Description
Pharmacological action
Pharmacotherapeutic group: central antihypertensive drug
Code ATC: РЎ02РђРЎ05
Pharmacological action of
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). Reduces the pressor effect of the sympathetic system on peripheral vessels, reduces peripheral vascular resistance, reduces systolic and diastolic pressure both with a single and long-term use, while cardiac output and heart rate (HR) are not significantly changed. With prolonged use, it reduces left ventricular myocardial hypertrophy, levels out signs of myocardial fibrosis, microarteriopathy, normalizes capillary blood supply to the myocardium. During treatment, the activity of norepinephrine and epinephrine, renin decreases, angiotensin II at rest and during exercise, atrial natriuretic peptide (during exercise) and plasma aldosterone.
Has a lower affinity for alpha2-adrenergic receptors, which explains the lower likelihood of developing a sedative effect and dry mouth.
Reduces tissue resistance to insulin. Does not affect glucose and lipid metabolism.
Pharmacokinetics
Absorption after oral administration – 90%. Eating does not affect the amount of absorption. Bioavailability is 88%. Communication with blood plasma proteins – 7.2%. The maximum concentration (Cmax) in plasma is determined 30-180 minutes after oral administration and is 1-3 ng / ml. Distribution volume – 1,4-3 l / kg. The main metabolite is dihydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 10% compared with moxonidine. Penetrates through the blood-brain barrier. It does not cumulate with prolonged use. The elimination half-life of moxonidine and metabolites is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys (78% – unchanged, 13% – in the form of dihydrogenated moxonidine, 8% – in the form of other metabolites). Less than 1% of the dose is excreted through the intestines. Moxonidine is slightly excreted during hemodialysis.
Pharmacokinetics in patients with arterial hypertension
In patients with arterial hypertension, there is no change in the pharmacokinetics of moxonidine.
Pharmacokinetics in elderly patients
Clinically insignificant changes in the pharmacokinetic parameters of moxonidine in elderly patients were noted, probably due to a decrease in the intensity of its metabolism and / or slightly higher bioavailability.
Pharmacokinetics for renal failure
Excretion of moxonidine is significantly correlated with creatinine clearance (CC). In patients with moderate renal failure (CC in the range of 30-60 ml / min), the equilibrium plasma concentrations and final half-life are approximately 2 and 1.5 times higher than in patients with normal renal function (CC more than 90 ml / min ) In patients with severe renal failure (CC less than 30 ml / min), the equilibrium plasma concentrations and the final half-life are 3 times higher than in patients with normal renal function. In patients with end-stage renal failure (CC less than 10 ml / min) on hemodialysis, equilibrium plasma concentrations and the final half-life, respectively, are 6 and 4 times higher than in patients with normal renal function. In patients with impaired renal function, the dosage should be selected individually.
Indications
Arterial hypertension.
Contraindications
– increased sensitivity to the components of the drug
– severe cardiac arrhythmias
– syndrome of weakness of the sinus node
– sinoatrial and atrioventricular block II and III degree srd acute mild acute insufficiency of functional class III and IV according to NYHA classification
— angioedema in the anamnesis of
— severe liver failure (more than 9 points on the Child-Pugh scale)
— chronic renal failure (CC her 30 ml / min, creatinine over 160 μmol / L)
-hemodialysis
-the simultaneous use of tricyclic antidepressants
-up to 18 years of age (efficacy and safety have not been established)
-addose over 75
-period of lactation.
Caution
– Parkinson’s disease (severe form)
– epilepsy
– glaucoma
– depressive
– “intermittent” lameness
– Raynaud’s disease
– atrioventricular lm but less than 60 ml / min)
– severe cerebrovascular disorders
– after myocardial infarction
– severe coronary vascular disease
– severe coronary heart disease or unstable angina (insufficient experience)
– Class II heart failure and Class I NYHA
– impaired liver function
– pregnancy.
Use during pregnancy and lactation
There is no clinical evidence of a negative effect on the course of pregnancy. However, the drug Moxonidine Canon should be prescribed to pregnant women only if the potential benefit to the mother outweighs the potential risk to the fetus.
Moxonidine passes into breast milk, therefore, if taking Moxonidine Canon is necessary during lactation, breast-feeding must be discontinued.
Special instructions
If it is necessary to cancel the simultaneous administration of beta-blockers and the drug Moxonidine Canon, beta-blockers and the drug Moxonidine Canon are canceled only after a few days.
It is not recommended to prescribe tricyclic antidepressants simultaneously with the drug Moxonidine Canon.
During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary.
The drug Moxonidine Canon can be prescribed with thiazide diuretics, inhibitors of angiotensin converting enzyme (ACE) and blockers of “slow” calcium channels.
Stop taking Moxonidine Canon should be gradual.
Effect on the ability to drive vehicles and mechanisms
Considering the potential occurrence of drowsiness and dizziness during treatment with Moxonidine Canon, patients should be careful when engaging in potentially hazardous activities requiring increased attention, such as driving a vehicle or operating machinery requiring increased concentration attention.
Composition
1 tablet, film-coated, 0.2 mg contains:
active substance: moxonidine 0, 2 mg
excipients: hyprolose (hydroxypropyl cellulose) 3 mg, mannitol 68 mg, croscarmellose sodium 3.3 mg, magnesium stearate 0.5 mg, microcrystalline cellulose 25 mg
film composition: Opadry II pink 3 mg, including: polyvinyl alcohol 1.2 mg, macrogol (polyethylene glycol) 0.606 mg, talc 0.444 mg, titanium dioxide 0.7206 mg, sunset yellow dye 0.0003 mg, indigo carmine dye 0.0045 mg, crimson dye [Ponceau 4R] 0.0246 mg
Dosage and administration
Inside, regardless of food intake, with plenty of fluids. In most cases, the initial dose of Moxonidine Canon 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, which should be divided into 2 doses (morning and evening) 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 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, which should be divided into 2 doses (morning and evening) 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 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, which should be divided into 2 doses (morning and evening) 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 normalFor renal function, the dosage recommendations are the same as for adult patients.
In patients with renal failure (creatinine clearance 30-60 ml / min) and patients on hemodialysis, a single dose should not exceed 0.2 mg, the maximum daily dose is 0.4 mg.
Side effects
WHO classification of the incidence of side effects:
very often -> 1/10 prescriptions (> 10%)
often -> 1/100 to <1/10 prescriptions (> 1% and
infrequently> 1/1000 to 0.1% and
rarely – from> 1/10000 to0.01% and
very rare –
Mental disorders
Often: decreased attention concentration Infrequently: depression, anxiety, nervousness
Disorders of the central nervous system
Often: fatigue, drowsiness, headache, dizziness.
Infrequently: paresthesia, insomnia, fainting
Disturbances from gastrointestinal tract
Often: dry oral mucosa, constipation, dyspeptic disorders.
Infrequently: nausea, anorexia.
Very rare: hepatitis, cholestasis.
Disorders of the skin and subcutaneous tissues
Infrequently: skin rash, itching, edema of various localization.
Very rare: angioedema.
Genitourinary disorders
Infrequently: urinary retention or incontinence, impotence, decreased libido.
Disorders of the liver and biliary tract
Rarely: hepatitis, stagnation of bile.
Visual disturbances
Infrequently: dry eyes, causing itching or burning sensation in the eyes.
Hearing impairment and labyrinthine disorders
Infrequently: ringing in the ears.
Vascular dysfunction
Often: symptoms of vasodilation.
Infrequently: lowering blood pressure (BP), orthostatic hypotension, Raynaud’s syndrome, peripheral circulation disorders.
Disorders of the endocrine system
Infrequently: gynecomastia.
Disorders of the musculoskeletal and connective tissue:
Often: back pain. Infrequently: neck pain.
General disorders and disorders at the injection site
Often: asthenia. Infrequently: weakness in the legs, fainting, pain in the parotid glands.
Drug Interactions
Moxonidine Canon can be prescribed with thiazide diuretics and “slow” calcium channel blockers. The combined use of the drug Moxonidine Canon with these and other antihypertensive drugs leads to an additive effect and an increase in the hypotensive effect.
When prescribing the drug Moxonidine Canon with hydrochlorothiazide, glibenclamide (glyburide) or digoxin pharmacokinetic interaction is absent.
Tricyclic antidepressants can reduce the effectiveness of central antihypertensive drugs, therefore, their simultaneous use is not recommended.
Moxonidine Canon moderately enhances cognitive decline in patients taking lorazepam.
Prescription of the drug Moxonidine Canon together with benzodiazepine derivatives may be accompanied by an increase in the sedative effect of the latter.
The drug Moxonidine Canon enhances the inhibitory effect on the central nervous system of anxiolytics, barbiturates and ethanol.
Beta-blockers when combined with moxonidine enhance bradycardia, the severity of the negative foreign and dromotropic effects.
When prescribing the drug Moxonidine Canon together with moclobemide, there is no pharmacodynamic interaction.
Overdose
Symptoms: headache, sedation, drowsiness, marked decrease in blood pressure, dizziness, general weakness, bradycardia, increased fatigue, dry oral mucosa, vomiting, and stomach pain. A paradoxical increase in blood pressure, tachycardia, hyperglycemia are also potentially possible.
Treatment: there is no specific antidote. Gastric lavage (immediately after administration), intake of activated charcoal and laxatives, symptomatic therapy. In the case of a marked decrease in blood pressure, it is recommended to restore the volume of circulating blood due to the introduction of fluid and the introduction of dopamine. Bradycardia can be stopped with atropine.
Alpha-adrenergic antagonists can reduce or eliminate transient arterial hypertension with an overdose of Moxonidine Canon.
Terms and conditions
prescription
The dosage form of
tablet
Canonfarm, Russia
