Moxonidine-ZZ, 0.4mg pills, 60pcs

Composition

Active ingredient:

moxonidine 0.4 mg

excipients (core):

croscarmellose sodium (primellose) – 3.0 mg;

lactose monohydrate (lactopress) (milk sugar) – 95.1 mg;

colloidal silicon dioxide (aerosil) – 0.5 mg;

sodium stearyl fumarate-1.0 mg;

excipients (shell):

Opadray II (polyvinyl alcohol, partially hydrolyzed-1.32 mg; titanium dioxide E 171-0.5751 mg; talc-0.6 mg; macrogol (polyethylene glycol 3350) – 0.3705 mg; soy lecithin E 322-0.105 mg; aluminum varnish based on Indigo Carmine-0.0018 mg; aluminum varnish based on azorubin-0.0153 mg; aluminum varnish based on dye red [Ponso 4R] -; 0.0123 mg).

Description:

Film-coated tablets of dark pink color, round, biconvex. Tablets on the break are white or almost white in color.

Pharmacological action

Pharmacotherapeutic group of the medicinal product:

Antihypertensive agent of central action.

ATX Code: [C 02 TO 05]

Pharmacodynamics

Moxonidine is an antihypertensive agent with a central mechanism of action. In the brain stem structures (rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazoline-sensitive receptors involved in the tonic and reflex regulation of the sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure (BP). Moxonidine differs from other sympatholytic antihypertensive agents in its lower affinity for α2-adrenergic receptors, which explains the lower likelihood of sedation and dry mouth. Taking moxonidine leads to a decrease in systemic vascular resistance and blood pressure. Moxonidine improves the insulin sensitivity index by 21% (compared to placebo) in patients with obesity, insulin resistance and moderate arterial hypertension. Pharmacokinetics

Suction:  

After oral use, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. Absolute bioavailability is approximately 88%. The time to reach the 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. Elimination The elimination half-lives (T 1/2) of moxonidine and the metabolite are 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys (about 78% in unchanged form and 13% in the form of dehydromoxonidine, 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: Compared with healthy volunteers, patients with arterial hypertension showed no changes in the pharmacokinetics of moxonidine.

Pharmacokinetics in the elderly

Clinically insignificant changes in the pharmacokinetic parameters of moxonidine in elderly patients were noted, 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 patients younger than 18 years of age, and therefore no pharmacokinetic studies have been conducted in this group. Pharmacokinetics in patients with renal insufficiency

Moxonidine clearance is strongly correlated with creatinine clearance (CC). In patients with moderate renal insufficiency (creatinine clearance in the range of 30-60 ml/min), steady-state plasma concentrations and final T 1/2 are approximately 2 and 1.5 times higher than in patients with normal renal function (creatinine clearance greater than 90 ml/min).

In patients with severe renal insufficiency (creatinine clearance less than 30 ml/min), steady-state plasma concentrations and final T 1/2 are 3 times higher than in patients with normal renal function. use of multiple doses of moxonidine leads to predictable accumulation in the body of patients with moderate to severe renal insufficiency. In patients with end-stage renal insufficiency (creatinine clearance less than 10 ml/min) undergoing hemodialysis, the steady-state plasma concentrations and final T 1/2 are 6 and 4 times higher, respectively, than in patients with normal renal function. In all groups, the maximum concentration of moxonidine in blood plasma is 1.5 – 2 times higher. In patients with impaired renal function, the dosage should be selected individually. Moxonidine is slightly eliminated during hemodialysis.

Indications

Arterial hypertension.

Contraindications

-hypersensitivity to the Active ingredient and other components of the drug; 

syndrome of weakness of the sinus node;

– severe bradycardia (heart rate of rest of less than 50 beats/min);

– atrioventricular block II and III degree;

– severe heart rhythm disorders; acute and chronic heart failure (III-IV functional class NYHA classification);

– simultaneous use of tricyclic antidepressants (see section “Interaction with other medicines”);

– severe renal failure (CC less than 30 ml/min);

– hemodialysis;

– lactation period;

– hereditary lactose intolerance, lactase deficiency or malabsorption of glucose – galactose;

– age over 75 years of age;

the age of 18 (due to the lack of data on safety and efficacy).

With caution

Special care should be taken when using moxonidine in patients with grade I atrioventricular block (risk of developing bradycardia), severe coronary artery disease, severe coronary artery disease or unstable angina (insufficient experience), chronic heart failure, severe hepatic insufficiency, and impaired renal function (creatinine clearance greater than 30 ml/min).

Side effects

The frequency of side effects listed below was determined according to the following: very common (>1/10); often (>>1/100, >><1/10); infrequently (>1/1000, <1/10); infrequently (>

From the central nervous system:

Common: headache*, dizziness (vertigo), drowsiness.

Infrequently: fainting*.

From the cardiovascular system:  

Infrequently: marked decrease in blood pressure, orthostatic hypotension*, bradycardia.

From the gastrointestinal tract:  

Very common: dryness of the oral mucosa.

Common: diarrhea, nausea, vomiting, dyspepsia.

Skin and subcutaneous tissue disorders:

Common: skin rash, pruritus.

Infrequently: angioedema.

Mental disorders:

Common: insomnia.

Infrequently: nervousness.

Hearing disorders and labyrinth disorders:

Infrequently: ringing in the ears.

Musculoskeletal and connective tissue disorders:

Common: back pain.

Infrequently: neck pain.

General disorders and disorders at the injection site:

Often: asthenia.

Infrequently: peripheral edema.

(*- the frequency is comparable to placebo).

Interaction

The combined use of moxonidine with other antihypertensive agents leads to an additive effect. Tricyclic antidepressants may reduce the effectiveness of central antihypertensive agents, and therefore they are not recommended to be taken together with moxonidine.

Moxonidine may enhance the effects of tricyclic antidepressants, tranquilizers, ethanol, sedatives, and sleeping pills.

Moxonidine is able to moderately improve impaired cognitive function in patients receiving lorazepam.

Moxonidine may increase the sedative effect of benzodiazepine derivatives when administered concomitantly.

Moxonidine is secreted by tubular secretion. Therefore, its interaction with other drugs released by tubular secretion is not excluded.

Beta-blockers increase bradycardia, the severity of negative ino-and dromotropic effects.

How to take, course of use and dosage

Inside, regardless of food intake. In most cases, the initial dose of Moxonidine is 0.2 mg per day. The maximum single dose is 0.4 mg.

The maximum daily dose, which should be divided into 2 doses, is 0.6 mg. Individual adjustment of the daily dose is necessary, depending on the patient’s tolerance to the therapy.

No dose adjustment is required for patients with hepatic insufficiency.

The initial dose for patients with moderate or severe renal insufficiency is 0.2 mg / day. If necessary and with good tolerability, the daily dose can be increased to a maximum of 0.4 mg.

Overdose

Several cases of non-fatal overdose have been reported with simultaneous doses of up to 19.6 mg.

Symptoms:  

headache, sedation, marked decrease in blood pressure, dizziness, asthenia, bradycardia, dry oral mucosa, vomiting, increased fatigue, epigastric pain, respiratory depression and impaired consciousness. In addition, short-term increases in blood pressure, tachycardia, and hyperglycemia are also possible, as has been shown in several high-dose animal studies.

Treatment:

There is no specific antidote. In the case of a marked decrease in blood pressure, it may be necessary to restore the volume of circulating blood through the introduction of fluid and dopamine (by injection).

Bradycardia can be stopped by atropine (injection).

In severe cases of overdose, it is recommended to carefully monitor disorders of consciousness and avoid respiratory depression.

Alpha-adrenergic antagonists may reduce or eliminate the paradoxical hypertensive effects of moxonidine overdose.

Moxonidine is slightly eliminated during hemodialysis.

Special instructions

If it is necessary to cancel simultaneously taking beta-blockers and the drug Moxonidine, first cancel beta-blockers and only after a few days Moxonidine. Currently, there is no evidence that discontinuation of Moxonidine leads to an increase in blood pressure. However, it is not recommended to stop taking Moxonidine abruptly, instead, gradually reduce the dose of the drug over two weeks. Avoid alcohol consumption during treatment. During treatment, regular monitoring of the heart rate and electrocardiography is necessary.

Influence on the ability to drive motor vehicles and manage mechanisms

The effect of Moxonidine on the ability to drive vehicles or operate machinery has not been studied. However, taking into account the possibility of dizziness and drowsiness, patients should exercise caution when engaging in potentially dangerous activities that require increased attention, such as driving vehicles or operating equipment that requires increased concentration of attention.

Form of production

Film-coated tablets of dark pink color, round, biconvex.

Tablets with a break of white or almost white color (dosage of 0.4 mg).

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Moxonidine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension