Moxonitex - instructions for use, doses, side effects, contraindications

Selective agonist imidazoline receptors responsible for reflex control of the sympathetic nervous system (localized in the ventro-lateral region of the medulla oblongata). Slightly associated with central alpha₂-adrenoceptors, lowers systolic and diastolic blood pressure (BP) for a single and prolonged use.

With long-term use, it reduces myocardial hypertrophy of the left ventricle, neutralizes the signs of myocardial fibrosis, microarthiopathy, normalizes the capillary blood supply of the myocardium, reduces the overall peripheral vascular resistance, pulmonary vascular resistance, while cardiac output and heart rate do not change significantly. Against the background of treatment, the activity of norepinephrine and epinephrine, renin, angiotensin II at rest and under load, atrial natriuretic peptide (under load) and aldosterone of blood plasma decrease. Reduces the resistance of tissues to insulin by 21% compared with placebo in obese patients,and insulin-resistant patients with moderate severity of hypertension, stimulates the release of growth hormone. Does not affect the exchange of glucose and lipids.

Pharmacokinetics:

Suction

After oral administration, it is quickly and almost completely absorbed from the gastrointestinal tract (about 90%). The intake of food by the amount of absorption is not affected. The maximum concentration in the blood plasma (C_m_Oh) is achieved after 30-180 minutes after oral administration and is 1-3 ng / ml. The interval between achievement C_m_Oh and a marked decrease in blood pressure at rest differs by an average of 10%, with a load - by 7.7%. The duration of action is more than 12 hours. Bioavailability with a single oral application is 88%, which indicates the absence of a significant effect of the "primary" passage through the liver.

Distribution

Penetrates through the blood-brain barrier. Do not cumulate with prolonged use.

The volume of distribution is 1.4-3 l / kg. Relationship with blood plasma proteins 7%.

Metabolism

Metabolized 10-20% of moxonidine with the formation of 4,5-dehydromoxonidine and aminomethanamine derivative.

Excretion

The half-life (T_1/2) is 2-3 hours.In the first 24 hours, kidneys excrete more than 90% (50-75% in unchanged form, 20% in the form of metabolites) and about 1% with bile. Moxonidine in a small amount is derived from hemodialysis.

Special patient groups

Elderly age

There were no significant differences in pharmacokinetics in young patients and elderly patients. Dose correction is not required provided normal renal function.

Impaired renal function

In patients with moderate (creatinine clearance (CK) 30-60 ml / min) and severe (KC <30 ml / min) renal dysfunction, the equilibrium concentrations in the blood plasma and the final T_1/2approximately 2 and 3 times higher, respectively, than in patients with arterial hypertension with normal renal function (CK> 90 ml / min). Therefore, for patients with severe renal dysfunction, the drug is contraindicated, and with moderate renal dysfunction, the drug should be used with caution, its dose should be selected individually.

Impaired liver function

There are no reliable studies of the use of moxonidine in patients with impaired liver function. As moxonidine practically not metabolized in the liver, the disruption of its function does not have a pronounced effect on the pharmacokinetics of the drug.

Indications:Arterial hypertension.

Contraindications:

- Hypersensitivity to moxonidine or any other component of the drug;

- hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

- severe cardiac rhythm disturbances (severe bradycardia (less than 50 beats per minute at rest), sinus node weakness syndrome or sinoatrial block, atrioventricular blockade of degree II and III);

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

- severe renal failure (CC <30 ml / min, serum creatinine concentration> 160 μmol / L) and hemodialysis;

- simultaneous use with tricyclic antidepressants;

- age to 18 years;

- the period of breastfeeding.

Carefully:

- Atrioventricular block of the 1st degree (risk of developing bradycardia), coronary artery disease (including ischemic heart disease, unstable angina, early post-infarction period),

- peripheral circulation diseases (including intermittent claudication, Raynaud's syndrome), epilepsy, Parkinson's disease, depression, glaucoma;

- moderate renal insufficiency (CK 30-60 ml / min, serum creatinine 105-160 μmol / l), hepatic insufficiency;

- Pregnancy.

Pregnancy and lactation:

There were no reliable studies of the use of moxonidine in pregnant women. Studies in animals have shown an embryotoxic effect.

There are no clinical data on the negative effect on the course of pregnancy. However, Moxonitex should be administered to pregnant women only if the potential benefit to the mother exceeds the possible risk to the fetus.

Moxonidine penetrates into breast milk, women during the period of treatment are recommended to stop breastfeeding or to cancel the drug.

Dosing and Administration:

Moxonitex is administered internally, regardless of food intake, with a sufficient amount of liquid. Dose regimen is selected individually.

In the absence of other prescriptions, Moxonitex should be given in the following doses: 0.2 mg of the drug in the morning as the initial dose. With insufficient therapeutic effect, the dose after 3 weeks is increased to 0.4 mg / day once or in 2 divided doses. The maximum daily dose is 0.6 mg, the maximum single dose is 0.4 mg.

In patients with mild renal impairment (CK 30-60 ml / min) single dose should not exceed 0.2 mg, and the maximum daily dose - 0.4 mg.

Side effects:

According to the World Health Organization (WHO), the side effects are classified according to their frequency of development as follows: often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1 / 10000, <1/1000) and very rarely (<1/10000), including individual messages.

From the side of the cardiovascular system

infrequently: bradycardia, marked decrease in blood pressure (including orthostatic hypotension).

From the central part of the system

often: dizziness (vertigo), headache, drowsiness, insomnia;

infrequently: fainting, increased excitability.

From the side of the hearing organ and labyrinthine disorders

infrequently: tinnitus.

From the digestive system

Often: dryness of the oral mucosa;

often: diarrhea, nausea, vomiting, indigestion.

From the skin and subcutaneous tissues

often: skin itching, skin rash;

infrequently: angioedema (angioedema) (angioedema).

From the musculoskeletal and connective tissue

often: backache;

infrequently: pain in the neck.

General disorders and disorders in the place of attention

often: asthenia;

infrequently: peripheral edema.

Overdose:

Symptoms: headache, marked decrease in blood pressure, bradycardia, palpitations, weakness, drowsiness, dryness of the oral mucosa, rarely vomiting and epigastric pain. Paradoxical arterial hypertension and hyperglycemia are potentially possible.

Treatment: symptomatic. There is no specific antidote. With a pronounced decrease in blood pressure, it is recommended that the volume of circulating blood be restored by introducing a liquid. Alpha-adrenoreceptor antagonists can reduce or eliminate transient hypertension in an overdose of moxonidine.

Interaction:

The combined use of moxonidine with other antihypertensive agents leads to an additive effect.

Tricyclic antidepressants can reduce the effectiveness of antihypertensive agents of central action, and therefore it is not recommended that they be taken together with moxonidine. Moxonidine can enhance the sedative effect of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.

Moxonidine is able to moderately improve the weakened cognitive function of patients receiving lorazepam.

Moxonidine may enhance the sedative effect of benzodiazepine derivatives when used simultaneously. Moxonidine is excreted by tubular secretion, therefore, its interaction with other drugs, excreted by tubular secretion, is not excluded.

Special instructions:

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

If it is necessary to cancel simultaneously taken beta-blockers and Moxonitex, beta-blockers are the first to be canceled and only a few days later the drug Moxoniteks. At present, there is no evidence that discontinuation of Moxonitex leads to an increase in blood pressure. However, Moxonitex should not be discontinued.

In elderly patients, the risk of developing cardiovascular complications due to the use of antihypertensive drugs may be increased, so therapy with Moxonitex should be started with a minimal dose.

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

The effect of the drug Moxoniteks ability to drive vehicles or control technology was not studied.However, taking into account the possible occurrence of dizziness and drowsiness, patients should be careful when dealing with potentially hazardous activities requiring increased attention, such as driving vehicles or controlling equipment that requires increased concentration.

Form release / dosage:

Tablets, film-coated, 0.2 mg, 0.3 mg and 0.4 mg.

Packaging:

For 7, 10 or 14 tablets per blister.

For 1, 2, 3, 4 and 5 blisters together with instructions for use in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000084/10

Date of registration:15.01.2010 / 30.12.2016

Expiration Date:Unlimited

The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia

Manufacturer: & nbsp

SALUTAS PHARMA, GmbH Germany

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp12.06.2018

Illustrated instructions

Instructions

Moxonitex (Moxonitex)