Physiotense - instructions for use, doses, side effects, contraindications

sheath: hypromellose - 1.30 mg, ethylcellulose - 1.20 mg, macrogol 0.25 mg, talc 0.9975 mg, iron oxide red (E 172) 0.0025 mg, titanium dioxide (E 171) -1 , 25 mg.

1 tablet, film-coated, with a dosage of 0.3 mg contains:

active substance: moxonidine 0.3 mg;

Excipients: lactose monohydrate - 95.70 mg, povidone - 0.70 mg, crospovidone - 3.00 mg, magnesium stearate - 0.30 mg;

sheath: hypromellose - 1.30 mg, ethyl cellulose - 1.20 mg, macrogol 0.25 mg, talc 0.975 mg, ferric oxide red oxide (E 172) 0.025 mg, titanium dioxide (E 171) 1.25 mg.

1 tablet, film-coated, with a dosage of 0.4 mg contains:

active substance: moxonidine 0.4 mg;

Excipients: lactose monohydrate - 95,60 mg, povidone - 0,70 mg, crospovidone - 3,00 mg, magnesium stearate - 0,30 mg;

sheath: hypromellose - 1.30 mg, ethyl cellulose - 1.20 mg, macrogol 0.25 mg, talc 0.875 mg, ferric oxide red oxide (E 172) 0.125 mg, titanium dioxide (E 171) - 1,25 mg.

Description:

Round biconvex tablets covered with a film membrane.

Tablets with a dosage of 0.2 mg - a pale pink color with engraving "0,2" on one side.

Tablets with a dosage of 0.3 mg - pink color with engraving "0,3" on one side.

Tablets with a dosage of 0.4 mg - brownish-pink color with engraving "0,4" with one side.

On the break the tablets are white.

Pharmacotherapeutic group:Hypotensive central agent

ATX: & nbsp

C.02.A.C.05 Moxonidine

Pharmacodynamics:

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

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

The administration of moxonidine leads to a decrease in systemic vascular resistance and blood pressure. The hypotensive effect of moxonidine is confirmed in double-blind, placebo-controlled, randomized studies.

The results of a clinical trial involving 42 patients with hypertension and left ventricular hypertrophy (LVH) demonstrated that with a similar decrease in blood pressure, the combination of receptor antagonists with angiotensin II with moxonidine allows a greater reduction in LVH compared with the free combination of a thiazide diuretic and a " slow "calcium channels (15% vs. 11%, p <0.05).

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

Pharmacokinetics:

Suction

After oral administration moxonidine quickly and almost completely absorbed in the upper parts of the gastrointestinal tract. Absolute bioavailability is approximately 88%, indicating that there is no significant "primary" effect. The time to reach the maximum concentration is about 1 hour. Eating does not affect the pharmacokinetics of the drug.

Distribution

The connection with plasma proteins is 7.2%.

Metabolism

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

Excretion

Half-life (T_1/2) 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% in unchanged form and 13% in the form of dehydrimeroxycinidine, while 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

In comparison with healthy volunteers, patients with hypertension do not have any changes in the pharmacokinetics of moxonidine.

Pharmacokinetics in old age

Clinically insignificant changes in 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 younger than 18 years of age, and therefore no pharmacokinetic studies have been performed in this group.

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), equilibrium concentrations in the blood plasma and the final T_1/2 approximately 2 and 1.5 times higher than in individuals with normal renal function (CC greater than 90 mL / min).

In patients with severe renal failure (CC less than 30 ml / min), equilibrium concentrations in the blood plasma and the final T_1/2 3 times higher than in patients with normal renal function.

The administration of multiple doses of moxonidine leads to predictable cumulation in patients with moderate and severe renal insufficiency.

In patients with terminal renal failure (CC less than 10 ml / min) on hemodialysis, the equilibrium plasma concentrations and the final T_1/2 respectively, 6 and 4 times higher 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 selected individually. Moxonidine is slightly excreted during hemodialysis.

Indications:Arterial hypertension.

Contraindications:

hypersensitivity to the active substance and other components of the drug;

syndrome of weakness of the sinus node;

pronounced bradycardia (heart rate (resting heart rate) less than 50 bpm);

atrioventricular block of the 2nd or 3rd degree;

acute and chronic heart failure;

lactation period;

hereditary intolerance to galactose, lactase deficiency or malabsorption of glucose-galactose;

age under 18 years (due to lack of safety data and effectiveness).

Carefully:

Special care must be taken with moxonidine in patients with stage I atrioventricular block (risk of developing bradycardia); severe coronary artery disease and unstable angina (experience with use is inadequate); renal insufficiency.

Moxonidine is contraindicated in patients with atrioventricular blockades of II and III degree (see section "Contraindications").

Pregnancy and lactation:

Pregnancy

Clinical data on the use of the drug Physiotense ® in pregnant women are absent.

In the course of animal studies, the embryotoxic effect of the drug was established.

Physiotens® should be given to pregnant women only after a thorough assessment of the risk-benefit relationship, when the benefit to the mother exceeds the potential risk to the fetus.

Lactation period

Moxonidine penetrates breast milk and should therefore not be given during breastfeeding.

If you need to use the drug Physiotense® during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, regardless of food intake. In most cases, the initial dose of Physiotense® is 0.2 mg per day. The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 divided doses, is 0.6 mg. Individual correction of the daily dose is necessary depending on the patient's tolerability of the therapy.

Dose adjustment for patients with hepatic insufficiency is not required.

The initial dose for patients on hemodialysis is 0.2 mg per day. If necessary and with good tolerability, the daily dose can be increased to 0.4 mg per day.

Patients with renal failure are advised to carefully select the dose, especially at the beginning of treatment. The initial dose should be 0.2 mg per day. If necessary and with good tolerability, the daily dose of the drug may be increased to a maximum of 0.4 mg for patients with moderate renal insufficiency (QC greater than 30 mL / min but less than 60 mL / min) and 0.3 mg for patients with severe renal disease insufficiency (CC less than 30 ml / min).

Side effects:

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

Patients who participated in placebo-controlled clinical trials of the Physiotense® drug had the following side effects.

The frequency of side effects, given below, was determined according to the following: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); including individual messages.

From the central nervous system:

Often: headache *, dizziness (vertigo), drowsiness.

Infrequently: fainting *.

From the cardiovascular system:

Infrequent: marked decrease in blood pressure, orthostatic hypotension *, bradycardia.

From the side gastrointestinal tract:

Very often: dry mouth.

Often: diarrhea, nausea, vomiting, indigestion.

From the skin and subcutaneous tissues:

Often: skin rash, itching.

Infrequently: angioedema.

Disorders of the psyche:

Often: insomnia.

Infrequently: nervousness.

From the side of the hearing organ and labyrinthine disorders:

Infrequent: ringing in the ears.

From the musculoskeletal and connective tissue:

Often: back pain.

Infrequent: pain in the neck.

General disorders and disorders at the site of administration:

Often: asthenia.

Infrequent: peripheral edema.

(* - frequency comparable to placebo).

Overdose:

There are reports of several cases of overdose without a lethal outcome, when doses up to 19.6 mg were applied at the same time.

Symptoms: headache, sedation, drowsiness, marked decrease in blood pressure, dizziness, asthenia, bradycardia, dry mouth, vomiting, fatigue, pain in the epigastric region, respiratory depression and impaired consciousness.

In addition, short-term increases in blood pressure, tachycardia and hyperglycemia are also possible, as shown in several studies on the study of high doses in animals.

Treatment

There is no specific antidote.

In the case of a marked decrease in blood pressure, it may be necessary to restore the volume of circulating blood by introducing fluid and dopamine (injection). Bradycardia can be stopped with atropine (injection injection). In severe cases of overdose, it is recommended to carefully monitor impairment of consciousness and not to allow respiratory depression.

Alpha-adrenoreceptor antagonists can reduce or eliminate paradoxical hypertensive effects in overdose with moxonidine.

Interaction:

The combined use of moxonidine with other antihypertensive agents leads to an additive effect. Tricyclic antidepressants can reduce the effectiveness of antihypertensive agents of central action, and therefore it is not recommended that they be taken together with moxonidine.

Moxonidine may enhance the sedative effect of tricyclic antidepressants (joint use should be avoided), tranquilizers, ethanol, sedatives and hypnotics. Moxonidine moderately improve impaired cognitive function in patients receiving lorazepam. Moxonidine can enhance the sedative effect of benzodiazepine derivatives when administered concomitantly.

Moxonidine is excreted by tubular secretion. Therefore, its interaction with other drugs released by tubular secretion is not excluded.

Special instructions:

In post-marketing surveillance, cases of atrioventricular blockage of varying severity in patients taking moxonidine. The relationship between taking the Physiotense® drug and slowing the atrioventricular conduction can not be completely ruled out. Thus, in the treatment of patients with a likely predisposition to the development of atrioventricular blockade, caution is recommended.

If it is necessary to cancel simultaneously taken beta-blockers and the Physiotense® drug, beta-blockers are first abolished and only after a few days of Physiotense®.

At present, there is no evidence that stopping the use of the Physiotense® drug leads to an increase in blood pressure.However, it is not recommended to stop taking the Physiotense® drug abruptly, instead you should gradually reduce the dose of the drug within two weeks.

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

Studies of the effect of the drug on the ability to drive and other mechanisms have not been carried out.

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; 0.3; 0.4 mg.

Packaging:

Tablets, film-coated, 0.2; 0.3; 0.4 mg: 14 tablets in PVC / PVDC / Al blister; 1, 2 or 7 blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C (for a dosage of 0.2 mg).

At a temperature of no higher than 30 ° C (for dosage of 0.3 mg, 0.4 mg).

Keep out of the reach of children!

Shelf life:

2 years (for a dosage of 0.2 mg).

3 years (for dosage of 0.3 mg, 0.4 mg).

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

Terms of leave from pharmacies:On prescription

Registration number:P N 015691/01

Date of registration:16.01.2009

The owner of the registration certificate:Abbott Laboratories, GmbHAbbott Laboratories, GmbH Germany

Manufacturer: & nbsp

Rottendorf Pharma, GmbH Germany

Representation: & nbspABBOTT LABORATORIES LLC ABBOTT LABORATORIES LLC Russia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Physiotens® (Physiotens®)