Composition and release form
| Film-coated tablets | 1 table |
| moxonidine | 0.2 mg |
| excipients: lactose monohydrate - 95.8 mg; povidone - 0.7 mg; crospovidone - 3 mg; magnesium stearate - 0.3 mg; hypromellose - 1.3 mg; ethylcellulose - 4 mg; macrogol 6000 - 0.25 mg; talc - 0.9975 mg; iron oxide red (E172) - 0.0025 mg; titanium dioxide (E171) - 1.25 mg |
14 pcs in blister; There are 1, 2 or 7 blisters in a box.
| Film-coated tablets | 1 table |
| moxonidine | 0.3 mg |
| excipients: lactose monohydrate - 95.7 mg; povidone - 0.7 mg; crospovidone - 3 mg; magnesium stearate - 0.3 mg; hypromellose - 1.3 mg; ethylcellulose - 4 mg; macrogol 6000 - 0.25 mg; talc - 0.975 mg; iron oxide red (E172) - 0.025 mg; titanium dioxide (E171) - 1.25 mg |
14 pcs in blister; There are 1, 2 or 7 blisters in a box.
| Film-coated tablets | 1 table |
| moxonidine | 0.4 mg |
| excipients: lactose monohydrate - 95.6 mg; povidone - 0.7 mg; crospovidone - 3 mg; magnesium stearate - 0.3 mg; hypromellose - 1.3 mg; ethylcellulose - 4 mg; macrogol 6000 - 0.25 mg; talc - 0.875 mg; iron oxide red (E172) - 0.125 mg; titanium dioxide (E171) - 1.25 mg |
14 pcs in blister; There are 1, 2 or 7 blisters in a box.
Analogues of Physiotenza
Level 4 ATC code matches: Tenzotran
Moxonitex
Albarel
Moxonidine
Clonidine
The most common analogue of Physiotens is a drug called moxogama . It contains the same active ingredient.
Other analogues: tenaxum, clonidine (various productions), estupik .
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.
Pharmacodynamics and pharmacokinetics
The active substance directly affects the imidazoline receptors of the central nervous system located in the medulla oblongata . This leads to a decrease in sympathetic activity. With. , and blood pressure decreases.
Due to the fact that imidazole has low affinity for alpha-adrenergic receptors , such common side effects as dry mucous membranes and pronounced sedation practically do not occur.
Depending on food intake, within an hour after administration, the maximum concentration of the active substance in the blood is observed. About 7% is bound to plasma proteins . In the body it is metabolized into guanine and 4,5-dihydromoxonidine (they are eliminated within 5 hours). Moxonidine itself is excreted within 24 hours, mainly by the kidneys.
Pharmacokinetic parameters change in liver and kidney diseases and slightly in elderly people.
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.
Instructions for use PHYSIOTENS®
Suction
After oral administration, moxonidine is rapidly and almost completely absorbed from the upper gastrointestinal tract. Absolute bioavailability is approximately 88%, indicating no significant first-pass metabolism through the liver. The time to reach Cmax is about 1 hour. Food intake does not affect the pharmacokinetics of the drug.
Distribution
Plasma protein binding, as determined in vivo, is 7.2%.
Metabolism
Based on the totality of analyses, only one metabolite of moxonidine was detected - dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 10% compared to moxonidine.
Removal
T1/2 of moxonidine and metabolite is 2.5 and 5 hours, respectively. Within 24 hours, 78% of the administered dose of the drug is excreted unchanged in the urine and 13% as dehydrated moxonidine; other metabolites in the urine account for approximately 8% of the dose taken. Less than 1% of the dose is excreted through the intestines.
Pharmacokinetics in special clinical situations
Compared with healthy volunteers, patients with arterial hypertension show no changes in the pharmacokinetics of moxonidine.
Clinically insignificant changes in the pharmacokinetic parameters of moxonidine were noted in elderly patients, probably due to a decrease in the intensity of its metabolism and/or slightly higher bioavailability.
Moxonidine is not recommended for use in children and adolescents under the age of 18 years, and therefore pharmacokinetic studies have not been conducted in this group.
Moxonidine excretion is significantly correlated with CC. In patients with moderate renal failure (creatinine clearance 30-60 ml/min), steady-state plasma concentrations and final T1/2 are approximately 2 and 1.5 times higher than in individuals with normal renal function (creatinine clearance more than 90 ml/min). In patients with severe renal failure (creatinine clearance less than 30 ml/min), steady-state plasma concentrations and final T1/2 are 3 times higher than in patients with normal renal function. The administration of multiple doses of moxonidine leads to predictable accumulation in the body of patients with moderate and severe renal failure.
In patients with end-stage renal failure (creatinine clearance less than 10 ml/min) on hemodialysis, the AUC value 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 dose should be adjusted individually.
Moxonidine is excreted to a small extent during hemodialysis.
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.
Physiotenza price (where to buy)
The price of Physiotenza with a dosage of 0.4 mg is about 420 rubles for 14 pieces. The cost of the same amount of 0.2 mg is 266 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Physiotens tab.
p/o captivity. 0.2 mg 98 pcs. JSC Veropharm RUB 1,836 order - Physiotens tablets p.p.o. 0.4 mg 28 pcs. JSC Nobel Almaty Pharmaceutical Factory/JSC VEROPHARM
RUB 863 order
- Physiotens tab. p/o captivity. 0.4 mg No. 14 JSC Nobel Almaty Pharmaceutical Factory/JSC VEROPHARM
RUR 454 order
- Physiotens tab. p/o captivity. 0.4 mg 14 pcs. JSC Veropharm
RUR 448 order
- Physiotens tab. p/o captivity. 0.4 mg 28 pcs. JSC Veropharm
RUB 882 order
Pharmacy Dialogue
- Physiotens tablets 0.2 mg No. 28Maylan
489 RUR order
- Physiotens tablets 0.4 mg No. 28Nobel Almatinksaya FF/Veropharm
RUB 884 order
- Physiotens (tab.p.pl/vol. 0.4 mg No. 14) Veropharm
RUB 487 order
- Physiotens tablets 0.2 mg No. 14Rottendorf/Maylan
RUB 279 order
- Physiotens tablets 0.2 mg No. 28Nobel Almatinksaya FF/Veropharm
570 rub. order
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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.
Physiotens®
Suction
After oral administration, moxonidine is rapidly and almost completely absorbed from the upper gastrointestinal tract. Absolute bioavailability is approximately 88%, indicating no significant first-pass effect.
The time to reach 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.
Removal
The half-life (T1/2) of moxonidine and metabolite is 2.5 and 5 hours, respectively. Within 24 hours, over 90% of moxonidine is excreted by the kidneys (about 78% unchanged and 13% as dehydriromoxonidine, other metabolites in the urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestines.
Pharmacokinetics in patients with arterial hypertension
Compared with healthy volunteers, patients with arterial hypertension show no changes in the pharmacokinetics of moxonidine.
Pharmacokinetics in old age
Clinically insignificant changes in the pharmacokinetic parameters of moxonidine were noted in elderly patients, 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 renal failure
Moxonidine excretion is significantly correlated with creatinine clearance (CC). In patients with moderate renal failure (creatinine clearance in the range of 30-60 ml/min), steady-state plasma concentrations and final T1/2 are approximately 2 and 1.5 times higher than in individuals with normal renal function (creatinine clearance more than 90 ml/min). min).
In patients with severe renal failure (creatinine clearance less than 30 ml/min), steady-state plasma concentrations and final T1/2 are 3 times higher than in patients with normal renal function.
The administration of multiple doses of moxonidine leads to predictable accumulation in the body of patients with moderate and severe renal failure.
In patients with end-stage renal failure (creatinine clearance less than 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 moderate renal failure, the maximum concentration of moxonidine in the blood plasma is 1.5-2 times higher.
In patients with impaired renal function, the dosage should be adjusted individually. Moxonidine is excreted to a small extent during hemodialysis.
