Fiziotenz

General characteristics. Structure:

Active ingredient: моксонидин 0,2 mg;
excipients: lactoses monohydrate — 95,7 mg; povidone — 0,7 mg; кросповидон — 3 mg; magnesium stearate — 0,3 mg; a gipromelloza — 1,3 mg; ethyl cellulose — 4 mg; macrogoal of 6000 — 0,25 mg; talc — 0,975 mg; ferrous oxide red (E172) — 0,025 mg; titanium dioxide (E171) — 1,25 mg;

Active ingredient: моксонидин 0,3 mg;
excipients: lactoses monohydrate — 95,7 mg; povidone — 0,7 mg; кросповидон — 3 mg; magnesium stearate — 0,3 mg; a gipromelloza — 1,3 mg; ethyl cellulose — 4 mg; macrogoal of 6000 — 0,25 mg; talc — 0,975 mg; ferrous oxide red (E172) — 0,025 mg; titanium dioxide (E171) — 1,25 mg;

Active ingredient: моксонидин 0,4 mg;
excipients: lactoses monohydrate — 95,6 mg; povidone — 0,7 mg; кросповидон — 3 mg; magnesium stearate — 0,3 mg; a gipromelloza — 1,3 mg; ethyl cellulose — 4 mg; macrogoal of 6000 — 0,25 mg; talc — 0,875 mg; ferrous oxide red (E172) — 0,125 mg; titanium dioxide (E171) — 1,25 mg;

Description of a dosage form:

Round, biconvex, coated tablets:
 
with a dosage of 0,2 mg — light pink color, with marking "0,2" on the one hand;
 
with a dosage of 0,3 mg — pale red color, with marking "0,3" on the one hand;
 
with a dosage of 0,4 mg — opaque red color, with marking "0,4" on the one hand.
 
On cross section two layers are visible.

Pharmacological properties:

Pharmacodynamics. Selectively interacting with imidazolinovy I1 receptors, located in a brainstem, reduces sympathetic activity.
Moksonidin has high affinity to imidazolinovy I1 receptors and only slightly contacts the central alfa2-adrenoceptors due to interaction with which dryness in a mouth and sedation speaks.
Reduces resistance of fabrics to insulin.
Influence on a hemodynamics: decrease in the systolic and diastolic ABP at single and long dose of a moksonidin is connected with reduction of pressor action of sympathetic system by peripheral vessels, decrease in peripheric vascular resistance while cordial emission and heart rate significantly do not change.

Pharmacokinetics. Absorption.
Absorption — 90%. Cmax in a blood plasma (after reception of a tablet with the maintenance of 0,2 mg of a moksonidin) makes 1,4–3 ng/ml and is reached in 60 min. Bioavailability — 88% (meal does not exert impact on pharmacokinetics).

Distribution. Distribution volume — 1,4–3 l/kg. Gets through GEB. Linkng with proteins of plasma — 7,2%.

Metabolism. Main metabolites: 4,5-digidromoksonidin and guanidine derivatives.

Removal. T1/2 of a moksonidin and metabolites makes 2,5 and 5 h respectively. During 24 h more than 90% of a moksonidin are removed by kidneys, about 78% in not changed look and 13% in the form of degidrogenizirovanny derivative. Less than 1% are removed with a stake. Does not kumulirut at prolonged use.

Pharmacokinetics at advanced age. The age changes of pharmacokinetics connected probably with a little higher bioavailability and/or reduced metabolic activity are observed. However these changes are not clinically significant.

Pharmacokinetics at a renal failure. Removal of a moksonidin substantially correlates with clearance of creatinine. At patients with a moderate renal failure (creatinine Cl 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 patients with arterial hypertension with normal function of kidneys (creatinine Cl> of 90 ml/min.). At patients with a heavy renal failure (creatinine Cl <30 ml/min.) equilibrium concentration in a blood plasma and final T1/2 is 3 times higher, than at persons with normal function of kidneys. Purpose of repeated doses of drug does not lead to cumulation in an organism of patients with a moderate renal failure. At late stages at patients with extremely heavy renal failure (equilibrium concentration in a blood plasma and final T1/2 respectively in 6 and 4 times is higher than the creatinine Cl <10 ml/min.) which are on a hemodialysis, than at patients with normal function of kidneys. 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, an initial dose (in most cases) — 0,2 mg a day; the maximum daily dose — 0,6 mg (to divide into 2 receptions); the maximum single dose — 0,4 mg;

at a renal failure (Cl of creatinine of 30-60 ml/min.) and at the patients who are on a hemodialysis, a single dose — 0,2 mg, maximum daily — 0,4 mg.

Features of use:

In need of cancellation of at the same time accepted beta adrenoblockers and Fiziotenz at first cancel beta adrenoblockers and only in several days — Fiziotenz®. During treatment regular control of the ABP, ChSS, ECG is necessary. It is necessary to stop Fiziotenz's reception gradually. Patients with rare hereditary pathology of intolerance of a galactose, deficit of lactase or malabsorption of glucose galactose should not accept this drug.

Data on adverse influence of a moksonidin on ability to driving of the car and to control of cars and mechanisms are absent. There are messages on drowsiness and dizziness during treatment moksonidiny. It should be considered when performing the above-stated actions.

Side effects:

From TsNS: dizziness, headache, drowsiness, sleep disorder.
From cardiovascular system: excessive decrease in the ABP, orthostatic hypotension.
From a GIT: dryness in a mouth, nausea.
From skin and hypodermic fatty tissue: skin rash, itch, Quincke's disease.
The general: adynamy.

These symptoms usually gradually decrease within the first weeks of treatment.

Interaction with other medicines:

Perhaps combined use with thiazide diuretics, APF inhibitors and blockers of slow calcium channels. There is mutual strengthening of action at combined use to these and other antihypertensives.

There is no pharmacokinetic interaction with a hydrochlorothiazide (perhaps combined use), Glibenclamidum (Glyburidum), digoxin. Tricyclic antidepressants can reduce efficiency of anti-hypertensive central acting agents (joint appointment is not recommended). Moderately increases reduced cognitive ability at the patients accepting lorazepam. Strengthens sedation of benzodiazepines. There is no pharmakodinamichesky interaction at joint appointment with moklobemidy.

Contraindications:

- hypersensitivity to drug components;
- a syndrome of weakness of a sinus node, the expressed bradycardia;
- age up to 18 years (efficiency and safety are not established).

With care:
- a heavy chronic renal failure and the expressed liver failure (because of a lack of experience of use);
- hemodialysis.

Use at pregnancy and feeding by a breast
There are no clinical data on a negative impact on the course of pregnancy. However it is necessary to be careful, appointing Fiziotenz® to pregnant women. During treatment it is recommended to stop breastfeeding since моксонидин gets into breast milk.

Overdose:

Symptoms: a headache, sedation, drowsiness, excessive decrease in the ABP, dizziness, the general weakness, bradycardia, dryness in a mouth, vomiting, fatigue and a stomach ache. Short-term increase in the ABP, tachycardia, a hyperglycemia are potentially possible.

Treatment: antagonists of alpha adrenoceptors can reduce or eliminate paradoxical arterial hypertension. In case of hypotension recovery of OTsK due to administration of liquid and introduction of a dopamine is recommended. Bradycardia can be stopped by atropine. The specific antidote does not exist.

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

In the blister of 14 pieces; in a box of 1, 2 or 7 blisters.