PHYSIOTENZ film-coated tablets 0.2 mg No. 14

Composition and release form

14 pcs in blister; There are 1, 2 or 7 blisters in a box.

14 pcs in blister; There are 1, 2 or 7 blisters in a box.

14 pcs in blister; There are 1, 2 or 7 blisters in a box.

Pharmacodynamics

Selectively interacting with imidazoline I1 receptors located in the brain stem, it 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 tissue resistance to insulin.

Effect on hemodynamics: a decrease in systolic and diastolic blood pressure with single and long-term use of moxonidine is associated with a decrease in the pressor effect of the sympathetic system on peripheral vessels, a decrease in peripheral vascular resistance, while cardiac output and heart rate do not change significantly.

Operating principle

Physiotens is an original drug manufactured by Abbott Products, located in the United States. This is a powerful, innovative drug, the main ingredient of which is moxonidine. The medication does not belong to the first group of drugs that have a positive effect on the body, gradually normalizing high blood pressure. However, there is a certain category of patients for whom this medicine is the drug of choice. This is explained not only by a pronounced hypotensive effect, but also by a strong influence on the metabolic process. A large number of clinical studies have shown that the active substance of the drug can prevent the development of insulin resistance. It can also quickly normalize the metabolic processes occurring in the body and eliminate any disturbances.

When using a drug called Physiotens, patients experience a dual mechanism of action. It provides not only short-term (usually through its effect on the sympathetic centers of the brain), but also long-term control of blood pressure by suppressing the release of renin. This is an enzyme that regulates high blood pressure. While taking the medication, the excretory function of the urinary system, in particular the kidneys, significantly improves. In real clinical practice, a medicine called Physiotens is often used as part of combination therapy.

Moxonidine is the active component of the drug, which differs significantly from classical drugs in that it acts for a long time over several hours (6-12 hours).

As for the features of the action, Physiotens has a strong stimulating effect on imidazoline receptors, which are located in the medulla oblongata. They play an important role in the central regulation of blood pressure. Modulate the activity of the sympatho-adrenal system. These receptors are also responsible for regulating the production of pancreatic hormones. The medication in question and all its analogues have therapeutic effects such as:

• Reduced hyperactivity of the sympathetic nervous system.
• Increased sensitivity of peripheral tissues to insulin.
• Significant improvement in fat metabolism indicators.
• Minimizing the concentration of glucose and leptin, a hormone in adipose tissue that is responsible for energy metabolism.

The drug significantly reduces the content of renin, aldosterone and angiotensin II in the blood plasma. These effects are extremely important for individuals who suffer from surges in blood pressure. It should be noted that a gradual decrease in the activity of the renin-angiotensin-aldosterone system can prevent the development and progression of all kinds of structural changes in the left ventricle of the heart muscle, as well as arteries, veins and capillaries.

In the course of research, while taking Physiotens, results were obtained that indicate a significant improvement in the diastolic function of the left ventricle of the heart muscle. If the patient took the medication for a long time, it was possible to reduce the increase in volume (hypertrophy) of the left ventricle.

Another interesting feature of the drug was discovered - if the initial blood pressure is very high, then it decreases more effectively than with a slight deviation from the norm. It is because of this that the possibility of eliminating the hypertensive crisis was considered.

Undesirable side effects such as dry mucous membranes and strong sedation are practically not found with the drug in question. This helps improve the tolerability of the medication.

Pharmacokinetics

Suction

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

Distribution

Volume of distribution - 1.4–3 l/kg. Penetrates through the BBB. Plasma protein binding - 7.2%.

Metabolism

Main metabolites: 4,5-dihydromoxonidine and guanidine derivatives.

Removal

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 a dehydrogenated derivative. Less than 1% is excreted in feces. Does not accumulate with prolonged use.

Pharmacokinetics in old age

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

Pharmacokinetics in renal failure

Moxonidine excretion is significantly correlated with creatinine clearance. In patients with moderate renal failure (Cl creatinine in the range of 30–60 ml/min), 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 failure (Cl creatinine <30 ml/min), steady-state plasma concentrations and final T1/2 are 3 times higher than in individuals with normal renal function. The administration of multiple doses of the drug does not lead to accumulation in the body of patients with moderate renal failure. At later stages, in patients with extremely severe renal failure (Cl creatinine <10 ml/min) on hemodialysis, steady-state plasma concentrations and final T1/2 are 6 and 4 times higher, respectively, than in patients with normal renal function. In patients with impaired renal function, the dosage should be adjusted individually. Moxonidine is excreted to a small extent during hemodialysis.

Physiotens 0.4 mg No. 14 tablet p.o.

Instructions for medical use of the drug Physiotens® Trade name Physiotens® International nonproprietary name Moxonidine Dosage form Film-coated tablets, 0.2 mg, 0.4 mg Composition One tablet contains the active substance - moxonidine 0.2 mg, or 0.4 mg, excipients: lactose monohydrate, povidone K25, crospovidone, magnesium stearate, shell composition: hypromellose 6 mPas, ethylcellulose 30% aqueous dispersion (in terms of dry matter), macrogol 6000, talc, red iron (III) oxide (E172), titanium dioxide (E171). Description Tablets are round in shape, with a biconvex surface, light pink film-coated, with “0.2” engraved on one side (for a dosage of 0.2 mg). Tablets are round in shape, with a biconvex surface, film-coated, pale red in color, with “0.4” engraved on one side (dosage 0.4 mg). Pharmacotherapeutic group Antihypertensive drugs. Central agonists. Alpha 2-adrenergic agonists are central, imidazoline derivatives. Moxonidine. ATC code C02AC05 Pharmacological properties Pharmacokinetics Absorption. When taken orally, moxonidine is rapidly and almost completely (Tmax about 1 hour) absorbed from the upper gastrointestinal tract. Absolute bioavailability is 88%, indicating the absence of primary hepatic metabolism. Food intake does not affect the pharmacokinetics of moxonidine. The binding to plasma proteins is 7.2%. Biotransformation. Only one metabolite of moxonidine is detected in the blood - dehydromoxonidine. Its pharmacological activity is 10 times less than moxonidine. Excretion. Within 24 hours, more than 78% of moxonidine is excreted by the kidneys, and 13% as dehydromoxonidine. Other, less significant metabolites are found in the urine in amounts of about 8% of the administered dose. Less than 1% of the dose is excreted in the feces in the form of metabolites: 4.5 dehydromoxonidine and guanidine derivatives. The half-life of moxonidine and its main metabolite is 2.5 and 5 hours, respectively. Pharmacokinetics in patients with arterial hypertension In patients with arterial hypertension, no changes in pharmacokinetics were detected. Pharmacokinetics in the Elderly In elderly patients, differences in the pharmacokinetics of moxonidine are observed compared to younger individuals, mainly due to reduced metabolic activity and/or increased bioavailability in the elderly. However, these pharmacokinetic differences are not clinically significant. Pharmacokinetics in children and adolescents under 18 years of age Pharmacokinetic studies in children and adolescents have not been conducted. Pharmacokinetics in renal failure The elimination of moxonidine is significantly correlated with creatinine clearance (CC). In patients with moderate renal failure (glomerular filtration rate (GFR) 30-60 ml/min), steady-state plasma concentrations and terminal half-life are, respectively, 2 and 1.5 times higher than in hypertensive patients with normal renal function ( GFR >90 ml/min). Moreover, the maximum plasma concentrations of moxonidine are 1.5-2 times higher in patients with moderate renal failure. In patients with severe renal impairment (GFR < 30 ml/min), steady-state plasma concentrations and terminal half-life are approximately 3 times higher than in hypertensive patients with normal renal function. Taking multiple doses does not lead to the accumulation of moxonidine in the body of patients in this group. In patients with end-stage renal disease (GFR < 10 mL/min) on dialysis, the area under the curve (AUC) and terminal half-life are 6 and 4 times higher, respectively, than in patients with normal renal function. Therefore, the dose of moxonidine in patients with renal failure should be titrated according to individual needs. Moxonidine is excreted to a small extent during hemodialysis. Pharmacodynamics Physiotens® is an antihypertensive drug. Available experimental data show that the localization of action of moxonidine is the central nervous system (CNS). Moxonidine has been shown to selectively stimulate imidazoline receptors in the brainstem. Imidazoline - sensitive receptors are concentrated in the rostral part of the ventrolateral part of the medulla oblongata - an area that is considered the center of regulation of the peripheral sympathetic nervous system. When imidazoline receptors are stimulated, the activity of the sympathetic nervous system decreases and blood pressure decreases. Moxonidine differs from other sympatholytic antihypertensive drugs by its low affinity for α2-adrenergic receptors compared to imidazoline receptors. This may explain the low likelihood of sedation and dry mouth with moxonidine. Moxonidine reduces blood pressure by reducing systemic vascular resistance, which has been proven in clinical studies. The antihypertensive effect of moxonidine has been demonstrated in double-blind, placebo-controlled, randomized studies. Published data show that in patients with hypertension and left ventricular hypertrophy (LVH), for similar blood pressure reduction, the use of an angiotensin II antagonist with moxonidine resulted in improved regression of LVH compared with the use of a combination of a thiazide diuretic and a calcium channel blocker. Moxonidine improves tissue sensitivity to insulin by 21% compared with placebo in obese and insulin-resistant patients with moderate hypertension. Indications for use: arterial hypertension. Method of administration and dosage. Tablets are taken orally with a sufficient amount of water, regardless of meals. In most cases, the initial dose of Physiotenza® is 0.2 mg per day; the maximum daily dose, which should be divided into 2 doses, is 0.6 mg. The maximum single dose is 0.4 mg. The dose and course of treatment are selected individually, depending on the clinical response. In patients with moderate or severe renal impairment, the initial dose of moxonidine is 0.2 mg per day. If necessary and well tolerated in patients with moderate renal failure, the dose of moxonidine can be increased to 0.4 mg per day, in patients with severe renal failure - up to 0.3 mg per day. In patients on hemodialysis, the initial dose is 0.2 mg per day. If necessary and well tolerated, the dose can be increased to 0.4 mg per day. The use of moxonidine in children and adolescents under 18 years of age is not recommended due to the lack of data on safety and effectiveness. Side effects Very common - dry mouth Common - dizziness, headache, drowsiness, insomnia, asthenia - diarrhea, nausea/vomiting, dyspepsia - rash, itching - back pain Uncommon - bradycardia, hypotension, including orthostatic hypotension - angioedema, peripheral swelling - pain in the neck - tinnitus - nervousness, fainting Contraindications - hypersensitivity to the components of the drug - sick sinus syndrome - bradycardia (resting heart rate less than 50 per minute) - atrioventricular block II or III degree - heart failure - children's and adolescence up to 18 years - pregnancy and lactation Drug interactions When Physiotens® is used together with other antihypertensive drugs, the effect is mutually enhanced. Since tricyclic antidepressants can reduce the effectiveness of centrally acting antihypertensive drugs, simultaneous use of Physiotens® with drugs of this group is not recommended. Physiotens® may enhance the sedative effect of tricyclic antidepressants (their coadministration should be avoided), tranquilizers, alcohol, sedatives and hypnotics. Physiotens® moderately improves reduced cognitive performance in patients taking lorazepam. Physiotens® enhances the sedative effect of benzodiazepines when taken together. Since Physiotens® is eliminated through tubular excretion, interaction with drugs that have the same route of elimination cannot be ruled out. Special instructions Physiotens® is prescribed with caution in patients with a possible predisposition to the development of atrioventricular block and in patients with 1st degree atrioventricular block in order to avoid bradycardia. Patients with severe coronary artery disease or unstable angina require careful monitoring, since experience with Physiotens® in this group of patients is limited. Particular caution must be exercised when using moxonidine in patients with severe coronary heart disease or unstable angina, since experience with the drug in this category of patients is limited. It is recommended to take precautions when prescribing Physiotens® to patients with renal failure, since moxonidine is excreted by the kidneys. These patients require careful dose selection, especially at the beginning of therapy. The initial dose of moxonidine should be 0.2 mg per day and, if clinically indicated and well tolerated, can be increased to a maximum of 0.4 mg per day in patients with moderate renal impairment (GFR > 30 ml/min but < 60 ml/min) and maximum up to 0.3 mg per day in patients with severe renal failure (GFR < 30 ml/min). If Physiotens® is taken in combination with a drug from the group of beta-blockers, then if it is necessary to cancel both drugs, first cancel the beta-blocker and only after a few days - Physiotens®. There is no withdrawal syndrome observed when stopping Physiotens. However, treatment should not be abruptly interrupted; It is recommended to gradually reduce the dose over two weeks. Patients with congenital galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take Physiotens®. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Overdose Symptoms: headache, sedation, drowsiness, hypotension, dizziness, asthenia, bradycardia, dry mouth, vomiting, fatigue and stomach pain. In cases of serious overdose, disturbances of consciousness and respiratory depression may occur. A short-term increase in blood pressure, tachycardia, and hyperglycemia are also potentially possible. Treatment: There are no specific antidotes. Hypotension may require dopamine administration and measures to maintain circulation, including infusion of solutions. Atropine can be used to eliminate bradycardia. Alpha-adrenergic antagonists may reduce or eliminate paradoxical hypertension. Release form and packaging 14 or 28 tablets are placed in a blister pack made of polyvinyl chloride film and aluminum foil. 1 blister pack together with instructions for medical use in the state and Russian languages ​​are placed in a cardboard pack. Storage conditions Store at a temperature not exceeding 25 ° C (for 0.2 mg). Store at a temperature not exceeding 30 °C (for 0.4 mg). Keep out of the reach of children! Shelf life: 2 years (for a dosage of 0.2 mg) 3 years (for a dosage of 0.4 mg) Do not use after the expiration date indicated on the package. Conditions for dispensing from pharmacies By prescription Name and country of the manufacturing organization Abbott Healthcare SAS, France Route de Belleville, Maillard 01400, Châtillon-sur-Chalaron Name and country of the holder of the marketing authorization Abbott Laboratories GmbH, Hannover, Germany Name and country of the packaging organization Abbott Healthcare CAC, France Route de Belleville, Maillard 01400, Chatillon-sur-Chalaron Address of the organization that accepts claims from consumers regarding product quality in the Republic of Kazakhstan Abbott Kazakhstan LLP 050059, Almaty, Dostyk Ave. 117/6, Business. tel., fax. Email

Interaction

Possible combined use with thiazide diuretics, ACE inhibitors and slow calcium channel blockers. There is a mutual enhancement of action when used together with these and other antihypertensive drugs.

There is no pharmacokinetic interaction with hydrochlorothiazide (combined use is possible), glibenclamide (glyburide), digoxin. Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive drugs (co-administration is not recommended). Moderately enhances reduced cognitive performance in patients taking lorazepam. Strengthens the sedative effect of benzodiazepines. There is no pharmacodynamic interaction when co-administered with moclobemide.

Overdose

Symptoms: headache, sedation, drowsiness, excessive decrease in blood pressure, dizziness, general weakness, bradycardia, dry mouth, vomiting, fatigue and stomach pain. A short-term increase in blood pressure, tachycardia, and hyperglycemia are potentially possible.

Treatment: Alpha-adrenergic antagonists may reduce or eliminate paradoxical hypertension. In case of hypotension, it is recommended to restore bcc through fluid administration and dopamine administration. Bradycardia can be relieved with atropine. There is no specific antidote.

special instructions

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

There is no data on the adverse effects of moxonidine on the ability to drive a car or operate machinery. There are reports of drowsiness and dizziness during treatment with moxonidine. This should be taken into account when performing the above steps.

Contraindications for use

The drug should not be prescribed to patients who suffer from sinus node weakness, severe bradycardia, lactose intolerance, or have hypersensitivity to the active substance of the drug.

Warning. Since no studies have been carried out regarding the effect of the main substance of the drug on the fetus, the drug in question is strictly forbidden to be taken by women in an interesting position.

You should be careful when taking Physiotens, as it can cause dizziness, sleep disturbances, headaches, and low blood pressure.