Setegis, tablets 5 mg 30 pcs

Setegis is an alpha-adrenolytic.

Pharmacodynamics

The α1-adrenoreceptor antagonists improve urodynamics in patients with BPH. The symptoms of BPH are associated with increased tone of smooth muscles of the bladder outlet region (bladder triangle and neck, proximal part of urethra) and prostate, which are controlled by α1-adrenoreceptors. In vivo terazosin inhibited human prostate smooth muscle contractions induced by phenylephrine. In clinical studies terazosin improved urodynamics and eliminated symptoms in patients with BPH.

Therazosin dilates arteries due to competitive antagonism to postsynaptic α1-adrenoreceptors. Terazosin causes a gradual decrease in BP with a subsequent long-term antihypertensive effect.

Terazosin in therapeutic doses decreases total blood cholesterol by 2-5% and the sum of LDL cholesterol and LDL cholesterol concentrations of blood by 3-7% compared to the rates before treatment. In addition, the increase in total cholesterol levels observed against the background of taking other antihypertensive drugs was not observed if terazosin was used in combination with them.

Pharmacokinetics

Therazosin is rapidly and almost completely absorbed from the gastrointestinal tract regardless of food intake. It has very little effect of first passage through the liver. Its bioavailability is close to 90%. Terazosin is largely (90-94%) bound to blood plasma proteins. It is metabolized in the liver; of the four known metabolites only one is pharmacologically active. T1/2 is approximately 12 h without significant change even with impaired renal function.

Therazosin starts to act about 15 min after a single dose, Cmax in blood plasma is reached within 1 h, and the maximum effect occurs 2-3 h after oral administration. Duration of action is 24 hours. About 40% of the taken dose is excreted by the kidneys and 60% – through the intestine. Renal function does not affect excretion of the drug.

Indications

Symptomatic treatment of benign prostatic hyperplasia (BPH); arterial hypertension (as monotherapy or in combination with other hypotensive drugs).

Active ingredient

Composition

Active ingredient:

terazosin 5 mg;

Associates:

Lactose monohydrate;

Pregelatinized corn starch;

Povidone K30;

Magnesium stearate;

Talc.

How to take, the dosage

To be taken orally, Setegis tablets should be taken whole, without chewing, regardless of meals.

PAD: initial dose is 1 mg once daily, maintenance dose is 5-10 mg once daily, maximum daily dose is 20 mg.

Interaction

The simultaneous use of Setegis with other antihypertensive drugs may increase the antihypertensive effect.

Special Instructions

After the first drug administration or during the first days of treatment, a “first dose effect” may occur: a marked drop in BP, mainly in the form of orthostatic hypotension with dizziness, insecurity, and fainting. Hypovolemia and salt restriction increase the risk of the “first dose effect”.

The same phenomenon can occur when treatment is resumed after several days of interruption, so treatment should be resumed using the starting dose.

Fainting occurs in about 1% of cases. In addition to the “first dose effect,” increasing the dose too rapidly and using diuretics and other antihypertensive medications at the same time can also cause syncope. Fainting is primarily due to marked orthostatic hypotension, but may be associated with tachycardia (120-160 bpm).

Orthostatic hypotension is most pronounced shortly after drug administration, and the risk of fainting is highest between 30 and 90 minutes. Standing up from a horizontal or sitting position, prolonged standing up, intense physical exertion, high ambient temperature, and the simultaneous ingestion of alcohol may provoke dizziness, uncertainty, or even loss of consciousness. If a patient faints, they should be laid down, elevate their legs, and use other supportive measures if necessary.

When using Setegis together with diuretics and/or other antihypertensive agents, it is recommended to reduce its dose. In order to avoid the development of severe arterial hypotension, it is recommended to prescribe the concomitant drug in a low dose and to monitor the patient carefully. The same precautions are required when adding Setegis to current antihypertensive therapy. The starting dose of Setegis in these cases is also 1 mg.

Elderly patients may be more sensitive to the hypotensive effects of terazosin.

Patients with predisposition to orthostatic hypotension, in CHD or other heart diseases, cerebral circulatory disorders, grade III or IV hypertensive retinopathy, insulin-dependent diabetes, and liver and renal function disorders should prescribe the drug with caution.

Before starting treatment with Setegis of benign prostatic hyperplasia, malignant neoplasm of the prostate must be excluded. If the drug is administered to patients with benign prostatic hyperplasia, BP should be monitored at the beginning of treatment and when changing the dose during therapy. The efficacy of Setegis in this disease is evaluated after 4 to 6 weeks of treatment with maintenance doses.

In case of lactose intolerance, consider the lactose content of the tablets (55 mg in each 1 mg tablet, 110 mg in each 2 mg tablet, 5 mg and 10 mg tablets).

Pediatric use

The efficacy and safety of the drug in children have not been established.

Impact on driving and operating machinery

At the beginning of treatment and when increasing the dose of the drug, patients are advised not to engage in potentially hazardous activities requiring increased attention and quick psychomotor reactions (including driving vehicles) for a period of time, the duration of which is determined individually. Thereafter the degree of restriction should be determined depending on the individual reaction of the patient.

Contraindications

With caution: angina pectoris, CHD or decompensated heart failure, renal/liver failure, impaired cerebral circulation, type I diabetes.

Side effects

In the beginning of treatment, “first dose phenomenon” – orthostatic hypotension up to and including fainting – may occur.

In addition, during treatment with Setegis dizziness, headache, asthenia, somnolence, palpitations, nausea, nasal congestion, visual disturbances, peripheral edema, weight gain may occur; rarely – postural hypotension, tachycardia, hemodilution phenomena.

Overdose

Symptoms: arterial hypotension, impaired coordination of movements, fainting.

Treatment: the patient should be put in horizontal position with elevated legs. Symptomatic therapy is carried out. There is no specific antidote. Hemodialysis is ineffective, because terazosin is highly bound to blood plasma proteins. In case of shock it is necessary to increase the blood circulation with subsequent administration of vasopressor drugs.

Pregnancy use

Setegis is contraindicated in pregnancy, lactation and childhood.

Similarities