Moksonidin-LF

General characteristics. Structure:

Active ingredient: 200 mkg, 300 mkg or 400 mkg of a moksonidin.

Excipients: кросповидон, magnesium stearate, lactoses monohydrate.

Structure of a cover: опадрай the II pink (polyvinyl alcohol, titanium dioxide (E171), polyethyleneglycol, talc, ferrous oxide red (E172), ferrous oxide yellow (E172)).

Pharmacological properties:

Pharmacodynamics. Anti-hypertensive means. The mechanism of action of a moksonidin is connected mainly with its influence on the central links of regulation of the ABP. Moksonidin is an agonist of preferential imidazolinovy receptors.

Exciting the specified receptors of neurons of a solitary path, моксонидин through system of brake interneyron promotes oppression of activity of a vasomotor center and thus – to reduction of the descending sympathetic influences on cardiovascular system. The ABP (systolic and diastolic) decreases gradually. Moksonidin differs from other sympatholytic antihypertensives in lower affinity to α2-адренорецепторам that explains smaller probability of development of sedation and dryness in a mouth.

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

Pharmacokinetics. After intake моксонидин quickly and almost it is completely absorbed in upper parts of a GIT. Absolute bioavailability makes about 88%. Time of achievement of Cmax - about 1 h. Meal does not exert impact on pharmacokinetics of a moksonidin. Linkng with proteins of a blood plasma makes 7.2%.

The main metabolite of a moksonidin - dehydrogenated моксонидин and guanidine derivatives.

Pharmakodinamichesky activity of the dehydrogenated moksonidin - about 10% in comparison with moksonidiny. T1/2 of a moksonidin and a metabolite 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 degidriromoksonidin, other metabolites in urine do not exceed 8% of the accepted dose). Less than 1% of a dose are removed through intestines.

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

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

Removal of a moksonidin substantially correlates with KK. At patients with a renal failure of average degree (KK of 30-60 ml/min.) of Css 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 renal failure of heavy degree (KK less than 30 ml/min.), and final T1/2 is 3 times higher than Css in a blood plasma, than at patients with normal function of kidneys. Use of a moksonidin in repeated doses leads to predictable cumulation in an organism at patients with a renal failure of average and heavy degree. At the patients with a terminal renal failure (KK less than 10 ml/min.) who are on a hemodialysis, and final T1/2 respectively in 6 and 4 times is higher than Css in a blood plasma, than at patients with normal function of kidneys.

In all Cmax groups of a moksonidin in a blood plasma is 1.5-2 times higher. At patients with renal failures a dose it is necessary 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:

Accept inside. The initial dose averages 200 mkg in 1 times / the Maximum single dose – 400 mkg. Individual correction of a daily dose depending on portability of therapy is necessary. The maximum daily dose – 600 mkg in 2 receptions.

For the patients with a renal failure of average and heavy degree and also who are on a hemodialysis an initial dose – 200 mkg. In case of need and at good tolerance the daily dose can be increased to the maximum 400 mkg.

Features of use:

Adequate and strictly controlled researches of safety of a moksonidin at pregnancy were not conducted therefore it should not be applied at this category of patients.

It is not necessary to apply in the period of a lactation as моксонидин it is allocated with breast milk. In need of use of a moksonidin in the period of a lactation, breastfeeding should be stopped

During pilot studies on animals embriotoksichesky effect of drug was established.

It is contraindicated at heavy disturbances of functions of a liver and kidneys.

 

  

 

Side effects:

Determination of frequency of side reactions: very often (> 1/10), it is frequent (> 1/100-<1/10), infrequently (> 1/1000-<1/100), it is unknown (it is impossible to define on the basis of the available data).

At the beginning of therapy most often - dryness in a mouth, dizziness, a headache, an adynamy and drowsiness. Intensity and frequency of side effects decreases at repeated reception.

From TsNS: often - a headache, dizziness, drowsiness, absent-mindedness, consciousness oppression; infrequently - a syncope.

From cardiovascular system: often - a vazodilatation; infrequently - bradycardia; sometimes - excessive decrease in the ABP, orthostatic hypotension, paresthesias of extremities, disturbances of peripheral circulation, Reynaud's syndrome.

From an acoustic organ and balance: infrequently - a sonitus.

From the alimentary system: very often - dryness in a mouth; often - diarrhea, vomiting, dispepsichesky frustration.

From integuments and a hypodermic fatty tissue: often - skin rash, an itch; infrequently - a Quincke's disease.

From a musculoskeletal system: often - a dorsodynia; infrequently - neck pain.

Mental disturbances: often - sleep disorders, difficulties of concentration of attention; infrequently - irritability.

Vision disorders: sometimes - dryness of an eye, an eye burning sensation.

Endocrine disturbances: sometimes - a gynecomastia, impotence and decrease in a libido.

The general: sometimes - hypostases of various localization, weakness in legs, anorexia, pain in the field of parotid glands.

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 therefore 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.

Contraindications:

— hypersensitivity to drug components;

— SSSU;

— sinuatrial and AV blockade of II and III degrees;

— the expressed bradycardia (ChSS at rest less than 50 уд. / mines);

— chronic heart failure III and IV classes (on NYHA classification);

— a Quincke's disease in the anamnesis;

— heavy liver failure;

— unstable stenocardia;

— chronic renal failure (KK <less than 30 ml/min., serum creatinine more than 160 µmol/l);

— children's and teenage age up to 18 years (efficiency and safety are not established);

— lactation period;

— pregnancy;

— a concomitant use with tricyclic antidepressants;

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

With care: Parkinson's disease (severe form), epilepsy, glaucoma, a depression, the alternating lameness, a Raynaud's disease, AV blockade of the I degree, a chronic renal failure (KK> of 30 ml/min., but less than 60 ml/min.), cerebrovascular diseases, after the postponed myocardial infarction, chronic heart failure I and II classes (on NYHA classification), the patient who is on a hemodialysis; because of a lack of experience of use - a moderate liver failure (more than 9 points on classification of Chayld-Pyyu).

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: the specific antidote does not exist. In case of decrease in the ABP recovery of OTsK due to administration of liquid and introduction of a dopamine is recommended. Bradycardia can be stopped by atropine. Antagonists of α-adrenoceptors can reduce or eliminate paradoxical arterial hypertension at overdose of a moksonidin.

Storage conditions:

Drug should be stored in the place, unavailable to children, in the place protected from moisture and light at a temperature not above 25 °C. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging. On the 3rd blister strip packagings in a cardboard pack.