Moxonidine - instructions for use, dose, side effects, contraindications

Excipients (core): lactose monohydrate (sugar milk) - 92,800 mg; croscarmellose sodium - 4,000 mg; Povidone-K25 - 2,000 mg; magnesium stearate - 1,000 mg.

Auxiliary substances (shell): hypromellose - 1,710 mg; Macrogol-4000 - 0.450 mg; dye iron oxide red - 0.025 mg; titanium dioxide - 0.815 mg.

Dosage 0.4 mg

Active substance: moxonidine 0.400 mg.

Excipients (core): lactose monohydrate (sugar milk) - 185,600 mg; croscarmellose sodium - 8,000 mg; povidone-K25 - 4,000 mg; magnesium stearate - 2,000 mg.

Auxiliary substances (shell): hypromellose - 3,420 mg; Macrogol-4000 - 0,900 mg; dye iron oxide red - 0.050 mg; titanium dioxide - 1,630 mg.

Description:

Round, biconvex tablets, covered with a film membrane from pink to pale pink. On the cross-section, two layers are visible: a nearly white core and a film shell.

Pharmacotherapeutic group:Hypotensive central agent

ATX: & nbsp

C.02.A.C.05 Moxonidine

Pharmacodynamics:

Moxonidine selective imidazoline receptor agonist. Selectively interacting with imidazoline I₁-receptors located in the brain stem, reduces sympathetic activity.

Moxonidine has a high affinity for imidazoline I₁-receptors and only slightly binds to the central alpha₂-adrenoceptors due to the interaction with which the dryness of the mucous membrane of the oral cavity and sedation are explained.

Reduces the resistance of tissues to insulin, stimulates the release of growth hormone.

Influence on hemodynamics: a decrease in systolic and diastolic blood pressure (BP) with a single and prolonged administration of moxonidine is associated with a decrease in the pressor effect of the sympathetic system on peripheral vessels, a reduction in peripheral vascular resistance, while cardiac output and heart rate do not change significantly.

The maximum antihypertensive effect is achieved approximately 2.5-7 hours after ingestion.

Pharmacokinetics:

Suction

Absorption - 90%. Maximum concentration (FROM_mOh) in blood plasma (after taking a tablet containing 0.2 mg of moxonidine) is 1.4-3 ng / ml and is reached after 30-180 minutes. Bioavailability is 88%, which indicates a lack of a significant effect of "primary transmission" (eating does not affect the pharmacokinetics).

Distribution

The volume of distribution is 1.8 ± 0.4 l / kg. Penetrates through the blood-brain barrier (BBB). Binding to plasma proteins is approximately 10%.

Metabolism

The main metabolites: 4,5-dihydromoxonidine and guanidine derivatives. The pharmacodynamic activity of 4,5-dihydromoxonidine is about 10% compared to moxonidine.

Excretion

The half-life (T_1/2) of moxonidine and metabolites is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys, about 50-75% unchanged, and 13% in the form of a dehydrogenated derivative. Less than 1% is excreted through the intestine. Do not cumulate with prolonged use. Average final T_1/2moxonidine in blood plasma is 2.2-2.3 hours, renal median terminal T_1/2 - 2.6-2.8 hours. Despite the fact that T_1/2moxonidine and its metabolites is 2.5 and 5 hours, it should not be used more often than twice a day.

Pharmacokinetics in patients with arterial hypertension

But in comparison with healthy volunteers, patients with hypertension do not have any changes in the pharmacokinetics of moxonidine.

Pharmacokinetics in old age

There are age-related changes in pharmacokinetics, probably associated with slightly higher bioavailability and / or reduced metabolic activity. However, these changes are not clinically significant.

Pharmacokinetics in children

Moxonidine is not recommended for use in patients younger than 18 years of age, and therefore pharmacokinetic studies have not been conducted in this group.

Pharmacokinetics in renal failure

The excretion of moxonidine is largely correlated with the clearance of creatinine (CC).

In patients with moderate renal failure (CK in the range of 30-60 ml / min), the equilibrium concentrations in the blood plasma and the final T_1/2 approximately 2 and 1.5 times higher than in patients with arterial hypertension with normal renal function (CC> 90 mL / min).

In patients with severe renal failure (CK <30 ml / min), equilibrium concentrations in the blood plasma and final T_1/2 3 times higher than in patients with normal renal function. The appointment of multiple doses of the drug does not lead to cumulation in the body of patients with moderate renal failure.

In the late stages of patients with terminal stage of renal failure (CC <10 ml / min) on hemodialysis, the equilibrium concentrations in the blood plasma and the final T_1/2 respectively, 6 and 4 times higher than in patients with normal function of the nights. In patients with impaired renal function, the dosage should be selected individually. Moxonidine is slightly excreted during hemodialysis.

Indications:Ahypertension.

Contraindications:

- Hypersensitivity to the components of the drug;

- pronounced bradycardia (heart rate (heart rate) less than 50 beats per minute) or severe bradyarrhythmia, including sinus node weakness syndrome, atrioventricular blockade of II and III degree;

- hemodynamically significant violations of the rhythm of the heart;

- severe chronic heart failure III-IV functional class by classification NYHA;

- use in patients aged 75 years and older;

- severe renal failure (CC less than 30 ml / min, creatinine of blood plasma more than 160 μmol / l);

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

- age under 18 years (effectiveness and safety not established);

- simultaneous reception with tricyclic antidepressants;

- due to lack of experience, moxonidine should be avoided in patients with concomitant "intermittent" lameness, Raynaud's disease, Parkinson's disease, epilepsy, glaucoma and depression.

Carefully:

Atrioventricular block of degree I, chronic heart failure I-II functional class by classification NYHA, bradycardia, chronic renal failure (QC more than 30, at less than 60 ml / min), angioedema in history, severe coronary artery disease, unstable angina, elderly age.

Pregnancy and lactation:

Due to a lack of clinical experience Moxonidine should not be administered during pregnancy, except when the expected benefit to the mother exceeds the potential risk to the fetus.

Moxonidine is excreted in breast milk.If you need to use the drug during lactation, breastfeeding is recommended to stop or cancel the drug.

Dosing and Administration:

Tablets are taken orally, regardless of food intake, with a sufficient amount of liquid.

In most cases, the drug Moxonidine Assign an initial dose of 0.2 mg at one time, preferably in the morning. If the therapeutic effect is inadequate, the dose can be increased after 3 weeks of therapy to 0.4 mg per day in 2 divided doses or once; if after 3 weeks of treatment the response to the therapy is unsatisfactory, you can increase the dose to 0.6 mg, divided into 2 doses (in the morning and in the evening). The maximum single dose is 0.4 mg; maximum daily dose divided by for 2 doses - 0.6 mg.

The initial dose for patients with renal insufficiency (CK 30-60 ml / min) is 0.2 mg. If necessary and good tolerability, the daily dose can be increased to 0.4 mg.

Have elderly patients with normal renal function recommendations for dosage are the same as for adult patients. Start therapy with a minimal dose and then increase the dose with caution.

The use of the drug in patients 75 years of age and older is contraindicated (see section "Contraindication").

Side effects:

The frequency of undesirable effects is as follows, according to the classification of the World Health Organization: very often (≥1/10), often (≥1/100 to <1/10), infrequently (≥1/1000 to <1/100), rarely (≥1/10 000 to <1/1 000), very rarely (<1/10 000), the frequency is unknown (it is impossible to determine based on available data).

From the side of the cardiovascular system: often - symptoms of vasodilation; infrequent - marked decrease in blood pressure (including orthostatic hypotension), peripheral circulation disorders.

From the central nervous system: often - dizziness, headache, drowsiness, vertigo, fatigue, sleep disturbance; infrequently, fainting, paresthesia.

Mental disorders: often - insomnia, cognitive impairment; infrequently - nervousness, anxiety.

From the side of the hearing organ: infrequently, noise in the ears.

From the digestive system: very often - dryness of the oral mucosa; often - nausea, vomiting, diarrhea, indigestion; infrequently - anorexia.

From the genitourinary system: infrequently - impotence and / or decreased libido.

From the side of the organ of vision: infrequent - dry eyes, burning sensation of the eyes.

From the side of the musculoskeletal system: often - pain in the back; infrequently - pain in the neck.

From the endocrine system: infrequently - gynecomastia.

Allergic reactions: often - skin rash, itching; infrequently - angioedema.

Other: often - asthenia; infrequently - peripheral edema, weakness in the legs, tenderness in the parotid glands.

Overdose:

Symptoms: headache, sedative effect, drowsiness, marked decrease in blood pressure, dizziness, fatigue, asthenia, bradycardia, dryness of the oral mucosa, rarely - vomiting, pain in the upper abdomen. Paradoxical arterial hypertension, tachycardia and hyperglycemia are potentially possible.

Treatment: symptomatic, there is no specific antidote. To reduce the absorption of moxonidine (in the case of a recent intake) - gastric lavage, Activated carbon, laxatives. In the case of a marked decrease in blood pressure, it is recommended that the volume of circulating blood (BCC) be restored through the introduction of fluid and dopamine, bradycardia - the introduction of atropine.

Α-adrenoreceptor antagonists can reduce or eliminate paradoxical antihypertensive effects in overdose of moxonidine.

Interaction:

With the combined use of moxonidine with antihypertensive agents, mutual enhancement of antihypertensive action occurs.

When moxonidine is used with glibenclamide, digoxin, hydrochlorothiazide, there is no pharmacokinetic interaction.

Moxonidine increases the inhibitory effect on the central nervous system of anxiolytics, barbiturates and ethanol.

Tricyclic antidepressants may reduce the effectiveness of antihypertensive agents of central action (see section "Contraindications").

Beta-adrenoblockers increase bradycardia, the severity of the negative foreign and dromotropic effects of moxonidine.

Moxonidine moderately increases the reduced cognitive ability in patients taking lorazepam.

The use of moxonidine together with benzodiazepine derivatives may be accompanied by an increase in the sedative effect of the latter.

Tolazolin dose-dependent decreases the antihypertensive effect of moxonidine.

Special instructions:

If it is necessary to cancel simultaneously taken beta-blockers and the drug Moxonidine first abolish beta-blockers and only after a few days - Moxonidine.

During treatment with the drug, regular monitoring of blood pressure, heart rate and ECG is necessary.

Discontinue taking the drug gradually within 2 weeks.

The drug should be used with extreme caution in patients with severe coronary heart disease and / or unstable angina due to limited experience with the drug in this patient population, as well as in patients with moderate CHF.

During treatment with the drug should avoid drinking alcohol.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions (risk of dizziness and drowsiness).

Form release / dosage:

Tablets, film-coated, 0.2 mg and 0.4 mg.

Packaging:

By 7, 10, 14 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 30, 40, 50, 60 or 100 tablets in cans of polyethylene terephthalate or cans of polymeric for medicines.

One jar or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002898

Date of registration:04.03.2015

Expiration Date:04.03.2020

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp12.06.2018

Illustrated instructions

Instructions

Moxonidine (Moxonidine)