Moxonidine is antihypertensive agent with a central mechanism of action. 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. Stimulation of the imidazoline receptors reduces peripheral sympathetic activity and blood pressure.
Moxonidine differs from other sympatholytic antihypertensives lower affinity for the a2-adrenergic receptors, which explains the lower probability of sedation and dry mouth.
Moxonidine leads to a reduction in systemic vascular resistance and blood pressure. The hypotensive effect of moxonidine confirmed in double-blind, placebo-controlled, randomized studies.
Moxonidine 21% improves masteron side effects insulin sensitivity index (compared to placebo) in obese patients, insulinrezistentnostnostyu to moderate hypertension.
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.
Relationship to plasma proteins is 7.2%.
The major metabolite – dehydrogenated moxonidine. Pharmacodynamic Activity dehydrogenated moxonidine – about 10% as compared with moxonidine.
half-life (T1 / 2) 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 degidriromoksonidina and other metabolites in the urine does not exceed 8% of the dose). Less than 1% of the dose is excreted through the intestines.
The pharmacokinetics in patients with hypertension:
Compared to healthy volunteers in hypertensive patients is not observed changes in the pharmacokinetics of moxonidine.
Pharmacokinetics in the elderly
is noted clinically insignificant changes in pharmacokinetic parameters Moxonidine in elderly patients, probably due to a decrease in the intensity of its metabolism masteron side effects somewhat higher bioavailability.
Pharmacokinetics in children
Moxonidine is not recommended for use in patients under the age of 18 years, in connection with which this group pharmacokinetic studies have not been conducted.
Pharmacokinetics in renal impairment
Excretion Moxonidine is largely correlated with creatinine clearance . Patients with moderate renal impairment (creatinine clearance in the range of 30-60 ml / min) Equilibrium concentration in plasma and the of approximately 2 and 1.5 times higher than those with normal renal function (creatinine clearance greater than 90 mL / min.). In patients with severe renal impairment (creatinine clearance less than 30 mL / min.), The equilibrium concentration in plasma and the final T1 / 2 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 , respectively 4 and 6 times higher than in patients with normal renal function. In all groups, the maximum concentrations of moxonidine in plasma over 1.5 – 2 times. In patients with impaired renal function the dosage should be individualized. Moxonidine slightly displayed during hemodialysis.
: Hypersensitivity to the active substance masteron side effects and other ingredients; sick sinus syndrome, bradycardia (heart rate , rest less than 50 u. / min).
Hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Due to the lack of data on safety and efficacy have not recommended the appointment of moxonidine to persons under 18 years of age.
Precautions: severe and terminal renal failure; patients on hemodialysis; due to lack of application experience – severe hepatic insufficiency .
Pregnancy and lactation
Clinical data on the treatment of pregnant women with moxonidine absent. In animal studies the direct or indirect negative impact on pregnancy, embryonic / fetal development, birth or postnatal development has not been established.
Assign masteron side effects 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. Nursing 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 dose masteron side effects 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.