Setegis tablets 5mg, No. 30

• Symptomatic therapy of benign prostatic hyperplasia;

• arterial hypertension (as monotherapy or as part of combination therapy).

Inside. The tablet should be swallowed completely without chewing.

The daily dose of the drug should be selected individually, depending on the patient's blood pressure.

Starting dose for adults

For both indications, take 1 mg at bedtime. The initial dose should not be higher than 1 mg due to the increased risk of episodes of hypotension after taking the first dose. The daily dose can be gradually increased by roughly doubling the dose at weekly intervals until the target BP is reached.

Maintenance dose for adults

Arterial hypertension: usually 2 to 10 mg once a day. Doses over 20 mg rarely improve drug efficacy; doses over 40 mg have not been studied.

BPH: The maintenance dose is usually 5Ц10 mg once daily. At present, there are no data showing an additional symptomatic effect at a dose of the drug over 10 mg / day. No dose adjustment is required in the elderly and in patients with renal impairment.

Tablets light pink (color irregularity is possible), round, flat, beveled, engraved 'E453' on one side, odorless.

1 tab.

terazosin hydrochloride dihydrate 5.935 mg,?

which corresponds to the content of terazosin 5 mg

Excipients: lactose monohydrate - 110 mg, pregelatinized corn starch - 40 mg, povidone K-30 - 5 mg, magnesium stearate - 2 mg, talc - 2 mg, sunset yellow dye - 0.01 mg.

• Arterial hypotension;

• lactation period;

• children's age (due to the lack of sufficient clinical data);

• hypersensitivity to terazosin, auxiliary components of the drug or other alpha-blockers.

• With caution, the drug should be prescribed for angina pectoris, coronary artery disease or heart failure in the stage of decompensation, renal / hepatic failure, impaired cerebral circulation, type 1 diabetes mellitus.

pharmachologic effect

Alpha1-blocker. Improves urodynamics in patients with benign prostatic hyperplasia (BPH). BPH symptoms are associated with an increase in the smooth muscle tone of the outlet of the bladder (triangle and neck of the bladder, proximal urethra) and prostate, which is controlled by ?1-adrenergic receptors. In vitro, terazosin inhibited phenylephrine-induced contractions of prostate smooth muscle. In clinical trials, terazosin improved urodynamics and relieved symptoms in patients with BPH.

Terazosin dilates arteries due to competitive antagonism with respect to postsynaptic ? 1-adrenergic receptors. It causes a gradual decrease in blood pressure, followed by a long-term antihypertensive effect.

In therapeutic doses, it reduces the content of total cholesterol in the blood by 2-5% and the sum of the concentrations of LDL cholesterol and VLDL cholesterol in the blood by 3-7% in comparison with the indicators before treatment. In addition, the increase in the concentration of total cholesterol, noted against the background of the use of other antihypertensive drugs, was not observed if terazosin was used in combination with them.

Terazosin begins to act approximately 15 minutes after the administration of a single dose, the maximum effect occurs within 2-3 hours after oral administration. Duration of action - 24 hours.

Pharmacokinetics

Suction

After oral administration, terazosin is rapidly and almost completely absorbed from the gastrointestinal tract. Food intake does not affect absorption. Slightly undergoes the effect of the 'first pass' through the liver. The bioavailability of terazosin is about 90%. Cmax is reached within 1 hour.

Distribution

Terazosin to a large extent (90-94%) binds to blood plasma proteins.

Metabolism

It is metabolized in the liver. Of the four known metabolites, only one is pharmacologically active.

Withdrawal

T1 / 2 is approximately 12 hours. Approximately 40% of the dose taken is excreted by the kidneys and 60% through the intestines.

Pharmacokinetics in special clinical situations

Renal function does not affect drug excretion. T1 / 2 does not change with impaired renal function.

Side effect

From the side of the cardiovascular system: palpitations, tachycardia, orthostatic hypotension, vasodilation. Not clearly associated with terazosin use - arrhythmia.

From the hematopoietic system: thrombocytopenia.

Mental disorders: decreased libido, depression, increased anxiety. Not clearly associated with terazosin use - anxiety, insomnia.

From the nervous system: fainting, dizziness, drowsiness, headache, paresthesia.

From the side of the organ of vision: visual impairment, amblyopia, in the case of cataract surgery in patients receiving ? 1-blockers, intraoperative iris instability syndrome (IFIS) was noted. Not clearly associated with the use of terazosin - atypical vision, conjunctivitis.

On the part of the organ of hearing and balance: dizziness. Not clearly associated with terazosin use - ringing in the ears.

From the respiratory system: nasal congestion, rhinitis, shortness of breath, sinusitis. Not clearly associated with the use of terazosin - bronchitis, epistaxis, cold symptoms, pharyngitis, increased cough.

From the digestive system: nausea. Not clearly associated with the use of terazosin - abdominal pain, constipation, diarrhea, dry mouth, dyspepsia, flatulence, vomiting.

From the urinary system: not clearly associated with the use of terazosin - an increase in the frequency of urge to urinate, urinary tract infections and involuntary urination in postmenopausal women.

On the part of the genitals and mammary gland: impotence, priapism.

On the part of the skin and subcutaneous tissues: not clearly associated with the use of terazosin - itching, rash, increased sweating.

From the musculoskeletal system: back pain, pain in the limbs. Not clearly associated with terazosin use - neck pain, shoulder pain, arthralgia, arthritis, joint disease, myalgia.

From the endocrine system: an increase in body weight. Not clearly associated with terazosin use - gout.

Others: asthenia, peripheral edema, edema. Not clearly associated with terazosin use - chest pain, facial swelling, fever.

Allergic reactions: anaphylactoid reaction.

Laboratory indicators: In studies, there was a small but statistically significant decrease in hematocrit, hemoglobin, leukocytes, total protein and albumin. These laboratory data indicate the ability to hemodilute. Treatment with terazosin for up to 24 months did not have a significant effect on the level of prostate-specific antigen (PSA).

Application during pregnancy and lactation

Due to the lack of clinical data on the use of terazosin during pregnancy and lactation, it is possible to use the drug during pregnancy only if the intended benefit to the mother outweighs the potential risk to the fetus. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Application for violations of liver function

The drug should be prescribed with caution to patients with impaired liver function.

Application for impaired renal function

No dose adjustment is required in patients with renal insufficiency .

The drug should be prescribed with caution to patients with impaired renal function.

Application in children

Contraindication: childhood.

Use in elderly patients

Elderly patients do not need dose adjustment. In elderly patients, the sensitivity to the hypotensive effect of terazosin may be increased.

special instructions

Like other alpha-blockers, terazosin is not recommended for patients with a history of fainting during urination.

After the first dose and the first days of therapy, the 'first dose' effect may develop: an excessive decrease in blood pressure, in particular, orthostatic hypotension (with dizziness, a feeling of loss of consciousness, fainting). Hypovolemia and salt restriction increase the risk of a 'first dose' effect. The same phenomenon can be observed when the treatment is resumed after a few days of interruption, therefore, in such cases, the initial dose should be reapplied. The incidence of syncope is approximately 1% of cases. In addition to the 'first dose' effect, increasing the dose too quickly and simultaneously using diuretics and other antihypertensive drugs can also cause fainting. Fainting is usually due to severe orthostatic hypotension, but it can also be associated with tachycardia (120-160 bpm).Orthostatic hypotension is most pronounced shortly after taking the drug, and the risk of fainting is highest between 30 and 90 minutes after taking the drug. Changing positions from a horizontal or sitting position, prolonged standing in a standing position, intense physical activity, high ambient temperatures and the simultaneous intake of alcohol can provoke dizziness, a feeling of insecurity, or even loss of consciousness. In case of fainting, the patient should be laid down with raised lower limbs, and, if necessary, symptomatic therapy should be initiated. When using terazosin in conjunction with diuretics and / or other antihypertensive agents, it is recommended to reduce its dose.In order to avoid severe hypotension, it is recommended to start the course of treatment with a concomitant drug also with low doses and to conduct careful medical monitoring of the patient. The same precautions are required when adding terazosin to ongoing diuretic or antihypertensive therapy. The initial dose of terazosin in these cases is also 1 mg.

In elderly patients, the sensitivity to the hypotensive effect of terazosin may be increased. The use of terazosin requires special care in patients with a predisposition to orthostatic hypotension, coronary artery disease, other severe heart diseases, cerebrovascular accident, grade III or IV hypertensive retinopathy, insulin-dependent diabetes, as well as impaired liver and kidney function. Before starting treatment with terazosin for benign prostatic hyperplasia, prostate carcinoma should be excluded. The patient's blood pressure should be measured regularly at the beginning of treatment for prostatic hypertrophy with terazosin, in the case of additional therapy, with an increase in the dose; you should also take into account the concomitant use of antihypertensive drugs.The efficacy of terazosin in benign prostatic hyperplasia should be assessed only after 4-6 weeks of using the drug in a maintenance dose.

During cataract surgery, patients who have previously received alpha1-blockers have a syndrome of intraoperative iris instability (IFIS). This phenomenon is a variant of Narrow Pupil Syndrome, in which the iris relaxes to the extent that it becomes unstable when irrigated. Despite the preoperative dilatation of the pupil, as a rule, with the help of mydriatic agents, miosis intensifies, and the iris sags towards the phacoemulsification incisions. In such cases, the operating surgeon should be prepared to change the technique of the operation, it may be necessary to use an iris hook, an iris retractor and viscoelastic materials. Preoperative interruption of therapy with? 1-blockers does not have an advantage over the continuation of therapy.

The tablets contain lactose monohydrate (55 mg or 110 mg), therefore, patients with galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not take SetegisЃ.

Influence on the ability to drive vehicles and use mechanisms

Dizziness, loss of consciousness and fainting may occur, especially in the first days of taking the drug, with an increase in the dose or with the resumption of therapy with SegetisЃ. Patients should be warned of possible side effects and situations where they may appear, and patients should also be advised to refrain from driving vehicles or engaging in potentially hazardous activities for about 12 hours after taking the initial dose or when the dose is increased. Later in the course of treatment, the degree of restriction should be set for each patient individually.

Overdose

Treatment: in case of severe hypotension, peripheral circulatory insufficiency, it is first of all important to transfer the patient to the supine position with the head of the bed lowered. In the event of shock, it is necessary to prescribe plasma-substituting agents, then vasopressors. Water and electrolyte balance should be maintained. Dialysis may be ineffective because terazosin binds to plasma proteins to a large extent.

Drug interactions

According to clinical studies, in patients with BPH receiving tarazosin in combination with an ACE inhibitor or diuretics, the proportion of dizziness or associated side effects was higher than in the general population of patients receiving terazosin.

Special precautions should be taken when terazosin is used with other antihypertensive drugs to prevent significant hypotension. When terazosin is added to therapy with diuretics or antihypertensive drugs, it may be necessary to reduce or re-titrate the dose.

Adsorbents and antacids reduce absorption.

Adrenostimulants weaken the effect.

NSAIDs (especially indomethacin) can reduce the hypotensive effect due to suppression of Pg synthesis and / or fluid and Na + retention.

There are reports of hypotension while taking terazosin with PDE-5 inhibitors. Concomitant treatment with terazosin and sildenafil or vardenafil should be started if the patient's condition is stable while taking terazosin. In addition, vardenafil should not be taken within 6 hours of terazosin, and sildenafil should not be taken within 4 hours of terazosin.