Setegis

General characteristics. Structure:

Tablets of 1 table.
Active agent: теразозин 1   mg 2 mg 5 mg 10 mg

in the blister of 10 pieces; in a pack cardboard 3 blisters.
Description of a dosage form

Tablets on 1 mg: round, flat, white color, on one party there is an engraving "Е 451", inodorous.
Tablets on 2 mg: round, flat, yellow color, on one party there is an engraving "Е 452", inodorous.
Tablets on 5 mg: round, flat, light orange color, on one party there is an engraving "Е 453", inodorous.
Tablets on 10 mg: round, flat, orange color, on one party there is an engraving "Е 454", inodorous.

Pharmacological properties:

Pharmacological action - alpha and adrenolytic. Blocking postsynaptic alfa1-adrenoceptors of unstriated muscles of a triangle and a neck of a bladder, a proximal part of an urethra and a prostate, reduces resistance to current of urine and normalizes an urination at patients with DGPZh. Drug does not influence prostate size.
Selectively blocks peripheral postsynaptic alfa1-adrenoceptors that leads to expansion of resistive (arterial) vessels, decrease in OPSS, the ABP and an afterload on heart. The tone of capacity (venous) vessels also decreases that leads to reduction of venous return and preload of heart. Terazozin is is long to the operating HP and is effective at arterial hypertension at single oral administration in days. Prolonged treatment terazoziny usually is not followed by reflex tachycardia. It influences cordial emission, perfusion of kidneys and a glomerular filtration rate a little.

Pharmacokinetics. At intake it is quickly and almost completely soaked up from a GIT irrespective of meal. Bioavailability — 90%. After reception of the smallest dose (1 mg) Cmax in blood is reached in 1 h Terazozin is defined in a blood plasma by 36 h after reception. Linkng with proteins of plasma — 90–94%. It is metabolized generally in a liver by hydrolysis, demethylation and dealkylation with formation of 5 metabolites. T1/2 is 12 h. It is removed with urine in not changed look (10%) and in the form of inactive metabolites (30%). Through a GIT 55–60% of the accepted dose are excreted. There are no messages on possible excretion of drug with breast milk.

Pharmacodynamics. The expressed therapeutic effect develops in 3 h after intake. The anti-hypertensive effect proceeds during 24 h.

Indications to use:

DGPZh, arterial hypertension (in the form of monotherapy or as a part of a combination therapy).

Route of administration and doses:

Inside, a pill should be taken entirely, without chewing, irrespective of meal.
DGPZh: an initial dose — 1 mg of 1 times a day, supporting — 5–10 mg of 1 times a day, the maximum daily dose — 20 mg.
With a renal failure and to aged people of correction of doses it is not required to patients.
Arterial hypertension: individual selection of a daily dose for each patient is recommended. The initial daily dose makes 1 mg and is appointed to night. In order to avoid risk of development of "a phenomenon of the first dose" the initial dosage under no circumstances should not exceed 1 mg. Increase in a daily dose is carried out gradually, it is recommended to double it with an interval of 1 week before achievement of a maintenance dose. Usually maintenance dose at hypertensia — 1–5 mg of 1 times a day.

Features of use:

After the first reception of Setegis or in an initial stage of treatment there can be "a phenomenon of the first dose" which is shown by the expressed decrease in the ABP and often orthostatic hypotension (dizziness, an incoordination of movements, a syncope). Reduction of volume of liquid in an organism and limited consumption of salt increase risk of developing of postural hypotension. It is necessary to remember that the similar phenomena can arise also when resuming treatment the Setegisy ambassador of his break for several days. In such cases it is necessary to resume treatment from a dose of 1 mg.
Unconscious states arise in 1% of cases. To development of faints can bring bystry increase in a dosage after emergence of "effect of the first dose", and also Setegis's appointment into combinations with diuretics and/or other anti-hypertensive means. Unconscious states, first of all, are shown by the expressed postural hypotension, in some cases they are followed by tachycardia (120–160 blows/min.). Postural hypotension is most expressed after administration of drug within a short period of time, and the risk of emergence of an unconscious state is highest in 30–90 min. after reception. Dizziness, an incoordination of movements and unconscious states are most often provoked by change of position of a body in space, long standing, increase in an exercise stress, hot weather and the use of alcoholic beverages.
Help measures at a faint: the patient should give lying situation with the raised legs, if necessary — symptomatic therapy.
Setegis patients should appoint with care with tendency to development of orthostatic hypotension (in the anamnesis), an ischemic heart disease and other heart diseases, frustration of cerebral circulation, a hypertensive retinopathy of III or IV degrees, an insulin-dependent diabetes mellitus, a liver and/or renal failure.
Before an initiation of treatment of DGPZh it is necessary to exclude existence of a malignant new growth. At patients with DGPZh it is necessary to control the ABP level in an initiation of treatment and at change of a dose of drug in the course of treatment. It is reasonable to estimate Setegis's efficiency at DGPZh after 4–6 weeks of treatment by maintenance doses.
In an initiation of treatment and at increase in a dose of drug by the patient it is not recommended to be engaged in potentially dangerous types of activity requiring special attention and speed of psychomotor reactions (including driving of vehicles). Further, during treatment, these restrictions are set individually.

Side effects:

In an initiation of treatment emergence of "a phenomenon of the first dose" — orthostatic hypotension is possible up to an unconscious state. Besides, at treatment by Setegis there can be dizziness, a headache, an adynamy, drowsiness, a heart consciousness, nausea, a nose congestion, a vision disorder, peripheral hypostases, increase in body weight; seldom — postural hypotension, tachycardia, the hemodilution phenomena.

Interaction with other medicines:

Drug should be combined with care with other anti-hypertensive means (possibly strengthening of anti-hypertensive effect). It is recommended to lower Setegis's dose at additional inclusion in the scheme of diuretics or other anti-hypertensive drugs. In order to avoid the expressed hypotension it is reasonable to appoint additional drug in low doses under strict observation of a condition of the patient. The same rules should follow if Setegis is used as an additional tool (at the same time its initial daily dose should not exceed 1 mg).

Contraindications:

Hypersensitivity to a terazozin or other alpha adrenceptor blocking agents.

Use at pregnancy and feeding by a breast

At pregnancy and a lactation apply carefully, only after careful comparison of a ratio between risk to a fruit or the child and positive effect to mother.

Overdose:

Symptoms: arterial hypotension, lack of coordination of movements, syncope.
Treatment: giving to the patient of situation "lying with the raised legs", symptomatic therapy; for removal from state of shock it is necessary to increase OTsK with the subsequent administration of angiotonic substances. The hemodialysis is inefficient. There is no specific antidote.

Storage conditions:

Period of validity 3 years. List B.: At a temperature of 15-30 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets, 1 mg, 2 mg, 5 mg and 10 mg. According to 10 tab. in the blister from PVC/PVDH / aluminum foil. 3 blisters are packed into a cardboard pack.