Description
Latin name
Tenzotran
Release form
Film-coated tablets.
Packing
28 tablets.
Pharmacological action
Tenzotran is a central antihypertensive.
Selective agonist of imidazoline receptors responsible for reflex control of the sympathetic nervous system (localized in the ventero-lateral region of the medulla oblongata). It has a low affinity for central alpha2-adrenergic receptors, due to the interaction with which the sedative effect and dryness of the oral mucosa are mediated. Moxonidine improves the insulin sensitivity index by 21% compared to placebo in obese patients and insulin-resistant patients with moderate arterial hypertension.
Effect on hemodynamics: a decrease in systolic and diastolic blood pressure (BP) with a single and prolonged administration of moxonidine is associated with a decrease in the pressor effect of the sympathetic system on peripheral vessels, a decrease in total peripheral vascular resistance, while cardiac output and heart rate (HR) do not significantly change.
Pharmacokinetics
After oral administration, moxonidine is rapidly and almost completely absorbed from the upper gastrointestinal tract. Tmax is approximately 1 hour. Absolute bioavailability is approximately 88%, the metabolism of the first passage through the liver is negligible. Eating does not affect the pharmacokinetics of the drug. Communication with plasma proteins is 7.2%.
Primary metabolite: dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 1/10 compared with moxonidine. 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 and 13% as dehydrogenated moxonidine. Other metabolites in urine make up approximately 8% of the dose. Less than 1% of the dose is excreted through the intestines.
Pharmacokinetics for renal failure
Excretion of moxonidine is significantly correlated with creatinine clearance (CC). In patients with moderate renal failure (CC in the range of 30-60 ml / min. ) equilibrium plasma concentrations and the final half-life are approximately 2 and 1.5 times higher than in patients with arterial hypertension with normal renal function (CC more than 90 ml / min.). In patients with severe renal failure (CC less than 30 ml / min.), The equilibrium plasma concentrations and the final half-life are 3 times higher than in patients with normal renal function. The appointment of multiple doses of moxonidine does not lead to cumulation in the body of patients with moderate and severe renal failure. In the later stages, in patients with end-stage renal failure (CC less than 10 ml / min.) Undergoing hemodialysis, the equilibrium plasma concentrations and the final half-life are 6 and 4 times higher, respectively, than in patients with normal renal function. In patients with impaired renal function, the dosage should be selected individually.
Moxonidine is slightly excreted during hemodialysis.
Penetrates the blood-brain barrier.
Indications
Arterial hypertension.
Contraindications
SSSL
sinoatrial blockade
AV block II and III degree
severe bradycardia (heart rate less than 50 beats / min, )
chronic heart failure of the III and IV functional class according to NYHA classification
unstable angina pectoris
history of angioedema
severe liver failure (more than 9 points on the Child-Pugh scale)
chronic renal failure, Cc <30 ml > 160 μmol / L)
age up to 18 years (efficacy and safety not established)
lactation period
galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome
increased chu ity of a moxonidine and other components Tenzotran drug.
With caution, the drug should be used for Parkinson’s disease (severe), epilepsy, glaucoma, depression, intermittent claudication, Raynaud’s disease, degree I AV block, chronic renal failure (CC> 30 ml / min, but <60 ml / min), severe cerebrovascular disorders, after myocardial infarction, chronic heart failure of functional classes I and II, impaired liver function, hemodialysis, during pregnancy. Use during pregnancy and lactation There is no clinical evidence of a negative effect on pregnancy. However, Tenzotran should be prescribed to pregnant women only if the potential benefit to the mother outweighs the potential risk to the fetus. moxonidine passes into breast milk, during treatment, women are advised to stop breastfeeding or to discontinue the drug. Composition 1 tablet contains: active ingredients: moxonidine 0.4 mg excipients: lactose monohydrate, povidone – K25, crospovidone, magnesium stearate, Opadry Y-1-7000, iron dye red oxide. Dosage and administration Inside, regardless of food intake, with plenty of fluids. In most cases, the initial dose of Tenzotran is 0.2 mg per day at a time, preferably in the morning. If the therapeutic effect is insufficient, the dose can be increased after 3 weeks of therapy to 0.4 mg per day in 2 divided doses (morning and evening) or once (in the morning). The maximum daily dose, which should be divided into 2 doses (morning and evening), is 0.6 mg. The maximum single dose is 0.4 mg. In elderly patients with normal renal function, the dosage recommendations are the same as for adult patients. In patients with renal failure (CC from 30-60 ml / min.) and patients those on hemodialysis, a single dose should not exceed 0.2 mg. The maximum daily dose is 0.4 mg. Side effects Most often, especially at the beginning of therapy: dry mouth, headache, asthenia and drowsiness. The intensity of their manifestation and frequency decrease with repeated use. Determination of the frequency of adverse reactions: 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 cardiovascular system: often – vasodilation, sometimes – a marked decrease in blood pressure, orthostatic hypotension, paresthesia, Raynaud’s syndrome, peripheral circulation disorders. From the nervous system: often – increased fatigue, drowsiness, headache, dizziness, sometimes – insomnia, asthenia. From the digestive tract: dry oral mucosa often – nausea, constipation and other disorders of the gastrointestinal tract sometimes – anorexia is very rare – hepatitis, cholestasis. Allergic reactions: sometimes – skin manifestations, angioedema. From the urinary system: sometimes – urinary retention or incontinence. From the reproductive system: sometimes – impotence, decreased libido, gynecomastia. From the side of the organ of vision: sometimes – dry eyes, causing itching or burning sensation. Other: sometimes – edema of various localization, weakness in the legs, fainting, fluid retention, pain in the parotid glands. Drug Interaction Moxonidine can be prescribed with thiazide diuretics, slow calcium channel blockers, and other antihypertensive agents. Co-administration of moxonidine with these and other antihypertensive agents leads to an additive effect and an increased antihypertensive effect. When prescribing moxonidine with hydrochlorothiazide, glibenclamide (glyburide) or digoxin no pharmacokinetic interaction. Tricyclic antidepressants may reduce the effectiveness of central antihypertensive agents, so it is not recommended that tricyclic antidepressants be given concomitantly with moxonidine. Moxonidine moderately enhances impaired cognitive performance in patients receiving lorazepam. The appointment of moxonidine with benzodiazepines may be accompanied by an increase in the sedative effect of the latter. Moxonidine can potentiate the effect of ethanol when used together. There is no pharmacodynamic interaction when moxonidine is co-administered with moclobemide. overdose There have been reports of multiple overdose cases with lethal outcomes when doses up to 19 were administered, 6 mg per dose. Symptoms: headache, sedation, drowsiness, marked BP, dizziness, asthenia, bradycardia, dry mouth, vomiting and stomach pain, fatigue. Potentially also possible: short-term increase in blood pressure, tachycardia, hyperglycemia. Treatment: There is no specific antidote. Gastric lavage, activated charcoal and laxatives, symptomatic therapy. In case of marked decrease in blood pressure, it is recommended to restore the volume of circulating blood due to the introduction of fluid and the introduction of dopamine. Bradycardia can be stopped with atropine. Alpha-adrenoceptor antagonists may reduce or eliminate transient hypertension in the case of overdose with moxonidine. Storage conditions At a temperature not exceeding 30 ° C. Keep out of the reach of children! Expiration 2 years. Deystvuyuschee substances Moksonydyn dosage form dosage form tablets Perrigo Israel Pharmaceuticals Ltd., Israel
