Tenzotran pills 0.4mg, 28pcs

Composition

1 tablet contains:  

active ingredients:  

• moxonidine 0.4 mg;

excipients:

• lactose monohydrate,

• povidone-K 25,

• crospovidone,

• magnesium stearate,

• Opadray Y-1-7000,

• iron oxide red dye.

Pharmacological action

Tensotran is a central antihypertensive agent.

Selective agonist of imidazoline receptors responsible for reflex control of the sympathetic nervous system (located in the venterolateral medulla oblongata).

It has a low affinity for central alpha-2-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 use 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 change significantly.

Pharmacokinetics

After oral use, moxonidine is rapidly and almost completely absorbed from the upper gastrointestinal tract. Tmax is approximately 1 h. Absolute bioavailability is approximately 88%, and the “first pass” metabolism through the liver is insignificant. Food intake does not affect the pharmacokinetics of the drug.

The binding to plasma proteins is 7.2%.

Main metabolite: dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 1/10 compared to moxonidine. T1 / 2 of moxonidine and its 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 the urine account for approximately 8% of the dose. Less than 1% of the dose is excreted through the intestine.

Pharmacokinetics in patients with renal insufficiency

Moxonidine clearance is strongly correlated with creatinine clearance (CC). In patients with moderate renal insufficiency (creatinine clearance in the range of 30-60 ml/min), steady-state 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 (creatinine clearance of more than 90 ml/min).

In patients with severe renal insufficiency (creatinine clearance less than 30 ml/min), steady-state plasma concentrations and the final half-life are 3 times higher than in patients with normal renal function.

use of multiple doses of moxonidine does not lead to accumulation in the body of patients with moderate and severe renal insufficiency.

In late-stage patients with end-stage renal insufficiency (creatinine clearance less than 10 ml/min) undergoing hemodialysis, the steady-state plasma concentrations and terminal 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 eliminated during hemodialysis.

Penetrates the blood-brain barrier.

Use during pregnancy and lactation

There are no clinical data on the negative effect on the course of pregnancy. However, Tenzotran should only be prescribed to pregnant women if the potential benefit to the mother outweighs the potential risk to the fetus.

Moxonidine penetrates into breast milk, and women are advised to stop breastfeeding or discontinue the drug during treatment.

Contraindications

• SSSU;
• sinoatrial block;
• AV-block II and III degree,
• severe bradycardia (heart rate less than 50 beats/min);
• chronic heart failure III and IV functional class NYHA classification;
• unstable angina;
• a history of angioedema;
• severe hepatic impairment (more than 9 points on a scale child-Pugh);
• chronic renal failure (KK < 30 ml/min, serum creatinine > 160 µmol/l);
• the age of 18 years (effectiveness and safety not established);
• lactation;
• galactose intolerance, lactase deficiency or malabsorption syndrome glucose-galactose;
• hypersensitivity to moxonidine and other components of the drug Tensitron.

The drug should be used with caution in patients with Parkinson’s disease (severe form), epilepsy, glaucoma, depression, intermittent claudication, Raynaud’s disease, AV block I degree, chronic renal failure (creatinine clearance > 30 ml/min, but >

Side effects

Most often, especially at the beginning of therapy: dry mouth, headache, asthenia and drowsiness. Their intensity 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 reports).

From the cardiovascular system:  often-vasodilation; sometimes-a marked decrease in blood pressure, orthostatic hypotension, paresthesia, Raynaud’s syndrome, peripheral circulatory disorders.

Nervous system disorders:  often – increased fatigue, drowsiness, headache, dizziness; sometimes-insomnia, asthenia.

From the digestive tract:  dryness of the oral mucosa; often – nausea, constipation and other gastrointestinal disorders; sometimes-anorexia; very rarely-hepatitis, cholestasis.

Allergic reactions:  sometimes-skin manifestations, angioedema.

From the urinary system:  sometimes-urinary retention or incontinence.

From the side of the reproductive system:  sometimes-impotence, decreased libido, gynecomastia.

From the side of the visual organ:  sometimes-dry eyes that cause itching or burning sensation.

Other services:  sometimes-edema of various localization, weakness in the legs, fainting, fluid retention, pain in the parotid glands

Interaction

Moxonidine can be administered with thiazide diuretics, slow calcium channel blockers, and other antihypertensive agents.

The combined use of moxonidine with these and other antihypertensive agents leads to an additive effect and an increase in the hypotensive effect.

When moxonidine is administered with hydrochlorothiazide, glibenclamide (glyburide) or digoxin, there is no pharmacokinetic interaction.

Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive agents, so it is not recommended to prescribe tricyclic antidepressants simultaneously with moxonidine.

Moxonidine modestly enhances cognitive decline in patients taking lorazepam.

The use of moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter. Moxonidine may potentiate the effect of ethanol when used together.

When moxonidine is co-administered with moclobemide, there is no pharmacodynamic interaction.

How to take, course of use and dosage

Inside, regardless of food intake, with a sufficient amount of liquid. In most cases, the initial dose of Tenzotran is 0.2 mg per day in one dose, 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 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 insufficiency (creatinine clearance from 30-60 ml / min) and patients on hemodialysis, a single dose should not exceed 0.2 mg. The maximum daily dose is 0.4 mg.

Overdose

Several cases of non-fatal overdose have been reported when doses of up to 19.6 mg per dose were used.

Symptoms:  headache, sedation, drowsiness, marked decrease in blood pressure, dizziness, asthenia, bradycardia, dryness of the oral mucosa, vomiting and stomach pain, increased fatigue. Potentially also possible: short-term increase in blood pressure, tachycardia, hyperglycemia.

Treatment:  there is no specific antidote. Gastric lavage, taking activated charcoal and laxatives, symptomatic therapy.

In the case of a marked decrease in blood pressure, it is recommended to restore the volume of circulating blood through the introduction of fluid and the introduction of dopamine. Bradycardia can be treated with atropine.

Alpha-adrenergic antagonists may reduce or eliminate transient hypertension in the case of moxonidine overdose.

Special instructions

If it is necessary to cancel simultaneously taken beta-blockers and Tensotran, first cancel beta-blockers and, only after a few days, Tensotran.

It is not recommended to prescribe tricyclic antidepressants simultaneously with Tensotran.

During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary.

Moxonidine can be given with thiazide diuretics, angiotensin converting enzyme (ACE) inhibitors, and slow calcium channel blockers.

Stop taking Tensotran gradually.

Patients with rare hereditary problems of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take this medicine.

Influence on the ability to drive a car and to control machines and mechanisms

There are no data on the adverse effect of moxonidine on the ability to drive a car and to control machines and mechanisms. Drowsiness and dizziness have been reported during treatment with moxonidine. This should be taken into account when performing the above actions.

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Moxonidine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Hypertension