Physiotens pills 0.2mg, 28pcs

Composition

Active ingredient:

moxonidine 0.2 mg.

Auxiliary substances:

lactose monohydrate-95.80 mg,

povidone-0.70 mg,

crospovidone-3.00 mg,

magnesium stearate-0.30 mg.

Shell:  hypromellose – 1.30 mg, ethylcellulose-1.20 mg, macrogol-0.25 mg, talc-0.9975 mg, iron oxide red dye (E 172) – 0.0025 mg, titanium dioxide (E 171) – 1.25 mg

Pharmacological action

Moxonidine is an antihypertensive agent with a central mechanism of action. In the brain stem structures (rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazoline-sensitive receptors involved in the tonic and reflex regulation of the sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure (BP).

Moxonidine differs from other sympatholytic antihypertensive agents by a lower affinity for a2-adrenergic receptors, which explains the lower probability of developing sedation and dry mouth.

Taking moxonidine leads to a decrease in systemic vascular resistance and blood pressure. The antihypertensive effect of moxonidine was confirmed in double-blind, placebo-controlled, randomized trials.

Moxonidine improves the insulin sensitivity index by 21% (compared to placebo) in patients with obesity, insulin resistance and moderate arterial hypertension.

Pharmacokinetics

Suction:  After oral use, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. Absolute bioavailability is approximately 88%. The time to reach the maximum concentration is about 1 hour. Food intake does not affect the pharmacokinetics of the drug.

Distribution The binding to plasma proteins is 7.2%.

Metabolism The main metabolite is dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 10% compared to moxonidine.

Deduction The elimination half-lives (T 1/2) of moxonidine and the metabolite are 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys (about 78% in unchanged form and 13% in the form of dehydromoxonidine, other metabolites in the urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestine.

Pharmacokinetics in patients with arterial hypertension:  

Compared with healthy volunteers, patients with arterial hypertension showed no changes in the pharmacokinetics of moxonidine.

Pharmacokinetics in the elderly

Clinically insignificant changes in the pharmacokinetic parameters of moxonidine in elderly patients were noted, probably due to a decrease in the intensity of its metabolism and/or slightly higher bioavailability.

Pharmacokinetics in children

Moxonidine is not recommended for use in persons under 18 years of age, and therefore no pharmacokinetic studies have been conducted in this group.

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 final T 1/2 are approximately 2 and 1.5 times higher than in patients with normal renal function (creatinine clearance greater than 90 ml/min). In patients with severe renal insufficiency (creatinine clearance less than 30 ml/min), steady-state plasma concentrations and final T 1/2 are 3 times higher than in patients with normal renal function. use of multiple doses of moxonidine leads to predictable accumulation in the body of patients with moderate to severe renal insufficiency.

In patients with end-stage renal insufficiency (creatinine clearance less than 10 ml/min) undergoing hemodialysis, the steady-state plasma concentrations and final T 1/2 are 6 and 4 times higher, respectively, than in patients with normal renal function. In all groups, the maximum concentration of moxonidine in blood plasma is 1.5 – 2 times higher. In patients with impaired renal function, the dosage should be selected individually. Moxonidine is slightly eliminated during hemodialysis.

Indications

Arterial hypertension.

Use during pregnancy and lactation

Pregnancy: There are no clinical data on the use of Fiziotenz® in pregnant women. In the course of animal studies, the embryotoxic effect of the drug was established. Fiziotenz® should be prescribed to pregnant women only after careful assessment of the risk-benefit ratio, when the benefit to the mother exceeds the potential risk to the fetus. Breast-feeding period: moxonidine is excreted in breast milk and should therefore not be administered during breast-feeding. If it is necessary to use the drug Fiziotenz® during lactation, breastfeeding should be discontinued.

Contraindications

Hypersensitivity to the Active ingredient and other components of the drug; sinus node weakness syndrome, severe bradycardia (resting heart rate less than 50 beats / min).

Hereditary problems of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.

Due to the lack of safety and efficacy data, moxonidine is not recommended for people under 18 years of age.

With caution:  severe and terminal renal insufficiency; patients undergoing hemodialysis; due to lack of experience with the use-severe liver failure (more than 9 points according to the Child-Pugh classification).

Side effects

From the central nervous system:  Common (1-10%): headache, dizziness, drowsiness. Infrequently (

From the cardiovascular system:  Rarely (

From the gastrointestinal tract:  Common (1-10%): dry mouth. Infrequently (

Skin and subcutaneous fat disorders: Infrequently ( Very rare (: angioedema.

Common:  Common (1-10%): asthenia.

The most common side effects in patients taking moxonidine are dry mouth, headache, dizziness, asthenia, and drowsiness. These symptoms often decrease after the first weeks of therapy.

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.

No pharmacokinetic interactions were observed when moxonidine was administered with hydrochlorothiazide, glibenclamide, or digoxin.

Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive drugs, and therefore they are not recommended to be taken together with moxonidine.

Moxonidine is able to moderately improve impaired cognitive function in patients receiving lorazepam.

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

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.

In most cases, the initial dose of Physiotenz ® is 0.2 mg per day. The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 doses, is 0.6 mg.

The daily dose for patients with moderate or severe renal insufficiency, as well as those on hemodialysis is 0.2 mg. If necessary and with good tolerability, the daily dose can be increased to 0.4 mg.

Overdose

Several cases of non-fatal overdose have been reported with simultaneous doses of up to 19.6 mg.

Symptoms:

headache, sedation, drowsiness, marked decrease in blood pressure, dizziness, fatigue, asthenia, bradycardia, dry mouth, vomiting and epigastric pain. A short-term increase in blood pressure, tachycardia, and hyperglycemia are also potentially possible.

Treatment:

There is no specific antidote. In the case of a 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 the paradoxical hypertensive effects of moxonidine overdose.

Description

Film-coated tablets of pale pink color, round, biconvex, with the inscription “0,2” on one side; on the break – white color.

Special instructions

If it is necessary to cancel the simultaneous use of beta-blockers and Fiziotenz, first cancel beta-blockers and, only after a few days, Fiziotenz®.

During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary. Stop taking the drug “Fiziotenz” should be gradually.

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

Studies of the effect of the drug on the ability to drive a car and other mechanisms have not been conducted.

Drowsiness and dizziness have been reported during treatment with moxonidine. This should be taken into account when performing the above actions.

Shelf life

1 year

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