Description
Release form
Tablets
Packing
30 pcs.
Pharmacological action
Pharmacodynamics
Moxonidine is a hypotensive drug with a central mechanism of action. In the brain stem structures (the rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazoline-sensitive receptors involved in the tonic and reflex regulation of the sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure.
Moxonidine differs from other adrenergic antihypertensive drugs in lower affinity for 1-adrenergic receptors, which explains the lower likelihood of developing a sedative effect and dryness of the oral mucosa.
Taking moxonidine leads to a decrease in systemic vascular resistance and blood pressure.
Moxonidine improves the insulin sensitivity index in patients with obesity, insulin resistance and moderate arterial hypertension.
Pharmacokinetics
Absorption. After oral administration, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. Absolute bioavailability is approximately 88%. Tmax – about 1 hour. Eating does not affect the pharmacokinetics of the drug.
distribution. Communication with plasma proteins is 7.2%.
Metabolism. The main metabolite is dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 10% compared with moxonidine.
Withdrawal. T1 / 2 of moxonidine and metabolite are 2.5 and 5 hours, respectively. Within 24 hours, over 90% of moxonidine is excreted by the kidneys (about 78% unchanged and 13% in the form of dehydromoxonidine, other metabolites in the urine do not exceed 8% of the dose). Less than 1% of the dose is excreted through the intestines.
Special patient groups
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 a slightly higher bioavailability.
Children. Moxonidine is not recommended for use in patients under 18 years of age, and therefore pharmacokinetic studies have not been conducted in this group.
Impaired renal function. Excretion of moxonidine is largely correlated with creatinine clearance. In patients with moderate renal failure (creatinine Cl 30-60 ml / min), plasma Css and final T1 / 2 are approximately 2 and 1.5 times higher than in patients with normal renal function (creatinine Cl more than 90 ml / min ) In patients with severe renal failure (creatinine Cl less than 30 ml / min), plasma Css and final T1 / 2 are 3 times higher than in patients with normal renal function. The administration of multiple doses of moxonidine leads to predictable cumulation in the body of patients with moderate and severe renal failure. In patients with terminal renal failure (creatinine Cl less than 10 ml / min) undergoing hemodialysis, plasma Css and final T1 / 2 are respectively 6 and 4 times higher than in patients with normal renal function.
In all groups, the maximum concentration of moxonidine in blood plasma is 1.5 2 times higher. In patients with impaired renal function, the dosage should be selected individually. Moxonidine is slightly excreted during hemodialysis.
Contraindications
severe cardiac arrhythmias
sinus node syndrome
AV block II and III degree
severe bradycardia (heart rate less than 50 beats / min)
acute and chronic heart failure (III-IV functional srdk class NYHA with tricyclic antidepressants
severe renal failure (CC less than 30 ml / min), including patients hemodialysis
age over 75 years old
age 18 years (the efficacy and safety of moxonidine have not been established)
breastfeeding period
lactose intolerance, lactase deficiency, glucose-galactose malabsorption
hypersensitivity to the active substance, other components.
Caution
impaired renal function (CC more than 30 ml / min)
severe liver failure (more than 9 points in the Child-Pugh classification)
AV block I degree
severe coronary vascular disease
severe coronary artery disease or unstable angina (experience is insufficient)
chronic heart failure.
Use during pregnancy and lactation
There are no clinical data on the treatment of pregnant women with Moxarel ®.
Prescribe Moxarel ® to pregnant women with caution only after a careful assessment of the risk-benefit ratio when the benefit to the mother outweighs the potential risk to the fetus.
Moxonidine passes into breast milk. Lactating women during the treatment period are advised to stop breastfeeding or to discontinue the drug.
Special instructions
There is currently no evidence that discontinuation of Moxarel ® leads to an increase in blood pressure. However, it is not recommended to stop taking Moxarel ® sharply, instead, the dose should be gradually reduced over a period of 2 weeks.
If necessary, the cancellation of simultaneously taken -adrenergic blockers and the drug Moxarel ® is first canceled -adrenergic blockers and only after a few days, moxonidine.
During treatment, regular monitoring of blood pressure, heart rate and ECG recording is necessary. Moxarel ® should be discontinued gradually.
Alcohol should be excluded during treatment with Moxarel ®.
Influence on the ability to drive vehicles and work with mechanisms. The effect of the drug Moxarel ® on the ability to drive vehicles or control machinery has not been studied. However, taking into account the possible occurrence of dizziness and drowsiness, patients should be careful when engaging in potentially hazardous activities, requiring increased attention, such as driving vehicles or operating machinery.
Composition
Active ingredient:
moxonidine 0.4 mg
Excipients:
lactose monohydrate
MCC
silicon dioxide colloidal
povidone K30
sodium croscarella.
Dosage and administration
Inside, regardless of food intake.
In most cases, the initial dose of Moxarel ® is 0.2 mg / day.
The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 doses, is 0.6 mg.
The initial dose for patients with moderate or severe renal failure, as well as for patients on hemodialysis, is 0.2 mg / day. If necessary and with good tolerance, the daily dose can be increased to 0.4 mg.
Side effects
From the central nervous system: often – headache, dizziness (vertigo), drowsiness infrequently – fainting.
From the CCC side: infrequently – marked decrease in blood pressure, orthostatic hypotension, bradycardia.
From the gastrointestinal tract: very often – dryness of the oral mucosa often – nausea, diarrhea, vomiting, dyspepsia.
From the skin and subcutaneous tissues: often – skin rash, itching infrequently – angioedema.
Mental disorders: often – insomnia infrequently – nervousness.
On the part of the hearing organ and labyrinth disorders: infrequently – ringing in the ears.
From the side of musculoskeletal and connective tissue: often – back pain infrequently – pain in the neck.
General disorders and disorders at the injection site: often – asthenia infrequently – peripheral edema.
Drug Interactions
The combined use of moxonidine with other antihypertensive drugs leads to an additive effect.
Tricyclic antidepressants can reduce the effectiveness of central antihypertensive drugs, therefore, it is not recommended to take them together with moxonidine.
Moxonidine may enhance the effects of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.
Moxonidine is able to moderately improve impaired cognitive function in patients receiving lorazepam.
The administration of moxonidine together with benzodiazepine derivatives may be accompanied by an increase in the sedative effect of the latter.
The simultaneous use of moxonidine with -adrenoblockers leads to increased bradycardia, the severity of foreign and dromotropic effects.
When prescribing moxonidine together with moclobemide, there is no pharmacodynamic interaction. Moxonidine is secreted by tubular secretion, therefore, its interaction with other drugs released by tubular secretion is not ruled out.
Overdose
Symptoms:
headache, sedation, drowsiness, severe BP, dizziness, fatigue, asthenia, bradycardia, dry mouth, vomiting and epigastric pain, epigastric pain, epigastric pain Short-term increases in blood pressure, tachycardia, and hyperglycemia are also possible.
Treatment:
no specific antidote for the drug exists. In case of marked decrease in AD, the introduction of a fluid for the recovery of BCC and dopamine is recommended. Bradycardia can be stopped with atropine. -Adrenoreceptor antagonists may reduce or eliminate paradoxical hypertensive effects of moxonidine overdose. In severe cases of overdose, it is recommended to carefully monitor the disturbance of consciousness and to prevent respiratory depression. Moxonidine is slightly excreted during hemodialysis.
Storage Conditions
In a dark place at a temperature not exceeding 25 ° C.
shelf life
3 years
Deystvuyushtee substance
Moxonidine
Terms and conditions
prescription
dosage form
tablets
Possible Product Names
Moxarel Tablet Coated. 0.4 mg, 30 pcs.
