Tenzotran - instructions for use, dose, side effects, contraindications

lactose monohydrate - 94.5 mg, povidone - K25 - 2.0 mg, crospovidone - 3.0 mg, magnesium stearate - 0.3 mg; sheath - Opadry Y-1-7000 (titanium dioxide, 1.093 mg, hypromellose -2.186 mg, macrogol-400 - 0.219 mg) - 3.498 mg, ferric oxide red oxide - 0.002 mg.

Each tablet, film-coated, 0.4 mg contains:

active substance:

moxonidine 0.4 mg;

Excipients:

lactose monohydrate - 94.3 mg, povidone-K25 - 2.0 mg, crospovidone 3.0 mg, magnesium stearate - 0.3 mg; shell - Fill Y-1-7000 (titanium dioxide - 1.083 mg, hypromellose - 2.165 mg, macrogol-400 - 0.217 mg) - 3.465 mg; iron oxide dye red - 0.035 mg.

Description:

Tablets 0.2 mg: round tablets of light pink color, covered with a film membrane.

Tablets 0.4 mg: round tablets of dark pink color, covered with a film shell.

Pharmacotherapeutic group:central antihypertensive drug

ATX: & nbsp

C.02.A.C.05 Moxonidine

Pharmacodynamics:

Selective agonist imidazoline receptors responsible for reflex control of the sympathetic nervous system (localized in the ventro-lateral region of the medulla oblongata). Has a low affinity with central alpha₂-adrenoceptors, due to the interaction with which mediated sedation and dryness of the oral mucosa. Moxonidine improves the insulin sensitivity index by 21% compared with placebo in obese patients and insulin-resistant patients with moderate degree of hypertension.

Influence 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 the overall peripheral vascular resistance,while cardiac output and heart rate (heart rate) do not change significantly.

Pharmacokinetics:

After oral administration moxonidine quickly and almost completely absorbed from the upper part of the gastrointestinal tract (GIT). T_mOh (time to reach the maximum concentration) is approximately 1 hour. Absolute bioavailability is approximately 88%, the metabolism of the "first pass" through the liver is insignificant. Food intake does not affect the pharmacokinetics of the drug. The connection with plasma proteins is 7.2%.

The main metabolite: dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 1/10 compared to moxonidine.

The half-life of moxonidine and metabolites is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys, about 78% unchanged and 13% in the form of dehydrated 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 renal failure

The excretion of moxonidine is largely correlated with the clearance of creatinine (CC).In patients with moderate renal insufficiency (CK in the range of 30-60 ml / min.), The equilibrium concentrations in the blood plasma and the final half-life period are approximately 2 and 1.5 times higher than in patients with arterial hypertension with normal renal function (CC greater than 90 ml / min). In patients with severe renal insufficiency (KC less than 30 ml / min), the equilibrium concentrations in the blood plasma and the final half-life is 3 times higher than in patients with normal renal function. The administration of multiple doses of moxonidine does not result in cumulation in the body of patients with moderate and severe renal insufficiency. In the late stages of patients with terminal renal failure (CC less than 10 ml / min) on hemodialysis, the equilibrium concentrations in the blood plasma 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 in hemodialysis.

Penetrates through the blood-brain barrier

Indications:Arterial hypertension.

Contraindications:

Hypersensitivity to moxonidine and other components of the drug, syndrome of sinus node weakness, sinoatrial and atrioventricular blockade of II and III degree, pronounced bradycardia (heart rate less than 50 beats / min), chronic cardiac insufficiency III and IV of the functional class according to classification NYHA, anginaevrotichesky edema in the anamnesis, unstable angina, pronounced hepatic insufficiency (more than 9 points on the scale Child-Pugh), chronic renal failure (CC less than 30 ml / min, creatinine more than 160 μmol / l), age 18 years (efficacy and safety not established), lactation period; intolerance to galactose, deficiency of lactase or glucose-galactose malabsorption syndrome.

Carefully:

Parkinson's disease (severe), epilepsy, glaucoma, depression, "intermittent" claudication, Raynaud's disease, atrioventricular block I degree, chronic renal failure (creatinine clearance of more than 30 but less than 60 ml / min) expressed by cerebrovascular disorders, post-myocardial infarction , chronic heart failure of I and II functional class, violations of liver function, hemodialysis, pregnancy.

Pregnancy and lactation:

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

Moxonidine penetrates into breast milk, women during the period of treatment are recommended to stop breastfeeding or to cancel the drug.

Dosing and Administration:

Inside, regardless of food intake, with enough liquid.

In most cases, the initial dose of Tenzotran is 0.2 mg per day at one time, preferably in the morning hours. 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 divided doses (morning and evening), is 0.6 mg. The maximum single dose is 0.4 mg.

In elderly patients with normal renal function recommendations for dosage are the same as for adult patients.

In patients with renal insufficiency (SC from 30-60 ml / min.) And patients on hemodialysis, single dose should not exceed 0.2 mg.The maximum daily dose is 0.4 mg.

Side effects:

Especially at the beginning of therapy, the most frequent adverse reactions were: dry mouth, headache, asthenia and drowsiness. The intensity of their manifestation and frequency decrease upon repeated admission.

Frequency of development: 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 cardiovascular system: often - vasodilation; sometimes - marked decrease in blood pressure, orthostatic hypotension, paresthesia, Raynaud's syndrome, peripheral circulation disorders;

From the central nervous system: often - increased fatigue, drowsiness, headache, dizziness; sometimes - insomnia, asthenia;

From the side of the digestive tract: dryness of the oral mucosa; often - nausea, constipation and other abnormalities of the gastrointestinal function; very rarely - hepatitis, cholestasis;

From the skin and skin: sometimes - allergic reactions;

From the genitourinary system: sometimes - urinary retention or incontinence, impotence, decreased libido;

From the side of the organ of vision: sometimes - dry eyes, causing itching or burning sensation;

Other: sometimes - edema of different localization, weakness in the legs, angioedema, syncope, fluid retention, anorexia, pain in the parotid glands, gynecomastia.

Overdose:

There are reports of several cases of overdose without a lethal outcome, when doses up to 19.6 mg per dose were applied.

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

Treatment: there is no specific antidote. Gastric lavage, intake of activated carbon and laxatives, symptomatic therapy.

In the case of a marked decrease in blood pressure, it is recommended that the volume of circulating blood be restored by introducing a liquid and dopamine administration. Bradycardia can be stopped with atropine.

Alpha-adrenoreceptor antagonists can reduce or eliminate transient hypertension in an overdose of moxonidine.

Interaction:

Moxonidine may be prescribed with thiazide diuretics, blockers of "slow" calcium channels 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 can reduce the effectiveness of antihypertensive agents of central action, therefore it is not recommended to prescribe tricyclic antidepressants concomitantly with moxonidine.

Moxonidine moderately increases the reduced cognitive ability in patients taking lorazepam.

The administration of moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter.

Moxonidine can potentiate the effect of ethanol when combined.

When moxonidine is administered together with moclobemide, pharmacodynamic interaction is absent.

Special instructions:

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

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

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

Moxonidine may be administered with thiazide diuretics, angiotensin-converting enzyme (ACE) inhibitors, and blockers of "slow" calcium channels.

Stop taking Tenzotrana should be gradual.

Patients with a rare hereditary pathology of intolerance to galactose, deficiency of lactase or malabsorption of glucose-galactose should not take this drug.

Effect on the ability to drive transp. cf. and fur:

Data on the adverse effects of moxonidine on the ability to drive a car and to control machines and mechanisms are absent. There are reports of drowsiness and dizziness during treatment with moxonidine. This should be taken into account when carrying out the above actions.

Form release / dosage:

Tablets, film-coated, 0.2 mg and 0.4 mg.

Packaging:

For 14 tablets in a blister of PVC / PVDC / Al.

For 1, 2 or 3 blisters together with instructions for use in a cardboard box.

Storage conditions:

At a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

For a dosage of 0.2 mg - 2 years.

For a dosage of 0.4 mg - 3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000080/10

Date of registration:15.01.2010 / 09.04.2013

Expiration Date:Unlimited

The owner of the registration certificate:AKTAVIS GROUP, AO AKTAVIS GROUP, AO Iceland

Manufacturer: & nbsp

Perrigo Israel Pharmaceuticals LTD Israel

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp04.09.2016

Illustrated instructions

Instructions

Tenzotran (Tenzotran)