Tenzotran
Tenzotran: 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: Tenzotran
ATX code: C02AC05
Active ingredient: Moxonidine (Moxonidine)
Producer: Perrigo Israel Pharmaceuticals (Israel)
Description and photo update: 2018-25-10
Prices in pharmacies: from 332 rubles.
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Tenzotran is a drug with an antihypertensive effect.
Release form and composition
The dosage form of Tenzotran is film-coated tablets: light pink, pink or dark pink (0.2, 0.3 or 0.4 mg, respectively), round (in a cardboard box 1-3 blisters of 14 pcs. in each).
Composition of 1 tablet:
- active substance: moxonidine - 0.2; 0.3 or 0.4 mg;
- additional components (0.2 / 0.3 / 0.4 mg): lactose monohydrate - 94.5 / 94.4 / 94.3 mg; povidone-K25 - 2/2/2 mg; crospovidone - 3/3/3 mg; magnesium stearate - 0.3 / 0.3 / 0.3 mg;
- shell: Opadry Y-1-7000 (hypromellose - 2.186 / 2.18 / 2.165 mg; titanium dioxide - 1.093 / 1.09 / 1.083 mg; macrogol-400 - 0.219 / 0.218 / 0.217 mg) - 3.498 / 3.488 / 3.465 mg; dye iron oxide red - 0.002 / 0.012 / 0.035 mg.
Pharmacological properties
Pharmacodynamics
Moxonidine is a selective agonist of imidazoline receptors, which are responsible for the reflex regulation of the sympathetic nervous system. Has a low affinity for central α 2 -adrenergic receptors, due to the interaction with which dryness of the oral mucosa and sedation are mediated.
Moxonidine increases the insulin sensitivity index by 21% compared to placebo in obesity and insulin resistance with moderate arterial hypertension.
A decrease in systolic and diastolic blood pressure (blood pressure) with a single and long-term use of moxonidine is associated with a decrease in the pressor effect of the sympathetic nervous system on peripheral vessels, a decrease in OPSS (total peripheral vascular resistance), while heart rate (heart rate) and cardiac output are significant are not subject to change.
Pharmacokinetics
Moxonidine after oral administration is almost completely and rapidly absorbed from the upper gastrointestinal tract. T max (time to reach the maximum concentration of the substance) is approximately 60 minutes. Absolute bioavailability is about 88%. The substance is slightly metabolized during the first passage through the liver. Food intake has no effect on the pharmacokinetics of the drug.
The binding of moxonidine to blood plasma proteins is 7.2%. The substance crosses the blood-brain barrier.
The main metabolite is dehydrated moxonidine, its pharmacodynamic activity is approximately 10% of the activity of moxonidine.
T 1/2 (half-life) of the substance and its metabolites is 2.5 and 5 hours, respectively. More than 90% of moxonidine is excreted by the kidneys within 24 hours (unchanged - about 78%, as dehydrated moxonidine - 13%). Other metabolites in urine account for approximately 8% of the dose. Less than 1% of the dose is excreted through the intestines.
Excretion of the substance largely correlates with CC (creatinine clearance) (in comparison with the indicators of patients with intact renal function):
- 30-60 ml / min: increase in C ss (stationary concentration of the substance) in blood plasma and the final T 1/2 by about 2 and 1.5 times, respectively;
- <30 ml / min: increase in C ss in blood plasma and the final T 1/2 by 3 times;
- <10 ml / min (in hemodialysis patients with end-stage renal failure): increase in C ss in blood plasma and final T 1/2 by 6 and 4 times, respectively.
In case of moderate / severe renal failure, prolonged use of moxonidine does not lead to cumulation in the body. In the presence of impaired renal function, the dose of the drug should be selected individually. During hemodialysis, the substance is excreted slightly.
Indications for use
According to the instructions, Tenzotran is prescribed for the treatment of arterial hypertension.
Contraindications
Absolute:
- sinoatrial blockade;
- sick sinus syndrome;
- atrioventricular block II – III degree;
- chronic renal failure (in patients with creatinine clearance 160 μmol / l);
- chronic heart failure III – IV functional class according to NYHA classification;
- severe bradycardia (with heart rate <50 beats / min);
- burdened history of angioedema;
- galactose intolerance, glucose-galactose malabsorption syndrome or lactase deficiency;
- unstable angina;
- severe liver failure (on the Child-Pugh scale> 9 points);
- age up to 18 years;
- lactation period;
- individual intolerance to any component of the drug.
Relative (Tenzotran is prescribed under medical supervision):
- atrioventricular block I degree;
- Parkinson's disease in severe form;
- hemodialysis;
- glaucoma;
- chronic heart failure I – II functional class;
- epilepsy;
- intermittent claudication;
- depression;
- cerebrovascular disorders in a pronounced course;
- Raynaud's disease;
- hepatic dysfunction;
- chronic renal failure (in patients with creatinine clearance of 30-60 ml / min);
- period after myocardial infarction;
- pregnancy.
Instructions for use of Tenzotran: method and dosage
Tenzotran is taken orally with a sufficient amount of liquid, regardless of food intake.
The starting dose is usually 0.2 mg per day in 1 dose, preferably in the morning. If necessary, after 3 weeks of use, the daily dose can be increased to 0.4 mg in 1 dose (morning) or 2 doses (morning and evening). The maximum daily dose taken in 1 dose is 0.4 mg, in 2 doses - 0.6 mg.
In patients with creatinine clearance of 30-60 ml / min and patients on hemodialysis, a single dose should not exceed 0.2 mg, the daily dose should not exceed 0.4 mg.
Side effects
Most often, during the course, especially at its beginning, the development of dry mouth, headache, asthenia and drowsiness is observed. With repeated administration, the frequency and intensity of their manifestation decrease.
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including isolated messages - very rare):
- digestive system: very often - xerostomia; often - constipation, nausea and other disorders; very rarely - cholestasis, hepatitis;
- central nervous system: often - drowsiness, increased fatigue, dizziness, headache; sometimes - asthenia, insomnia;
- genitourinary system: sometimes - impotence, incontinence or urinary retention, decreased libido;
- cardiovascular system: often - vasodilation; sometimes - Raynaud's syndrome, a significant decrease in blood pressure, paresthesias, orthostatic hypotension, disorders of peripheral microcirculation;
- organ of vision: sometimes - dry eyes, leading to itching or burning;
- allergic reactions: sometimes - angioedema, skin manifestations;
- others: sometimes - gynecomastia, anorexia, fainting, weakness in the legs, edema of various localization, fluid retention, pain in the parotid glands.
Overdose
There are reports of several cases of overdose using doses up to 19.6 mg in one dose without death.
The main symptoms are: increased fatigue, vomiting and stomach pain, dizziness, sedation, headache, drowsiness, a marked decrease in blood pressure, asthenia, bradycardia, xerostomia. Hyperglycemia, tachycardia, a short increase in blood pressure are potentially possible.
There is no specific antidote. Therapy includes gastric lavage, laxatives and activated charcoal intake, symptomatic treatment. In cases of a pronounced decrease in blood pressure, it is recommended to introduce a liquid to restore the volume of circulating blood and the use of dopamine. Bradycardia can be controlled with atropine. In case of an overdose of moxonidine, α-adrenergic receptor antagonists can eliminate / reduce transient arterial hypertension.
special instructions
You need to stop taking Tenzotran gradually.
During treatment, patients should regularly monitor blood pressure, heart rate and ECG.
If it is necessary to cancel simultaneously taken Tenzotran and beta-blockers, the latter are canceled first, Tenzotran can be canceled after a few days.
Moxonidine can be taken simultaneously with thiazide diuretics, slow calcium channel blockers, and angiotensin-converting enzyme inhibitors.
Influence on the ability to drive vehicles and complex mechanisms
Patients during the period of therapy should take into account the likelihood of developing adverse reactions, including drowsiness and dizziness.
Application during pregnancy and lactation
- lactation period: therapy is contraindicated;
- pregnancy: Tenzotran is prescribed with caution.
Pediatric use
Patients under the age of 18 are not prescribed Tenzotran, which is due to the lack of the necessary data.
With impaired renal function
- CC 160 μmol / l: Tenzotran is not prescribed;
- CC 30-60 ml / min: therapy can be carried out with caution.
For violations of liver function
- severe hepatic impairment (Child-Pugh scale> 9 points): Tenzotran is contraindicated;
- liver dysfunction: therapy can be carried out with caution.
Use in the elderly
In the absence of impaired renal function, a change in the dosage regimen is not required.
Drug interactions
Possible interactions:
- thiazide diuretics, blockers of slow calcium channels and other drugs with an antihypertensive effect: increased hypotensive effect (combined use is possible);
- tricyclic antidepressants: decrease in the effectiveness of Tenzotran (the combination is not recommended);
- lorazepam: moderate enhancement of the impaired cognitive ability of patients;
- benzodiazepines: enhancing their sedative effect;
- ethanol: potentiation of the effect.
Analogs
Analogs of Tenzotran are: Physiotens, Moxonidin, Moxonitex, Moxarel.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 30 ° C.
Expiry date (depending on the dosage of the tablets):
- 0.2 mg - 2 years;
- 0.3 and 0.4 mg - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tenzotran
According to reviews, Tenzotran is an effective drug with an antihypertensive effect, used as monotherapy or in combination with other drugs. A convenient dosing regimen and a quick effect are noted. The development of side effects is rarely reported.
Price for Tenzotran in pharmacies
The approximate price for Tenzotran (28 tablets of 0.2 or 0.4 mg) is 209-438 or 422-546 rubles.
Tenzotran: prices in online pharmacies
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Drug name Price Pharmacy |
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Tenzotran 0.2 mg film-coated tablets 28 pcs. 332 RUB Buy |
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Tenzotran 0.4 mg film-coated tablets 28 pcs. RUB 515 Buy |
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Tenzotran tablets p.p. 0.4mg 28 pcs. 634 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!
