Moksonidin

General characteristics. Structure:

Active agent: моксонидин 0,2 mg,

Excipients: cellulose microcrystallic, A-380 aerosil, polyvinylpirrolidone, magnesium stearate, hydroxypropyl cellulose (klutset), castor oil, the twin-80.

Pharmacological properties:

Pharmacodynamics. The selection agonist of the imidazolinovy receptors which are responsible for tonic and reflex control over a sympathetic nervous system (are localized in ventero-lateral department of a myelencephalon). Reduces the arterial pressure (AP). Slightly contacts the central alfa2-adrenoceptors with which due to interaction are mediated dryness in a mouth and sedation.
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 the heart rate (HR) significantly do not change.

Pharmacokinetics. Absorption after intake – 90%. Meal does not influence the size of absorption. Bioavailability – 88%. Communication with proteins of a blood plasma – 7%. Cmax in plasma is defined in 30 – 180 min. after oral administration and makes 1 – 3 ng/ml. Distribution volume –
1,4 – 3 l/kg. Passes through a blood-brain barrier. It does not kumulirutsya at prolonged use. An elimination half-life – 2 – 3 h. By kidneys it is brought to 90% (70% – in not changed look, 20% – in the form of metabolites). Reliable distinctions in pharmacokinetics at young and elderly patients are not revealed.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Inside, irrespective of meal, washing down with enough liquid.
In most cases the initial dose of a moksonidin makes 0,2 mg a day, in one step, more preferably in the morning. At insufficiency of therapeutic effect the dose can be increased after 3 weeks of therapy to 0,4 mg a day for 2 receptions or once. The maximum daily dose which should be divided into 2 receptions (in the morning and in the evening) makes 0,6 mg. The maximum single dose makes 0,4 mg.

Elderly patients with normal function of kidneys have recommendations about a dosage same, as well as for adult patients.
At patients with a renal failure (clearance of creatinine of 30 - 60 ml/min.) and the patients who are on a hemodialysis, the single dose should not exceed 0,2 mg, the maximum daily dose of 0,4 mg.

Features of use:

In need of cancellation of at the same time accepted beta adrenoblockers and a moksonidin, at first cancel beta adrenoblockers and, only in several days, моксонидин.
It is not recommended to appoint tricyclic antidepressants along with moksonidiny. During treatment alcohol intake is excluded.
During treatment regular control of the ABP, ChSS and ECG is necessary.
Moksonidin can be appointed with thiazide diuretics, APF inhibitors and blockers of "slow" calcium channels.

It is necessary to stop reception of a moksonidin gradually.

Influence on ability to driving of the car and to control of cars and mechanisms
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 (especially in an initiation of treatment).

Side effects:

Especially at the beginning of therapy the most frequent side reactions were: dryness in a mouth, a headache, dizziness, an adynamy, peripheral hypostases, allergic reactions, nausea, a lock, drowsiness. Intensity of their manifestation and frequency decrease at repeated reception. It was reported about cases of anorexia, pain in the field of parotid glands, a delay or an incontience of urine, dryness of an eye, orthostatic hypotension, Reynaud's syndrome, endocrine disturbances, a zhelchekamenny disease.

Interaction with other medicines:

Moksonidin can be appointed with thiazide diuretics and blockers of "slow" calcium channels. At combined use of a moksonidin to these and other antihypertensives there is mutual strengthening of action of a moksonidin.
At purpose of a moksonidin with a hydrochlorothiazide, Glibenclamidum (Glyburidum) or digoxin pharmacokinetic interaction is absent.
Tricyclic antidepressants can reduce efficiency of anti-hypertensive central acting agents.
Beta adrenoblockers strengthen bradycardia, expressiveness of negative other and dromotropic effect of a moksonidin.
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 sick sinus syndrome, a sinuatrial and atrioventricular block of II and III degrees, the expressed bradycardia (heart rate less than 50 уд. / min.), chronic heart failure III and IV classes (on NYHA classification), a Quincke's disease in the anamnesis, unstable stenocardia, a heavy liver failure, a chronic renal failure (clearance of creatinine less than 30 ml/min., creatinine more than 160 µmol/l), age up to 18 years (efficiency and safety are not established), pregnancy and the period of a lactation, a concomitant use with tricyclic antidepressants.

With care: Parkinson's disease (severe form), epilepsy, glaucoma, a depression, the "alternating" lameness, a Raynaud's disease, an atrioventricular block of the I degree, a chronic renal failure (clearance of creatinine more than 30, but less than 60 ml/min.), cerebrovascular diseases, after the postponed myocardial infarction, chronic heart failure of I and II classes, the expressed liver failure – because of a lack of experience of use, a hemodialysis.

Overdose:

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

Treatment: symptomatic. A gastric lavage (right after reception), administration of absorbent carbon and purgatives, symptomatic therapy.
In case of decrease in the ABP recovery of volume of the circulating blood due to administration of liquid is recommended. Bradycardia can be stopped by atropine.
Antagonists of alpha adrenoceptors can reduce or eliminate passing arterial hypertension at overdose moksonidiny. As a specific antidote enter идазоксан (the antagonist of imidazolines).

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C.
To store in the places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 0,2 mg.
On 10 or 14 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.
1, 2, 3 or 4 blister strip packagings on 10 tablets or 1, 2, 3, 4, 5 or 7 blister strip packagings on 14 tablets together with the application instruction in a pack from a cardboard.