The stem structures of the brain (rostral layer of the lateral ventricles) moxonidine selectively stimulate imidazoline-sensitive receptors are involved in the tonic and reflex regulation of the sympathetic nervous system. Imidazoline receptor what is testosterone propionate stimulation reduces peripheral sympathetic activity and blood pressure (BP).
Moxonidine differs from other sympatholytic antihypertensives lower affinity for the α 1 adrenoceptor which explains the lower probability of sedation and dryness of the oral mucosa.
Receiving Moxonidine reduces systemic vascular resistance and blood pressure. Moxonidine improves insulin sensitivity index in patients with obesity, insulin resistance and moderate hypertension.
Pharmacokinetics Absorption After oral administration moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. The absolute bioavailability of approximately 88%. Time to maximum concentration – about 1 hour. Food intake has no effect on the pharmacokinetics of the drug. Distribution Relationship to plasma proteins is 7.2%. Metabolism The major metabolite – dehydrogenated moxonidine. Pharmacodynamic Activity dehydrogenated moxonidine – about 10% as compared with moxonidine. Elimination half-life (T ½ ) of moxonidine and metabolite of 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine excreted by the kidneys (about 78% unchanged and 13% as degidromoksonidina and other metabolites in the urine does not exceed 8% of the dose). Less than 1% of the dose is excreted through the intestines. Pharmacokinetics in elderly patients with clinically insignificant changes in pharmacokinetic parameters what is testosterone propionate in elderly patients, probably due to a decrease in the intensity of its metabolism and / or somewhat higher bioavailability. Pharmacokinetics in children Moxonidine is not recommended for use in patients under the age of 18, in connection with which this group pharmacokinetic studies have not been conducted. Pharmacokinetics in renal impairment Excretion moxonidine is largely correlated with creatinine clearance (CC). In patients with moderate renal impairment (creatinine clearance in the range of 30-60 ml / min), the equilibrium concentration in the blood plasma and the final T ½ of approximately 2 and 1.5 times higher than in patients with normal renal function (creatinine clearance greater than 90 mL / min ). In patients with severe renal failure (creatinine clearance less than 30 mL / min), the equilibrium concentration in the blood plasma and the final T ½ to 3 times higher than in patients with normal renal function. Assigning multiple doses of moxonidine leads to a predictable accumulation in the body of patients with moderate to severe renal insufficiency. Patients with end-stage renal failure (creatinine clearance less than 10 mL / min) on hemodialysis, the equilibrium concentration in plasma and the final T ½ , respectively, 6 and 4 times greater than in patients with normal renal function. In all groups, the maximum concentration of moxonidine plasma above 1.5-2. In patients with renal function impairment, the dosage should be individualized. Moxonidine slightly displayed during hemodialysis.
- Hypersensitivity to the active substance, other components of the drug;
- The expressed disturbances of heart rhythm;
- sick sinus syndrome;
- atrioventricular block II and III degree;
- bradycardia (heart rate (HR) of less than 50 beats / min);
- acute and chronic heart failure (III-IV functional class NYHA classification);
- the simultaneous use of tricyclic antidepressants (see “Interaction with other medicinal products” section.)
- severe renal insufficiency (creatinine clearance less than 30 ml / min), including patients on hemodialysis;
- age over 75 years;
- age of 18 years (moxonidine efficacy and safety have not been established);
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
- renal dysfunction (creatinine clearance 30 mL / min);
- severe hepatic insufficiency (more than 9 points on the Child-Pugh classification);
- atrioventricular block of I degree;
- severe coronary artery disease;
- severe coronary heart disease or unstable angina (application experience is insufficient);
- chronic heart failure.
Use during pregnancy and during breastfeeding
Clinical data on the treatment of pregnant drug Moksarel® absent. Assign Moksarel “pregnant with caution only after a careful assessment of risks and benefits when benefit to the mother outweighs the potential risk to the fetus.
Moxonidine passes into breast milk. Breastfeeding women during treatment is recommended to stop breast-feeding or stop the drug.
Dosing and Administration
Inside, regardless of meals.
In most cases, the initial is 0.2 mg per 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 starting dose for patients with moderate or severe renal insufficiency, and also for patients on hemodialysis was 0.2 mg / day. If necessary and if tolerated daily dose may be increased to 0.4 mg.
The incidence of adverse events listed below was determined according to the following: very often – at least 10%; often – at least 1% but less than 10%; infrequently – at least 0.1% but less than 1%; rare – less than 0.01% but less than 0.1%; very rarely – less than 0.01% (including isolated cases). On the part of the central nervous system : often – headache, dizziness (vertigo), somnolence uncommon – a faint. From the circulatory system: rare – marked reduction in blood pressure, orthostatic hypotension, bradycardia. On the part of the gastrointestinal tract: often – dryness of the oral mucosa, often – nausea, diarrhea, vomiting, dyspepsia. From the side of the track and subcutaneous tissue disorders: often – skin rash, itching, rarely – angioedema. Violations psyche : often – insomnia; rarely – nervousness. On the part of the ear and labyrinth disorders : rarely – ringing in the ears. On the part of the musculoskeletal and connective tissue disorders : often – back pain, rarely – pain in the neck. General disorders and at the injection site : often – fatigue, rarely – peripheral edema.
headache, sedation, drowsiness, marked reduction in blood pressure, dizziness, fatigue, asthenia, bradycardia, dry oral mucosa, vomiting and epigastric pain, respiratory depression, impaired consciousness.Potentially also possible transient increase in blood pressure, tachycardia, hyperglycemia. Treatment No specific antidote exists. In the case of significant decrease of blood pressure is recommended fluid administration to restore the circulating blood volume and dopamine. Bradycardia can be stopped by atropine. Alpha-adrenoceptor antagonists can reduce or eliminate the paradoxical hypertensive effects of an overdose of moxonidine. In severe cases of overdose is recommended what is testosterone propionate to carefully monitor the human consciousness and to prevent respiratory depression. Moxonidine slightly displayed during hemodialysis.
Interaction with other drugs combined use of Moxonidine with other antihypertensive agents results in additive effects. Tricyclic antidepressants may decrease the effectiveness of antihypertensive drugs central action, and therefore it is not recommended taking them together with moxonidine. Moxonidine may enhance the effects of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.moxonidine is able to moderately improve cognitive impairment in patients receiving lorazepam. Appointment moxonidine together with benzodiazepines may be accompanied by increased sedative effect of the latter. The simultaneous use of moxonidine with beta-blockers leads to increased bradycardia, severity and for- dromotropic action. In appointing Moxonidine together with moclobemide pharmacodynamic interaction is absent. Moxonidine is allocated by tubular secretion, so it is possible its interaction with other drugs, recovered by tubular secretion
There is currently no evidence that discontinuation of the drug Moksarel ® leads to increased blood pressure. However, it is not recommended to stop taking the drug Moksarel ® sharply, instead, gradually reduce the dose of the drug for two weeks.
If you want to cancel both received beta-blockers and drug Moksarel ® first cancel beta-blockers, and only after moxonidine few days.
During treatment, requires regular monitoring of blood pressure, heart rate and recording electrocardiography (ECG). Stop taking the drug should be gradually.
During treatment Moksarel should exclude alcohol.
Effects on ability to drive vehicles and mechanisms
Effect of the on the ability to drive vehicles or operate machinery has not been studied. However, taking into account the possible occurrence of dizziness and somnolence, patients should be careful during the occupation of potentially hazardous activities that require attention, such as driving a vehicle or management technique, which requires high concentration of attention. webutations review oxydine metabolics buy halotestin online