Tachiben
Takhiben: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Tachyben
ATX code: C02CA06
Active ingredient: urapidil (Urapidil)
Producer: Senexi SAS (Cenexi SAS) (France)
Description and photo update: 2020-21-01
Prices in pharmacies: from 995 rubles.
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Tachiben is an antihypertensive drug.
Release form and composition
The product is produced in the form of a solution for intravenous (i / v) administration: a clear, colorless or pale brown liquid [5, 10 or 20 ml each in an ampoule made of transparent colorless glass, with a breaking point and 2 yellow marking rings (5 ml), or 1 ring of white (10 ml) or blue (20 ml); in a contour acheikova package 5 ampoules, in a cardboard box 1 package and instructions for use of Takhiben].
1 ml of solution contains:
- active substance: urapidil - 5 mg;
- additional components: sodium dihydrogen phosphate dihydrate, concentrated hydrochloric acid (37% m / m), sodium hydrogen phosphate dihydrate, sodium hydroxide (4% m / m), propylene glycol, diluted hydrochloric acid (3.7% m / m), water for injection …
Pharmacological properties
Pharmacodynamics
Urapidil is an alpha-blocker with a central and peripheral mechanism of action. By inhibiting postsynaptic α1-adrenergic receptors, it reduces total peripheral vascular resistance (OPSS). As a result of stimulation of serotonin 5-HT1A-receptors of the vasomotor (vasomotor) center, it participates in the regulation of the central mechanism for maintaining vascular tone (prevents a reflex increase in the tone of the sympathetic nervous system). Under the influence of urapidil, there are no changes in the heart rate (HR) and cardiac output (CO), the growth of low CO is provided by a decrease in OPSS. The substance usually has no orthostatic effect.
Urapidil inhibits vasoconstriction caused by α2-adrenergic receptors and does not lead to the development of reflex tachycardia associated with vasodilation. It mainly blocks peripheral postsynaptic α1-adrenergic receptors, as a result of which the vasoconstrictor effect of catecholamines is suppressed. By weakening the OPSS, Tachiben balances the systolic and diastolic blood pressure (BP); also has a weak β-adrenergic blocking effect. Reduces pre- and afterload on the heart, provides effective contraction of the myocardium, which in the absence of arrhythmia contributes to an increase in the reduced cardiac output.
Urapidil does not lead to fluid retention in the body, does not affect the metabolism of uric acid and indicators of carbohydrate metabolism.
Pharmacokinetics
After intravenous administration of urapidil at a dose of 25 mg, a two-phase decrease in concentration is noted: α-phase (initial) - a rapid decrease, β-phase (subsequent) - slow. The volume of distribution (V d) of the drug is 0.8 l / kg (0.6-1.2 l / kg), the distribution period is 35 minutes, it is metabolized mostly in the liver. The main metabolite, which practically does not have antihypertensive activity, is urapidil, hydroxylated at the 4-position of the phenolic ring. The O-demethylated metabolite is formed in small amounts and exhibits almost the same activity as the parent substance.
Approximately 50–70% of the main component and its metabolites (15% - in the form of an active substance) are excreted by the kidneys, the rest of the dose received is excreted through the intestine, mainly in the form of inactive n-hydroxylated urapidil. After the jet injection of the solution in / during the half-life (T 1/2) averages 2.7 hours (1.8-3.9 hours). The substance binds to plasma proteins at a level of 80%. Due to the relatively low degree of binding to blood proteins, the possible interaction of urapidil with drugs that have a high degree of this connection has not been established.
In the elderly and in patients with severe hepatic and / or renal clearance, and the V d urapidil reduced and T 1/2 - upgraded. Tachiben crosses the blood-brain barrier (BBB) and the placenta.
Indications for use
- therapy of refractory and severe arterial hypertension, hypertensive crisis;
- control of the decrease in blood pressure during its growth during and / or after surgery.
Contraindications
Absolute:
- open arterial (Botallov) duct;
- the presence of coarctation of the aorta and arteriovenous shunt (except when the dialysis shunt is hemodynamically inactive);
- pregnancy, lactation period;
- age up to 18 years;
- hypersensitivity to any component of the product.
Relative (Tachiben should be used with caution):
- heart failure due to violations of the mechanical function of the heart, such as stenosis of the aortic or mitral valve, pulmonary embolism, impaired myocardial contractility caused by diseases of the heart bag (including chronic pericarditis, tamponade);
- moderate / severe renal dysfunction;
- liver dysfunction;
- hypovolemia;
- elderly age;
- simultaneous use with cimetidine.
Takhiben, instructions for use: method and dosage
Tachiben solution in ampoules is injected in / in a stream or drip by means of a long-term IV infusion - in the patient's supine position.
Dosage regimen for the treatment of hypertensive crisis, refractory arterial hypertension, grade III arterial hypertension:
- IV injection: slowly at a dose of 10-50 mg with constant monitoring of blood pressure, the expected decrease in the latter - within 5 minutes after injection; taking into account the therapeutic effect, repeated administration of the solution is allowed;
- intravenous drip / continuous infusion using a perfusion pump: maintenance dose: an average of 9 mg / h, i.e. urapidil at a dose of 250 mg (10 or 5 ampoules of 5 and 10 ml, respectively) is diluted in 500 ml of solution for infusion (1 mg = 44 drops ~ 2.2 ml); the maximum allowable ratio is 4 mg of the drug per 1 ml of solution for infusion, the recommended maximum rate at the beginning of administration is 2 mg / min; the drip rate is set depending on the blood pressure of a particular patient.
For infusion drip, carried out in order to maintain blood pressure, it is generally recommended to dilute Tachiben at a dose of 250 mg in 500 ml of solvent. In the case of using a perfusion pump, the drug should be injected into its syringe at a dose of 100 mg (1 ampoule of 20 ml / 2 ampoules of 10 ml / 4 ampoules of 5 ml) and add the solvent to a volume of 50 ml. The solvent used is a 0.9% sodium chloride solution, a 5 or 10% dextrose / glucose solution.
The control of the decrease in blood pressure during and / or after surgery in order to maintain the blood pressure values achieved by intravenous injection is carried out by continuous infusion of the solution using a perfusion pump or drip. It is recommended to infusion with an initial rate of up to 6 mg per 1–2 minutes, with a further decrease.
Parenteral administration of Tachiben solution for a controlled (controlled) decrease in blood pressure is performed according to one of the following schemes:
- I - 5 ml of solution is injected intravenously (dose - 25 mg), if blood pressure decreases, after 2 minutes an infusion is carried out to stabilize it;
- II - 5 ml of solution is injected intravenously (dose - 25 mg), if blood pressure cannot be lowered, after 2 minutes repeat intravenous injection at a dose of 25 mg, when blood pressure is reduced after 2 minutes, infusion is performed to stabilize it;
- III - 5 ml of solution is injected intravenously (dose - 25 mg), if blood pressure cannot be lowered after 2 minutes, repeat the intravenous injection at a dose of 25 mg, when after the second injection of the solution after 2 minutes it is not possible to lower blood pressure, intravenously 10 ml of solution (dose 50 mg) is slowly injected, with a decrease in blood pressure, an infusion is carried out after 2 minutes to stabilize it.
The introduction of the solution can be single or multiple. With a new increase in blood pressure, it is possible to repeat the course of therapy. IV injection of Tachiben can be combined with further drip infusion.
Treatment for 7 days is safe, but in most cases with parenteral use of antihypertensive drugs, this period should not be exceeded. It is possible to start the continuous use of antihypertensive oral drugs simultaneously with the emergency parenteral therapy.
If in the previous period other antihypertensive drugs were used, then Tachiben should be administered after a time, during which the effect of the previously used drugs should appear. At the same time, starting therapy with urapidil is required with lower doses.
Side effects
During the use of Tachiben, the following negative side reactions from systems and organs may develop:
- cardiovascular system: infrequently - a feeling of palpitations or chest compression, bradycardia, tachycardia, arrhythmias, respiratory distress syndrome;
- blood and lymphatic system: extremely rare - thrombocytopenia;
- nervous system: often - headache, vestibular dizziness;
- psyche: extremely rarely - a feeling of anxiety;
- general disorders: infrequently - increased fatigue; very rarely - asthenia;
- digestive tract: often - nausea; infrequently - vomiting;
- skin and subcutaneous tissues: infrequently - increased sweating; rarely - rash, pruritus, exanthema and other symptoms of allergic skin reactions;
- urinary system: often - proteinuria; rarely - nephrotic syndrome, nephropathy;
- reproductive system and mammary gland: rarely - priapism;
- respiratory system: rarely - nasal congestion.
Most of the above adverse events are associated with a sharp drop in blood pressure, however, as the experience of clinical use shows, they disappear within a few minutes after stopping the administration of Tachiben, including after drip infusion. In the event of severe adverse reactions, discontinuation of treatment may be required.
Overdose
Symptoms of a urapidil overdose may include lethargy, dizziness, fatigue, orthostatic hypotension, and collapse.
Against the background of a significant decrease in blood pressure, the patient should be laid down, raising his legs above the level of the pelvis, and measures should be taken to replenish the circulating blood volume (BCC). If these measures are ineffective, intravenous vasoconstrictors are administered with simultaneous monitoring of blood pressure. In some cases, catecholamines are prescribed - epinephrine (adrenaline) at a dose of 0.5–1 mg, added to 10 ml of 0.9% sodium chloride solution.
special instructions
Special precautions to be observed when handling the drug:
- The Tahiben ampoule is intended for single use.
- Before opening the ampoule, you should visually check the solution for foreign inclusions and discoloration.
- The drug should not be mixed with other drugs, except for 0.9% sodium chloride solution or 5 or 10% dextrose (glucose) solutions. Mixing Tachiben with alkaline injection / infusion solutions can cloud the liquid and cause flocculation.
- After opening the ampoule, the solution should be used immediately or within 24 hours if it has been stored at a temperature of 2-8 ° C.
- If the drug was not administered immediately after its dilution, the user is responsible for the storage conditions and time.
With too rapid a decrease in blood pressure, the threat of developing bradycardia or cardiac arrest increases.
In conditions that cause hypovolemia (for example, nausea or vomiting), the hypotensive effect of Tachiben is enhanced.
Since the solution contains propylene glycol, after intravenous administration of the drug, symptoms similar to those when using ethanol may occur.
Tachiben practically does not contain sodium - in 1 dose it is less than 1 mmol / l (23 mg).
Influence on the ability to drive vehicles and complex mechanisms
In the course of therapy with Tachiben, it is recommended to abandon driving vehicles and controlling complex, potentially dangerous mechanisms.
Application during pregnancy and lactation
It is contraindicated for pregnant women to prescribe Tachiben, since there is no reliable information about its use during pregnancy.
It has been found that the antihypertensive agent crosses the placenta. In the course of experimental studies, reproductive toxicity of the drug was noted in the absence of signs of teratogenicity. The potential risk to humans due to the paucity of these studies has not been identified.
It is not known whether urapidil is excreted in breast milk, therefore, if it is necessary to use it during lactation, it is necessary to stop breastfeeding.
Pediatric use
Patients under 18 years of age are not prescribed Tachiben, since the efficacy and safety of urapidil in children and adolescents has not been established.
With impaired renal function
In the presence of moderate to severe renal dysfunction, Tachiben should be used with caution. A reduction in recommended doses may be required.
For violations of liver function
In the presence of functional disorders of the liver, it is recommended to use Tachiben with caution, in doses reduced compared to the recommended ones.
Use in the elderly
In elderly patients, therapy with Tachiben should be carried out with caution. The initial dose of the drug should be reduced compared to the recommended dose, since in patients of this age category, a change in sensitivity to drugs of this class is often recorded (V d is reduced, and T 1/2 is increased).
Drug interactions
- α-blockers, baclofen, vasodilators and other drugs that lower blood pressure; ethanol; drugs used for urological indications: enhance the hypotensive effect of urapidil;
- corticosteroids: weaken the hypotensive effect of Tachiben as a result of sodium and fluid retention; this combination requires caution;
- cimetidine: the plasma level of urapidil in the blood increases by 15%, therefore, correction of its dose is recommended;
- imipramine, antipsychotics: the hypotensive effect increases and the risk of orthostatic hypotension increases; caution should be exercised;
- alkaline solutions for injections and infusions: the appearance of turbidity and the formation of a flocculent sediment is possible when mixed with Takhiben; the drug should not be diluted in these solutions;
- angiotensin-converting enzyme (ACE) inhibitors: it is not recommended to use it in combination with urapidil due to insufficient clinical data.
Analogs
Takhiben's analogs are Ebrantil, Urapidil-native, Urapidil Karino, etc.
Terms and conditions of storage
Keep out of the reach of children at a temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Takhiben
The few reviews about Takhiben are usually positive. Patients consider the drug an effective antihypertensive agent, providing a rapid decrease in blood pressure to normal in severe hypertension and hypertensive crisis. At the same time, they warn that Tachiben should be used exclusively as a means of emergency parenteral therapy and administered only under medical supervision, since it has a powerful effect and can reduce blood pressure too sharply and quickly, which also poses a health hazard.
The price of Takhiben in pharmacies
The average price for Takhiben in the form of a solution for intravenous administration (5 mg / ml), for 5 ampoules of 5 ml is 490 rubles, for 5 ampoules of 10 ml - 930 rubles.
Takhiben: prices in online pharmacies
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Drug name Price Pharmacy |
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Tachiben 5 mg / ml solution for intravenous administration 10 ml 5 pcs. 995 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
