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Moxonidine-LF

Suction

After oral administration, moxonidine is rapidly and almost completely absorbed from the upper gastrointestinal tract. Absolute bioavailability is approximately 88%, indicating no significant first-pass effect.

The time to reach maximum concentration is about 1 hour. Food intake does not affect the pharmacokinetics of the drug.

Distribution

The binding to plasma proteins is 7.2%.

Metabolism

The main metabolite is dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 10% compared to moxonidine.

Removal

The half-life (T1/2) of moxonidine and metabolite is 2.5 and 5 hours, respectively. Within 24 hours, over 90% of moxonidine is excreted by the kidneys (about 78% unchanged and 13% as dehydriromoxonidine, other metabolites in the urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestines.

Pharmacokinetics in patients with arterial hypertension

Compared with healthy volunteers, patients with arterial hypertension show no changes in the pharmacokinetics of moxonidine.

Pharmacokinetics in old age

Clinically insignificant changes in the pharmacokinetic parameters of moxonidine were noted in elderly patients, probably due to a decrease in the intensity of its metabolism and/or slightly higher bioavailability.

Pharmacokinetics in children

Moxonidine is not recommended for use in persons under 18 years of age, and therefore no pharmacokinetic studies have been conducted in this group.

Pharmacokinetics in renal failure

Moxonidine excretion is significantly correlated with creatinine clearance (CC). In patients with moderate renal failure (creatinine clearance in the range of 30-60 ml/min), steady-state plasma concentrations and final T1/2 are approximately 2 and 1.5 times higher than in individuals with normal renal function (creatinine clearance more than 90 ml/min). min).

In patients with severe renal failure (creatinine clearance less than 30 ml/min), steady-state plasma concentrations and final T1/2 are 3 times higher than in patients with normal renal function.

The administration of multiple doses of moxonidine leads to predictable accumulation in the body of patients with moderate and severe renal failure.

In patients with end-stage renal failure (creatinine clearance less than 10 ml/min) on hemodialysis, steady-state plasma concentrations and final T1/2 are 6 and 4 times higher, respectively, than in patients with normal renal function. In patients with moderate renal failure, the maximum concentration of moxonidine in the blood plasma is 1.5-2 times higher. In patients with renal impairment, the dosage should be adjusted individually. Moxonidine is excreted to a small extent during hemodialysis.

Moxonidine-LF tablets p/o 0.2 mg No. 10x3

Name

Moxonidine-LF tablet coated volume 0.2 mg in container pack No. 10x3

Description

Round, film-coated tablets, light pink in color, biconvex in shape (dosage 0.2 mg).

Main active ingredient

Moxonidine

Release form

Film-coated tablets, 0.2 mg.

Dosage

0.2 mg

special instructions

If it is necessary to cancel concomitantly taken beta-blockers and moxonidine, first cancel the beta-blockers and only after a few days moxonidine. It is not recommended to prescribe tricyclic antidepressants simultaneously with moxonidine. During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary. Moxonidine should be stopped gradually.

Indications for use

Arterial hypertension.

Directions for use and doses

Inside, regardless of food intake, with a sufficient amount of liquid. In most cases, the initial dose of moxonidine is 0.2 mg per day in one dose, preferably in the morning. If the therapeutic effect is insufficient, the dose can be increased after 3 weeks of therapy to 0.4 mg per day in 2 doses or once. The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 doses, is 0.6 mg. Abrupt discontinuation of moxonidine is not recommended. Moxonidine should be discontinued gradually over 2 weeks. In patients with moderate renal failure (GFR more than 30 ml/min, but less than 60 ml/min), a single dose of moxonidine 0.2 mg and a daily dose of moxonidine 0.4 mg should not be exceeded. In patients on hemodialysis, the initial dose is 0.2 mg per day. If necessary and if well tolerated, the dose can be increased to 0.4 mg per day. Studies on the use of moxonidine in patients with liver failure have not been conducted. In elderly patients with normal renal function, dosage recommendations are the same as for adult patients.

Use during pregnancy and lactation

There are no clinical data on the treatment of pregnant women with moxonidine. Animal studies have revealed embryotoxic effects. As a precaution, taking moxonidine during pregnancy is not recommended. Moxonidine passes into breast milk. Breastfeeding women are advised to stop breastfeeding or discontinue the drug during treatment.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Carefully

Parkinson's disease (severe), epilepsy, glaucoma, depression, intermittent claudication, Raynaud's disease, first degree atrioventricular block, chronic renal failure (creatinine clearance more than 30 but less than 60), cerebrovascular diseases, after myocardial infarction, chronic heart disease insufficiency class I and II (according to the NYHA classification), for patients on hemodialysis; due to lack of experience in use - moderate liver failure (more than 9 points according to the Child-Pugh classification).

Interaction with other drugs

Concomitant use of other antihypertensive drugs enhances the hypotensive effect of moxonidine. Since tricyclic antidepressants may reduce the effect of centrally acting antihypertensive drugs, coadministration of tricyclic antidepressants with moxonidine is not recommended. Moxonidine may enhance the effect of tricyclic antidepressants (simultaneous use should be avoided), tranquilizers, alcohol, sedatives and hypnotics. Moxonidine may moderately improve impaired cognitive function in patients receiving lorazepam. Prescribing moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter. Moxonidine is eliminated by tubular secretion. Interactions with other drugs eliminated by tubular secretion cannot be excluded. When taken orally simultaneously with glibenclamide, the bioavailability of glibenclamide is reduced by 11%.

Contraindications

Hypersensitivity to the components of the drug; sick sinus syndrome, sinoatrial and atrioventricular block II and III degrees, severe bradycardia (resting heart rate (HR) less than 50 beats/min), chronic heart failure class III and IV (NYHA classification), history of angioedema, severe liver failure, unstable angina, chronic renal failure (creatinine clearance less than 30 ml/min, creatinine more than 160 µmol/l), age under 18 years (efficacy and safety have not been established), lactation, pregnancy, concomitant use with tricyclic antidepressants. Hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Compound

One film-coated tablet contains: active substance: moxonidine – 0.2 mg. excipients: crospovidone, magnesium stearate, lactose monohydrate; for a dosage of 0.2 mg opadry II pink: polyvinyl alcohol, titanium dioxide (E171), polyethylene glycol, talc, iron oxide red (E172), iron oxide yellow (E172)

Overdose

Symptoms: headache, sedation, drowsiness, excessive decrease in blood pressure, dizziness, general weakness, bradycardia, dry mouth, vomiting, fatigue and stomach pain. A short-term increase in blood pressure, tachycardia, and hyperglycemia are also potentially possible. Treatment: There is no specific antidote. In case of a decrease in blood pressure, it is recommended to restore circulating blood volume by administering fluids and administering dopamine. Bradycardia can be relieved with atropine. Alpha-adrenergic antagonists may reduce or eliminate paradoxical hypertension following moxonidine overdose.

Side effect

The frequency of adverse reactions indicated below was determined using the following scale: very often (> 1/10), often (> 1/100 - 1/1000 -

Storage conditions

In a place protected from moisture and light at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Moxonidine FT

Pharmacodynamics

Moxonidine has been shown to be a potent antihypertensive agent in various animal models. Available experimental data convincingly indicate that the site of manifestation of the antihypertensive effect of moxonidine is the central nervous system. It has been established that moxonidine selectively interacts with I1-imidazoline receptors located in the brain stem. These imidazoline-sensitive receptors are concentrated in the rostral ventrolateral medulla, an area responsible for central regulation of the peripheral sympathetic nervous system. The binding of moxonidine to I1-imidazoline receptors leads to suppression of sympathetic nerve activity (indicated for cardiac, visceral and renal sympathetic nerves).

Moxonidine differs from other centrally acting antihypertensive drugs by its lower affinity for central alpha2-adrenergic receptors compared to I1-imidazoline receptors; Alpha2-adrenergic receptors are the molecular target through which the most common adverse reactions of centrally acting antihypertensive drugs, such as sedation and dry mouth, occur. In humans, moxonidine leads to a decrease in systemic vascular resistance and, consequently, blood pressure.

Pharmacokinetics

Absorption: After oral administration, moxonidine is rapidly absorbed. In humans, approximately 90% of the oral dose of moxonidine is absorbed; it is not subject to the first pass effect through the liver, and its bioavailability is 88%. Food intake does not affect the pharmacokinetics of moxonidine.

Distribution: only about 7% of moxonidine is bound to plasma proteins (volume of distribution is 1.8 ± 0.4 l/kg). Maximum plasma concentrations of moxonidine are achieved 30 to 180 minutes after taking the film-coated tablet.

Metabolism: About 10 – 20% of moxonidine is metabolized mainly to 4,5-dehydromoxonidine and guanidine derivatives due to opening of the imidazoline ring. The hypotensive effect of 4,5-dehydromoxonidine is only 1/10 that of moxonidine, and for guanidine derivatives it is less than 1/100.

Excretion: Moxonidine and its metabolites are almost completely excreted through the kidneys. More than 90% of the dose is excreted through the kidneys during the first 24 hours after administration and about 1% is excreted in the feces. The proportion of excreted unchanged moxonidine is approximately 50–75%. The average half-life of moxonidine from blood plasma is 2.2 - 2.3 hours, the half-life by the kidneys is 2.6 - 2.8 hours.

Pharmacokinetics in elderly patients Slight differences in the pharmacokinetic properties of moxonidine in healthy elderly patients and healthy young adults are not clinically significant. Since moxonidine does not accumulate, there is no need for dose adjustment if normal renal function is maintained.

Pharmacokinetics in children Pharmacokinetic studies in children have not been conducted.

Pharmacokinetics in patients with impaired renal function With moderately reduced renal function (glomerular filtration rate 30 - 60 ml/min), AUC increased by 85%, and clearance decreased by 52%. In such patients, the hypotensive effect of moxonidine should be carefully monitored, especially at the beginning of treatment. Doses should be adjusted individually for these patients, with the maximum daily dose not exceeding 0.4 mg and the maximum single dose not exceeding 0.2 mg. In patients with severe renal impairment (glomerular filtration rate <30 ml/min), clearance is reduced by 68%, and the half-life increases to 7 hours. In these patients, the initial dose of moxonidine is 0.2 mg per day and, if clinically indicated and well tolerated, can be increased to a maximum of 0.3 mg per day. The hypotensive effect of moxonidine should be carefully monitored, especially at the beginning of treatment.