf. and fur:Within 12 hours after the first dose, after increasing the dose or interrupting therapy, patients are not recommended to engage in potentially hazardous activities requiring increased attention and speed of psychomotor reactions (including driving). In the future, the degree of restrictions should be set depending on the individual reaction of the patient.

Form release / dosage:

Tablets 2 mg, 5 mg.

For 10 tablets in a PVC / aluminum blister.

For 2 or 3 blisters together with instructions for use in a cardboard bundle.

Packaging:(10) - blister (2) - a pack of cardboard
(10) - blister (3) - Pack of cardboard

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000884

Date of registration:18.10.2011

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Industries, Ltd. Israel

Representation: & nbspTeva Teva Israel

Information update date: & nbsp17.09.2015

Illustrated instructions

Instructions

Terazozin-Teva (Terazosin-Teva)