Цинт

General characteristics. Structure:

Active agent: моксонидин 0,2 mg

Excipients: lactoses monohydrate — 95,8 mg; povidone — 0,7 mg; кросповидон — 3 mg; magnesium stearate — 0,3 mg  

Covering: a gipromelloza — 1,3 mg; ethyl cellulose — 1,2 mg; a macrogoal — 0,25 mg; talc — 0,9975 mg; dyes: ferrous oxide red (E172) — 0,0025 mg; titanium dioxide (E171) — 1,25 mg.

Active agent: моксонидин 0,3 mg

Excipients: lactoses monohydrate — 95,7 mg; povidone — 0,7 mg; кросповидон — 3 mg; magnesium stearate — 0,3 mg  

Covering: a gipromelloza — 1,3 mg; ethyl cellulose — 1,2 mg; a macrogoal — 0,25 mg; talc — 0,975 mg; dyes: ferrous oxide red (E172) — 0,025 mg; titanium dioxide (E171) — 1,25 mg

Active agent: моксонидин 0,4 mg

Excipients: lactoses monohydrate — 95,6 mg; povidone — 0,7 mg; кросповидон — 3 mg; magnesium stearate — 0,3 mg
 
Covering: a gipromelloza — 1,3 mg; ethyl cellulose — 1,2 mg; a macrogoal — 0,25 mg; talc — 0,875 mg; dyes: ferrous oxide red (E172) — 0,125 mg; titanium dioxide (E171) — 1,25 mg.

Pharmacological properties:

Pharmacodynamics. Moksonidin selectively interacts with imidazolinovy I1 receptors, located in a brainstem that leads to decrease in sympathetic activity.
Moksonidin has high affinity to imidazolinovy I1 receptors and only slightly communicates with central α2-адренорецепторами due to interaction with which are mediated dryness in a mouth and sedation.
Reduces resistance of fabrics to insulin.
Influence on a hemodynamics: decrease the GARDEN and DAD 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 ChSS significantly do not change.
The maximum of hypotensive effect is reached approximately in 2,5–7 h after intake.

Pharmacokinetics. Absorption — 90%. Cmax in a blood plasma (after reception of the tab. of 0,2 mg) — 1,4–3 ng/ml is also reached in 30–180 min. Bioavailability — 88%. Meal does not exert impact on drug pharmacokinetics.
Distribution volume — 1,4–3 l/kg. Gets through GEB. Linkng with proteins of a blood plasma — 7,2%.
Main metabolites: 4,5 дегидромоксонидин and guanidine derivatives.
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 a degidrogenizirovanny moksonidin. Less than 1% of a dose are removed with a stake. Moksonidin does not kumulirut at prolonged use.

Pharmacokinetics at advanced age. Age changes of pharmacokinetics which are probably caused by reduced metabolic activity and/or a little higher bioavailability of a moksonidin at elderly patients are observed. However these pharmacokinetic distinctions are not clinically significant.

Pharmacokinetics at a renal failure. Removal of a moksonidin substantially correlates with creatinine Cl. At patients with a heavy renal failure (creatinine Cl <30 ml/min.) equilibrium concentration in a blood plasma and final T1/2 is about 3 times higher, than at persons with normal function of kidneys (creatinine Cl> of 90 ml/min.). At patients with a renal failure of moderate severity (creatinine Cl> of 30-60 ml/min.) equilibrium concentration in a blood plasma and the final elimination half-life is higher, than at patients with normal function of kidneys approximately for 80 and 35% respectively. In both groups the maximum concentration of a moksonidin in a blood plasma are only 50% higher. Purpose of repeated doses of a moksonidin does not lead to cumulation of connection in an organism of patients with a moderate renal failure.

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 an initial dose of Tsinta® — 0,2 mg of 1 times a day; the maximum daily dose — 0,6 mg, divided into 2 receptions.
The maximum single dose — 0,4 mg.

Initial daily dose for patients with a renal failure (creatinine Cl — 30–60 ml/min.) and the patients who are on a hemodialysis — 0,2 mg. The maximum daily dose — 0,4 mg.

Features of use:

The company has no data that Tsint® cannot be used at a chronic renal failure (creatinine Cl <30 ml/min., creatinine> 160 µmol/l).

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

It is not recommended to appoint tricyclic antidepressants along with moksonidiny.

During treatment regular control of the ABP, ChSS and ECG is necessary.

Цинт® it can be appointed with thiazide diuretics, APF inhibitors and blockers of slow calcium channels.

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: seldom — dizziness, a headache, a sleep disorder, increased fatigue; often — an adynamy, drowsiness.
From cardiovascular system: excessive decrease in the ABP, orthostatic hypotension.
From a GIT: dryness in a mouth.
Allergic reactions: peripheral hypostases.

Interaction with other medicines:

There is mutual strengthening of action of a moksonidin at combined use to other antihypertensives.

At purpose of a moksonidin with a hydrochlorothiazide, glibenclamide or digoxin pharmacokinetic interaction is absent.

Tricyclic antidepressants can reduce efficiency of anti-hypertensive central acting agents.

Moksonidin moderately increases reduced cognitive ability at the patients accepting lorazepam.

Purpose of a moksonidin together with benzodiazepines can be followed by strengthening of sedation of the last.

At purpose of a moksonidin together with a moklobemidy pharmakodinamichesko interaction is absent.

Contraindications:

- hypersensitivity to drug components;
- a syndrome of weakness of a sinus node, the expressed bradycardia, sinuatrial and AV blockade;
- heavy chronic heart failure (III–IV stage), unstable stenocardia;
- the expressed liver failure;
- age up to 18 years (efficiency and safety are not established).

With care:
- parkinsonism, epilepsy, depression;
- glaucoma;
- the alternating lameness, a Raynaud's disease (due to the 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. Researches on animals did not reveal direct or indirect harmful effects on pregnancy, embryonic development, childbirth and post-natal development. However it is necessary to be careful, appointing Tsint® to pregnant women. Moksonidin gets into breast milk, women during treatment are recommended to stop breastfeeding or to cancel drug.

Overdose:

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

Treatment: specific antidotes do not exist.
In case of hypotension recovery of OTsK due to administration of liquid and a dopamine is recommended.
Bradycardia can be stopped by atropine.
Antagonists of alpha adrenoceptors can reduce or eliminate paradoxical arterial hypertension at overdose of a moksonidin.

Storage conditions:

At a temperature not above 30 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

In piece blister 10 or 14; in a box 1, 2, 3 or 4 blisters.