MOXONIDINE 400MCG PILLS

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MOXONIDINE 400MCG PILLS -28 TABS

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Moksonidin-SZ

moxonidine

Dosage form

film coated tablets

1 tablet, film coated, contains:

dosage 0.2 mg: active substance: 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 fumarate -; 1.0 mg;

excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed -; 1.32 mg; titanium dioxide E 171 -; 0.6027 mg; talc -; 0.6 mg; macrogol (polyethylene glycol 3350) -; 0.3705 mg; soybean lecithin E 322 -; 0.105 mg; iron dye oxide (II) yellow -; 0.0003 mg; iron dye oxide (II) red -; 0.0015 mg).

dosage 0.3 mg: active substance: moxonidine 0.3 mg excipients (core): croscarmellose sodium (primellose); 3.0 mg; lactose monohydrate (lactopress) (milk sugar) -; 95.2 mg; colloidal silicon dioxide (aerosil) -; 0.5 mg; sodium fumarate; 1.0 mg; excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed -; 1.32

mg; titanium dioxide E 171 -; 0.6003 mg; talc-; 0.6 mg; macrogol (polyethylene glycol 3350) -; 0.3705 mg; soy lecithin E 322 -; 0.105 mg; aluminum lacquer based on the crimson dye [Ponso 4R] -; 0.0039 mg; aluminum varnish based on dye sunsets yellow 0.0003 mg).

dosage 0.4 mg: active substance: moxonidine 0.4 mg excipients (core): to roscarmellose sodium (primellose) -; 3.0 mg; lactose monohydrate (lactopress) (milk sugar) -; 95.1 mg; colloidal silicon dioxide (aerosil) -; 0.5 mg; sodium fumarate -; 1.0 mg; excipients (shell): Opadry 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; soybean lecithin E 322 -; 0.105 mg; aluminum lacquer based on indigo carmine -; 0.0018 mg; aluminum lacquer based on dye azorubine -; 0.0153 mg; aluminum lacquer based on dye crimson [Ponso 4R] -; 0, 0123 mg).

Antihypertensive agent of central action.

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

Moxonidine differs from other sympatholytic antihypertensive drugs by its lower affinity for α2-adrenoreceptors, which explains the lower likelihood of developing a sedative effect and dry mouth.

Acceptance of moxonidine leads to a decrease in systemic vascular resistance and blood pressure.

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

Suction:

After oral administration, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. Absolute bioavailability is approximately 88%. Time to reach maximum concentration; about 1 hour Eating does not affect the pharmacokinetics of the drug.

Distribution

Communication with plasma proteins is 7.2%.

Metabolism

The main metabolite is; dehydrated moxonidine. Pharmacodynamic activity of dehydrated moxonidine -; about 10% compared with moxonidine.

Removal

The half-life (T1 / 2) of moxonidine and metabolite is 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 dehydriromaxonidine, other metabolites in the urine do not exceed 8% of the accepted dose). Less than 1% of the dose is excreted through the intestines.

Pharmacokinetics in patients with arterial hypertension:

Compared with healthy volunteers, there are no changes in moxonidine pharmacokinetics in patients with arterial hypertension.

Pharmacokinetics in the elderly

Clinically insignificant changes in the pharmacokinetic parameters of moxonidine in elderly patients are 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, and therefore in

no pharmacokinetic studies were performed for this group.

Pharmacokinetics for renal failure

Moxonidine clearance is significantly correlated with creatinine clearance (CK).

In patients with moderate renal insufficiency (CC in the range of 30-60 ml / min) equilibrium plasma concentrations and a final T1 / 2 are approximately 2 and 1, 5 times higher than in patients with normal renal function (CC more than 90 ml / min.) In patients with severe renal insufficiency (CC is less than 30 ml / min.), The equilibrium 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 cumulation in the body of patients with moderate to severe renal failure. In patients with end-stage renal failure (CC less than 10 ml / min) on hemodialysis, plasma plasma equilibrium concentrations and final T1 / 2 are 6 and 4 times higher, respectively, than in patients with normal renal function. In all groups, the maximum concentration of mocidine in plasma is 1.5–2 times higher. In patients with impaired renal function, the dosage should be adjusted individually. Moxonidine is slightly excreted during hemodialysis.

Indications for use

Arterial hypertension.

Contraindications

- increased sensitivity to the active substance and other components of the drug;

- syndrome of weakness of the sinus node;

- pronounced bradycardia (resting heart rate less than 50 beats / min);

- atrioventricular block II and III;

-expressed heart rhythm disturbances;

- acute and chronic heart failure (III

- IV functional class (NYHA classification);

- simultaneous use with tricyclic antidepressants (see the section "Interaction with other medicines");

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

-hemodialysis;

- lactation period;

- hereditary lactose intolerance, lactase deficiency or glucose malabsorption

- galactose;

- age over 75 years;

- age up to 18 years (due to lack of data on safety and efficacy).

Special care must be taken when using moxonidine in patients with

atrioventricular block I degree (risk of developing bradycardia); severe coronary vascular disease, severe coronary heart disease or unstable angina (insufficient use of experience), chronic heart failure, severe liver failure, with impaired renal function (CC more than 30 ml / min).

Pregnancy and Breastfeeding

Pregnancy

Clinical data on the use of moxonidine in pregnant women are not available. In animal studies, the embryotoxic effect of the drug was established. Moxonidine should be administered to pregnant women only after a thorough assessment of the risk-benefit ratio, when the benefit to the mother outweighs the potential risk to the fetus.

Lactation period

Moxonidine passes into breast milk and therefore should not be administered during breastfeeding.If you need to use Moxonidine during lactation, breastfeeding should be stopped.

Inside, regardless of the meal. In most cases, the initial dose of the drug 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. An individual adjustment of the daily dose depending on the patient's tolerance of the therapy being performed is required. Dose adjustment for patients with liver failure is not required. The initial dose for patients with moderate or severe renal insufficiency is 0.2 mg / day. If necessary and with good tolerance, the daily dose may be increased to a maximum of 0.4 mg.

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

From the side of the central nervous system:

Often: headache *, dizziness (vertigo), drowsiness. Infrequently: faint *.

Since the cardiovascular system:

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

From the gastrointestinal tract:

Very often: dryness of the oral mucosa.

Often: diarrhea, nausea, vomiting, dyspepsia .

Skin and Subcutaneous Tissues:

Often: skin rash, itching.

Infrequently: angioedema.

Mental Disorders:

Often: insomnia.

Infrequently: nervousness.

On the part of the organ of hearing and labyrinth disorders:

Infrequently: ringing in the ears.

From the musculoskeletal and connective tissue:

Often: back pain.

Infrequently: pain in the neck.

General disorders and disorders at the site of administration:

Often: asthenia.

Infrequently: peripheral edema. (* Frequency comparable to placebo).

There are reports of several cases of overdose without fatal outcome, when doses of up to 19.6 mg were simultaneously applied.

Symptoms:

headache, sedation, marked reduction in blood pressure, dizziness, asthenia, bradycardia, dry oral mucosa, vomiting, fatigue, pain in the epigastric region, 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 studies in animals.

Treatment

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

Bradycardia can be stopped by atropine (injectable). In severe cases of overdose, it is recommended to carefully monitor impairment of consciousness and avoid respiratory depression. Alpha-adrenoreceptor antagonists can reduce or eliminate the paradoxical hypertensive effects of moxonidine overdose. Moxonidine is slightly excreted during hemodialysis.

Interaction with other drugs

The combined use of moxonidine with other antihypertensive drugs leads to an additive effect. Tricyclic antidepressants can reduce the effectiveness of centrally acting antihypertensive drugs, and therefore they are not recommended in conjunction with moxonidine.

Moxonidine can enhance the action of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics. Moxonidine can moderately improve impaired cognitive function in patients receiving lorazepam. Moxonidine may enhance the sedative effect of benzodiazepine derivatives when administered concurrently. Moxonidine is secreted by tubular secretion. Therefore, its interaction with other drugs secreted by tubular secretion is not excluded. Beta-blockers enhance bradycardia, the severity of negative foreign and dromotropic action.

If you need to cancel simultaneously taken beta-blockers and

drug Moxonidine, first cancel beta-blockers, and only a few days later Moxonidine.

Currently, there is no evidence that discontinuation of the drug Moxonidine leads to an increase in blood pressure. However, it is not recommended to stop taking the drug Moxonidine abruptly, instead, you should gradually reduce the dose of the drug over two weeks.

During treatment, exclude alcohol.

During treatment, regular monitoring of heart rate and

electrocardiography.

Influence on ability to drive motor transport and control mechanisms

The effect of Moxonidine on the ability to drive a vehicle or control equipment has not been studied. However, taking into account the possibility of dizziness and drowsiness, patients should be careful when engaging in potentially hazardous activities that require increased attention, such as driving a vehicle or controlling equipment that requires high concentration of attention.

In a dry, dark place, at a temperature not higher than 25 ° C.

Keep out of the reach of children.

 

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