Selective imidazoline receptor agonists responsible for the reflex control of the sympathetic nervous system (localized in the ventral-lateral medulla). Slightly communicates with the central alpha2-adrenergic receptors reduces systolic and diastolic blood testosterone propionate buy pressure (BP) and after a single long-term use.
With long-term use reduces hypertrophy of the left ventricular myocardium, eliminates signs of myocardial fibrosis, mikroarteriopatii normalizes capillary blood flow to the myocardium, reduces the total peripheral vascular resistance, pulmonary vascular resistance, while cardiac output and heart rate (HR) did not change significantly. The treatment reduces the activity of norepinephrine and epinephrine, renin, angiotensin II at rest and during exercise, the atrial natriuretic peptide (load), and plasma aldosterone. Decreases Resistance to insulin by 21% compared to placebo in patients with obesity and insulin-resistant patients with moderate hypertension, it stimulates the release of growth hormone. It does not affect glucose metabolism and lipid.
Once inside quickly and almost completely absorbed from the gastrointestinal tract (about 90%). Eating on the amount of absorption is not affected. Maximum plasma concentration (Cmax) is reached after 30-180 minutes and after oral administration is 1-3 ng / ml. The interval between reaching Cmax and pronounced decrease in blood pressure at rest varies on average by 10%, with a load – by 7.7%. Duration -. The bioavailability of more than 12 hours after a single application of 88% inside, indicating no significant effect of “primary” passing through the liver.
It penetrates the blood-brain barrier. Not accumulates long-term use.
The volume of distribution – 1,4-3 l / kg. Communication plasma protein 7%.
Metabolized 10-20% of moxonidine to form 4,5-degidromoksonidina and aminometanamidinovogo derivative.
half-life (T 1/2 ) is 2-3 hours in the first 24 hours the kidneys derived more than 90% (50-75% – unchanged, 20% – in the form of metabolites)., And about 1% – with bile. In testosterone propionate buy a small amount of Moxonidine appears in hemodialysis.
Special patient groups
No significant differences in pharmacokinetics in younger patients and elderly patients were found. Correction dose is not required under normal renal function.
In patients with mild (creatinine clearance (CC) of 30-60 mL / min) and severe (creatinine clearance <30 mL / min) in violation of the plasma equilibrium concentration of kidney function and the final T 1/2about 2 or 3 times respectively higher than in hypertensive patients with normal renal function (creatinine clearance of> 90 ml / min). Therefore, patients with severe renal impairment is contraindicated drug, and with moderate kidney dysfunction drug should be used with caution, the dose should be individualized.
Abnormal liver function
no reliable trials of moxonidine in patients with impaired liver function no. Since moxonidine practically not metabolized in the liver, disturbance of its function does not have a pronounced effect on the pharmacokinetics of the drug.
Indications for use:
- hypersensitivity to moxonidine or any other component of the drug;
- Hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
- The expressed disturbances of heart rhythm (bradycardia (less than 50 beats / min at rest), sick sinus syndrome or sinoatrial block, atrioventricular block grade II and III);
- Chronic heart failure (III-IV functional class NYHA classification);
- severe renal insufficiency (creatinine clearance <30 mL / min creatinine concentration in the serum of> 160 mmol / l) and hemodialysis;
- the simultaneous use of tricyclic antidepressants;
- age of 18 years;
- during breastfeeding.
atrioventricular block of I degree (risk of bradycardia), coronary artery disease (including coronary heart disease, unstable angina, myocardial early period), diseases of the peripheral circulation (including intermittent claudication, Raynaud’s syndrome), epilepsy Parkinson’s disease, depression, glaucoma; moderate renal insufficiency (creatinine clearance 30-60 ml / min, serum creatinine 105-160 mmol / l), liver failure; pregnancy.
Application of pregnancy and during breastfeeding
No significant trials of moxonidine in pregnant women have been conducted. Animal studies have shown embryotoxic effect. Clinical data on the negative impact on the course of pregnancy there. However, you should use the pregnancy only if the potential benefit to the mother outweighs the potential risk to the fetus.
Moxonidine passes into breast milk, women during treatment is recommended to stop breast-feeding or stop the drug.
Dosing and Administration
Moksoniteks appointed inside, regardless of meals, drinking plenty of fluids. the dose regime selected individually.
Unless otherwise Moksoniteks prescriptions should be administered in the following doses: as an initial dose of 0.2 mg of the drug administered in the morning. When insufficient therapeutic effect, the dose 3 weeks later increased to 0.4 mg / day in single or 2 divided doses. The maximum daily dose – 0.6 mg, the maximum single dose of 0.4 mg.
In patients with moderately severe renal function lesions (CC 30 – 60 ml / min), a single dose should not exceed 0.2 mg and the maximum daily dose – 0.4 mg.
According to the World Health Organization (WHO) side effects are classified according to their rate of development as follows: common (> 1/100, <1/10), uncommon (> 1/1000, <1/100), rarely (> 1 / 10,000, <1/1000) and very rare (<1/10000), including isolated reports.
Uncommon: bradycardia, marked reduction in blood pressure (including orthostatic hypotension).
On the part of the central nervous system
often: dizziness (vertigo), headache, somnolence, insomnia
Uncommon: fainting, increased excitability.
On the part of the organ of hearing and labyrinth disorders
From the digestive system
very often: dryness of the oral mucosa;
frequently: diarrhea, nausea, vomiting, dyspepsia.
Skin and subcutaneous tissue disorders
common: pruritus, rash,
rare: angioneurotic edema (angioedema).
On the part of the musculoskeletal and connective tissue disorders
common: pain testosterone propionate buy in the back,
rare: pain in the neck.
General disorders and administration site in
rare: peripheral edema.
Symptoms: headache, marked reduction of blood pressure, bradycardia, palpitations, weakness, drowsiness, dryness of the oral mucosa, rarely – vomiting, and epigastric pain. Potentially possible paradoxical hypertension and hyperglycemia.
Treatment: symptomatic. No specific antidote.
In marked decrease in blood pressure it is recommended to restore the circulating blood volume due to fluid administration.
Alpha-adrenoceptor antagonists can reduce or eliminate transient hypertension moxonidine in overdose.
Interaction with other drugs
The combined use of Moxonidine with other antihypertensives leads to additive effect. 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 sedative effect of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.
Moxonidine is able to moderately improve cognitive impairment in patients receiving lorazepam.
Moxonidine may enhance the sedative effects of benzodiazepines in their simultaneous application.
Moxonidine is obtained by tubular secretion, so it is possible its interaction with other drugs that are excreted by tubular secretion.
During treatment requires regular monitoring of blood pressure, heart rate and ECG. If necessary, cancel both received beta-blockers and drug Moksoniteks first cancel beta-blockers, and only after a few days of preparation Moksoniteks.
There is currently no evidence that discontinuation of Moksoniteks drug leads to increased blood pressure. But we should not abruptly stop the drug use Moksoniteks. Elderly patients may be at increased risk of cardiovascular complications due to the use of antihypertensive drugs, so drug therapy Moksoniteks should start with the lowest dose.
Effects on ability to drive vehicles and mechanisms
Effect of the drug Moksoniteks on ability to drive vehicles or operate machinery has not been studied. However, taking into account the possibility of dizziness, drowsiness, 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 testosterone propionate buy of attention. Anastrozole side effects, anastrozole 1 mg bodybuilding anastrozole for men.