Instruction for use: Physiotens

Dosage form: Coated tablets; Film-coated tablets

Active substance: Moxonidinum

ATX

C02AC05 Moxonidine

Pharmacological group

Hypotensive central agent [I1-imidazoline receptor agonists]

Nosological classification (ICD-10)

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

Composition and release form

Tablets, coated with a coating.

Moxonidine 0.2 mg

Auxiliary substances: lactose monohydrate - 95.8 mg; Povidone 0.7 mg; Crospovidone - 3 mg; Magnesium stearate - 0.3 mg; Hypromellose - 1.3 mg; Ethyl cellulose - 4 mg; Macrogol 6000 - 0.25 mg; Talc - 0.9975 mg; Iron oxide red (E172) - 0.0025 mg; Titanium dioxide (E171) 1.25 mg

In a blistere of 14 pcs .; In the box 1, 2 or 7 blisters.

Tablets, coated with a coating.

Moxonidine 0.3 mg

Auxiliary substances: lactose monohydrate - 95.7 mg; Povidone 0.7 mg; Crospovidone - 3 mg; Magnesium stearate - 0.3 mg; Hypromellose - 1.3 mg; Ethyl cellulose - 4 mg; Macrogol 6000 - 0.25 mg; Talc - 0.975 mg; Iron oxide red (E172) - 0.025 mg; Titanium dioxide (E171) 1.25 mg

In a blistere of 14 pcs .; In the box 1, 2 or 7 blisters.

Tablets, coated with a coating.

Moxonidine 0.4 mg

Auxiliary substances: lactose monohydrate - 95.6 mg; Povidone 0.7 mg; Crospovidone - 3 mg; Magnesium stearate - 0.3 mg; Hypromellose - 1.3 mg; Ethyl cellulose - 4 mg; Macrogol 6000 - 0.25 mg; Talc - 0.875 mg; Iron oxide red (E172) - 0.125 mg; Titanium dioxide (E171) 1.25 mg

In a blistere of 14 pcs .; In the box 1, 2 or 7 blisters.

Description of dosage form

Round, biconcave, coated tablets:

With a dosage of 0.2 mg - a pale pink color, labeled "0.2" on one side;

With a dosage of 0.3 mg - a pale red color, labeled "0.3" on one side;

With a dosage of 0.4 mg - matte-red color, with the mark "0,4" on one side.

Two layers are visible on the cross-section.

Pharmachologic effect

Mode of action - hypotensive.

Pharmacodynamics

Selectively interacting with imidazoline I1-receptors located in the brainstem reduces sympathetic activity.

Moxonidine has a high affinity for imidazoline I1 receptors and only slightly binds to central alpha2-adrenergic receptors due to interaction with which dry mouth and sedation are explained.

Reduces the resistance of tissues to insulin.

Influence 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 pressure of the sympathetic system on the peripheral vessels, a reduction in peripheral vascular resistance, while cardiac output and heart rate do not change significantly.

Pharmacokinetics

Suction

Absorption - 90%. Cmax in blood plasma (after taking a tablet containing 0.2 mg of moxonidine) is 1.4-3 ng / ml and is achieved after 60 minutes. Bioavailability - 88% (eating does not affect the pharmacokinetics).

Distribution

The volume of distribution is 1.4-3 l / kg. It penetrates through the BBB. Binding to plasma proteins - 7.2%.

Metabolism

The main metabolites are 4,5-dihydromoxonidine and guanidine derivatives.

Excretion

T1 / 2 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% as a dehydrogenated derivative. Less than 1% is excreted with feces. Do not cumulate with prolonged use.

Pharmacokinetics in old age

There are age-related changes in pharmacokinetics, probably associated with slightly higher bioavailability and / or reduced metabolic activity. However, these changes are not clinically significant.

Pharmacokinetics in renal failure

The excretion of moxonidine is largely correlated with the clearance of creatinine. In patients with moderate renal insufficiency (Cl creatinine in the range 30-60 ml / min), the equilibrium plasma concentrations and final T1 / 2 are approximately 2 and 1.5 times higher than in patients with arterial hypertension with normal renal function (Cl creatinine > 90 ml / min). In patients with severe renal insufficiency (Cl creatinine <30 ml / min), the equilibrium concentrations in the blood plasma and the final T1 / 2 are 3 times higher than in persons with normal renal function. The appointment of multiple doses of the drug does not lead to cumulation in the body of patients with moderate renal insufficiency. In the late stages of patients with extremely severe renal failure (Cl creatinine <10 ml / min) on hemodialysis, the equilibrium plasma concentrations and final T1 / 2, respectively, are 6 and 4 times higher than in patients with normal renal function. In patients with renal impairment, the dosage should be individualized. Moxonidine is slightly excreted in hemodialysis.

Indications of Physiotens

Arterial hypertension.

Contraindications

Hypersensitivity to the components of the drug;

Syndrome of weakness of the sinus node, pronounced bradycardia;

Age to 18 years (effectiveness and safety not established).

Carefully:

Severe chronic renal failure and severe hepatic insufficiency (due to lack of experience of use);

hemodialysis.

Application in pregnancy and lactation

There are no clinical data on the negative effect on the course of pregnancy. However, care should be taken when prescribing Physiotens® to pregnant women. During the period of treatment, it is recommended to stop breastfeeding, tk. Moxonidine penetrates into breast milk.

Side effects

From the side of the central nervous system: dizziness, headache, drowsiness, sleep disturbance.

From the cardiovascular system: excessive reduction of blood pressure, orthostatic hypotension.

From the digestive tract: dry mouth, nausea.

From the skin and subcutaneous fat: skin rash, itching, angioedema.

General: asthenia.

These symptoms usually decrease gradually during the first weeks of treatment.

Interaction

Possible joint use with thiazide diuretics, ACE inhibitors and slow calcium channel blockers. There is a mutual reinforcement of action when combined with these and other antihypertensive agents.

There is no pharmacokinetic interaction with hydrochlorothiazide (possibly combined use), glibenclamide (glyburide), digoxin. Tricyclic antidepressants may reduce the effectiveness of antihypertensive agents of central action (joint use is not recommended). Moderately increases the reduced cognitive ability in patients taking lorazepam. Enhances the sedative effect of benzodiazepines. There is no pharmacodynamic interaction when co-administered with moclobemide.

Dosing and Administration

Inside, regardless of food intake, the initial dose (in most cases) - 0.2 mg per day; The maximum daily dose is 0.6 mg (divided into 2 divided doses); The maximum single dose is 0.4 mg;

With renal insufficiency (Cl creatinine 30-60 ml / min) and in patients on hemodialysis, a single dose of 0.2 mg, the maximum daily - 0.4 mg.

Overdose

Symptoms: headache, sedation, drowsiness, excessive lowering of blood pressure, dizziness, general weakness, bradycardia, dry mouth, vomiting, fatigue and stomach pain. Potential short-term increases in blood pressure, tachycardia, hyperglycemia are possible.

Treatment: antagonists of alpha-adrenergic receptors can reduce or eliminate paradoxical arterial hypertension. In the case of hypotension, the recovery of BCC due to fluid administration and dopamine administration is recommended. Bradycardia can be stopped with atropine. There is no specific antidote.

Special instructions

If it is necessary to cancel simultaneously taken beta-blockers and Physiotense, first abolish beta-blockers and only after a few days - Physiotens®. During treatment, regular monitoring of blood pressure, heart rate, and ECG is necessary. Stop taking Fiziootenz gradually. Patients with a rare hereditary pathology of intolerance to galactose, deficiency of lactase or malabsorption of glucose-galactose should not take this drug.

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.

Manufacturer by

Solvay Pharmaceuticals GmbH, Germany.

Conditions of supply of pharmacies

On prescription.

Storage conditions of the drug Physiotens

At a temperature not exceeding 25 ° C.

Keep out of the reach of children.

The shelf life of the drug Physiotens

Tablets, coated with 0.2 mg - 2 years.

Tablets coated with 0.4 mg - 3 years.

Tablets coated with 0.3 mg - 3 years.

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