Description
Release form
Tablets.
Packing
14 pcs.
Pharmacological action
Pharmacodynamics
Selective agonist of imidazoline receptors, responsible for tonic and reflex control of the sympathetic nervous system (localized in the ventero-lateral region of the medulla oblongata). Lowers blood pressure (BP). Slightly associated with central alpha2-adrenoresponsors, due to the interaction with which dry mouth and sedation are mediated.
Reduces tissue resistance to insulin.
Effect on hemodynamics: a decrease in systolic and diastolic blood pressure with a single and prolonged administration of moxonidia 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%. Eating does not affect the amount of absorption. Bioavailability is 88%. Communication with blood plasma proteins – 7%. Cmax in plasma is determined 30-180 minutes after oral administration and is 1-3 pg / ml. Distribution volume – 1,4-3 l / kg. Passes through the blood-brain barrier. It does not cumulate with prolonged use. The elimination half-life is 2-3 hours. The kidneys are excreted by 90% (70% – unchanged, 20% – in the form of metabolites). Significant differences in pharmacokinetics in young and elderly patients were not found.
Contraindications
Hypersensitivity to drug components, sinus node syndrome, sinoatrial and atrioventricular block II and III degree, severe bradycardia (heart rate less than 50 beats / min.), chronic heart failure III and IV class (according to NYHA classification ), history of angioedema, unstable angina, severe liver failure, chronic renal failure (creatinine clearance less than 30 ml / min., creatinine more than 160 Ојmol / l), age under 18 years (efficacy and safety have not been established), pregnancy and lactation, simultaneous administration with tricyclic antidepressants.
Precautions: Parkinson’s disease (severe), epilepsy, glaucoma, depression, intermittent claudication, Raynaud’s disease, grade I atrioventricular block, chronic renal failure (creatinine clearance greater than 30, but less than 60 ml / min.), cerebrovascular disease, after myocardial infarction, chronic heart failure class I and II, severe liver failure – due to a lack of experience in use, hemodialysis.
Special instructions
If you need to cancel the simultaneously taken beta-blockers and moxonidine, first beta-blockers and, only after a few days, moxonidine are canceled. It is not recommended to prescribe tricyclic antidepressants simultaneously with moxonidine. During treatment, the use of alcohol is excluded. During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary.
Moxonidine may be prescribed with thiazide diuretics, ACE inhibitors, and slow calcium channel blockers.
Moxonidine should be discontinued gradually.
Dosage and administration
Inside, regardless of food intake, with plenty of fluids. In most cases, the initial dose of moxonidine is 0.2 mg per day, in one dose, preferably in the morning. If the therapeutic effect is insufficient, the dose can be increased after 3 weeks of therapy to 0.4 mg per day for 2 doses or once. 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, the dosage recommendations are the same as for adult patients.
In patients with renal failure (clearance of cretinin 30-60 ml per minute) and patients undergoing hemodialysis, a single dose should not exceed 0.2 mg, the maximum daily dose of 0.4 mg.
Side effects of
Especially at the beginning of therapy, the most common adverse reactions were: dry mouth, headache, dizziness, asthenia, peripheral edema, allergic reactions, nausea, constipation, drowsiness. The intensity of their manifestation and frequency decrease with repeated use. Reported cases of anorexia, pain in the parotid gland, urinary retention or incontinence, dry eyes, orthostatic hypotension, Raynaud’s syndrome, endocrine disorders, cholelithiasis.
Drug Interactions
Moxonidine may be prescribed with thiazide diuretics and slow calcium channel blockers. With the combined use of moxonidine with these and other antihypertensive drugs, a mutual increase in the effect of moxonidine occurs.
When prescribing moxonidine with hydrochlorothiazide, glibenclamide (glyburide) or digoxin, there is no pharmacokinetic interaction.
Tricyclic antidepressants may decrease the effectiveness of centrally acting antihypertensive drugs.
Beta-blockers increase bradycardia, the severity of the negative foreign and dromotropic effects of moxonidine.
Moxinidine moderately enhances cognitive decline 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 prescribing moxonidine together with moclobemide, there is no pharmacodynamic interaction.
Overdose
Symptoms: headache, sedation, drowsiness, overly pronounced decrease in blood pressure, dizziness, general weakness, bradycardia, dry mouth, vomiting, fatigue, stomach pain. A short-term increase in blood pressure, tachycardia, hyperglycemia are also potentially possible.
Treatment: symptomAtic. Gastric lavage (immediately after administration), the introduction of activated charcoal and laxatives, symptomatic therapy. In the case of lowering blood pressure, it is recommended to restore the volume of circulating blood due to the introduction of fluid. Bradycardia can be stopped with atropine. Alpha-adrenergic antagonists can reduce or eliminate transient arterial hypertension in case of an overdose of moxonidine. Idazoxane (an imidazoline antagonist) is administered as a specific antidote.
Storage Conditions
In a dry, dark place.
Expiration
2 years.
Conditions of dispatch from
pharmacies Prescription
lekarstvennaja form
tablets
Northern Star, Russia
