Moxonidine-ZZ, 0.3mg pills, 28pcs

Composition

Active ingredient:

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 stearyl fumarate; 1.0 mg;

excipients (shell):

Opadray 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 varnish based on the dye crimson [Ponceau 4R] – 0.0039 mg; aluminum varnish based on the dye sunny sunset yellow 0.0003 mg).

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

Use during pregnancy and lactation

Pregnancy

There are no clinical data on the use of Moxonidine in pregnant women.

In the course of animal studies, the embryotoxic effect of the drug was established. Moxonidine should be given to pregnant women only after careful assessment of the risk-benefit ratio, when the benefit to the mother outweighs the potential risk to the fetus.

Lactation period

Moxonidine is excreted in breast milk and should therefore not be administered during breast-feeding. If it is necessary to use Moxonidine during lactation, breastfeeding should be discontinued.

Contraindications

• Renal failure severe (CC less than 30 ml/min);
• severe heart rhythm disturbances;
• SSSU;
• bradycardia (heart rate at rest of less than 50 beats/min);
• AV-block II and III degree
• acute and chronic heart failure (III-IV functional class NYHA classification);
• the simultaneous use of tricyclic antidepressants;
• hemodialysis;
• lactation;
• age older than 75 years;
• the age of 18 (due to the lack of data on safety and efficacy);
• hereditary lactose intolerance, lactase deficiency or malabsorption of glucose-galactose;
• hypersensitivity to the Active ingredient and other components of the drug.

With caution

Special care should be taken when using moxonidine in patients with grade I AV block (risk of developing bradycardia), severe coronary artery disease, severe CHD or unstable angina (insufficient experience), chronic heart failure, severe hepatic insufficiency, 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*. Mental disorders: often-insomnia; infrequently-nervousness. From the side of the organ of hearing and labyrinth disorders: infrequently-tinnitus. From the cardiovascular system: infrequently-marked decrease in blood pressure, orthostatic hypotension*, bradycardia. From the digestive system: very often – dryness of the oral mucosa; often-diarrhea, nausea, vomiting, dyspepsia. From the skin and subcutaneous tissues: often – skin rash, itching. From the musculoskeletal system: often-back pain; infrequently-pain in the neck. Allergic reactions: infrequently-angioedema. 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 it, course of use and dosage

Inside, regardless of food intake. 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.

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, excessive lowering of 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 studies of the use of the drug in high doses in animals.

Treatment:  there is no specific antidote.In the case of an excessive decrease in blood pressure, it may be necessary to restore the BCC by injecting fluid and dopamine. 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-SZ, first cancel beta-blockers and only after a few days Moxonidine-SZ. Currently, there is no evidence that discontinuation of Moxonidine-SZ leads to an increase in blood pressure. However, it is not recommended to stop taking Moxonidine-SZ 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.

Storage conditions

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

Shelf life

3 years

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