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

Selective agonist imidazoline receptors responsible for tonic and reflex control of the sympathetic nervous system (localized in the ventro-lateral region of the medulla oblongata).Reduces blood pressure (BP). Slightly associated with central alpha₂-adrenoceptors, due to the interaction with which mediated dry mouth and sedative effect.

Reduces the resistance of tissues to insulin.

Influence on hemodynamics: a decrease in systolic and diastolic blood pressure 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 decrease in peripheral vascular resistance, while cardiac output and heart rate (HR) do not change significantly.

Pharmacokinetics:

Absorption after oral administration - 90%. The intake of food by the amount of absorption is not affected. Bioavailability - 88%. Connection with blood plasma proteins - 7%. FROM_mOh in plasma is determined 30-180 minutes after oral administration and is 1-3 ng / ml. The volume of distribution is 1.4-3 l / kg. Passes through the blood-brain barrier. Do not cumulate with prolonged use. The half-life period is 2-3 hours. The kidneys are excreted by 90% (70% in unchanged form, 20% in the form of metabolites). There were no significant differences in pharmacokinetics in young and elderly patients.

Indications:

Arterial hypertension.

Contraindications:

Increased sensitivity to the drug, sick sinus syndrome and sinoatrial atrioventricular block II and III degree, bradycardia (heart rate less than 50 beats / min), chronic heart failure III and class (classification NYHA), Angioneurotic edema history, unstable angina, severe hepatic failure, chronic renal failure (creatinine clearance less than 30 mL / min, creatinine 160 umol / L), age 18 years (efficacy and safety have not been established), pregnancy and lactation , simultaneous reception with tricyclic antidepressants.

Carefully:BUsable Parkinson (severe), epilepsy, glaucoma, depression, "intermittent" claudication, Raynaud's disease, atrioventricular block I degree, chronic renal failure (creatinine clearance of more than 30 but less than 60 ml / min), cerebrovascular disease, post-myocardial infarction , chronic heart failure class I and II, expressed hepatic failure - due to lack of experience application hemodialysis.

Pregnancy and lactation:

During pregnancy and during breastfeeding, the use of the drug is contraindicated.

Dosing and Administration:

Inside, regardless of the reception of the poor, with enough liquid.

In most cases, the initial dose of moxonidine is 0.2 mg per day, at one time, preferably in the morning hours. If the therapeutic effect is insufficient, the dose can be increased after 3 weeks of therapy to 0.4 mg per day for 2 divided doses or once. The maximum daily dose, which should be divided into 2 divided doses (morning and evening), is 0.6 mg. The maximum single dose is 0.4 mg.

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

In patients with renal insufficiency (clearance of creatinine 30-60 ml / min) and patients on hemodialysis, single dose should not exceed 0.2 mg, the maximum daily dose of 0.4 mg.

Side effects:

Especially at the beginning of therapy the most frequent adverse reactions were: dry mouth, headache, dizziness, asthenia, peripheral edema, allergic reactions, nausea, constipation, drowsiness.The intensity of their manifestation and frequency decrease upon repeated admission.

There have been reports of anorexia, pain in the parotid gland, urinary retention or incontinence, dry eye, orthostatic hypotension, Raynaud's syndrome, endocrine disorders, cholelithiasis.

Overdose:

Symptoms: headache, sedation, drowsiness, excessive decrease in blood pressure, dizziness, general weakness, bradycardia, dry mouth, vomiting, fatigue, stomach pain. Potential short-term increases in blood pressure, tachycardia, and hyperglycemia are also possible.

Treatment: symptomatic. Gastric lavage (immediately after administration), administration of activated carbon and laxatives, symptomatic therapy.

In the case of a reduction in blood pressure, it is recommended that the volume of circulating blood be restored by introducing a liquid. Bradycardia can be stopped with atropine.

Alpha-adrenoreceptor antagonists can reduce or eliminate transient hypertension in an overdose of moxonidine. As a specific antidote, iodazoxane (an antagonist of imidazolines) is administered.

Interaction:

Moxonidine may be administered with thiazide diuretics and blockers of "slow" calcium channels. With the combined use of moxonidine with these and other antihypertensive agents, the effect of moxonidine increases.

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

Tricyclic antidepressants can reduce the effectiveness of antihypertensive agents of central action.

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

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

The administration of moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter.

When moxonidine is administered together with moclobemide, pharmacodynamic interaction is absent.

Special instructions:

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

It is not recommended to appoint tricyclic antidepressants simultaneously with moxonidine. During treatment, alcohol is excluded.

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

Moxonidine may be administered with thiazide diuretics, ACE inhibitors and blockers of "slow" calcium channels.

Stop taking moxonidine gradually.

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

Data on the adverse effects of moxonidine on the ability to drive a car and to control machines and mechanisms are absent. There are reports of drowsiness and dizziness during treatment with moxonidine. This should be taken into account when performing the above actions (especially at the beginning of treatment).

Form release / dosage:

Tablets, film-coated, 200 mcg.

Packaging:

For 10 or 14 tablets per contour cell packaging made of polyvinylchloride film and foil aluminum.

1, 2, 3 or 4 contour packs of 10 tablets or 1, 2, 3, 4, 5 or 7 contour packs of 14 tablets together with instructions for use in a pack of cardboard.

Storage conditions:

In dry, 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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-009265/08

Date of registration:21.11.2008 / 14.09.2015

Expiration Date:Unlimited

The owner of the registration certificate:FARMZASCHITA NPC, GP FARMZASCHITA NPC, GP Russia

Manufacturer: & nbsp

FARMZASCHITA NPC, FSUE Russia

Information update date: & nbsp12.06.2018

Illustrated instructions

Instructions

Moxonidine (Moxonidine)