Физиотенз®

General characteristics. Structure:

Active agent: моксонидин 0,2 mg.

Excipients: lactoses monohydrate — 95,80 mg, povidone — 0,70 mg, кросповидон — 3,00 mg, magnesium stearate — 0,30 mg.

Cover: a gipromelloza — 1,30 mg, ethyl cellulose — 1,20 mg, a macrogoal — 0,25 mg, talc - 0,9975 mg, dye ferrous oxide red (Е 172) — 0,0025 mg, titanium dioxide (Е 171) - 1,25 mg.

1 tablet film coated with a dosage of 0,3 mg contains:

Active agent: моксонидин 0,3 mg.

Excipients: lactoses monohydrate — 95,70 mg, povidone — 0,70 mg, кросповидон — 3,00 mg, magnesium stearate — 0,30 mg.

Cover: a gipromelloza — 1,30 mg, ethyl cellulose — 1,20 mg, a macrogoal — 0,25 mg, talc - 0,975 mg, dye ferrous oxide red (Е 172) — 0,025 mg, titanium dioxide (Е 171) - 1,25 mg.

1 tablet film coated with a dosage of 0,4 mg contains:

Active agent: моксонидин 0,4 mg.

Excipients: lactoses monohydrate — 95,60 mg, povidone — 0,70 mg, кросповидон — 3,00 mg, magnesium stearate — 0,30 mg.

Cover: a gipromelloza — 1,30 mg, ethyl cellulose — 1,20 mg, a macrogoal — 0,25 mg, talc — 0,875 mg, dye ferrous oxide red (Е 172) — 0,125 mg, titanium dioxide (Е 171) 1,25 mg.

Description

Round biconvex tablets, film coated.

Tablets with a dosage of 0,2 mg — light pink color with an engraving "0,2" on the one hand.

Tablets with a dosage of 0,3 mg — pink color with an engraving "0,3" on the one hand.

Tablets with a dosage of 0,4 mg — brownish-pink color with an engraving "0,4" on the one hand.

On a break of a tablet of white color.

Pharmacological properties:

Pharmacodynamics. Moksonidin is an antihypertensive with the central mechanism of action. моксонидин selectively stimulates imidazoline in trunk structures of a brain (a rostral layer of side ventricles) - the sensitive receptors which are taking part in tonic and reflex regulation of a sympathetic nervous system. Stimulation of imidazolinovy receptors reduces peripheral sympathetic activity and the arterial pressure (AP).

Moksonidin differs from other sympatholytic antihypertensives in lower affinity to a2-adrenoceptors that explains smaller probability of development of sedation and dryness in a mouth.

Reception of a moksonidin leads to decrease in system vascular resistance and the ABP. The hypotensive effect of a moksonidin is confirmed in double blind people, placebo - controlled, randomized researches.

Moksonidin improves for 21% a sensitivity index to insulin (in comparison with placebo) at patients with obesity, an insulinrezistentnostnost and moderate degree of arterial hypertension.

Pharmacokinetics. Absorption:

After intake моксонидин quickly and almost it is completely absorbed in upper parts of digestive tract. Absolute bioavailability makes about 88%. Time of achievement of the maximum concentration - about 1 hour. Meal does not exert impact on drug pharmacokinetics.

Distribution

Communication with proteins of a blood plasma makes 7,2%.

Metabolism

The main metabolite — dehydrogenated моксонидин.

Pharmakodinamichesky activity of the dehydrogenated moksonidin — about 10% in comparison with moksonidiny.

Removal

The elimination half-life (T1/2) of a moksonidin and metabolite makes 2,5 and 5 hours respectively. Within 24 hours over 90% of a moksonidin are removed by kidneys (about 78% in not changed look and 13% in the form of a degidriromoksonidin, other metabolites in urine do not exceed 8% of the accepted dose). Less than 1% of a dose are removed through intestines.

Pharmacokinetics at patients with arterial hypertension:

In comparison with healthy volunteers at patients with arterial hypertension changes of pharmacokinetics of a moksonidin are not noted.

Pharmacokinetics at advanced age

Clinically insignificant changes of pharmacokinetic indicators of a moksonidin at elderly patients which are possibly caused by decrease in intensity of his metabolism and/or a little higher bioavailability are noted.

Pharmacokinetics at children

Moksonidin is not recommended for use at persons under 18 in this connection in this group pharmacokinetic researches were not conducted.

Pharmacokinetics at a renal failure

Removal of a moksonidin substantially correlates with the clearance of creatinine (CC). At patients with a moderate renal failure (KK in the range of 30-60 ml/min.) equilibrium concentration in a blood plasma and final T1/2 approximately in 2 and 1,5 times is higher, than at persons with normal function of kidneys (KK more than 90 ml/min.).

At patients with a heavy renal failure (KK less than 30 ml/min.), equilibrium concentration in a blood plasma and final T1/2 is 3 times higher, than at patients with normal function of kidneys. Purpose of repeated doses of a moksonidin leads to predictable cumulation in an organism of patients with a moderate and heavy renal failure. At the patients with a terminal renal failure (KK less than 10 ml/min.) who are on a hemodialysis, equilibrium concentration in a blood plasma and final T1/2 respectively in 6 and 4 times is higher, than at patients with normal function of kidneys. In all groups the maximum concentration of a moksonidin in a blood plasma is 1,5 — 2 times higher. At patients with renal failures the dosage has to be selected individually. Moksonidin in insignificant degree is brought when carrying out a hemodialysis.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Inside, irrespective of meal.

In most cases the initial dose of the drug Fiziotenz® makes 0,2 mg a day. The maximum single dose makes 0,4 mg. The maximum daily dose which should be divided into 2 receptions makes 0,6 mg.

Individual correction of a daily dose depending on portability by the patient of the carried-out therapy is necessary.

Dose adjustment for patients with a liver failure is not required.

Initial dose for the patients with a moderate or heavy renal failure and also who are on a hemodialysis — 0,2 mg a day. In case of need and at good tolerance the daily dose can be increased to the maximum 0,4 mg.

Side effects:

The most frequent side effects at the patients accepting моксонидин: dryness in a mouth, dizziness, an adynamy and drowsiness. These symptoms often decrease after the first weeks of therapy.

At the patients who were taking part in placebo - controlled clinical trials of the drug Fiziotenz®, the following side effects are noted

Frequency of the side effects given below was defined according to the following: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100);

including separate messages.

From the central nervous system:

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

Infrequently: обморок*.

From cardiovascular system:

Infrequently: the expressed decrease in the ABP, orthostatic hypotension *, bradycardia.

From digestive tract:

Very often: dryness in a mouth.

Often: diarrhea, nausea, vomiting, dyspepsia.

From skin and hypodermic fabrics:

Often: skin rash, itch.

Infrequently: Quincke's disease.

Disturbances of mentality:

Often: sleeplessness.

Infrequently: nervousness.

From an acoustic organ and labyrinth disturbances:

Infrequently: a ring in ears.

From skeletal and muscular and connecting fabric:

Often: dorsodynia.

Infrequently: pain in a neck.

The general frustration and disturbances in an injection site:

Often: adynamy.

Infrequently: peripheral hypostases.

(* - frequency is comparable to placebo).

Interaction with other medicines:

Combined use of a moksonidin with other antihypertensives results in the additive effect.

Tricyclic antidepressants can reduce efficiency of antihypertensives of the central action in this connection their reception together with moksonidiny is not recommended.

Moksonidin can strengthen effect of tricyclic antidepressants, tranquilizers, ethanol, sedative and hypnagogues.

Moksonidin is capable to improve moderately weakened cognitive functions at the patients receiving lorazepam. Moksonidin can strengthen sedation of derivatives of benzodiazepine at their co-administration.

Moksonidin is allocated by canalicular secretion. Therefore its interaction with other drugs which are emitted by canalicular secretion is not excluded.

Influence on ability to driving of the car and to control of cars and mechanisms

Researches of influence of drug on ability to drive the car and other mechanisms were not conducted.

There are messages on drowsiness and dizziness during treatment moksonidiny. It should be considered when performing the above-stated actions.

Contraindications:

— hypersensitivity to active agent and other components of drug;

— sick sinus syndrome;

— the expressed bradycardia (the heart rate (HR) of rest less than 50 уд. / mines);

— atrioventricular block of the 2nd or 3rd degree;

— acute and chronic heart failure;

— lactation period;

— hereditary intolerance of a galactose, deficit of lactase or malabsorption of glucose galactose;

— age up to 18 years (due to the lack of data on safety and efficiency).

Precautionary measures at use

It is necessary to observe extra care at use of a moksonidin for patients with an atrioventricular block of the 1st degree (risk of development of bradycardia); a serious illness of coronary vessels and unstable stenocardia (experience of use is insufficient); renal failure.

In need of cancellation of at the same time accepted beta adrenoblockers and the drug Fiziotenz®, at first cancel beta adrenoblockers and only in several days of Fiziotenz®.

There are no confirmations that the termination of administration of drug of Fiziotenz® leads to increase in the ABP now.

However it is not recommended to stop administration of drug of Fiziotenz® sharply, instead it is necessary to reduce gradually a drug dose within two weeks.

Pregnancy and period of a lactation

Pregnancy

Clinical data on use of Fiziotenza® for pregnant women are absent.

During the researches on animals embriotoksichesky effect of drug was established.

Физиотенз® it is necessary to appoint pregnant, only after careful assessment of a ratio of risk and advantage when the advantage for mother exceeds potential risk for a fruit.

Lactation period

Moksonidin gets into breast milk and therefore it should not be appointed during feeding a breast.

In need of use of Fiziotenza® in the period of a lactation, breastfeeding needs to be stopped.

Overdose:

There are messages on several cases of overdose without a lethal outcome when doses to 19,6 mg were in one step applied.

Symptoms: a headache, sedation, drowsiness, the expressed decrease in the ABP, dizziness, an adynamy, bradycardia, dryness in a mouth, vomiting, fatigue, pain in epigastric area, respiratory depression and disturbance of consciousness.

Besides, also short-term increase in the ABP, tachycardia and a hyperglycemia as it was shown in several researches on studying of high doses on animals are possible.

Treatment

The specific antidote does not exist. In case of the expressed decrease in the ABP recovery of volume of the circulating blood due to administration of liquid and a dopamine can be required (injektsionno).

Bradycardia can be stopped by atropine (injection introduction).

In hard cases of overdose it is recommended to control carefully disturbances of consciousness and not to allow respiratory depression.

Antagonists of alpha adrenoceptors can reduce or eliminate paradoxical hypertensive effects at overdose moksonidiny.

Storage conditions:

At a temperature not above 25 °C (for a dosage of 0,2 mg).

At a temperature not above 30 °C (for a dosage of 0,3 mg; 0,4 mg).

To store in the place, unavailable to children!

Period of validity

2 years (for a dosage of 0,2 mg).

3 years (for a dosage of 0,3 mg; 0,4 mg).

Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets film coated 0,2; 0,3; 0,4 mg: on 14 tablets in PVC/PVDH / the blister Is scarlet; on 1, 2 or 7 blisters together with the application instruction place in a cardboard pack.