Selective imidazoline receptor agonists responsible for the tonic and reflex control of the sympathetic nervous system (localized to Venter-lateral medulla). It lowers blood pressure (BP). Slightly communicates with the central alpha2-adrenoretssptorami, due to the interaction which are mediated by dry mouth and sedation.
Reduces the resistance of tissues to insulin.
The impact on hemodynamics: reduction testosterone propionate dosage in systolic and diastolic blood pressure with a single and long-term treatment moksonidiia associated with a reduced pressor effect of the sympathetic system peripheral vessels, a decrease in peripheral vascular resistance, while cardiac output and heart rate (HR) did not change significantly.
Absorption after oral administration – 90%. Eating on the amount of absorption is not affected. Bioavailability – 88%. Communication with plasma proteins – 7%. Cmax in the plasma is determined by 30-180 min after oral administration is 1-3 and pg / ml. The volume of distribution – 1,4-3 l / kg. It passes through the blood-brain barrier. Do not cumulated with prolonged use. The half -. 2-3 hours Kidneys output by 90% (70% – unchanged, 20% – in the form of metabolites). No significant differences in the pharmacokinetics in young and elderly patients have not been found.
: Hypersensitivity to the drug, sick sinus syndrome, sinoatrial and atrioventricular block II and III degree, bradycardia (heart rate less than 50 bpm. / Min.), Chronic heart failure class III and IV (in NYHA classification), angioedema swelling in history, unstable angina, severe liver failure, chronic renal insufficiency (creatinine clearance less than 30 ml / min., creatinine 160 umol / l), age 18 years (effectiveness and safety have not been established), pregnancy and lactation period, simultaneous receiving tricyclic antidepressants.
Precautions: Parkinson’s disease (severe), epilepsy, glaucoma, depression, “intermittent” claudication, Raynaud’s disease, atrioventricular block I degree, chronic renal insufficiency (creatinine clearance of more than 30 but less than 60 ml / min.), Cerebrovascular disease, after myocardial infarction, chronic heart failure class I and II expressed liver failure – due to lack of experience in the application, hemodialysis.
Dosing and Administration
Inside, regardless of meals, drinking plenty of fluids. In most cases, the initial dose of 0.2 mg moxonidine per day, in one portion, preferably in the morning. When insufficient therapeutic effect dose can be increased after 3 weeks of treatment, and 0.4 mg per day for single or 2 divided doses. The maximum daily dose, which should be divided into 2 doses (morning and evening), is 0.6 mg. The maximum single dose is 0.4 mg.
In elderly patients with normal renal function, recommended dosages are the same as for adult patients.
In patients with renal failure (clearance Kretinina 30-60 ml / min.), And patients undergoing testosterone propionate dosage hemodialysis na , the single dose should not exceed 0.2 mg, the maximum daily dose of 0.4 mg.
, especially in the beginning of the therapy the most common adverse reactions were dry mouth, headache, dizziness, asthenia, peripheral edema, allergic reactions, nausea, constipation, drowsiness. The intensity and frequency of their symptoms decrease with readmission. Reported cases of anorexia, pain in the parotid glands, delayed or incontinence, dryness, orthostatic hypotension, Raynaud’s syndrome, endocrine disorders, gallstones.
Overdose Symptoms: headache, sedation, somnolence, excessively pronounced decrease in blood pressure, dizziness, weakness, bradycardia, dry mouth, vomiting, fatigue, pain in the stomach. Potentially also possible transient increase in blood pressure, tachycardia, hyperglycemia. Treatment: symptomatic. Gastric lavage (immediately after administration), administration of activated charcoal and laxatives, symptomatic therapy. In case of reduction of blood pressure is recommended to restore the circulating blood volume due to fluid administration. Bradycardia can be stopped by atropine. Alpha-adrenoceptor antagonists can reduce or eliminate transient hypertension moxonidine in overdose. In idazoxan (imidazoline antagonist) is administered as a specific antidote.
Interaction with other drugs
moxonidine may be administered with thiazide diuretics and blockers “slow” calcium channels. In a joint application of moxonidine with these and other antihypertensives mutual strengthening of moxonidine action.
In the appointment of moxonidine with hydrochlorothiazide, glibenclamide (glyburide), or digoxin farmakokinetichskoe no interaction.
Tricyclic antidepressants may decrease the effectiveness of antihypertensive drugs central action.
Beta-blockers increase the bradycardia, the severity of the negative ino and dromotropic action of moxonidine.
Moksinidin moderately enhances cognitive decline in patients receiving lorazepam.
appointment moxonidine together with benzodiazepines may be accompanied by increased sedative effect of the latter.
in the appointment of moxonidine together with moclobemide pharmacodynamic interaction is absent.
If necessary, cancel both received beta-blockers and moxonidine, first cancel the beta-blockers, and only a few days, moxonidine. Not recommended to prescribe tricyclic antidepressants concurrently with moxonidine. During treatment excludes alcohol. During treatment requires regular monitoring of blood pressure, heart rate and ECG.
Moxonidine can be administered with thiazide diuretics, ACE inhibitors, and blockers “slow” calcium testosterone propionate dosage channels.
Stop receiving moxonidine should be gradual.
Effects on ability to drive the car and to the management of machines and mechanisms
Data on the adverse effect of moxonidine on the ability to drive a car and to the engines and there are no management mechanisms. There are reports of drowsiness and dizziness during treatment with moxonidine. This should be considered in carrying out the above steps (especially at the beginning of treatment).