Physiotensis, 0.4 mg 28 pcs

Moxonidine is a hypotensive agent with a central mechanism of action. In brain stem structures (rostral layer of lateral ventricles) moxonidine selectively stimulates imidazoline-sensitive receptors participating in tonic and reflex regulation of sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure (BP).

Moxonidine differs from other sympatholytic hypotensive agents in its lower affinity for a2-adrenoreceptors, which explains the lower likelihood of sedation and dry mouth.

The administration of moxonidine leads to a decrease in systemic vascular resistance and BP. The hypotensive effect of moxonidine has been confirmed in double-blind, placebo-controlled, randomized trials.

Moxonidine improves insulin sensitivity index by 21% (compared to placebo) in patients with obesity, insulin resistance and moderate arterial hypertension.

Pharmacokinetics

Intake:
After oral administration, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. Absolute bioavailability is approximately 88%. Time of reaching maximum concentration is about 1 hour. Food intake has no effect on the pharmacokinetics of the drug.

Distribution: Binding to plasma proteins is 7.2%.

Metabolism:The main metabolite is dehydrated moxonidine. The pharmacodynamic activity of dehydrated moxonidine is about 10% compared to moxonidine.

Elimination: The elimination half-life (T1/2) of moxonidine and the 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 dehydroromoxonidine, other metabolites in the urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestine.

Pharmacokinetics in patients with arterial hypertension:

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

Pharmacokinetics in elderly patients:

Clinically insignificant changes in pharmacokinetic parameters of moxonidine have been observed in elderly patients, probably due to decreased metabolic rate and/or slightly higher bioavailability.

Pharmacokinetics in children:

Moxonidine is not recommended for use in persons younger than 18 years of age; therefore, no pharmacokinetic studies have been performed in this group.

Indications

Active ingredient

Composition

How to take, the dosage

Ingestion, regardless of meals.

In most cases, the starting dose of Physiotens® is 0.2 mg per day. The maximum single dose is 0.4 mg. The maximum daily dose to be divided into 2 doses is 0.6 mg.

The daily dose for patients with moderate to severe renal impairment and those on hemodialysis is 0.2 mg. If necessary and if well tolerated, the daily dose may be increased to 0.4 mg.

Interaction

Moxonidine may be administered with thiazide diuretics, “slow” calcium channel blockers and other hypotensive agents. Co-administration of moxonidine with these and other antihypertensive agents leads to an additive effect.

When prescribing moxonidine with hydrochlorothiazide, glibenclamide or digoxin no pharmacokinetic interaction has been found.

Tricyclic antidepressants may decrease the effectiveness of centrally acting antihypertensive agents, and therefore their use with moxonidine is not recommended.

Moxonidine may moderately improve impaired cognitive function in patients receiving lorazepam.

The administration of moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter.

There is no pharmacodynamic interaction when prescribing moxonidine with moclobemide.

Special Instructions

A BP, HR and ECG should be monitored regularly during treatment. In CKG below 60 ml/min the dose is reduced by half, below 30 ml/min – the dose is discontinued.

At the time of treatment, caution should be exercised while driving motor transport and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Synopsis

Contraindications

Hypersensitivity to the active substance and other ingredients of the drug; sinus node weakness syndrome, marked bradycardia (resting heart rate (HR) less than 50 bpm).

Hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

In the absence of safety and efficacy data, it is not recommended to prescribe moxonidine to persons under 18 years of age.

With caution: severe and terminal renal failure; patients undergoing hemodialysis; due to lack of experience, severe hepatic insufficiency (more than 9 points by the Child-Pugh classification).

Side effects

Central nervous system disorders: Often (1-10%): headache, dizziness, somnolence. Infrequent (< 1%): insomnia.

Cardiovascular system: Rarely (< 0.1%): excessive BP decrease, orthostatic hypotension.

Gastrointestinal tract: Often (1-10%): dry mouth. Infrequent (< 1%): nausea.

Skin and subcutaneous fatty tissue: Infrequent (< 1%): skin rash, itching. Very rarely (< 0.01%): angioedema.

General: Often (1-10%): asthenia.

The most common side effects in patients taking moxonidine are: dry mouth, headache, dizziness, asthenia, and drowsiness. These symptoms often decrease after the first weeks of therapy.

Overdose

There have been reports of several non-fatal overdoses when doses up to 19.6 mg were used at one time.

Symptoms: headache, sedation, drowsiness, marked BP decrease, dizziness, fatigue, asthenia, bradycardia, dry mouth, vomiting and epigastric pain. Short-term elevation of BP, tachycardia, and hyperglycemia are also possible.

Treatment:

There is no specific antidote. In case of decreased blood pressure, restoration of circulating blood volume through fluid administration and dopamine administration is recommended.

Bradycardia can be controlled with atropine.

Alpha-adrenoreceptor antagonists may reduce or eliminate paradoxical hypertensive effects in moxonidine overdose.

Pregnancy use

Similarities