Setegis, tablets 2 mg 30 pcs

Setegis is an alpha-adrenolytic.

Pharmacodynamics

The α₁-adrenoceptor antagonists improve urodynamics in patients with BPH. The symptoms of BPH are associated with increased tone of the smooth muscles of the bladder outlet (bladder triangle and neck, proximal 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 through competitive antagonism to postsynaptic α₁ adrenoreceptors. Terazosin causes a gradual decrease in BP with a subsequent long-term antihypertensive effect.

Terazosin in therapeutic doses reduces total blood cholesterol by 2-5% and the sum of LDL cholesterol and LDL cholesterol concentrations of blood by 3-7% compared to the pre-treatment values. 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. T_1/2 is approximately 12 h without significant change even with impaired renal function.

Therazosin begins to act approximately 15 min after a single dose, C_max in plasma is reached within 1 h, and 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 the excretion of the drug.

Indications

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

Pharmacological effect

Setegis is an alpha-adrenolytic.

Pharmacodynamics

α1-adrenergic receptor antagonists improve urodynamics in patients with BPH. Symptoms of BPH are associated with increased tone of the smooth muscles of the bladder outlet (triangle and bladder neck, proximal urethra) and prostate, which is controlled by α1-adrenergic receptors. In vitro, terazosin inhibited phenylephrine-induced contractions of human prostate smooth muscle. In clinical studies, terazosin improved urodynamics and relieved symptoms in patients with BPH.

Terazosin dilates arteries due to competitive antagonism of postsynaptic α1-adrenergic receptors. Terazosin causes a gradual decrease in blood pressure followed by a long-term antihypertensive effect.

Terazosin in therapeutic doses reduces total blood cholesterol by 2–5% and the sum of LDL cholesterol and VLDL cholesterol concentrations in the blood by 3–7% compared to pre-treatment values. In addition, the increase in total cholesterol levels observed with other antihypertensive drugs was not observed when terazosin was used in combination with them.

Pharmacokinetics

Terazosin is quickly and almost completely absorbed from the gastrointestinal tract, regardless of food intake. Has very little first pass effect through the liver. Its bioavailability is close to 90%. Terazosin is highly (90–94%) bound to plasma proteins. Metabolized in the liver; of the four known metabolites, only one is pharmacologically active. T1/2 is approximately 12 hours without significant changes, even with impaired renal function.

Terazosin begins to act approximately 15 minutes after taking a single dose, Cmax in blood plasma is achieved within 1 hour, and the maximum effect occurs 2-3 hours after oral administration. Duration of action is 24 hours. Approximately 40% of the dose taken is excreted by the kidneys and 60% through the intestines. Renal function does not affect the elimination of the drug.

Special instructions

After the first dose of the drug or in the first days of the course of treatment, a “first dose effect” may occur: a pronounced drop in blood pressure, mainly in the form of orthostatic hypotension with dizziness, a feeling of uncertainty and fainting. Hypovolemia and salt restriction increase the risk of a “first dose effect.” The same phenomenon can be observed when resuming treatment after a few days of break, so treatment should be resumed using the initial dose.
Fainting occurs in approximately 1% of cases.

In addition to the “first dose effect,” increasing the dose too quickly and concomitant use of diuretics and other antihypertensive drugs can also cause syncope. Fainting is primarily due to severe orthostatic hypotension, but may be associated with tachycardia (120-160 beats/min). Orthostatic hypotension is most pronounced soon after dosing, and the risk of syncope is highest between 30 and 90 minutes.

Rising from a horizontal or sitting position, standing for long periods of time, intense physical effort, high ambient temperatures and the simultaneous consumption of alcohol can cause dizziness, a feeling of uncertainty or even loss of consciousness. If the patient faints, lie down, elevate the legs, and, if necessary, apply other supportive therapy measures.

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

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

The drug should be prescribed with caution to patients with a predisposition to orthostatic hypotension, with ischemic heart disease or other heart diseases, cerebrovascular accidents, grade III or IV hypertensive retinopathy, insulin-dependent diabetes mellitus, impaired liver and kidney function.

Before starting treatment with Setegis for benign prostatic hyperplasia, malignant neoplasm of the prostate should be excluded. When prescribing the drug to patients with benign prostatic hyperplasia, blood pressure should be monitored at the beginning of treatment and when changing the dose during therapy. The effectiveness of Setegis for this disease is assessed after 4-6 weeks of treatment with maintenance doses.

If you are lactose intolerant, you should take into account its content in the tablets (55 mg in each 1 mg tablet, 110 mg in each 2 mg, 5 mg and 10 mg tablet).

Use in pediatrics

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

Impact on the ability to drive vehicles and operate machinery

At the beginning of treatment and when increasing the dose of the drug, patients are not recommended to engage in potentially hazardous activities that require increased attention and speed of psychomotor reactions (including driving) for a period of time, the duration of which is determined individually.

In the future, the degree of restrictions should be set depending on the individual response of the patient.

Active ingredient

Terazosin

Composition

Active ingredient:

terazosin 2 mg;

Excipients:

lactose monohydrate;

pregelatinized corn starch;

povidone K30;

magnesium stearate;

talc.

Pregnancy

Setegis is contraindicated during pregnancy, breastfeeding and childhood.

Contraindications

hypersensitivity to the active substance or to any other structural analogues of α-adrenergic receptor antagonists, or to excipients;
arterial hypotension;
lactation period;
children’s age (due to the lack of sufficient clinical data).

With caution: angina pectoris, coronary artery disease or heart failure in the stage of decompensation, renal/liver failure, cerebrovascular accident, type I diabetes mellitus.

Side Effects

At the beginning of treatment, a “first dose phenomenon” may occur – orthostatic hypotension up to fainting.

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

Interaction

When Sethegis is used simultaneously with other antihypertensive drugs, the antihypertensive effect may be enhanced.

Overdose

Symptoms: arterial hypotension, loss of coordination, fainting.

Treatment: the patient should be placed in a horizontal position with raised legs.

Symptomatic therapy is carried out.

There is no specific antidote. Hemodialysis is ineffective because Terazosin is highly bound to plasma proteins.

When shock develops, it is necessary to increase the volume of blood volume followed by the introduction of vasopressor drugs.

Storage conditions

At 15–30 °C

Shelf life

3 years

Manufacturer

EGIS, Hungary