Tenzotran pills 0.2 mg 28 pcs
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Active ingredients
Moxonidine
Release form
Pills
Composition
Moxonidine 200 mcg. Adjuvants: lactose monohydrate - 94.5 mg, povidone (K25) - 2 mg, crospovidone - 3 mg, magnesium stearate - 0.3 mg. Coat composition: opadry Y-1-7000 (titanium dioxide - 1.093 mg, hypromellose - 2.186 mg , macrogol 400 - 0.219 mg) - 3.498 mg, iron dye red oxide - 0.002 mg.
Pharmacological effect
Selective imidazoline receptor agonist responsible for the reflex regulation of the sympathetic nervous system (localized in the ventro-lateral division of the medulla oblongata). It has a low affinity for central α2 -adrenoreceptors, through interaction with which sedation and dryness of the oral mucosa are mediated. Moxonidine increases insulin sensitivity by 21% compared with placebo in patients with obesity, insulin resistance with a moderate degree of arterial hypertension. Effect on hemodynamics: a decrease in systolic and diastolic blood pressure with a single and prolonged administration of moxonidine is associated with a decrease in the pressor action of sympathetic nervous system Stem on the peripheral blood vessels, decrease in peripheral vascular resistance, while cardiac output and heart rate did not change significantly.
Pharmacokinetics
Absorption and distribution After oral administration, moxonidine is rapidly and almost completely absorbed from the upper GI tract. Tmax is approximately 1 hour. Absolute bioavailability is approximately 88%. It is slightly metabolized during the first passage through the liver. Eating does not affect the pharmacokinetics of the drug. Binding to plasma proteins is 7.2%. Moxonidine penetrates the BBB. Metabolism The main metabolite is dehydrated moxonidine, the pharmacodynamic activity of which is about 1/10 of the activity of moxonidine. Excretion of T1 / 2 of moxonidine and metabolites is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys: approximately 78% - unchanged, 13% - as dehydrated moxonidine. Other metabolites in the urine account for approximately 8% of the dose. Less than 1% of the dose is excreted through the intestines. Pharmacokinetics in special groups of patients. Excretion of moxonidine is significantly correlated with CC.In patients with moderate renal insufficiency (CC 30-60 ml / min), plasma Css and end T1 / 2 are approximately 2 and 1.5 times higher than in patients with arterial hypertension with normal kidney function (CC more than 90 ml / min) . In patients with severe renal failure (CC less than 30 ml / min), plasma Css and end T1 / 2 are 3 times higher than in patients with normal renal function. The use of moxonidine in multiple doses does not lead to cumulation in the body of patients with moderate to severe renal failure. In patients with end-stage renal disease (CC less than 10 ml / min) on hemodialysis, plasma Css and end T1 / 2 are 6 and 4 times higher, respectively, than in patients with normal renal function. In patients with impaired renal function, the dose should be selected individually. Moxonidine is slightly excreted during hemodialysis.
Indications
- arterial hypertension.
Contraindications
- SSSU; - sinoatrial blockade; - AV block II and III degree; - severe bradycardia (heart rate less than 50 beats / min); - chronic heart failure III and IV functional class according to NYHA classification; - unstable angina; - angioedema in the history; severe hepatic impairment (more than 9 points on the Child-Pugh scale); chronic renal insufficiency (QC less than 30 ml / min; serum creatinine content greater than 160 μmol / l); age up to 18 years (efficacy and safety not established); - lactation period; - intolerance ha lactose, lactase deficiency or glucose-galactose malabsorption syndrome; - hypersensitivity to moxonidine and other components of the drug. The drug should be used with caution in Parkinson’s disease (severe), epilepsy, glaucoma, depression, intermittent claudication, Raynaud’s disease, AV blockade I degree, chronic renal failure (CC more than 30 ml / min, but less than 60 ml / min), marked cerebrovascular disorders, after myocardial infarction, chronic heart failure, I and II functional class Ca, abnormal liver function, hemodialysis, during pregnancy.
Precautionary measures
In the course of treatment, exacerbation of psoriasis is possible. During pheochromocytoma, propranolol can be used only after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually,under the supervision of a doctor. Against the background of treatment with propranolol, it is necessary to avoid intravenous injection of verapamil, diltiazem. For several days before undergoing anesthesia, it is necessary to stop taking propranolol or to choose a remedy for anesthesia with minimal negative inotropic effect. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
There are no clinical data on the negative impact on the course of pregnancy. However, it should be prescribed Tenzotran pregnant only if the intended benefit to the mother outweighs the potential risk to the fetus. Moxonidine is excreted in breast milk. During the period of treatment it is recommended to stop breastfeeding or stop the drug.
Dosage and administration
The drug is prescribed by mouth, regardless of the meal. Tablets should be taken with a sufficient amount of liquid. In most cases, the initial dose of Tenzotran is 200 μg / day per dose, preferably in the morning. In case of insufficiency of the therapeutic effect, the dose can be increased after 3 weeks of therapy to 400 μg / day in 2 doses (in the morning and in the evening) or in 1 dose (in the morning). The maximum daily dose which should be divided into 2 receptions (in the morning and in the evening), makes 600 mkg. The maximum single dose is 400 mcg. In elderly patients with normal renal function, the recommendations for dosing regimen are the same as for adult patients. In patients with renal insufficiency (CC from 30-60 ml / min) and patients on hemodialysis, single dose should not exceed 200 micrograms. The maximum daily dose is 400 micrograms.
Side effects
The most frequent adverse reactions, especially at the beginning of therapy, were dry mouth, headache, asthenia and drowsiness. The intensity of their manifestation and the frequency decrease with repeated admission. The frequency of adverse reactions is determined as follows: very often (more than 1/10), often (more than 1/100, less than 1/10), sometimes (more than 1/1000 and less than 1/100), very rarely (less than 1/1000, including individual messages). From the side of the central nervous system: often - increased fatigue,drowsiness, headache, dizziness; sometimes - insomnia, asthenia. From the cardiovascular system: often - vasodilation; sometimes - excessive reduction of blood pressure, orthostatic hypotension, paresthesia, Raynaud's syndrome, impaired peripheral microcirculation. From the side of the gastrointestinal tract: very often - dry mucous membrane of the oral cavity; often - nausea, constipation and other violations of the gastrointestinal tract; very rarely - hepatitis, cholestasis. From the urogenital system: sometimes - urinary retention or incontinence, impotence, decreased libido. Allergic reactions: sometimes - skin manifestations, angioedema. From the organ of vision: sometimes - dry eyes, causing itching or burning sensation .Other: sometimes - swelling of different localization, weakness in the legs, fainting, fluid retention, anorexia, pain in the region of the parotid glands, gynecomastia.
Overdose
There are reports of several cases of overdose without death, when doses up to 19.6 mg were applied at a time. Symptoms: headache, sedation, drowsiness, marked reduction in blood pressure, dizziness, asthenia, bradycardia, dry mouth, vomiting and stomach pain, increased fatigue. Short-term increase in blood pressure, tachycardia, hyperglycemia are potentially possible. Treatment: There is no specific antidote. Gastric lavage, taking activated charcoal and laxatives, symptomatic therapy. In the case of a pronounced decrease in blood pressure, the introduction of a liquid to restore the BCC and the introduction of dopamine are recommended. Bradycardia can be stopped by atropine. Α-adrenoreceptor antagonists can reduce or eliminate transient hypertension in overdose with moxonidine.
Interaction with other drugs
Moxonidine can be administered with thiazide diuretics, slow calcium channel blockers and other antihypertensive drugs. The combined use of moxonidine with these and other antihypertensive drugs leads to an additive effect and enhances the hypotensive effect. When prescribing moxonidine with hydrochlorothiazide, glibenclamide (glyburide) or digoxin, there is no pharmacokinetic interaction.therefore, it is not recommended to prescribe tricyclic antidepressants at the same time as moxonidine. Moxonidine moderately enhances reduced cognitive ability in patients taking lorazepam. Appointment of moxonidine together with benzodiazepines may be accompanied by increased sedative effect of the latter. Moxonidine is able to potentiate the effect of ethanol when used in combination. no interaction.
special instructions
If you need to cancel simultaneously taken beta-blockers and Tenzotran, first cancel beta-blockers and only a few days - Tenzotran. Stop taking Tenzotran gradually. It is not recommended to appoint tricyclic antidepressants at the same time with Tenzotran. Moxonidine can be prescribed with thiazide diuretics, ACE inhibitors and slow calcium channel blockers. Patients with a rare hereditary pathology intolerance galactose, lactase deficiency or glucose-galactose malabsorption syndrome should not be taken by Tenzotran. Effect on ability to drive vehicles and control mechanisms There are no data on the adverse effect of moxonidine on the ability to drive vehicles and control mechanisms. There are reports of the development of drowsiness and dizziness during treatment with moxonidine. This should be taken into account when prescribing the drug to patients who are engaged in potentially hazardous activities that require high concentration of attention and speed of psychomotor reactions.