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Active ingredients
Terazosin
Release form
Pills
Composition
Terazosin (in the form of hydrochloride dihydrate) 2 mg; Excipients: lactose monohydrate, microcrystalline cellulose, corn starch, talc, dye yellow (E104), colloidal silicon dioxide (anhydrous), magnesium stearate.
Pharmacological effect
Peripheral postsynaptic 1-adrenergic receptor blocker. By blocking the 1-adrenoreceptors of the smooth muscles of the prostate gland and bladder neck, the drug helps to normalize urination in patients with benign prostatic hyperplasia. which reduces blood pressure. Onset of hypotensive action 15 minutes after ingestion (single dose). The duration of the hypotensive effect is 24 hours. The maximum effect when taking a single dose is achieved within 2-3 hours. The maximum hypotensive effect is achieved after 6-8 weeks of therapy. With prolonged use, a decrease in blood pressure is not accompanied, as a rule, by the development of reflex tachycardia.; The drug contributes to the normalization of lipid metabolism: lowers cholesterol, TG, LDL and VLDL in the blood, while increasing the amount of HDL. .
Pharmacokinetics
Absorption and distribution; After ingestion, it is rapidly and completely absorbed from the gastrointestinal tract. The degree of absorption does not depend on the simultaneous ingestion of food. Cmax in plasma is achieved after 1 h after administration.; Plasma protein binding is 90-94%; Metabolism and excretion; Biotransformed in the liver to form 4 metabolites, one of which (piperazine derivative of terazosin) has antihypertensive activity.; T1 / 2 is 12 hours. It is excreted in the bile (60%) and in the kidneys (40%, of which 10% is unchanged); Pharmacokinetics in special clinical situations; In hepatic insufficiency, the clearance decreases.
Indications
- benign prostatic hyperplasia (symptomatic treatment); - arterial hypertension.
Contraindications
- childhood; - Hypersensitivity to the drug. With caution, you should prescribe the drug for angina, coronary artery disease, hepatic or renal failure, impaired cerebral circulation, diabetes mellitus type 1.
Use during pregnancy and lactation
Kornam can be used during pregnancy and during breastfeeding in the event that the potential benefit to the mother outweighs the possible risk to the fetus or infant.
Dosage and administration
With benign prostatic hyperplasia, the initial dose is 1 mg 1 time / day before bedtime. Gradually, the dose is increased to 2-10 mg / day until the optimum effect is achieved. The therapeutic effect is usually marked 2 weeks after the start of treatment. To achieve a lasting effect, the course of treatment should be 4-6 weeks.; For hypertension, the drug is prescribed in an initial dose of 1 mg / day before bedtime. Gradually increase the dose to achieve a clinical effect. Maintenance dose is 1-10 mg 1 time / day. The maximum daily dose is 20 mg. In the case of a temporary cessation of the drug, treatment is resumed according to the same scheme.
Side effects
In the treatment of benign prostatic hyperplasia; On the part of the cardiovascular system: rarely - orthostatic hypotension; On the side of the central nervous system: drowsiness, dizziness, asthenia.; Other: nasal congestion.; hypotension - the “first dose effect” (observed in 1% of patients, mostly receiving diuretics or beta-blockers at the same time), manifested by dizziness, tachycardia, fainting; rarely - palpitations, peripheral edema, nasal congestion. From the side of the central nervous system: rarely - dizziness, asthenia, drowsiness, impaired clarity of visual perception. .; Other: rarely - reduced potency, nausea.
Overdose
Symptoms: pronounced decrease in blood pressure, impaired coordination of movements, fainting.; Treatment: it is necessary to put the patient down by lowering the head end of the bed. If necessary, appoint hypertensive agents, in / in the introduction of fluid. Hemodialysis is not effective.
Interaction with other drugs
With simultaneous use of Kornam and beta-blockers, diuretics, calcium channel blockers, ACE inhibitors, the antihypertensive effect may be enhanced.Special caution is required with the simultaneous administration of terazosin and antihypertensive drugs of central action.; Terazosin absorption is reduced while taking adsorbents and antacids.; Adrenomimetic drugs weaken the effect of terazosin; sodium.
special instructions
To prevent the development of orthostatic hypotension, treatment should begin with the appointment of Kornam at a dose of 1 mg / day before bedtime, after which the patient should be in bed for 6–8 hours; the risk of orthostatic hypotension (the “first dose effect”) is highest during 30-90 min after taking the drug and increased in patients simultaneously receiving beta-blockers and diuretics, with a decrease in the BCC, hypo-salt diet, as well as the resumption of drug treatment after the break (several days) .; In the case of time When the treatment is discontinued, therapy is resumed from the same dose. During treatment, the level of the specific antigen of the prostate gland does not change. Prior to treatment of benign prostatic hyperplasia, prostate cancer should be excluded.; The patient should be informed about the increased risk of orthostatic hypotension when drinking alcohol, prolonged standing or exercise, and in hot weather.; Effect on ability to drive vehicles and control mechanisms ; Within 12 hours after taking the first dose, after increasing the dose or interrupting therapy, it is not recommended to engage in a potentially dangerous species. activities that require increased attention and quickness of psychomotor reactions.