Pharmacological properties of the drug Setegis
Terazosin (2-[4-tetrahydrofuranylcarbonyl)-1-piperazinyl]-6,7-dimethoxy-4-quinazolinamine monohydrochloride dihydrate). Terazosin is a selective α1-adrenergic receptor blocker. Its antihypertensive effect is due to the blockade of postsynaptic α1-adrenergic receptors, which leads to vasodilation, a decrease in peripheral vascular resistance and a decrease in venous return. Terazosin is a long-acting drug, which allows it to be prescribed for hypertension (arterial hypertension) once a day. Long-term treatment is not accompanied by the development of reflex tachycardia; it has little effect on cardiac output, renal perfusion, and glomerular filtration rate. The drug also increases the rate of urine outflow and reduces obstructions to its outflow. This leads to improved urodynamics in patients with benign prostatic hyperplasia (BPH). The drug does not affect the size of the prostate gland. Terazosin is quickly and almost completely absorbed from the digestive tract after oral administration. Its bioavailability is 90%, the action begins 15 minutes after application. The maximum concentration of the drug in the blood plasma is achieved 1 hour after administration. The therapeutic effect develops within 2–3 hours. The antihypertensive effect persists for 24 hours after taking the drug. Terazosin is 90–94% bound to plasma proteins. Extensively metabolized in the liver by hydrolysis, demethylation and dealkylation to form 5 different metabolites. The half-life is 12 hours and practically does not change with impaired renal function. Approximately 10 and 20% of the dose taken are excreted unchanged in urine and feces, respectively.
Setegis tablets 5 mg No. 10x3
Name
Setegis 5 mg No. 10x3
Description
Tablets are light pink (color inhomogeneity is possible), round, flat, beveled, engraved “E453” on one side, odorless.
Main active ingredient
Terazosin
Release form
Tablets are light pink (color inhomogeneity is possible), round, flat, beveled, engraved “E453” on one side, odorless.
Dosage
5 mg №10x3
special instructions
Like other alpha-blockers, terazosin is not recommended for use in patients with a history of syncope when urinating. 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 may occur when restarting treatment after a few days' break; therefore, in such cases, the initial dose should be reapplied. The incidence of fainting is 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 usually caused by severe orthostatic hypotension, but can also be associated with tachycardia (120-160 beats/min). Orthostatic hypotension is most pronounced soon after taking the drug, and the risk of fainting is highest between 30 and 90 minutes after taking the drug. Changing position from a horizontal or sitting position, standing for long periods of time, intense physical activity, high ambient temperatures and simultaneous intake of alcohol can cause dizziness, a feeling of uncertainty, or even loss of consciousness. In case of fainting, the patient should be placed with the lower limbs elevated, and, if necessary, symptomatic therapy should be started. When using terazosin together with diuretics and/or other antihypertensive drugs, it is recommended to reduce its dose. To avoid severe hypotension, it is recommended to begin treatment with the concomitant drug also at low doses and conduct careful medical monitoring of the patient. The same precautions are necessary when adding terazosin to ongoing diuretic or antihypertensive therapy. The initial dose of terazosin in these cases is also 1 mg. Elderly patients may be more sensitive to the hypotensive effects of terazosin. The use of terazosin requires special caution in patients with a predisposition to orthostatic hypotension, coronary artery disease, other severe heart diseases, cerebrovascular accidents, grade III or IV hypertensive retinopathy, insulin-dependent diabetes, and impaired liver and kidney function. Before initiating 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, when the dose is increased; Concomitant antihypertensive medications should also be taken into account. The effectiveness of terazosin for benign prostatic hyperplasia should be assessed only after 4-6 weeks of use of the drug at a maintenance dose. During cataract surgery in patients who have previously received alpha1-blockers, intraoperative iris instability syndrome (IFIS) is observed. This phenomenon is a variant of pinhole pupil syndrome, in which the iris relaxes to such an extent that it becomes unstable when irrigated. Despite preoperative pupil dilation, usually with the help of mydriatic agents, miosis increases and the iris sag towards the phacoemulsification incisions. In such cases, the operating surgeon should be prepared to modify the surgical technique, which may require the use of an iris hook, an iris retractor, and viscoelastic agents. Preoperative interruption of β1-blocker therapy has no advantage over continuation of therapy. The tablets contain lactose monohydrate (55 mg or 110 mg), so patients with galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not take Setegis®. Effect on the ability to drive vehicles and operate machinery Dizziness, loss of consciousness and fainting may occur, especially in the first days of taking the drug, when the dose is increased or when therapy with Segetis is resumed. Patients should be warned about possible side effects and the situations in which they may occur, and patients should be advised to refrain from driving or engaging in potentially hazardous activities for approximately 12 hours after taking the initial dose or when the dose is increased. Later in treatment, the degree of restrictions should be determined individually for each patient.
pharmachologic effect
Alpha1-adrenergic blocker. Improves urodynamics in patients with benign prostatic hyperplasia (BPH). Symptoms of BPH are associated with increased tone of the smooth muscles of the bladder outlet (triangle and neck of the bladder, proximal urethra) and prostate, which is controlled by β1-adrenergic receptors. In vitro, terazosin inhibited prostate smooth muscle contractions induced by phenylephrine. In clinical studies, terazosin improved urodynamics and relieved symptoms in patients with BPH. Terazosin dilates arteries due to competitive antagonism of postsynaptic β1-adrenergic receptors. 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% compared to the values before treatment. In addition, the increase in total cholesterol concentrations observed with the use of other antihypertensive drugs was not observed when terazosin was used in combination with them. Terazosin begins to act approximately 15 minutes after administration of a single dose, the maximum effect occurs 2-3 hours after oral administration. Duration of action - 24 hours.
Pharmacokinetics
Absorption After oral administration, terazosin is rapidly and almost completely absorbed from the gastrointestinal tract. Eating does not affect absorption. Slightly subject to first pass effect through the liver. The bioavailability of terazosin is about 90%. Cmax is reached within 1 hour. Distribution Terazosin is largely (90-94%) bound to plasma proteins. Metabolism Metabolized in the liver. Of the four known metabolites, only one is pharmacologically active. Elimination 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 the elimination of the drug. T1/2 does not change with impaired renal function.
Indications for use
— symptomatic treatment of benign prostatic hyperplasia; - arterial hypertension (as monotherapy or as part of combination therapy).
Directions for use and doses
The drug is taken orally. The tablets should be swallowed whole without chewing. The dose of the drug should be selected individually depending on the patient’s blood pressure. For adults, the drug is prescribed at an initial dose of 1 mg 1 time / day before bedtime. Due to the increased risk of developing arterial hypotension after taking the first dose, the initial dose should not exceed 1 mg. The daily dose should be increased gradually at intervals of 1 week until the maintenance dose is reached. For benign prostatic hyperplasia, the maintenance dose is 5-10 mg 1 time / day. Currently, there is no data confirming an additional symptomatic effect when using the drug at a dose of more than 10 mg/day. For arterial hypertension, the maintenance dose is usually from 2 mg to 10 mg 1 time / day. Doses greater than 20 mg rarely improve the effectiveness of the drug; doses greater than 40 mg have not been studied. In elderly patients and patients with renal failure, no dose adjustment is required.
Use 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 expected 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.
Precautionary measures
The drug should be prescribed with caution for angina pectoris, coronary artery disease or heart failure in the stage of decompensation, renal/liver failure, cerebrovascular accident, type 1 diabetes mellitus.
Interaction with other drugs
In clinical studies, patients with BPH receiving tarazosin in combination with an ACE inhibitor or diuretics had a higher incidence of dizziness or associated side effects than in the general population of patients receiving terazosin. Particular caution should be observed when terazosin is used with other antihypertensive drugs to prevent the occurrence of significant hypotension. When terazosin is added to diuretic or antihypertensive therapy, dosage reduction or retitration may be necessary. Adsorbents and antacids reduce absorption. Adrenergic stimulants weaken the effect. NSAIDs (especially indomethacin) may reduce the hypotensive effect by inhibiting Pg synthesis and/or fluid and Na+ retention. There are reports of hypotension occurring when terazosin is taken concomitantly with PDE5 inhibitors. Concomitant treatment with terazosin and sildenafil or vardenafil should be started if the patient is stable on terazosin. In addition, vardenafil should not be taken within 6 hours of taking terazosin, and sildenafil should not be taken within 4 hours of taking terazosin.
Contraindications
- 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.
Compound
In 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 dye yellow - 0.01 mg.
Overdose
Treatment: in case of severe hypotension and peripheral circulatory insufficiency, it is first of all important to transfer the patient to a supine position with the head of the head lowered. If shock occurs, it is necessary to prescribe plasma substitutes, then vasopressors. Water and electrolyte balance should be maintained. Dialysis may not be effective because terazosin is highly bound to plasma proteins.
Side effect
From the cardiovascular system: palpitations, tachycardia, orthostatic hypotension, vasodilation. Not clearly associated with the use of terazosin is arrhythmia. From the hematopoietic system: thrombocytopenia. Mental disorders: decreased libido, depression, increased excitability. Not clearly associated with terazosin use - anxiety, insomnia. From the nervous system: fainting, dizziness, drowsiness, headache, paresthesia. On the part of the visual organ: visual impairment, amblyopia; in the case of cataract surgery in patients receiving β1-blockers, intraoperative iris instability syndrome (IFIS) was observed. Not clearly associated with the use of terazosin - atypical vision, conjunctivitis. From the organ of hearing and balance: dizziness. Not clearly associated with terazosin use is tinnitus. From the respiratory system: nasal congestion, rhinitis, shortness of breath, sinusitis. Not clearly associated with terazosin use - bronchitis, nosebleeds, 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 urination, urinary tract infections and involuntary urination in postmenopausal women. From the genital organs and mammary gland: impotence, priapism. From 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 the use of terazosin - neck pain, shoulder pain, arthralgia, arthritis, joint diseases, myalgia. From the endocrine system: weight gain. Not clearly associated with terazosin use is gout. Other: asthenia, peripheral edema, edema. Not clearly associated with terazosin use - chest pain, facial swelling, fever. Allergic reactions: anaphylactoid reaction. Laboratory parameters: in studies, a small but statistically significant decrease in hematocrit, hemoglobin, leukocytes, total protein and albumin was noted. These laboratory findings indicate the ability to undergo hemodilution. Treatment with terazosin for up to 24 months had no significant effect on prostate-specific antigen (PSA) levels.
Storage conditions
The drug should be stored out of the reach of children at a temperature of 15° to 30°C.
Use of the drug Setegis
AH (arterial hypertension) The initial daily dose is 1 mg 1 time per day at night. It is recommended to increase the daily dose gradually, doubling it at weekly intervals until the desired effect is achieved. The maintenance dose is 1–5 mg 1 time per day. BPH The initial daily dose is 1 mg 1 time per day at night. Maintenance dose: 5–10 mg 1 time per day. The maximum daily dose is 20 mg. Patients with renal failure and the elderly do not require dose adjustment. The tablets should be taken without chewing, regardless of meals. The drug is not recommended for children.
Side effects of the drug Setegis
dizziness, in severe cases - collapse. To avoid this, it is recommended to start treatment with a dose of 1 mg at night. Possible orthostatic hypotension, dizziness, general weakness, peripheral edema may appear when using the drug in high doses. Possible tachycardia, angina pectoris, visual disturbances, nausea, vomiting, nasal congestion, disorders of the digestive tract, decreased libido and impotence, drowsiness, anaphylactic reactions.
Reviews
Veterinarians often prescribe Setegis as part of complex therapy for cystitis and urolithiasis. Many people recommend this drug, which is relatively safe and, in the correct dosage, acts gently. Among the advantages of the medicine, buyers note good tolerability and the absence of side effects.
Marina, cat owner, Moscow: “Our cat was given a catheter under anesthesia. The catheter was in place for 4 days. Then he walked lethargically, and we still saw droplets of blood in his urine. We informed the doctor about this, he told me to take additional Setegis to avoid complications and also prescribed drops.
A couple of days later the cat began to be active again at home. I was so happy that I even forgot to add drops.”
Anastasia, cat owner, Murmansk: “Kidney stones are not uncommon for cats. Ours is already 10 years old. Unknowingly, we fed her cheap dry food and ended up with MSD. It’s good that cats pass stones relatively easily. The veterinarian prescribed us a bunch of urine acidifiers and Setegis to improve urination.
The first days of treatment, the cat was lethargic, but within a day she began to eat well. On the fifth day, all symptoms of stones disappeared. I started going to the toilet normally, there was no more blood. I think Setegis helped. At first the cat urinated a lot, but then it returned to normal.”
Nadezhda Ivanovna, veterinarian, Moscow: “Setegis is a useful drug. Especially for cats, since their urinary tract obstruction is physiologically caused. It relaxes the urethra, relieves smooth muscle spasms and swelling.
In fact, Setegis removes all obstacles to normal urination. It acts purposefully and there is almost nothing that can replace it in veterinary practice.”
Special instructions for the use of the drug Setegis
At the beginning of treatment, the effect of the first dose may be observed - a sharp decrease in blood pressure, dizziness, loss of coordination of movements, loss of consciousness. Similar phenomena may occur when the drug is resumed after a break in treatment for several days. In such cases, the drug should be prescribed at a dose of 1 mg. Dizziness and poor coordination of movements often occur when moving from a sitting or lying position to a vertical one. With caution, Setegis tablets should be prescribed to patients with a tendency to develop orthostatic hypotension, as well as patients with coronary artery disease, other heart diseases, cerebrovascular accidents, and hypertensive retinopathy of grade III–IV. Before starting treatment for BPH, prostate cancer must be ruled out. In patients, it is necessary to monitor blood pressure levels at the beginning of treatment and when changing the dose of the drug. It is advisable to evaluate the effectiveness of BPH treatment after 4–6 weeks of treatment. The lactose content in each Setegis tablet should be taken into account in case of lactase deficiency, galactosemia or glucose/lactose malabsorption syndrome. In 1 tablet 1 mg - 55.0 mg; 2 mg; 5 mg; 10 mg - 110 mg lactose. At the initial stage of using Setegis and after each dose increase, you should refrain from performing potentially hazardous activities that require concentration, including driving.
Price
Depending on the region, the price of the medicine ranges from 720-780 rubles. per package 30 tablets of 2 mg.
Setegis is a prescription drug. So you need to first go to an appointment and get a prescription from your doctor. Setegis can be purchased with a prescription at any pharmacy. The product is often sold in specialized veterinary pharmacies at clinics.
