Moxonidine-ZZ, 0.2mg pills, 28pcs

Composition

1 film-coated tablet contains: dosage 0.2 mg:

Active ingredient:

moxonidine 0.2 mg

excipients (core):

croscarmellose sodium (primellose) – 3.0 mg;

lactose monohydrate (lactopress) (milk sugar) – 95.3 mg;

colloidal silicon dioxide (aerosil) – 0.5 mg;

sodium stearyl fumarate-1.0 mg;

excipients (shell):

Opadry II (polyvinyl alcohol, partially hydrolyzed -; of 1.32 mg;

titanium dioxide E 171 -; 0,6027 mg;

talc -; 0.6 mg;

macrogol (polyethylene glycol 3350) -; 0,3705 mg;

soy lecithin E 322 -; 0,105 mg;

dye iron oxide (II) yellow; 0,0003 mg;

dye iron oxide (II) red; 0.0015 mg).

Description The film-coated tablets are light pink, round, and 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]Pharmacodynamicamoxonidine 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. Pharmacokineticsabsorption: 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. The distribution of 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 were observed in elderly patients, probably due to a decrease in the intensity of its metabolism and/or slightly higher bioavailability. Pharmacokinetics in children Amoxonidine is not recommended for use in patients under 18 years of age, and therefore no pharmacokinetic studies have been conducted in this group. Pharmacokinetics in renal insufficiency, the elimination of moxonidine significantly correlates 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; – sinus node weakness syndrome; – severe bradycardia (resting heart rate less than 50 beats / min);- atrioventricular block of II and III degrees; – severe cardiac arrhythmias; – acute and chronic heart failure (NYHA functional class III-IV);- concomitant use with tricyclic antidepressants (see section “Interaction with other medicinal products”);- severe renal insufficiency (creatinine clearance less than 30 ml / min);- hemodialysis;- lactation period;- hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;- age over 75 years;- under 18 years of age (due to lack of safety and efficacy data). 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, with 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: Often: headache*, dizziness (vertigo), drowsiness. Infrequently: fainting*. From the cardiovascular system: Infrequently: marked decrease in blood pressure, orthostatic hypotension*, bradycardia. From the gastrointestinal tract: Very often: 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. From the side of the organ of hearing 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: Common: asthenia. Infrequently: peripheral edema. (*- the frequency is comparable to placebo).

Interaction

Moxonidine can be given with thiazide diuretics and slow calcium channel blockers. When moxonidine is co-administered with these and other antihypertensive agents, the effect of moxonidine is mutually enhanced.

When moxonidine is administered with hydrochlorothiazide, glibenclamide (glyburide) or digoxin, there is no pharmacokinetic interaction.

Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive drugs.

Beta-blockers increase bradycardia, the severity of the negative ino-and dromotropic effects of moxonidine. Moxinidine modestly enhances cognitive decline in patients taking lorazepam.

The use of moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter. When moxonidine is co-administered with moclobemide, there is no pharmacodynamic interaction.

How to take, course of use and dosage

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 daily dose, which should be divided into 2 doses (morning and evening), is 0.6 mg. The maximum single dose is 0.4 mg.

In elderly patients with normal renal function, the dosage recommendations are the same as for adult patients.

In patients with renal insufficiency (cretinin clearance 30-60 ml per minute) and patients undergoing hemodialysis, a single dose should not exceed 0.2 mg, the maximum daily dose is 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. 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.

Composition

Tablet Form of production

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 prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Hypertension